Active substanceAcyclovirAcyclovir
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  • Dosage form: & nbsppills
    Composition:Each tablet contains an active substance: acyclovir 400 mg in terms of anhydrous substance;
    auxiliary substances: lactose (sugar milk) - 301.6 mg, potato starch 93.8 mg, sucrose 0.4 mg, magnesium stearate 6 mg, povidone (polyvinylpyrrolidone) 16 mg, stearic acid 2.2 mg.
    Description:

    Tablets are white or almost white, flat cylindrical, with a facet on both sides and risk from one side.

    Pharmacotherapeutic group:Antiviral agent
    ATX: & nbsp

    S.01.A.D   Antiviral drugs

    Pharmacodynamics:

    Antiviral drug, a synthetic analogue of acyclic purine nucleoside, which has a highly selective effect on herpes viruses. Inside virus-infected cells under the influence of viral thymidine kinase, a number of consecutive reactions of the transformation of acyclovir into mono-, di- and triphosphate of acyclovir occur. Acyclovirtriphosphate is inserted into the viral DNA chain and blocks its synthesis by competitive inhibition of the viral DNA polymerase.

    In vitro Acyclovir is effective against herpes simplex virus - Herpes simplex type I and II, against the virus Varicella zoster; higher concentrations are required to inhibit the Epstein-Barr virus. In vitro Acyclovir is therapeutically and prophylactically effective, especially in viral infections caused by Herpes simplex.

    Pharmacokinetics:

    When administered orally, the bioavailability is 15-30%. Acyclovir well penetrates into all organs and tissues of the body, including the brain and skin. Binding to plasma proteins is 9-33% and does not depend on its concentration in the plasma. The concentration in the cerebrospinal fluid is about 50% of its concentration in the plasma. Acyclovir penetrates the placental barrier and accumulates in breast milk. The maximum concentration after ingestion of 200 mg 5 times a day is 0.7 μg / ml, the time to reach the maximum concentration is 1.5-2 hours.

    Metabolised in the liver to form a 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 (with the concentration of acyclovir in the plasma decreases to 60% of the initial value). About 84% is allocated by the kidneys in an unchanged form and 14% - in the form of a metabolite. Aciclovir's renal clearance is 75 to 80 % of the total plasma clearance. Less than 2% of acyclovir is excreted from the body through the intestine.

    Indications:

    1 Treatment of infections of the skin and mucous membranes caused by viruses Herpes simplex type I and II, both primary and secondary, including genital herpes.

    2 Prevention of exacerbations of recurrent infections caused by viruses Herpes simplex type I u II, the patients with normal immune status.

    3 Prevention of primary and recurrent infections caused by viruses Herpes simplex type I u II the of patients with immunodeficiency.

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

    5 Treatment of primary and recurrent infections caused by the virus Varicella zoster (chicken pox, as well as shingles - Herpes zoster).

    Contraindications:

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

    The drug is contraindicated during lactation.

    Children under 3 years (for this dosage form).

    Carefully:Pregnancy; elderly people and patients receiving large doses, especially against dehydration; impaired renal function; neurologic disorders or neurological reactions to the use of cytotoxic drugs (including in the anamnesis).
    Pregnancy and lactation:

    Acyclovir penetrates the placental barrier and accumulates in breast milk. Use during pregnancy is only possible 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:

    Inside. The drug is taken during or immediately after a meal and is 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 type I u II:

    Adults: the drug is prescribed at 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 the doctor's prescription up to 10 days. As part of complex therapy with severe immunodeficiency, including when the clinical picture of HIV infection (including, early clinical manifestations of HIV infection and stage of AIDS), after the implantation of the bone marrow is prescribed 400 mg 5 times a day.

    To prevent recurrence of infections caused by viruses Herpes simplex type I and II, patients with normal immune status and relapse of the disease are prescribed 200 mg 4 times a day every 6 hours, the duration of the course is from 6 to 12 months.

    To prevent infections caused by viruses Herpes simplex type I and II, adults with immunodeficiency, the drug is recommended to appoint 200 mg 4 times a day every 6 hours, the maximum dose - up to 400 mg of acyclovir 5 times a day, depending on the severity of the infection.

    Children: to treat infection caused by Herpes simplex and prevention of this infection in patients with weakened immune defenses, children older than 3 years receive the same dose as adults.

    In the treatment of infections caused by Varicella zoster:

    Adults: 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: with chicken pox it is prescribed 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 once a day for 5 days.

    In the treatment of 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:

    In the treatment and prevention of 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 twice a day with 12-hour intervals.

    In the treatment of 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 with 12-hour intervals; with a creatinine clearance of up to 25 ml / min, 800 mg 3 times a day with 8 hour intervals is prescribed.

    Side effects:

    The drug is usually well tolerated.

    From the gastrointestinal tract: in isolated cases - abdominal pain, nausea, vomiting, diarrhea.

    In the blood: a transient slight increase in the activity of liver enzymes, rarely a slight increase in levels of urea and creatinine, hyperbilirubinemia, leukopenia, erythropenia.

    From the side of the central nervous system: rarely - headache, weakness; in some cases, tremors, dizziness, fatigue, exhaustion, drowsiness, insomnia, paresthesia, confusion, hallucinations, decreased concentration, agitation.

    Allergic reactions: anaphylactic reactions, skin rash, itching, Lyell's syndrome, urticaria, multiforme exudative erythema, incl. Stevens-Johnson syndrome, fever.

    Other: rarely - alopecia, peripheral edema, visual impairment, lymphadenopathy, myalgia, malaise.

    Overdose:There were no cases of overdose after oral administration of acyclovir.
    Interaction:

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

    With simultaneous admission with nephrotoxic drugs, the risk of renal dysfunction increases. An increase in the effect is noted with the simultaneous appointment of immunostimulants.
    Special instructions:

    Use strictly according to the doctor's prescription in order to avoid complications in adults and children older than 3 years.

    Caution is prescribed for 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 liquid.

    When taking the drug should monitor the function of the kidneys (the level of blood urea and blood plasma creatinine).

    Acyclovir does not prevent sexual transmission of herpes, therefore during treatment it is necessary to abstain from sexual intercourse, even in the absence of clinical manifestations.

    Form release / dosage:

    Tablets 400 mg.

    Packaging:

    For 10, 20 tablets in a contour mesh box made of polyvinylchloride film and aluminum foil printed lacquered.

    By 10, 20, 30, 40, 50 or 100 tablets into a polymer container for medicines.

    One container or 1, 2, 3, 4, 5, 6, 8 or 10 contour mesh packages together with the instruction 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:

    3 years. Do not use after the expiration date.

    Terms of leave from pharmacies:On prescription
    Registration number:LSR-006438/08
    Date of registration:11.08.2008
    The owner of the registration certificate:OZONE, LLC OZONE, LLC Russia
    Manufacturer: & nbsp
    Information update date: & nbsp23.08.2011
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