Zelixa - Zelixa was withdrawn from the U.S. market in October 2010.
Zelixa affects chemicals in the brain that affect weight maintenance.
Zelixa is used together with diet and exercise to treat obesity that may be related to diabetes, high cholesterol, or high blood pressure.
Zelixa may also be used for other purposes not listed in this medication guide.
Zelixa is an drug for the treatment of central action obesity. The mechanism of action is due to selective inhibition of serotonin reuptake of norepinephrine and, to a lesser extent, of dopamine. This medication accelerates the onset and prolong satiety, which leads to a decrease in food consumption. It increases energy expenditure by stimulating thermogenesis mediated by activation of beta3-adrenergic receptors. Acts on both sides of the balance of energy and helps reduce body weight.
Zelixa and its metabolites did not release monoamines, and they are not MAO inhibitors, have no affinity for serotonergic, adrenergic, dopaminergic, muscarinic, histamine, benzodiazepine and NMDA receptors.
Zelixa is an orally administered agent for the treatment of obesity. Zelixa exerts its pharmacological actions predominantly via its secondary (M1) and primary (M2) amine metabolites. The parent compound, sibutramine, is a potent inhibitor of serotonin and norepinephrine reuptake in vivo, but not in vitro. However, metabolites M1 and M2 inhibit the reuptake of these neurotransmitters both in vitro and in vivo. In human brain tissue, M1 and M2 also inhibit dopamine reuptake in vitro, but with ~3-fold lower potency than for the reuptake inhibition of serotonin or norepinephrine. Sibutramine, M1 and M2 exhibit no evidence of anticholinergic or antihistaminergic actions. In addition, receptor binding profiles show that sibutramine, M1 and M2 have low affinity for serotonin (5-HT1, 5-HT1A, 5-HT1B, 5-HT2A, 5-HT2C), norepinephrine (b, b1, b3, a1 and a2), dopamine (D1 and D2), benzodiazepine, and glutamate (NMDA) receptors. These compounds also lack monoamine oxidase inhibitory activity in vitro and in vivo.
Adult: Initially, 10 mg daily in the morning. Re-evaluate treatment in patients whose weight loss is <2 kg in the 1 st 4 wk of treatment. May increase dose to 15 mg daily. Reassess 4 wk later. Discontinue treatment if weight loss is still <2 kg. Max: 15 mg daily.