Acyclovir forte helps. Acyclovir forte - description of the drug, instructions for use, reviews. Description of the active components of the drug "Acyclovir"
Treatment of infections of the skin and mucous membranes caused by Herpes simplex viruses type I and II, both primary and secondary, including genital herpes. - Prevention of exacerbations of recurrent infections caused by Herpes simplex viruses type I and II in patients with normal immune status. - Prevention of primary and recurrent infections caused by Herpes simplex viruses type I and II in patients with immunodeficiency. - As part of complex therapy for patients with severe immunodeficiency: with HIV infection (stage of AIDS, early clinical manifestations and detailed clinical picture) and in patients who have undergone bone marrow transplantation. - Treatment of primary and recurrent infections caused by the Varicella zoster virus (chickenpox, as well as herpes zoster).
Pharmacotherapeutic group
Antiviral drug.
Pharmacological property
An antiviral drug, a synthetic analogue of an acyclic purine nucleoside, which has a highly selective effect on herpes viruses. Inside virus-infected cells, under the influence of viral thymidine kinase, a series of sequential reactions of transformation of acyclovir into mono-, di- and triphosphate of acyclovir takes place. Acyclovir a triphosphate is integrated into the viral DNA chain and blocks its synthesis through competitive inhibition of viral DNA polymerase. In vitro, acyclovir is effective against the herpes simplex virus - Herpes simplex types I and II, against the Varicella zoster virus; higher concentrations are required to inhibit Epstein-Barr virus.
Contraindications
Hypersensitivity to acyclovir, ganciclovir or any excipient of the drug. - Taking the drug is contraindicated during lactation. - Children under 3 years of age (for this dosage form). - Galactose intolerance, lactase deficiency, glucose-galactose malabsorption. With caution: Pregnancy; elderly people and patients receiving large doses, especially due to dehydration; renal dysfunction; neurological disorders or neurological reactions to taking cytotoxic drugs (including in history).
Application
Inside. The drug is taken during or immediately after a meal and washed down with a sufficient amount of water. The dosage regimen is set individually depending on the severity of the disease. For the treatment of infections of the skin and mucous membranes caused by Herpes simplex type I and II: Adults: the drug is prescribed 200 mg 5 times a day for 5 days at 4-hour intervals during the day and at 8-hour intervals at night. In more severe cases of the disease, the course of treatment can be extended as prescribed by a doctor to 10 days. As part of complex therapy for severe immunodeficiency, including with a full-blown clinical picture of HIV infection (including early clinical manifestations of HIV infection and the stage of AIDS), after bone marrow implantation, 400 mg is prescribed 5 times a day. To prevent relapses of infections caused by Herpes simplex viruses type I and II, patients with normal immune status and in case of relapse of the disease are prescribed 200 mg 4 times a day every 6 hours, course duration is from 6 to 12 months. For the prevention of infections caused by Herpes simplex viruses type I and II in adults with immunodeficiency, the drug is recommended to be prescribed 200 mg 4 times a day every 6 hours, the maximum dose is up to 400 mg of acyclovir 5 times a day, depending on the severity of the infection. Children: For Herpes simplex infection and prevention of this infection in patients with weakened immune defenses, children over 3 years of age receive the same dose as adults. For the treatment of infections caused by Varicella zoster: Adults: the drug is prescribed 800 mg 5 times a day every 4 hours during the day and at 8-hour intervals at night. The duration of treatment is 7-10 days. Children: for chickenpox, prescribe 20 mg/kg 4 times a day for 5 days (maximum single dose 800 mg), children from 3 years to 6 years: 400 mg 4 times a day, over 6 years: 800 mg 4 times per day for 5 days. When treating infections caused by Herpes zoster, adults are prescribed 800 mg 4 times a day every 6 hours for 5 days. In patients with impaired renal function: When treating and preventing infections caused by Herpes simplex, in patients with creatinine clearance less than 10 ml/min, the dosage of the drug should be reduced to 200 mg 2 times a day at 12-hour intervals. When treating infections caused by Varicella zoster in patients with creatinine clearance less than 10 ml/min, it is recommended to reduce the dosage of the drug to 800 mg 2 times a day at 12-hour intervals; with creatinine clearance up to 25 ml/min, 800 mg is prescribed 3 times a day at 8-hour intervals.
Side effects
The drug is usually well tolerated. - From the gastrointestinal tract: in isolated cases - abdominal pain, nausea, vomiting, diarrhea. - In the blood: transient slight increase in the activity of liver enzymes, rarely - a slight increase in urea and creatinine levels, hyperbilirubinemia, leukopenia, erythropenia. - From the central nervous system: rarely - headache; weakness; in some cases, tremor, dizziness, increased fatigue, exhaustion, drowsiness, insomnia, paresthesia, confusion, hallucinations, decreased concentration, agitation. - Allergic reactions: anaphylactic reactions, skin rash, itching, Lyell's syndrome, urticaria, erythema multiforme, incl. Stevens-Johnson syndrome, fever. - Other: rarely - alopecia, peripheral edema, blurred vision, lymphadenopathy, myalgia, malaise.
tab. 400 mg: 10, 20 or 30 pcs. Reg. No.: LSR-007061/09
Clinical and pharmacological group:
Antiviral drug
Release form, composition and packaging
10 pieces. - contour cellular packaging (1) - cardboard packs.
10 pieces. - contour cell packaging (2) - cardboard packs.
10 pieces. - contour cell packaging (3) - cardboard packs.
Description of the active components of the drug " Acyclovir»
pharmachologic effect
Antiviral agent. Thymidine kinase in virus-infected cells actively converts acyclovir through a series of sequential reactions into acyclovir mono-, di- and triphosphate. The latter interacts with the viral DNA polymerase and is integrated into the DNA that is synthesized for new viruses. Thus, “defective” viral DNA is formed, which leads to suppression of the replication of new generations of viruses.
Acyclovir is active against Herpes simplex virus types 1 and 2, Varicella zoster virus, Epstein-Barr virus and cytomegalovirus.
Indications
For systemic use (orally and intravenously): infections caused by Herpes simplex viruses types 1 and 2 and Varicella zoster; prevention of infections caused by Herpes simplex and Varicella zoster viruses (including in patients with reduced immunity); as part of complex therapy for severe immunodeficiency (including the clinical picture of HIV infection) and in patients who have undergone bone marrow transplantation; prevention of cytomegalovirus infection after bone marrow transplantation.
For topical use in ophthalmology: keratitis and other eye lesions caused by the Herpes simplex virus.
For external use: skin infections caused by Herpes simplex and Varicella zoster viruses.
Dosage regimen
Orally for adults and children over 2 years old - 200-400 mg 3-5 times a day, if necessary - 20 mg/kg (up to 800 mg per dose) 4 times a day. In children under 2 years of age, use a dose equal to half the dose for adults. Duration of treatment is 5-10 days. In case of renal failure, adjustment of the dosage regimen is recommended.
IV drip for adults and children over 12 years old - 5-10 mg/kg, interval between injections - 8 hours. Children aged 3 months to 12 years - 250-500 mg/m 2 body surface, interval between injections - 8 hours. For newborns, the dose is 10 mg/kg, the interval between doses is 8 hours.
Apply locally and externally 5 times a day. The dose and duration of treatment depend on the indications and dosage form used.
Maximum doses: for adults with intravenous administration - 30 mg/kg/day.
Side effect
When taken orally: nausea, vomiting, diarrhea, abdominal pain, skin rash, headache, dizziness, fatigue, decreased concentration, hallucinations, drowsiness or insomnia, fever; rarely - hair loss, transient increase in blood concentrations of bilirubin, urea, creatinine, liver enzyme activity, lymphocytopenia, erythropenia, leukopenia.
With intravenous administration: acute renal failure, crystalluria, encephalopathy (confusion, hallucinations, agitation, tremor, convulsions, psychosis, drowsiness, coma), phlebitis or inflammation at the injection site, nausea, vomiting.
For local use: burning sensation at the application site, superficial punctate keratitis, blepharitis, conjunctivitis.
For external use: at the site of application, a burning sensation, skin rash, itching, peeling, erythema, dry skin are possible; upon contact with mucous membranes - inflammation.
Contraindications
Hypersensitivity to acyclovir and valacyclovir; with intravenous administration - lactation (breastfeeding).
Pregnancy and lactation
The use of acyclovir during pregnancy is possible in cases where the expected benefit to the mother outweighs the potential risk to the fetus.
IV use of acyclovir during lactation is contraindicated (excreted in breast milk).
IN experimental studies Animal studies have shown that acyclovir penetrates the placental barrier.
Use for renal impairment
In case of renal failure, adjustment of the dosage regimen is necessary.
Use in old age
Application for children
Orally for children over 2 years old - 200-400 mg 3-5 times a day, if necessary - 20 mg/kg (up to 800 mg per dose) 4 times a day. In children under the age of 2 years, use at a dose equal to half the adult dose. The duration of treatment is 5-10 days.
special instructions
It should be taken into account that when using acyclovir, acute renal failure may develop due to the formation of sediment from acyclovir crystals, which is especially likely with rapid intravenous administration, simultaneous use of nephrotoxic drugs, in patients with impaired renal function and with insufficient water load.
When using acyclovir, it is necessary to monitor renal function (determining the level of urea nitrogen in the blood and creatinine in the blood plasma).
Treatment of elderly patients should be carried out with a sufficient increase in water load and under the supervision of a physician, because in this category of patients, the half-life of acyclovir increases.
When treating genital herpes, you should avoid sexual intercourse or use condoms, because the use of acyclovir does not prevent the transmission of the virus to partners.
Acyclovir in the form of dosage forms for external use should not be applied to the mucous membranes of the mouth, eyes, or vagina.
Drug interactions
Drug interactions
With simultaneous use, probenecid reduces the tubular secretion of acyclovir and thereby increases the plasma concentration and half-life of acyclovir.
With the simultaneous use of acyclovir with nephrotoxic drugs, the risk of developing nephrotoxicity increases (especially in patients with impaired renal function).
An increase in the effect of acyclovir is observed with the simultaneous administration of immunostimulants.
When mixing solutions, it is necessary to take into account the alkaline reaction of acyclovir for intravenous administration (pH 11).
Compound
1 tablet contains:
active substance: acyclovir 400 mg;
Excipients: potato starch, lactose (milk sugar), povidone, sugar (sucrose), sodium lauryl sulfate, magnesium stearate.
Indications for use Acyclovir Forte
Treatment and prevention of infections caused by Herpes simplex viruses types 1 and 2 and Varicella zoster:
- simple herpes of the skin and mucous membranes (primary and recurrent);
- genital herpes (primary and recurrent);
- herpes zoster (shingles);
- chickenpox (in the first 24 hours after the appearance of a typical rash);
- in patients with severe immunodeficiency (including after transplantation, when taking immunosuppressive drugs, in HIV-infected patients, during chemotherapy).
Contraindications to the use of Acyclovir Forte
- hypersensitivity to acyclovir, ganciclovir or components of the drug;
- lactation period (breastfeeding).
- children under 3 years of age.
WITH caution the drug should be prescribed for dehydration, renal failure, neurological disorders, incl. in the anamnesis.
The dosage regimen is set individually depending on the severity of the disease.
In the treatment of infections of the skin and mucous membranes caused by the Herpes simplex virus type 1 and 2,
Acyclovir is prescribed 200 mg 5 times a day for 5 days at intervals of 4 hours during the day and at intervals of 8 hours at night. In more severe cases of the disease, it is possible to increase the course of treatment.
As part of complex therapy for severe immunodeficiency, including with a full-blown clinical picture of HIV infection (including early clinical manifestations of HIV infection and the stage of AIDS), after bone marrow implantation Prescribe 400 mg 5 times a day.
For the prevention of relapse of infections caused by the Herpes simplex virus types 1 and 2, in patients with normal immune status and in case of relapse of the disease Prescribe 200 mg 4 times a day every 6 hours.
To prevent infections caused by Herpes simplex virus types 1 and 2,adults and children over 2 years old
with immunodeficiency, the drug is prescribed 200 mg 4 times a day every 6 hours, the maximum dose is 400 mg 5 times a day.
, adults
Prescribe 800 mg 5 times a day at intervals of 4 hours during the day and at intervals of 8 hours at night. The duration of treatment is 7-10 days. Children over 2 years old
prescribed 20 mg/kg body weight 4 times a day for 5 days, children weighing more than 40 kg
the drug is prescribed in the same dosage as for adults.
In the treatment of herpes zoster (Herpes zoster), adults
appoint 800 mg 4 times / day every 6 hours for 5 days. Children over 6 years old
- 800 mg 4 times a day; 2-6 years
- 400 mg 4 times a day; under 2 years old
- 200 mg 4 times a day. More accurately, the dose can be determined at the rate of 20 mg/kg, but not more than 800 mg 4 times a day. The course of treatment is 5 days.
In patients with severe renal impairment (CK) with treatment and prevention of infections caused by the Herpes simplex virus, the drug is prescribed 200 mg 2 times a day at intervals of 12 hours.
In the treatment of infections caused by the Varicella zoster virus, For patients with CC, the drug is prescribed 800 mg 2 times a day at intervals of 12 hours; at CC from 10 to 25 ml/min- 800 mg 3 times a day at intervals of 8 hours.
The drug should be taken during or immediately after meals and washed down with enough water.
pharmachologic effect
Acyclovir is an antiviral (antiherpetic) agent for external use - a synthetic analogue of thymidine nucleoside, which is a natural component of DNA.
In infected cells containing viral thymidine kinase, phosphorylation occurs and is converted to acyclovir monophosphate. Under the influence of acyclovir guanylate cyclase, monophosphate is converted into diphosphate and, under the action of several cellular enzymes, into triphosphate. High selectivity of action and low toxicity to humans are due to the absence of the necessary enzyme for the formation of acyclovir triphosphate in intact cells of the macroorganism.
Acyclovir triphosphate inhibits the synthesis (replication) of viral DNA by three mechanisms: 1) competitively replaces deoxyguanosine triphosphate in DNA synthesis; 2) “integrates” into the DNA chain being synthesized and stops its elongation; 3) inhibits the DNA polymerase enzyme of viruses. As a result, the reproduction of the virus in the human body is disrupted.
The specificity and very high selectivity of action are also due to its predominant accumulation in cells affected by the herpes virus.
Highly active against Herpes simplex viruses type 1 and 2; the virus that causes chickenpox and herpes zoster (Varicella zoster); Epstein-Barr virus (types of viruses are listed in increasing order of the minimum inhibitory concentration of acyclovir).
Moderately active against cytomegalovirus.
In case of herpes, it prevents the formation of new rash elements, reduces the likelihood of skin dissemination and visceral complications, accelerates the formation of crusts, and reduces pain in the acute phase of herpes zoster. Has an immunostimulating effect.
Side effects of Acyclovir Forte
From the digestive system: in isolated cases - abdominal pain, nausea, vomiting, diarrhea; rarely - transient increase in liver enzyme activity, hyperbilirubinemia.
From the hematopoietic system: rarely - leukopenia, erythropenia.
From the side of the central nervous system: rarely - headache, weakness; in some cases - tremor, dizziness, increased fatigue, drowsiness, hallucinations.
Allergic reactions: skin rash; rarely - allergic dermatitis (when using ointment).
Others: rarely - alopecia, fever, increased levels of urea and creatinine.
special instructions
With caution, Acyclovir should be prescribed to patients with impaired renal function, elderly patients due to an increase in the half-life of acyclovir.
When using the drug, it is necessary to ensure the supply of a sufficient amount of fluid.
The ointment is not recommended to be applied to the mucous membranes of the mouth, eyes, genitals, because. development of the expressed local inflammation is possible.
The effectiveness of treatment when applying the ointment will be the higher, the earlier it is started.
In patients with immunodeficiency, with multiple repeated courses of treatment, viral resistance to acyclovir sometimes develops.
When taking the drug, kidney function should be monitored (blood urea and plasma creatinine levels).
Drug interactions
When used simultaneously with probenecid, the average half-life of acyclovir increases and the clearance of acyclovir decreases.
When taken simultaneously with nephrotoxic drugs, the risk of developing renal dysfunction increases.
Storage conditions
Store in a dry place, protected from light, out of reach of children, at a temperature not exceeding 25°C.
Release form: Solid dosage forms. Pills.
General characteristics. Compound:
Active ingredient: 400 mg of acyclovir.
Excipients: potato starch, lactose (milk sugar), povidone, sugar (sucrose), sodium lauryl sulfate, magnesium stearate.
An antiviral drug with a highly selective effect on herpes viruses.
Pharmacological properties:
Pharmacodynamics. An antiviral drug, a synthetic analogue of an acyclic purine nucleoside, which has a highly selective effect on herpes viruses. Inside virus-infected cells, under the influence of viral thymidine kinase, a series of sequential reactions of transformation of acyclovir into mono-, di- and triphosphate of acyclovir takes place. Acyclovir a triphosphate is integrated into the viral DNA chain and blocks its synthesis through competitive inhibition of viral DNA polymerase.
In vitro, acyclovir is effective against the herpes simplex virus - Herpes simplex types I and II, against the Varicella zoster virus; higher concentrations are required to inhibit Epstein-Barr virus.
Pharmacokinetics. When taken orally, bioavailability is 15-30%. Acyclovir penetrates well into all organs and tissues of the body, including the brain and skin. Plasma protein binding is 9-33% and is independent of its plasma concentration. The concentration in the cerebrospinal fluid is about 50% of its concentration in plasma. Acyclovir crosses the placental barrier and accumulates in breast milk. The maximum concentration after oral administration of 200 mg 5 times a day is 0.7 mcg/ml, the time to reach the maximum concentration is 1.5-2 hours.
Metabolized in the liver to form the pharmacologically inactive compound 9-carboxymethoxymethylguanine. The half-life in adults with normal renal function is 2-3 hours. In patients with severe renal failure, the half-life is 20 hours, with hemodialysis - 5.7 hours (at the same time, the concentration of acyclovir in plasma decreases to 60% of the initial value). About 84% is excreted by the kidneys unchanged and 14% - in the form of a metabolite. The renal clearance of acyclovir is 75-80% of the total plasma clearance. Less than 2% of acyclovir is excreted from the body through the intestines.
Indications for use:
· Treatment of infections of the skin and mucous membranes caused by Herpes simplex viruses type I and II, both primary and secondary, including.
· Prevention of exacerbations of recurrent infections caused by Herpes simplex viruses type I and II in patients with normal immune status.
· Prevention of primary and recurrent infections caused by Herpes simplex viruses type I and II in patients with immunodeficiency.
· As part of complex therapy for patients with severe immunodeficiency: at the stage of early clinical manifestations and a detailed clinical picture) and in patients who have undergone bone marrow transplantation.
· Treatment of primary and recurrent infections caused by the Varicella zoster virus (chickenpox, as well as herpes zoster).
Important! Get to know the treatment
Directions for use and dosage:
Inside. The drug is taken during or immediately after a meal and washed down with a sufficient amount of water.
The dosage regimen is set individually depending on the severity of the disease.
In the treatment of infections of the skin and mucous membranes caused by Herpes simplex types I and II:
Adults: the drug is prescribed 200 mg 5 times a day for 5 days at 4-hour intervals during the day and at 8-hour intervals at night. In more severe cases of the disease, the course of treatment can be extended as prescribed by a doctor to 10 days. As part of complex therapy for severe immunodeficiency, including with a full-blown clinical picture of HIV infection (including early clinical manifestations of HIV infection and the stage of AIDS), after bone marrow implantation, 400 mg is prescribed 5 times a day.
To prevent relapses of infections caused by Herpes simplex viruses type I and II, patients with normal immune status and in case of relapse of the disease are prescribed 200 mg 4 times a day every 6 hours, course duration is from 6 to 12 months.
For the prevention of infections caused by Herpes simplex viruses type I and II in adults with immunodeficiency, the drug is recommended to be prescribed 200 mg 4 times a day every 6 hours, the maximum dose is up to 400 mg of acyclovir 5 times a day, depending on the severity of the infection.
Children: For Herpes simplex infection and prevention of this infection in patients with weakened immune defenses, children over 3 years of age receive the same dose as adults.
When treating infections caused by Varicella zoster:
Adults: the drug is prescribed 800 mg 5 times a day every 4 hours during the day and at 8-hour intervals at night. The duration of treatment is 7-10 days.
Children: for chickenpox, prescribe 20 mg/kg 4 times a day for 5 days (maximum single dose 800 mg), children from 3 years to 6 years: 400 mg 4 times a day, over 6 years: 800 mg 4 times per day for 5 days.
When treating infections caused by Herpes zoster, adults are prescribed 800 mg 4 times a day every 6 hours for 5 days.
In patients with impaired renal function. When treating and preventing infections caused by Herpes simplex in patients with creatinine clearance less than 10 ml/min, the dosage of the drug should be reduced to 200 mg 2 times a day at 12-hour intervals.
When treating infections caused by Varicella zoster in patients with creatinine clearance less than 10 ml/min, it is recommended to reduce the dosage of the drug to 800 mg 2 times a day at 12-hour intervals; with creatinine clearance up to 25 ml/min, 800 mg is prescribed 3 times a day at 8-hour intervals.
Features of application:
Use strictly as prescribed by a doctor to avoid complications in adults and children over 3 years of age. Prescribe with caution to patients with impaired renal function and elderly patients due to an increase in the half-life of acyclovir.
When using the drug, it is necessary to ensure the supply of a sufficient amount of fluid.
When taking the drug, kidney function should be monitored (blood urea and plasma creatinine levels).
Acyclovir does not prevent the sexual transmission of herpes, so during the treatment period it is necessary to abstain from sexual intercourse, even in the absence of clinical manifestations.
Due to the presence of lactose, patients with rare hereditary diseases such as galactose intolerance, lactase deficiency, glucose-galactose malabsorption should not take the drug.
Pregnancy and lactation period. Acyclovir crosses the placental barrier and accumulates in breast milk.
Use during pregnancy is only possible if the expected benefit to the mother outweighs the potential risk to the fetus. If it is necessary to take acyclovir during lactation, interruption of breastfeeding is required.
Side effects:
The drug is usually well tolerated.
From the gastrointestinal tract: in isolated cases - abdominal pain,...
In the blood: transient slight increase in the activity of liver enzymes, rarely - a slight increase in urea and creatinine levels, hyperbilirubinemia, erythropenia.
From the central nervous system: rarely - ; weakness; in some cases, increased fatigue, exhaustion, drowsiness, insomnia, confusion,
An enhanced effect is observed with the simultaneous administration of immunostimulants.
Contraindications:
Hypersensitivity to acyclovir, ganciclovir or any excipient of the drug.
Taking the drug is contraindicated during lactation.
Children under 3 years of age (for this dosage form).
Galactose intolerance, lactase deficiency, glucose-galactose malabsorption.
Carefully. Pregnancy; elderly people and patients receiving large doses, especially against the background of; renal dysfunction; neurological disorders or neurological reactions to taking cytotoxic drugs (including in history).
Overdose:
There have been no reported cases of overdose following oral administration of acyclovir.
Storage conditions:
List B. In a dry place, protected from light, at a temperature not exceeding 25 °C. Keep out of the reach of children. Shelf life - 2 years. Do not use after expiration date.
Vacation conditions:
On prescription
Package:
Tablets 400 mg. 5, 10, 12, 15, 20 or 30 tablets per blister pack. 1, 2 or 3 blister packs with instructions for use are placed in a cardboard pack.
Active substance: acyclovir.