home Analyzes What penicillin antibiotics? List and brief instructions for antibiotics related to penicillin drugs. Properties of antibiotics of the penicillin group

What penicillin antibiotics? List and brief instructions for antibiotics related to penicillin drugs. Properties of antibiotics of the penicillin group

- penicillins, cephalosporins, carbopenems - form the basis of modern chemotherapy. They have a bactericidal effect due to the destruction of peptidoglycan, a mucopeptide of the bacterial cell wall. The drugs have synergism against gram-negative flora with aminoglycosides and fluoroquinolones, but they cannot be mixed in the same syringe or infusion system due to physicochemical incompatibility. To overcome resistance, they are combined with beta-lactamase inhibitors.

Side effects: allergic rashes, eosinophilia, less often other immediate hypersensitivity reactions (angioedema, urticaria), anaphylactic shock in children is extremely rare, as are neutro- and thrombocytopenia, hemolytic anemia, interstitial nephritis, phlebitis at the injection site. Ampicillin and cephalosporins rarely cause. Only benzylpenicillin sodium salt is administered endolumbarally - extremely carefully for health reasons. When prescribing to patients with renal failure, the content of potassium and sodium in the preparations is taken into account.

Contraindications. Persons with a history of anaphylaxis, urticaria, or severe rash immediately after penicillin administration are at risk of developing an immediate reaction to other drugs in this group and should not be administered them. Patients allergic to a penicillin drug will react allergically to all penicillins, but only 10% of them will react allergically to cephalosporins and other beta-lactams. Individuals with a history of minimal rash (not a confluent rash on a small surface area of the body) or a rash that occurred 72 hours or more after penicillin administration may not be allergic to penicillins; they should not refuse its use for serious infections, providing everything for the treatment of anaphylaxis.

Penicillins

Penicillins penetrate well into body tissues and fluids, incl. in the CSF during inflammation of the meninges and the administration of high doses. They are excreted mainly in the urine. Carbenicillin has lost its importance; ticarcillin and ureidopenicillins are used only in combination with lactamase inhibitors.

Drug interactions. They increase the risk of bleeding when used with direct and indirect anticoagulants, NSAIDs, and salicylates. When taken together with potassium supplements, potassium-sparing diuretics, ACE inhibitors, hyperkalemia is possible. Increases the toxicity of methotrexate.

Natural penicillins

Benzylpenicillin(in Russia more often called penicillin) is a low-toxic drug that creates high concentrations (at a dose of 50 mg/kg IM - 15-25 mcg/ml in the blood and 60-70% of it in the tissues). Pneumococci in Russia retain 90-95% sensitivity to penicillin; sensitivity is lower in children in kindergartens and, especially, in boarding schools. Benzylpenicillin derivatives have the same antibacterial spectrum; Due to its lower effectiveness, phenoxymethylpenicillin should not be used to treat serious infections. In children with otitis and uncomplicated otitis, phenoxymethylpenicillin-benzathine (Ospen-syrup) has proven its worth; its concentration in the blood at a dose of 50 mg/kg is 4-6 mcg/ml.

Benzathine benzylpenicillin provides a prolonged effect when administered intramuscularly; it is used for infections caused by highly sensitive pathogens (GABHS, spirochete pallidum) to maintain a low therapeutic concentration for a long time.

Side effects. Jarisch-Herzheimer reaction (treatment of syphilis and other infections caused by spirochetes) - associated with the release of endotoxins.

Benzylpenicillin

Indications. Acute otitis media, pneumococcal infection (, meningitis), streptococcal infections (acute, erysipelas, scarlet fever, endocarditis, necrotizing fasciitis), meningococcal infection, tick-borne borreliosis, leptospirosis, anthrax; actinomycosis, gas gangrene, syphilis.

Dosing: IM or IV slowly or by infusion: children from 1 month to 12 years, 100-200 thousand units/kg per day in 2-3 doses, for severe diseases - up to 500,000 units/kg/day vital indications (see below). Syphilis - see Section 6.3.

Side effects. At doses >20 million units/day - DNS disorders, increased creatinine levels.

Release form: powder for the preparation of solution for intravenous and intramuscular injections of 250,000, 500,000 and 1 million units (1 mg = 1610 units) (Benzylpenicillin - Russia)

Phenoxymethylpenicillin - Penicillin V (phenoxymethylpenicillin)

Indications: Streptococcal pharyngitis, secondary prevention of rheumatism; prevention of relapses of pneumococcal meningitis after traumatic brain injury, pneumococcal infection in children after splenectomy or with hypogammaglobulinemia; for the treatment of acute otitis media; erysipelas.

Dosage: orally, children over 12 years old - 500 mg every 6 hours, children under 1 year old - 50 mg/kg/day, from 1 to 6 years old - 30 mg/kg/day, 6-12 years old - 20-30 mg/day kg/day in 3-4 doses. Secondary prevention of rheumatism: orally, children - 500 mg 1-2 times a day.

Side effects: See above, also nausea and diarrhea.

Release form: Phenoxymethylpenicillin-benzathine syrup 750 mg/5 ml (Ospen-750 - Sandoz, Austria), tablet. 100 mg, 250 mg, dragee 100,000 units, powder for suspension: 250 mg/5 ml, 60 mg/ml (Phenoxymethylpenicillin - Russia).

Benzathine benzylpenicillin

Indications: acute streptococcal group A, erysipelas, prevention of rheumatism, treatment of diphtheria carriers; syphilis.

Contraindications: neurosyphilis. Do not administer intravenously or intra-arterially.

Carefully: renal failure.

Dosing. In the treatment of acute tonsillitis, scarlet fever, erysipelas, wound infections in the acute phase, therapy begins with penicillin, benzathine continues with benzyl-penicillin: 1-2 injections of 1.2 million units once a week. For rheumatism, 2.4 million units intramuscularly every 15 days. For the prevention of scarlet fever in children under 7 years of age (or weighing up to 25 kg) 600,000 units, over 7 years of age (or weighing more than 25 kg) - 1,200,000 units. For the treatment of tonsillitis and the treatment of diphtheria carriers, these doses are once, for the prevention of rheumatism - same doses every 2 weeks, Syphilis: see Section 6.3.

Side effects: Rarely embolism; pain and inflammation at the injection site.

Release form: Por. d/prig. solution for intramuscular injection, benzathine benzylpenicillin in bottles: 300, 600 thousand, 1.2 and 2.4 million units. (Bicillin-1 (Russia); 1.2 and 2.4 million units (Retarpen, Extencillin - Sandoz, Austria).

Antistaphylococcal penicillins

Oxacillin

Oxacillin is used to treat infections caused by staphylococci, incl. producing beta-lactamase, but not MRSA. The rest of the spectrum of action is the same as that of natural penicillins, but the sensitivity of pneumococci and streptococci to it is lower than to penicillin. Bioavailability when taken orally is low.

Indications: Infectious diseases caused by staphylococci, incl. producing beta-lactamase: acute sinusitis, septicemia, abscesses, phlegmon, cholecystitis, infected burns, bacterial endocarditis.

Carefully: bronchial asthma, chronic renal failure; liver failure.

Dosage: IM or IV for newborns - 20-40 mg/kg/day for 2 injections, for children 100-150 (up to 200) mg/kg/day - max, up to 12 g/day for 2-4 injections.

Side effects. Rarely - liver dysfunction, jaundice at high doses (in adults >12 g/day). Fever, nausea, vomiting, eosinophilia, anemia, neutropenia, transient hematuria in children.

Release form: Lyophilisate d/prig. solution for intravenous and intramuscular administration 250 mg, 500 mg (Oxacillin - Russia).

Aminopenicillins

Ampicillin and amoxicillin, unlike natural pencillins, act on some gram-negative microorganisms, in particular, H. influenzae, which in Russia remains sensitive to aminopenicillins due to the low frequency of production of beta-lactamases. Ampicillin acts on E. fecalis, which in Russia is 90% sensitive to it. Activity against Salmonella and Shigella varies geographically. The value of empirical therapy with IMG1 is limited due to the high frequency of secondary resistance of E. coli. The drugs are inactivated by beta-lactamase produced by S. aureus, M. catarrhalis, N. gonorrhoeae, and enterobacteria.

Amoxicillin acts better than ampicillin and penicillin on; when taken orally, it has 2-2.5 times greater bioavailability than ampicillin (especially in the form of Solutab dispersible tablets), gives higher concentrations in plasma and tissues and is less likely to cause diarrhea. Ampicillin is used only parenterally.

Contraindications. Leukemoid reactions of the lymphatic type, lymphocytic leukemia.

Carefully. Acute (possible mononucleosis), erythematous rashes characteristic of infectious mononucleosis, breastfeeding. Increased diaper rash - does not prevent repeated use.

Side effects. A feature of aminopenicillins is the development (about 7% of courses) of a maculopapular (“ampicillin”) rash (especially against the background of infection with the Ensteia-Barra virus - most recognize its non-allergic nature) on days 3-5 of treatment; the rash disappears without stopping the drug. Rarely vomiting, diarrhea, very rarely -.

Interaction. Reduce the contraceptive effect of estrogen-containing drugs. Allopurinol increases the risk of ampicillin rash.

Ampicillin

Indications. Acute otitis media, acute sinusitis, community-acquired, UTI, IZhP, shigellosis, salmonellosis, meningitis, bacterial endocarditis, septic infection of newborns (in combination with gentamicin), erysipelas.

Dosing: IM, slow IV or IV infusion. 100-200 mg/kg/day, meningitis, endocarditis - 200-300 mg/kg/day. (up to 8-12 g/day).

Release form: Powder for the preparation of solution for injection 250 mg, 500 mg, 1 and 2 g (Ampicillin - Russia).

Amoxicillin

Indications: upper respiratory tract infections (sinusitis, acute otitis media),: UTI. systemic tick-borne borreliosis (Lyme disease); prevention of endocarditis: eradication of H. pylori, dysentery, salmonellosis, salmonellosis carriage in the presence of sensitivity.

Dosage: orally, children 45 mg/kg/day, dose if there is a possibility of pneumococcal resistance (antibiotic treatment, visiting a child care facility) - 80-100 mg/kg/day. The course of treatment is 5-12 days.

Release form: dispersible tablets. 0.125, 025, 0.5 and 1 g. caps., tab. 0.25 and 0.5 g; table, p/obol. 0.5 and 1.0 g; por. and gran, d/prig. susp. 125 mg/5 ml and 250 mg/5 ml: por. d/prig. drops, 0.1 g/ml (Flemoxin Solutab - Astellas Pharma Europe B.B.. Netherlands. Amoxicillin - Russia Ospamox - Sanoz, Austria. Hiconcil - KRKA, Slovenia).

Inhibitor-protected penicillins

They are a combination of a penicillin drug and a beta-lactamase inhibitor. The most widely used is amoxicillin/clavulanate, active against resistant H. influenzae, E. coli, M. catarrhalis, S. aureus, (but not MRSA); more active against pneumococci with reduced sensitivity than ceftriaxone. Ticarcillin/clavulanate is effective against Serratia, Citrobacter, as well as some strains of P. aeruginosa and Acinetobacter. The addition of beta-lactamase inhibitors does not overcome the resistance of Pseudomonas aeruginosa. Only 20-30% of P strains are sensitive to ticarcillin aeruginosa. All drugs are bactericidal against anaerobes, including B. fragilis, Prevotella melaninogenicus. Used for perioperative prophylaxis in abdominal surgery. Sulbactam has its own clinically significant antibacterial activity against Neisseria and Acinetobacter.

Side effects. Nausea and vomiting, diarrhea, rarely - hepatitis, cholestatic jaundice. There have been cases of vasculitis, serum sickness, erythema multiforme (including Stevens-Johnson syndrome), exfoliative; Surface plaque on teeth is possible when using the suspension.

Interaction. Antacids, laxatives, and glucosamine reduce the absorption of protected penicillins.

Amoxicillin/clavulanic acid

Indications. Infections of the respiratory tract, skin and soft tissues, bones, genitourinary and abdominal, caused by beta-lactamase-producing microorganisms. As a first-choice drug, it is used in children recently discharged from hospital or treated with antibiotics for a period of 3 months before the present illness, as well as in groups at increased risk for the resistance of pneumotropic flora (boarding schools, preschool children). The drug of choice for anaerobic infections (Vincenta, lung abscess, deep wounds), abscesses, fasciitis and cellulitis, animal bites, dental infections, as well as for antibacterial prophylaxis during operations on the abdominal and pelvic organs.

Contraindications. History of jaundice or hepatic dysfunction associated with the use of clavulanic acid. Increased diaper rash - does not prevent repeated use.

Carefully. Kidney, liver failure; erythematous rashes characteristic of infectious mononucleosis, chronic lymphocytic leukemia.

Dosage (for amoxicillin): Orally for children under 12 years of age - 45 mg/kg/day in 2 divided doses (up to 750 mg/day), over 12 years of age and adults - 1750 mg per day in 2 divided doses (875×2). If necessary, the dose is increased to 80-100 mg/kg/day, preferably using drugs with a ratio of amoxicillin to clavulanate of 7:1 or higher. IV for newborns - 60 mg/kg/day for 2 injections, for children from 1 month. up to 12 years old - 40-60 (up to 90-120) mg/kg/day, over 12 years old and adults - 3-4 (up to 6) g/day for 3-4 administrations.

Release form. Amoxicillin to clavulanate ratio:

2:1 - table. 0.25/0.125 g (Augmentin - original amoxicillin/clavulanate produced by GlaxoSmithKline, UK, Medoklav - Medohsmi, Cyprus, Amoxiclav - Lek, Slovenia);
4:1 - table. 500/125 mg, por. d/prig. susp. 125 mg/31.25 mg/5 ml, 250 mg/62.5 mg/5 ml (Amoxiclav, Augmentin, Medoclav);
4:1 - table. dispersible 125 mg/31.25 mg; 250 mg/62.5 mg and 500 mg/125 mg (Flemoklav Solutab - Astellas Pharma Europe B.V., the Netherlands). 5:1 - time. for IV solution 500/100 mg, 1000/200 mg (Augmentin, Amoxiclav, Medoclav) 7:1 - table. 0.875/0.125 g (Amoxiclav)
7:1 - table. 0.875/0.125 g, por. d/prig. susp. 200/28.5 mg/5 ml and 400/57 mg/5 ml (Augmentin - dosing forms 2 times a day with the best ratio of amoxicillin and clavulanate).

Ampicillin/sulbactam

Indications and contraindications. Same as amoxicillin/clavulanate, hypersensitivity to sulbactam.

Dosing. Children of all ages, including newborns - 150 mg/kg/day, (100 mg/kg/day ampicillin and 50 mg/kg/day sulbactam) for 3-4 (for newborns - for 2) administrations, adults - 1.5-12 g per day for 2-4 administrations IM or IV.

Release forms: por. d/prig. solutions 0.5/0.25 g, 1/0.5 g, 2/1 g (Unasin-Pfizer, USA).

Ticarcillin + clavulanic acid (ticarcilliri/clavulanic acid)

Indications. Severe (lungs, abdominal cavity, bones, soft tissues, urinary tract), caused by multiresistant gram-negative flora, including anaerobic.

Dosage (for ticarcillin): children over 3 months. with a weight of up to 60 kg - 200-300 mg/kg/day for 4-6 injections, for children weighing 60 kg or more, as well as adults - 12-18 g for 4-6 injections intravenously (in 30 minutes) .

Side effects: dizziness, neutropenia, hypokalemia.

Release form: liof. por. d/prig. 1500/100 mg and 3000/200 mg (15:1) (Timentin-GlaxoSmith-Klein, UK).

Content

Penicillins were discovered at the beginning of the 20th century, but medical science has continuously improved their properties. Thus, modern drugs have become resistant to penicillinase, which previously deactivated them, and have become immune to the acidic gastric environment.

Classification of penicillins

A group of antibiotics produced by molds of the genus Penicillium are called penicillins. They are active against most gram-positive and some gram-negative microbes, gonococci, spirochetes, and meningococci. Penicillins are part of a large group of beta-lactam antibiotics. They are divided into natural and semi-synthetic, have the general properties of low toxicity, and a wide range of dosages.

Classification of antibiotics:

Natural (benzylpenicillins, bicillins, phenoxymethylpenicillin).
Isoxazolepenicillins (oxacillin, flucloxacillin).
Amidinopenicillins (amdinocillin, acidocillin).
Aminopenicillins (ampicillin, amoxicillin, pivampicillin).
Carboxypenicillins (carbenicillin, carindacillin, ticarcillin).
Ureidopenicillins (azlocillin, piperacillin, mezlocillin).

According to the source of production, spectrum of action and combination with beta-lactamases, antibiotics are divided into:

Natural: benzylpenicillin, phenoxymethylpenicillin.
Antistaphylococcal: oxacillin.
Extended spectrum (aminopenicillins): ampicillin, amoxicillin.
Active against Pseudomonas aeruginosa (Pseudomonas aeruginosa): carboxypenicillins (ticarcillin), ureidopenicillins (azlocillin, piperacillin).
Combined with beta-lactamase inhibitors (inhibitor-protected): in combination with amoxicillin, ticarcillin, ampicillin/sulbactam clavunate.

	Drug names	Spectrum of action
Natural	Bicillin, Benzathine, Penicillin, Ecobol	Streptococci, staphylococci, bacilli, enterococci, listeria, corynebacteria, neisseria, clostridia, actinomycetes, spirochetes
Semi-synthetic	Oxacillin, Ticarcillin, Methicillin, Mecillam, Nafcillin	Enterobacteriaceae, Haemophilus influenzae, spirochetes
With an extended spectrum of action (antipseudomonas)	Amoxicillin, Augmentin, Ampicillin trihydrate	Klebsiella, Proteus, Clostridia, Staphylococcus, Gonococcus
With a broad antibacterial spectrum	Carbenicillin, Azlocillin, Piperacillin, Azithromycin	Enterobacteriaceae, Klebsiella, Proteus

Penicillin group drugs

Antibiotics of a number of penicillins are available in the form of tablets and injections, sold with a prescription from a doctor, but over-the-counter drugs are also available.

They are used in dentistry, otorhinolaryngology, surgery, urology, gynecology, ophthalmology, and venereology.

Pills

The penicillin series of antibiotics is represented by popular tablets:

Drug name	Indications for use	Method of administration	Side effects	Contraindications
Amoxicar	Pharyngitis, bronchitis, pneumonia, cystitis, osteomyelitis	1 piece each every 8 hours for no longer than 14 days in a row	Vomiting, dyspepsia, diarrhea, hepatitis, leukopenia, itching, urticaria, dizziness, superinfection, convulsions	Intolerance to the components of the composition, history of cholestatic jaundice, phenylketonuria
Amoxiclav	Sinusitis, otitis, abscess, tonsillitis, pharyngitis, acute cholangitis	1 piece each every 8 hours for 5–45 days	Loss of appetite, vomiting, nausea, hepatitis, colitis, erythema, dermatitis, candidiasis	Jaundice, allergy to the components of the composition
Ampicillin	Cholangitis, cholecystitis, pneumonia, bronchitis, abscess, meningitis, gastroenteritis, typhoid fever, paratyphoid fever, endocarditis, peritonitis, septicemia, pyelitis, gonorrhea	Half an hour before or 2 hours after meals, 250–1000 mg every 6 hours	Allergy, skin rash, itching, rhinitis, urticaria, conjunctivitis, erythema, nausea, diarrhea, vomiting, fever, joint pain, hepatitis, tremor, convulsions	Intolerance to the components of the composition, severe impairment of the kidneys, liver, leukemia, HIV infection
Augmentin	Pneumonia, bronchitis, bronchopneumonia, cystitis, urethritis, pyelonephritis, gonorrhea, osteomyelitis, periodontitis, septic abortion	1 piece each three times a day for a course of 5–14 days	Candidiasis, anemia, vasculitis, dizziness, convulsions, diarrhea, vomiting, nausea, gastritis, stomatitis, colitis, itching, rash, urticaria, crystalluria	Intolerance to the components of the composition, history of jaundice, phenylketonuria
Flemoklav Solutab	Otitis, sinusitis, pharyngitis, tonsillitis, bronchitis, community-acquired pneumonia	1 piece each three times a day for a course of 5–14 days	Allergy, nausea, diarrhea, vomiting, superinfection, urticaria	Jaundice, mononucleosis, lymphocytic leukemia, age up to 2 years
	Pneumonia, bronchitis, pyelitis, cystitis, gonorrhea, cervicitis, peritonitis, enterocolitis, borreliosis, erysipelas, meningitis, salmonellosis		Urticaria, erythema, fever, edema, rhinitis, dermatitis, dysbacteriosis, enterocolitis, agitation, insomnia, leukopenia, candidiasis, tachycardia	Allergic diathesis, hay fever, bronchial asthma, lactation, liver failure

Injections

Antibiotics of the penicillin group in the form of injections:

Drug name	Indications for use	Method of administration	Side effects	Contraindications
Ospamox	Bronchitis, pneumonia, whooping cough, pyelonephritis, gonorrhea, adnexitis, paratyphoid fever, shigellosis, leptospirosis, listeriosis, septicemia	1.5-2 g per day in 2-3 injections for 10 days	Nausea, glossitis, stomatitis, urticaria, joint pain, erythema, headache, fatigue	Respiratory viral infections
Timentin	Sepsis, bacteremia, endometritis, pyelonephritis	Intravenous 1.6-3.2 g every 6-8 hours	Necrolysis, vomiting, diarrhea, colitis, hypokalemia	Prematurity of children, intolerance to the components of the composition
Hiconcil	Borreliosis, Lyme disease, gonorrhea, endocarditis	500 mg three times a day for 5–12 days	Nausea, allergies, diarrhea	Hypersensitivity to the components of the composition

Penicillin antibiotics for children

Doctors prescribe penicillin antibiotics to children with caution because they are at increased risk of developing negative effects. In the first years of life, the child is given benzylpenicillins to treat sepsis, meningitis, and pneumonia. Contraindications include: intolerance to the components of the composition, insufficiency of the kidneys and liver.

Children's bodies are more sensitive to antibiotics. Penicillins can accumulate, causing seizures. List of oral medications used for the treatment of bacterial diseases for children:

Amoxicillin;
Augmentin;
Amoxiclav.

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ANTIBIOTICS OF THE PENICILLIN GROUP

According to the modern classification, antibiotics of the penicillin group are divided into short-acting biosynthetic penicillins (benzylpenicillin sodium salt, benzylpenicillin potassium salt, benzylpenicillin novocaine salt, phenoxymethylpenicillin), long-acting biosynthetic penicillins (bicillin-1, bicillin-5, benzathine benzyl-penicillin), semi-synthetic penicillins: aminopenicillins (amoxicillin, ampicillin, bacampicillin, penicillin, timentin), isoxazolylpenicillins (cloxacillin, oxacillin, flucloxacillin), carboxypenicillins (carbenicillin), ureidopenicillins (azlocillin, mezlocillin, piperacillin).

AZLOCILLIN (Azlocillin)

Synonyms: Securopen, Azlin.

Semi-synthetic beta-lactam antibiotic of the acylureidopenicillin group.

Pharmachologic effect. It has a bactericidal (bacteria-destroying) effect on a large number of pathogenic (disease-causing) gram-negative, indol-positive and gram-positive microorganisms. Not resistant to beta-lactamases (enzymes secreted by microbes that destroy penicillins). Synergism (increased effect when used together) with aminoglycoside antibiotics has been proven.

Indications for use. Urogenital infections (infectious diseases of the urinary and genital organs), septic conditions (diseases associated with the presence of microbes in the blood) of various origins, infections of bones and soft tissues, respiratory (respiratory tract), biliary, gastrointestinal infections, serositis (inflammation of the membrane, lining the cavity of the body, for example, the peritoneum), infected (contaminated with microbes) large areas of burns, etc. For local washing in the form of drainage (introduction through a tube into the cavity of an organ or tissue), the drug is prescribed for osteomyelitis (inflammation of the bone marrow and adjacent bone tissue), pleuroempyema (accumulation of pus between the membranes of the lungs), the presence of purulent cavities, fistulas (channels formed as a result of the disease that connect body cavities or hollow organs with the external environment or with each other).

Method of administration and dose. Before prescribing a drug to a patient, it is advisable to determine the sensitivity to it of the microflora that caused the disease in this patient. The drug is administered intravenously, rarely intramuscularly. The average daily dose for adults is from 8 g (2 g 4 times) to 15 g (5 g 3 times), for severe

infections, 20 g per day is allowed (5 g - 4 times). Premature babies weighing 1.5; 2.0 and 2.5 kg, the drug is administered in a single dose of 50 mg/kg 2 times a day. The average daily dose for newborns is 100 mg/kg body weight 2 times; for infants under 1 year of age - 100 mg/kg 3 times; for children aged 1 to 14 years - 75 mg/kg 3 times. The duration of treatment is at least 3 days after the temperature has normalized and clinical symptoms have disappeared. Used in the form of a 10% aqueous solution, administered intravenously (stream or drip) at a rate of 5 ml/min for 20-30 minutes.

Patients with impaired renal function require dose adjustment of azlocillin. Children whose creatinine clearance values (the rate of blood purification from the final product of nitrogen metabolism - creatinine) are less than 30 ml/min require a 2-fold reduction in the daily dose of the drug. For adult patients with creatinine clearance more than 30 ml/min, the drug is prescribed 5 g every 12 hours. For creatinine clearance less than 10 ml/min, the initial dose of the drug is 5 g, then 3.5 g is prescribed every 12 hours. With concomitant liver dysfunction These doses should be further reduced.

Side effect. Nausea, vomiting, flatulence (accumulation of gases in the intestines), loose stools, diarrhea (diarrhea) are possible; transient (transient) increase in the concentration of liver transaminases and alkaline phosphatase (enzymes) in the blood; rarely - increased concentration of bilirubin (bile pigment) in the blood. Sometimes - skin rash, itching, urticaria, rarely - drug fever (a sharp rise in body temperature in response to the administration of azlocillin), acute interstitial nephritis (inflammation of the kidney with primary damage to connective tissue), vasculitis (inflammation of the walls of blood vessels). In some cases - anaphylactic shock; leukopenia (decrease in the level of leukocytes in the blood), thrombocytopenia (decrease in the number of platelets in the blood), pancytopenia (decrease in the content of all formed elements in the blood - red blood cells, leukocytes, platelets, etc.). These side effects disappear after discontinuation of the drug. Impaired taste and smell (these effects occur when the rate of administration of the solution exceeds 5 ml/min). Rarely - erythema (limited redness of the skin), soreness or thrombophlebitis (inflammation of the vein wall with its blockage) at the injection site. In some cases, hypokalemia (low potassium levels in the blood), increased concentrations of creatinine and residual nitrogen in the blood serum. With the introduction of increased doses of the drug, due to an increase in its concentration in the cerebrospinal fluid (cerebrospinal fluid), convulsions may develop.

With prolonged or repeated use of azlocillin, superinfection may develop (severe, rapidly developing forms of an infectious disease caused by drug-resistant microorganisms that were previously in the body, but do not manifest themselves).

Contraindications. Hypersensitivity to penicillins and cephalosporins.

Release form. Lyophilized (dehydrated by freezing in a vacuum) powder for the preparation of an injection solution in bottles of 0.5; 1.0; 2.0 g in packs of 5 and 10 pieces.

Storage conditions. List B. In a dry, cool and dark place.

AMOXICILLIN

Synonyms: Amine, Amoxillat, amoxicillin-Rati ofarm, Amoxicillin-Teva, Apo-Amoxi, Gonoform, Grunamox, Dedoxil, Isoltil, Ospamox, Taysil, Flemoxin solutab, Hiconcil.

Pharmachologic effect. Bactericidal (bacteria-destroying) antibiotic from the group of semisynthetic penicillins. It has a wide spectrum of action, including gram-positive and gram-negative cocci, some gram-negative bacilli (Escherichia coli, Shigella, Salmonella, Klebsiella). Microorganisms that produce penicillinase (an enzyme that destroys penicillins) are resistant to the drug. The drug is acid-resistant and is absorbed quickly and almost completely in the intestine.

Indications for use. Bacterial infections: bronchitis (inflammation of the bronchi), pneumonia (inflammation of the lungs), tonsillitis, pyelonephritis (inflammation of the kidney tissue and renal pelvis), urethritis (inflammation of the urethra), colienteritis (inflammation of the small intestine caused by E. coli), gonorrhea, etc., - caused by microorganisms sensitive to the drug.

Method of administration and dose. Before prescribing a drug to a patient, it is advisable to determine the sensitivity to it of the microflora that caused the disease in this patient. Doses of the drug are set individually, taking into account the severity of the infection and the sensitivity of the pathogen. For adults and children over 10 years of age (with a body weight of more than 40 kg), the drug is prescribed 0.5 g 3 times a day; in case of severe infection, the dose can be increased to 1.0 g 3 times a day. Children aged 5-10 years are prescribed 0.25 g 3 times a day. Children aged from

Children 2 to 5 years old are prescribed 0.125 g 3 times a day. Children under 2 years of age are prescribed a daily dose of 20 mg/kg body weight in 3 divided doses. For children under 10 years of age, it is advisable to prescribe the drug in the form of a suspension (suspension in liquid). For the treatment of acute uncomplicated gonorrhea, it is prescribed

3 g once, it is advisable to simultaneously prescribe 1 g probenecid. When treating gonorrhea in women, it is recommended to repeat the indicated dose.

Side effect. Allergic reactions: urticaria, erythema (limited redness of the skin), Quincke's edema, rhinitis (inflammation of the nasal mucosa), conjunctivitis (inflammation of the outer membrane of the eye); rarely - fever (sharp increase in body temperature), joint pain, eosinophilia (increased number of eosinophils in the blood); extremely rarely - anaphylactic (allergic) shock. The development of superinfections (severe, rapidly developing forms of an infectious disease caused by drug-resistant microorganisms that were previously in the body but do not manifest themselves) is possible, especially in patients with chronic diseases or reduced resistance (resistance) of the body.

Contraindications. Hypersensitivity to penicillins, infectious mononucleosis (an acute viral disease that occurs with a high rise in body temperature, enlargement of the palatine lymph nodes and liver).

Prescribe the drug to pregnant women with caution; patients prone to allergic reactions. In patients who are hypersensitive to penicillins, cross-allergic reactions with cephalosporin antibiotics are possible.

Release form. 1.0 g tablets, film-coated; capsules of 0.25 g and 0.5 g; forte capsules; solution for oral (by mouth) use (1 ml - 0.1 g); suspension for oral use (5 ml - 0.125 g); dry substance for injection 1 g.

Storage conditions.

AUGMENTIN (Augmentm)

Synonyms: amoxicillin, potentiated with clavulanate, Amoxiclav, Amoklavin, Clavocin.

Pharmachologic effect. Broad-spectrum antibiotic. It has a bacteriolytic (bacteria-destroying) effect. Active against a wide range of aerobic (developing only in the presence of oxygen) and anaerobic (capable of existing in the absence of oxygen) gram-positive and aerobic gram-negative microorganisms, including strains that produce beta-lactamase (an enzyme that destroys penicillins). Clavulanic acid, which is part of the drug, ensures the resistance of amoxicillin to the effects of beta-lactamases, expanding its spectrum of action.

Indications for use. Bacterial infections caused by microorganisms sensitive to the drug: upper respiratory tract infections - acute and chronic bronchitis (inflammation of the bronchi), lobar bronchopneumonia (combined inflammation of the bronchi and lungs), empyema (accumulation of pus), abscesses (ulcers) of the lungs; bacterial infections of the skin and soft tissues; genitourinary tract infections - cystitis (inflammation of the bladder), urethritis (inflammation of the urethra), pyelonephritis (inflammation of the kidney tissue and renal pelvis); sepsis (blood infection by microbes from a source of purulent inflammation) during abortion, pelvic organ infections, syphilis, gonorrhea; osteomyelitis (inflammation of the bone marrow and adjacent bone tissue); septicemia (a form of blood infection by microorganisms); peritonitis (inflammation of the peritoneum); postoperative infections.

For children under 1 year of age, the drug is prescribed in the form of drops. Single dose for children up to 3 months. - 0.75 ml, for children from 3 months. up to one year - 1.25 ml. In severe cases, a single intravenous dose for children over 3 months of age. up to 12 years of age is 30 mg/kg body weight; the drug is administered every 6-8 hours. Children under 3 months are administered a single dose of 30 mg/kg body weight: premature babies and children in the perinatal period (up to the 7th day of life of newborns) - every 12 hours, then every 8 hours. Treatment The drug should not be continued for more than 14 days without reviewing the clinical situation.

Children under 12 years of age are prescribed the drug in the form of a syrup or suspension. A single dose depends on age and is: for children aged 7-12 years - 10 ml (0.156 g/5 ml) or 5 ml (0.312 g/5 ml); for children aged 2-7 years - 5 ml (0.156 g/5 ml); children aged 9 months and older. before

2 years - 2.5 ml of syrup (0.156 g/5 ml) 3 times a day. For severe infections, these doses can be doubled.

Adults and children over 12 years of age with mild to moderate infections are prescribed 1 tablet (0.375 g) 3 times a day. For severe infection, the single dose is 1 tablet. 0.625 g or 2 tablets. 0.375 g each

3 times a day. It is also possible to administer the drug intravenously in a single dose of 1.2 g every 6-8 hours. If necessary, the drug can be administered every 6 hours. The maximum single dose is 1.2 g, the maximum permissible daily dose for intravenous administration is 7.2 g.

Patients with moderate or severe renal excretory dysfunction require adjustment of the drug dosage regimen. When creatinine clearance (the rate of blood purification from the final product of nitrogen metabolism - creatinine) is more than 30 ml/min, no change in dosage regimen is required; at 10-30 ml/min - the initial dose of the drug is 1.2 g intravenously, then 0.6 g every 12 hours. With creatinine clearance less than 10 ml/min, the initial dose of the drug is 1.2 g, then 0.6 g every 24 hours. Augmentin is excreted during dialysis (a method of blood purification). When using the drug in patients on dialysis, additional intravenous administration of the drug is prescribed at a dose of 0.6 g during and 0.6 g at the end of the dialysis procedure.

Augmentin should not be mixed in the same syringe or dropper with aminoglycoside antibiotics, as inactivation (loss of activity) of the latter occurs. The drug should not be mixed with blood products and protein-containing (protein-containing) fluids.

Side effect. Rarely - dyspepsia (digestive disorders). The severity of dyspeptic side effects may decrease when taking the drug with food. Isolated cases of liver dysfunction, the development of hepatitis, and cholestatic jaundice (jaundice associated with stagnation of bile in the biliary tract) have been described. There are isolated reports of the development of pseudomembranous colitis (intestinal colic, characterized by attacks of abdominal pain and the release of large amounts of mucus in the stool). Rarely - urticaria, Quincke's edema (allergic edema); very rarely - anaphylactic (allergic) shock, erythema multiforme (an infectious-allergic disease characterized by redness of symmetrical areas of the skin and a rise in temperature), Stevens-Johnson syndrome (a disease characterized by redness and hemorrhage in the mucous membranes of the mouth, urethra and conjunctiva / outer membrane of the eye /), exfoliative dermatitis (redness of the skin of the entire body with severe peeling). Rarely - candidiasis (fungal disease) and other types of superinfection (severe, rapidly developing forms of infectious disease caused by drug-resistant microorganisms that were previously in the body, but do not manifest themselves). In some cases, phlebitis (inflammation of the vein) may develop at the injection site.

Contraindications. Hypersensitivity to the components of the drug.

Intravenous administration should be used with caution in patients with severe liver dysfunction. If urticaria or erythematous rash appears, treatment should be discontinued.

It is not recommended to use the drug during pregnancy (especially in the first trimester) and breastfeeding.

The drug should be prescribed with caution to patients with a history of allergic reactions (medical history).

Release form. Tablets of 0.375 g (0.25 g amoxicillin and 0.125 g clavulanic acid); tablets of 0.625 g (0.5 g amoxicillin and 0.125 g clavulanic acid). Syrup in bottles (5 ml contain 0.156 g /0.125 g amoxicillin and 0.03125 g clavulanic acid/ or 0.312 g /0.25 g amoxicillin and 0.0625 g clavulanic acid/).

Dry substance for the preparation of suspension (1 measuring spoon contains 0.125 g of amoxicillin and 0.031 g of clavulanic acid) and suspension-forte (1 measuring spoon contains 0.25 g of amoxicillin and 0.062 g of clavulanic acid). Dry substance for the preparation of drops (1 ml of drops contains 0.05 g of amoxicillin and 0.0125 g of clavulanic acid). In dosage forms for oral (by mouth) use, amoxicillin is in the form of a trihydrate, and clavulanic acid is in the form of a potassium salt.

Powder for injection 0.6 g (0.5 g amoxicillin and 0.1 g clavulanic acid) in vials. Powder for injection 1.2 g (1.0 g amoxicillin and 0.2 g clavulanic acid). In dosage forms for intravenous use, amoxicillin is in the form of a sodium salt, and clavulanic acid is in the form of a potassium salt. Each 1.2 g vial contains approximately 1.0 mmol potassium and 3.1 mmol sodium.

Storage conditions. List B. In a cool, dry place.

CLONACOM-X

Pharmachologic effect. A combined drug containing semi-synthetic penicillins. The combination of amoxicillin with penicillinase-resistant (resistant to the action of the enzyme that destroys penicillins) cloxacillin expands the spectrum and in some cases enhances the effect of each drug separately. Amoxicillin has a wide spectrum of action, is active against most gram-negative (with the exception of Pseudomonas aeruginosa) and gram-positive bacteria (with the exception of penicillinase-forming / penicillin-destroying enzyme - penicillinase / staphylococci). Not resistant to penicillinase. Cloxacillin has a spectrum of action similar to benzylpenicillin, but is resistant to penicillinase.

Indications for use. Infectious diseases caused by microorganisms sensitive to the drug: upper respiratory tract infections, bronchitis (inflammation of the bronchi), pneumonia (pneumonia), urinary tract infections, skin and soft tissue infections, gastrointestinal infections, infections of bones and joints, gonorrhea.

Method of administration and dose. Before prescribing a drug to a patient, it is advisable to determine the sensitivity to it of the microflora that caused the disease in this patient. Adults are recommended to take 1 capsule every 6-8 hours, depending on the severity of the disease. If renal function is impaired, a dose reduction is necessary.

Side effect.

Contraindications. Infectious mononucleosis (an acute viral disease that occurs with a high rise in body temperature, enlargement of the palatine lymph nodes and liver). Hypersensitivity to penicillin antibiotics. The drug should be prescribed with caution to patients with a history of allergic reactions (medical history).

Release form. Capsules in a package of 100 pieces. One capsule contains amoxicillin trihydrate and cloxacillin sodium in quantities corresponding to 0.25 g of amoxicillin and 0.25 g of cloxacillin.

Storage conditions. List B. In a dry place, protected from light. . .

AMPICILLIN (AmpiciUinum)

Synonyms: Pentrexil, Abetaten," Acidocycline, Aniline, Acrocilin, Agnopen, Albercilin, Amil, Amecillin, Ampen, Ampeksin, Ampiphen, Ampilin, Ampiopenil, Amplenil, Amplital, Bactipen, Biampen, Binotal, Britapen, Broadocillin, Cimexillin, Diacyclin, Dicillin, Domicillin , Domipen, Eurocillin, Fortapen, Grampenil, Isticillin, Lificillin, Maxibiotic, Maxipred, Morepen, Negopen, Opicillin, Oracillina, Penberin, Penibrin, Pentrex, Policillin, Riomycin, Roscillin, Semicillin, Synteline, Sinpenin, Totacillin, Ultrabion, Vampen, Vexampil , Vidopen, Zimopen, Apo-Ampi, Mencillin, Standacillin, Dedoompil, Campicillin, etc.

Pharmachologic effect. ampicillin is a semisynthetic antibiotic obtained by acylation of 6-aminopenicillanic acid with an amino-phenylacetic acid residue.

The drug is not destroyed in the acidic environment of the stomach and is well absorbed when taken orally. Active against gram-positive microorganisms affected by benzylpenicillin. In addition, it acts on a number of gram-negative microorganisms (Salmonella, Shigella, Proteus, Escherichia coli, Klebsiella pneumoniae /Friedlander's bacillus/, Pfeiffer's bacillus /influenza bacillus/) and is therefore considered as a broad-spectrum antibiotic and is used for diseases caused by mixed infections.

Ampicillin has no effect on penicillinase-forming (forming penicillinase, an enzyme that destroys penicillins) staphylococci that are resistant to benzylpenicillin, since it is destroyed by penicillinase.

Indications for use. Ampicillin is used to treat patients with pneumonia (inflammation of the lungs), bronchopneumonia (combined inflammation of the bronchi and lungs), with abscesses (ulcers) of the lungs, tonsillitis, peritonitis (inflammation of the peritoneum), cholecystitis (inflammation of the gallbladder), sepsis (blood poisoning by microbes from a purulent focus). inflammation), intestinal infections, postoperative soft tissue infections and other infections caused by microorganisms sensitive to it. The drug is highly effective against urinary tract infections caused by Escherichia coli, Proteus, enterococci or mixed infections, since it is excreted unchanged in the urine in high concentrations. Ampicillin also enters the bile in large quantities. The drug is effective in the treatment of gonorrhea.

Method of administration and dose. Before prescribing a drug to a patient, it is advisable to determine the sensitivity to it of the microflora that caused the disease in this patient. Ampicillin is prescribed orally (regardless of food intake). A single dose for adults is 0.5 g, a daily dose is 2-3 g. Children are prescribed at the rate of 100 mg/kg. The daily dose is divided into 4-6 doses.

The duration of treatment depends on the severity of the disease and the effectiveness of therapy (from 5-10 days to 2-3 weeks or more).

Side effect. When treated with ampicillin, allergic reactions may occur in the form of skin rash, urticaria, angioedema, etc., and in rare cases, anaphylactic shock (mainly with the administration of ampicillin sodium salt).

If allergic reactions occur, it is necessary to stop administering the drug and carry out desensitizing (preventing or inhibiting allergic reactions) therapy. If signs of anaphylactic shock appear, urgent measures should be taken to remove the patient from this state.

With long-term treatment with ampicillin in weakened patients, it is possible to develop superinfection (severe, rapidly developing forms of an infectious disease caused by drug-resistant microorganisms that were previously in the body, but do not manifest themselves), caused by drug-resistant microorganisms (yeast-like fungi, gram-negative microorganisms). It is advisable for these patients to simultaneously prescribe B vitamins and vitamin C, and, if necessary, nystatin or levorin.

Contraindications. The drug is contraindicated in case of hypersensitivity to penicillin. For liver failure, use under monitoring of liver function; for bronchial asthma, hay fever and other allergic diseases only if absolutely necessary. At the same time, desensitizing agents are prescribed.

Ampicillin enhances the effect of oral anticoagulants (medicines taken by mouth that prevent blood clotting).

The drug should be prescribed with caution to patients with a history of allergic reactions (medical history).

Release form. Tablets and capsules 0.25 each. g in packs of 10 or 20 pieces. Powder for preparing a suspension (suspension) in 60 g orange glass jars (5 g of active substance). White powder with a yellowish tint (sweet taste), with a specific odor (contains sugar, vanillin and other fillers). Taken orally in the same dose as ampicillin based on the content of the active substance. Mix the powder with water or wash it down with water.

Storage conditions.

AMPIOX (Ampioxum)

A combination drug containing ampicillin and oxacillin. For oral administration, ampiox is produced, which is a mixture of ampicillin trihydrate and oxacillin sodium salt (1:1), and for parenteral use, ampiox-sodium (Ampioxum-natrium), which is a mixture of the sodium salts of ampicillin and oxacillin (2:1).

Pharmachologic effect. The drug combines the spectrum of antimicrobial action of ampicillin and oxacillin; acts on gram-positive (staphylococcus, streptococcus, pneumococcus) and gram-negative (gonococcus, meningococcus, E. coli, Pfeiffer's bacillus /influenza bacillus/, salmonella, shigella, etc.) microorganisms. Due to the content of oxacillin, it is active against penicillinase-forming (forming penicillinase - an enzyme that destroys penicillins) staphylococci.

The drug penetrates well into the blood when taken orally and parenterally (bypassing the digestive tract).

Indications for use. Used for infections of the respiratory tract and lungs (bronchitis - inflammation of the bronchi, pneumonia - inflammation of the lungs, etc.), tonsillitis, cholangitis (inflammation of the bile ducts), cholecystitis (inflammation of the gallbladder), pyelitis (inflammation of the renal pelvis), pyelonephritis (inflammation of tissue kidneys and renal pelvis), cystitis (inflammation of the bladder), infected wounds, skin infections, etc. Especially indicated in cases of severe diseases: sepsis (blood infection by microbes from the source of purulent inflammation), endocarditis (inflammation of the internal cavities of the heart), postpartum infection etc. With an unidentified antibiogram (the spectrum of antibiotic activity that characterizes the sensitivity of pathogens to it) and an unidentified pathogen, with a mixed infection caused by staphylococci or streptococci that are sensitive and insensitive to benzylpenicillin and gram-negative bacteria, with burn disease, kidney infections. It is used for the prevention of purulent postoperative complications during surgical operations and for the prevention and treatment of infections in newborns.

In the treatment of gonorrhea, ampiox is used in cases caused by benzylpenicillin-resistant strains of gonococci.

When administered parenterally, a single dose of ampiox sodium for adults is 0.5-1.0 g, daily - 2-4 g.

For newborns, premature babies and children under 1 year of age, a daily dose of 100-200 mg per 1 kg of body weight is administered; children from 1 year to 7 years - 100 mg/kg per day; from 7 to 14 years - 50 mg/kg per day; Children over 14 years of age are prescribed the adult dose. In case of severe infection, doses can be increased by 1.5-2 times.

To prepare solutions for intramuscular injection, add 2 ml of sterile water for injection to the contents of the bottle with ampiox sodium (0.1; 0.2; 0.5 g).

The duration of treatment ranges from 5-7 days to 3 weeks. and more.

For intravenous administration (jet), a single dose of the drug is dissolved in 10-15 ml of sterile water for injection or isotonic sodium chloride solution and administered slowly over 2-3 minutes. For intravenous drip administration to adults, the drug is dissolved in 100-200 ml of isotonic sodium chloride solution or 5% glucose solution and administered at a rate of 60-80 drops per minute. For drip administration to children, a 5-10% glucose solution (30-100 ml) is used as a solvent. It is administered intravenously for 5-7 days, followed by a transition (if necessary) to intramuscular administration. Solutions are used immediately after preparation; It is unacceptable to mix them with other medications.

When taken orally, a single dose of ampiox for adults is 0.5-1.0 g, daily - 2-4 g. Children from 3 to 7 years old are prescribed 100 mg/kg per day, from 7 to 14 years old - 50 mg/kg per day, over 14 years - in the adult dose. Duration of treatment - from 5-7 days to 2 weeks. and more. The daily dose is divided into 4-6 doses.

Side effect. Possible side effects: with parenteral (bypassing the digestive tract) administration of ampiox sodium - pain at the injection site and allergic reactions, in rare cases - anaphylactic (allergic) shock; when taking Ampiox orally - nausea, vomiting, loose stools, allergic reactions. If necessary, desensitizing (preventing or inhibiting allergic reactions) agents are prescribed.

Contraindications. Ampiox and ampiox sodium are contraindicated if there is a history (medical history) of toxic-allergic reactions to drugs of the penicillin group.

Release form. For parenteral administration, ampiox sodium is produced in bottles of 0.1; 0.2 or 0.5 g, indicating “Intravenous” or “Intramuscular” on the label. For oral administration, Ampiox is available in capsules of 0.25 g in a package of 20 pieces.

Storage conditions.

AMPICILLIN SODIUM SALT (Ampicillinum-natrium)

Synonyms: Penbritin, Penbrok, Policillin, Ampicide.

Pharmachologic effect. Broad-spectrum semi-synthetic penicillin. Active against coccal microorganisms (staphylococci that do not form penicillinase /an enzyme that destroys penicillins/, streptococci, pneumococci, gonococci and meningococci) and most gram-negative bacteria (E. coli, Salmonella, Shigella, Proteus mirabilis, H. influenzae and some strains of KJ. pneumoniae).

It is quickly absorbed into the blood and penetrates into the tissues and fluids of the body. It is excreted mainly by the kidneys. Does not have cumulative properties (the ability to accumulate in the body). Low toxicity (does not have a pronounced damaging effect on the body).

Indications for use. Inflammatory diseases of the respiratory tract: pneumonia (pneumonia), bronchitis (inflammation of the bronchi), pharyngitis (inflammation of the pharynx), etc.; urological diseases: pyelonephritis (inflammation of the kidney tissue and renal pelvis), cystitis (inflammation of the bladder), prostatitis (inflammation of the prostate gland), intestinal infections: dysentery, salmonellosis, enterocolitis (inflammation of the small and large intestines), septic endocarditis (inflammation of the internal cavities of the heart due to the presence of microbes in the blood), meningitis (inflammation of the membranes of the brain), erysipelas, etc.

Method of administration and dose. Before prescribing a drug to a patient, it is advisable to determine the sensitivity to it of the microflora that caused the disease in this patient. It is used for intramuscular and intravenous (jet or drip) administration. For both routes of administration, a single dose of the drug for adults is 0.25-0.5 g; daily - 1-3 g. For severe infections, the daily dose can be increased to 10 g or more. For meningitis - up to 14 g per day. The frequency of administration is 6-8 times. The drug is prescribed to newborns at a daily dose of 100 mg/kg, to children of other age groups - 50 mg/kg. In case of severe infection, the indicated doses can be doubled.

The daily dose is administered in 4-6 doses at intervals of 4-6 hours.

A solution for intramuscular administration is prepared ex tempore (before use) by adding 2 ml of sterile water to the contents of the bottle (0.25 or 0.5 g). injections. The duration of treatment is 7-14 days or more.

For intravenous jet administration, a single dose of the drug (no more than 2 g) is dissolved in 5-10 ml of sterile water for injection or isotonic sodium chloride solution and administered slowly over 3-5 minutes (1-2 g over 10-15 minutes). For a single dose exceeding 2 g, the drug is administered intravenously. For intravenous drip administration, a single dose of the drug is dissolved in a small volume of sterile water for injection (7.5-15.0 ml, respectively), then the resulting antibiotic solution is added to 125-250 ml of isotonic sodium chloride solution or 5-10% glucose solution and administered at a rate of 60-80 drops per minute. For drip administration to children, a 5-10% glucose solution (30-50 ml depending on age) is used as a solvent. Solutions are used immediately after preparation; It is unacceptable to add other medications to them. The daily dose is divided into 3-4 injections. The duration of treatment is 5-7 days, followed by a transition (if necessary) to intramuscular administration.

Side effect. Allergic reactions.

Contraindications. Allergy to penicillin drugs, liver dysfunction.

The drug should be prescribed with caution to patients with a history of allergic reactions (medical history).

Release form. The bottles contain sterile powder complete with a solvent of 0.25 g, 0.5 g each; powder 5 g in a bottle for suspension; 10 mcg discs, 100 pieces per pack.

Storage conditions. List B. In a dry place, protected from light, at room temperature.

AMPICILLIN TRHYDRATE (Ampicillium trihydras)

Synonyms: A-Pen.

Pharmachologic effect. The same as ampicillin and its sodium salt. It differs from ampicillin in the presence of 3 molecules of crystallized water in its structure.

Indications for use. Same as for ampicillin.

Method of administration and dose. Before prescribing a drug to a patient, it is advisable to determine the sensitivity to it of the microflora that caused the disease in this patient. Orally 0.5 g every 4-6 hours, for severe infections - up to 10 g or more per day; children under 13 years old - 0.1-0.2 g (kg/day). The course of treatment is 7-14 days or more.

Side effects and contraindications are the same as for ampicillin.

Release form. Tablets of 0.25 g in a package of 24 pieces; capsules of 0.25 g in a package of 6 pieces.

Storage conditions. List B. In a dry place, protected from light, at room temperature.

CLONACOM-P

Pharmachologic effect. A combined drug containing semi-synthetic penicillins. The combination of ampicillin with penicillinase-resistant (resistant to the action of the enzyme that destroys penicillins) cloxacillin expands the spectrum and in some cases enhances the effect of each drug separately. Ampicillin has a wide spectrum of action, is active against most gram-negative (with the exception of Pseudomonas aeruginosa) and gram-positive bacteria (with the exception of penicillinase-forming / penicillinase-forming enzymes that destroy penicillins / staphylococci). Not resistant to penicillinase. Cloxacillin has a spectrum of action similar to benzylpenicillin, but is resistant to penicillinase.

Indications for use. Infectious diseases caused by microorganisms sensitive to the drug: upper respiratory tract infections, bronchitis (inflammation of the bronchi), pneumonia (pneumonia), infections of the urinary tract, skin and soft tissues, gastrointestinal tract, bones and joints, gonorrhea.

If renal function is impaired, a dose reduction is necessary.

Side effect. Allergic reactions, skin rash; possible diarrhea, nausea, vomiting; in some cases, pseudomembranous colitis (intestinal colic, characterized by attacks of abdominal pain and the release of large amounts of mucus in the stool) may develop.

The drug should be prescribed with caution to patients with a history of allergic reactions (medical history).

Release form. Capsules in a package of 100 pieces. One capsule contains 0.25 g ampicillin and 0.25 g cloxacillin.

Storage conditions. List B. In a dry place, protected from light.

SULTAMICILLIN

Synonyms: Sulaillin, Betamp, Unazin.

A combined drug containing ampicillin-sodium and sulbactam-sodium in a 2:1 ratio.

Pharmachologic effect. Sulbactam sodium does not have pronounced antibacterial activity, but irreversibly inhibits (suppresses the activity) beta-lactamase (an enzyme that destroys the beta-lactam nucleus of the penis). When used together with penicillins, sulbactam protects the latter from hydrolysis (decomposition with water) and inactivation (partial or complete loss of biological activity). Unazine (a combination of sulbactam + ampicillin) is a highly effective drug that acts on gram-positive and gram-negative aerobes (microorganisms that develop only in the presence of oxygen) and anaerobes (microorganisms that can exist in the absence of oxygen), including penicillin-resistant strains.

Indications for use. Unasin is used for pneumonia (inflammation of the lungs), bronchitis (inflammation of the bronchi), otitis (inflammation of the ear cavity), sinusitis (inflammation of the paranasal sinuses), purulent surgical infections (abscesses - ulcers, phlegmon - acute, not clearly demarcated purulent inflammation, osteomyelitis - inflammation bone marrow and adjacent bone tissue, etc.), peritonitis (inflammation of the peritoneum), urological (urinary tract) and gynecological infections, for the prevention of postoperative purulent complications, gonorrhea and other infections.

Children weighing less than 30 kg - 25-50 mg/kg per day in 2 divided doses, depending on the severity of the infection and at the discretion of the doctor. With a body weight of 30 kg or more - the same as for adults, i.e. 375-750 mg (1-2 tablets) 2 times a day. For children, the drug can be prescribed in the form of a suspension (suspension).

The course of treatment usually lasts from 5 to 14 days, but can be extended if necessary. After normalization of temperature and disappearance of the main pathological symptoms, treatment continues for another 48 hours.

In the treatment of uncomplicated gonorrhea, sultamicillin can be prescribed as a single dose of 2.25 g (6 tablets of 375 g). To extend the residence time of sulbactam and ampicillin in the blood plasma,

As a concomitant drug, 1 g of necid should be prescribed.

In patients with gonorrhea with suspected syphilis, microscopic tests should be performed throughout treatment and monthly serological tests for at least 4 months.

When treating any infection caused by hemolytic streptococci, to prevent the occurrence of rheumatism or glomerulonephritis (kidney disease), it is recommended to carry out antibacterial therapy for 10 days.

In patients with severely impaired renal function (creatinine clearance / rate of blood clearance from the final product of nitrogen metabolism - creatinine / less than 30 ml/min), the dynamics of the release of sulbactam and ampicillin are subject to the same effect, therefore, the ratio of one to the other in plasma will remain constant. In such patients, the dose of sultamicillin is prescribed at large intervals in accordance with the usual practice of using ampicillin.

After dilution, the suspension should be stored in the refrigerator for no more than 14 days.

Side effect. The most common side effect is diarrhea (diarrhea), nausea, vomiting, epigastric pain (the area of the abdomen located directly below the junction of the costal arches and the sternum), abdominal pain and colic. As with the treatment of other ampicillin antibiotics, in rare cases enterocolitis (inflammation of the small and large intestine) and pseudomembranous colitis (intestinal colic, characterized by attacks of abdominal pain and the release of large amounts of mucus in the stool) are observed. Rash, itching and other skin reactions. Drowsiness, malaise, headache. In rare cases, anemia (decreased hemoglobin content in the blood), thrombocytopenia (decreased number of platelets in the blood), eosinophilia (increased number of eosinophils in the blood) and leukopenia (decreased level of leukocytes in the blood). These effects disappear after stopping treatment. There may be a transient increase in the levels of alanine transferase and asparagine transferase enzymes. When administered intramuscularly, pain at the injection site is possible. In isolated cases, the development of phlebitis (inflammation of a vein) after intravenous administration of the drug.

Contraindications. History of allergies to any of the penicillins (previous).

The drug should be prescribed with caution to patients with a history of allergic reactions.

Release form. Sterile powder for intramuscular and intravenous administration 0.75 g in 10 ml bottles (ampicillin sodium 0.5 g, sulfabactam sodium 0.25 g). Sterile powder for intramuscular and intravenous administration 1.5 g in 20 ml bottles (ampicillin sodium 1.0 g, sulfabactam sodium 0.5 g). Sterile powder for intramuscular and intravenous administration 3 g in 20 ml bottles (ampicillin sodium 2.0 g, sulfabactam sodium 1.0 g). Tablets of 0.375 g of the drug. Powder for preparing a suspension (5 ml - 0.25 g of the drug).

Storage conditions. List B. In a place protected from light.

Mushrooms are a kingdom of living organisms. Mushrooms come in many varieties: some of them end up in our diet, some cause skin diseases, and some are so poisonous that they can cause death. But fungi of the genus Penicillium save millions of human lives from pathogenic bacteria.

Penicillin antibiotics based on this mold (mold is also a fungus) are still used in medicine.

In the 30s of the last century, Alexander Fleming conducted experiments with staphylococci. He studied bacterial infections. Having grown a group of these pathogens in a nutrient medium, the scientist noticed that there were areas in the dish around which there were no living bacteria. The investigation showed that the culprit for these stains was ordinary green mold, which likes to settle on stale bread. The mold was called Penicillium and, as it turned out, produced a substance that kills staphylococci.

Fleming studied the issue further and soon isolated pure penicillin, which became the world's first antibiotic. The principle of action of the medicine is as follows: when a bacterial cell divides, each half restores its cell membrane with the help of a special chemical element, peptidoglycan. Penicillin blocks the formation of this element, and the bacterial cell simply “resolves” in the environment.

But difficulties soon arose. Bacterial cells learned to resist the drug - they began to produce an enzyme called “beta-lactamase,” which destroys beta-lactams (the basis of penicillin).

For the next 10 years, an invisible war took place between pathogens that destroy penicillin, and scientists who modify this penicillin. This is how many modifications of penicillin were born, which now form the entire penicillin series of antibiotics.

The drug for any type of use spreads quickly throughout the body, penetrating almost all its parts. Exceptions: cerebrospinal fluid, prostate and visual system. In these places the concentration is very low, under normal conditions it does not exceed 1 percent. With inflammation, a rise of up to 5% is possible.

Antibiotics do not affect the cells of the human body, since the latter do not contain peptidoglycan.

The medicine is quickly eliminated from the body; after 1-3 hours, most of it exits through the kidneys.

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All drugs are divided into: natural (short and long-acting) and semi-synthetic (antistaphylococcal, broad-spectrum drugs, antipseudomonas).

These drugs obtained directly from mold. At the moment, most of them are obsolete, as pathogens have become immune to them. In medicine, benzylpenicillin and Bicillin are most often used, which are effective against gram-positive bacteria and cocci, some anaerobes and spirochetes. All these antibiotics are used only as injections into the muscles, since the acidic environment of the stomach quickly destroys them.

Benzylpenicillin in the form of sodium and potassium salts is a natural short-acting antibiotic. Its effect wears off after 3-4 hours, so frequent repeated injections are necessary.

Trying to eliminate this deficiency, pharmacists created natural long-acting antibiotics: Bicillin and benzylpenicillin novocaine salt. These drugs are called “depot forms” because after injection into the muscle they form a “depot” in it, from which the medicine is slowly absorbed into the body.

Examples of drugs: benzylpenicillin salt (sodium, potassium or novocaine), Bicillin-1, Bicillin-3, Bicillin-5.

Several decades after penicillin was obtained pharmacists were able to isolate its main active ingredient, and the process of modification began. Most drugs, after improvement, became resistant to the acidic environment of the stomach, and semi-synthetic penicillins began to be produced in tablets.

Isoxazolepenicillins are drugs that are effective against staphylococci. The latter have learned to produce an enzyme that destroys benzylpenicillin, and drugs from this group interfere with the production of the enzyme. But you have to pay for the improvement - drugs of this type are less well absorbed into the body and have a smaller spectrum of action compared to natural penicillins. Examples of drugs: Oxacillin, Nafcillin.

Aminopenicillins are broad-spectrum drugs. They are inferior to benzylpenicillins in the fight against gram-positive bacteria, but cover a wider range of infections. Compared to other drugs, they remain in the body longer and penetrate better through some body barriers. Examples of drugs: Ampicillin, Amoxicillin. You can often find Ampiox - Ampicillin + Oxacillin.

Carboxypenicillins and ureidopenicillins – antibiotics effective against Pseudomonas aeruginosa. At the moment, they are practically not used, since infections quickly become resistant to them. Occasionally you can find them as part of a comprehensive treatment.

Examples of drugs: Ticarcillin, Piperacillin

Sumamed

Active ingredient: azithromycin.

Indications: respiratory tract infections.

Contraindications: intolerance, severe renal failure, children under 6 months of age.

Price: 300-500 rubles.

Oxacillin

Active ingredient: oxacillin.

Indications: infections sensitive to the drug.

Price: 30-60 rubles.

Amoxicillin Sandoz

Indications: respiratory tract infections (including sore throat, bronchitis), genitourinary system infections, skin infections, other infections.

Contraindications: intolerance, children under 3 years of age.

Price: 150 rubles.

Ampicillin trihydrate

Indications: pneumonia, bronchitis, tonsillitis, other infections.

Contraindications: hypersensitivity, liver failure.

Price: 24 rubles.

Phenoxymethylpenicillin

Active ingredient: phenoxymethylpenicillin.

Indications: streptococcal diseases, mild to moderate infections.

Price: 7 rubles.

Amoxiclav

Active ingredient: amoxicillin + clavulanic acid.

Indications: infections of the respiratory tract, urinary system, gynecological infections, other infections sensitive to amoxicillin.

Contraindications: hypersensitivity, jaundice, mononucleosis and lymphocytic leukemia.

Price: 116 rubles.

Injections

Bicillin-1

Active ingredient: benzathine benzylpenicillin.

Indications: acute tonsillitis, scarlet fever, wound infections, erysipelas, syphilis, leishmaniasis.

Contraindications: hypersensitivity.

Price: 15 rubles per injection.

Ospamox

Active ingredient: amoxicillin.

Indications: infections of the lower and upper respiratory tract, gastrointestinal tract, genitourinary system, gynecological and surgical infections.

Contraindications: hypersensitivity, severe gastrointestinal infections, lymphocytic leukemia, mononucleosis.

Price: 65 rubles.

Ampicillin

Active ingredient: ampicillin.

Indications: infections of the respiratory and urinary tract, gastrointestinal tract, meningitis, endocarditis, sepsis, whooping cough.

Contraindications: hypersensitivity, impaired renal function, childhood, pregnancy.

Price: 163 rubles.

Benzylpenicillin

Indications: severe infections, congenital syphilis, abscesses, pneumonia, erysipelas, anthrax, tetanus.

Contraindications: intolerance.

Price: 2.8 rubles per injection.

Benzylpenicillin novocaine salt

Active ingredient: benzylpenicillin.

Indications: similar to benzylpenicillin.

Contraindications: intolerance.

Price: 43 rubles for 10 injections.

Amoxiclav, Ospamox, Oxacillin are suitable for treating children. But Before using the medicine, you must consult your doctor to adjust the dose.

Indications for use

Antibiotics of the penicillin group are prescribed for infections; the type of antibiotics is selected based on the type of infection. These can be various cocci, rods, anaerobic bacteria, and so on.

Most often, infections of the respiratory tract and genitourinary system are treated with antibiotics.

In the case of treating children, you must follow the instructions of the doctor, who will prescribe the right antibiotic and adjust the dose.

In case of pregnancy, antibiotics must be used with extreme caution, as they penetrate into the fetus. During lactation, it is better to switch to mixtures, since the medicine also penetrates into the milk.

There are no special guidelines for older people, although the doctor should consider the condition of the patient's kidneys and liver when prescribing treatment.

The main and, often, the only contraindication is individual intolerance. It occurs frequently - in approximately 10% of patients. Additional contraindications depend on the specific antibiotic and are specified in the instructions for use.

If side effects occur, you should immediately seek medical help, discontinue the drug and carry out symptomatic treatment.

Where does penicillin mold grow?

Almost everywhere. This mold includes dozens of subspecies, and each of them has its own habitat. The most notable representatives are penicillin mold, which grows on bread (it also attacks apples, causing them to quickly rot) and the mold used in the production of some cheeses.

What can replace penicillin antibiotics?

If the patient is allergic to penicillin, non-penicillin antibiotics can be used. Names of drugs: Cefadroxil, Cephalexin, Azithromycin. The most popular option is Erythromycin. But you need to know that Erythromycin often causes dysbiosis and stomach upset.

Penicillin antibiotics are a powerful remedy against infections caused by various bacteria. There are quite a few types of them, and treatment must be selected according to the type of pathogen.

They seem harmless to the body due to the fact that the only contraindication is a hypersensitivity reaction, but improper treatment or self-medication can provoke resistance of the pathogen to the antibiotic, and you will have to select another treatment, more dangerous and less effective.

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Antibacterial drugs that are common today made a real revolution in medicine less than a century ago. Humanity has received powerful weapons to fight infections that were previously considered fatal.

The first antibiotics were penicillin, which saved many thousands of lives during the Second World War and is still relevant in modern medical practice. It was with them that the era of antibiotic therapy began and thanks to them all other antimicrobial drugs were obtained.

This section provides a complete list of currently relevant antimicrobial drugs. In addition to the characteristics of the main compounds, all trade names and analogues are given.

Main title	Antimicrobial activity	Analogs
Benzylpenicillin potassium and sodium salts	Affects mainly gram-positive microorganisms. Currently, most strains have developed resistance, but spirochetes are still sensitive to the substance.	Gramox-D, Ospen, Star-Pen, Ospamox
Benzylpenicillin procaine	Indicated for the treatment of streptococcal and pneumococcal infections. Compared to potassium and sodium salts, it has a longer effect, since it dissolves more slowly and is absorbed from the intramuscular depot.	Benzylpenicillin-KMP (-G, -Teva, -G 3 mega)
Bicillins (1, 3 and 5)	It is used for chronic rheumatism for prophylactic purposes, as well as for the treatment of infectious diseases of moderate and mild severity caused by streptococci.	Benzicillin-1, Moldamine, Extincillin, Retarpin
Phenoxymethylpenicillin	It has a therapeutic effect similar to the previous groups, but is not destroyed in the acidic gastric environment. Available in tablet form.	V-Penicillin, Kliatsil, Ospen, Penicillin-Fau, Vepicombin, Megacillin Oral, Pen-os, Star-Pen
Oxacillin	Active against staphylococci that produce penicillinase. It is characterized by low antimicrobial activity and is completely ineffective against penicillin-resistant bacteria.	Oksamp, Ampioks, Oksamp-Sodium, Oksamsar
Ampicillin	Extended spectrum of antimicrobial activity. In addition to the main range of inflammatory diseases of the gastrointestinal tract, it also treats those caused by Escherichia, Shigella, and Salmonella.	Ampicillin AMP-KID (-AMP-Forte, -Ferein, -AKOS, -trihydrate, -Innotek), Zetsil, Pentrixil, Penodil, Standacillin
Amoxicillin	Used to treat inflammation of the respiratory and urinary tract. After identifying the bacterial origin of the stomach ulcer, Helicobacter pylori is used to eradicate.	Flemoxin solutab, Hiconcil, Amosin, Ospamox, Ecobol
Carbenicillin	The spectrum of antimicrobial action includes Pseudomonas aeruginosa and Enterobacteriaceae. Digestibility and bactericidal effect are higher than those of Carbenicillin.	Securopen
Piperacillin	Similar to the previous one, but the level of toxicity is increased.	Isipen, Pipracil, Picillin, Piprax
Amoxicillin/clavulanate	Due to the inhibitor, the spectrum of antimicrobial activity is expanded compared to an unprotected agent.	Augmentin, Flemoklav solutab, Amoxiclav, Amklav, Amovicombe, Verklav, Ranklav, Arlet, Klamosar, Rapiklav
Ampicillin/sulbactam		Sulacillin, Liboccil, Unazin, Sultasin
Ticarcillin/clavulanate	The main indication for use is nosocomial infections.	Hymentin
Piperacillin/tazobactam	The main indication for use is nosocomial infections.	Tazocin

The information provided is for informational purposes only and is not a guide to action. All prescriptions are made exclusively by a doctor, and therapy is carried out under his supervision.

Despite the low toxicity of penicillins, their uncontrolled use leads to serious consequences: the formation of resistance in the pathogen and the transition of the disease to a chronic form that is difficult to cure. It is for this reason that most strains of pathogenic bacteria today are resistant to first-generation ALD.

The medication prescribed by the specialist should be used for antibacterial therapy. Independent attempts to find a cheap analogue and save money can lead to a worsening of the condition.

For example, the dosage of the active substance in a generic may differ up or down, which will negatively affect the course of treatment.

When you have to change a medicine due to an acute lack of finances, you need to ask a doctor about this, since only a specialist can choose the best option.

Drugs of the penicillin group belong to the so-called beta-lactams - chemical compounds that have a beta-lactam ring in their formula.

This structural component is crucial in the treatment of bacterial infectious diseases: it prevents bacteria from producing a special biopolymer of peptidoglycan, which is necessary for the construction of the cell membrane. As a result, the membrane cannot form and the microorganism dies. There is no destructive effect on human and animal cells due to the fact that they do not contain peptidoglycan.

Medications based on waste products of mold fungi have become widespread in all areas of medicine due to the following properties:

High bioavailability - drugs are quickly absorbed and distributed throughout the tissues. The weakening of the blood-brain barrier during inflammation of the meninges also contributes to penetration into the cerebrospinal fluid.
Extensive spectrum of antimicrobial action. Unlike first-generation chemicals, modern penicillins are effective against the vast majority of gram-negative and positive bacteria. They are also resistant to penicillinase and the acidic environment of the stomach.
Lowest toxicity among all antibiotics. They are approved for use even during pregnancy, and proper use (as prescribed by a doctor and according to the instructions) almost completely eliminates the development of side effects.

In the process of research and experiments, many medications with different properties were obtained. For example, if they belong to the general series, penicillin and ampicillin are not the same thing. All penicillin antibiotics are well compatible with most other drugs. As for complex therapy with other types of antibacterial drugs, combined use with bacteriostatics weakens the effectiveness of penicillins.

A careful study of the properties of the first antibiotic showed its imperfection. Despite a fairly wide spectrum of antimicrobial action and low toxicity, natural penicillin turned out to be sensitive to a special destructive enzyme (penicillinase) produced by some bacteria. In addition, it completely lost its qualities in an acidic gastric environment, so it was used exclusively in the form of injections. In search of more effective and stable compounds, various semi-synthetic drugs have been created.

Today, penicillin antibiotics, a full list of which is given below, are divided into 4 main groups.

Produced by the mold fungi Penicillium notatum and Penicillium chrysogenum, benzylpenicillin is an acid in molecular structure. For medical purposes, it is chemically combined with sodium or potassium to form salts. The resulting compounds are used to prepare injection solutions that are quickly absorbed.

The therapeutic effect is observed within 10-15 minutes after administration, but lasts no more than 4 hours, which requires frequent repeated injections into muscle tissue (in special cases, the sodium salt can be administered intravenously).

These drugs penetrate well into the lungs and mucous membranes, and to a lesser extent into the cerebrospinal and synovial fluids, myocardium and bones. However, with inflammation of the meninges (meningitis), the permeability of the blood-brain barrier increases, which allows for successful treatment.

To prolong the effect of the drug, natural benzylpenicillin is combined with novocaine and other substances. The resulting salts (novocainic, Bicillin-1, 3 and 5) after intramuscular injection form a medicinal depot at the injection site, from where the active substance enters the blood constantly and at a low speed. This property allows you to reduce the number of administrations to 2 times a day while maintaining the therapeutic effect of potassium and sodium salts.

These drugs are used for long-term antibiotic therapy of chronic rheumatism, syphilis, and focal streptococcal infection.
Phenoxymethylpenicillin is another form of benzylpenicillin intended for the treatment of moderate infectious diseases. Differs from those described above in its resistance to hydrochloric acid of gastric juice.

This quality allows the medicine to be produced in the form of tablets for oral use (4 to 6 times a day). Most pathogenic bacteria, except spirochetes, are currently resistant to biosynthetic penicillins.

Read also: Instructions for using penicillin in injections and tablets

Natural benzylpenicillin is inactive against staphylococcus strains that produce penicillinase (this enzyme destroys the beta-lactam ring of the active substance).

For a long time, penicillin was not used to treat staphylococcal infections, until oxacillin was synthesized on its basis in 1957. It inhibits the activity of beta-lactamases of the pathogen, but is ineffective against diseases caused by strains sensitive to benzylpenicillin. This group also includes cloxacillin, dicloxacillin, methicillin and others, which are almost never used in modern medical practice due to increased toxicity.

This includes two subgroups of antimicrobial agents intended for oral use and having a bactericidal effect against most pathogenic microorganisms (both gram+ and gram-).

Compared to the previous groups, these compounds have two significant advantages. Firstly, they are active against a wider range of pathogens, and secondly, they are available in tablet form, which makes them much easier to use. Disadvantages include sensitivity to beta-lactamase, that is, aminopenicillins (ampicillin and amoxicillin) are unsuitable for the treatment of staphylococcal infections.

However, in combination with oxacillin (Ampiox) they become resistant.

The drugs are well absorbed and act for a long time, which reduces the frequency of use to 2-3 times every 24 hours. The main indications for use are meningitis, sinusitis, otitis, infectious diseases of the urinary and upper respiratory tract, enterocolitis and eradication of Helicobacter (the causative agent of stomach ulcers). A common side effect of aminopenicillins is a characteristic rash of a non-allergic nature, which immediately disappears after discontinuation.

They are a separate penicillin series of antibiotics, the name of which makes their purpose clear. Antibacterial activity is similar to aminopenicillins (with the exception of pseudomonas) and is pronounced against Pseudomonas aeruginosa.

According to the degree of effectiveness they are divided into:

Carboxypenicillins, the clinical significance of which has recently decreased. Carbenicillin, the first of this subgroup, is also effective against ampicillin-resistant Proteus. Currently, almost all strains are resistant to carboxypenicillins.
Ureidopenicillins are more effective against Pseudomonas aeruginosa and can also be prescribed for inflammation caused by Klebsiella. The most effective are Piperacillin and Azlocillin, of which only the latter remains relevant in medical practice.

Today, the vast majority of strains of Pseudomonas aeruginosa are resistant to carboxypenicillins and ureidopenicillins. For this reason, their clinical significance is decreasing.

The ampicillin group of antibiotics, highly active against most pathogens, is destroyed by penicillinase-forming bacteria. Since the bactericidal effect of oxacillin, which is resistant to them, is significantly weaker than that of ampicillin and amoxicillin, combined medications were synthesized.

In combination with sulbactam, clavulanate and tazobactam, antibiotics obtain a second beta-lactam ring and, accordingly, immunity to beta-lactamases. In addition, inhibitors have their own antibacterial effect, enhancing the main active ingredient.

Inhibitor-protected drugs successfully treat severe nosocomial infections, strains of which are resistant to most drugs.

Read also: About the modern classification of antibiotics by group of parameters

Its broad spectrum of action and good tolerance by patients have made penicillin the optimal treatment for infectious diseases. At the dawn of the era of antimicrobial drugs, benzylpenicillin and its salts were the drugs of choice, but at the moment most pathogens are resistant to them. However, modern semi-synthetic penicillin antibiotics in tablets, injections and other dosage forms occupy one of the leading places in antibiotic therapy in a variety of fields of medicine.

The discoverer also noted the particular effectiveness of penicillin against pathogens of respiratory diseases, so the drug is most widely used in this area. Almost all of them have a detrimental effect on bacteria that cause sinusitis, meningitis, bronchitis, pneumonia and other diseases of the lower and upper respiratory tract.

Inhibitor-protected drugs treat even particularly dangerous and persistent nosocomial infections.

Spirochetes are one of the few microorganisms that remain susceptible to benzylpenicillin and its derivatives. Benzylpenicillins are also effective against gonococci, which makes it possible to successfully treat syphilis and gonorrhea with minimal negative effects on the patient’s body.

Intestinal inflammation caused by pathogenic microflora responds well to treatment with acid-resistant medications.

Of particular importance are aminopenicillins, which are part of the complex eradication of Helicobacter.

In obstetric and gynecological practice, many penicillin drugs from the list are used both to treat bacterial infections of the female reproductive system and to prevent infection of newborns.

Here, penicillin antibiotics also occupy a worthy place: eye drops, ointments and injection solutions treat keratitis, abscesses, gonococcal conjunctivitis and other eye diseases.

Diseases of the urinary system that are of bacterial origin respond well to treatment only with inhibitor-protected medications. The remaining subgroups are ineffective, since pathogen strains are highly resistant to them.

Penicillins are used in almost all areas of medicine for inflammation caused by pathogenic microorganisms, and not only for treatment. For example, in surgical practice they are prescribed to prevent postoperative complications.

Treatment with antibacterial medications in general and penicillins in particular should be carried out only as prescribed by a doctor. Despite the minimal toxicity of the medicine itself, its improper use seriously harms the body. In order for antibiotic therapy to lead to recovery, you should follow medical recommendations and know the characteristics of the drug.

The scope of application of penicillin and various drugs based on it in medicine is determined by the activity of the substance against specific pathogens. Bacteriostatic and bactericidal effects occur in relation to:

Gram-positive bacteria - gonococci and meningococci;
Gram-negative - various staphylococci, streptococci and pneumococci, diphtheria, pseudomonas and anthrax bacilli, Proteus;
Actinomycetes and spirochetes.

Low toxicity and a broad spectrum of action make antibiotics of the penicillin group the optimal treatment for tonsillitis, pneumonia (both focal and lobar), scarlet fever, diphtheria, meningitis, blood poisoning, septicemia, pleurisy, pyemia, osteomyelitis in acute and chronic forms, septic endocarditis, various purulent infections of the skin, mucous membranes and soft tissues, erysipelas, anthrax, gonorrhea, actinomycosis, syphilis, blenorrhea, as well as eye diseases and ENT diseases.

Strict contraindications include only individual intolerance to benzylpenicillin and other drugs in this group. Also, endolumbar (injection into the spinal cord) administration of drugs to patients with diagnosed epilepsy is not permitted.

During pregnancy, antibiotic therapy with penicillin drugs should be treated with extreme caution. Despite the fact that they have minimal teratogenic effects, tablets and injections should be prescribed only in cases of urgent need, assessing the degree of risk to the fetus and the pregnant woman herself.

Since penicillin and its derivatives pass freely from the bloodstream into breast milk, it is advisable to avoid breastfeeding during therapy. The medicine can provoke a severe allergic reaction in a baby even at the first use. To prevent lactation from stopping, milk must be expressed regularly.

Among other antibacterial agents, penicillins stand out due to their low toxicity.

Undesirable consequences of use include:

Allergic reactions. Most often they manifest themselves as skin rash, itching, urticaria, fever and swelling. Extremely rarely, in severe cases, anaphylactic shock is possible, requiring immediate administration of an antidote (adrenaline).
Dysbacteriosis. An imbalance of natural microflora leads to digestive disorders (flatulence, bloating, constipation, diarrhea, abdominal pain) and the development of candidiasis. In the latter case, the mucous membranes of the mouth (in children) or vagina are affected.
Neurotoxic reactions. The negative effect of penicillin on the central nervous system is manifested by increased reflex excitability, nausea and vomiting, convulsions, and sometimes coma.

Timely medicinal support of the body will help prevent the development of dysbiosis and avoid allergies. It is advisable to combine antibiotic therapy with the use of pre- and probiotics, as well as desensitizers (if sensitivity is increased).

Tablets and injections should be prescribed to children with caution, taking into account possible negative reactions, and the choice of a specific drug should be approached thoughtfully.

In the first years of life, benzylpenicillin is used in cases of sepsis, pneumonia, meningitis, and otitis media. For the treatment of respiratory infections, sore throat, bronchitis and sinusitis, the safest antibiotics from the list are selected: Amoxicillin, Augmentin, Amoxiclav.

A child's body is much more sensitive to drugs than an adult's. Therefore, you should carefully monitor the baby’s condition (penicillin is excreted slowly and, when accumulated, can cause convulsions), and also take preventive measures. The latter include the use of pre- and probiotics to protect the intestinal microflora, diet and comprehensive strengthening of the immune system.

A little theory:

The discovery, which made a real revolution in medicine at the beginning of the 20th century, was made by accident. It must be said that the antibacterial properties of mold fungi were noticed by people in ancient times.

Alexander Fleming - discoverer of penicillin

The Egyptians, for example, 2500 years ago treated inflamed wounds with compresses made from moldy bread, but scientists took up the theoretical side of the issue only in the 19th century. European and Russian researchers and doctors, studying antibiosis (the property of some microorganisms to destroy others), attempted to derive practical benefits from it.

This was achieved by Alexander Fleming, a British microbiologist, who in 1928, on September 28, discovered mold in Petri dishes with colonies of staphylococcus. Its spores, which got onto the crops due to the negligence of the laboratory staff, sprouted and destroyed pathogenic bacteria. Interested, Fleming carefully studied this phenomenon and isolated a bactericidal substance called penicillin. For many years, the discoverer worked to obtain a chemically pure, stable compound suitable for treating people, but others invented it.

In 1941, Ernst Chain and Howard Florey were able to purify penicillin from impurities and conducted clinical trials with Fleming. The results were so successful that by 1943, mass production of the drug was organized in the United States, which saved many hundreds of thousands of lives during the war. The services of Fleming, Chain and Flory to humanity were recognized in 1945: the discoverer and developers became Nobel Prize laureates.

Subsequently, the original chemical was constantly improved. This is how modern penicillins appeared, resistant to the acidic environment of the stomach, resistant to penicillinase and more effective in general.

Read a fascinating article: The inventor of antibiotics or the story of saving humanity!

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Penicillin antibiotics are several types of drugs that are divided into groups. In medicine, drugs are used to treat various diseases of infectious and bacterial origin. The drugs have a minimal number of contraindications and are still used to treat various patients.

Once Alexander Fleming was studying pathogens in his laboratory. He created a nutrient medium and grew staphylococcus. The scientist was not particularly clean; he simply put beakers and cones in the sink and forgot to wash them.

When Fleming needed the dishes again, he discovered that they were covered with fungus - mold. The scientist decided to test his guess and examined one of the containers under a microscope. He noticed that where there was mold, there was no staphylococcus.

Alexander Fleming continued his research; he began to study the effect of mold on pathogenic microorganisms and discovered that the fungus has a destructive effect on the membranes of bacteria and leads to their death. The public could not be skeptical about the research.

The discovery helped save many people's lives. It saved humanity from those diseases that previously caused panic among the population. Naturally, modern medicines are relatively similar to those drugs that were used at the end of the 19th century. But the essence of the medications and their action have not changed so dramatically.

Penicillin antibiotics were able to revolutionize medicine. But the joy of the discovery did not last long. It turned out that pathogenic microorganisms and bacteria can mutate. They change and become insensitive to drugs. This led to significant changes in antibiotics such as penicillin.

Scientists spent almost the entire 20th century “fighting” microorganisms and bacteria, trying to create the ideal drug. The efforts were not in vain, but such improvements have led to the fact that antibiotics have changed significantly.

New generation drugs are more expensive, act faster, and have a number of contraindications. If we talk about those drugs that were obtained from mold, they have a number of disadvantages:

Poorly digestible. Gastric juice acts on the fungus in a special way, reducing its effectiveness, which undoubtedly affects the result of treatment.
Penicillin antibiotics are drugs of natural origin, for this reason they do not have a wide spectrum of action.
Medicines are quickly eliminated from the body, approximately 3-4 hours after injection.

Important: These medications have virtually no contraindications. It is not recommended to take them if you have an individual intolerance to antibiotics, or if you develop an allergic reaction.

Modern antibacterial agents differ significantly from the familiar penicillin. In addition to the fact that today you can easily purchase medications of this class in tablets, there are a great variety of them. Classification and generally accepted division into groups will help you understand the drugs.

Antibiotics of the penicillin group are conventionally divided into:

Natural.
Semi-synthetic.

All medicines based on mold are antibiotics of natural origin. Today, such medications are practically not used in medicine. The reason is that pathogenic microorganisms have become immune to them. That is, the antibiotic does not act on bacteria properly; the desired result in treatment can only be achieved by administering a high dose of the drug. The drugs in this group include: Benzylpenicillin and Bicillin.

The drugs are available in powder form for injection. They effectively act on: anaerobic microorganisms, gram-positive bacteria, cocci, etc. Since the medications are of natural origin, they cannot boast of a long-term effect, injections are often given every 3-4 hours. This allows you not to reduce the concentration of the antibacterial agent in the blood.

Penicillin antibiotics of semi-synthetic origin are the result of modification of drugs produced from mold. It was possible to impart some properties to medications belonging to this group; first of all, they became insensitive to acid-base environments. This made it possible to produce antibiotics in tablets.

Medicines also appeared that acted on staphylococci. This class of drugs is different from natural antibiotics. But the improvements have significantly affected the quality of the drugs. They are poorly absorbed, do not have such a wide sector of action, and have contraindications.

Semi-synthetic drugs can be divided into:

Isoxazolepenicillins are a group of drugs that act on staphylococci; examples include the names of the following drugs: Oxacillin, Nafcillin.
Aminopenicillins - several drugs belong to this group. They have a wide sector of action, but are significantly inferior in strength to antibiotics of natural origin. But they can fight a large number of infections. Drugs from this group remain in the blood longer. Such antibiotics are often used to treat various diseases, for example two very well-known drugs: Ampicillin and Amoxicillin.

Attention! The list of medications is quite large; they have a number of indications and contraindications. For this reason, you should consult your doctor before starting antibiotics.

Antibiotics belonging to the penicillin group are prescribed by a doctor. It is recommended to take the drugs if you have:

Diseases of an infectious or bacterial nature (pneumonia, meningitis, etc.).
Respiratory tract infections.
Diseases of an inflammatory and bacterial nature of the genitourinary system (pyelonephritis).
Skin diseases of various origins (erysipelas, caused by staphylococcus).
Intestinal infections and many other diseases of an infectious, bacterial or inflammatory nature.

Information: Antibiotics are prescribed for extensive burns and deep wounds, gunshot or knife wounds.

In some cases, taking medications helps save a person's life. But you should not prescribe such drugs yourself, as this can lead to addiction.

What contraindications do medications have:

You should not take medications during pregnancy or lactation. The drugs may affect the growth and development of the child. They can change the quality of milk and its taste characteristics. There are a number of drugs that are conditionally approved for the treatment of pregnant women, but such an antibiotic must be prescribed by a doctor. Since only a doctor can determine the permissible dosage and duration of treatment.
The use of antibiotics from the groups of natural and synthetic penicillins for treatment is not recommended for the treatment of children. Drugs of these classes can have a toxic effect on the child's body. For this reason, medications are prescribed with caution, determining the optimal dosage.
You should not use medications without obvious indications. Use medications for a long period of time.

Direct contraindications for the use of antibiotics:

Individual intolerance to drugs of this class.
Tendency to allergic reactions of various kinds.

Attention! The main side effects of taking medications are long-term diarrhea and candidiasis. They are due to the fact that the drugs affect not only pathogenic microorganisms, but also beneficial microflora.

The penicillin series of antibiotics is distinguished by the presence of a small number of contraindications. For this reason, drugs in this class are prescribed very often. They help to quickly cope with the disease and return to a normal rhythm of life.

The latest generation of medicines have a wide spectrum of action. Such antibiotics do not have to be taken for a long time, they are well absorbed and, with adequate therapy, can “put a person back on his feet” in 3–5 days.

The question is which antibiotics are best? can be considered rhetorical. There are a number of drugs that doctors prescribe more often than others for one reason or another. In most cases, drug names are well known to the general public. But it’s still worth studying the list of medications:

Sumamed is a drug used to treat infectious diseases of the upper respiratory tract. The active ingredient is erythromycin. The medication is not used to treat patients with acute or chronic renal failure, and is not prescribed to children under 6 months of age. The main contraindication to the use of Sumamed should still be considered individual intolerance to the antibiotic.
Oxacillin is available in powder form. The powder is diluted, and then the solution is used for intramuscular injections. The main indication for the use of the drug is infections that are sensitive to this medicine. Hypersensitivity should be considered a contraindication to the use of Oxacillin.
Amoxicillin belongs to a number of synthetic antibiotics. The drug is quite well known; it is prescribed for sore throat, bronchitis and other respiratory tract infections. Amoxicillin can be taken for pyelonephritis (inflammation of the kidneys) and other diseases of the genitourinary system. The antibiotic is not prescribed to children under 3 years of age. Intolerance to the medication is also considered a direct contraindication.
Ampicillin - the full name of the medicine: Ampicillin trihydrate. Indications for the use of the drug should be considered infectious diseases of the respiratory tract (sore throat, bronchitis, pneumonia). The antibiotic is excreted from the body by the kidneys and liver; for this reason, Ampicillin is not prescribed to people with acute liver failure. Can be used to treat children.
Amoxiclav is a drug that has a combined composition. It is considered one of the latest generation antibiotics. Amoxiclav is used to treat infectious diseases of the respiratory system and genitourinary system. It is also used in gynecology. Contraindications to the use of the medication include hypersensitivity, jaundice, mononucleosis, etc.

List or list of penicillin antibiotics, which are available in powder form:

Benzylpenicillin novocaine salt is an antibiotic of natural origin. Indications for the use of the drug include severe infectious diseases, including congenital syphilis, abscesses of various etiologies, tetanus, anthrax and pneumonia. The medicine has practically no contraindications, but in modern medicine it is used extremely rarely.
Ampicillin is used to treat the following infectious diseases: sepsis (blood poisoning), whooping cough, endocarditis, meningitis, pneumonia, bronchitis. Ampicillin is not used to treat children or people with severe renal failure. Pregnancy can also be considered a direct contraindication to the use of this antibiotic.
Ospamox is prescribed for the treatment of diseases of the genitourinary system, gynecological and other infections. Prescribed in the postoperative period if there is a high risk of developing an inflammatory process. The antibiotic is not prescribed for severe infectious diseases of the gastrointestinal tract, in the presence of individual intolerance to the drug.

Important: Called an antibiotic, the drug must have an antibacterial effect on the body. All those medications that affect viruses have nothing to do with antibiotics.

Sumamed - cost varies from 300 to 500 rubles.

Amoxicillin tablets - price is about 159 rubles. per package.

Ampicillin trihydrate - cost of tablets is 20–30 rubles.

Ampicillin in powder form, intended for injection - 170 rubles.

Oxacillin - the average price for the drug varies from 40 to 60 rubles.

Amoxiclav - cost - 120 rubles.

Ospamox - price varies from 65 to 100 rubles.

Benzylpenicillin novocaine salt - 50 rub.

Benzylpenicillin - 30 rub.

Penicillin antibiotics are β-lactam antibiotics. β-lactam antibiotics β-lactams, which are united by the presence of a β-lactam ring in their structure, include penicillins, cephalosporins, carbapen

ems and monobactams that have a bactericidal effect. The similarity of the chemical structure determines, firstly, the same mechanism of action of all β-lactams - inhibition of penicillin-binding proteins (PBPs), enzymes involved in the process of bacterial cell wall synthesis (under conditions of PBP inhibition, this process is disrupted, which entails lysis of the bacterial cell) , and, secondly, cross-allergy to them in some patients.

It is important that the cellular structures of bacteria, which are the target of the action of β-lactams, are absent in mammals, therefore, specific toxicity towards the macroorganism is not typical for these antibiotics.

Penicillins, cephalosporins and monobactams are sensitive to the hydrolyzing action of special enzymes - β-lactamases, produced by many bacteria. Carbapenems are characterized by significantly higher resistance to β-lactamases.
Given their high clinical efficacy and low toxicity, β-lactam antibiotics have been the basis of antimicrobial chemotherapy for many years, occupying a leading place in the treatment of most bacterial infections.

Antibiotics of the penicillin group

Penicillins- the first antimicrobial drugs developed on the basis of biologically active substances produced by microorganisms. The ancestor of all penicillins, benzylpenicillin, was obtained in the early 40s. XX century. Its discovery marked a kind of revolutionary revolution in medicine, since, firstly, it transferred many bacterial infections from the category of inevitably lethal to potentially treatable, and secondly, it determined the fundamental direction on the basis of which many other antibacterial drugs were subsequently developed.

Currently, the group of penicillins includes more than ten antibiotics, which, depending on the sources of production, structural features and antimicrobial activity, are divided into several subgroups. At the same time, some antibiotics, primarily carboxypenicillins and ureidopenicillins, have lost their original meaning and are not used as single drugs.

General properties of penicillins

Antibacterial drugs from the penicillin group have the following properties:

They have a bactericidal effect.
They are well distributed in the body, penetrate into many organs, tissues and environments, with the exception of non-inflamed meninges, eyes, prostate, organs and tissues. Creates high concentrations in the lungs, kidneys, intestinal mucosa, reproductive organs, bones, pleural and peritoneal fluid.
In small quantities they pass through the placenta and enter breast milk.
They penetrate poorly through the BBB (with meningitis, permeability increases, and the concentration of penicillin in the cerebrospinal fluid is 5% of the serum level), the blood-ophthalmic barrier (BOB), and into the prostate gland.
They are excreted by the kidneys, mainly through active excretion by the renal tubules.
The half-life is 0.5 hours.
The therapeutic level in the blood remains within 4-6 hours.

Side effects of penicillin ov

Allergic reactions(according to various sources, in 1-10% of cases): urticaria; rash; Quincke's edema; fever; eosinophilia; bronchospasm.

The most dangerous is anaphylactic shock, causing up to 10% mortality (in the USA, about 75% of deaths from anaphylactic shock are caused by the administration of penicillin).

Local irritant effect with intramuscular injection (pain, infiltrates).

Neurotoxicity: convulsions, which are more often observed in children, when using very high doses of penicillin, in patients with renal failure, when administering more than 10 thousand units endolumbarally.

Electrolyte imbalance- in patients with heart failure, when large doses of sodium salt are administered, edema may increase, and in case of hypertension, blood pressure (BP) may increase (1 million units contains 2.0 mmol of sodium).

Sensitization. Please be aware that the degree of sensitization to penicillin may vary over time in some people. In 78% of them, skin tests become negative after 10 years. Therefore, the statement about penicillin allergy as a lifelong clinical diagnosis is incorrect.

Prevention measures

Careful history taking, use of freshly prepared penicillin solutions, observation of the patient for 30 minutes after the first administration of penicillin, detection of hypersensitivity by skin testing.

Measures to help with the development of anaphylactic shock: ensuring airway patency (intubation if necessary), oxygen therapy, adrenaline, glucocorticoids.

It should be noted that with bronchial asthma and other allergic diseases, the risk of developing allergic reactions to penicillins (as well as to other antibiotics) is somewhat increased, and if they occur, they can be more severe. However, the prevailing point of view that penicillins should not be prescribed to persons with allergic diseases is erroneous.

Indications for the use of penicillins

Infections caused by GABHS: tonsillopharyngitis, erysipelas, scarlet fever, acute rheumatic fever.
Meningitis in children over 2 years of age and in adults.
Infectious endocarditis (necessarily in combination with gentamicin or streptomycin).
Syphilis.
Leptospirosis.
Anthrax.
Anaerobic infections: gas gangrene, tetanus.
Actinomycosis.

Natural penicillin preparations

Natural penicillin preparations include the following:

Phenoxymethylpenicillin

A natural penicillin preparation intended for oral administration.
The spectrum of activity is practically no different from penicillin. Compared to penicillin, it is more acid-resistant. Bioavailability is 40-60% (slightly higher when taken on an empty stomach).

The drug does not create high concentrations in the blood: taking 0.5 g of phenoxymethylpenicillin orally approximately corresponds to administering 300 thousand units of penicillin intramuscularly. The half-life is about 1 hour.

Side effects

Allergic reactions.
Gastrointestinal tract (GIT) - pain or discomfort in the abdomen, nausea; less often vomiting, diarrhea.

Indications for use

Prevention of pneumococcal infections in persons after splenectomy.

Benzathine phenoxymethylpenicillin

A derivative of phenoxymethylpenicillin. Compared to it, it is more stable in the gastrointestinal tract, absorbed faster, and better tolerated. Bioavailability is independent of food.

Indications for use

Streptococcal (GABHS) infections of mild to moderate severity: tonsillopharyngitis, skin and soft tissue infections.

Long-acting penicillin preparations

Long-acting penicillin preparations, or so-called depot penicillins, include b enzylpenicillin novocaine salt And benzathine benzyl penicillin, as well as combination drugs created on their basis.

Side effects long-acting penicillin preparations

Allergic reactions.
Pain, infiltrates at the injection site.
She (Hoigne) syndrome is ischemia and gangrene of the extremities due to accidental injection into an artery.
Nicholau syndrome is an embolism of the blood vessels of the lungs and brain when injected into a vein.

Prevention of vascular complications: strict adherence to the insertion technique - intramuscularly into the upper outer quadrant of the buttock using a wide needle, with the patient in a horizontal position. Before insertion, it is necessary to pull the syringe plunger towards you to make sure that the needle is not in the vessel.

Indications for use

Infections caused by microorganisms highly sensitive to penicillin: streptococcal (GABHS) tonsillopharyngitis; syphilis (except neurosyphilis).
Prevention of anthrax after contact with spores (benzylpenicillin novocaine salt).
Year-round prevention of rheumatic fever.
Prevention of diphtheria, streptococcal cellulitis.

Benzylpenicillin novocaine salt

With intramuscular administration, the therapeutic concentration in the blood is maintained for 12-24 hours, but it is lower than with the introduction of an equivalent dose of benzylpenicillin sodium salt. The half-life is 6 hours.

It has a local anesthetic effect and is contraindicated if you are allergic to procaine (Novocaine). In case of overdose, mental disorders are possible.

Benzathine Benzylpenicillin

It acts longer than benzylpenicillin novocaine salt, up to 3-4 weeks. After intramuscular administration, peak concentrations are observed after 24 hours in children and after 48 hours in adults. The half-life is several days.

Pharmacokinetic studies of domestic preparations of benzathine benzylpenicillin, conducted at the State Scientific Center for Antibiotics, showed that when used, the therapeutic concentration in the blood serum is maintained for no more than 14 days, which requires their more frequent administration than the foreign analogue, Retarpen.

Combination drugs penicillins

Bicillin-3, Bicillin-5.

Isoxazolylpenicillins (antistaphylococcal penicillins)

Isoxazolylpenicillin drug – Oxacillin.

The first isoxazolylpenicillin with antistaphylococcal activity was methicillin, which was later discontinued due to lack of advantages over newer analogues and nephrotoxicity.

Currently, the main drug of this group in Russia is oxacillin. Nafcillin, cloxacillin, dicloxacillin and flucloxacillin are also used abroad.

Oxacillin

Activity spectrum
Oxacillin is resistant to penicillinase, which is produced by more than 90% of S. aureus strains. Therefore, they are active against penicillin-resistant S. aureus (PRSA) and a number of strains of S. epidermidis resistant to natural penicillins, amino-, carboxy- and ureidopenicillins. This is the main clinical significance of this drug.

At the same time, oxacillin is significantly less active against streptococci (including S. pneumoniae). It has virtually no effect on most other penicillin-sensitive microorganisms, including gonococci and enterococci.

One of the serious problems is the spread of strains (especially nosocomial) of S. aureus that are resistant to isoxazolylpenicillins and, based on the name of the first of them, received the abbreviation MRSA (raeticillin-resistant S. aureus). In fact, they are multidrug-resistant, since they are resistant not only to all penicillins, but also to cephalosporins, macrolides, tetracyclines, lincosamides, carbapenems, fluoroquinolones and other antibiotics.

Side effects

Allergic reactions.
Gastrointestinal tract - abdominal pain, nausea, vomiting, diarrhea.
Moderate hepatotoxicity - increased activity of liver transaminases, especially when administered in high doses (more than 6 g/day); As a rule, it is asymptomatic, but can sometimes be accompanied by fever, nausea, vomiting, and eosinophilia (liver biopsy shows signs of nonspecific hepatitis).
Decreased hemoglobin level, neutropenia.
Transient hematuria in children.

Indications for use

Confirmed or suspected staphylococcal infections of various localizations (with sensitivity to oxacillin or a slight risk of spreading methicillin resistance):

bone and joint infections;
pneumonia;
infective endocarditis;
meningitis;
sepsis.

Aminopenicillins

Aminopencillins include ampicillin And amoxicillin. Compared to natural penicillins and isoxazolylpenicillins their antimicrobial spectrum is expanded to include some gram-negative bacteria of the family Enterobacteriaceae and H. influenzae.

Ampicillin

Differences from penicillin in the spectrum of antibacterial activity

It acts on a number of gram(-) bacteria: E. coli, P. mirabilis, salmonella, shigella (the latter are resistant in many cases), N. influenzae (strains that do not produce β-lactamases).
More active against enterococci (E. faecalis) and listeria.
Slightly less active against streptococci (GABHS, S. pneumoniae), spirochetes, and anaerobes.

Ampicillin has no effect on gram-negative pathogens of nosocomial infections, such as Pseudomonas aeruginosa (P. aeruginosa), Klebsiella, Serration, Enterobacter, Acinetobacter, etc.

It is destroyed by staphylococcal penicillinase, therefore inactive against most staphylococci.

Side effects

Allergic reactions.
Gastrointestinal disorders - abdominal pain, nausea, vomiting, most often diarrhea.
“Ampicillin” rash (in 5-10% of patients), according to most experts, is not associated with an allergy to penicillin.

The rash is maculopapular in nature, is not accompanied by itching and may go away without stopping the drug. Risk factors: infectious mononucleosis (rash occurs in 75-100% of cases), cytomegaly, chronic lymphocytic leukemia.

Indications for use

Acute bacterial infections of the upper respiratory tract (otitis media, rhinosinusitis - if necessary, parenteral administration).
Community-acquired pneumonia (if parenteral administration is necessary).
Urinary tract infections (UTI) - cystitis, pyelonephritis (not recommended for empirical therapy due to the high level of pathogen resistance).
Intestinal infections (salmonellosis, shigellosis).
Meningitis.
Infectious endocarditis.
Leptospirosis.

Warnings and precautions

Ampicillin can only be dissolved in water for injection or 0.9% sodium chloride solution. Freshly prepared solutions must be used. When stored for more than 1 hour, the activity of the drug sharply decreases.

Amoxicillin

It is an ampicillin derivative with improved pharmacokinetics.

According to the antimicrobial spectrum, amoxicillin is close to ampicillin (the microflora exhibits cross-resistance to both drugs).

amoxicillin is the most active among all oral penicillins and cephalosporins against S. pneumoniae, including pneumococci with intermediate levels of resistance to penicillin;
has a slightly stronger effect on E. faecalis than ampicillin;
clinically ineffective against Salmonella and Shigella, regardless of the results of in vitro susceptibility testing;
highly active in vitro and in vivo against H. pylori.

Similar to ampicillin, amoxicillin is destroyed by β-lactamases.

Side effects

Allergic reactions.
"Ampicillin" rash.
Gastrointestinal tract - mostly moderate abdominal discomfort, nausea; diarrhea is observed much less frequently than when using ampicillin.

Indications for use

Upper respiratory tract infections - acute otitis media, acute rhinosinusitis.
Lower respiratory tract infections - exacerbation of chronic obstructive pulmonary disease (COPD), community-acquired pneumonia.
Urinary tract infections - cystitis, pyelonephritis (not recommended for empirical therapy due to the high level of pathogen resistance).
Eradication of H. pylori (in combination with antisecretory drugs and other antibiotics).
Tick-borne borreliosis (Lyme disease).
Prevention of infective endocarditis.
Prevention of anthrax (in pregnant women and children).

Warnings

Cannot be used in the treatment of shigellosis and salmonellosis.
Amoxicillin preparations - Ampicillin-AKOS, Ampicillin-Ferein, Ampicillin sodium salt, Amoxicillin, Amoxicillin Sandoz, Amosin, Ospamox, Flemoxin Solutab, Hiconcil.

Carboxypenicillins

Carboxypenicillins include carbenicillin (discontinued and no longer in use) and ticarcillin (part of the ticarcillin/clavulanate combination drug).

Their main advantage for a long time was their activity against P. aeruginosa, as well as some gram-negative bacteria resistant to aminopenicillins (Enterobacter, Proteus, Morganella, etc.). However, to date, carboxypenicillins have practically lost their “anti-pseudomonas” value due to the high level of resistance of Pseudomonas aeruginosa and many other microorganisms to them, as well as poor tolerability.

They have the greatest neurotoxicity among penicillins; they can cause platelet aggregation disorders, thrombocytopenia, and electrolyte imbalances - hypernatremia, hypokalemia.

Ureidopenicillins

Ureidopenicillins include azlocillin (not currently used) and piperacillin (used as part of the combination drug piperacillin + tazobactam. Compared to carboxypenicillins, they have a wider antimicrobial spectrum and are somewhat better tolerated.

Initially, they were more active than carboxypenicillins against P. aeruginosa, but currently most strains of Pseudomonas aeruginosa are resistant to ureidopenicillins.

Inhibitor-protected penicillins

The main mechanism for the development of bacterial resistance to β-lactam antibiotics is their production of special enzymes, β-lactamases, which destroy the β-lactam ring - the most important structural element of these drugs, ensuring their bactericidal effect. This protective mechanism turns out to be one of the leading ones for such clinically important pathogens as S. aureus, H. influenzae, M. catarrhalis, K. pneumoniae, B. fragilis, and many others.

Taking a simplified approach to the systematization of β-lactamases produced by microorganisms, they can be divided into several types, depending on the direction of action:

1) penicillinases that destroy penicillins;

2) cephalosporinases that destroy cephalosporins of the I-II generations;

3) extended spectrum β-lactamases (ESBLs), combining the properties of the first two types and, in addition, destroying cephalosporins of the III and IV generations;

4) metallo-β-lactamases, which destroy almost all β-lactams (except monobactams).

In order to overcome this mechanism of resistance, compounds that inactivate β-lactamases were obtained: clavulanic acid (clavulanate), sulbactam and tazobactam.

On this basis, combination preparations have been created containing a penicillin antibiotic (ampicillin, amoxicillin, piperacillin, ticarcillin) and one of the β-lactamase inhibitors.

Such drugs are called inhibitor-protected penicillins.

As a result of the combination of penicillins with β-lactamase inhibitors, the natural (primary) activity of penicillins against many staphylococci (except MRSA), gram-negative bacteria, non-spore-forming anaerobes is restored, and their antimicrobial spectrum is expanded due to a number of gram-negative bacteria (Klebsiella, etc.) with natural resistance to penicillins.

It should be emphasized that β-lactamase inhibitors overcome only one of the bacterial resistance mechanisms. Therefore, for example, tazobactam cannot increase the sensitivity of P. aeruginosa to piperacillin, since resistance in this case is caused by a decrease in the permeability of the outer membrane of the microbial cell to β-lactams.

Amoxicillin+clavulanate

The drug consists of amoxicillin and potassium clavulanate. The ratio of components in preparations for oral administration ranges from 2:1, 4:1 and 8:1, and for parenteral administration - 5:1. Clavulanic acid, used as a potassium salt, is one of the most powerful inhibitors of microbial β-lactamases. Therefore, amoxicillin in combination with clavulanate is not destroyed by β-lactamases, which significantly expands the spectrum of its activity.

Spectrum of antibacterial activity

Amoxicillin + clavulanate acts on all microorganisms sensitive to amoxicillin. Additionally, unlike amoxicillin:

has higher antistaphylococcal activity: acts on PRSA and some strains of S. epidermidis;
acts on enterococci producing (3-lactamases;
active against gram(-) flora producing (3-lactamase (N. influ enzae, M. catarrhalis, N. gonorrhoeae, E. coli, Proteus spp., Klebsiella spp., etc.), except for ESBL producers;
has high antianaerobic activity (including B. fragilis).
Does not affect gram(-) bacteria resistant to aminopenicillins: P. aeruginosa, Enterobacter, Citrobacter, Serration, Providence, Morganella.

Side effects

Like Amoxicillin. In addition, due to the presence of clavulanate, in rare cases (usually in older people), hepatotoxic reactions (increased transaminase activity, fever, nausea, vomiting) are possible.

Indications for use

Bacterial infections of the upper respiratory tract (acute and chronic rhinosinusitis, acute otitis media, epiglottitis).
Bacterial infections of the lower respiratory tract (exacerbation of COPD, community-acquired pneumonia).
Biliary tract infections (acute cholecystitis, cholangitis).
Urinary tract infections (acute pyelonephritis, cystitis).
Intra-abdominal infections.
Infections of the pelvic organs.
Bone and joint infections.

Amoxicillin+sulbactam

The drug consists of amoxicillin and sulbactam in ratios of 1:1 and 5:1 for oral administration and 2:1 for parenteral administration.
The spectrum of activity is close to amoxicillin + clavulanate. Sulbactam, in addition to inhibiting β-lactamases, exhibits moderate activity against Neisseria spp., M. catarrhalis, Acinetobacter spp.
Side effects

Same as Amoxicillin.

Indications for use

UTI infections (acute pyelonephritis, cystitis).
Intra-abdominal infections.
Infections of the pelvic organs.
Skin and soft tissue infections (including wound infections after bites).
Bone and joint infections.
Perioperative antibiotic prophylaxis.

Ampicillin+sulbactam

The drug consists of ampicillin and sulbactam in a ratio of 2:1. The prodrug sultamicillin, which is a compound of ampicillin and sulbactam, is intended for oral administration. During absorption, hydrolysis of sultamicillin occurs, and the bioavailability of ampicillin and sulbactam exceeds that when taking an equivalent dose of regular ampicillin.

Ampicillin + sulbactam is similar in most parameters to amoxicillin + clavulanate and amoxicillin + sulbactam.

Indications for use

Bacterial infections of the upper respiratory tract (acute and chronic rhinosinusitis, acute otitis media, epiglottitis).
Bacterial infections of the respiratory tract (exacerbation of COPD, community-acquired pneumonia).
Infections of the gallbladder (acute cholecystitis, cholangitis).
Infections of the bladder (acute pyelonephritis, cystitis).
Intra-abdominal infections.
Infections of the pelvic organs.
Skin and soft tissue infections (including wound infections after bites).
Bone and joint infections.
Perioperative antibiotic prophylaxis.

It has an advantage over amoxicillin + clavulanate for infections caused by Acinetobacter.

Warning

When administered intramuscularly, the drug should be diluted with a 1% lidocaine solution.

Ticarcillin+clavulanate

A combination of carboxypenicillin ticarcillin with clavulanate in a ratio of 30:1. Unlike inhibitor-protected aminopenicillins, it acts on P. aeruginosa (but many strains are resistant) and surpasses them in activity against nosocomial strains of enterobacteria.

Gram-positive cocci: staphylococci (including PRSA), streptococci, enterococci (but inferior in activity to inhibitor-protected aminopenicillins).
Gram-negative rods: representatives of the family Enterobacteriaceae (E. coli, Klebsiella spp., Proteus spp., Enterobacter spp., Serratia spp., C. diversus, etc.); P. aeruginosa (but not superior to ticarcillin); non-fermenting bacteria - S. maltophilia (superior to other β-lactams in activity).
Anaerobes: spore-forming and non-spore-forming, including B. fragilis.

Side effects

Allergic reactions.
Neurotoxicity (tremor, seizures).
Electrolyte disturbances (hypernatremia, hypokalemia - especially in patients with heart failure).
Impaired platelet aggregation.

Indications for use

Severe, predominantly nosocomial infections of various locations:

intra-abdominal infections;
pelvic organ infections;
skin and soft tissue infections;
bone and joint infections;
sepsis.

Piperacillin+tazobactam

Combination of ureidopenicillin piperacillin with tazobactam in a ratio of 8:1. Tazobactam is superior to sulbactam in terms of β-lactamase inhibition and is approximately equivalent to clavulanate. Piperacillin + tazobactam is considered the most powerful inhibitor-protected penicillin.

Spectrum of antibacterial activity

Gram-positive cocci: staphylococci (including PRSA), streptococci, enterococci.
Gram-negative rods: representatives of the family Enterobacteriaceae (E. coli, Klebsiella spp., Proteus spp., Enterobacter spp., Serratia spp., C. diversus, etc.); P. aeruginosa (but not superior to piperacillin); non-fermenting bacteria - S. maltophilia.
Anaerobes: spore-forming and non-spore-forming, including B. fra-ilis.

Side effects

The same as Ticarcillin + clavulanate.

Indications for use

Severe, predominantly nosocomial infections of various localizations caused by multidrug-resistant and mixed (aerobic-anaerobic) microflora:

lower respiratory tract infections (pneumonia, lung abscess, pleural empyema);
complicated urinary tract infections;
intra-abdominal infections;
pelvic organ infections;
skin and soft tissue infections;
bone and joint infections;
sepsis.

Preparations of inhibitor-protected penicillins

(Amoxicillin + clavulanate) - Amovycombe, Amoxiclav, Amoxivan, Arlet, Augmentin, Bactoclav, Betaclave, Verclave, Klamosar, Medoclav, Panclave 2X, Rapiclav, Fibell, Flemoclav Solutab, Foraclave, Ecoclave.

(Amoxicillin + sulbactam) - Trifamox IBL, Trifamox IBL DUO.

(Ampicillin+sulbactam)— Ampisid, Libaccil, Sultasin.

(Ticarcillin + clavulanate) – Timentin.

(Piperacillin + tazobactam) - Santaz, Tazocin, Tazrobida, Tacillin J.