Description
Release form
Tablets
Packing
10 pcs.
Pharmacological action
Farmgroup: antiviral agent.
Pharmaceutical Action: Nucleoside inhibitor of DNA herpesvirus polymerase.
Blocks viral DNA synthesis and virus replication.
In the human body, it turns into acyclovir and L-valine as a result of phosphorylation of active acyclovir triphosphate from acyclovir, which competitively inhibits viral DNA polymerase.
The first phase of phosphorylation occurs under the influence of a virus-specific enzyme (for Herpes simplex types 1 and 2, Varicella zoster is a viral thymidine kinase that is found only in cells infected with the virus).
More active against Herpes simplex than Varicella zoster.
Pharmacokinetics: Absorption – high, quickly and almost completely turns into acyclovir and L-valine. The bioavailability of acyclovir when taking 1 g of valaciclovir is 54% (3-5 times higher than when taking acyclovir orally). After applying valaciclovir at a dose of 1 g 4 times a day, the AUC is approximately equal to AUC with iv administration of acyclovir at a dose of 5 mg every 8 hours. Cmax after a single dose of 1 g is 15-25 μmol / ml, TCmax 1.6-2.1 hours 3 h unmetabolized valaciclovir in plasma is not determined.
Communication with proteins of valaciclovir – 13-18%, acyclovir – 9-33%.
Acyclovir is widely distributed in tissues and body fluids, including the brain, kidneys, lungs, liver, aqueous humor, lacrimal fluid, intestines, muscles, spleen, uterus, mucous membrane and vaginal secretion, sperm, amniotic fluid, CSF (50% of concentration in plasma), liquid of herpetic vesicles. The highest concentrations are in the kidneys, liver, and intestines. It crosses the placenta and into breast milk.
T1 / 2 of valaciclovir – less than 30 min of acyclovir – 2.5-3.3 h, at the terminal stage of renal failure – 14 hours, in elderly patients (65-83 years) – 3.3-3.7.
It is excreted by the kidneys (45.6%), mainly in the form of acyclovir and its metabolite 9-carboxymethoxymethylguanine, less than 1% unchanged and with feces (47.12%) for 96 hours.
Indications
In adults:
cold sores, genital herpes (primary and recurrent infection, prolonged suppressive therapy of recurrent genital herpes in people with immunodeficiency, including HIV infection, reducing the risk of transmission of the infection to the sexual partner), herpes zoster.
In adults and children over 12 years of age:
prophylaxis of cytomegalovirus infection during organ transplantation.
Contraindications
Hypersensitivity, HIV infection with a CD4 + lymphocyte count of less than 100 / Ојl, children (up to 12 years old with CMV, up to 18 years old according to other indications).
Caution. Hepatic / renal failure, old age, hypohydration, concomitant use of nephrotoxic drugs, pregnancy, lactation, childhood.
Special instructions
Elderly patients, persons with dehydration during treatment should increase the amount of fluid consumed (risk of developing acute renal failure).
In the treatment of genital herpes, sexual contact should be avoided, as the drug does not protect against transmission.
Taking 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 fatal outcome.
In case of side effects from the central nervous system (including agitation, hallucinations, confusion, delirium, seizures and encephalopathy), the drug is canceled.
Composition
Valaciclovir 500 mg.
Dosage and Administration
Inside, regardless of food intake.
Adults, including with CRF and CC less than 50 ml / min / 1.73 sq.m: for cold sores of the lips (treatment begins when tingling, itching or burning) – 2 g every 12 hours, with KK 30-49 – 1 g every 12 hours, with KK 10-29 – 500 mg every 12 hours, with KK less than 10 – 500 mg once. The course of treatment is 1 day
with primary genital herpes (including with KK 30-49 ml / min / 1.73 sq.m) – 1 g 2 times a day, with KK 10-29 – 1 g every 24 h, with CC less than 10 – 500 mg every 24 hours. The course of treatment is 10 days
with recurrent genital herpes (including CC 30-49 ml / min / 1.73 sq.m) – 500 mg 2 times per day, with CC less than 30 – 500 mg every 24 hours. The course of treatment is 3 days. Treatment begins with the first signs or symptoms of
recurrence with prolonged suppressive therapy of recurrent genital herpes in people with immunodeficiency, including HIV infection – 1 g per day (including with CC 30-49), with CC less than 30 – 500 mg every 24 hours, with a relapse rate of less than 9 per year, it is possible to use (including with KK 30-49) – 500 mg per day, with KK less than 30 – 500 mg every 48 hours, in HIV-infected patients with more than CD4 + cells 100 / ?l (including with KK 30-49) – 500 mg 2 times a day, with KK less than 30 – 500 mg every 24 hours
to reduce the risk of transmission of the infection to the sexual partner when the number of relapses is less than 9 per year 500 mg is prescribed to the sexual partner once a day.
with herpes zoster – 1 g every 8 hours for 7 days (treatment begins within 48 hours after the rash appears), with KK 30-49 – 1 g every 12 hours, with KK 10-29 – 1 g every 24 hours, with CC less than 10 – 500 mg every 24 hours.
Adults and children over 12 years of age, including with CRF and CC less than 75 ml / min / 1.73 sq.m: prevention of CMV infection during organ transplantation – 2 g 4 times a day with CC 50-75 – 1.5 g 4 times a day with CC 25-50 – 1.5 g 3 times a day with CC 10-25 – 1.5 g 2 times a day with CC less than 10 and for patients undergoing hemodialysis, 1.5 g once a day. The course of treatment is 90 days. Take the drug as soon as possible after transplantation.
In patients undergoing hemodialysis, the drug is administered after the hemodialysis procedure. T1 / 2 in such patients – 4 hours during the 4-hour procedure, 30% of the drug is removed. With peritoneal dialysis, the drug is removed to a lesser extent, other pharmacokinetic parameters remain the same.
Side effects of the
From the digestive system: nausea, abdominal pain, vomiting, diarrhea, increased activity of ALT, AST, alkaline phosphatase, hepatitis.
On the part of the nervous system: headache, dizziness, depression, aggressive behavior, agitation, ataxia, coma, confusion or depression of consciousness, dysarthria, encephalopathy, mania, psychosis, including auditory and visual hallucinations, convulsions, tremors.
On the part of the sensory organs: impaired vision.
From the urinary system: pain in the projection of the kidneys, acute renal failure.
From the hemopoietic organs: neutropenia, thrombocytopenia, aplastic anemia, leukoclastic vasculitis, thrombotic thrombocytopenic purpura.
From the skin: erythema multiforme, rash, photosensitivity, alopecia.
Allergic reactions: angioedema, shortness of breath, itching, rash, urticaria, anaphylactic reactions.
Laboratory findings: Hb reduction, hypercreatininemia.
Other: dysmenorrhea, arthralgia, nasopharyngitis, respiratory tract infections, swelling of the face, increased blood pressure, tachycardia, fatigue additionally in children – fever, dehydration, rhinorrhea.
Drug interactions
Cimetidine and tubular secretion blockers reduce the effect (reduce the speed, but not the fullness of conversion to acyclovir). In individuals with normal CC, correction of the dosage regimen is not required.
Nephrotoxic drugs (including cyclosporine, tacrolimus) increase the risk of nephrotoxicity.
Overdose
Symptoms: possible deposition of acyclovir in the renal tubules, with the development of acute renal failure and anuria.
Treatment: hemodialysis.
Deystvuyuschee substances
valaciclovir
Conditions of release from drugstores
By recipe
Formulation
tablets
Appointment
Dlya vzrosl h
Indications
Colds, Cytomegalovirus infection, Herpes, Shingles, Vetryanaya ospa
Kanonfarma, Russia
