Description
Release form
Film-coated tablets.
Packing
42 pcs.
Pharmacological action
Valcicon is an antiviral agent of the group of nucleoside analogues. Valaciclovir is an acyclovir L-valine ester, thus being a prodrug. After absorption into the blood, valaciclovir is almost completely converted to acyclovir under the influence of the hepatic enzyme valacyclovir hydrolase.
Acyclovir formed from valaciclovir, in turn, penetrates into cells infected with the virus, where, under the influence of the viral enzyme, thymidine kinase is converted into monophosphate, then, under the influence of cellular kinases, into diphosphate and active triphosphate. Acyclovir triphosphate inhibits DNA polymerase and, thus, disrupts the replication of the DNA of the virus.
In addition, impaired viral DNA replication may result from the incorporation of acyclovir into its structure. Thus, the high selectivity of valaciclovir for tissues affected by the virus is due to the fact that stage I of the phosphorylation reaction chain is mediated by the enzyme produced by the virus itself. Active against Herpes simplex viruses types 1 and 2, Varicella zoster, cytomegalovirus, Epstein-Barr virus, human herpes virus 6.
Indications
Treatment and prevention of infectious diseases caused by Herpes zoster.
Prevention of cytomegalovirus infection developing during organ transplantation.
Contraindications
Hypersensitivity to valaciclovir, acyclovir.
Pregnancy and lactation
Limited data are available on the use of valaciclovir during pregnancy. Valacyclovir is used only in cases where the potential benefit to the mother outweighs the potential risk to the fetus.
Recorded pregnancy outcome in women taking valaciclovir or acyclovir (an active metabolite of valaciclovir) did not show an increase in the number of birth defects in their children compared to the general population. Since the register includes a small number of women who took valaciclovir during pregnancy, it is impossible to draw reliable and definite conclusions about the safety of using valaciclovir during pregnancy.
Acyclovir, the main metabolite of valaciclovir, is excreted in breast milk. After taking valaciclovir orally at a dose of 500 mg, Cmax of acyclovir in breast milk was 0.5 2.3 times (on average 1.4 times) higher than the corresponding concentrations of acyclovir in maternal blood plasma. The mean concentration of acyclovir in breast milk was 2.24 μg / ml (9.95 μmol / L).
When a mother takes valaciclovir orally at a dose of 500 mg 2 times / day, the child will undergo the same effects of acyclovir as when taking acyclovir orally at a dose of about 0.61 mg / kg / day.
Special instructions
Elderly patients, persons with dehydration during the treatment period need to 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
1 tablet contains:
valaciclovir hydrochloride 556 mg, which corresponds to the content of 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 CC 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 hours, with KK less than 10 – 500 mg every 24 hours. – 10 days
with recurrent genital herpes (including with KK 30-49 ml / min / 1.73 sq.m) – 500 mg 2 times a day, with KK less than 30 – 500 mg every 24 hours. treatment – 3 days.
Treatment is started at the onset of signs or symptoms of relapse 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 the number of CD4 + cells more than 100 / μl (including with CC 30-49) – 500 mg 2 times a day, with CC less than 30 – 500 mg every 24 hours
to reduce the risk of transmission of the infection to the sexual partner with the number of relapses less than 9 per year, the sexual partner is prescribed 500 mg 1 time per 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 on hemodialysis, 1.5 g 1 time per day. The course of treatment is 90 days.
Take the drug as soon as possible after transplantation. For patients on 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
From the side of the central nervous system: headache, dizziness, psychotic symptoms, agitation, decreased mental ability, ataxia, coma, confusion or depression of consciousness, dysarthria, encephalopathy, mania, hallucinations, convulsions, tremors. These reactions are reversible and are usually observed in patients with impaired renal function or against the background of other predisposing conditions. In patients with a transplanted organ, receiving valaciclovir in high doses (8 g / day) for the prevention of cytomegalovirus infection, neurological reactions develop more often than when taken in lower doses.
From the respiratory system: dyspnea.
From the digestive system: nausea, abdominal discomfort, vomiting, diarrhea, reversible impairment of functional liver tests (increased activity of ALT, AST, alkaline phosphatase), which are sometimes regarded as manifestations of hepatitis.
From the hemopoietic system: leukopenia (mainly observed in patients with reduced immunity), thrombocytopenia, anemia, thrombotic thrombocytopenic purpura.
From the skin: erythema multiforme, rashes, photosensitivity, alopecia.
Allergic reactions: itching, urticaria, angioedema, anaphylaxis.
From the urinary system: pain in the projection of the kidneys, impaired renal function, including acute renal failure, renal colic. Renal colic may be associated with impaired renal function.
On the part of the sensory organs: impaired vision.
On the part of laboratory parameters: a decrease in hemoglobin, hypercreatininemia.
Other: dysmenorrhea, nasopharyngitis, respiratory tract infections, increased blood pressure, tachycardia, fatigue.
Patients with severely impaired immunity, especially in adult patients with advanced stages of HIV infection who have been receiving valaciclovir in high doses (8 g / daily) for a long time, have observed cases of renal failure, microangiopathic hemolytic anemia and thrombocytopenia (sometimes combined) . Similar adverse reactions were noted in patients with the same diseases, but not receiving valaciclovir.
Drug Interactions
Cimetidine and tubular secretion blockers reduce the effect (decrease the rate, 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: Acute renal failure and the development of neurological symptoms, including confusion, hallucinations, agitation, depression of consciousness and coma, may also occur with valaciclovir overdose. To prevent overdose, caution should be exercised when using the drug. Many cases of overdose have been associated with the use of the drug for the treatment of patients with impaired renal function and elderly patients, due to non-compliance with the dosing regimen (repeated doses of valacyclovir exceeding the recommended).
Treatment. Patients should be closely monitored for timely diagnosis of toxicities. Hemodialysis significantly accelerates the excretion of acyclovir from the blood plasma and may be considered as the optimal treatment in the case of symptomatic overdose.
Storage Conditions
The product should be stored out of reach of children, protected from light at a temperature not exceeding 25 ° C.
Shelf life
2 years.
Active ingredient
Valaciclovir
Terms and conditions
prescription
dosage form
tablets
Indications
Indications
Genital herpes, , Tinea
Vertex, Russia
