Valacyclovir Tab n / a film about 500mg 10 pieces canon

Description

Composition
Active substance:
1 tablet coated with a film coating comprising valaciclovir hydrochloride (as monohydrate) based on the valaciclovir 500 mg ;.
Excipients:
Corn starch 56.8 mg colloidal silica (Aerosil) 2 mg Sodium croscarmellose 29 mg magnesium stearate 4 mg microcrystalline cellulose 72 mg;
Composition of film-coating: Opadry II White 22 mg, including: polyvinyl alcohol, 10.32 mg macrogol (polyethylene glycol) 5.19 mg talc 3.83 mg titanium dioxide 2.66 mg.
Description:
Oval biconvex tablets with Valium, film-coated white or nearly white. On the cross-section of the core is almost white.
Product form:
Tablets, film-coated, 500 mg.
At 7, 10, 14, 15 tablets in blisters of PVC film or PVC film / PVDC or PVC film / PCTFE printed and lacquered aluminum foil.
1, 2, 3, 6, the contour of cellular packages of 7 tablets or 1, 2, 3, 6 contour cell packs of 10 tablets, or 1, 3 blisters of 14 tablets, or 2, 4 blisters 15 tablets together with instructions for use placed in a pile of cardboard.
Contraindications
-Giperchuvstvitelnost to valaciclovir, aciclovir and any auxiliary ingredients in the preparation. – Clinically expressed form of HIV to CD4 + lymphocytes content of less than 100 / ml. -Children’s age (12 years for the prevention of cytomegalovirus infection), up to 18 years – for other indications).
Carefully:
Valaciclovir should be used with caution in the following situations: – Renal and hepatic failure -pozhiloy age -gipogidratatsiya -klinicheski expressed form of HIV – concomitant use of nephrotoxic drugs -Pregnancy and lactation.
Dosage
500 mg
Indications
Adults: -Treatment shingles (Herpes zoster) (drug helps relieve pain, reduce its duration and percentage of patients with pain caused by herpes zoster, including acute and post-herpetic neuralgia). -Treatment of infections of the skin and mucous membranes caused by the herpes simplex virus (HSV), including first identified and recurrent genital herpes (Herpes genitalis), as well as labial herpes (Herpes labialis). -Profilaktika (suppression) of recurrences of skin infections and mucous membranes caused by HSV, including genital herpes. prevention of transmission of herpes healthy general partner at reception as a suppressive therapy in combination with safer sex.
Adults and adolescents aged 12 years and older: – Prevention of cytomegalovirus (CMV) infection and acute transplant rejection reactions (in patients with kidney transplants). -Profilaktika opportunistic infections and other herpes virus infections (HSV, VZV) after organ transplantation.
Interaction with other drugs
Clinically significant interactions have not been established. Acyclovir is excreted by the kidneys mostly unchanged, actively secreting in the renal tubules. After assigning 1g valaciclovir, cimetidine and probenecid blocking tubular secretion, increase AUC acyclovir and reduce its renal clearance. However, this dose valaciclovir does not require any correction due to the wide therapeutic index of aciclovir.
Care must be taken in the case of simultaneous use of valaciclovir at higher doses (4 grams a day or more) and drugs that compete with acyclovir for elimination way since there is a potential threat increase in the plasma level of one or both drugs or their metabolites. AUC increase was noted acyclovir and inactive metabolite of mycophenolate mofetil, an immunosuppressive drug used in transplantation, while the use of these drugs. It should also be taken (observe the change of renal function) when combined valaciclovir at higher doses (4 g per day and more) with drugs that affect the other kidney (e.g. cyclosporin, tacrolimus).
Overdose
Symptoms and signs. Acute renal failure and neurological disorders, including confusion, hallucinations, agitation, depression of consciousness and coma, as well as nausea and vomiting have been observed in patients who received a dose of valaciclovir, exceeding recommended. Such conditions were more common in patients with renal impairment and elderly patients receiving repeated in excess of the recommended dose of valaciclovir, as a result of non-compliance with the dosing regimen.
Doing. Patients should be monitored closely to detect signs of toxic effects. Hemodialysis significantly enhances the removal of acyclovir from the blood and may be considered the method of choice in the management of patients with an overdose of valaciclovir.
pharmachologic effect
Pharmacological group:
An antiviral agent.
Pharmacodynamics:
In humans, valacyclovir is rapidly and completely converted to acyclovir, under the influence of valatsiklovirgidrolazy enzyme. Acyclovir has in vitro specific inhibitory activity against viruses: herpes simplex virus (HSV) 1 and type 2, varicella zoster virus and herpes zoster (VZV – varicella zoster virus), Cytomegalovirus (CMV), Epstein-Barr virus (EBV ), type 6 human herpes virus. Acyclovir inhibits viral DNA synthesis and the phosphorylation immediately after conversion into the active acyclovir triphosphate form. The first stage of phosphorylation requires the activity of a virus-specific enzyme. For HSV, VZV, EBV this enzyme is a viral thymidine kinase, which is present in infected cells by a virus. Partial selectivity in phosphorylation stored and cytomegalovirus mediated through phosphotransferase gene product of UL 97. Activation of acyclovir specific viral enzyme to a great extent explains its selectivity.
Acyclovir phosphorylation process (conversion of a mono- triphosphate) is completed by cellular kinases. Acyclovir triphosphate nucleoside is incorporated into the viral DNA, which leads to rupture obligate chain termination of DNA synthesis and therefore to block viral replication.
In patients with preserved immune to HSV and VZV with reduced sensitivity to valacyclovir are extremely rare, but can sometimes be found in patients with severe immune disorders, eg, bone marrow transplant patients receiving chemotherapy for malignant tumors and in HIV-infected patients.
Resistance is usually due to a thymidine kinase deficiency, which leads to an excessive spread of the virus in the host organism. Sometimes reduction of sensitivity to acyclovir due to the appearance of virus strains with impaired viral thymidine kinase or DNA polymerase structure. The virulence of the virus species resembles that of his wild strain.
Pharmacokinetics:
After oral administration valaciclovir is well absorbed from the gastrointestinal tract. With the participation of the liver enzyme valatsiklovirgidralazy rapidly and almost completely converted to aciclovir and valine. After a single dose valaciclovir dose 250-2000 mg average maximum concentration of acyclovir in plasma in healthy volunteers with normal renal function is 10-37 mmol (2.2 – 8.3 ug / ml), and the median time to reach this concentration of 1-2 hours. When receiving a valaciclovir dose of 1000 mg of acyclovir bioavailability is 54% and is independent of food intake. Maximum concentration in plasma valacyclovir is only 4% of the concentration of acyclovir, the average time to maximum concentration – 30-100 minutes postdose, valaciclovir limit of quantification in plasma achieved through 3 hour, or before. Valaciclovir and acyclovir have similar pharmacokinetic parameters after oral administration.
Distribution: The degree of binding to plasma proteins valaciclovir is very low (only 15%).
Excretion: patients with normal renal function, the half-life of acyclovir in plasma after ingestion of valaciclovir is about 3 hours. Valaciclovir is excreted primarily in the urine as acyclovir (more than 80% of the dose) and metabolite 9-karboksimetoksimetilguanina acyclovir, is eliminated in unmodified form at least 1% of the formulation.
Special groups of patients: patients with end-stage renal failure average half-life of about 14 hours.
Characteristics of patients: the pharmacokinetics of valaciclovir and aciclovir are largely not impaired in patients infected with HSV and VZV. In late pregnancy steady daily indicator “area under curve” concentration-time »» (AUC) after receiving 1000 mg valaciclovir was greater than about 2 times, than that when taking acyclovir at a dose of 1200 mg per day.
Valaciclovir 1000 mg or 2000 mg does not violate the disposition and pharmacokinetic parameters of valaciclovir in HIV-infected patients compared to healthy individuals.
In organ transplant recipients receiving valaciclovir 2000 mg four times a day, peak acyclovir concentrations equal to or greater than that in healthy volunteers receiving the same dose of drug, and the daily area under the curve parameters have significantly higher.
Pregnancy and breast-feeding
Pregnancy.
Data on the use of valaciclovir in pregnancy is not enough. Valacyclovir should be used during pregnancy only if the potential benefit outweighs the potential risk.
The data records of the outcome of pregnancy in women taking valacyclovir, showed no increase in the number of birth defects in their children compared to the general population. Since the register included a small number of women taking valacyclovir during pregnancy, the reliable and specific on the safety of valaciclovir can not be done during pregnancy.
Lactation.
Acyclovir, the main metabolite of valaciclovir, is excreted in breast milk. After assigning the valaciclovir 500 mg of acyclovir into the maximum concentration (Cmax) in breast milk in 0.5 – 2.3 times (an average 1.4 times) higher than the corresponding concentration of acyclovir in maternal plasma. The ratio of AUC of acyclovir present in breast milk, to acyclovir AUC maternal plasma ranged from 1.4 to 2.6 (mean 2.2). The mean value of the concentration of acyclovir in breast milk was 2.24 micrograms / ml (9.95 micromol / L). When receiving the mother valaciclovir 500 mg 2 times a day child undergo a similar treatment of acyclovir as when taking it orally at a dose of about 0.61 mg / kg / day. The half-life of acyclovir from breast milk is the same as from the blood plasma. Valacyclovir in unchanged form was not detected in maternal plasma, breast milk, urine, or child.
Valaciclovir should be used with caution in nursing women. However / in a acyclovir at 30 mg / kg / day is used in neonates to treat diseases caused by herpes simplex virus.
Conditions of supply of pharmacies
On prescription.
side effects
Adverse reactions listed below in accordance with the classification of the main systems and organs and occurrence frequency.
Classification of the WHO frequency of side effects: very frequent -> 1/10 assignments (> 10%) frequently – by> 1/100 to 1%, and
special instructions
The degree of hydration
In patients at risk of dehydration, especially in elderly patients, it is necessary to provide adequate fluid replacement.
The use in renal failure
valaciclovir dose should be adjusted depending on the degree of renal dysfunction.
Patients with renal impairment are at increased risk of developing neurological complications. Typically, these reactions are reversible after discontinuation of the drug.
The use of higher doses of valaciclovir in hepatic failure and liver transplantation
No data on the use of valaciclovir at higher doses (4 g per day and more) in patients with liver disease, so high doses of valaciclovir they must be administered with caution. Special studies on the effect of valaciclovir at a liver transplant is not carried out. However, it has been shown that prophylactic intravenous administration at high doses of acyclovir reduces CMV infection.
Application of genital herpes
Suppressive valacyclovir therapy decreases the risk of transmission of genital herpes, but does not exclude it completely and does not lead to a complete cure. Valacyclovir therapy is recommended in combination with safer sex.
Effects on ability to drive vehicles and mechanisms:
It is necessary to take into account the clinical condition of the patient and the adverse reaction profile of valaciclovir in assessing a patient’s ability to drive a car or moving machinery.
Storage conditions
In a dry, dark place at a temperature not higher than 25 ° C.
Keep out of the reach of children.
Dosing and Administration
Valaciclovir Canon drug should be taken regardless of meals, pills should be taken with water.
Treatment of herpes zoster: adults Valaciclovir administered in a dose of 1 g three times a day for 7 days.
Treatment of infections caused by HSV: adults Valaciclovir administered in a dose of 500 mg 2 times a day. In the case of relapse, treatment should continue for 3 or 5 days. In more severe cases, the primary treatment should be started as early as possible, and its duration should be increased from 5 to 10 days. In recurrent HSV is considered the ideal appointment of valaciclovir in the prodromal period or immediately upon appearance of the first symptoms of the disease.
Alternatively, for the treatment of herpes labialis (lip fever) effectively assignment valaciclovir dose of 2 g twice a day. The second dose is to be taken after about 12 hours (but not earlier than 6 hours) after the first dose. By using such dosing regimen duration of treatment should not exceed 1 day as it was shown to provide no additional clinical benefit. Tearpiya should be started with the appearance of the earliest symptoms of fever lip (ie, tingling, itching, burning).
Prevention (suppression) of relapse of infections caused by HSV (adults) patients with immunocompetent valacyclovir administered in a dose of 500 mg once a day.
In patients with very frequent recurrences (10 and over a year) an additional effect can be achieved by assigning valacyclovir in a daily dose of 500 mg, divided into two doses (250 mg, 2 times a day).
For adult patients with immunodeficiencies recommended dose valaciclovir 500 mg 2 times a day. The treatment duration of 4-12 months.
Prevention of infection with genital herpes healthy partner.
Infected heterosexual adults with immunocompetent and the number of exacerbations of up to 9 per year, valacyclovir should take 500 mg 1 time a day for a year or more, each day at a regular sexual life, with occasional sexual intercourse receiving valacyclovir should be started 3 days before the alleged sexual contact.
Information about prevention in other populations of patients does not exist.
Prevention of CMV disease after transplant: dose for adults and adolescents (from 12 years)
It encouraged to nominate valacyclovir at a dose of 2 g 4 times a day, as soon as possible after transplantation. The dose should be reduced according to creatinine clearance.
The duration of treatment is 90 days, but in patients with high risk, treatment may be longer.
Special patient groups. In patients with impaired renal function Dosage adjustment of valaciclovir, depending of type of creatinine clearance *. * For details, see. In the instructions for use.
Patients with impaired liver function. In patients with mild and moderate hepatic cirrhosis (hepatic synthetic function maintained) adjusting the dose of the drug Valacyclovir Canon is not required. Pharmacokinetic data in patients with severe liver cirrhosis (with impaired liver synthetic function and the presence of shunts between the portal system and general vascular bed) also indicate the need to adjust the dose of valaciclovir, however, the experience of its clinical application is limited in this pathology.
Children under the age of 12 years. There are no data on the use of valaciclovir in children.
Elderly patients. Dose adjustment is required, except for a significant renal dysfunction. It is necessary to maintain an adequate fluid and electrolyte balance.
Information
Appearance may differ from that depicted in the picture. There are contraindications. You need to read the manual or consult with a specialist