Saturday, September 09, 2006

Pharmacokinetics:

Suction and distribution after the single method Of efektina of depot Cmax of venlafaxine and its active metabolite are achieved during 5.5 and 9 h respectively. The method of preparation with the food does not have an effect on absorption and biotransformation of venlafaxine. Binding with the proteins of the plasma of venlafaxine and its metabolite composes 27% and 30% respectively. Metabolism and removal Of venlafaxine under action P450 CYP2D6 to a considerable degree biotransform in the liver with the formation of active metabolite O -desmetilvenlafaxine . Venlafaxine and its metabolites are derived predominantly by kidneys. Approximately 87% of dose for 48 h are derived with the urine, 5% - in the unchanged form, 29% - in the form unconjugated O -desmetilvenlafaxine , 26% - in the form conjugated O -desmetilvenlafaxine and 27% - in the form of other metabolites. Pharmacokinetics in the special clinical cases age and sex of patients do not have an effect on the pharmacokinetic parameters of preparation. In patients with the disturbances of the function of the liver (c by cirrhosis in the stage of compensation) was noted reduction in the metabolism of venlafaxine and removal of its active metabolite, which led to an increase in their concentration in the plasma of the blood. In patients with the moderately expressed or heavy disturbances of the function of kidneys was noted reduction in the clearance and increase T1/2 in venlafaxine and O -desmetilvenlafaxine. Reduction in the general clearance was more expressed in patients with the clearance of endogenous creatinine below 30 ml/min.