Valvir - instructions for use, analogs, reviews and release forms (tablets 500 mg and 1000 mg) of the drug for the treatment of labial and genital herpes, shingles in adults, children and pregnancy. Composition and alcohol

In this article, you can read the instructions for using the drug Valvier. Presented are reviews of visitors to the site - consumers of this medication, as well as opinions of physicians specialists on the use of Valvir in their practice. A big request is to actively add their feedback on the drug: the medicine helped or did not help get rid of the disease, which were observed complications and side effects, possibly not declared by the manufacturer in the annotation. Analogues of Valvir in the presence of existing structural analogs. Use for the treatment of labial and genital herpes, shingles in adults, children, as well as during pregnancy and lactation. Composition and interaction of the drug with alcohol.

Valvier - antiviral drug. In the human body Valaciclovir (the active substance of the drug Valvir) quickly and completely turns into Acyclovir and L-valine under the influence of valacyclovirhydrolase.

Acyclovir has specific inhibitory activity against Herpes simplex virus types 1 and 2 (herpes simplex), Varicella zoster (shingles) and Epstein-Barr, cytomegalovirus (CMV) and human herpesvirus type 6. Acyclovir inhibits the synthesis of viral DNA immediately after phosphorylation and conversion into active form of acyclovir triphosphate. The first stage of phosphorylation occurs with the participation of virus-specific enzymes. For viruses Herpes simplex, Varicella zoster and Epstein-Barr, such an enzyme is viral thymidine kinase, which is present in virus-infected cells. Partial selectivity of phosphorylation persists in CMV and is mediated through the product of the phosphotransferase UL 97 gene. Activation of acyclovir with a specific viral enzyme to a great extent explains its selectivity.

The process of phosphorylation of acyclovir (conversion from mono- to triphosphate) is completed by cellular kinases. Acyclovir triphosphate competitively inhibits viral DNA polymerase and, being an analogue of the nucleoside, is inserted into viral DNA,which leads to an obligate (complete) rupture of the chain, termination of DNA synthesis and, consequently, to blocking the replication of the virus.

In patients with preserved immunity, Herpes simplex and Varicella zoster viruses with a low sensitivity to valacyclovir are extremely rare (less than 0.1%), but can sometimes be found in patients with severe impairment of immunity, for example, with bone marrow transplant, in chemotherapy for malignant neoplasms and those infected with HIV.

Resistance is caused by a deficiency of thymidine kinase of the virus, which leads to excessive spread of the virus in the host organism. Sometimes a decrease in sensitivity to acyclovir is due to the appearance of strains of the virus with a violation of the structure of the viral thymidine kinase or DNA polymerase. The virulence of these varieties of the virus resembles that of its wild strain.

Composition

Valaciclovir hydrochloride hydrate + auxiliary substances.

Pharmacokinetics

Valaciclovir and acyclovir have similar pharmacokinetic parameters after oral administration. After oral administration, valaciclovir is well absorbed from the digestive tract,quickly and almost completely converted into acyclovir and L-valine. This transformation is catalyzed by the enzyme valacyclovirhydrolase, isolated from the human liver. When taking valaciclovir in a dose of 1 g, the bioavailability of acyclovir is 54% and does not depend on the intake of food. The degree of binding of acyclovir to plasma proteins is very low - about 15%. Acyclovir is rapidly distributed among body tissues, especially in the liver, kidneys, muscles, lungs. It also penetrates the secret of the vagina, cerebrospinal fluid and herpetic vesicle fluid. Valacyclovir is excreted in the urine, mainly in the form of acyclovir (more than 80% of the dose) and its metabolite 9-carboxymethoxymethylguanine, less than 1% of the drug is unchanged.

Indications

• treatment of herpes zoster;
• treatment and prevention of recurrences of infections of the skin and mucous membranes caused by the herpes simplex virus (including newly diagnosed and recurrent genital herpes);
• treatment of labial herpes;
• reducing the infection of genital herpes of a healthy partner, if taken as a suppressive therapy in combination with safe sex;
• Prevention of cytomegalovirus infection that occurs during organ transplantation (reduces the severity of the reaction of acute graft rejection in patients with kidney transplants, the development of opportunistic infections and other viral infections caused by the viruses Herpes simplex and Varicella zoster) in adults and children over 12 years of age.

Forms of release

Tablets coated with 500 mg and 1000 mg.

Other dosage forms, whether capsules, ointment or cream, at the time of publication of the drug in the Directory did not exist.

Instructions for use and dosing regimen

The drug is administered to adults inside.

With herpes zoster, 1000 mg 3 times a day for 7 days.

With simple herpes, 500 mg twice a day. In case of relapse, the course should be 3 or 5 days. At the first episode with a heavy course, the duration of treatment can be increased to 10 days (with relapses, it is ideal to appoint Valvir in the prodromal period or when the first symptoms of the disease, i.e., tingling, itching, burning) occur.

For the treatment of labial herpes, it is effective to administer the drug at a dose of 2 grams 2 times for 1 day: the second dose should be taken after about 12 hours (but not earlier than 6 hours) after the first dose (do not apply this dosing regimen for more than 1 day, because the,as shown, this does not provide additional clinical benefits).

Prevention of recurrence 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 twice a day; for adult patients with immunodeficiency - 500 mg 2 times a day. The duration of the course is 4-12 months.

Prevention of infection with genital herpes of a healthy partner: infected heterosexual adults with preserved immunity and with the number of exacerbations up to 9 a year prescribed 500 mg once a day for 1 year or more, every day with regular sexual activity, with occasional sexual intercourse, Valvir should be taken start 3 days before the alleged sexual contact (data on the prevention of infection in other populations of patients are absent).

Prevention of cytomegalovirus infection: adults and adolescents over 12 years - 2 grams 4 times a day (as soon as possible, after transplantation). The duration of the course is 90 days, but in patients at high risk, treatment may be longer.

Patients on dialysis should be prescribed Valvir after the end of the hemodialysis session.

It is often necessary to determine the clearance of creatinine (CC), especially during periods when the kidney function changes rapidly, for example, immediately after transplantation or engraftment of the graft. In this case, the dose of Valvir is adjusted in accordance with the QA indices.

With poorly and moderately expressed liver cirrhosis (the synthetic function of the liver is preserved), correction of the dose of the drug is not required. Pharmacokinetic data in patients with severe liver cirrhosis (with a violation of the synthetic function of the liver and the presence of shunts between the portal system and the common vascular bed) also do not indicate the need for correction of the dose of Valvir, but the experience of its clinical use for this pathology is limited.

In elderly people, dose adjustment is not required, except for a significant impairment of kidney function. It is necessary to maintain an adequate water-electrolyte balance.

Side effect

• nausea;
• discomfort in the abdomen, incl. abdominal pain, vomiting, diarrhea;
• reversible violations of functional liver tests, which are sometimes regarded as manifestations of hepatitis;
• anaphylaxis;
• headache;
• agitation, including aggressive behavior;
• dizziness;
• confusion of consciousness;
• hallucinations;
• decreased mental abilities;
• excitation;
• tremor;
• ataxia;
• dysarthria;
• psychotic symptoms, including mania;
• depression;
• convulsions;
• encephalopathy;
• coma;
• rashes, including photosensitivity manifestations;
• itching;
• hives;
• angioedema;
• hematuria (often associated with other disorders of the kidneys);
• impaired renal function;
• acute renal insufficiency;
• renal colic (may be associated with impaired renal function);
• precipitation of acyclovir crystals in the lumen of renal tubules;
• impaired vision;
• leukopenia (mainly in patients with reduced immunity), thrombocytopenia, neutropenia, aplastic anemia, leukoplastic vasculitis, thrombotic thrombocytopenic purpura;
• erythema multiforme;
• decreased hemoglobin;
• dysmenorrhea;
• arthralgia;
• nasopharyngitis;
• respiratory tract infections;
• swelling of the face;
• increased blood pressure;
• tachycardia;
• fatigue;
• fever;
• dehydration;
• rhinorrhea.

Contraindications

• clinically expressed forms of HIV infection with a CD4 + lymphocyte content of less than 100 / μL;
• bone marrow transplantation;
• kidney transplantation;
• children's age (up to 12 years with CMV, up to 18 years - according to other indications);
• increased sensitivity to valacyclovir, acyclovir and other components of the drug.

Carefully

In patients with renal insufficiency; in patients with clinically expressed forms of HIV infection; with the simultaneous administration of nephrotoxic drugs.

Application in pregnancy and lactation

Use in pregnancy is possible if the expected effect of therapy for the mother exceeds the potential risk to the fetus (information on use in pregnancy is not enough).

Acyclovir, the main metabolite of valacyclovir, is excreted in breast milk. When Valvir therapy Valium breast feeding is possible, if the expected effect of therapy for the mother exceeds the potential risk for the child.

Use in children

Contraindicated for children under 12 years with CMV, up to 18 years - for the rest of the indications. The experience of clinical use of the drug in children is absent.

Application in elderly patients

In elderly people, dose adjustment is not required, except for a significant impairment of kidney function. It is necessary to maintain an adequate water-electrolyte balance.

special instructions

The use of the drug in high doses for a long time in 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 lethal outcome. When there are side effects from the central nervous system (including agitation, hallucinations, confusion, delusions, convulsions and encephalopathy), the drug is canceled.

Patients with a risk of dehydration, especially elderly patients, during treatment with Valvir should ensure adequate hydration of the body. Patients with renal insufficiency have an increased risk of developing neurological complications.

If liver function is impaired in patients with mild to moderate liver cirrhosis (the synthetic function of the liver is preserved), Valve's dose adjustment is not required. In the study of pharmacokinetics in patients with severe cirrhosis of the liver (with a violation of the synthetic function of the liver and the presence of shunts between the portal system and the common vascular bed)evidence of the need for correction of the dosing regimen; However, the clinical experience of using Valvir in this category of patients is organic. There is no data on the use of Valvir in high doses (4 g per day or more) in patients with liver disease, so caution should be given to the drug in high doses of this category of patients.

Older patients are not required to adjust the dose, except in cases of significant renal dysfunction. It is necessary to maintain an adequate water-electrolyte balance.

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

Impact on the ability to drive vehicles and manage mechanisms

Care should be taken in case of development of adverse reactions affecting the speed of psychomotor reactions.

Drug Interactions

The simultaneous use of Valvir with nephrotoxic drugs, including. aminoglycosides, organic compounds of platinum, iodinated contrast agent, methotrexate, pentamidine, foscarnet, cyclosporine and tacrolimus should be performed with caution, especially in patients with impaired renal function, and requires regular monitoring of renal function.

It is forbidden to use Valvir together with alcohol because of potential hepatotoxicity and the negative effect of this combination on the liver.

Clinically significant interaction is not established

Cimetidine and probenecid after taking 1 g of valaciclovir increases the AUC of acyclovir, decreasing its renal clearance (however, dose adjustment of valacyclovir is not required because of the wide therapeutic range of acyclovir).

Caution should be exercised in case of simultaneous use of valacyclovir in high doses (4 g per day) and drugs that compete with acyclovir for elimination (the latter is eliminated with urine unchanged as a result of active tubular secretion);since there is a potential threat of an increase in plasma concentrations of one or both of the drugs or their metabolites.

With the simultaneous use of acyclovir with mycophenolate mofetil, there was an increase in the AUC of acyclovir and the inactive metabolite of mycophenolate mofetil.

Analogues of Valvir

Structural analogs for the active substance:

• Vairova;
• Valavir;
• Valaciclovir;
• Walogard;
• Valtrex;
• Valtsikon;
• Wirdel.

Analogues on the curative effect (agents for the treatment of herpes simplex):

• Amiksin;
• Anaferon;
• Anaferon child;
• Antigerpes;
• Arbidol;
• Acyclovir;
• Walogard;
• Valtrex;
• Valtsikon;
• Vectavir;
• Virazole;
• Wirdel;
• Virolex;
• Virosept;
• Vitaherpavak;
• Viferon;
• Galavit;
• Gevisos;
• Gerpevir;
• Herpes;
• Herpferon;
• Groprinosin;
• Devirs;
• Zovirax;
• Isoprinosine;
• Immunomax;
• Kagocel;
• Kipferon;
• Lavomax;
• Lysavir;
• Lycopid;
• Lorinden C;
• Neovir;
• Panavir;
• Supperan;
• Famvir;
• Fenistil Pencivir;
• Ferrovir;
• Cyclovax;
• Cyclovir;
• Cycloviral;
• Cycloferon;
• Cytivir;
• Epigene Intim;
• Erazaban;
• Ergoferon.

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