oral testosterone

Absorption – high. The maximum concentration  in plasma is achieved after 1-2 h, oral testosterone in women above 20%, the area under the curve ;  in patients with alcoholic liver cirrhosis 16 times, times higher than normal. Food somewhat reduces the rate and duration of absorption of the drug (25% and 9% respectively)  cholesterol reduction similar to that in the application of atorvastatin without food. The concentration of atorvastatin in the evening application in lower than in the morning (approximately 30%). A linear relationship between dose and degree of absorption of the drug.
Bioavailability – 12% systemic bioavailability of inhibitory activity against  reductase – 30%. The low systemic bioavailability due to first-pass metabolism in the mucosa of the gastrointestinal tract, and the “first pass” through the liver.
The average volume of distribution – 381 liters, the connection with plasma proteins – 98%. It is metabolized primarily in the liver under the influence of isozymes  with the formation of pharmacologically active metabolites (ortho and paragidroksilirovannyh derivatives, beta-oxidation products). With In vitro, ortho and paragidroksilirovainye metabolites have an inhibitory effect on HMG-CoA reductase, comparable to that of . atorvastatin
The inhibitory effect of the drug with respectreductase inhibitors by about 70% determined by the activity of circulating metabolites.
displayed through the intestine with the bile after hepatic and / or extrahepatic metabolism (not exposed to pronounced enterohepatic recirculation).
The half-life – 14 hours inhibitory. activity  reductase remains about 20-30 hours due to the presence of active metabolites. Less than 2% of an oral dose is determined in urine. Not output during hemodialysis.

INDICATIONS

  • In combination with oral testosterone a diet to reduce elevated total cholesterol,  cholesterol, apolipoprotein B, and triglycerides, and increasing concentrations of HDL cholesterol in patients with primary hypercholesterolemia, heterozygous familial and non-familial hypercholesterolaemia and combined (mixed) hyperlipidemia (type IIa and IIb according to Frederickson);
  • In combination with a diet for the treatment of patients with elevated serum triglyceride concentrations (familial endogenous hypertriglyceridemia type IV according to Frederickson) and patients with disbetalipoproteinemiey (type III according to Frederickson), whose diet therapy does not provide adequate effect;
  • To reduce the concentration of total cholesterol  cholesterol in patients with homozygous familial hypercholesterolemia, when diet therapy and other non-pharmacological treatments are not sufficiently effective (as an addition to lipid-lowering therapy, including autologous transfusion purified from the blood LDL)
  • Diseases of the cardiovascular system (in patients with elevated occurrence of coronary heart disease risk factors – older age over 55, smoking, hypertension, diabetes mellitus, peripheral vascular disease, of stroke, left ventricular hypertrophy, a protein / albuminuria, coronary heart disease in the immediate family ), including: against the background of dyslipidemia – secondary prevention to reduce the overall risk of death, myocardial infarction, stroke, rehospitalization for angina and the need for revascularization procedures.

CONTRAINDICATIONS

  • Hypersensitivity to the drug;
  • Active liver disease or increased serum activity of “liver” transaminases (more than 3 times the upper limit of normal) of unknown origin, hepatic failure (severity A and B on the scale of Child-Pugh);
  • Hereditary diseases, such as lactose intolerance, lactase deficiency or glucose-galactose malabsorption (due to the presence of lactose);
  • Pregnancy, lactation;
  • Women of childbearing age not using adequate methods of contraception;
  • Age 18 years (effectiveness and safety have been established).

Precautions:
alcohol abuse, history of liver disease, the oral testosterone expressed disturbances of water and electrolyte balance, endocrine and metabolic disorders, arterial hypotension, severe acute infection (sepsis), uncontrolled epilepsy, extensive surgery, trauma, skeletal muscle disease.