Valavir tablets 500mg №42

Description for VALAVIR ® Tablets 500 mg

General Characteristics

International and chemical name: valasiclovir; L-valine-2-[(2-amino-1 ,6-dihydro-6-oxo-9H-purin-9-yl) methoxy] ethyl ester hydrochloride.

The main physical and chemical properties: tablets of elongated shape with a lenticular surface, scored, film-pearl shell, almost white.

Ingredients: 1 tablet contains valacyclovir hydrochloride (in terms of valacyclovir 100% anhydrous substance) 500 mg.

Inactive ingredients: microcrystalline cellulose 101, a low molecular weight polyvinylpyrrolidone medical, aerosil, crospovidone, magnesium stearate, Serifilm 050 kandurin.

Product type

Film-coated tablets.

Pharmacotherapeutic group

Antivirals for systemic use. Valacyclovir. ATC code GO5A ^ V 11.

Pharmacological properties

Pharmacodynamics. Antiviral drug. Selective inhibitor of viral DNA polymerase. The human body turns into acyclovir and valine. Interacting with the viral DNA polymerase, blocking viral replication and reproduction. Effective against viruses Negres simr1eh types I and II, Varicella zoster, Epstein-Barr virus, cytomegalovirus, human herpesvirus type VI. Custom antiherpetic activity due to affinity for the thymidine kinase Negres simr1eh, Varicella zoster, Epstein-Barr virus, which is present only in cells infected with the virus. As a result of phosphorylation of acyclovir triphosphate is converted to active acyclovir, which competitively inhibits viral DNA synthesis.

Resistance to the drug is very rare, and mostly in immunocompromised patients (infection with HIV, patients who receive chemotherapy due to malignant neoplasms after bone marrow transplantation). Pharmacokinetics. Rapidly absorbed from the gastrointestinal tract after oral administration and almost completely hydrolyzed (forming acyclovir and valine). Bioavailability - 54%, independent of food intake. The maximum concentration of valacyclovir in the blood plasma In the mid-30 - 60 minutes after ingestion. Since plasma protein binds 15% of the drug. Half Life - 2.5 - 3.3 hours. Excreted in the urine of 45% (in the form of acyclovir and its metabolite 9-karboksimetoksitilguanina), with feces - 47%. Renal clearance is about 255 ml / min,

Indications for Use

Shingles (acute and postherpetic neuralgia, inclusive), infections of the skin and mucous membranes caused by the herpes simplex virus (primary and recurrent genital herpes, inclusive), prevention of recurrent herpes simplex (including genital herpes). The drug reduces the intensity and duration of pain in herpes infection, decreases the incidence of zosterassotsiirovannoy pain, including acute pain and postherpetic neuralgia.

Prevention of cytomegalovirus infection on the background of immunodeficiency (HIV infection, organ transplantation and bone marrow of cancer chemotherapy).

Dosage and administration

Inside, regardless of the meal. For the treatment of herpes zoster Valavir adults appoint 1000 mg 3 times daily for 7 days (the maximum efficiency observed when treatment was initiated within 48 hours after onset of rash).

When simplex virus, including genital herpes, including at relapse, 500 mg 2 times a day for 5 days, the first episode with severe treatment period may be extended to 10 days. Prevention of recurrence of infections caused by herpes simplex virus: patients with normal immune status is prescribed 500 mg 1 time per day. Patients with immunodeficiency - 500 mg 2 times a day. For the prevention of cytomegalovirus infection in adults and adolescents over 12 years, administered in a dose of 2 g 4 times a day as soon as possible after transplantation. Patients with renal insufficiency the dose is reduced:

    * Patients with herpes zoster with creatinine clearance 15-30 ml / min, appoint 1 000 mg 2 times a day, with creatinine clearance below 15 ml / min - 1 000 mg per day;
    * Patients with simple (including genital) herpes with creatinine clearance below 15 ml / min, administered at 500 mg 1 time a day in order to prevent recurrences of herpes simplex with creatinine clearance below 15 ml / min or hemodialysis - 250 mg 1 time a day;
    * For prevention of cytomegalovirus infection in creatinine clearance 50 - 75 ml / min to reduce the dose of 1.5 g 4 times a day, with creatinine clearance 25 - 50 ml / min
    * 1.5 g 3 times a day, with creatinine clearance 10-25 ml / min - 1.5 g 2 times a day, with creatinine clearance below 10 ml / min or dialysis - 1.5 g 1 per day.

Side effect

    * Digestive system: nausea, diarrhea, increased liver function tests.
    * The system of blood is rare - and thrombocytopenia.
    * Allergic reactions: rash, hives, itching, photosensitivity, rarely - angioedema, dyspnea, and anaphylaxis.
    * Kidneys are rarely - the deterioration of the function.
    * Nervous system: dizziness, hallucinations, very rarely - a coma, especially in patients with renal insufficiency.
    * Other: there is information about the occurrence of renal insufficiency, microangiopathy, hemolytic anemia and thrombocytopenia.

Contraindications

Hypersensitivity to valacyclovir or acyclovir, the other ingredients. Children under the age of 12.

Overdose

In case of overdose, the risk of side effects. In case of overdose - symptomatic and supportive therapy, hemodialysis accelerates the excretion of the drug.

Features of the application

Elderly patients during the treatment period is necessary to increase fluid intake. Patients with kidney disease in the history increases the risk of neurological complications. Patients who are on hemodialysis, should be taken Valavir after hemodialysis. In patients with liver cirrhosis mild or moderate severity is not necessary to dose adjustment. The data for the drug in children are missing.

Pregnancy and lactation. Experience in use for the treatment of pregnant and breastfeeding women is limited, care should be taken to appoint (especially in the first trimester of pregnancy), only if the expected benefit of therapy outweighs the potential risk to the fetus. Acyclovir in experimental conditions causes changes in the thymus and functional immunodeficiency. Valavir enters the breast milk, so the drug should be used with caution during lactation.

The effect on driving ability and other mechanisms

Valavir does not affect driving ability and other mechanisms.

Interaction with other medicinal products

No signs of clinically significant drug interaction has not been established. Acyclovir is excreted in the urine by active tubular secretion, and therefore other drugs that compete for this inference, can increase the concentration of acyclovir in the blood.

Tsimetedin, probenecid reduces renal clearance of some of acyclovir, but there is no need for dose adjustment of medication.

In combination with nephrotoxic drugs increases the risk of renal failure and disorders of the central nervous system.

Shelf life

Store in a dry place, protected from light and away from children at or above 25 ° C. Shelf life - 2 years.

Conditions of supply

Prescription.

Packaging

Of 6 tablets in blisters. By 7 stripes package (from B pills), nested in a pack. 10 tablets in blisters, nested in a pack.