Management of Obesity
Nobese of Getz Pharma is the first orally administered serotonin (5-hydroxytryptamine, 5-HT) and noradrenaline reuptake inhibitor (SNRI) used for the management of obesity. Nobese is chemically Sibutramine Hydrochloride.
How Nobese Works
Nobese has been shown to reduce body weight by dual actions: reduction in food intake through enhancement of satiety and increase of energy expenditure by induction thermogenesis. Nobese produces its therapeutic effects primarily by serotonin and noradrenaline reuptake inhibition.
Nobese is rapidly absorbed from the Gartro Intestinal Tract following oral administration. Peak plasma concentration of the parent drugu appears after 1.2 hours and of its pharmacologically active metabolites M1 and M2, three to four hours, on average, atleast 77% of a single oral dose of Nobese is absorbed.
Nobese and its metabolites M1 and M2 are extensively bound (97% and 94%) respectively. To human plasma protein. It is extensively distributed to the renal and hepatic tissues.
Nobese undergoes extensive first-pass metabolism. Nobese is principally metabolized by the cytochrome P450 isoenzyme CYP3A4 to two demethyled active metabolites which are secondary and primary amine metabolites. These active metabolites are further metabolized by hydroxylation and conjugation to inactive M5 and M6 metabolites.
The primary route of excretion for the active metabolites is hepatic metabolism and for inactive metabolites is renal excretion. Plasma illumination half life is 14-16 hours.
In patients with moderate hepatic impairment receiving a single 15 mg oral dose of Nobese, the combined AUCs of M1 and M2 increased by 24% which does not warrant dose adjustment.
Illumination of inactive hydroxyl metabolites, which are renally excreted, may be affected in this population.