Bitsiklol of the tab. of 25 mg No. 18

Pharmacological properties

Pharmacodynamics. on chemical structure bitsiklol it is similar to a bifendat. by pharmakodinamichesky researches it is proved that bitsiklol the increased level of transaminases in hepatitis is capable to reduce, damage of a liver chloroform, d-galaktozaminom and acetaminophen and to restore the broken structures of hepatic fabric of various degrees of severity. as a result of pilot studies of in vitro on colony of cells 2.2.1.5 it is established that bitsiklol it is capable to oppress secretion of surface antigen of a virus of hepatitis b (hbsag), e-antigen of a virus of hepatitis b (hbeag), DNA of a virus of hepatitis b and RNA of a virus of hepatitis with. bitsiklol oppresses products of tumor necrosis factor (fno) active neutrophils, cells of a kupfer and macrophages and also brings out of cells free radicals. thus, bitsiklol the oxidizing tension caused by dysfunction of mitochondrions of hepatocytes that necrosis and apoptosis in hepatocytes warns oppresses. bitsiklol apoptosis of hepatocytes, stimulated fno and cytotoxic t cells also detains. it, in turn, leads to restoration of damages of a kernel and DNA of hepatocytes.

Pharmacokinetics. T _½ in the first phase of two-phase model (t _½ka ) makes 0.84 h, T _½ in the second phase of two-phase model (t _½ke ) makes 6.26 h, time of achievement of the C _max (t _peak ) — 1.8 h, the C _max in blood plasma — 50 ng/ml. The C _max and AUC are in direct dependence on accepted medicament doses, but other pharmacokinetic parameters, such as t _½ka , t _½ke , Vd/F (attitude of volume of distribution (Vd) of medicine towards bioavailability (F)), CL/F (attitude of system clearance (CL) towards bioavailability (F)) and t _peak , change insignificantly (depending on a dose) and correspond to features of linear pharmacokinetics.

C _max can increase at use of medicament after a meal.

Metabolism of a bitsiklol happens in a liver with the participation of P450 cytochrome to formation of the main metabolites 4’OH-Bicyclol and 4OH-Bicyclol.

Drug is revealed in blood of the person in not changed look in 15 min. after intake. The C _max note a bitsiklol in a liver in 4 h after administration of drug. Extent of linking with proteins of blood plasma reaches 78%. Less than 30% of a bitsiklol are brought out of an organism through a GIT with a stake during 24 h. About 1.3% are removed with urine and 0.03% — with bile.

Indication

Hepatitis which is followed by increase in activity of transaminases of a liver:

• chronic viral hepatitis of B;
• chronic viral hepatitis of C;
not alcoholic steatogepatit
• ;
• alcoholic hepatitis;
• toxic (including medicinal) hepatitis.

Use

to Adults and children is aged more senior than 12 years medicament appoint inside in a dose of 25 mg (1 tablet) 3 times a day; in case of need — 50 mg (2 tablets) 3 times a day.

Drug Bitsiklol is taken in 2 h after a meal.

Minimum period of treatment — 6 months or on doctor's orders.

to Elderly people (70 years are more senior) a dose of medicament is defined individually.

Children. Not to apply at children aged up to 12 years.

Contraindication

Hypersensitivity to medicament components. acute hepatitis. period of pregnancy and feeding by a breast. children's age up to 12 years.

Bitsiklol is usually well had by

. side reactions (in case of emergence) have temporality, easy or moderate degree of manifestation and pass independently after medicament withdrawal or by means of symptomatic therapy. with a frequency less than 0.5% there can be dizziness, rash on skin, an abdominal distension and vomiting. at a small number of patients (0.1%) the headache, a sleep disorder, discomfort in epigastric area, increase in level of activity of transaminases, reduction of quantity of thrombocytes and increase in level of glucose and creatinine in blood are possible.

Special instructions

during medicament treatment bitsiklol should control constantly a condition of the patient and function of a liver.

With care to use medicament to patients with a hypoalbuminemia, cirrhosis, a gullet varicosity, in hepatic encephalopathy, with a severe form of hepatitis, a renal failure, essential the increased bilirubin level, ascites, a gepatorenalny syndrome. It is necessary to appoint with extra care medicament in autoimmune hepatitis.

Use during pregnancy or feeding by a breast. Not to apply.

Ability to influence speed of response at control of vehicles or work with other mechanisms. Very seldom during treatment the dizziness therefore it is necessary to be careful at control of vehicles or work with other mechanisms is observed.

Interaction

At simultaneous use of a bitsiklol with nukleozidny drugs, such as lamivudin, decrease in efficiency of medicament is possible.

According to the conducted clinical trials at use of a bitsiklol in a dose of 150 mg 3 times a day were not observed by

any case of overdose. besides, exceeding a usual dose for the person by 400 times did not cause toxic reaction.

Storage conditions

In original packing at a temperature not above 25 °C.