Valvira tab n / 500mg film about 10 pc

$15.86

Valvira tab n / 500mg film about 10 pc

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Description

Composition
Active substance:
valaciclovir hydrochloride hydrate 611.70 mg corresponding to 500 mg
Excipients:
microcrystalline cellulose 59,60mg, povidonK30 24.50 mg magnesium stearate 4.20 mg;
Film coating: Opadry White Y-5-7068 (3sR hypromellose 7.35 mg, giproloza 6.30 mg, 4.20 mg of titanium dioxide, macrogol / PEG 400 2.10 mg, 1.05 mg of Hypromellose 50sR) – 21 mg .
Description:
500 mg Tablets: oval biconvex tablets of white or almost white VC2 with a marking with one hand.
Product form:
500 mg Tablets: 10 tablets in blisters of PVC / Aluminum foil. 1 blister together with instructions for use in a cardboard package.
Contraindications
– Hypersensitivity to valaciclovir, aciclovir and any other component, part of the drug;
– Children up to age 12 years;
– Children up to age 18 years in the treatment of herpes zoster and ophthalmic zoster.
Dosage
500 mg
Indications
Adults and adolescents aged 12 to 18 years – Treatment of infections of the skin and mucous membranes caused by HSV, including first identified and recurrent genital herpes (Herpes genitalis), as well as labial herpes (Herpes labialis);
– prevention (suppression) of recurrences of skin infections and mucous membranes caused by HSV, including genital herpes, including adults with immunodeficiency;
– prevention of infections caused by cytomegalovirus (CMV), and diseases following transplantation of parenchymal organs.
Adults – treatment of shingles (Herpes zoster) and ophthalmic zoster.
Interaction with other drugs
Clinically significant interactions have not been established.
Acyclovir is excreted by the kidneys, substantially unaltered by the active renal secretion. The combined use of drugs with the same mechanism of elimination can lead to increased concentrations of acyclovir in the plasma.
After assigning valaciclovir 1000 mg and drugs cimetidine and probenecid, which are output in the same way, an increase in AUC of acyclovir and thus reduced renal clearance of acyclovir. However, because of the wide therapeutic index of acyclovir, valacyclovir dosage adjustment is not required.
When treating labial herpes prevention and treatment of diseases caused by CMV, care must be taken in the case of simultaneous use of valaciclovir at higher doses (4000 mg per day or higher) and drugs that compete with acyclovir for road clearance, since there is a potential threat increase in plasma concentrations of one or both drugs or their metabolites. AUC increase was noted acyclovir and inactive metabolite mycophenolate mofetil (immunosuppressant used in organ transplant patients) while the application of these drugs.
The simultaneous use of valaciclovir with nephrotoxic drugs, including aminoglycosides, organic platinum compounds, iodinated contrast agent, methotrexate, pentamidine, foscarnet, cyclosporin and tacrolimus,
should be carried out with caution, especially in patients with impaired renal function, and require regular monitoring of renal function.
Overdose
Currently, data are insufficient valacyclovir overdose.
Symptoms: Single administration of an overdose of acyclovir to 20 g, which partially is absorbed from the gastrointestinal tract, is not accompanied by toxic effects of the drug. When administered in a few days ultrahigh doses of acyclovir developed nausea, vomiting, headache, confusion; with a / in the introduction – an increased concentration of serum creatinine, renal failure, confusion, hallucinations, agitation, seizures, coma.
Treatment: Patients should be under close medical supervision 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 valacyclovir.
pharmachologic effect
Pharmacological group:
antiviral agent
Pharmacodynamics:
Mechanism of action
Valaciclovir is the antiviral agent is an L-valine ester of acyclovir. Acyclovir is a nucleoside analogue of a purine (guanine).
In humans, valacyclovir is rapidly and almost completely converted to aciclovir and valine, presumably under the influence of valatsiklovirgidrolazy enzyme.
Acyclovir is a specific inhibitor of herpes viruses with in vitro activity against herpes simplex virus (HSV) types 1 and 2, varicella-zoster virus (VZV) (Varicella zoster virus), cytomegalovirus (CMV), Epstein-Barr virus (EBV) and herpes virus human type 6. Acyclovir inhibits viral DNA synthesis and the phosphorylation immediately after conversion to the active form – atsiklovirtrifosfat.
The first stage of phosphorylation requires the activity of a virus-specific enzyme.
For HSV, VZV and EBV this enzyme is the viral thymidine kinase, which is only present in virus infected cells. Partially selectivity in phosphorylation supported indirectly through phosphotransferase cytomegalovirus UL97 gene product. This need for activation of acyclovir specific viral enzyme largely explains its selectivity. Acyclovir phosphorylation process (conversion of a mono- triphosphate) is completed by cellular kinases.
Atsiklovirtrifosfat competitively inhibits viral DNA polymerase, and being a nucleoside analogue, is incorporated into the viral DNA, which leads to rupture obligate chain termination of DNA synthesis and therefore to block viral replication.
Resistance to acyclovir is usually due to a thymidine kinase deficiency, which leads to an excessive spread of the virus in the host organism. In rare cases, reduced 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.
Based on the results of extensive studies of HSV and VZV strains taken from patients treated with acyclovir or its use in the prevention, found that viruses with reduced sensitivity to valacyclovir are extremely rare, but can be found in the rare cases in patients with severe immune disorders, e.g., bone marrow transplant recipients or organ of patients receiving chemotherapy for malignant tumors, and HIV-infected individuals.
Valacyclovir helps relieve pain: it reduces the duration and reduces the percentage of patients with pain caused by herpes zoster, including acute postherpetic neuralgia.
Pharmacokinetics:
Suction
After oral administration valaciclovir is well absorbed from the gastrointestinal tract and rapidly and almost completely transformed into aciclovir and valine. This transformation is probably carried valatsiklovirgidralazoy liver enzyme.
When receiving a valaciclovir dose of 1000 mg of acyclovir bioavailability is 54% and is not reduced by food intake. The pharmacokinetics of valaciclovir is not dose-dependent. The rate and extent of absorption decreases with increasing dose, resulting in a less than proportional increase in maximum plasma concentration (Smah) compared to the therapeutic dose range and reduced bioavailability at doses above 500 mg.
The results of evaluation of pharmacokinetics acyclovir when receiving single doses of valaciclovir 250 mg to 2000 mg in healthy volunteers with normal liver function
Pharmacokinetic 250 mg 500 mg 1000 mg 2000 mg acyclovir parameters (N = 15) (N = 15) (N = 15) (N = 15)
Cmax
mol / l 9,78 ± 1,71 15,0 ± 4,23 23,1 ± 8,53 36,9 ± 6,36
ug / ml 2,20 ± 0,38 3,37 ± 0,95 5,20 ± 1,92 8,30 ± 1,43
Tmax
hours (h) 0.75 (0,75-1,5) 1.0 (0,75-2,5) 2.0 (0,75-3,0) 2.0 (1,5-3, 0)
AUC
h x mol / l 24,4 ± 3,65 49,3 ± 7,77 83,9 ± 20,1 131 ± 28,3
x h / ml 5,50 ± 0,82 11,1 ± 1,75 18,9 ± 4,51 29,5 ± 6,36
Cmax – Maximum plasma concentration; Tmax – time to maximum plasma concentration; AUC – area under the curve “concentration-time”.
Cmax and AUC values ​​represent mean standard deviation.
The values ​​for T max represent the median and range of values.
The maximum concentration of valacyclovir in plasma represents only 4% of the concentration of acyclovir, the median time to achieve it is from 30 to 100 min after dosing. After 3 hours of ingestion of valaciclovir concentration reaches a level quantifying or lower.
Valaciclovir and acyclovir have similar pharmacokinetic parameters after single and multiple doses. VZV and HSV does not significantly alter the pharmacokinetics of valaciclovir after acyclovir and valaciclovir receiving inside.
Distribution
Degree of valaciclovir binding to plasma proteins is very low (15%). The degree of penetration into the cerebrospinal fluid (CSF) is defined as the ratio of AUC in CSF to AUC in plasma and is about 25% for acyclovir and metabolite gidroksiatsiklovira 8 (8-OH-ACV); about 2.5% to metabolite 9- (carboxymethoxy) methyl-guanine (CMMG).
Metabolism
After oral valacyclovir is converted into acyclovir and L-valine by first-pass metabolism in the intestine and / or liver metabolism. Acyclovir is converted into small metabolites: CMMG under the influence of ethyl alcohol and aldehyde dehydrogenase; 8-OH-ACV under the influence of aldehyde. Approximately 88% of the total cumulative effect on blood plasma falls on acyclovir, 11% – CMMG
and 1% – 8-OH-ACV. Valaciclovir and acyclovir is not metabolised by cytochrome P450 isozymes system.
breeding
In patients with normal renal function, half-life of acyclovir from blood plasma after single or multiple dose valaciclovir is about 3 hours.
Less than 1% of the received valaciclovir dose excreted by the kidneys in unchanged form.
Valaciclovir is excreted mainly by the kidneys in the form of acyclovir (80% of the dose) and metabolite acyclovir – CMMG.
Special patient groups
Patients with impaired renal function. Excretion acyclovir correlated with kidney function, exposure of acyclovir increases with increasing severity of renal insufficiency. Patients with end-stage renal failure average T1 / 2 of acyclovir after administration of valacyclovir is approximately 14 hours compared with approximately 3 hours at normal renal function.
Exposure of acyclovir and its metabolites CMMG and 8-OH-ACV in blood plasma and CSF were evaluated at steady state after multiple administration of valacyclovir in 6 patients with normal renal function (mean creatinine clearance 111 ml / min, the range of 91-144 ml / min) receiving 2000 mg every 6 hours, and 3 patients with severe renal failure (26 ml / min, the range of the average creatinine clearance
17-31 ml / min) receiving 1500 mg every 12 hours. In severe renal failure compared to normal kidney function in blood plasma, as well as in CSF concentration of acyclovir, CMMG and 8-OH-ACV were 2 , 4 and 6.5 times higher respectively. There was no difference in the degree of penetration of acyclovir into the CSF
(Defined as the ratio of AUC in CSF to plasma AUC), CMMG or 8-GHACV between two populations with severe renal impairment and normal renal function.
Patients with impaired liver function
Pharmacokinetic data indicate that in patients with liver failure decreases the rate of conversion of valacyclovir to acyclovir, but not the extent of conversion. The half-life of acyclovir does not depend on the liver function.
Pregnancy
In the study, pharmacokinetics of valaciclovir and acyclovir in late pregnancy is established daily AUC values ​​increase in a stable condition with daily intake valaciclovir 1000 mg per day, which is about 2 times higher than the AUC when administered acyclovir at a dose of 1200 mg per day.
HIV infection
Patients with HIV infection distribution and pharmacokinetic characteristics of acyclovir after oral administration of single or multiple doses of 1000 mg or 2000 mg valaciclovir remain unchanged compared to healthy volunteers.
organ transplantation
The maximum concentration of acyclovir in patients after organ transplantation treated with 2000 mg valaciclovir 4 times / day was comparable or higher than the maximum concentration observed in healthy volunteers who received the same dose.
Installed AUC daily values ​​may be characterized as significantly higher.
Pregnancy and breast-feeding
fertility
In animal studies, valacyclovir had no effect on fertility. However, use of high doses of acyclovir when administered parenterally caused testicular effects in rats and dogs.
Studies of the effect of valaciclovir on fertility have not been conducted in humans. However, no changes were registered in an amount motility and morphology of spermatozoa in 20 patients after 6 months of daily application of valaciclovir at doses of 400 mg to 1000 mg.
Pregnancy
There are limited data on the use Valvira the drug during pregnancy.
The drug should be used during pregnancy only if the potential benefit to the mother outweighs the potential risk to the fetus.
Registers pregnant were documented pregnancy outcomes in women taking the drug valaciclovir or other preparations containing acyclovir (acyclovir is an active metabolite of valaciclovir), 111 and 1246 observations, respectively (of which 29 and 756 took drugs I trimester) were outcomes pregnancy, registered prospectively. Analysis of the data in the register pregnant women exposed to acyclovir, showed no increase in the number of birth defects in children as compared with the general population, none of malformations revealed no specificity or patterns, indicating a common cause. Since pregnancy registries small number of women were included who received valacyclovir during pregnancy, the reliable and specific on the safety of the use of valaciclovir in pregnancy can not be done.
Breastfeeding
Acyclovir, the main metabolite of valaciclovir, enters the breast milk. Upon receiving the valaciclovir 500 mg Cmax inwardly in breast milk in 0,5-2,3 times (an average 1.4 times) higher than the corresponding concentration of acyclovir in plasma, maternal blood. The ratio of AUC values ​​of acyclovir in breast milk to AUC in maternal serum 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 valaciclovir mother at a dose of 500 mg of 2 times / day children who are breast-fed, subjected to the same effects 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 the plasma of the mother’s blood, breast milk and urine of a child. valaciclovir medications should be used with caution in women during breastfeeding. However, acyclovir for on / in the treatment of HSV used for infants at a dose of 30 mg / kg / day.
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, which is defined as follows: very often (> 1/10), often (> 1/100
special instructions
Hydration
In patients at risk of dehydration, especially in elderly patients, it is necessary to provide adequate water and electrolyte balance.
Use in patients with impaired renal function and in elderly patients
Because acyclovir is excreted by the kidneys, the dose should be reduced Valvira in patients with impaired renal function. Elderly patients may experience impaired renal function, so you should consider reducing the dose for this patient group. As elderly patients and patients with impaired renal function are at increased risk of developing neurological complications in these patients is necessary to provide a thorough medical control. As a rule, these reactions generally are reversible in case withdrawal of the drug.
herpes labialis treatment and prophylaxis of CMV infections and diseases
The use of high doses Valvira with abnormal liver function after a liver transplant. No data on the use Valvira drug in high doses (4000 mg per day and above) in patients with liver disease, so these patients Valvira high dose should be administered with caution. Special studies on the effect of the drug in Valvira liver transplants have been conducted. However, it was found that the prophylactic high dose acyclovir reduces the manifestations of CMV infection and disease.
Use in genital herpes
Patients should be advised to abstain from sex when symptoms are present even if antiviral treatment Valvira already begun.
Suppressive therapy with Valvira reduces the risk of transmission of genital herpes, but does not completely eliminate the risk of infection and does not lead to a complete cure.
Valvira drug therapy is recommended in conjunction with a reliable means of barrier contraception.
Use in Pediatrics
Clinical experience with the drug in children is missing.
Effects on ability to drive a vehicle, the mechanism
Care must be taken in the case of side reactions affecting the speed of psychomotor reactions.
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
At temperatures above 25 ° C.
Keep out of the reach of children!
Dosing and Administration
Valvira drug can be taken without regard to food intake, tablets should be taken with water.
Treatment of infections of the skin and mucous membranes caused by HSV, including first identified and recurrent genital herpes (Herpes genitalis), as well as labial herpes (Herpes labialis)
Immunocompetent adults and adolescents aged 12 to 18 years
The recommended dose is 500 mg 2 times a day.
В случае рецидивов лечение должно продолжаться 3 или 5 дней. В случае первичного герпеса, который может протекать в более тяжелой форме, лечение следует начинать как можно раньше, а его продолжительность должна быть увеличена с 5 до 10 дней. При рецидивах ВПГ наиболее верным считается, назначение препарата Валвир в продромальном периоде или сразу же после появления первых симптомов заболевания.
Применение валацикловира может предотвратить развитие поражения, если его применять при первых признаках и симптомах рецидива, вызванного ВПГ.
В качестве альтернативного лечения лабиального герпеса эффективно назначение препарата Валвир в дозе 2000 мг 2 раза в сутки в течение 1 суток. Вторая доза должна быть принята приблизительно через 12 часов (но не раньше, чем через 6 часов) после приема первой дозы. При использовании такого режима дозирования продолжительность лечения не должна превышать 1 сутки, т.к. превышение продолжительности этого курса лечения не приводит к дополнительной клинической пользе.
Терапия должна быть начата при появлении самых ранних симптомов лабиального герпеса (т.е. пощипывание, зуд, жжение).
Профилактика (супрессия) рецидивов инфекций кожи и слизистых оболочек, вызванных ВПГ, включая генитальный герпес, в том числе. у взрослых с иммунодефицитом
Иммунокомпетентные взрослые и подростки в возрасте от 12 до 18 лет
У иммунокомпетентных пациентов рекомендуемая доза составляет 500 мг 1 раз в сутки.
Через 6-12 месяцев лечения необходимо оценить эффективность терапии.
Взрослые с иммунодефицитом
У взрослых пациентов с иммунодефицитом рекомендуемая доза составляет 500 мг 2 раза в сутки. Через 6-12 месяцев лечения необходимо оценить эффективность терапии.
Профилактика инфекций, вызванных ЦМВ, и заболеваний после трансплантации паренхиматозных органов
Взрослые и подростки в возрасте от 12 до 18 лет
Рекомендуемая доза составляет 2000 мг 4 раза в сутки, назначается как можно раньше, после трансплантации. Дозу следует снижать в зависимости от клиренса креатинина.
Продолжительность лечения обычно составляет 90 дней, но у пациентов с высоким риском курс лечения может быть продлен.
Лечение опоясывающего герпеса (Herpes zoster) и офтальмичеcкого опоясывающего герпеса
Adults
Рекомендуемая доза составляет 1000 мг 3 раза в сутки в течение 7 дней.
Special patient groups
Children
Эффективность лечения препаратом Валвир у детей не исследовали.
Elderly patients
Необходимо учитывать возможное нарушение функции почек у пациентов пожилого возраста, доза препарата Валвир должна быть соответствующим образом скорректирована. Необходимо поддерживать адекватный водно-электролитный баланс.
Patients with impaired renal function
Дозу препарата Валвир рекомендуется уменьшать у пациентов с выраженным нарушением функции почек. У таких пациентов необходимо поддерживать адекватный водно-электролитный баланс.
Коррекция дозы препарата Валвир для применения у взрослых и подростков в возрасте от 12 до 18 лет с нарушением функции почек
1. Коррекция дозы препарата Валвир для применения у взрослых и подростков в возрасте от 12 до 18 лет с нарушением функции почек:
– Клиренс креатинина не менее 50 мл/мин + Валвир
1000 мг 3 раза в сутки – Клиренс креатинина от 30 до 49 мл/мин + Валвир
1000 мг 2 раза в сутки – Клиренс креатинина от 10 до 29 мл/мин + Валвир 1000 мг 1 раз в сутки – Клиренс креатинина менее 10 мл/мин + Валвир 500 мг 1 раз в сутки
2. ВПГ (лечение)
Иммунокомпетентные взрослые и подростки в возрасте от 12 до 18 лет:
– Клиренс креатинина не менее 30мл/мин + Валвир 500 мг 2 раза в сутки – Клиренс креатинина менее 30 мл/мин + Валвир 500 мг 1 раз в сутки
Лабиальный герпес у иммунонекомпетентных взрослых и подростков в возрасте от 12 до 18 лет (лечение)
– Клиренс креатинина не менее 50мл/мин + Валвир 2000 мг 2 раза в сутки – Клиренс креатинина от 30 до 49 мл/мин + Валвир 1000 мг 2 раза в сутки – Клиренс креатинина от 10 до 29 мл/мин + Валвир 500 мг 2 раза в сутки – Клиренс креатинина менее 10 мл/мин + Валвир 500 мг 1 раз в сутки
3. ВПГ (профилактика (супрессия))
Иммунокомпетентные взрослые и подростки в возрасте от 12 до 18 лет – Клиренс креатинина не менее 30 мл/мин + Валвир 500 мг 1 раз в сутки – Клиренс креатинина менее 30 мл/мин + Валвир 500 мг 1 раз в двое суток
Взрослые с иммунодефицитом – Клиренс креатинина не менее 30 мл/мин + Валвир 500 мг 2 раза в сутки – Клиренс креатинина менее 30 мл/мин + Валвир 500 мг 1 раз в сутки
Профилактика инфекций, вызванных ЦМВ, у взрослых и подростков в возрасте от 12 до 18 лет – Клиренс креатинина не менее 75 мл/мин + Валвир 2000 мг 4 раза в сутки – Клиренс креатинина от 50 до 75 мл/мин + Валвир 1500 мг 4 раза в сутки – Клиренс креатинина от 25 до 50 мл/мин + Валвир 1500 мг 3 раза в сутки – Клиренс креатинина от 10 до 25 мл/мин + Валвир 1500 мг 2 раза в сутки – Клиренс креатинин менее 10 мл/мин или у пациентов на гемодиализе + Валвир 1500 мг 1 раз в сутки
Дополнительная информация для показания: лечение инфекций кожи и слизистых оболочек, вызванных ВПГ, включая впервые выявленный и рецидивирующий генитальный герпес (Herpes genitalis), а также лабиальный герпес (Herpes labialis)
Опыт применения препарата Валвир у детей со значениями клиренса креатинина менее 50 мл/мин/1,73 м2 отсутствует.
Дополнительная информация для показания: профилактика инфекций, вызванных ЦМВ, и заболеваний после трансплантации паренхиматозных органов
Необходимо часто определять КК, особенно в период, когда функция почек быстро меняется, например, сразу после трансплантации или приживления трансплантата, при этом доза препарата Валвир корректируется в соответствии с показателями клиренса креатинина.
Дополнительная информация для показания: лечение опоясывающего герпеса (Herpes zoster) и офтальмического опоясывающего герпеса
Препарат Валвир следует применять после гемодиализа у пациентов, которым проводят периодический гемодиализ.
Patients with impaired liver function
На основании исследования с применением однократной дозы валацикловира 1000 мг у взрослых пациентов с циррозом печени легкой или средней степени тяжести (при сохраненной синтетической функции печени) коррекции дозы препарата Валвир не требуется.
Фармакокинетические данные у взрослых пациентов с тяжелой степенью нарушения функции печени (декомпенсированным циррозом), с нарушением синтетической функции печени и наличием портокавальных анастомозовтакже не свидетельствуют о необходимости коррекции дозы препарата Валвир, однако клинический опыт при данных патологиях ограничен.
Информация о дозах более 4000 мг в сутки для пациентов с инфекциями, вызванными ВПГ и ЦМВ, указана в разделе “Особые указания”.
Information
Appearance may differ from that depicted in the picture. There are contraindications. You need to read the manual or consult with a specialist

Additional information

Weight0.100 kg
Manufacturer

TEVA

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