Sibutramine

From Freepedia

Image:Sibutramine.png Sibutramine
1-(4-chlorophenyl)-N,N- dimethyl-a-(2-methylpropyl)- cyclobutanemethanamine
CAS number 106650-56-0	ATC code A08AA10
Chemical formula	C₁₇H₂₆ClN
Molecular weight	334.33
Bioavailability	?
Metabolism	?
Elimination half-life	?
Excretion	?
Pregnancy category	?
Legal status	Schedule IV (USA)
Routes of administration	Oral

Sibutramine (Meridia® in the USA, Reductil® in Europe), usually as sibutramide hydrochloride monohydrate, is an orally administered agent for the treatment of obesity. It is a centrally-acting stimulant chemically related to amphetamine, methamphetamine, and phentermine (one of the drugs in the Fen-Phen combination). Sibutramine is classified as a Schedule IV controlled substance in the United States.

Sibutramine is a neurotransmitter reuptake inhibitor that helps control appetite by inhibiting the reuptake of serotonin, norepinephrine, and dopamine; as such it is an anorectic (i.e. it decreases appetite) although it also has antidepressant properties. It was approved by the Food and Drug Administration (FDA) in November 1997^[1] for the treatment of obesity.

Sibutramine acts by increasing serotonin and noradrenaline levels in the brain. The serotonergic action, in particular, is thought to influence appetite. Recognised side-effects are dry mouth, headache, constipation and insomnia. It may increase blood pressure in a small proportion of individuals, and is therefore contraindicated in patients with arterial hypertension, or others in whom a rise in blood pressure would be harmful (e.g. patients with angina). Pulmonary hypertension, a problem in some other anorectics, is not a recognised side-effect.

A study is ongoing into reports of sudden death, heart failure, renal failure and gastrointenstinal problems. Despite petitions^[2], the drug has not been banned by the FDA, but was part of a Senate hearing in 2005^[3].

A large randomized-controlled study with over 9000 patients (SCOUT) is currently ongoing to examine whether or not sibutramine reduces the risk for cardiovascular complications in people at high risk for heart disease.

References

^ FDA 1997 approval
^ Petition by Public Citizen to FDA to withdraw sibutramine
^ Bruce Japsen. "FDA weighs decision on Meridia ; Health advisory likely for Abbott obesity drug". Chicago Tribune. Chicago, Ill.: Mar 13, 2005. pg. 1.