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.

Side-line actions. side effects

Side-line actions: Tablets with the immediate liberation the side effects, connected with the curtailment of treatment by 19% of patients (537/2897) with the depression, obtained Venlafaxine, with conducting of studies of phase 2 and phase 3 ended treatment in connection with the appearance of side effects. Most general effects (?1%), which were been the reason for the curtailment of therapy and those considering as the caused by method medicines (i.e. observed approximately 2 or more times more frequent with the method of Venlafaxine in the comparison with the placebo), they were following (in the brackets it was indicated percentage in the group of placebo): sleepiness 3% (1%), insomnia 3% (1%), vertigo 3% (1%), headache 3% (1%), anxiety 2% (1%), nervousness 2% (1%), asthenia 2% (1%); dryness in mouth 2% (1%), nausea 6% (1%), the disturbance of ejaculation 3% (1%), sweating 2% (1%). The side effects, which were being observed in the controlled tests by the most frequent side effects, connected with the method of venlafaksina of the hydrochloride (frequency of occurrence 5% and more), not equivalent in the frequency of occurrence in the group of placebo, i.e., with the method venlafaksina of hydrochloride were observed at least 2 times more frequently than in the group of the placebo (see Table 1), there were asthenia, sweating, nausea, bolt, anorexia, vomiting, sleepiness, dryness in the mouth, vertigo, nervousness, anxiety, tremor, carelessness of sight, disturbance of eyakulyatsii/orgazma and impotence in men. The side effects, which were being observed with a frequency of?1% in patients, treated of Venlafaxine by hydrochloride (tabl.y). Table 1 presents the side effects, noted in patients, who obtained Venlafaxine hydrochloride in the form of tablets at the doses of 75-375 mg/day with conducting of short term tests (4 and 8- weekly). These effects were observed with a frequency of?1% and exceeded in the frequency of placebo. Table shows the percentage of the patients in each group, in whom was noted at least one case of separate side effect within the period of treatment.

Description, contra-evidence, the application

Latin name: Venlafaxine The pharmacological groups: Acting Substance (MNN) Of venlafaksin * (Venlafaxine *)
According to the data Physicians Desk Reference (2004), venlafaksina hydrochloride in the form of tablets with the immediate liberation is shown for treating the depression. Venlafaxina hydrochloride in the form of capsules with the modified liberation is shown for treating of depression, generalizovannogo alarming disorder and social phobias. Contra-evidence: Hypersensitivity, the simultaneous method of the inhibitors OF MAO (see the "precautionary measures"). Limitations to the application: Recently transferred myocardial infarction and unstable , change AD, the increased intraocular pressure and glaucoma, maniacal states in anamnesis, the initially lowered mass of body, insufficiency, age of up to 18 years (safety and the effectiveness of application they are not established).