Active substanceAcyclovirAcyclovir
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  • Dosage form: & nbsppills
    Composition:

    1 tablet contains:

    Active substance:

    acyclovir

    - 200 mg

    Excipients


    lactose monohydrate

    - 86 mg

    potato starch

    - 97 mg

    sucrose (sugar)

    - 21 mg

    silicon dioxide colloid (aerosil)

    - 2 mg

    magnesium stearate

    - 4 mg

    Average weight of a tablet - 410 mg

    Description:Tablets are white, round, flat-cylindrical with a facet and a risk.
    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 1 and 2 types, against the virus Varicella zoster, higher concentrations are required to inhibit the Epstein-Barr virus. In vivo 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 blood-brain and placental barrier, excreted in breast milk. The maximum concentration after the administration 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 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:

    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 viruses Herpes simplex 1 and 2 types, in patients with normal immune status.

    Prevention of primary and recurrent infections caused by viruses Herpes simplex 1 and type 2 in patients with immunodeficiency.

    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.

    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, valaciclovir or any auxiliary substance of the drug. Deficiency of lactase, sucrose / isomaltase, lactose intolerance, fructose, glucose-galactose malabsorption. Children under 3 years.

    Carefully:

    Patients with impaired renal function; elderly patients due to an increase in the half-life of acyclovir; dehydration, renal failure, neurological disorders, incl. in the anamnesis.

    Pregnancy and lactation:

    Acyclovir penetrates through the placental barrier, excreted 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 use the drug during breastfeeding, breastfeeding should be discarded.

    Dosing and Administration:

    Inside, during or immediately after eating, squeezed with enough water.The dose and duration of treatment are 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 1 and type 2, adults and children over 3 years of age, the drug is prescribed 200 mg 5 times a day for 5 days at 4 hour intervals during the day and with an 8 hour interval overnight. In more severe cases, the course of treatment can be extended to the doctor's prescription. As part of complex therapy in cases of severe immunodeficiency, including with the expanded clinical picture of HIV infection (including early clinical manifestations of HIV infection and stage of AIDS), 400 mg 5 times a day are prescribed after bone marrow transplantation.

    Genital herpes: initial therapy - 200 mg every 4 hours during wakefulness, 5 times a day for 10 days. Recurrent genital herpes (less than 6 episodes a year): intermittent therapy - 200 mg every 4 hours during wakefulness, 5 times a day for 5 days. Recurrent genital herpes (more than 6 episodes a year): prolonged suppressive therapy - 400 mg 2 times a day or 200 mg 3-5 times a day.

    To prevent recurrence of infections caused by viruses Herpes simplex 1 and 2 types, patients with normal immune status and recurrent disease are prescribed 200 mg 4 times a day every 6 hours. Treatment with the drug should be interrupted periodically for 6-12 months to identify possible changes in the course of the disease.

    To prevent infections caused by viruses Herpes simplex 1 and 2 types, adults and children older than 3 years with immunodeficiency, the drug is recommended to appoint 200 mg 4 times a day every 6 hours, the maximum dose - up to 400 mg 5 times a day, depending on the severity of the infection. The duration of the preventive course of therapy is determined by the length of the period when there is a risk of infection.

    In the treatment of infections caused by Varicella zoster, adults are prescribed 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 older than 3 years with a body weight of less than 40 kg are prescribed 20 mg / kg 4 times a day for 5 days, children with a body weight of more than 40 kg of the drug are prescribed 800 mg 5 times a day every 4 hours in the afternoon and 8 hour interval at night, for 7-10 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 dose should be reduced to 200 mg 2 times a day from 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 dose of the drug to 800 mg twice 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 digestive system: abdominal pain, nausea, vomiting, diarrhea.

    From the side of the blood: a slight increase in the concentration of urea and creatinine, hyperbilirubinemia, leukopenia, erythropenia.

    From the central nervous system: headache, weakness, tremor, dizziness, fatigue, drowsiness, hallucinations, agitation, confusion, malaise, paresthesia.

    From the sense organs: impaired vision.

    From the manifestation of allergic reactions: rash, itching, Lyell syndrome, urticaria, anaphylactic reactions, multiform exudative erythema, incl. Stevens-Johnson syndrome.

    Other: lymphadenopathy, peripheral edema, increased activity of "liver" transaminases, myalgia, alopecia, fever.

    If any of the side effects listed in the manual are aggravated, or if you notice any other side effects not listed in the instructions, tell your doctor.

    Overdose:

    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: maintenance of vital functions, hemodialysis.

    Interaction:

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

    Special instructions:

    Long-term or repeated treatment with acyclovir patients with reduced immunity can lead to the appearance of strains of viruses that are insensitive to its action. Use strictly according to the doctor's prescription to avoid complications in adults and children over 3 years of age.

    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.

    The majority of isolated 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 action of acyclovir on isolated strains of the virus Herpes simplex may cause the appearance of less sensitive strains.

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

    During the period of treatment, it is recommended to refrain from driving vehicles, servicing moving mechanisms and practicing other potentially dangerous activities requiring increased attention and speed of psychomotor reactions.

    Form release / dosage:

    Tablets 200 mg.

    Packaging:

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

    2 contour squares, together with instructions for use, are placed in a pack of cardboard.

    Storage conditions:

    In a dry, protected from light 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 expiry date printed on the package.

    Terms of leave from pharmacies:On prescription
    Registration number:LS-002612
    Date of registration:22.03.2012
    Expiration Date:Unlimited
    The owner of the registration certificate:KIROVSKAYA PHARMACEUTICAL COMPANY, LTD. KIROVSKAYA PHARMACEUTICAL COMPANY, LTD. Russia
    Manufacturer: & nbsp
    Information update date: & nbsp30.09.2017
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