Active substanceAcyclovirAcyclovir
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  • Dosage form: & nbsppills
    Composition:

    Composition per 1 tablet:

    active substance: acyclovir - 200 mg;

    auxiliary substances: potato starch - 66.2 mg, lactose monohydrate (sugar milk) - 119.4 mg, povidone (polyvinylpyrrolidone low molecular weight medical) - 5.6 mg, sucrose (sugar) - 13.2 1 mg, sodium lauryl sulfate - 1.6 mg, magnesium stearate - 3.4 mg, stearic acid - 0.6 mg.

    Description:Ploskotsilindricheskie tablets are white, with a facet and a risk.
    Pharmacotherapeutic group:Antiviral agent
    ATX: & nbsp

    S.01.A.D   Antiviral drugs

    Pharmacodynamics:

    The antiviral drug is a synthetic analogue of the acyclic purine nucleoside, which has a highly selective effect on herpes viruses. In virus-infected cells under the action of viral thymidine kinase, phosphorylation occurs and further sequential transformation of acyclovir into mono-, di-, and triphosphate. Acyclovirtriphosphate is inserted into the viral DNA chain and blocks its synthesis by competitive inhibition of the viral DNA polymerase.

    In vitro - acyclovir Effective against herpes simplex virus - Herpes simplex 1 and 2 types; against the virus Varicella zoster, causing varicella and shingles; higher concentrations are required to inhibit the Epstein-Barr virus. Moderately active against cytomegalovirus.

    In vivo Acyclovir is therapeutically and prophylactically effective especially in viral infections caused by the virus Herpes simplex 1 and 2 types.

    Warns the formation of new elements of the rash, reduces the likelihood of cutaneous dissemination and visceral complications, accelerates the formation of crusts, reduces pain in the acute phase of herpes zoster.
    Pharmacokinetics:

    After oral administration, the bioavailability is 15-30%, and dose-dependent concentrations are created sufficient to effectively treat viral diseases. Food has no significant effect on the absorption of acyclovir. Acyclovir well penetrates into many organs, tissues and body fluids. The binding with plasma proteins is 9-33% and does not depend on it concentration in plasma. Concentration in cerebrospinal fluid fluid is about 50% of its concentration in the plasma. Acyclovir penetrates through blood-brain and placental barriers, accumulates in breast milk. After ingestion of 1 g / day, the concentration of acyclovir in breast milk is 60-410% of its plasma concentration in (the organism of a child with mother's milk acyclovir comes in a dose of 0.3 mg / kg / day).

    The maximum concentration of the drug in the blood plasma (CmOh) after oral administration of 200 mg 5 times a day - 0.7 μg / ml, the minimum concentration (Cmin) -0,4 μg / ml;; time to reach the maximum plasma concentration (TCmax) - 1,5-2 hours. Metabolised in the liver to form a pharmacologically inactive compound 9-carboxymethoxymethylguanine. It is excreted by the kidneys by glomerular filtration and tubular secretion, about 84% is excreted by the kidneys unchanged, 14 % - in the form of a metabolite. Aciclovir's renal clearance is 75-80% of the total plasma clearance. The half-life (T1/2) in adults - with a normal kidney function is 2-3 hours. In patients with severe renal insufficiency half-life - 20 hours, with hemodialysis - 5,7 hours, while the concentration of acyclovir in the plasma decreases to 60% of the initial value. Less than 2% of acyclovir is excreted from the body through the intestine.

    Indications:

    Treatment of infections of the skin and mucous membranes caused by viruses Herpes simplex 1 and 2 types, both primary and secondary, including genital herpes;

    prevention of exacerbations of recurrent infections caused by Herpes simplex l and 2 types, in patients with normal immune status;

    prevention of primary and recurrent infections of the viruses Herpes simplex 1 and 2 types, in patients with immunodeficiency;

    in the complex therapy of patients with severe immunodeficiency: in HIV infection (stage of AIDS, early clinical manifestations and a detailed clinical picture) and in patients who underwent bone marrow transplantation;

    treatment of primary and recurrent infections caused by the virus Varicella zoster (chickenpox, smallpox, also shingles - Herpes zoster).

    Contraindications:

    Hypersensitivity to acyclovir, ganciclovir, or to any auxiliary substance of the drug.

    Deficiency lactase, sugarase / isomaltase, lactose intolerance, fructose, glucose-galactose malabsorption.

    The drug is contraindicated during lactation.

    Children under 3 years (for this dosage form).

    Carefully:Pregnancy; elderly patients and patients taking large doses of acyclovir, especially against dehydration; impaired renal function; neurological disorders or neurological reactions to the administration of cytotoxic drugs (including in the anamnesis).
    Pregnancy and lactation:Acyclovir penetrates through the placental barrier and accumulates in breast milk. The use of the drug during pregnancy is possible only if the intended benefit to the mother exceeds the potential risk to the fetus. If you need to take acyclovir during lactation, interruption of breastfeeding is required.
    Dosing and Administration:

    Acyclovir 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.

    Treatment of infections of the skin and mucous membranes caused by Herpes simplex 1 and 2 types: adults: acyclovir appoint 200 mg 5 times a day for 5 days: with 4-hour intervals during the day and with an 8-hour interval at night. In more severe cases of the disease, the course of treatment can be extended to a doctor's prescription for up to 40 days as part of a comprehensive therapy for severe immunodeficiency, including. with a developed clinical picture of HIV infection, including early clinical manifestations of HIV infection and the stage of AIDS; after bone marrow transplantation or when there is a violation of absorption from the intestine, 400 mg 5 times a day are prescribed.

    Treatment should be started as soon as possible after the onset of infection; at relapses acyclovir prescribe in the prodromal period or with the manifestation of the first elements of the rash.

    Prevention of recurrence of infections caused by Herpes simplex 1 u 2 types in patients with normal immune status.

    The recommended dose is 200 mg 4 times a day (every 6 hours), or 400 mg twice a day (every 12 hours). In some cases, lower doses are effective - 200 mg 3 times a day (every 8 hours) or 2 times a day (every 12 hours).

    Prevention of infections caused by Herpes simplex 1 and 2 types, in patients with immunodeficiency.

    The recommended dose is 200 mg 4 times a day (every 6 hours). In case of severe immunodeficiency (for example, after bone marrow transplantation) or if there is a violation of absorption from the intestine, the dose is increased to 400 mg 5 times a day. Duration The preventive course of therapy is determined by the duration of the infection risk period.

    Treatment of infections caused by the virus Varicella zoster (chickenpox).

    Adults: prescribe 800 mg 5 times a day every 4 hours in the afternoon and with an 8-hour interval at night. Duration of treatment 7-10 days. Children: prescribe 20 mg / kg, 4 times a day for 5 days (maximum single dose 800 mg), children from 3 to 6 years: 400 mg 4 times a day, over 6 years: 800 mg 4 times a day day for 5 days.

    Treatment should be started when the earliest signs or symptoms of chicken pox appear.

    Treatment of infections caused by the virus Herpes zoster (shingles).

    Adults: prescribe 800 mg 4 times a day every 6 hours for 5 days. Children over the age of 3 years the drug is administered in the same dose as and adults.

    Treatment and prevention of infections caused by Herpes simplex 1 and 2 types, children of children with immunodeficiency and normal immune status.

    Children from 3 years to 6 years - 400 mg once a day; over 6 years - 800 mg 4 times a day. A more accurate dose is determined from the calculation of 20 mg / kg body weight, but not more than 800 mg / day. The course of treatment is 5 days.

    Data on the prevention of recurrence of infections caused by a simple virus herpes, and treatment of herpes zoster in children with normal immunity indices are absent.

    Treatment of pediatric patients with severe immunodeficiency.

    For treatment of children older than 3 years, prescribed 800 mg of acyclovir 4 times in day every 6 hours (as well as for the treatment of adults with immunodeficiency).

    Patients of advanced age.

    In the elderly, there is a decrease in clearance of acyclovir in the body in parallel with a decrease in the clearance of creatinine. Patients elderly age, taking large doses of the drug inside, should receive a sufficient amount of fluid. With renal insufficiency it is necessary to solve the problem of reducing the dose of the drug.

    Patients with renal insufficiency.

    Care must be taken when administering acyclovir to patients with renal insufficiency.In such patients, taking the drug inside at recommended doses from the purpose of treatment and prevention of infections caused by the herpes simplex virus does not lead to cumulation of the drug to concentrations exceeding the established safe levels. However, in patients with severe renal failure (creatinine clearance (CK) less than 10 ml / min), the dose of acyclovir should be reduced to 200 mg twice daily with 12-hour intervals.

    When treating infections caused by a virus Varicella zoster, Herpes zoster, a also in the treatment of patients with severe immunodeficiency, the recommended dosages are: terminal renal failure (creatinine clearance less than 10 ml / min) - 800 mg twice a day every 12 hours; severe renal failure (clearance of creatinine 10-25 ml / min) - 800 mg 3 times a day every 8 hours.

    Side effects:

    The drug is usually well tolerated.

    The following classification of undesirable reactions is used depending on the frequency of occurrence: very often (> 1/10), often (> 1/10, <1/100), sometimes (> 1/1000, <1/100), rarely (> 1 /10.000, <1/1000), very rarely (<1 / 10,000).

    From the gastrointestinal tract: often - nausea, vomiting, diarrhea; very rarely - hepatitis, jaundice, in isolated cases - abdominal pain.

    In blood: rarely - transient insignificant, increased activity of liver enzymes, a slight increase in urea concentration and creatinine, hyperbilirubinemia, very rarely leukopenia, erythropenia, anemia, thrombocytopenia.

    From the central nervous system: often headache pain, dizziness; very rarely - agitation, confusion, tremor, ataxia, dysarthria, hallucinations, psychotic symptoms of convulsions, drowsiness, encephalopathy, coma. Usually these side effects were observed in patients with renal insufficiency or in the presence of other provoking factors and were mainly reversible.

    From the respiratory system: rarely - shortness of breath.

    Allergic reactions: anaphylactic reactions, skin rash, itching, urticaria, Lyell's syndrome, Stevens-Johnson syndrome.

    From the skin and subcutaneous tissue: often itching; urticaria, rash, in including sensitization, rarely - alopecia, rapid diffuse prolapse hair (since this type of alopecia is observed in various diseases and when treated with many drugs, its association with acyclovir is not established); very rarely Lyell's syndrome, Stevens-Johnson syndrome.

    Other: often fatigue, fever; rarely - peripheral edema, visual impairment, lymphadenopathy, myalgia, malaise.

    Overdose:There have been no cases of overdose with oral administration of acyclovir. It was reported that 20 g of acyclovir was ingested. Symptoms: agitation, coma, cramps, lethargy. It is possible to precipitate acyclovir in the renal tubules if its concentration exceeds the solubility in the renal tubules (2.5 mg / ml). Treatment: symptomatic.
    Interaction:

    Simultaneous application with probenecid results in an increase in the mean half-life and a decrease in the clearance of acyclovir.

    Strengthening the effect of acyclovir is noted with the simultaneous administration of immunostimulants.

    With simultaneous admission with nephrotoxic drugs, the risk of developing renal dysfunction increases.

    Special instructions:

    Acyclovir is used strictly according to the doctor's prescription to avoid complications in adults and children older than 3 years.

    Duration or repeated treatment with acyclovir in patients with reduced immunity can lead to the emergence of strains of viruses, insensitive to its action.The majority of detected strains of viruses, insensitive to acyclovir, show a relative lack of viral thymidine kinase; strains with altered thymidine kinase or with altered DNA polymerase were isolated. In vitro act acyclovir on isolated strains of the virus Herpes simplex may cause the appearance of less sensitive strains.

    With caution, the drug is prescribed to patients with impaired renal function, elderly patients age in connection with an increase in the half-life of acyclovir.

    When applying should be provided sufficient amount of liquid.

    When taking the drug should monitor the function of the kidneys (the concentration of blood urea and blood plasma creatinine). Acyclovir does not prevent sexual transmission of herpes, therefore during the treatment it is necessary to refrain from sexual intercourse, even in the absence of clinical manifestations. It is necessary to inform patients about the possibility of transmission of the virus of genital herpes in the period of rashes, as well as cases of asymptomatic virus carrying.

    Effect on the ability to drive transp. cf. and fur:

    No data.However, it should be borne in mind that dizziness may develop during acyclovir treatment, therefore, care must be taken when driving vehicles and engaging in potentially dangerous activities requiring increased concentration of attention and speed of psychomotor reactions (see "Side effect" section).

    Form release / dosage:Tablets 200 mg.
    Packaging:10 tablets per contour cell packaging made of polyvinylchloride film and aluminum foil.

    2 contour mesh packs together with instructions for use are placed in a pack of cardboard.

    Storage conditions:

    Store in a dry, dark place at a temperature of no higher than 25 ° C. Keep out of the reach of children.

    Shelf life:

    2 years.

    Do not use after the expiration date.

    Terms of leave from pharmacies:On prescription
    Registration number:LP-000199
    Date of registration:09.02.2011
    The owner of the registration certificate:AVEKSIMA, JSC AVEKSIMA, JSC Russia
    Manufacturer: & nbsp
    Information update date: & nbsp09.02.2011
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