Active substanceAcyclovirAcyclovir
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  • Dosage form: & nbsppills
    Composition:

    1 tablet contains

    active substance - Acyclovir 200.0 mg; 400.0 mg; 800.0 mg;

    Excipients - microcrystalline cellulose 60.5 / 121.0 / 242.0 mg, carboxymethyl starch sodium (sodium starch glycolate type A) - 16.25 / 32.5 / 65.0 mg, copovidone 5.0 / 10.0 / 20 , 0 mg, magnesium stearate 4.5 / 9.0 / 18.0 mg, silicon colloidal dioxide 1.25 / 2.5 / 5.0 mg.

    Description:

    Tablets 200 mg:

    Round biconvex tablets of white color with marking VS 1.

    Tablets 400 mg:

    Round biconvex tablets of white color with marking VS2.

    Tablets 800 mg:

    Oblong white tablets with a risk on both sides and labeling VS3.

    Pharmacotherapeutic group:Antiviral agent
    ATX: & nbsp

    S.01.A.D   Antiviral drugs

    Pharmacodynamics:

    Antiviral drug, a synthetic analogue of the acyclic purine nucleotide thymidine. The mechanism of action of acyclovir is realized due to its selective, active accumulation in infected cells, its high affinity for viral thymidine kinase.

    Thymidine kinase in virus-infected cells converts acyclovir in monophosphate, then monophosphate with the participation of other cellular enzymes is converted sequentially into diphosphate and triphosphate. Acyclovir triphosphate is a substrate and an inhibitor of the virus-specific DNA polymerase. Acyclovir triphosphate, "embedded" in the DNA synthesized by the virus, blocks the multiplication of the virus.

    Acyclovir is highly active against the virus Herpes simplex 1 and 2 types; a virus that causes varicella and shingles (Varicella Zoster), of the Epstein-Barr virus (virus species are listed in order of increasing value of the minimum inhibitory concentration (MIC) of acyclovir). Moderately active against cytomegalovirus.

    Acyclovir in herpes prevents the formation of new elements of the rash, reduces the likelihood of cutaneous dissemination and visceral complications, accelerates the formation of crusts, relieves pain in the acute phase of the disease. It has an immunostimulating effect.

    Pharmacokinetics:

    Bioavailability of acyclovir for oral administration is 15 - 30%, which is due to its low lipophilicity; at the same time, concentrations sufficient to effectively treat viral diseases are created. Food has no significant effect on the absorption of acyclovir. The maximum concentration in the blood plasma (CmOh) after oral administration of 200 mg 5 times a day - 0.7 μg / ml, the time to reach the maximum concentration (TCmOh) - 1,5 - 2 hours Half-life (T1/2) with normal kidney function is 2.5 to 3.3 hours.

    Stationary concentration (Css) Acyclovir is achieved on the second day of taking the drug. When taking 200 mg of acyclovir every 4 hours, the average Css max in plasma is 3.1 μmol (0.7 μg / ml), and the mean Css min 1.8 μmol (0.4 μg / ml). When taking 400 mg and 800 mg of acyclovir every 4 hours Css max is 5.3 μmol (1.2 μg / ml) and 8 μmol (1.8 μg / ml), respectively, and the mean Css min - 2.7 μmol (0.6 μg / ml) and 4 μmol (0.9 μg / ml), respectively.

    The connection with plasma proteins varies in the range of 9 - 33%. Acyclovir penetrates into all organs and tissues, including the brain and skin; It is defined in saliva, vaginal discharge, contents of vesicles. In the cerebrospinal fluid, the concentration of acyclovir in the amount of 50% of the plasma level is detected.

    Overcomes the placental barrier, penetrates into breast milk.

    Acyclovir is metabolized in the liver with the participation of cytochrome P450 1A2 (CYP 1A2) to form a metabolite - 9-carboxymethoxymethylguanine. It is excreted by the kidneys by glomerular filtration (mainly) and tubular secretion, 62 - 91% unchanged, 14,4% (8,6 - 19,8%) - in the form of a metabolite. Less than 2% are excreted through the gastrointestinal tract; trace amounts are determined in the exhaled air. If the kidney function is impaired, the dose should be adjusted based on the creatinine clearance. Hemodialysis removes 60% of the circulating acyclovir in the body. Pharmacokinetics in children over the age of 1 year and adults is comparable.

    Indications:

    - Primary and recurrent infections of the skin and mucous membranes: herpes simplex skin and mucous membranes, genital herpes (treatment and prevention of relapses);

    - Shingles (herpes);

    - Chickenpox;

    - Severe immunodeficiency states (as part of combination therapy, including in patients after bone marrow transplantation on the background of chemotherapy, with the use of immunosuppressive drugs, in HIV-infected patients, etc.).

    Contraindications:

    Hypersensitivity to acyclovir and / or other components of the drug, hypersensitivity to valacyclovir, lactation (breastfeeding should be discontinued), children under 5 years of age (this dosage form is not recommended).

    Carefully:

    Pregnancy, renal insufficiency, dehydration, severe neurological disorders, incl. in the anamnesis.

    Pregnancy and lactation:

    Acyclovir penetrates the placental barrier and into breast milk. Application in pregnancy time is possible only if the intended benefit to the mother exceeds the potential risk to the fetus. If it is necessary to take acyclovir during lactation, breastfeeding should be interrupted.

    Dosing and Administration:

    Inside, with meals or immediately after eating, with a glass of water.The drug should be taken as early as possible with the first signs of the disease. The dosage regimen is set individually, depending on the severity of the disease and the degree of immunosuppression. The duration of prophylactic use of Acyclostad® in patients with varying degrees of immunosuppression, especially in severe immunodeficient conditions, is determined by the time period during which there is a risk of developing a herpes infection.

    Infections of the skin and mucous membranes caused by Herpes simplex I and II types. Adults and children over 5 years with a normal immune status, the drug is prescribed 200 mg 4 times a day for 5 days, with a 4-hour interval during the day and with an 8-hour interval overnight. In severe cases, as prescribed by the doctor, the course of treatment can be extended.

    Herpes simplex skin and mucous membranes in patients with immunodeficiency (treatment): 200-400 mg 5 times a day for 10 days.

    Herpes simplex skin and mucous membranes (prevention): 200 mg 4 times a day, every 6 hours; or 400 mg every 12 hours. In a number of cases, low doses of acyclovir are effective: 200 mg three times a day (every 8 hours) or twice a day (every 12 hours). The course of treatment - individually (see above).

    Relapse prevention Herpes simplex in patients with immunodeficiency: 200 mg 4 times a day every 6 hours. In case of severe immunodeficiency (after transplantation bone marrow or with a violation of absorption from the intestine) - 400 mg 5 times a day. The course of treatment - individually (see above).

    Genital herpes: Primary infection - 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 twice a day or 200 mg 3 - 5 times a day. Course treatment - up to 12 months. At the end of the course, i.е. After 1 year of suppressive therapy, an assessment should be made of the patient's condition and the appropriateness of continuing treatment with Acyclostad®.

    Shingles (herpes): 800 mg every 4 hours during wakefulness, 5 times a day for 7-10 days.

    Chickenpox: 800 mg 4 times a day, for 5 days. Children a single dose is calculated at 20 mg / kg, but not more than 800 mg. Children weighing 40 kg or more are prescribed a dose for adults.

    Heavy immunodeficiency conditions (as part of combination therapy): 800 mg 4 times a day (every 6 hours).The course of treatment - individually (see above).

    When chronic renal failure correction of the dosing regimen is required.

    Recommended

    mode

    dosing with normal kidney function

    Clearance

    creatinine

    (ml / min / 1.73 m2)

    Recommended dosing regimen for chronic renal failure



    single dose of acyclovir

    interval between doses, multiplicity of reception

    200 mg every 4 hours

    >10

    200

    every 4 hours - 5 times a day


    0-10

    200

    every 12 hours, 2 times a day

    400 mg every 12 hours

    >10

    400

    every 12 hours, 2 times a day


    0-10

    200

    every 12 hours, 2 times a day

    800 mg every 4 hours

    >25

    800

    every 4 hours, 5 times a day


    10-25

    800

    every 8 hours, 3 times a day


    0-10

    800

    every 12 hours, 2 times a day

    After hemodialysis lasting 6 hours, the concentration of acyclovir in the blood decreases by 60%. In this connection, after each hemodialysis, the patient needs an additional single dose of acyclovir.

    Side effects:

    From the digestive system: nausea, vomiting, diarrhea, abdominal pain (abdominal pain), increased activity of "liver" transaminases, bilirubin concentrations, hepatitis.

    From the urinary system: crystalluria, an increase in the concentration of creatinine and urea in the blood, acute renal failure, renal colic.

    From the nervous system: headache, dizziness, insomnia, drowsiness, confusion, agitation, hallucinations, visual impairment, paresthesia, agitation, tremor, ataxia, dysarthria, psychotic symptoms, seizures, encephalopathy, coma.

    From the organs of hematopoiesis and lymphatic system: anemia, leukopenia, thrombocytopenia, lymphadenopathy.

    Allergic reactions: anaphylactic reactions, skin allergic reactions (itching, rash, Lyell's syndrome, urticaria, multiforme exudative erythema, including Stevens-Johnson syndrome).

    Other: malaise, fever, dyspnea, peripheral edema, alopecia, myalgia, photosensitivity.

    Overdose:

    It is known about ingestion of 20 g of acyclovir.

    Symptoms: nausea, vomiting, agitation, coma, convulsions, 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:

    The possible interaction of acyclovir is associated with a competitive excretion through the kidneys, in connection with which it is necessary to be careful when prescribing with it drugs,Competing for the pathway of elimination because of the potential increase in plasma concentrations of one, both drugs or their metabolites.

    Due to competition for the pathway with cimetidine, with probenecid, with calcium channel blockers, the area under the pharmacokinetic curve (concentration-time) of acyclovir is increased by 20-30%. Similarly acyclovir interacts with an inactive metabolite of mycophenolate mofetil. However, correction of the dosage regimen of acyclovir is not required due to its wide therapeutic range.

    With the joint appointment of acyclovir with zidovudine, development of paresthesia, seizures, lethargy is possible.

    An increase in the effect is noted with the simultaneous administration of acyclovir with immunostimulants (interferon).

    Special instructions:

    In order to prevent crystalluria during therapy with acyclovir, it is necessary to ensure the supply of a sufficient amount of liquid.

    During therapy with acyclovir, elderly patients should be monitored for kidney function.

    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.

    In vitro action of acyclovir on isolated strains of the virus herpes simplex may cause the appearance of less sensitive strains. Most strains of viruses that are insensitive to acyclovir show an altered thymidine kinase or a relative lack of it; strains with altered DNA polymerase were also isolated. Long-term or repeated treatment with acyclovir patients with reduced immunity can lead to the appearance of strains of viruses that are insensitive to the drug.

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

    During the use of the drug, patients should be very careful to drive and engage in other potentially hazardous activities requiring high rates of psychomotor reactions, due to possible drowsiness and visual impairment.

    Form release / dosage:Tablets 200 mg, 400 mg, 800 mg.
    Packaging:

    Tablets 200 mg

    For 5 or 10 tablets in a planar cell package. 10 contour cell packs of 10 tablets or 5 contour cell packs of 5 tablets with instructions for medical use of the drug in a cardboard pack.

    Tablets 400 mg, 800 mg

    5 tablets in a planar cell package.5 or 7 contour cell packs with instructions for medical use of the drug in a cardboard bundle.

    Storage conditions:

    Store at a temperature not exceeding 25 ° C.

    Keep out of the reach of children.

    Shelf life:

    Shelf life 5 years.

    Do not use the product after the expiry date printed on the package.

    Terms of leave from pharmacies:On prescription
    Registration number:П N011036 / 01
    Date of registration:23.03.2012
    Date of cancellation:2017-09-05
    The owner of the registration certificate:SHTADA Artznajmittel AGSHTADA Artznajmittel AG Germany
    Manufacturer: & nbsp
    Representation: & nbspNizhpharm, JSCNizhpharm, JSCRussia
    Information update date: & nbsp05.09.2017
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