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Brand names,
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Analogs
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Brand Names Mixture
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Chemical_Formula
C17H26ClN
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RX_link
http://www.rxlist.com/cgi/generic/sibutramine.htm
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fda sheet
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msds (material safety sheet)
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Synthesis Reference
No information avaliable
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Molecular Weight
279.848 g/mol
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Melting Point
191-192 oC
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H2O Solubility
2.9 mg/mL (in pH 5.2 water)
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State
Solid
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LogP
5.906
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Dosage Forms
Capsules
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Indication
For the treatment of obesity.
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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-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.
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Absorption
Rapid absorption following oral administration. Absolute bioavailability is not known, but at least 77% of a single oral dose of sibutramine is absorbed.
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side effects and Toxicity
Side effects include dry mouth, anorexia, insomnia, constipation and headache.
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Patient Information
APRD00456_PI.txt
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Organisms Affected
Humans and other mammals