Product description
Antiviral agent.
Composition
1 tablet contains:
Active ingredient: acyclovir 200 mg.
Excipients: corn starch, lactose monohydrate, magnesium stearate, indigo carmine (E 132)
Pharmacological action
Pharmacodynamics
Acyclovir is an antiviral drug, a synthetic analog of acyclic purine nucleoside, which has a highly selective effect on herpes viruses. Inside virus-infected cells, viral thymidine kinase undergoes a series of sequential reactions of transformation of acyclovir into mono -, di-and triphosphate of acyclovir. Acyclovir triphosphate is incorporated into the viral DNA chain and blocks its synthesis by competitive inhibition of viral DNA polymerase.
In vitro, acyclovir is effective against herpes simplex virus-Herpes simplex type I and II, against Varicella zoster virus; higher concentrations are required to inhibit Epstein-Barr virus. In vivo, acyclovir is therapeutically and prophylactically effective, primarily for viral infections caused by Herpes simplex.
When taken orally, bioavailability is 15-30%. Acyclovir penetrates well 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 plasma. The concentration in the cerebrospinal fluid is about 50% of its concentration in plasma. Acyclovir crosses the placental barrier and accumulates in breast milk. The maximum concentration after oral use of 200 mg 5 times a day is 0.7 mcg / ml, the time to reach the maximum concentration is 1.5-2 hours.
It is metabolized in the liver to form the pharmacologically inactive compound 9-carboxymethoxymethylguanine. The elimination half-life in adults with normal renal function is 2-3 hours. In patients with severe renal insufficiency, the half-life is 20 hours, with hemodialysis -5.7 hours (while the concentration of acyclovir in plasma decreases to 60% of the initial value). About 84% is excreted unchanged by the kidneys and 14% in the form of a metabolite. The renal clearance of acyclovir is 75-80% of the total plasma clearance. Less than 2% of acyclovir is eliminated from the body through the intestines.
Indications
-Treatment of skin and mucosal infections caused by Herpes simplex viruses type I and II, both primary and secondary, including genital herpes.
– Prevention of exacerbations of recurrent infections caused by Herpes simplex viruses type I and II in patients with normal immune status. Prevention of primary and recurrent infections caused by Herpes simplex viruses type I and II in patients with immunodeficiency.
– As part of the complex therapy of patients with severe immunodeficiency: with HIV infection (AIDS stage, early clinical manifestations and detailed clinical picture) and in patients who have undergone bone marrow transplantation.
– Treatment of primary and recurrent infections caused by Varicella zoster virus (chickenpox, as well as shingles – Herpes zoster).
Use during pregnancy and lactation
Use during pregnancy is only possible if the intended benefit to the mother outweighs the potential risk to the fetus. Acyclovir crosses the placental barrier and accumulates in breast milk. If it is necessary to take acyclovir during lactation, discontinuation of breastfeeding is required.
Contraindications
Hypersensitivity to acyclovir, ganciclovir, famciclovir, valacyclovir or any excipient of the drug.
The drug is contraindicated during lactation.
Children under 3 years of age (for this dosage form)
With caution: pregnancy, the elderly, and patients receiving high doses, especially in the presence of dehydration, impaired renal function, neurological disorders, or neurological reactions to cytotoxic medications (including in the anamnesis).
Side effects
From the gastrointestinal tract: in isolated cases – abdominal pain, nausea, vomiting, diarrhea.
Laboratory parameters: 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, tremor, dizziness, fatigue, exhaustion, drowsiness, insomnia, confusion, hallucinations, decreased concentration.
Allergic reactions: skin rash, pruritus, Lyell’s syndrome, urticaria, erythema multiforme, including Stevens-Johnson syndrome, fever.
Other: rarely-alopecia, peripheral edema, visual impairment, lymphadenopathy.
Interaction
Concomitant use with probenecid leads to an increase in the average half-life and a decrease in the clearance of acyclovir. Concomitant use with nephrotoxic drugs increases the risk of impaired renal function.
How to take, course of use and dosage
Inside. The drug is taken during or immediately after a meal and washed down with a sufficient amount of water. Treatment should be started as soon as possible, immediately after the first symptoms of the disease appear.
The dosage regimen is set individually depending on the severity of the disease.
In the treatment of skin and mucosal infections caused by Herpes simplex type I and II:
Adults: the drug is prescribed 200 mg 5 times a day for 5 days at 4-hour intervals during the day and at 8-hour intervals at night. In more severe cases of the disease, the course of treatment can be extended by a doctor’s prescription for up to 10 days. As part of complex therapy for severe immunodeficiency, including with a detailed clinical picture of HIV infection (including early clinical manifestations of HIV infection and the stage of AIDS), after bone marrow implantation,400 mg is prescribed 5 times a day.
To prevent relapses of infections caused by Herpes simplex viruses type I and II, patients with normal immune status and with 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.
For the prevention of infections caused by Herpes simplex viruses type I and II, adults with immunodeficiency, the drug is recommended to be prescribed 200 mg 4 times a day every 6 hours, the maximum dose is up to 400 mg of acyclovir 5 times a day, depending on the severity of the infection.
Children: for the treatment of Herpes simplex infection and prevention of this infection in patients with weakened immune defenses, children over 3 years of age receive the same dose as adults.
In the treatment of Varicella zoster infections:
Adults: 800 mg 5 times a day every 4 hours during the day and at 8-hour intervals at night. The duration of treatment is 7-10 days.
Children: with chickenpox,20 mg/kg is prescribed 4 times a day for 5 days (the maximum single dose is 800 mg), children from 3 to 6 years: 400 mg 4 times a day, older than 6 years: 800 mg 4 times 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:
When treating and preventing 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 2 times a day at 12-hour intervals.
In the treatment of Varicella zoster infections 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 creatinine clearance up to 25 ml / min,800 mg 3 times a day with 8-hour intervals is prescribed.
Overdose
Oral use of 20 g of acyclovir did not lead to the development of specific symptoms.
Side effects may occur from the side. CNS – convulsions, tremors, lethargy.
In case of overdose after oral use, it is necessary to induce vomiting (preferably within 30 minutes after taking the drug) and take absorbents.
In case of acute renal failure and anuria: maintenance of vital functions, hemodialysis. Peritoneal dialysis is less effective.
Description
Round flat-cylindrical blue tablets with beveled edges on both sides and a risk on one side.
Special instructions
Long-term or repeated treatment with acyclovir in patients with reduced immunity may lead to the appearance of virus strains that are insensitive to its action.
Use strictly as prescribed by your doctor to avoid complications.
Caution should be used in 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 intake of a sufficient amount of fluid.
When taking the drug, renal function (blood urea and plasma creatinine levels) should be monitored.
Acyclovir does not prevent sexual transmission of herpes, so during treatment it is necessary to refrain from sexual contact, even in the absence of clinical manifestations.
Form of production
Tablets 200 mg. 10 tablets each in an aluminum strip. 1 strip in a cardboard box with instructions.
Storage conditions
At a temperature not exceeding 25 °C, in a place protected from light. Keep out of reach of children.
Shelf
life is 4 years. Do not use the product after the expiration date.
Active ingredient
Acyclovir
Conditions of release from pharmacies
By prescription
Dosage form
Tablets
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