Acyclovir - instructions for use, dose, side effects, contraindications

1 tablet contains: Active substance: acyclovir	- 206.0 mg
in terms of dry matter	- 200 mg
Excipients:
lactose	- 135.7 mg
potato starch	- 39.8 mg
povidone	- 8.0 mg
sucrose	- 16.0 mg
sodium lauryl sulfate	- 1.5 mg
magnesium stearate	3.0 mg

Average weight of a tablet - 410.0 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:

The antiviral drug is a synthetic analogue of the acyclic purine nucleoside thymidine, which has a highly selective effect on herpes viruses. Inside the virus-infected cells under the action of viral thymidine kinase, phosphorylation and conversion to acyclovir monophosphate occurs. Under the influence of guanylyl cyclase acyclovir, monophosphate is converted to diphosphate and under the influence of several cellular enzymes - into triphosphate. Acyclovir triphosphate is inserted into the viral DNA chain and blocks its synthesis by competitive inhibition of the viral DNA polymerase. High selectivity of action and low toxicity for humans are due to the lack of the necessary enzyme for the formation of acyclovir triphosphate in intact cells of the macroorganism.

In vitro Acyclovir is effective against herpes simplex virus Herpes simplex 1 and 2 type, 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 the virus Herpes simplex. Moderately active against cytomegalovirus.

Pharmacokinetics:

When administered orally, bioavailability is 15-30%, but at the same time, dose-related concentrations are created sufficient to effectively treat viral diseases. Food has no significant effect on the absorption of acyclovir. It penetrates well into all organs and tissues of the body. The concentration in the cerebrospinal fluid is 50 % from concentration of the drug in the blood. Binding to plasma proteins is 9-33% and does not depend on its concentration in the plasma. It penetrates the placental barrier and accumulates in breast milk.

The maximum concentration after taking the drug inside 200 mg 5 times at day - 0,7 mkg / ml, the minimum concentration - 0,4 mkg / ml, the time to reach the maximum concentration is 1.5-2 h.

Metabolized in the liver with the formation of a pharmacologically inactive compound - 9-carboxymethoxymethylguanine.

The half-life in adults with normal renal function is 2-3 hours. In severe renal failure, the half-life is 20 hours, with hemodialysis 5.7 hours, while the concentration of acyclovir in the plasma decreases to 60% of the initial value.

About 84% of acyclovir is excreted by the kidneys unchanged, 14% is excreted in the form of a metabolite. Aciclovir's 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 (including in patients with impaired immunity).

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 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 developed clinical picture) and in patients who underwent bone marrow transplantation.

Treatment of primary and recurrent infections caused by the virus Varicella zoster (chickenpox), Herpes zoster (shingles).

Contraindications:Hypersensitivity to acyclovir (ganciclovir, valaciclovir) or other components of the drug, deficiency of lactase, sucrose / isomaltase, lactose intolerance, fructose, glucose-galactose malabsorption, pregnancy, breast-feeding period, children under 3 years.

Carefully:

Patients with impaired renal function, including history, with neurological disorders, with dehydration, elderly patients due to an increase in the half-life of acyclovir.

Pregnancy and lactation:

Use of the drug is possible if the expected benefit for the mother exceeds the potential risk to the fetus.

Acyclovir penetrates the placental barrier and accumulates in breast milk. 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 depend on the nature, severity of the disease and effectiveness of treatment.

To treat infections of the skin and mucous membranes caused by viruses Herpes simplex 1 - and 2 types, adults and children over 3 years: 200 mg 5 times a day every 4 hours during the day and with an 8-hour interval at night. The course of treatment is 5 days. In severe cases, the course of treatment can be extended at the doctor's prescription.

As part of complex therapy for severe immunodeficiency, including in the unfolded clinical picture of HIV-infection (including early clinical manifestations of HIV infection and stage of AIDS), after bone marrow transplantation:

To prevent recurrence of infections caused by viruses Herpes simplex 1 and 2 types, in patients with normal immune status and with relapse of the disease: adults - 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 over 3 years old with immunodeficiency: 200 mg 4 times a day every 6 hours. The maximum dose of 400 mg - 5 times a day, depending on the severity of the disease. The duration of the preventive course of therapy is determined by the length of the period when there is a risk of infection.

For the treatment of infections caused by Varicella zoster: adults - 800 mg 5 times a day every 4 hours during the day and with an 8-hour interval at night, for 7-10 days; children older than 3 years with a body weight of less than 40 kg - 20 mg / kg 4 times a day for 5 days, children with a body weight of more than 40 kg - 800 mg 5 times a day every 4 hours during the day and with an 8-hour interval at night.

For the treatment of infections caused by Herpes zoster: adults - 800 mg 4 times a day every 6 hours for 5 days.

In patients with impaired renal function, dosage adjustment is necessary depending on the amount of creatinine clearance:

- for the treatment and prevention of infections caused by Herpes simplex, in patients with creatinine clearance less than 10 ml / min: 200 mg 2 times a day with 12-hour intervals;

- for the treatment and prevention of infections caused by Varicella zoster, in patients with creatinine clearance less than 10 ml / min: 800 mg 2 times a day at 12-hour intervals, in patients with creatinine clearance up to 25 ml / min: 800 mg 3 times daily with 8 hour intervals.

Side effects:

The drug is usually well tolerated.

From the gastrointestinal tract: nausea, vomiting, diarrhea, abdominal pain.

From the skin and subcutaneous tissues: allergic reactions, rash, hives, itching; Lyell's syndrome, multiforme exudative erythema, including Stevens-Johnson syndrome, photosensitivity.

From the immune system: angioedema, anaphylaxis.

From the central nervous system: headache, dizziness, weakness, fatigue, drowsiness, confusion, hallucinations, agitation, tremor, paresthesia, encephalopathy, convulsions, coma.Usually these side effects were observed in patients with renal insufficiency, who took the drug in doses exceeding the recommended ones.

From the liver and bile excretory ways: hyperbilirubinemia, increased activity of "liver" transaminases.

From the side of the blood and lymphatic system: leukopenia, erythropenia.

From the side of the kidneys and urinary tract: increase in urea concentration and Creatinine in the blood, acute renal failure, renal colic.

Other: lymphadenopathy, peripheral edema, myalgia, alopecia, fever.

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

Overdose:

Oral reception 20 g of acyclovir did not lead to the development of toxic effects.

Symptoms: with repeated doses exceeding the recommended ones within several days, they were noted violations from the gastrointestinal tract (nausea, vomiting) and neurological (headache and confusion consciousness). Sometimes there may be shortness of breath, diarrhea, impaired renal function, agitation, confusion, hallucinations, 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. Patients need careful medical supervision to identify possible symptoms of intoxication.

Interaction:

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

When simultaneous admission with nephrotoxic drugs (aminoglycosides, amphotericin B, bacitracin, vancomycin, methotrexate, polymyxins, X-ray contrast preparations, rifampicin, streptomycin, sulfonamides, ciprofloxacin and others) increases the risk of impaired renal function.

An increase in the effect is noted with the simultaneous use of immunostimulants.

Special instructions:

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 concentration of urea in the blood and creatinine plasma blood).

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

Effect on the ability to drive transp. cf. and fur:At the time of taking the drug should be be careful when driving vehicles and engaging in other potentially hazardous activities that require increased attention and speed of psychomotor reactions.

Form release / dosage:Tablets 200 mg.

Packaging:

For 10, 15, 20 or 30 tablets in a contour mesh box made of polyvinylchloride film and aluminum foil printed lacquered.

For 1, 2, 3 contour squares, together with instructions for use, are placed in a pack of cardboard.

Storage conditions:

In dry the dark place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

Shelf life 3 years.

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

Terms of leave from pharmacies:On prescription

Registration number:LS-000956

Date of registration:12.03.2012 / 06.06.2013

Expiration Date:Unlimited

The owner of the registration certificate:OBOLENSKOE PHARMACEUTICAL ENTERPRISE, CJSC OBOLENSKOE PHARMACEUTICAL ENTERPRISE, CJSC Russia

Manufacturer: & nbsp

OBOLENSKOE PHARMACEUTICAL ENTERPRISE, CJSC Russia

Information update date: & nbsp30.09.2017

Illustrated instructions

Instructions

Acyclovir (Aciclovir)