valaciclovir | Valvir tablets is covered.pl.ob. 500 mg 10 pcs.

Release form

Film-coated tablets.

Packing

10 pcs.

Pharmacological action of

In the human body, valaciclovir is rapidly and completely converted to acyclovir and L-valine under the influence of valaciclovir hydrolase.

Acyclovir in vitro has specific inhibitory activity against viruses: Herpes simplex types 1 and 2, Varicellazoster, Epstein-Barr, cytomegalovirus (CMV), human herpes virus type 6

Acyclovir inhibits the synthesis of viral deoxyribonucleic acid (DNA) immediately after phosphorylation into the active form of acyclovir triphosphate. Acyclovir triphosphate competitively inhibits viral DNA polymerase and, being a nucleoside analogue, integrates into viral DNA, which leads to complete chain breaking and termination of DNA synthesis (hence, blocking virus replication).

Contraindications

- hypersensitivity to valaciclovir, acyclovir and other components of the drug

- clinically pronounced forms of HIV infection with a CD4 + lymphocyte count of less than 100 / Ојl

- bone marrow transplantation

- children under 12 years old , up to 18 years - according to other indications).

Precautions: liver failure (high doses of the drug), renal failure, pregnancy, lactation.

Special instructions

Taking the drug in high doses for a long time under conditions accompanied by severe immunodeficiency (bone marrow transplantation, clinically expressed forms of HIV infection, kidney transplantation), led to the development of thrombocytopenic purpura and hemolytic-uremic syndrome, up to a fatal outcome. In case of side effects from the central nervous system (including agitation, hallucinations, confusion, delirium, seizures and encephalopathy), the drug is canceled.

Patients at risk of dehydration, especially elderly patients, need adequate hydration during treatment with Valvir. Patients with renal failure have an increased risk of developing neurological complications.

In cases of impaired liver function in patients with mild or moderate hepatic cirrhosis (synthetic liver function is preserved), dose adjustment of Valvir is not required. In the study of pharmacokinetics in patients with severe cirrhosis of the liver (with impaired synthetic liver function and the presence of shunts between the portal system and the common vascular bed), no data were obtained indicating the need for correction of the dosage regimen, however, clinical experience with the use of the drug Valvir in this category of patients is organic. There is no data on the use of Valvir in high doses (4 g / or more) in patients with liver diseases, therefore, it is necessary to prescribe the drug with high doses in this category of patients.

Elderly patients do not need dose adjustment except in cases of significant impairment of renal function. It is necessary to maintain an adequate water-electrolyte balance.

Special studies to study the effect of Valvir in patients with liver transplantation have not been conducted. However, it has been shown that prophylactic administration of acyclovir in high doses reduces cytomegalovirus infection. Suppressive therapy with Valvir reduces the risk of transmission of genital herpes, but does not completely exclude it and does not lead to a complete cure. During drug therapy, Valvirpatsient should take measures to ensure the safety of the partner during sexual intercourse.

Composition

1 film-coated tablet contains: active substance: valacyclovir hydrochloride hydrate 611.70 mg, corresponding to 500 mg of valacyclovir excipients film coating - for details, read the instructions.

Dosage and Administration

Inside. Adults

Herpes Zoster - 1000 mg 3 times a day for 7 days.

Herpes simplex - 500 mg 2 times a day. In case of relapse, the course should be 3 or 5 days. In the first episode with a severe course, the duration of treatment can be increased to 10 days (for relapses, it is ideal to prescribe Valvir in the prodromal period or when the first symptoms of the disease appear, i.e., pinching, itching, burning).

For the treatment of labial herpes, it is effective to prescribe the drug in a dose of 2 g 2 times for 1 day: the second dose should be taken after about 12 hours (but not earlier, less than 6 hours) after the first dose (do not use this dosage regimen for more than 1 day, since, as shown, this does not provide additional clinical benefits). Prevention of relapse of infections caused by the herpes simplex virus: in patients with preserved immunity - 500 mg once a day with very frequent relapses (10 or more per year) - 250 mg 2 times a day for adult patients with immunodeficiency - 500 mg 2 once a day. The duration of the course is 4-12 months.

Prevention of infection with a healthy partner with genital herpes: an infected heterosexual adult with immunity and with exacerbations of up to 9 per year - 500 mg once a day for 1 year or more, every day with regular sexual activity, with irregular sexual contacts, Valvira should be started 3 days before the alleged sexual contact (data on infection prevention in other patient populations are not available). Prevention of cytomegalovirus infection: adults and adolescents over 12 years old - 2 g 4 times a day (as soon as possible, after transplantation). The course lasts 90 days, but in patients at high risk, treatment may be longer.

Side effects

The most common adverse reactions with valaciclovir are: headache and nausea, more serious adverse reactions: thrombotic thrombocytopenic purpura / hemolytic-uremic syndrome, acute renal failure and neurological disorders.

Adverse reactions are listed below in accordance with the classification of major systems and organs and frequency of occurrence: very often -? 1/10 often -? 1/100 or <1/10 sometimes -? 1/1000 or <1/100 rarely - 1/10000 or < 1/1000 is very rare - <1/10000.

From the gastrointestinal tract: often - nausea is rare - abdominal discomfort, including abdominal pain, vomiting, diarrhea is very rare - reversible impaired liver function tests, which are sometimes regarded as manifestations of hepatitis.

From the blood and lymphatic system: very rarely - leukopenia (mainly in patients with reduced immunity), thrombocytopenia.

On the part of the immune system: very rarely - anaphylaxis.

Mental disorders and disorders of the nervous system: often - headache sometimes - agitation, including aggressive behavior rarely - dizziness, confusion, hallucinations, decreased mental ability very rarely - agitation, tremor, ataxia, dysarthria, psychotic symptoms, including mania depression, convulsions, encephalopathy, coma. The listed symptoms are reversible and are usually observed in patients with impaired renal function or with other diseases. In patients with a transplanted organ receiving high doses of valaciclovir (8 g / day) for the prevention of CMV infection, neurological reactions develop more often than when taking lower doses.

On the part of the respiratory and mediastinal organs: sometimes - dyspnea.

On the part of the skin and subcutaneous tissue: sometimes rashes, including photosensitivity manifestations rarely - itching.

Allergic reactions: very rarely - urticaria, angioedema.

From the urinary system: rarely - impaired renal function very rarely - acute renal failure, renal colic (may be associated with impaired renal function).

Other: in patients with severely impaired immunity, especially in patients with advanced stages of acquired immune deficiency syndrome, receiving high doses of valaciclovir (8 g / day) for a long time, there have been cases of renal failure, microangiopathic hemolytic anemia and thrombocytopenia (sometimes in combination). Similar complications were noted in patients with the same diseases, but not receiving valaciclovir.

It is not possible to determine the frequency of some adverse reactions according to the available data.

On the part of the sensory organs: impaired vision.

From the hemopoietic organs: neutropenia, aplastic anemia, leukoplastic vasculitis, thrombotic thrombocytopenic purpura.

From the skin: erythema multiforme.

Laboratory indicators: hemoglobin decrease, hypercreatininemia.

Other: dysmenorrhea, arthralgia, nasopharyngitis, respiratory tract infections, swelling of the face, increased blood pressure, tachycardia, fatigue in children additionally - fever, dehydration, rhinorrhea.

Drug Interactions

No clinically significant interactions have been established.

Cimetidine and probenecid after taking 1 g of valaciclovir increase the AUC of acyclovir, reducing its renal clearance (however, dose adjustment of valacyclovir is not required due to the wide therapeutic index of acyclovir).

Caution must be exercised in the case of simultaneous use of valaciclovir in high doses (4 g /) and drugs that compete with acyclovir for the elimination route (the latter is eliminated unchanged in the urine as a result of active tubular secretion), since there is a potential threat of an increase in plasma levels of one or both drugs or their metabolites. With the simultaneous use of acyclovir with mycophenolate mofetil, an increase in AUC of the first and inactive metabolite of the second was noted.

Caution should also be exercised when combining valaciclovir in high doses (4 g / above) with drugs that affect kidney function (eg, cyclosporine, tacrolimus).

Overdose of

There are currently not enough data on overdose of valaciclovir.

Symptoms: A single dose of an overdose of acyclovir up to 20 g, which was partially absorbed from the gastrointestinal tract, was not accompanied by the toxic effect of the drug. When ingested within a few days, ultra-high doses of acyclovir developed nausea, vomiting, headache, confusion with iv administration - increased serum creatinine concentration, development of renal failure, confusion, hallucinations, agitation, convulsions, coma.

Treatment: Patients should be closely monitored for signs of toxicity. Hemodialysis significantly enhances the removal of acyclovir from the blood and can be considered the treatment of choice for patients with an overdose of valacyclovir.

Storage conditions

At a temperature not exceeding 30 РC. Keep out of reach of children.

The Expiration of

is 18 months.

Do not use after the expiry date.

active substance

Valaciclovir

lekarstvennaja form

tablets

Appointment

for adults

eye disease indications

Indications

Herpes, Cytomegalovirus infection, Genital herpes, Herpes zoster