Soft dosage forms of liniments. The positive qualities are
Soft dosage forms include ointments (and their varieties: creams and gels), pastes, liquid ointments, suppositories.
OINTMENTS
Ointment- a dosage form for application to the skin, wound surfaces, mucous membranes, obtained by mixing one or more medicinal substances with the so-called ointment bases.
Singular Nominative unguentum, Genitive Unguenti(Ung.).
As ointment bases Vaseline is most often used - white or yellow ( Vaselinum albums. flavum), lanolin ( Lanolinum), lard ( Adeps Suillus s. Axungia porcina), fat-like oils, beeswax, spermaceti, polyethylene glycols, and other substances that have a soft consistency. The amount of ointment prescribed depends on the method of application. Eye ointments are prescribed in the amount of 5.0 - 10.0; ointments for lips, nose, ears in the amount of 10.0 - 20.0; for lubrication of affected areas of the skin - from 15.0 to 100.0 or more.
When prescribing ointments in the main prescription, the medicinal substance that is part of the ointment and the ointment base are indicated. In ointments of powdered substances should be no more than 25%.
An ointment consisting of one medicinal substance and an ointment base is called simple ointment. If petroleum jelly is used as an ointment base (the most common option), then such an ointment can be prescribed in an abbreviated form. The recipe starts with Ung. (ointment).
The drug concentration is indicated as a percentage.
RECIPE EXAMPLE
write out
50.0 ointment containing 2% salicylic acid ( salicylicum acid)
Apply to affected areas of the skin
Rp: Ung. acidi Salicylici 2% - 50.0
D.S. Apply to affected areas of the skin.
A simple ointment cannot be prescribed in an abbreviated form in cases where: the ointment base is not vaseline, but other substances (or a mixture thereof); the ointment contains substances whose activity is expressed in units of action ( ED), in this case use expanded form prescription.
RECIPES EXAMPLES
write out
50.0 ointment containing 750,000 units of mycoheptin ( mycoheptinum). Assign to lubricate the affected areas of the skin 2 times a day.
Rp: Mycoheptini 750000 ED
Vaseline ad 50.0
M.f. ung.
D.S. Lubricate the affected areas of the skin 2 times a day.
write out
30.0 ointment containing 5.0 potassium iodide ( Kalii iodidum) and lanolin ( Lanolinum). Spread on the nail plates to soften them
Rp: Kalii iodidi 5.0
Lanolini ad 30.0
M.f. ung.
D.S. Apply on nails
to soften them.
If the composition of the ointment includes several medicinal substances, then such an ointment is called difficult. The ointment is also complex, which includes one medicinal substance and a mixture of ointment bases (vaseline and lanolin).
A complex ointment can only be written out in a detailed prescription - it is necessary to indicate the weight quantities of both medicinal substances and the ointment base. The recipe ends with a sentence M.f. ung. (Misce fiat unguentum - « Mix to make an ointment»).
RECIPE EXAMPLE
write out
100.0 ointment containing 10% ichthyol ( Ichthyolum), vaseline and lanolin in equal amounts. Apply to affected areas of the skin.
Rp: Ichthyoli 10.0
Vselini
Lanolini ana ad 100.0
M.f. ung.
D.S. Apply to affected areas of the skin 3 times a day.
day.
Currently, most simple and complex ointments are produced by the pharmaceutical industry in finished form. Such ointments are official and are issued only in abbreviated form without indicating their full composition and, in some cases, concentration. In this case, the prescription begins with the word unguentum in the genitive singular ( Unguenti ).
RECIPE EXAMPLE
write out
25.0 ointment Triderm ( Triderm). Apply to affected areas of the skin.
Rp: Ung. Triderm 25.0
D.S. Apply to the affected areas of the skin.
write out
20.0 ointment Finalgon (finalgon). Apply 3 times a day to the area of the affected joint.
Rp.: Ung. Finalgon 20.0
D.S. Apply 3 times a day to the area
the affected joint.
Creams And gels are a type of ointment. Therefore, the abbreviated prescription for these dosage forms begins with the word Unguenti , then in parentheses indicate the consistency ( Gel, Creame ).
Cream (creame ) - ointment of soft consistency, which is an oil-in-water or water-in-oil emulsion. The content of powdered substances in creams in accordance with regulatory requirements should be no more than 5%.
Gel (Gel ) is a colloidal solution of jelly-like consistency, capable of retaining its shape and possessing elasticity and plasticity.
RECIPE EXAMPLE
write out
20.0 5% official ointment (cream) Acyclovir ( Acyclovir). Apply to affected areas.
Rp: Ung. (creame) Acyclovir 5% - 20.0
D.S. Apply to affected areas.
write out
40.0 2% ointment (gel) Troxevasin ( Troxevasin). Apply to the skin of the lower extremities with superficial thrombophlebitis.
Rp: Ung. (gel) "Troxevasin" 2% - 40.0
D.S. Apply to the skin of the lower extremities
superficial thrombophlebitis.
PASTES
Pastes- these are varieties of ointments in which the amount of powdered substances contains from 25% to 65%, as a result, the pastes have a thicker consistency and, when applied to the skin, can remain at the site of application for a longer time.
Singular nominative Pasta, singular genitive Pastae (Past).
The therapeutic advantage of pastes over ointments is that they have a more pronounced adsorbing and drying ability, which is useful in the presence of effusions. If the amount of the medicinal substance included in the paste is less than 25%, then any indifferent powdered products are added to give the required consistency. substances (most often starch - Amylum, talc - Talcum,
zinc oxide - Zinci oxydum, white clay - Bolus alba and etc.)
Official pastes are prescribed in prescriptions similarly to official ointments.
RECIPES EXAMPLES
write out
25.0 official zinc paste ( Pasta Zinci). Assign for application to the affected areas of the skin.
Rp: past. Zinci 25.0
D.S. Apply to affected areas of the skin.
write out
107.0 paste containing 2.0 boric acid ( Acidum boricum); 5.0 Naftalan ( Naphthalanum) and equally 25.0 zinc oxide ( Zincum oxydum), talc ( Talcum), vaseline ( Vaselinum), lanolin ( Lanolinum). Apply to the affected areas of the skin.
Rp: Acidi borici 2.0
Naphthalani 5.0
Zinci oxydi
Vasellini
Lanolini ana 25.0
M.f. past.
D.S. Apply to the affected areas of the skin.
write out
20.0 paste containing 5% anesthesin ( Anaesthesinum). Lubricate the affected areas.
Rp: Anaesthesini 1.0
Zinci oxydi
Amyli ana 5.0
Vaselli ad 20.0
M.f. past.
D.S. Lubricate the affected areas of the skin.
LIQUID OINTMENTS (LINIMENTS ).
Liniments- a dosage form for external use, which is a thick liquid or gelatinous mass that melts at body temperature.
Soft dosage forms include ointments, creams, pastes, suppositories and patches. Fats and fat-like substances obtained from oil, synthetic polymers are used as forming bases.
Ointments (Unguenta, Ung.)- soft dosage form of a viscous consistency, used for external use and containing less than 25% dry (powder) substances.
Ointments are obtained by mixing various medicinal substances (basis) with shaping substances (constituens), called ointment bases. As ointment bases, substances or mixtures of substances with high smearing ability are usually used, which mix well, but do not react with medicinal substances and do not change their property under the influence of light and air. Certain petroleum products (vaseline, vaseline oil), animal fats (purified pork fat), fat-like substances, waxes (lanolin, beeswax, spermaceti) and synthetic substances meet these requirements to varying degrees. Ointments are non-dosed lek. forms, therefore, in prescriptions they are prescribed in total. Only when prescribing substances for resorptive action in ointments, ointments should be prescribed in doses (single doses). There are simple and complex ointments. Simple - comp. from 2 ingredients: one active and one shaping in-va. Complex - are part of more than 2 ingredients.
Pastes (Pastae, Past.)- these varieties of ointments contain at least 25% dry matter, not more than 60-65%, at body temperature the pastes soften. Pastes last longer than ointments at the site of application. Due to the higher content of powdery substances, pastes, unlike ointments, have pronounced adsorbing and drying properties.
Pastes are among the non-dosed dosage forms, so they are prescribed in total. Trunk pastes are prescribed only in expanded form, indicating all the ingredients and their quantities. The recipe ends with the prescription: M.f. pasta (Misce ut fiat pasta. - Mix to form a paste).
If the amount of powdered substances in the paste is less than 25%, one or more indifferent powders are added, such as starch (Amylum), zinc oxide (Zinci oxydum), white clay (Bolus alba), etc.
Candles (suppositories, Suppositoria, Supp.) -
dosage forms that are solid at room temperature and melt or dissolve at body temperature. There are rectal suppositories (candles) - suppositoria rectalia, vaginal - suppositoria vaginalia and bacilli (GPC). Substances are used as constituens for the preparation of suppositories
dense consistency, which melt at body temperature (not higher than 37 ° C), do not have irritating properties, are poorly absorbed through the mucous membranes, do not enter into chemical interaction with medicinal substances.
The most suitable bases for suppositories are cocoa butter and Japanese cinnamon fat. In addition, gelatin-glycerin bases (a mixture of gelatin, glycerin and water) and soap-glycerin bases (an alloy of medical soap and glycerin) have received wide application in the production of candles.
Medicinal substances in suppositories are used for local, and in rectal suppositories - for resorptive action. In this regard, when prescribing toxic and potent substances in rectal suppositories, it is necessary to follow the same rules about higher doses as for oral dosage forms.
Rectal suppositories usually have the shape of a cone or cylinder with a pointed end. Their mass ranges from 1.1 to 4.0 g1. The maximum allowable diameter is 1.5 cm. If the mass of rectal suppositories is not indicated in the recipe, then they are made with a mass of 3.0 g.
Vaginal suppositories in shape they can be spherical (balls - globuli), ovoid (ovuli - ovula) or in the form of a flat body with a rounded end (pessaries - pessaria) The mass of vaginal suppositories is from 1.5 to 6.0 g. indicated, they are usually made with a mass of 4.0 g.
Currently, most suppositories are produced in finished form by the pharmaceutical industry.
Suppositories produced by the pharmaceutical industry, like all other official dosage forms, are prescribed using an abbreviated prescription form. In this case, the prescription begins with an indication of the dosage form - Suppositorium ... (Suppository ... - wine. p. units. h.). Further, after the preposition cum (c), the name of the medicinal substance (in TV units) and its dose follow. The prescription ends with the prescription D.t.d.N. and signature.
Plasters (Emplastra) is a dosage form in the form of a plastic mass that has the ability to soften at body temperature and adhere to the skin, or in the form of the same mass on a flat carrier. Use patches for external use.
According to the aggregation state, solid and liquid patches are distinguished.
Hard patches are firm at room temperature and soften at body temperature.
Liquid patches (skin adhesives) are volatile liquids that leave a film on the skin after evaporation of the solvent.
Most of the plasters used in modern medical practice are manufactured by the pharmaceutical industry.
Solid plasters are produced either smeared on fabric or in the form of conical and cylindrical blocks. Depending on this, among solid plasters one should distinguish between smeared and non-smeared.
Liquid patches are available in bottles and vials. In recent years, some liquid patches have been released in aerosol cans.
When prescribing patches, they use abbreviated writing. In the recipes for smeared plasters, an indication of their size is made. Non-smeared and liquid patches are prescribed in total (not divided into individual doses).
Alpha-blockers, classification, mechanism of action, pharmacodynamics, comparative characteristics of drugs (phentolamine, dihydroergotoxin, nicergoline, doxazosin). Indications for use, side effects, contraindications.
The presence of substances α-adrenergic blocking effect is easily detected by their ability to reduce the pressor action of adrenaline or pervert it. The latter is manifested in the fact that against the background of the action of α-blockers, adrenaline does not increase blood pressure, but reduces it. This is due to the fact that against the background of the block of α-adrenergic receptors, the effect of the stimulating effect of adrenaline on the β-adrenergic receptors of the vessels is manifested, which is accompanied by their expansion (the tone of smooth muscles decreases). Synthetic drugs that block α1- and α2-adrenergic receptors include phentolamine and tropafen.
Phentolamine (Regitin) is a derivative of imidazoline. It is characterized by a pronounced, but short-term α-adrenergic blocking effect (10-15 minutes when administered intravenously). Reduces blood pressure, due to its α-adrenergic blocking and myotropic antispasmodic action. Causes tachycardia (partly due to the block of presynaptic α2-adrenergic receptors). Increases the motility of the gastrointestinal tract, increases the secretion of the glands of the stomach.
Fentolamine has almost no effect on the hyperglycemic effect of adrenaline. It is poorly absorbed from the gastrointestinal tract. Phentolamine and its metabolites are excreted by the kidneys.
Tropafen refers to tropine esters. It combines a fairly high α-blocking activity and some atropine-like properties, and therefore causes a decrease in blood pressure and tachycardia. Tropafen is an antagonist of α-agonists. It has a rather long α-adrenergic blocking effect (measured in hours) and is superior in this respect to phentolamine and dihydrated ergot alkaloids.
Semi-synthetic drugs include dihydrated ergot alkaloids - dihydroergotoxin And dihydroergotamine.
Dihydrated ergot alkaloids differ from natural ones in a more pronounced α-adrenergic blocking effect, the absence of a stimulating effect on the myometrium (non-pregnant uterus), less vasoconstrictive action and lower toxicity.
In medical practice, drugs that block α1- and α2-adrenergic receptors are used relatively rarely. The most important effect of a-blockers is the expansion of peripheral vessels. This is related to their use in various disorders of the peripheral circulation (endarteritis, Raynaud's disease, etc.), including shock (hemorrhagic, cardiogenic), for which arteriole spasm is typical. It is natural to prescribe a-blockers for pheochromocytoma1. Sometimes a-blockers are used for hypertensive crises.
The considered drugs block both post- and presynaptic α-adrenergic receptors (α 1 and α2). It should be borne in mind that the block of presynaptic a2-adrenergic receptors disrupts the physiological autoregulation of the release of the norepinephrine mediator. As a result of a violation of negative feedback, its excessive release occurs, which contributes to the restoration of adrenergic transmission. The latter explains the insufficient stability of the block of postsynaptic α1-adrenergic receptors when using non-selective antagonists (blockers of α1- and α2-adrenergic receptors). Severe tachycardia is also the result of an increased release of norepinephrine. From this point of view, adrenergic blockers acting mainly on postsynaptic α1-adrenergic receptors are more interesting for practical medicine. Thanks to the functioning presynaptic α2-adrenergic receptors, the negative feedback mechanism is preserved and, therefore, increased release of norepinephrine does not occur. In this case, the block of postsynaptic α1-adrenergic receptors becomes longer. In addition, there is no pronounced tachycardia
Drugs with a predominant effect on postsynaptic α1-adrenergic receptors include prazosin. In terms of α1-adrenergic blocking activity, it exceeds phentolamine by about 10 times. The main effect of prazosin is to lower blood pressure. This effect is due to a decrease in the tone of arterial and, to a lesser extent, venous vessels, a decrease in venous return and heart function. The heart rate changes little (possible slight tachycardia). There is evidence of an inhibitory effect of prazosin on phosphodiesterase.
The drug is effective when administered orally. Its action occurs in 30-60 minutes and lasts for 6-8 hours.
Prazosin is used as an antihypertensive agent; appoint usually inside.
α1-Adrenergic blockers ( tamsulosin, terazosin, alfuzosin etc.) are also used for benign prostatic hyperplasia. The predominant effect on α1A-adrenergic receptors of the prostate gland is tamsulosin (omnic). Unlike other α1-blockers, tamsulosin only slightly affects systemic hemodynamics.
The following varieties of α1-adrenergic receptors are known: α1Α, α1Β and α1D1. α1A-adrenergic receptors are involved in the regulation of prostate smooth muscle contractions, and α1Β - vascular smooth muscle contractions. Of the total number of α1-adrenergic receptors in the human prostate gland, 70% belong to the α1Α subtype. The affinity of tamsulosin for the latter is 7-38 times greater than for α1B-adrenergic receptors. Blockade of α1A-adrenergic receptors reduces the tone of the smooth muscles of the prostate, bladder neck and prostatic urethra. This leads to an increase in the rate of urine flow and, in general, to an improvement in its outflow from the bladder.
Tamsulosin taken orally once a day. Absorbed almost completely. Metabolized in the liver. The drug and metabolites are excreted by the kidneys (only 10% unchanged). t1 / 2 = 12-19 hours. Side effects may include dizziness, impaired ejaculation, headache, palpitations, etc.
Of the α1-blockers for the treatment of prostatic hyperplasia, it is successfully used doxazosin(cardura, tonocardin), acting longer than other drugs in this group. The total duration of action of doxazosin may exceed 36 hours. It does not have a selective effect on individual subtypes of α1-adrenergic receptors.
By main location helminths in the human body distinguish between intestinal and extraintestinal helminthiases, the causative agents of which can be roundworms (nematodes), as well as flatworms - tapeworms (cestodes) and flukes (trematodes).
According to the mechanism of action antihelminthics are divided into a number of groups:
1) cell poisons
Ethylene tetrachloride
2) drugs that disrupt the function of the neuromuscular system in roundworms:
Pyrantela pamoate,
piperazine and its salts,
Ditrazine,
Levamisole,
Naftamon
3) drugs that paralyze the neuromuscular system mainly in flatworms and destroy their integumentary tissues:
Praziquantel,
Fenasal,
Bitionol,
4) means acting mainly on the energy processes of helminths
Aminoakrikhin,
pirvinia pamoate,
Levamisole,
mebendazole
With intestinal nematodosis - ascariasis- the main drugs are mebendazole (vermox), pyrantel pamoate, levamisole (decaris).
Imidazole derivative mebendazole has a depressing effect on most round helminths (especially active in trichuriasis, ascariasis and enterobiasis). Suppresses the utilization of glucose by helminths and paralyzes them. It has a detrimental effect on the eggs of whipworm, roundworm and hookworm. Absorbed from the intestines poorly (10%). Nevertheless, in large doses it can be used to treat extraintestinal helminthiases - trichinosis and echinococcosis. Rapidly metabolized in the liver. Metabolites are excreted mainly by the kidneys within 24-48 hours. The drug is well tolerated. Side effects are rare (sometimes there are dyspepsia, headache, allergic skin reactions, pain in the abdomen, etc.).
Highly effective in ascariasis Levamisole (Decaris). Deworming is due to the fact that the drug paralyzes helminths. This is due to the depolarization of their muscles. In addition, levamisole inhibits fumarate reductase and in this way disrupts the metabolism of helminths. A single administration of levamisole provides deworming in 90-100% of patients, regardless of the degree of infection. In the doses used, levamisole practically does not cause side effects.
With intestinal cestodiasis praziquantel, fenasal, aminoacryquine have been used
For the treatment of intestinal trematodosis(metagonimose) use praziquantel.
From extraintestinal nematodes the most common are various filariasis (including onchocerciasis, which affects the eyes, often up to blindness).
Drugs that have a detrimental effect on microfilariae include dithrazine citrate(diethylcarbamazine citrate, loscuran). It is well absorbed from the gastrointestinal tract. Its maximum concentration in blood plasma accumulates after 3 hours. It is excreted by the kidneys in the form of metabolites and partially unchanged during the first 2 days.
When infested with round helminths, it is successfully used pyrantela pamoate. It disrupts neuromuscular transmission, inhibits cholinesterase and causes spastic paralysis in helminths. Poorly absorbed from the digestive tract (up to 50%). It is most often used for ascariasis, enterobiasis and ankylostomiasis. The drug is well tolerated. Side effects are rare and mild (loss of appetite, headache, nausea, diarrhea).
Has a wide spectrum of anthelmintic activity praziquantel (biltricid). It is highly effective in intestinal cestodosis, as well as extraintestinal trematodosis and cysticercosis. According to the chemical structure, it can be attributed to pyrazinoisoquinoline derivatives. Violates calcium metabolism in helminths, which leads to muscle dysfunction and paralysis.
It is well soaked up at enteral introduction. Rapidly metabolized in the liver. t1/2 = 60-90 min. Metabolites are excreted mainly by the kidneys.
The drug is well tolerated. Side effects are expressed to a small extent (dyspepsia, headache, dizziness, etc.).
Fenasal (niclosamide) inhibits oxidative phosphorylation in cestodes and paralyzes them. In addition, it reduces the resistance of tapeworms to proteolytic enzymes of the digestive tract, which destroy cestodes. In this regard, the drug is not recommended for use in taeniasis, the causative agent of which is the armed (pork) tapeworm, since this may cause cysticercosis1.
Only a small part of the administered drug is absorbed from the gastrointestinal tract.
Fenasal is used for intestinal cestodosis caused by a wide tapeworm, unarmed (bovine) tapeworm, dwarf tapeworm. With the subsequent intake of saline laxatives, the effectiveness of fenasal decreases. Fenasal is well tolerated. Does not cause serious side effects. Sometimes there are dyspeptic phenomena.
Ticket 7
Question1. Recipe, its structure and content. Rules for writing out prescriptions for medicines for outpatients. Prescription forms.
Recipe(from lat. receptum ─ taken) is a written request from a doctor to a pharmacy about dispensing a drug to a patient in a certain dosage form and dosage, indicating the method of its use. It is a medical and legal document. The rules for issuing prescriptions for outpatients and dispensing drugs for them are established by the relevant order of the Ministry of Health.
The prescription is written in a special form in Latin, while the prescription for the patient is written in Russian or in the national languages. It is customary to write a recipe in a clear, clear handwriting, in ink or a ballpoint pen on a letterhead. Recipe modifications are not allowed.
The age of the patient is indicated in cases where a prescription is issued to a child under 18 years of age or to a patient over 60 years of age, as well as when prescribing drugs on preferential terms.
The composition of the medicinal product, the designation of the dosage form and the doctor's request to the pharmacist about the manufacture and dispensing of the medicinal product are written in Latin.
The Latin text begins with an appeal to the pharmacist - "Recipe:", which means "Take:". On the prescription form, it is abbreviated as Rp. Then list the names of the substances included in this recipe in the genitive case, indicating their quantities.
There are abbreviated and extended prescriptions. When prescribing medicines, abbreviated in the prescription, first indicate the dosage form (Solutionis ... (Solution ...); Suspensionis ... (Suspensions ...); Unguenti ... (Ointments ...), etc.), then ─ the name of the medicinal product, concentration (if necessary ), quantity. In expanded form, list all the ingredients and their quantities included in the medicinal product. In the event that several components are included in the prescription, the main drug substance, Basis, is prescribed first, followed by auxiliary substances, Adjuvans. Sometimes prescribe substances that improve the taste, smell of the drug, which are called corrective - Corrigens. The dosage form is determined in some cases by the drug itself. However, there may be a need for Constituens - a substance that gives the drug a certain consistency. In this case, Constituens is given in the recipe after the main and auxiliary substances. Further, using the accepted designations, mark the dosage form that must be made, for example, M. f. unguentum (Misce ut fiat unguentum - Mix to form an ointment).
Doses of medicinal substances are indicated in the decimal system of measurement. The unit of mass is 1.0 ─ one gram. When dosing drugs, values less than 1.0 are also used: 0.1 - one decigram, 0.01 - one centigram. 0.001 - one milligram, 0.0001 - one decimilligram, 0.00001 - one centimilligram, etc. The amount of liquid substances is given in milliliters (ml), grams or drops. The number of drops is indicated by a Roman numeral preceded by gtts (short for the word guttas-drops - in the accusative plural), for example gtts. V (drops five). When prescribing drugs dosed in units of action (U), the number of U is indicated in the prescription instead of weight or volume quantities.
Sometimes the doctor does not give the amount of Constituens (for example, in suppositories), leaving the pharmacist the right to take it as needed; in this case write q. s. (quantum satis), that is, as much as needed, but this applies only to indifferent substances. If several medicinal substances are prescribed in the same dose, then its numerical value is indicated only once after the name of the last substance. To indicate that the marked quantity applies to all the items listed above, they put the sign aa, which means ana ─ equally.
The quantities of substances included in the recipe are indicated on the right side of the prescription form next to the name of the substance (or one line below). In cases where the maximum dose of toxic or potent substances is exceeded, it is necessary to indicate their amount in words with the addition of an exclamation mark and a signature to confirm that the large dose was not prescribed by chance. If the correctness of the prescribed dose is not confirmed, the pharmacist reduces the dose of the substance (up to 50% of the highest single dose indicated in the Pharmacopoeia).
At the end of the prescription, after the designation S. (Signa. Signetur. - Designate. Let it be designated) give instructions to the patient or medical staff about the method of using the drug. In this part of the recipe, called the signature (Signatura), it is briefly and exhaustively stated:
1) dosage (1 powder, 1 tablet, 1 tablespoon, 20 drops, etc.);
2) the time and frequency of taking the drug (how many times a day, before meals or after meals, at night, etc.);
3) method of application of the drug (intravenously, subcutaneously, administered slowly, etc.).
When issuing a prescription to patients, the doctor must sign the prescription and put a personal seal.
If the patient's condition requires the immediate release of the drug from the pharmacy, then Cito (Soon) or Statim (Immediately) is written on the prescription at the top left. In this case, the medicinal product must be manufactured and dispensed out of turn.
question2. Adrenomimetic means of direct type of action. Localization of alpha and beta adrenoreceptors, their functional features. Epinephrine (adrenaline), norepinephrine (norepinephrine). Mechanism of action, pharmacological effects, indications for use, side effects.
Direct adrenomimetics include adrenaline and norepinephrine, as well as substances similar to them in structure.
Epinephrine and noradrenaline are degraded in the intestine and have a short duration of action when administered parenterally due to their rapid reuptake and metabolism. Adrenaline increases blood pressure, increases the frequency and strength of heart contractions (b1-adrenergic effect). Stimulation of a-adrenergic receptors of blood vessels leads to their narrowing (vessels of internal organs, skin), and activation of b2-adrenergic receptors causes vasodilation of skeletal muscles, while the total peripheral vascular resistance can be significantly reduced.
Adrenaline reproduces most of the effects of the sympathetic nervous system, that is, it is a sympathomimetic.
Synthetic adrenomimetics do not act on all receptors, but only on some. Even norepinephrine, introduced from the outside, and not released directly in the synapse, does not affect all receptors and affects them to varying degrees. Therefore, there are several groups of direct adrenomimetics.
Adrenaline hydrochloride excites both a- and b-adrenergic receptors. Excitation of a- and b-adrenergic receptors of the gastrointestinal tract leads to relaxation and a decrease in gastrointestinal motility.
Excitation of a-adrenergic receptors of blood vessels leads to their narrowing (this increases blood pressure and narrows the vessels of the nasal mucosa in rhinitis). Excitation of a-adrenergic receptors of the radial muscle of the eye leads to pupil dilation. Excitation of a-adrenergic receptors of the uterus leads to a decrease in the tone of the uterus.
Excitation of b-adrenergic receptors of the heart leads to an increase in the work of the heart. Excitation of b-receptors of the bronchi leads to the expansion of the bronchi. Excitation of β-receptors of vessels dilates the vessels of vital organs and skeletal muscles. Excitation of b-receptors also leads to the excitation of adenylate cyclase, accumulation of cAMP, increased glycogenolysis, lipolysis, accumulation of glucose, and an increase in metabolic processes.
As a result, adrenaline increases blood pressure, dilates the pupil, slows down the intestines, enhances the work of the heart, dilates the vessels of vital organs, expands the bronchi, increases metabolism, reduces the capsule of the spleen, is used for allergic reactions, hypoglycemic coma. Injection administration of adrenaline is used for anaphylactic shock.
It is used only subcutaneously and intracardially. Intravenous use is not recommended to avoid the occurrence of cardiac arrhythmias.
Adrenaline and a-agonists lower intraocular pressure by constricting the blood vessels of the ciliary body.
a-agonists (mezaton, naphthyzinum, galazolin, norepinephrine hydrotartrate)
Norepinephrine has practically no effect on β-adrenergic receptors, and acting on α-adrenergic receptors of blood vessels, narrows them and increases blood pressure, which leads to the appearance of reflex bradycardia, which prevails over direct β-adrenergic stimulating action. It is used only intravenously.
α1-agonists (α1-adrenergic receptor agonists) are used for rhinitis as a means of increasing blood pressure. a-agonist mezaton (phenylephrine) causes mydriasis without changing the reaction of the pupil to light and without disturbing the process of accommodation. After completion of the fundus examination, physostigmine or pilocarpine can be used as mydriatic antagonists.
a2-agonists (agonists of a2-adrenergic receptors in the central nervous system), in particular, clonidine (clonidine) are centrally acting antihypertensive drugs.
b1 and b2-agonists (izadrin (isoprenaline)) stimulate b-adrenergic receptors, increasing the frequency and strength of heart contractions and causing vasodilation. As a result, diastolic pressure decreases and systolic pressure changes little.
They are used for blockades of impulse conduction, for bronchial asthma.
b1-agonists (dobutamine) are sometimes used in acute heart failure to stimulate myocardial contractility.
b2-agonists (salbutamol, asthmapent, alupent, fenoterol, terbutaline) are not absolutely selective agents. They have a pronounced bronchodilatory effect when used in doses that have a minimal effect on the heart, relax the smooth muscles of the endometrium, so they are used in bronchial asthma and as tocolytics to prevent preterm birth. They are not destroyed by monoamine oxidase and probably do not undergo neuronal reuptake.
Side effects:
Adrenaline: heart rhythm disturbances
Norepinephrine: Side effects are rare. Respiratory disorders, headache, arrhythmias are possible.
question 3. Antiprotozoal agents - metronidazole (trichopol), trichomonacid, monomycin, tetracyclines, solusurmin. Classification, mechanisms of action. Indications for appointment.
1. Medications used to prevent and treat malaria: Hingamine, Primaquine,
Chloridine, Quinine
Sulfanilamides and sulfones, Mefloquine
2. Means used in the treatment of amoebiasis: Metronidazole, Chingamine
Emetine hydrochloride, Tetracyclines, Quiniofon
3. Means used in the treatment of giardiasis: Metronidazole, Furazolidone, Akrikhin
4. Means used in the treatment of trichomoniasis: Metronidazole, Tinidazole, Trichomonacid, Furazolidone
5. Means used in the treatment of toxoplasmosis: Chloridine, Sulfadimezin
6. Means used in the treatment of balantidiasis: Tetracyclines, Monomycin, Quiniofon
7. Means used in the treatment of leishmaniasis: Solyusurmin, Sodium stibogluconate, Metronidazole
1. Malaria is caused by Plasmodium. Three-day malaria is caused by Plasmodium vivax and P. ovale, tropical - by P. falciparum, four-day - by P. malariae. The most common malaria pathogens are P. vivax and P. falciparum. Malarial Plasmodium has two cycles of development. The asexual cycle (schizogony) takes place in the human body, the sexual cycle (sporogony) - in the body of the mosquito.
Antimalarial drugs differ from each other in their tropism for certain forms of development of plasmodium in the human body. In this regard, there are:
1) hematoschizotropic agents (affect erythrocyte schizonts);
2) histoschizotropic agents (affect tissue schizonts);
a) affecting pre-erythrocyte (primary tissue) forms;
b) affecting paraerythrocyte (secondary tissue) forms;
3) gamototropic agents (affect sexual forms).
HEMATO-SHISOTROPIC DRUGS
Chingamine (chloroquine, delagil, rezoquin) is especially widely used. It is a derivative of 4-aminoquinoline. The main thing in its antimalarial effect is the hematoschizotropic action aimed at the erythrocyte forms of Plasmodium.
Chingamine is absorbed from the gastrointestinal tract quickly and almost completely. With this route of administration, the drug accumulates in the blood plasma at maximum concentrations after 1-2 hours. About half of the substance binds to plasma proteins.
Chingamine is used for all types of malaria, as well as for extraintestinal amebiasis. In addition, it is effective (apparently due to immunosuppressive properties) in collagenoses (for example, in rheumatism and rheumatoid arthritis). It is also prescribed prophylactically for cardiac arrhythmias and amyloidosis. Chingamine is usually administered orally, sometimes parenterally.
Chingamine is well tolerated in the treatment of malaria. Side effects occur mainly with its long-term use in large doses (in the treatment of collagenoses). They manifest themselves in the form of dermatitis, dyspeptic phenomena, dizziness. A severe complication is visual impairment (including retinopathy). Rarely observed leukopenia, depression of liver function. With prolonged use of hingamin, monitoring of the state of vision, liver function and hematopoiesis is required.
The great advantage of quinine is the rapid development of the effect. Quinine is characterized by significant toxicity. When it is used, a variety of side effects are often observed (dizziness, hearing and vision impairment, inhibition of kidney function, nausea, vomiting, diarrhea, allergic reactions).
Quinine is of greatest interest for the relief and treatment of chingamine-resistant tropical malaria, as well as for multiple resistance.
As medicines, quinine sulfate, hydrochloride and dihydrochloride are used.
Hematoschizotropic activity is also possessed by sulfonamides and sulfones. Their effectiveness is associated with the ability to disrupt the utilization of para-aminobenzoic acid by malarial plasmodium.
Of the sulfonamides, sulfazine, sulfapyridazine, sulfadimethoxine, sulfalene, sulfadoxine are used. Of the group of sulfones known as anti-leprosy agents, diaphenylsulfone (dapsone) is mainly used in the treatment and prevention of malaria.
Combination preparations are often used, for example fansidar (chloridine + sulfadoxine).
With resistance to hingamin, the tetracycline antibiotic doxycycline is sometimes used.
HISTO-SHISOTROPIC DRUGS
The 8-aminoquinoline derivative primaquine has a detrimental effect on the paraerythrocyte forms of Plasmodium. It also acts on the sexual forms of Plasmodium (gamotocidal action). It is well absorbed from the gastrointestinal tract. The maximum plasma concentration is reached after 2 hours. In the body, the drug quickly undergoes chemical transformations. It is excreted by the kidneys, mainly in the form of metabolites (within 1 day).
The main indication for use is the prevention of distant relapses of three-day malaria, as well as the spread of malaria through the vector (due to gamonotropic action).
Of the side effects, dyspeptic symptoms, methemoglobinuria, leukopenia, and sometimes agranulocytosis are possible. In persons with a certain type of genetic enzymopathy (with insufficiency of glucose-6-phosphate dehydrogenase of erythrocytes), acute hemolysis and hemoglobinuria occur.
Primaquine can be combined with other drugs (simultaneously and sequentially).
GAMONTOTROPIC DRUGS
Drugs that affect germ cells can have both gamontocidal (primaquine) and gamontostatic (chloridine) effects. When exposed to gamontocidal agents, the germ cells of Plasmodium die in the human body. Gamontostatic agents only damage germ cells, resulting in disruption of the sporogony process (at different stages).
2. MEDICINES USED IN THE TREATMENT OF AMEBIASIS
The causative agent of amoebiasis, which is very widespread in countries with a hot climate, is Entamoeba histolytica. Amoebiasis most often affects the large intestine (amebic dysentery). At the same time, amoebas are found both in the intestinal lumen and in its wall. However, systemic amebiasis with extraintestinal lesions is also possible. Spreading from the intestine through the portal vein system, amoebas can cause hepatitis and liver abscesses. Abscesses of the lungs and other organs are sometimes noted.
Depending on the localization of the causative agent of amoebiasis, certain antiamebic agents are required. They can be represented by the following main groups:
Amebicides effective in any localization of the pathological process-Metronidazole
Amoebicides of direct action, effective mainly in the localization of amoebae in the intestinal lumen-Quiniofon
Amebicides of indirect action, effective in the localization of amoebae in the lumen and in the intestinal wall-Tetracyclines
Tissue amoebicides acting on amoebae in the intestinal wall and in the liver-Emetine hydrochloride
Tissue amoebicides, effective mainly in the localization of amoebae in the liver-Hingamin
Metronidazole is a universal remedy effective for intestinal and extraintestinal amoebiasis. It is least effective against amoebas in the intestinal lumen. Therefore, in amoebic dysentery, it is usually combined with quiniofon or iodoquinol. Metronidazole has no effect on cysts.
Quiniofon (yatren) is absorbed from the gastrointestinal tract only by 10-15%, therefore, high concentrations of the substance necessary for the amebicidal action are created in the intestines.
The drug has low toxicity. Diarrhea is a typical side effect. Possible optic neuritis.
Similar to quiniofon in structure and direction of action, the drug is iodoquinol.
Quite widespread in the treatment of amoebiasis was the alkaloid of the root of ipecac (Cephaelis ipecacuanha) emetine. The drug used is emetine hydrochloride. It is administered intramuscularly, since when taken orally, it causes severe irritation of the mucous membrane of the gastrointestinal tract (in this case, vomiting of reflex origin often occurs).
Emetine acts on amoebae localized both extraintestinally (for example, in the liver, where the substance accumulates in high concentrations) and in the intestinal wall. The drug does not affect amoebas in the intestinal lumen.
Emetine is excreted by the kidneys for a long time (more than 1 month). In this regard, it accumulates, which is the main cause of overdose and the development of toxic effects.
Side effects relate to the cardiovascular system (tachycardia, cardiac arrhythmias, pain in the heart, hypotension), gastrointestinal tract (nausea, diarrhea, vomiting), neuromuscular system (muscle weakness, tremor, neuralgia). Possible violations of the kidneys and liver, therefore, during treatment with emetine, periodic monitoring of the functions of the heart, kidneys and liver is required. In organic diseases of the heart and kidneys, the drug is contraindicated.
When using tetracyclines, the intestinal flora is suppressed, and this indirectly adversely affects the growth and reproduction of amoebas located in the lumen and intestinal wall. Such drugs may be referred to as indirect antiamebic agents. In terms of effectiveness in amoebiasis, tetracyclines are inferior to direct-acting amebicides.
In the treatment of acute intestinal amoebiasis, monomycin is sometimes used (introduced orally).
In many cases, the treatment of amebiasis can be limited to the use of metronidazole. However, combinations of substances are often used. So, with amoebic dysentery, it is advisable to combine drugs that act in the intestinal lumen, in its wall, and also protect the liver from amoebas (for example, metronidazole + quiniofon; emetine hydrochloride + tetracycline + quiniofon).
3. MEDICINES USED IN THE TREATMENT OF giardiasis
The causative agent of giardiasis is Giardia (lamblia) intestinalis. In the presence of lamblia in the intestine, its dysfunction (duodenitis, enteritis) is observed. For the treatment of giardiasis, metronidazole, aminoquinol and furazolidone are used.
Aminoquinol is a derivative of quinoline. It is effective in giardiasis, toxoplasmosis, cutaneous leishmaniasis, and also in some collagenoses. In most cases, the drug is well tolerated. May cause dyspeptic disorders, headache, tinnitus, allergic reactions.
4 .MEDIUMS USED IN THE TREATMENT OF TRICHOMONOSIS
With trichomoniasis caused by Trichomonas vaginalis (manifested by colpitis and vulvovaginitis in women, urethritis in men), metronidazole is the drug of choice.
Metronidazole (flagyl, klion, trichopolum, vagimid) is a derivative of nitroimidazole (see structure). It has a detrimental effect not only on Trichomonas, but also on amoebas and Giardia. In addition, metronidazole is effective against non-spore-forming anaerobes.
It is well absorbed from the gastrointestinal tract. In the body, to a large extent, it undergoes chemical transformations. Metronidazole, its metabolites and conjugates are excreted mainly by the kidneys. Small amounts of the drug are excreted by the salivary glands, intestines, and during lactation - by the mammary glands.
The drug is usually well tolerated. Of the side effects, dyspeptic symptoms are most often noted (appetite disturbance, metallic taste in the mouth, nausea, diarrhea). Described violations of the central nervous system (tremor, impaired coordination), with the appearance of which the drug is canceled. Possible damage to the skin, mucous membranes.
The group of nitroimidazoles, in addition to metronidazole, also includes tinidazole (Fasigine). It is highly effective in trichomoniasis, amoebiasis and giardiasis. In addition, it has a bactericidal effect against a number of obligate anaerobes. Well absorbed from the gastrointestinal tract. When using tinidazole in the blood plasma, higher concentrations are created than when using metronidazole. Tinidazole acts longer than the last.
Trichomonacid also belongs to the drugs used for trichomoniasis. It is a derivative of aminoquinoline. Apply it inside and topically. It has an irritating effect on mucous membranes.
With trichomoniasis, nitazole and furazolidone are also effective.
5 .DRUGS USED IN THE TREATMENT OF TOXOPLASMOSIS
Toxoplasmosis is caused by Toxoplasma gondii. There are different forms of the disease, which are accompanied by damage to the lymph nodes, intestines, lungs and other internal organs, eyes, central nervous system. Infection with Toxoplasma can cause premature birth, spontaneous abortion, deformities. The main drugs used in this disease are chloridine (see section 1 for details) and sulfonamides (see chapter 29.2).
It should be borne in mind that chloridine, which inhibits the transition of dihydrofolic acid to tetrahydrofolic acid, should not be prescribed in the first half of pregnancy (it has a negative effect on the fetus). In this situation, sulfonamides are used to prevent infection of the fetus.
Pentamidine is also used in toxoplasmosis.
6. MEDICINES USED IN THE TREATMENT OF BALANTHIDIAZIS
The causative agent of balantidiasis is the infusoria Balantidium coli, which affects the large intestine.
Treatment of balantidiasis is carried out mainly with the help of monomycin, tetracyclines, quiniofon
7. MEDICINES USED IN THE TREATMENT OF LEISHMANIASIS
There are cutaneous leishmaniasis (one of the pathogens is Leishmania tropica) and visceral leishmaniasis (the pathogen is Leishmania donovani).
In the treatment of visceral leishmaniasis (kala-azar) in our country, the pentavalent antimony drug solyusurmin is most widely used.
Enter the drug parenterally. Most patients tolerate it well. Side effects include nausea, headache, skin rashes, and rarely agranulocytosis. In case of an overdose of solyusurmin, unithiol can be used as its antidote.
Of the preparations of pentavalent antimony in leishmaniasis, sodium stibogluconate is also used. It is administered intramuscularly and intravenously. From the negative effects may occur vomiting, anorexia, bradycardia, hypotension, retrosternal pain.
Consideration should be given to the development of Leishmania resistance to antimony preparations.
Both antimonials are also effective in cutaneous leishmaniasis.
Local treatment for cutaneous leishmaniasis consists in soaking the infiltrates with a solution of quinacrine.
For resorptive action, an antibiotic of the aminoglycoside group monomycin is used, which has a high anti-leishmania activity. Along with its effectiveness in cutaneous leishmaniasis, it is characterized by a fairly wide spectrum of antibacterial action. It has a negative effect on the kidneys, sometimes causes neuritis of the auditory nerve. Less toxic than neomycin. Metronidazole is also used in this form of leishmaniasis.
MEDICINES USED IN THE TREATMENT OF TRYPANOSOMIASE
Trypanosomiasis is caused by Trypanosoma gambiense and Trypanosoma rhodesiense, which cause sleeping sickness, and Trypanosoma cruzi, which is associated with Chagas disease.
Of the organic preparations of arsenic for sleeping sickness (common in South Africa), melarsoprol is used, which penetrates well through the blood-brain barrier and is the drug of choice in the treatment of this disease. In addition, the aromatic diamidine pentamidine and the polyanionic compound suramin are used. However, the last two drugs do not penetrate the brain, and therefore they are used in the early stages of the disease, when the CNS is not yet involved in the process. The drugs are quite toxic and cause many side effects.
In Chagas disease (South America), the primaquine antibiotic puromycin and a number of other drugs are used.
Ticket 6
question1. Principles of discovery of new drugs, ways of introducing them into medical practice
The progress of pharmacology is characterized by the continuous search and creation of new drugs. The creation of drugs begins with the research of chemists and pharmacologists, whose creative collaboration is absolutely essential in the discovery of new drugs. At the same time, the search for new funds is developing in several directions.
The main route is the CHEMICAL synthesis of drugs, which can be realized in the form of a DIRECTIONAL synthesis or have an EMPIRICAL path. If directed synthesis is associated with the reproduction of biogenic substances (insulin, adrenaline, norepinephrine), the creation of antimetabolites (PABA-sulfanilamides), the modification of molecules of compounds with known biological activity (changes in the structure of acetylcholine - the ganglioblocker hygronium), etc., then the empirical path consists of either from random finds, or search by screening, that is, sifting various chemical compounds for pharmacological activity.
One example of empirical findings is the case of the discovery of a hypoglycemic effect when using sulfonamides, which subsequently led to the creation of sulfonamide synthetic perforal antidiabetic agents (butamide, chlorpropamide).
Another variant of the empirical way of creating drugs is also very laborious - the SCREENING METHOD. However, it is inevitable, especially if a new class of chemical compounds is being investigated, the properties of which, based on their structure, are difficult to predict (an inefficient way). And here a huge role is currently played by the computerization of scientific research.
Currently, drugs are obtained mainly through directed chemical synthesis, which can be carried out a) by similarity (introduction of additional chains, radicals) b) by complementarity, that is, by matching to any receptors of tissues and organs.
In the arsenal of medicines, in addition to synthetic drugs, a significant place is occupied by drugs and individual substances from MEDICINAL RAW MATERIALS of plant or animal origin, as well as from various minerals. These are, first of all, galenic, novogalenic preparations, alkaloids, glycosides. Thus, morphine, codeine, papaverine are obtained from opium, reserpine from rauflphia serpentine, and cardiac glycosides - digitoxin, digoxin - from foxglove; from a number of endocrine glands of cattle - hormones, immunoactive drugs (insulin, thyroidin, taktivin, etc.).
Some medicines are waste products of fungi and microorganisms. An example is antibiotics. Medicinal substances of plant, animal, microbial, fungal origin often serve as the basis for their synthesis, as well as subsequent chemical transformations and the production of semi-synthetic and synthetic drugs.
They are gaining momentum in the creation of drugs through the use of genetic engineering methods (insulin, etc.).
A new drug, having passed through all these "sieves" (the study of pharmacoactivity, pharmacodynamics, pharmacokinetics, the study of side effects, toxicity, etc.), is allowed for clinical trials. It uses the "blind control" method, the placebo effect, the double "blind control" method, when neither the doctor nor the patient knows when the placebo is being used. Only a special commission knows. Clinical trials are being conducted on humans, and in many countries this is done on volunteers. Here, of course, there is a mass of legal, deontological, moral aspects of the problem that require their clear development, regulation and approval of laws in this regard.
Some discoveries in the field of pharmacology and their implementation in medical practice:
1865 - the effect of cardiac glycosides on the heart was established
1879 - discovery of nitroglycerin
1921 - discovery of insulin
1939 - discovery of penicillin
1942 - discovery of the first anticancer drugs
1952 - discovery of psychotropic drugs
1955 - oral contraceptives
1958 - the first β-blockers
1987 - a group of statins (lipid-lowering drugs)
1992 - ACE inhibitors
1994 Proton Pump Inhibitors
question2. . Muscle relaxants of peripheral action (curare-like drugs). Classification, mechanism of action, pharmacodynamics. Drugs: pipecuronium bromide (arduan), suxamethonium iodide (ditilin), atracurium (trakrium), tubocurarine. Indications and contraindications for use. Overdose measures.
Classification:
1) Anti-depolarizing agents:
tubocurarine chloride
Pancuronium bromide
Pipecuronium bromide
2) Depolarizing agents:
3) In-va mixed type of action:
dioxonium
1 .Antidepolarizing drugs block n-cholinergic receptors and prevent the depolarizing action of acetylcholine. The blocking effect on ion channels is of secondary importance. Antidepolarizing agents can be competitive and non-competitive n-anticholinergics. Thus, true competitive antagonism is possible between a curariform substance (for example, tubocurarine) and acetylcholine in terms of its effect on n-cholinergic receptors. If, against the background of a neuromuscular block caused by tubocurarine, in the region of the n-cholinergic receptors of the end plate, the concentration of acetylcholine is significantly increased, this will lead to the restoration of neuromuscular transmission (competitively acting acetylcholine will displace tubocurarine associated with cholinergic receptors). If at the same time the concentration of tubocurarine is again increased to certain values, then the blocking effect will again occur. Curariform drugs acting on this principle are called competitive. Competitive drugs also include pancuronium (pavulon), pipecuronium (arduan). In addition, there are drugs of a non-competitive type (for example, prestonal). In this case, the curare-like drug and acetylcholine appear to react with different but related end plate receptor substrates.
2. Depolarizing agents (for example, dithylin) excite n-cholinergic receptors and cause persistent depolarization of the postsynaptic membrane. Initially, the development of depolarization is manifested by muscle twitches-fasciculations (neuromuscular transmission is relieved for a short time). After a short period of time, a myoparalytic effect occurs.
3. Separate curariform drugs have a mixed type of action (there may be a combination of depolarizing and antidepolarizing properties). This group includes dioxonium (depolarizing-non-competitive drug). First, it causes a short-term depolarization, which is replaced by a non-depolarizing block.
According to the duration of the myoparalytic action, curare-like drugs can be conditionally divided into three groups: short-acting (5-10 minutes) - ditilin, medium-term (20-50 minutes) - tubocurarine, pipecuronium, pancuronium.
Most curare-like drugs have a high selectivity of action in relation to neuromuscular synapses. However, they can also affect other parts of the reflex arc. A number of antidepolarizing substances have a moderate ganglioblocking activity (especially tubocurarine), one of the manifestations of which is a decrease in blood pressure, as well as a depressant effect on the n-cholinergic receptors of the carotid sinus zone and the adrenal medulla. For some substances (pancuronium), a pronounced m-anticholinergic (vagolytic) effect on the heart was noted, which leads to tachycardia.
Tubocurarine and some other drugs can stimulate the release of histamine, which is accompanied by a decrease in blood pressure, an increase in bronchial muscle tone.
Depolarizing curare-like agents have a certain effect on the electrolyte balance. As a result of depolarization of the postsynaptic membrane, potassium ions leave the skeletal muscles and their content in the extracellular fluid and blood plasma increases. This may be the cause of cardiac arrhythmias.
Depolarizing curariform substances stimulate the annulospiral endings of skeletal muscles. This leads to an increase in afferent impulses in proprioceptive fibers and can cause inhibition of monosynaptic reflexes.
Curare-like drugs, which are quaternary ammonium compounds, are poorly absorbed in the gastrointestinal tract, so they are administered parenterally, usually intravenously.
Curare-like drugs are widely used in anesthesiology during a variety of surgical interventions. By causing relaxation of skeletal muscles, they greatly facilitate many operations on the organs of the chest and abdominal cavities, as well as on the upper and lower extremities. They are used for tracheal intubation, bronchoscopy, reduction of dislocations and reposition of bone fragments. In addition, these drugs are sometimes used in the treatment of tetanus, with electroconvulsive therapy.
Side effects of curare-like drugs are not threatening. Blood pressure can decrease (tubocurarine) and increase (ditilin). For a number of drugs, tachycardia is typical. Sometimes there are cardiac arrhythmias (ditilin), bronchospasm (tubocurarine), increased intraocular pressure (ditilin). Depolarizing substances are characterized by muscle pain. In persons with a genetically determined deficiency of plasma cholinesterase, ditilin can cause prolonged apnea (up to 6-8 hours or more instead of the usual 5-10 minutes).
Curare-like drugs should be used with caution in diseases of the liver, kidneys, as well as in old age.
It should be remembered that curare-like drugs depress or completely turn off breathing. Therefore, they can be used in medical practice only in the presence of antagonists and all the necessary conditions for artificial respiration.
Question3. Antianginal agents beta-blockers, and calcium channel blockers. Mechanism of antianginal action, pharmacodynamics. Comparative characteristics - propranolol (anaprilin), atenolol (tenormin), verapamil, (isoptin), nifedipine. Indications for appointment. Side effect.
BETA-BLOCKERS
In recent years, this group of drugs has found wide distribution for the treatment of a number of therapeutic diseases.
There are non-selective beta-blockers (timolol, propranolol, sotalol, nadolol, oxprenolol, pindolol, etc.) and selective beta-1-blockers (metoprolol, atenolol, acebutolol, etc.).
The therapeutic activity of this group of drugs in angina pectoris is due to their ability to block the influence of the sympathetic nervous system on the heart, which leads to a decrease in its work and a decrease in myocardial oxygen consumption.
ANAPRILIN (propranolol, inderal, obzidan; tablets 0.01 and 0.04) is a non-cardioselective beta-blocker without its own sympathomimetic activity with a short duration of action. Anaprilin reduces all 4 functions of the heart, primarily myocardial contractility. The most pronounced effect is observed within 30-60 minutes, the therapeutic effect, due to the short half-life (2.5-3.2 hours), lasts 5-6 hours. This means that the drug should be taken 4-5 times a day. Anaprilin is used only for the prevention of angina attacks, only in its typical form, since with a vasospastic form of angina against the background of blocked beta-adrenergic receptors, catecholamines will increase the spasm of the coronary vessels.
Side effects: decrease in myocardial contractility, bradycardia, AV blockade, bronchospasm; nausea, vomiting, diarrhea, general weakness, dizziness, sometimes allergic reactions. Depression is possible. With the simultaneous use of hypoglycemic agents - the risk of hypoglycemia.
CALCIUM ANTAGONISTS (CALCIUM CHANNEL BLOCKERS)
The importance of calcium in the performance of vital functions by the body is enormous. Calcium is necessary for the regulation of excitatory and inhibitory processes in both smooth and skeletal muscles. Coming from the external environment or from the intracellular depot under the influence of various stimuli, calcium interacts with calcium-binding cytoplasmic proteins that act as regulators.
For the heart and blood vessels, the value of calcium is somewhat different, which is associated with the predominance (in the heart or blood vessels) of specific calcium-binding proteins. In myocardiocytes there is a special protein - troponin (leiotonin), and in smooth vascular myocytes - a special thermostable calcium-dependent protein calmodulin. Depending on whether they act more on troponin or calmodulin, some calcium channel blockers affect the heart to a greater extent, while others affect the vessels. For example, such a calcium antagonist as VERAPAMIL has a greater effect on the heart (its antiarrhythmic effect is very important).
The antianginal effect of this group of drugs is associated both with their direct action on the myocardium and, above all, with the effect on peripheral hemodynamics. Calcium antagonists block its entry into the smooth muscle cell, thus reducing its ability to contract. The action of these drugs on the coronary vessels is characterized as antispastic, as a result, the coronary blood flow increases, and due to the action on the peripheral vessels, blood pressure decreases. This reduces the afterload on the heart, improves blood flow in the ischemic zone. These drugs reduce the mechanical work of the heart and myocardial oxygen demand, increase the number of collaterals. When used in patients, the frequency and intensity of angina attacks decreases, and tolerance to physical activity increases.
Most often, nifedipine is used for this purpose (synonyms: fenigidin, corinfar, cordafen, cordipin, etc.; tab. 0, 01). The effect comes in 15-20 minutes and lasts 4-6 hours. The drug is inferior to nitroglycerin in terms of the strength of the antianginal effect.
Unlike verapamil, the drug has weak antiarrhythmic activity, greatly reduces diastolic pressure. Especially well relaxes the coronary vessels in vasospastic angina pectoris. In general, with this form of angina, calcium antagonists are preferable. In addition to nifedipine, for the chronic treatment of angina pectoris, second-generation nifedipine derivatives created in the 80s are used: isradipine (syn.: lomir).
This group of drugs gives a small number of side effects: lowering blood pressure, headaches, muscle weakness, nausea, constipation. Continuous use of drugs for 2-3 months leads to the development of tolerance.
For angina pectoris with bradycardia, an ephedrine derivative is used - OXYFEDRIN (ildamen, MYOPHEDRIN; tablets of 0.016). The drug has a partial agonistic activity in relation to the beta-1 receptors of the heart, has a direct coronary dilating effect, increases myocardial contractility without an excessive increase in oxygen demand. Another similar drug NONAKHLAZIN, of domestic production, is available in tablets of 0.03 - a derivative of phenothiazine. The drug has a positive inotropic effect and reduces the tone of the coronary arteries.
In the treatment of patients with angina pectoris, such a drug as dipyridamole (curantil), a pyrimidine derivative, is also used. This drug acts on blood microcirculation in small vessels, preventing platelet aggregation, increases the number of collaterals and the intensity of collateral blood flow, however, it can cause a "steal" symptom, especially when administered intravenously in patients with severe coronary atherosclerosis, since the drug causes expansion of those vessels, who are not affected by sclerosis. On the other hand, this drug is indicated for patients who have angina pectoris, and also, due to various reasons, increased blood clotting.
Means such as validol have a reflex type of action. The composition of this drug includes menthol (25% solution of menthol in menthol ester of isovaleric acid). It is a weak antianginal agent, has a sedative effect and a moderate reflex vasodilating effect. It is indicated for mild forms of angina pectoris.
Ticket 10
Soft dosage forms are thick mixtures that are most often applied externally by rubbing. Most often used to treat skin diseases, torn ligaments, muscles and some other diseases. Such medicines are stored, as a rule, in vials, tubes, jars, etc.
Classification
Here are the main types of soft dosage forms:
- Ointments.
- Gels.
- Jelly.
- Creams.
- Liniments.
- Pastes.
- Plasters.
- Suppositories.
Let's consider all of them in more detail.
Ointments
Ointments are most often used externally - to affect the skin and mucous membranes (eye, vaginal, urethral, rectal). Ointments consist of a hydrophobic (greasy water-repellent) or hydrophilic (water) base and active ingredients evenly distributed in the base. Sometimes the composition of the ointment includes active substances that are easily absorbed through the skin into the blood or lymph (for example, ointments containing nitroglycerin as an active substance). Some ointments are used as a means of protection against the harmful effects of acids or alkalis on the skin.
Depending on the consistency, ointments themselves are distinguished, as well as gels, jellies, creams, liniments and pastes.
All ointments (gels, jellies, creams, liniments, pastes) are stored in their original packaging, which ensures the stability of the active substance during the specified shelf life, in a cool, dark place, unless otherwise indicated in the instructions for the drug.
Gels
Gels are transparent hydrophilic-based ointments (derivatives of cellulose, gelatin, polymers of acrylic acid and other substances) with active ingredients distributed in it.
Gels are:
- for external use;
- eye;
- nasal (for the nose);
- dental;
- for internal use;
- rectal;
- vaginal.
Unlike ointments, gels are better absorbed, do not stain clothes and, most importantly, as a rule, release active ingredients more easily.
Currently, more and more soft dosage forms are produced in the form of gels (for example, alpizarin gel for the treatment of herpes, benzyl benzoate gel for the treatment of scabies, gel with chloramphenicol and methyluracil for wound healing, etc.).
Jelly
Transparent ointments on a hydrophilic basis for external use. Jelly has a more viscous consistency than gel and is applied to the skin in a thicker layer. Jellies are prescribed by a doctor infrequently, for specific diseases, only a few companies produce them.
Creams
Emulsion ointments, which include a hydrophobic base, water and an emulsifier (a substance that promotes the penetration of active substances through the cell membrane).
Creams are less viscous in their consistency than ointments, they are more often used in medical cosmetics (antifungal creams Clotrimazole, Lamisil and Terbifin, Zovirax anti-herpes cream, etc.).
Liniments
Ointments, which are a thick liquid or gelatinous mass, applied externally by rubbing into the skin (from Latin linire - “rub”), for example, streptocide liniment for the treatment of skin diseases, Vishnevsky liniment (anti-inflammatory), lidocaine liniment (used for pain relief in dentistry and pediatrics), etc.
The most common liniments, which are based on fats: vegetable oils (sunflower, linseed, etc.), lanolin, sometimes lard, etc.
Pastes
Pastes are the most viscous of all ointments. The content of solids in them exceeds 20%,
In this form, most toothpastes are produced, as well as, for example, Lassar paste, consisting of zinc oxide, etc.
plasters
Dosage form for external use, which has a therapeutic effect on the skin, subcutaneous tissues, and in some cases - on the entire body. In recent years, transdermal therapeutic systems (TTS) have been created that have the ability not only to stick to the skin, but also to pass drugs through the skin barrier (most often cardiovascular, lowering blood pressure, painkillers, sleeping pills). The advantage of TTS is that the entire dose of the active substance is outside the human body, and the patient himself can regulate it by removing a strip of patch from the skin or reducing its area.
The plasters are produced in the form of a plastic mass (corn plaster), on a special substrate (adhesive plaster, pepper plaster) and without it, as well as in the form of a pad with active ingredients fixed on an adhesive tape (pepper plaster with an extract of capsicum, arnica and belladonna).
Plasters without active ingredients in the form of adhesive tape (adhesive plasters) are used to fix dressings and for other purposes.
Store patches in a dry, dark place, unless otherwise indicated in the instructions.
suppositories
Suppositories are dosed soft dosage forms that melt or dissolve at body temperature.
There are suppositories:
- rectal (for insertion into the rectum);
- vaginal (for insertion into the vagina);
- urethral (for insertion into the urethra);
- sticks (for insertion into the vagina and urethra).
The rectal suppository (maximum diameter 1.5 cm) may be conical or otherwise shaped.
The mass of one suppository for adults is 1-4 g. If the mass is not indicated, then it is 3 g. The mass of a suppository for children is 0.5-1.5 g.
Vaginal suppositories can be spherical (balls), ovoid (ovules) or flat with a rounded end (pessaries). Their mass is 1.5-6 g. If the mass of the vaginal suppository is not indicated, then it is not less than 4 g.
Sticks (candles) - have the shape of a cylinder with a pointed end and a diameter of not more than 1 cm. The mass of the stick is 0.5-1 g.
Suppositories packed in paraffin paper, cellophane, foil or plastic cases are stored in a dry, cool place.
Solutions (Solutio) - a liquid dosage form obtained by dissolving a medicinal substance in a solvent. The most commonly used solvents are distilled water (Aqua destillata), ethanol (Ethanol; ethyl alcohol, Spiritus aethylicus) 70%, 90%, 95% and liquid oils - peach (Oleum Persicorum), vaseline (Oleum Vazelini), etc. Solutions must be transparent and free of suspended particles or sediment. Use solutions for external and internal use, as well as for injection.
Solutions for external use used in the form of eye, ear drops, nose drops, lotions, rinses, washes, douching. There are two forms of prescribing solutions - abbreviated and expanded.
Abbreviated form solution begins with the name of the dosage form, i.e. from the word Solutionis (rod.p. Solution). Next, indicate the name of the medicinal substance in the genitive case, the concentration of the solution and its amount. Then comes D.S. If the solvent is water, then the nature of the solution (water) is not indicated in the abbreviated prescription.
The concentration of a solution can be expressed in three ways:
in percentages;
relations (for example, 1:1000, 1:5000, etc.);
mass-volume ratios (for example, 0.6-200 ml, i.e. 200 ml contains 0.6 g of the drug substance).
For example:
Rp.: solutionis Nitrofurali 0,02% - 500 ml
D. S. For gargling 4 times a day.
Rp.: solutionis Nitrofurali 1:5000 – 500 ml
D. S
Rp.: solutionis Nitrofurali 0,1 – 500 ml
D. S. For gargling 4 times a day
Alcoholic and oily solutions in abbreviated form are prescribed with the designation of the nature of the solution - alcohol (spirituosae), oily (oleosae), which is given after the name of the medicinal substance.
For example:
Rp.: Solutionis Acidi borici spirituosae 1% - 10ml
D. S. Ear drops. 3 drops 2 times a day.
Rp.: solutionis Camphorae oleosae 10% - 30 ml
D. S. For rubbing the joint area.
In cases where an oil or alcohol solution requires a certain oil or alcohol of a certain concentration, only a detailed prescription of the solution is possible. In this case, the soluble substance is indicated first, and then the solvent with the designation of quantities. The prescription ends with the M.D.S. and S.
For example:
Rp.: Mentholi 0,1
Olei Vasellini ad 10 ml
M. D. S. Instill 5 drops into the nose.
Solutions for internal use usually dosed with graduated cups, tablespoons and teaspoons, as well as drops.
1 tablespoon contains an average of 15 ml of an aqueous solution;
in 1 teaspoon - 5 ml;
1 ml of water contains 20 drops.
Knowing a single dose of a medicinal substance and a single amount of a solution, its concentration can be calculated.
For example:
Rp.: solutionis sodium bromidi 1% - 180 ml
D. S
Suspensions (suspension) - suspension of particles of solid medicinal substances in a liquid. Suspensions are prescribed internally and externally. Sterile suspensions can be administered intramuscularly. Typically, water is used to make the suspension. In this case, an abbreviated prescription of the suspension is possible. Such a prescription begins with the name of the dosage form Suspensionis (genus item Suspensions), followed by the name of the medicinal substance, the concentration of the suspension, its amount and D.S.
For example:
Rp.: Suspensionis Hydrocortisoni acetatis 0,5% - 10 ml
D. S. Instill in the eye 2 drops 4 times a day.
Emulsions (Emulsum) - a liquid dosage form in which water-insoluble liquids (for example, liquid oils) are in suspension in the form of tiny particles. Emulsions are used internally and externally. Most often, oil emulsions are used. They are prepared from liquid oils (castor, almond, etc.). To emulsify the oil (separation into the smallest particles), special emulsifiers are added.
The prescription of the emulsion begins with the name of the dosage form - Emulsi (genus item Emulsions), after which the amount of oil in ml and the total amount of the emulsion are indicated.
For example:
Rp.: Emujsi olei Ricini 20ml – 100ml
D. S. for 1 appointment.
Infusions (infusum) and decoctions (Decoctum). When processing herbal medicinal raw materials (leaves, grass, roots, etc.) with water at a temperature of 100 0 C, their active principles are extracted from medicinal plants with some admixture of ballast substances. They are called infusions and decoctions. infusions more often prepared from leaves, flowers, herbs. Decoctions- from the coarser, denser parts of plants (roots, rhizomes, bark) and therefore differ from infusions in a longer extraction of active principles.
To prepare infusions and decoctions, a weighed amount of medicinal raw materials is placed in a vessel called an infunder and filled with water at room temperature. Infundirka is placed in a boiling water bath: infusions - for 15 minutes, decoctions - for 30 minutes. Then the medicine is filtered and filtered: decoctions - after 10 minutes. (hot), infusions - after complete cooling. Because infusions and decoctions quickly deteriorate, they are prepared immediately before issuing to the patient, in the amount required for no more than 3-4 days.
Assign infusions and decoctions, most often inside with tablespoons. In addition, these dosage forms are also used externally for rinsing, washing, etc.
There is only one form of prescribing infusions and decoctions. After the name of the dosage form: Infusi ... (Infusion ...) or Decocti ... (Decoction ...) indicate the part of the plant from which the medicine is prepared (leaves, grass, root, etc.), the name of the plant, the amount of medicinal raw materials and (through a dash) the total amount infusion or decoction. Then D.S.
For example:
Rp.: Infusion herbae Thermopsidis 0,5 – 200 ml
D. S. 1 tablespoon 4 times a day.
Galenic preparations - tinctures (Tinctura) and extracts (Extractum) - most often - these are alcohol extracts from herbal medicinal raw materials. Tinctures are prepared in a concentration of 1:5 or 1:10, and extracts: 1:1 or 1:2. Unlike infusions and decoctions, they can be stored for a long time, and therefore they are made at factories according to certain technical standards. The recipes do not indicate the parts of the plants from which they are made, as well as their concentration.
The prescription of tinctures begins with the name of the dosage form - Ticturae ... (genus p. Tinctures ...). Then indicate the name of the plant and the amount of tincture. After that comes D.S.
For example:
Rp.: Tincturae Valerianae 25 ml
D. S. 25 drops 3 times a day.
extracts, depending on the consistency, are divided into liquid, thick and dry. Liquid extracts, like tinctures, are colored liquids. Thick - viscous masses with a moisture content of not more than 25%. Dry - loose masses with a moisture content of not more than 5%.
The prescription of extracts begins with the name of the dosage form - Extracti ... (Extract ...). This is followed by the name of the plant and the type of extract must be indicated - Fluidi (liquid), spissi (thick), sicci (dry). After that, the amount of extract and D.S.
For example:
Rp.: Extracti Frangulae fluidi 25 ml
D. S. 25 drops at night.
Novogalenic preparations
Novogalenic preparations are extracts from herbal medicinal raw materials, maximally freed from ballast substances (containing the amount of biologically active substances of plants) and suitable not only for oral administration, but also for parenteral administration. Each novogalenny drug has a special name. They are prepared in factories.
When prescribing a drug for oral administration, indicate its name, amount and D.S.
For example:
Rp.: Adonisidi 15 ml
D. S. 15 drops 3 times a day.
potions- mixtures of liquid or liquid and solid medicinal substances. Mixtures can be clear, cloudy and even with sediment (the latter should be shaken before use). Medicines are prescribed mainly inside.
Medicines are prescribed in expanded or semi-abbreviated form. The recipe lists all the ingredients of the mixture and their quantities, followed by the M.D.S. The word "potion" is not used in the recipe.
For example:
Rp.: Solutionis Natrii bromidi 2% - 180 ml
Coffeini-natrii benzoatis 0.6
M. D. S. 1 tablespoon 3 times a day.
Liniments (Linimentum) - dosage forms for external use. Most liniments are homogeneous mixtures in the form of thick liquids.
Liniments are written out most often in an expanded form of prescription. After listing the constituent parts of the liniment and their quantities, write M.f. linimentum (Misce ut fiat linimentum - Syeshay to make liniment); followed by D.S.
For example:
Rp.: Chloroformi 20 ml
Olei Hyosciami 40ml
M.f. linimentum
D. S. For rubbing joints
Liniments of industrial production are written out in an abbreviated form.
For example:
Rp.: Linimenti Synthomicini 5% - 25 ml
D. S. Apply to the wound.
Soft dosage forms include ointments, liniments, pastes, suppositories, patches.
Ointments (Unguenta)
(im. p. unit h. - Unguentum,
genus. p. units hours - Unguenti, abbreviation - Ung.)
Ointment - a soft dosage form for external use, having a viscous consistency, capable of forming a continuous film on the surface of the skin and mucous membranes.
Ointments consist of a base and one or more medicinal substances evenly distributed in it. The composition of ointments may include stabilizers, surface-active substances (surfactants), preservatives and other excipients.
Ointments are widely used in various fields of medicine - in dermatology, otorhinolaryngology, proctology, gynecology, etc. They are also used as a means of protecting the skin from adverse effects (organic irritants, acids, alkalis, etc.), as a cosmetic product (for removing age spots, improving skin nutrition, treating and removing hair).
Currently, medicinal substances belonging to almost all pharmacological groups (antiseptics, local anesthetics, hormones, vitamins, antifungal agents, analgesics, antibiotics, etc.) are prescribed in the form of ointments. The bases of ointments are also very diverse. They are able to influence the pharmacokinetics of drugs and other parameters.
The requirements for ointments are due to both the method of application and the complexity of the composition of this dosage form.
Ointments should have a soft consistency, which would ensure the convenience of applying them to the skin, mucous membranes and would contribute to the formation of an even continuous film on the surface.
To achieve the desired therapeutic effect, medicinal substances in the ointment should be as dispersed as possible and evenly distributed throughout its mass.
The composition of the ointment should not change during application and storage.
The concentration of medicinal substances in the ointment and its mass must correspond to what is written in the prescription.
Eye ointments, in addition, must be sterile, without mechanical impurities. They should not irritate or damage the mucous membrane. The pH value of their aqueous solution should be in the range of 7.3-9.7.
There are several classifications of ointments depending on the place of application, the features of the action and the type of disperse system.
Depending on the place of application, ointments are divided into the following types:
Dermatological (unguenta dermatology, unguenta propria)",
Nasal ointments (unguenta nosales, unguenta rinales);
Eye (unguenta Ophthalmica, Oculenta)",
Dental (unguenta stomatologica);
Vaginal (unguenta vaginales)",
Rectal (unguenta rectales)",
Urethral (unguenta urethrales).
The last three varieties of ointments are usually used with the help of special syringes. The most widely used are dermatological ointments, eye and nasal ointments.
According to the nature of the action, ointments are divided into two groups.
1. Ointments that have a local (local) effect directly on the upper layer of the epidermis of the skin or the surface of the mucous membrane
(for example, dermatol, zinc, xeroform and other ointments used to treat dermatitis, eczema and other skin diseases).
2. Ointments of resorptive action, penetrating deeply into the skin or mucous membrane, reaching the bloodstream and lymph and having a general effect on the entire body or individual organs.
An example of this kind of ointment is Nitrong ointment containing a 2% oil solution of nitroglycerin. It is used to prevent angina attacks. The ointment is applied to the skin of the chest, abdomen or arms, smearing with a thin layer. For better absorption, the lubricated skin area is covered with an impermeable material (polyethylene film). The effect usually occurs within 30-40 minutes and persists for 3-6 hours.
Depending on the type of dispersed system, homogeneous and heterogeneous ointments are distinguished.
Homogeneous ointments are characterized by the absence of an interfacial interface between medicinal substances and the base. In such ointments, medicinal substances are distributed in the base according to the type of solution, i.e. brought to molecular or micellar fineness. Depending on the method of preparation, these can be ointments-alloys, ointments-solutions and extraction ointments.
Heterogeneous ointments are characterized by the presence of an interfacial surface between medicinal substances and the base. Depending on the distribution of medicinal substances in the base, heterogeneous ointments are divided into suspension (trituration), emulsion and combined.
The following requirements are imposed on the bases of ointments:
Soft texture;
Compliance with the purpose of the appointment;
Physical and chemical stability;
Biological harmlessness;
Antimicrobial stability;
Neutral reaction;
Absence of allergenic, irritating and sensitizing action;
Ease of removal from the application site.
The soft consistency of the base is necessary for the convenience of applying the ointment to the skin and mucous membranes. The chemical inertness of the base guarantees the absence of its interaction with medicinal substances, as well as changes under the influence of external factors (air, light, moisture, temperature) and, therefore, ensures the physicochemical stability of the ointment. The absence of an allergenic, irritating and sensitizing effect of the ointment largely depends on the biological safety of its base.
It is also important that the bases of ointments do not violate the physiological functions of the skin (heat, moisture, gas exchange). It is known that the outer layer of the skin (epidermis) normally has an acidic reaction, which prevents the reproduction of microorganisms. Therefore, the requirement of neutrality of ointment bases, maintaining the original pH value of the skin are of great importance. The presence of microorganisms can be the cause of re-infection of inflamed skin and mucous membranes, as well as a decrease in the activity of drug exposure and changes in the consistency of ointments.
Of great practical importance is the question of the ease of removing the remnants of the ointment from linen, the surface of the skin, especially from its hairy areas. The properties of the base must correspond to the purpose of the ointment. Bases for surface-acting ointments should not contribute to the deep absorption of medicinal substances. The bases for resorptive ointments, on the contrary, should ensure the absorption of medicinal substances through the stratum corneum of the skin, as well as through the hair follicles, sebaceous and sweat glands. Bases for protective ointments should dry quickly and fit snugly to the surface of the skin.
All ointment bases are divided into three groups:
Lipophilic;
hydrophilic;
Lipophilic-hydrophilic (diphilic).
Lipophilic bases are chemically heterogeneous substances with pronounced hydrophobicity. The group of lipophilic bases includes fats and their derivatives, waxes, hydrocarbons and silicone bases.
Fats and their derivatives are triglycerides of fatty acids, similar in properties to the fatty secretions of the skin. In addition to esters, fats contain a small amount of unsaponifiable components, among which free fatty acids, sterols (cholesterol - in animal fats, phytosterol - in vegetable fats) are usually found. Fat bases are insoluble in water, sparingly soluble in ethanol, freely soluble in ether, chloroform.
Pork fat (Adeps su il lus, Axungia porcina) is a mixture of triglycerides of palmitic, stearic, oleic and linoleic acids. Ointments prepared with pork fat are well absorbed
skin. They are easily washed off the skin, hair, linen with soapy water. The low chemical stability of pork fat, as well as its value as a food product, has sharply reduced the use of pork fat as an ointment base.
Vegetable oils (Olea pingua) - sunflower (Oleum Helianthi), peach (Oleum Persicorum), almond (Oleum Amygdalärum) and others are characterized by a high content of glycerides of unsaturated acids. They, like pork fat, penetrate the epidermis of the skin, while ensuring good absorption of medicinal substances from liniments and ointments. Due to the liquid consistency, vegetable oils are used as a base only in liniment technology; in other ointments they are used as additives to the bases.
Hydrogenated fats are semi-synthetic products obtained by catalytic hydrogenation of vegetable oils. In this case, unsaturated glycerides become saturated. Liquid oils, depending on the degree of hydrogenation, change the liquid consistency to soft and solid. Hydrogenated fat from refined vegetable oils is used - lard, or hydrofat (Adeps hydrogenisatus), similar in properties to pork fat, but of a denser consistency. Alloys of hydrofat (80-90%) with vegetable oil (20-10%) and combined fat (Adeps composite) are proposed - an alloy of hydrofat (55%), vegetable oil (30%) and beef or pork fat (15%), which has a soft consistency. Hydrogenated fats, unlike other fats, are more stable during storage.
Waxes are esters of fatty acids and higher monohydric alcohols. As components of the bases, beeswax and spermaceti are used.
Beeswax (Cega) is a hard, brittle mass of dark yellow (Cega flava) or yellowish-white or white (Cera alba), granular on fracture, melting at a temperature of 63-65 °C. Due to the presence of free alcohols, beeswax has little emulsifying power. It is insoluble in water, ethanol; partially
soluble in ether, chloroform, fatty oils. Beeswax is chemically inert, fuses well with fats, hydrocarbons and is mainly used to seal ointment bases.
Spermaceti (Ce(aceit) is an ester of cetyl alcohol and fatty acids (palmitic, stearic, etc.). A solid, greasy to the touch crystalline mass, melting at a temperature of 42-54 ° C. Spermacet easily fuses with fats, hydrocarbons, giving them peculiar slipperiness and the ability to absorb aqueous liquids, in connection with which it is used in the technology of creams, cosmetic ointments.Spermaceti is also used to seal soft ointment bases.
Lanolin (LapoChpit anNus1psit, Aceps Lapae) is a fat-like substance that is obtained from the washing waters of sheep's wool. It is a thick, viscous mass of yellow-brown color, with a peculiar smell, melting at a temperature of 36-42 ° C. The composition of lanolin is very complex and has not been fully studied to date. Basically, it is a mixture of esters of macromolecular alcohols (cholesterol, isocholesterol, etc.) with higher fatty acids (myristic, palmitic, cerotinic, etc.) and free macromolecular alcohols. According to its properties, lanolin is close to human sebum. In chemical terms, it is quite inert, neutral, stable during storage. The most valuable property of lanolin is its ability to emulsify approximately 180-200% (of its own weight) of water, 140% of glycerol and 40% of ethanol (70% concentration) to form a water/oil type emulsion. Adding a small amount of lanolin to fats and hydrocarbons increases their ability to mix with water and aqueous solutions. This led to the widespread use of lanolin in the composition of lipophilic-hydrophilic bases. High viscosity, stickiness, unpleasant odor, as well as allergic reactions caused by it in some patients, make lanolin unsuitable as an ointment base. It is usually used in combination with other bases. If, in accordance with the instructions of the State Pharmacopoeia, the prescription contains Lanoum,
release Lanolinum hydricum, which is a mixture of 70 parts of anhydrous lanolin and 30 parts of water. Anhydrous lanolin is used in ointment technology only if it is prescribed.
Hydrocarbons are products of oil refining, of which vaseline, paraffin, vaseline oil, petrolat, ozokerite, ceresin are used as bases. They are characterized by chemical stability, inertness. These qualities, as well as availability, low cost, are the reason for their wide use in the technology of ointments.
Vaseline (Vaselinum) is a mixture of liquid, semi-liquid and solid saturated hydrocarbons with the number of carbon atoms from 7 to - 35. In appearance, it is a homogeneous, thread-stretching mass of white (Vaselinum album) or yellow (Vaselinum flavum) color. Both varieties of Vaseline are equivalent. Depending on the oil from which petroleum jelly is obtained, its melting point ranges from 37-50 °C. Vaseline is insoluble in water, slightly soluble in ethanol, soluble in ether, chloroform, miscible in all proportions with fats, fatty oils (except castor) and waxes. Vaseline is not absorbed by the skin and mucous membranes, slowly and incompletely releases medicinal substances, so it is advisable to use it for the preparation of ointments that act superficially. Some undesirable properties of petroleum jelly should be borne in mind: a possible violation of the physiological functions of the skin (heat, moisture, gas exchange), poor rinsability from the skin, linen, hair. In some cases, vaseline has an allergenic and sensitizing effect.
Petrolat (Petrolatum) is a refractory analogue of petroleum jelly (melting point above 60 ° C). It is used as a sealant for soft vaseline bases.
Solid paraffin (Paraffmum solidum) - a mixture of high molecular weight hydrocarbons. White, oily to the touch crystalline mass melts at a temperature of 50-57 °C. Paraffin is used to seal soft bases, as well as to protect the ointment from melting in hot climates.
Vaseline oil (Oleum Vaselini) is chemically similar to vaseline. Vaseline oil is used as an auxiliary substance to facilitate the dispersion of medicinal substances administered in suspension-type ointments.
Silicone bases can be obtained by fusing polyorganosiloxanes with petroleum jelly, paraffin, ceresin, vegetable and animal fats. Polyorganosiloxane liquids ("Esilon-4", "Esilon-5") are an essential component of silicone bases. Another way is to thicken silicone fluids with aeroside or other fillers. An aerosil base consisting of 84 parts of Esilon-5 and 16 parts of aerosil has been developed and proposed for use. This is a highly viscous colorless gel, the structure of which is destroyed by stirring, but then restored again (the phenomenon of thixotropy). The base has a neutral or slightly acidic reaction, close to the pH value of the skin (pH 5.0-7.0), does not have an irritating and allergenic effect. The undoubted advantage of the aerosil base is its chemical inertness and physiological stability. Esilon-aerosil base does not go rancid during long-term storage and does not delaminate. This base, being anhydrous, provides local surface action and chemical stability of medicinal substances that are hydrolyzed in the presence of water.
hydrophilic bases. A feature of hydrophilic bases is the ability to dissolve in water or mix with it. This makes it possible to introduce significant amounts of aqueous solutions of medicinal substances into hydrophilic bases, ensuring their high resorption from ointments. Some of these bases form elastic films on the skin. Hydrophilic bases do not leave greasy marks and are easily washed off from the skin and linen.
The disadvantage of water-containing hydrophilic bases is low resistance to microbial contamination. The group of hydrophilic bases includes gels of high molecular weight carbohydrates and proteins, synthetic high molecular weight compounds, and inorganic substances.
Sources for obtaining gels of high molecular weight carbohydrates and proteins are starch, cellulose ethers, gelatin, collagen.
The ancestor of these bases is starch gels. Starch-glycerin gel, or glycerin ointment, is a 7% starch solution prepared with glycerin. Colorless, transparent, homogeneous, viscous mass, easily distributed on the mucous membranes and skin. The low stability of glycerin ointment due to syneresis (stratification) and the impossibility of long-term storage are the reasons for the sharp reduction in the use of this base in pharmacy practice.
Of the cellulose ethers, methylcellulose (MC) and sodium carboxymethylcellulose (sodium CMC) have found use as ointment bases. The most widely used are 5-7% aqueous solutions of MC, which are viscous structured gels. When dried, MC solutions form elastic films on the skin, which is the basis for their use in the technology of protective ointments.
Sodium-CMC gels (most often 4-6% concentration) are prepared by heating, sometimes with the addition of gelatin. They are transparent, colorless, but due to the alkaline environment (pH 6.5-8.0) they can change the acid reaction of the skin epidermis, which should be taken into account when making ointments on sodium-CMC gel. It should be borne in mind that MC and sodium-CMC are incompatible with certain medicinal substances: resorcinol, tannin, iodine solutions, salts of heavy metals, etc.
It has been established that sodium-CMC gels, in contrast to lipophilic bases, have a high osmotic activity, and therefore they contribute to the rejection of necrotic masses, cleanse the wound, absorbing the wound discharge.
Gelatin gels are used in the form of gelatin-glycerin bases, which contain 1-3% gelatin, 10-30% glycerol and 70-80% water. It is a clear, light yellow gel that liquefies easily when rubbed into the skin. Gelatin gels are used to obtain protective ointments, the so-called skin adhesives, which solidify on the skin in the form of a strong elastic film. Gelatin gels are applied to the skin in molten form with a brush. The disadvantage of gelatin bases is the ability to syneresis and low resistance to microbial contamination.
A lot of work is being done on the introduction into practice in the form of collagen gels. Collagen powder obtained in the process of low-temperature dispersion, when mixed with water at a concentration of 2-5%, swells, forming a viscous colorless gel, which can be used as an ointment base. Collagen provides resorption and utilization of the base, stimulates the regeneration of damaged tissues. In terms of the completeness of the release of medicinal substances, the soft base is several times superior to the mixture of vaseline with lanolin and other bases.
The main representative of the gels of inorganic compounds are the bases of clay minerals - bentonite bases.
Bentonite gel spreads easily on the skin, but dries quickly. To reduce dryness, up to 10% glycerin is added to the composition of bentonite gels. The best known is the bentonite base, containing 13-20% bentonite, 10% glycerin, 70-77% water. Bentonite bases are distinguished by chemical inertness, emulsifying properties, absorb skin exudates well, and eliminate unpleasant odors.
Lipophilic-hydrophilic bases. These are artificially created compositions of various composition that have both lipophilic and hydrophilic properties. Both water- and fat-soluble substances, aqueous solutions of medicinal substances can be easily introduced into them. Lipophilic-hydrophilic bases, unlike hydrocarbon bases, provide high resorption of medicinal substances from ointments, without interfering with gas and heat exchange of the skin, maintain their water balance, have good consistency properties, lipophilic-hydrophilic bases are the most promising bases. Among them, there are absorption and emulsion ointment bases. As a mandatory component, they include an emulsifier - surfactant.
Absorption ointment bases are anhydrous compositions of lipophilic bases with surfactants that have the ability to incorporate the aqueous phase to form a water/oil type emulsion system. The composition of absorption ointment bases most often includes mixtures of vaseline, vaseline oil, ceresin and other hydrocarbons with emulsifiers. Surfactants that are part of the absorption bases, as a rule, enhance the therapeutic activity of ointments. Adsorption bases are used for the preparation of emulsion ointments, ointments with medicinal substances, which undergo hydrolysis in the presence of water.
Emulsion is called multicomponent ointment bases, which differ from absorption ones in that they contain water in their composition. They can be of two types: oil/water and water/oil. This makes it possible to introduce medicinal substances into both the aqueous and oil phases. Emulsion ointment bases are of great interest due to their ability to dramatically increase skin resorption of medicinal substances that make up ointments. This is due to the presence of a surfactant emulsifier in the base. In addition, the emulsified aqueous phase, when rubbed, is introduced into the excretory ducts of the sebaceous and sweat glands, which facilitates absorption. Emulsion types of water/oil, applied to the skin in a thick layer, promote maceration and warming of the skin, which causes superficial blood circulation and also promotes the absorption of medicinal substances. Ointments prepared on emulsion bases are characterized by low viscosity and low adhesive properties, they are easily applied to the skin and mucous membranes.
Alcohols have a high emulsifying ability: lauryl (C12H25OH), cetyl (C| 6 HszOH), stearyl (C 8 H 3 sOH). Their introduction into the bases in an amount of 5-10% allows incorporating approximately 50% of water or aqueous solutions of medicinal substances. A very promising emulsifier for lipophilic-hydrophilic bases, stabilization of emulsions, suspensions, liniments is lauryl sulfate-sodium salt of sulfuric acid dodecyl ester.
Esters of polyhydric alcohols. This group of emulsifiers primarily includes derivatives of polymerized glycerol - emulsifiers T-1 and T-2, used in the production of margarine. Emulsifier T-1 - a mixture of diglycerin mono- and distearate. Emulsifier T-2 is a product of esterification of stearic acid with triglycerin (triglycerol distearate). Solid waxy mass of yellow or light brown color with the smell of stearin melts at a temperature of 40 °C. Emulsifier T-2 is used not only in lipophilic-hydrophilic ointment bases, but also as a stabilizer and plasticizer in the technology of emulsion, liniments and suppositories.
Derivatives of anhydrosorbitol and oleic acid - sorbitanoleate; pentaerythritol and oleic acid - pentode. Good emulsifying properties of these emulsifiers, biological safety, absence of irritating effect on the skin led to their widespread use in cosmetic creams.
Zhirosugar - incomplete esters of higher fatty acids and sucrose. Zhirosugar is currently used in the food industry, the production of cosmetics. They can be successfully used in the technology of ointments, liniments.
The production of ointments is carried out according to certain rules. Drugs that are insoluble or hardly soluble in ointment bases are first converted into the finest powder and triturated with a small amount of the appropriate liquid (vaseline oil, fatty oil, water) or melted base, and then the rest of the base is added, bringing to the required mass. Medicines that are highly soluble in water are mixed with the base, after dissolving them in a minimum amount of water. Easily soluble in the ointment base, fats and fatty oils, the products are first triturated with a small amount of oil or dissolved in a small amount of the molten base, and then the rest of its amount is added. Volatile substances are introduced into the composition of ointments last.
Rules for writing prescriptions for ointments
To prescribe an ointment, it is necessary to know the current concentration of the drug, its total amount (30-100 g for dermatological ointments and 5-20 g for eye ointments) and prescriptions (main, official, expanded and abbreviated ^).
Ointments are prescribed in abbreviated and expanded words. If the doctor did not indicate the concentration of the drug, then the ointment is prepared with a 10% concentration (with the exception of poisonous and potent drugs).
A simple ointment is prescribed in abbreviated terms indicating the percentage concentration (the first number shows the concentration of the drug in percent, the second - the total amount of ointment).
First, the name of the dosage form is written - Unguentum (Ung.) And the medicinal substance, then the percentage concentration and amount of ointment are indicated. This is followed by an appeal to the pharmacist - "Da" (abbreviation D.) - "issue" and the signature (S.) (indicates the method of applying the ointment).
An example of an official recipe
Exercise
Write out 10 g of ointment "Oksizon" Yar.: 11! Shch. "Ohuzopit" 10.0 for application to the affected 0.5. On the affected
skin patches 3 times a day skin patches 3 times
“The ointments that are prepared on petroleum jelly are abbreviated.
| The peculiarity of this prescription is that it is official, therefore, it does not indicate the percentage of substances. This is an ointment consisting of several components. A full (expanded) recipe is a recipe, in |
This is a complex ointment, so the prescription is written in expanded words. First, the name of the substance contained in the smallest dose of either a potent or poisonous substance is written, then other ingredients. Vaseline is chosen as an ointment base, if it is not specified. This is followed by an instruction to the pharmacist - Misce fiant unguentum (M. f. ung.) - to mix to make an ointment.
Rules for the use of ointments
Wash your hands, rinse and dry the place of application of the ointment. Squeeze out the prescribed amount of ointment, rub it in. Remove excess ointment with a swab.
Eye ointment.
1. Wash your hands, do not touch any objects with the tip of the tube.
2. Tilt your head back, take the tube in your hand, pull the lower eyelid with the other hand, making a “groove”. Bring the tip of the tube to the groove and squeeze out the prescribed amount of ointment.
3. Close the eye for 2 minutes, remove the excess ointment with a cotton or gauze swab.
4. Wipe the tip of the tube with another swab.
Vaginal ointment, cream, gel (most of these dosage forms are sold with an applicator).
1. Wash your hands.
2. Remove the cap from the tube, screw the applicator to the tube, squeeze out the prescribed amount of the drug from the tube into the applicator, disconnect the applicator from the tube, holding the piston.
3. Apply a little cream to the outside of the applicator.
4. Take a position lying on your back, bend your knees and push them apart.
5. Carefully insert the applicator into the vagina (as deep as possible, but without force). Holding the outer part of the applicator with the other hand, press the plunger, thus introducing the drug into the vagina.
6. Remove the applicator from the vagina and discard it if it is intended for single use, if not, then wash thoroughly with boiled water and soap.
Pasta
(im. p. unit h. - Pasta, gen. p. unit h. - Pastae, abbreviation - Past.)
Pastes are varieties of ointments containing at least 25% powdered substances. The amount of powdered substances in pastes usually does not exceed 60-65%. Pastes soften at body temperature.
Pastes are longer than ointments and are held in place. Due to the high content of powdered substances, pastes, unlike ointments, have pronounced adsorbing and drying properties.
Pastes, like ointments, consist of medicinal substances, ointment bases and indifferent powders (thickeners), starch (Amylum), talc (Talcum), white clay (Bolus alba), zinc oxide (Zinci oxydum). Thickeners are added if the amount of powdered substances in the paste is less than
25%. Pastes have a denser pasty consistency. They have some porosity and are therefore permeable to moisture.
Depending on the purpose, dermatological, dental and toothpastes are distinguished. When applied to the skin, pastes stick to it better, are more difficult to erase and last longer than ointments. The peculiarity of the therapeutic effect of pastes lies in their adsorbing and drying properties. Dental pastes are used to introduce into the cavity of a diseased tooth. They consist of various powdered substances that are glued into a doughy mass using glycerin, clove oil or other liquids. Dental pastes are prepared in the form of a fairly dense pasty mass by carefully grinding powdered ingredients and very carefully adding liquids to them.
Pastes are non-dosed dosage forms. They are most often written in expanded cursive. When compiling a prescription for a paste, they proceed from the current concentration of the drug, the percentage of the density of the paste and its total amount (30-100 g, an average of 50 g).
The amount of powdered substances in the paste should be at least 25%. In this case, the paste consists of an equal amount of medicinal substances: anesthesin (5 g), acetylsalicylic acid (5 g), starch (10 g). The total amount of powdered substances in the paste is 20 g (or 40%), which meets the requirements for pastes. By-
the next in the recipe indicate petroleum jelly as an ointment base, then follows the indication to the pharmacist - Misce fiant pasta (M.f.past.) - mix to make a paste.
An example of an official recipe for pasta
Sample execution
Write out 30 g of zinc paste Rp: Past. Zinci 30.0
for application to affected D.S. For affected students
patches of skin
The peculiarity of this prescription is that it is official, therefore, it does not indicate the percentage of the substance, but only the amount of paste.
Suppositories (Suppositoria)
(im. p. unit h. - Suppositorium,
genus. n. pl. h. - Suppositoria, abbreviation - Supp.)
Suppositories are dosage forms that are solid at room temperature and melt or dissolve at body temperature.
There are rectal suppositories (suppositoria recta Na), vaginal (suppositoria vaginalia) and sticks (bacilli) (Fig. 1).
The mass of the rectal suppository (candles) ranges from 1.1-4 g, the length is 2.5-4 cm; the maximum allowable diameter is 1.5 cm. If the weight of the candle is not indicated in the recipe, then it should be 3 g. For children, the weight of the candle must be indicated in the recipe. Rectal suppositories can be in the form of a cone, a cylinder, with a pointed end, a cigar.
The mass of the vaginal suppository ranges from 1.5-6 g. If the mass of the vaginal suppository is not indicated in the recipe, then it should be 4 g.
The shape of vaginal suppositories can be spherical (balls - globuli), ovoid (ovuli - ovuli) or in the form of a flat body with a rounded end (pessaries - pessariä).
The sticks are cylindrical in shape with a pointed end. The size of the sticks must be specified in the recipe. As a rule, their diameter is 2-5 mm; the length reaches 12 cm. The sticks are intended for insertion into fistulas, etc.
It is believed that in terms of the speed of "delivery" of medicinal substances, suppositories can compete with dosage forms for injections. Due to the fact that the medicinal substances contained in suppositories enter directly into the bloodstream, bypassing the liver, it is necessary to check their doses in suppositories.
GF XI sets out the requirements for suppositories.
A description of the form is given and the mass of vaginal and rectal suppositories is indicated (fluctuations in mass should not exceed 5%). Suppositories must have a certain hardness (mechanical strength), since when administered they have to overcome the resistance of tissues or sphincters. Suppositories should melt at body temperature. The time of complete deformation of the suppositories was determined - 3-15 minutes. The suppository mass should
be homogeneous, on the cut - without inclusions, marbling, sparkles.
As bases for suppositories, cocoa butter, vegetable and hydrogenated fats and their alloys with wax, spermaceti, deresined ozokerite, hard paraffin and various emulsifiers are used; lanol, gelatin-glycerin and soap-glycerin gels; polyethylene oxides, etc.
The basis of the suppository should be solid and plastic at room temperature, melt or dissolve at body temperature, promote the resorption of drugs by mucous membranes, mix with as many drugs as possible, and be chemically and pharmacologically indifferent. In addition, the base should easily release medicinal substances, not have an irritating effect, and be resistant to light, moisture, air oxygen, and microorganisms.
The bases for suppositories used in pharmaceutical practice can be divided into two groups: hydrophobic and hydrophilic.
Hydrophobic bases include fats and fat-like substances, their alloys with emulsifiers or substances of hydrocarbon origin. The classic basis for this group of suppositories is cocoa butter.
Cocoa butter (Oleum Cacao, Butyrum Cacao) is a dense vegetable fat obtained from the seeds of the chocolate tree. Cocoa butter at room temperature is light yellow in color, has a faint aromatic odor and a pleasant taste. If the base is not specified in the recipe, cocoa butter should be used, as it is the most indifferent, mixes well with most medicinal substances, and is plastic. Cocoa butter has a number of disadvantages. It hardly incorporates water (aqueous solutions); has polymorphism, i.e. after heating and cooling, it changes the melting point, so it is used only for manual formation or rolling out of suppositories.
Hydrophilic include gelatin-glycerin, soap-glycerin, polyethylene oxide bases.
The official recipe for a gelatin-glycerin base: 1 part gelatin, 2 parts water, 5 parts glycerin.
The base is an elastic, easily hardening mass, used mainly for the preparation of vaginal suppositories.
Official prescription of soap-glycerin suppositories for 20 suppositories: glycerin 60 g, sodium carbonate 2.6 g and stearic acid 5 g.
Rules for prescribing suppositories in a prescription
Suppositories are prescribed in three ways: abbreviated, official and expanded in words.
Abbreviated example
Exercise
Write out 20 vaginal Rp.: Supp. Nystatini 250,000 IU N.20 suppositories containing D.S. 1 suppository 2 x 250,000 IU of nystatin per day in the vagina
for introduction into the vagina, 1 suppository 2 times a day for candidal vaginitis
First write the name of the dosage form, the medicinal substance, a single dose and the number of suppositories. This is followed by an appeal to the pharmacist and a signature indicating the method, dose and frequency of prescribing the drug.
An example of an official prescription
Sample execution
Write out 10 rectal supp- Rp: Supp. "Anusolum" N.10 positories "Anuzol" for the introduction of D.S. 1 suppository into the rectum 1 2 times a day in the
suppository 2 times a day I wash the intestines
with hemorrhoids
This prescription is official, therefore it does not indicate the dose of the substance in the suppository, but only the number of suppositories.
This prescription is detailed, therefore, it first indicates the medicinal substance and its dose, then the base (But. Cacao in the amount of 3 g for rectal suppositories, 4 g for vaginal suppositories). Next comes the prescription to the pharmacist: Misce fiant suppositorium rectale (A/. / supp. rect.) - mix to make rectal suppositories. Indicate the number of candles (D. t. d. N.10). The signature describes the method of introducing candles and the frequency of their appointment.
Rules for the use of suppositories.
Rectal suppositories:
1. Wash your hands, remove the wrapper if the suppositories are not too soft. If the suppositories are too soft, cool 1 suppository in the refrigerator or under running cold water without removing the shell, and then remove it.
2. Remove possible sharp protrusions by warming the suppository in your hands; soak it in cold water.
3. Take a position lying on your side, pull your knees up to your stomach.
4. Carefully insert the suppository with the rounded end forward into. anus.
5. Do not get up for 2-5 minutes.
6.Wash your hands. Do not empty your bowels for 1 hour.
Vaginal suppositories:
]. Wash hands, remove wrapper.
2. Take a supine position.
3. Slightly bend your knees and push them apart.
4. Carefully insert the suppository into the vagina (as deep as possible, but without force). Remain in this position for 2-5 minutes.
5. Wash your hands.
Plasters (Etriayaia)
(them. p. unit h. - Etriiagigit,
genus. p. units hours - Etriaiїgі, abbreviation - Etri)
Patches - a dosage form for external use, which has the ability to stick to the skin after softening at body temperature. The patches are easily removed from the skin without leaving a trace. This is one of the oldest dosage forms included in all pharmacopoeias of the world. Currently, the nomenclature of patches and their purpose are extremely diverse.
The composition of the patches may include resins, paraffin, wax, salts of higher fatty acids (lead soap), fats, rubber, salts of resin acids (zinc resinate), lanolin, petroleum jelly, ceresin, volatile solvents (ether, ethanol) and various medicinal substances. The combination of these substances gives the plasters the necessary structural and mechanical properties, providing the ability to gradually soften, stay on the skin and have a therapeutic effect.
The patches are produced in the form of a mass applied in a thin layer on a cloth (paper), or packaged in the form of tiles, sticks, cylinders, as well as in the form of a liquid poured into vials, placed in aluminum tubes or aerosol cans. Thus, depending on the state of aggregation, they can be solid and liquid. Hard patches are firm, non-staining at room temperature and soften and sticky at body temperature. Liquid
patches (skin adhesives) - liquids that leave a film on the skin after evaporation. Depending on the degree of dispersion of the mass, plasters can be alloys, solutions, suspensions, emulsions or combined systems.
Depending on the medical purpose, patches are divided into epidermal, endermatic and diadermatic. Epidermal patches have the necessary stickiness. They may not contain medicinal substances. Epidermal patches are used as dressings, to strengthen dressings, to bring wound edges together, to hide skin defects, to protect it from traumatic environmental factors, and to treat certain skin diseases. When an epidermal patch is applied, due to the cessation of gas, moisture and heat exchange, the skin under the patch softens, local blood circulation increases, and resorption processes improve. Endermatic patches contain medicinal substances (keratolytic, depilatory, etc.) in their composition. They are used in the treatment of skin diseases. Diadermic patches contain drugs that penetrate the skin and have an effect on deep-lying tissues or a general (resorptive) effect.
According to the composition of the masses, the plasters are classified into resin-wax, lead and liquid.
Liquid plasters are volatile liquids that leave an elastic, sticky, durable film on the skin after the solvent has evaporated. Liquid patches, or skin adhesives, are used as dressings to fix surgical dressings on the skin and treat minor skin lesions (abrasions, scratches). The adhesive film is formed using substances such as collodion, rosin, polymeric materials (ethylcellulose, vinylpyrrolidone-vinyl acetate copolymer, polymethacrylates and acrylates, etc.).
In recent years, liquid plasters in the form of aerosols have found wide application in medical practice. Film-forming compositions by spraying are applied during the primary treatment of small damage
of skin obtained at home and at work, in inpatient and outpatient treatment in gynecology, dermatology, and surgery.
Rules for prescribing patches
The patches are prescribed in a piece (with indication of the dose) or spread on canvas, calico, silk or other material (indicating the size of the patch in centimeters), as well as in the form of a solution (indicating the concentration and volume), which is then applied to any material. or the patient's skin.
An example of a patch
 |
Sample execution
Rules for the use of transdermal patches.
1. Find out from the annotation the place of application of the patch.
2. Do not use the patch on damaged areas of the skin, and do not stick it on skin folds or places that are in close contact with clothing.
3. Regularly change places of application. Hands must be clean and dry.
4. Wipe and dry the patch area.
5. Remove the cover covering the patch without touching the therapeutic side of the patch. Place the patch on the skin and press firmly. For a tighter adhesion, press the edges of the patch.
6. Remove and replace the patch according to the instructions for use of medicinal products.
Linimentae (Linimentae)
(the name of the unit of hours is Linimentum; the genus of the unit of hours is Linimenti; the abbreviation is Linim)
Liniment is a dosage form for external use, which is a thick liquid or gelatinous mass that melts at body temperature. In physicochemical terms, liniments are free dispersed systems of varying degrees of homogeneity, which makes it possible to distinguish between homogeneous (liniments-solutions), emulsion and suspension liniments.
Homogeneous liniments are either liquid transparent mixtures of mutually soluble ingredients - fatty oils (almond, peach, linseed, sunflower, etc.), chloroform, methyl salicylate, ammonia solution, alcohols and alcohol solutions or translucent homogeneous gelatinous mixtures (soaps in alcohol). The composition of homogeneous liniments also includes solid drugs (menthol, camphor, anestezin, etc.). Emulsion liniments - two-phase emulsions such as oil in water (O / W) or water in oil (W / O), usually consisting of a mixture of fatty oils with alkalis (usually ammonia solution); emulsifiers are formed during the interaction of soap.
To obtain liniment, vegetable oils are often used (sunflower oil - Oleum Helianthi, linseed oil - Oleum Lini, olive oil - Oleum Olivarum, castor oil - Oleum Ricini) and cod fish oil (Oleum jecoris Aselli). Cod fish oil is better than sunflower oil, it is absorbed by the skin and softens it.
In addition, due to the content of vitamins in it, it also exhibits a therapeutic effect.
Suspension liniments are thin suspensions of insoluble powdery substances (the smallest powders of zinc oxide, starch, etc.) in water, glycerin, oils and other liquids; for their formation, the addition of emulsifiers is necessary.
Liniments are produced in the form of finished dosage forms by pharmaceutical factories, if necessary, they are also prepared in pharmacy conditions.
Liniments can be used in the form of aerosol preparations, which, when sprayed, form plastic films at the application site. Such dosage forms do not injure the affected skin, mucous membranes, wound surface.
