Active substanceAcyclovirAcyclovir
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  • Dosage form: & nbsppills
    Composition:

    One tablet contains:

    active substance: Acyclovir - 200.0 mg in terms of 100% dry matter;

    Excipientslactose, potato starch, povidone (polyvinylpyrrolidone low molecular weight medical 12600 ± 2700, kollidon 30), sucrose (sugar), sodium lauryl sulfate (sodium dodecyl sulfate), magnesium stearate (magnesium stearate for the pharmaceutical industry) is sufficient to prepare a tablet weighing 410.0 mg.

    Description:Tablets are white or almost white in color, flat-cylindrical.
    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.

    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 period half-life - 20 hours, with hemodialysis - 5.7 hours (with the concentration of acyclovir in the plasma decreases to 60% of the original value). About 84% is excreted by the kidneys unchanged and 14% - in the form of a metabolite. Aciclovir renal clearance is 75-80% 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 and II, in patients with normal immune status.

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

    4 In the complex therapy of patients with severe immunodeficiency: in 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).

    Intolerance to galactose, deficiency of lactase, glucose-galactose malabsorption.

    Carefully:

    Pregnancy; elderly people and patients receiving large doses, 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 the placental barrier and accumulates in breast milk. Application during pregnancy is possible only in the event that,when the intended use for 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 and 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: for 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: the drug is given 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 chickenpox appoint 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 daily 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 a creatinine clearance less than 10 ml / min, it is recommended to reduce the dosagedrug up 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 blood: a 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, 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.

    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.

    Form release / dosage:

    Tablets 200 mg.

    Packaging:

    For 10 tablets in a planar cell packaging made of polyvinylchloride film and aluminum foil printed lacquered. Two contour mesh packs, along with instructions for medical use of the drug, are placed in a pack of cardboard.

    Storage conditions:

    List B.

    Store at a temperature not exceeding 25 ° C.

    Keep out of the reach of children.

    Shelf life:

    2 years. Do not use the drug after the expiration date.

    Terms of leave from pharmacies:On prescription
    Registration number:P N003292 / 01
    Date of registration:14.10.2008
    The owner of the registration certificate:NIZHFARM, JSC NIZHFARM, JSC Russia
    Manufacturer: & nbsp
    Information update date: & nbsp15.12.2009
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