Valtsikon tab n / 500mg film about 10 pc

$19.81

Valtsikon tab n / 500mg film about 10 pc

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Description

Composition
Active substance:
1 tablet contains: valaciclovir hydrochloride – 556.00 mg (calculated as 500.00 mg valaciclovir).
Film coating: [hypromellose – 10.50 mg, giproloza (hydroxypropyl) – 4.07 mg talc – 4.12 mg titanium dioxide – 2.31 mg] or [dry film coating mixture – white, containing hypromellose (50 %), hydroxypropyl cellulose (19.4%), talcum (19.6%), titanium dioxide (11%)] – 21.00 mg.
Excipients:
1 tablet contains: microcrystalline cellulose – 95.00 mg, giproloza (hydroxypropyl) – 14.00 mg Crospovidone – 28.00 mg magnesium stearate – 7.00 mg.
Description:
Round biconvex tablets, film-coated white or almost white. The cross-sectional core of a white or nearly white.
Product form:
Tablets, film-coated, 500 mg.
5, 10 or 14 tablets in blisters of PVC film and aluminum foil.
For 42, 50 or 60 tablets per polymer jar. 2 or 4 blisters of 5 tablets, 1, 2, 3, 4, 5 or 6 contour cell packs of 10 tablets or 3 blisters of 14 tablets, or a bank together with instructions for use placed in a pile of cardboard.
Contraindications
Hypersensitivity to valaciclovir, aciclovir and any other component, part of the drug; HIV infection in CD4 + lymphocytes content of less than 100 in 1 mm; children’s age (up to 12 years for the prevention of cytomegalovirus infection after transplantation, up to 18 years – for other indications).
Carefully
Hepatic / renal failure, advanced age, hypohydration, simultaneous nephrotoxic drugs, pregnancy, lactation, symptomatic forms of HIV infection in patients.
Dosage
500 mg
Indications
Adults: – treatment of shingles (Herpes zoster) (preparation promotes pain relief, reduces the 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 virus Herpes simplex 1,2 type, including first identified and recurrent genital herpes (Herpes genitalis), and labial herpes (Herpes labialis); – prevention (suppression) of recurrences infections of the skin and mucous membranes, caused by the virus Herpes simplex 1,2 type, including genital herpes; – prevention of transmission of genital herpes healthy partner when using the drug as suppressive therapy in combination with safe sex;
Adults and children aged 12 years and older: – the prevention of cytomegalovirus (CMV) infection and acute transplant rejection reactions (in patients with renal transplant patients), opportunistic infections and other herpes virus infections (HSV, VZV) after organ transplantation.
Interaction with other drugs
Cimetidine and tubular secretion blockers reduce the effect (reduced rate but not the completeness of the conversion to acyclovir). Correction of dosing regimen in patients with normal creatinine clearance is not required.
Nephrotoxic drugs increase the risk of renal dysfunction. Care must be taken (observe the change of renal function) when combined Valtsikon drug at higher doses (4 g per day and more) with drugs, co-torye influence other kidney (eg, cyclosporine, tacrolimus).
Acyclovir is excreted by the kidneys, in largely unaltered by the active renal secretion. The combined use of drugs with the same mechanism of elimination can lead to increased concentration of acyclovir in plasma.
After assigning Valtsikon drug in a dose of 1000 mg probenecid and cimetidine, are derived in the same manner as valaciclovir, aciclovir AUC value is increased and thus reduce its renal clearance. In view of the wide therapeutic index of acyclovir, the drug dosage adjustment Valtsikon in this case is not required.
Care must be taken in the case of simultaneous use of valaciclovir at higher doses (4 g per day and higher) and drugs that compete with acyclovir for elimination way since there is a potential threat increase in blood plasma levels of one or both drugs or their metabolites. It was noted an increase in magnitude AUC acyclovir and mycophenolate mofetil inactive metabolite while the use of these drugs.
The pharmacokinetics of valaciclovir does not change when concomitantly with digoxin, aluminum / magnesium-containing antacids, thiazide diuretics.
Overdose
Symptoms: an overdose of valacyclovir may cause acute renal failure and the development of neurological symptoms, including confusion, hallucinations, agitation, depression of consciousness and coma, nausea, and vomiting are also marked. To prevent overdose should follow caution when using the drug. Many cases of overdose were associated with the use of a drug for treating patients with impaired kidney function and elderly patients, due to non-compliance with the dosing regimen (repeatedly received valaciclovir dose exceeding the recommended).
Treatment. Patients subject to careful monitoring for timely diagnosis toxic manifestations. Hemodialysis greatly accelerates the removal of acyclovir from the blood plasma and can be considered an optimal treatment method in case of symptomatic overdose.
pharmachologic effect
Pharmacological group:
An antiviral agent.
Pharmacodynamics:
Valacyclovir – nucleoside inhibitor of DNA polymerase of herpes viruses. Blocks the synthesis of viral DNA and viral replication. The human body valaciclovir completely converted to acyclovir and L-valine. Acyclovir has a specific in vitro inhibitory activity against herpes simplex virus (HSV) type 1.2 (Herpes simplex 1,2 types) virus, and varicella zoster virus (VZV – varicella-zoster virus, Varicella zoster), cytomegalovirus (CMV) , Epstein-Barr virus (EBV) virus and human herpes type 6. Acyclovir inhibits viral DNA synthesis and the phosphorylation immediately after conversion to the active form atsiklovirtrifosfat. The first stage of phosphorylation takes place with the participation of virus enzymes. For viruses, HSV, VZV and EBV this enzyme is the 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 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.
Patients with immunocompetent HSV and VZV virus with reduced sensitivity to valacyclovir-ness are rare (less than 0.1%), but can sometimes be obna-o n patients with severely impaired immune system, such as bone marrow transplant patients receiving chemotherapy for malignant tumors and in HIV-infected patients.
Resistance is caused by deficiency virus thymidine kinase, that leads to excessive proliferation 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:
Suction
After oral administration valaciclovir is well absorbed from the gastrointestinal tract, is rapidly and almost completely converted to aciclovir and valine. This conversion is catalysed by the enzyme liver – valatsiklovirgidrolazoy.
After a single dose of 250-2000 mg valaciclovir mean maximum concentration (Cmax) of acyclovir in plasma in healthy volunteers with normal renal function is on average 10-37 micromol / l (2,2-8,3 g / ml), and the average time maxi-mal achieve a concentration of 1-2 hours. When receiving valaciclovir dose of 1000 mg of acyclovir bioavailability is 54% and is independent of food intake. Valaciclovir Cmax in plasma is only 4% of the concentration of acyclovir and reached an average of 30-100 minutes after taking the drug; after 3 h Cmax level remains the same or decreases. Valatsik-lovir and acyclovir have similar pharmacokinetic parameters after oral administration.
Distribution
Communication with valaciclovir proteins – 13-18%, acyclovir – 9-33%. Acyclovir is well distributed, wish to set up in the tissues and fluids of the body, including the brain, kidneys, lungs, liver, leading-aqueous humor, lacrimal fluid, intestine, muscle, spleen, uterus, mucous membranes, and the secret of the vagina, semen, amniotic fluid, cerebrospinal fluid (50% of the con-centration in the plasma), the liquid herpetic vesicles. Highest concentrations are in the kidneys, liver and intestines. It crosses the placenta and breast milk.
breeding
Valaciclovir excreted in the urine, mainly as acyclovir (more than 80% of the dose) and its metabolite 9-karboksimetoksimetilguanina, unchanged output of less than 1% of the formulation. The half-life (T 1/2) of valacyclovir is less than 30 minutes, acyclovir -. 2.5-3.3 hours in older patients (65-83 years) T 1/2 acyclovir is 3.3-3.7 hours, and in patients with end stage renal disease – about 14 hr.
The pharmacokinetics of valacyclovir and acyclovir largely impaired in Paci-ENTOV infected with HSV and VZV.
In HIV-infected patients, the pharmacokinetic parameters of acyclovir after oral administration of valaciclovir at a dose of 1000 mg and 2000 mg comparable to the parameters observed in healthy volunteers.
In organ transplant recipients receiving valaciclovir 2000 mg 4 times / day, Cmax acyclovir is equal to or exceeds that in healthy volunteers who received the same dose of drug, and the daily parameters area under the pharmacokinetic curve (AUC) were significantly higher.
In late pregnancy steady daily indicator farmakoki area under the curve after-kinetic-receiving 1000 mg valaciclovir was greater than about 2 times, than that when taking acyclovir at a dose of 1200 mg per day.
Pregnancy and breast-feeding
There are limited data on the use of valaciclovir in pregnancy. Valatsik-lovir apply only in cases where the potential benefit to the mother outweighs the potential risk to the fetus.
Recorded data on the outcome of pregnancy in women taking valacyclovir or acyclovir (the active metabolite of valaciclovir), showed no increase in the number vrozh-dennyh defects in their children, compared with the general population. Since the register included a small number of women taking valacyclovir during pregnancy, it is reliable and specific on the safety of the use of valaciclovir in pregnancy can not be done.
Acyclovir, the main metabolite of valaciclovir, is excreted in breast milk. After PRIE-ma valaciclovir oral dose of 500 mg, Cmax acyclovir 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 mean value of the concentration of acyclovir in breast milk was 2.24 micrograms / ml (9.95 micromol / L). When receiving valaciclovir mother oral dose of 500 mg of 2 times / day child undergo a similar treatment of acyclovir as when taking acyclovir orally at a dose of about 0.61 mg / kg / day.
Conditions of supply of pharmacies
Prescription.
side effects
Central nervous system: headache, dizziness, psychotic symptoms, agitation, mental decline, ataxia, coma, confusion or depression of consciousness, dysarthria, encephalopathy, mania, hallucinations, convulsions, tremor. These reactions are reversible and usually seen in patients with impaired renal function or in the background of other predisposing conditions. Patients with organ transplant receiving valacyclovir in high doses (8 g / day) for the prevention of cytomegalovirus infection often develop neurological reactions than when lower doses.
The respiratory system: dyspnea.
From the digestive system: nausea, abdominal discomfort, vomiting, diarrhea, reversible disturbances of liver function tests (alanine aminotransferase activity increase, aspartate aminotransferase, alkaline phosphatase), which are sometimes regarded as manifestations of hepatitis.
From hemopoiesis system: a leukopenia (mainly seen in patients with lowered immunity), thrombocytopenia, anemia, thrombotic thrombocytopenic purpura.
For the skin: erythema multiforme, rash, photosensitivity, alopecia.
Allergic reactions: pruritus, urticaria, angioneurotic edema, anaphylaxis.
From the urinary system: pain in the kidney projection, impaired renal function, including acute renal failure, renal colic. Renal colic can be associated with impaired renal function.
From the senses: blurred vision.
Laboratory indicators: reduction of hemoglobin, hypercreatininemia.
Other: dysmenorrhea, nasopharyngitis, respiratory tract infection, increased blood pressure, tachycardia, fatigue; in patients with severely impaired immune system, especially in adult patients with advanced stages of HIV infection receiving valacyclovir in high doses (8 g / day daily) for a long time, the cases of renal failure was observed, microangiopathic hemolytic anemia and thrombocytopenia (sometimes in combination ). These adverse reactions were observed in patients with the same disease but not receiving valacyclovir.
special instructions
In patients at risk of dehydration, especially in elderly patients, in the period leche-tion necessary to ensure adequate fluid replacement.
Because acyclovir is excreted by the kidneys, the dose of the drug Valtsikon be adjusted according to the degree of renal impairment. In patients with renal failure there is an increased risk of developing neurological complications, these patients must be thoroughly monitored. Typically, these reactions are reversible and disappear after discontinuation of the drug.
In patients with chronic renal failure (CRF) is often recommended to determine creatinine clearance, particularly at a time when kidney function is changing rapidly (for example, immediately after transplantation or engraftment), the valaciclovir dose adjusted according to the creatinine clearance.
No data on the use of valacyclovir in high doses (4 g or more per day) in patients with liver disease, however high dose Valtsikon they must be administered with caution.
Suppressive valacyclovir therapy decreases the risk of transmission of genital herpes, but does not exclude the risk of infection and does not lead to a complete cure. Valtsikon drug therapy is recommended in combination with safer sex.
The drug in high doses for long time under conditions involving severe immunodeficiency (bone marrow transplantation, symptomatic forms of HIV infection, kidney transplantation), led to the development thrombocytopenic purpura and hemolytic-uremic syndrome, until death.
At occurrence of side effects on the central nervous system (including agitation, hallucinations, confusion, delirium, seizures and encephalopathy) drug overturned.
Impact on the management of vehicles and mechanisms
No data on the effect of valacyclovir used in therapeutic doses, the ability to drive vehicles and mechanisms. However, in assessing the patient’s ability to drive a car or moving machinery should be aware that you may experience side effects on the central nervous system, so be careful.
Storage conditions
In the dark place at a temperature not higher than 25 ° C.
Keep out of the reach of children.
Dosing and Administration
Inside, regardless of the meal with water.
Treatment of shingles (Herpes zoster)
Adults:
The recommended dose is 1000 mg 3 times daily for 7 days.
Treating infections caused by HSV
Adults:
The recommended dose for the treatment of episodes of 500 mg 2 times a day for 5 days.
In more severe cases of the disease debut should be initiated as early as possible, and its duration can be increased from 5 to 10 days. In the case of relapse, treatment should continue for 3 or 5 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.
As an alternative for treating labial herpes effective 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 is 1 day. Therapy should be initiated with the appearance of the earliest symptoms of herpes labialis (eg tingling, itching, burning).
Prevention (suppression) of relapse of infections caused by HSV
Adults:
Patients with immunocompetent recommended dose is 500 mg once a day.
In immunocompromised patients the recommended dosage is 500 mg two times a day.
Prevention of transmission of genital herpes healthy partner
Инфицированным иммунокомпетентным лицам с рецидивами не более 9 раз в год рекомендуемая доза валацикловира составляет 500 мг 1 раз в день в течение года и более каждый день.
Данные о профилактике инфицирования в других популяциях больных отсутствуют.
Профилактика цитомегаловирусной (ЦМВ) инфекции после трансплантации
Взрослые и подростки в возрасте от 12 лет и старше:
Рекомендуемая доза составляет 2 г 4 раза в день, назначается как можно раньше после трансплантации.
Дозу следует снижать в зависимости от клиренса креатинина.
Продолжительность лечения составляет 90 дней, но у пациентов с высоким риском курс лечения может быть продлен.
Special patient groups
Patients with impaired renal function
Лечение опоясывающего лишая и инфекций, вызываемых ВПГ, профилактика (супрессия) рецидивов инфекции, вызванной ВПГ, профилактика передачи генитального герпеса здоровому партнеру
Дозу валацикловира рекомендуется уменьшать у пациентов со значительным снижением функции почек
Опоясывающий лишай (Herpes zoster): – при клиренсе креатинина 15-30 мл/мин по 1 г валацикловира 2 раза в день; – при клиренсе креатинина менее 15 мл/мин по 1 г валацикловира 1 раза в день.
Лечение инфекции, вызванной ВПГ (по схеме 500 мг 2 раза в сутки): – при клиренсе креатинина менее 15 мл/мин по 500 мг валацикловира 1 раза в сутки.
Лечение лабиального герпеса (по схеме 2 г 2 раза в день в течение одних суток): – при клиренсе креатинина 31-49 мл/мин по 1 г валацикловира 2 раза в день; – при клиренсе креатинина 15-30 мл/мин по 500 мг валацикловира 2 раза в день; – при клиренсе креатинина менее 15 мл/мин по 500 мг однократно.
Профилактика (супрессия) рецидивов инфекций, вызванных ВПГ: – пациенты с нормальным иммунитетом при клиренсе креатинина менее 15 мл/мин по 250 мг валацикловира 1 раза в день; – пациенты со сниженным иммунитетом при клиренсе креатинина менее 15 мл/мин по 500 мг валацикловира 1 раза в день; – снижение риска передачи генитального герпеса при клиренсе креатинина менее 15 мл/мин по 250 мг валацикловира 1 раза в день.
У таких пациентов необходимо поддерживать адекватную гидратацию.
Опыта применения валацикловира у детей со значениями клиренса креатинина менее 50 мл/мин/1,73 м2 нет.
Пациентам, находящимся на гемодиализе, рекомендуется применять валацикловир сразу после окончания сеанса гемодиализа в такой же дозе, как пациентам с клиренсом креатинина менее 15 мл/мин.
Профилактика цитомегаловирусной (ЦМВ) инфекции после трансплантации: – при клиренсе креатинина 75 и более мл/мин по 2 г валацикловира 4 раза в день; – при клиренсе креатинина от 50 до менее 75 мл/мин по 1,5 г валацикловира 4 раза в день; – при клиренсе креатинина от 25 до менее 50 мл/мин по 1,5 г валацикловира 3 раза в день; – при клиренсе креатинина от 10 до менее 25 мл/мин по 1,5 г валацикловира 2 раза в день; – при клиренсе креатинина менее 10 или диализ* по 1,5 г валацикловира 1 раза в день; * У пациентов, находящихся на гемодиализе, валацикловир следует назначать после окончания сеанса гемодиализа.
Необходимо часто определять клиренс креатинина, особенно в период, когда функция почек быстро меняется, например, сразу после трансплантации или приживления трансплантата, при этом доза валацикловира корректируется в соответствии с показателями клиренса креатинина.
Patients with impaired liver function
У взрослых пациентов с нарушение функции печени легкой и умеренной степени тяжести при сохранной синтетической функции коррекции дозы валацикловира не требуется. Фармакокинетические данные у взрослых пациентов с тяжелыми нарушениями функции печени (декомпенсированным циррозом), с нарушением синтетической функции печени и наличием порто-кавальных анастомозов также не свидетельствуют о необходимости корректировать дозу валацикловира, однако, клинический опыт при данной патологии ограничен.
Дети в возрасте до 12 лет
Нет данных о применении препарата Валцикон у детей.
Elderly patients
Коррекции дозы не требуется за исключением значительного нарушения функции почек. Необходимо поддерживать адекватный водно-электролитный баланс.
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

VERTEX

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