Sibutramine

Sibutramine Brand names, Sibutramine Analogs

Sibutramine Brand Names Mixture

No information avaliable

Sibutramine Chemical_Formula

C₁₇H₂₆ClN

Sibutramine RX_link

http://www.rxlist.com/cgi/generic/sibutramine.htm

Sibutramine fda sheet

Sibutramine FDA

Sibutramine msds (material safety sheet)

Sibutramine Synthesis Reference

No information avaliable

Sibutramine Molecular Weight

279.848 g/mol

Sibutramine Melting Point

191-192 ^oC

Sibutramine H₂O Solubility

2.9 mg/mL (in pH 5.2 water)

Sibutramine State

Solid

Sibutramine LogP

5.906

Sibutramine Dosage Forms

Capsules

Sibutramine Indication

For the treatment of obesity.

Sibutramine Pharmacology

Sibutramine is an orally administered agent for the treatment of obesity. Sibutramine 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-HT_1A, 5-HT_1B, 5-HT_2A, 5-HT_2C), 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.

Sibutramine Absorption

Rapid absorption following oral administration. Absolute bioavailability is not known, but at least 77% of a single oral dose of sibutramine is absorbed.

Sibutramine side effects and Toxicity

Side effects include dry mouth, anorexia, insomnia, constipation and headache.

Sibutramine Patient Information

APRD00456_PI.txt

Sibutramine Organisms Affected

Humans and other mammals