Sibutramine Tablets

Mechanism Of Action Inhibits reuptake of norepinephrine, serotonin, and dopamine. May stimulate satiety center in brain, causing appetite suppression. Inhibits reuptake of Serotonin(5.H.T) nor adrenaline and to a lesser extent, dopamine in Vivo and in vitro M1 and M2 Metabolite are pharmacologically active and are up to about 100-fold more potent reuptake inhibitors than sibutramine has no effects on dopamine receptors, some thermogenic activity is evident at doses of 10mg apparent low abuse potential in humans. Sibutramine produce its therapeutic effect by Norepinephrine, Serotonin and dopamine reuptake inhibition. Pharmaco Kinetics Reduce reaches maximum therapeutic concentration in 1.2hrs. Food delays the absorption by 3hrs. Approximately 77% of the single oral dose is absorbed. Steady state reached with in 4days. Sibutramine is extensively bound and is rapidly and extensively distributed into tissue. It undergoes extensive first pas metabolism and is primarily by cytochromep4503A4 isoenzyme. Approximately 85% of the drug eliminated through urine. Indications Management of obesity, including weight loss and maintenance of weight loss and should be used in conjugation with a reduced calorie diet. Dosage Its recommended for obese patients with an initial BMI 30kg/m2 or 27kg/m2 in the presence of the risk factors(e.g. hypertension,diabetes,dyslipidemia).Initially 10mg of sibutramine is given once daily with or without food. If there is inadequate weight loss, the dose may be titrated after four weeks to a total of 20mg once daily.