Last modified
09/30/2018 - 06:40

Sibutramine

Product Details

Name Sibutramine
Alias Meridia
CAS  No. 106650-56-0
Formula C17H26ClN
Weight 279.85 g/mol
Usage Diet Pills / Pharmaceuticals
Appearance White crystalline powder

Product Description

Sibutramine, a chemical name of 1-(4-chlorophenyl)-N,N-dimethyl-indole-(2-methylpropyl)cyclobutanamine, is a white crystalline powder.It is an appetite suppressant acting on the central nervous system. Its chemical structure is related to amphetamine, but its mechanism of action is different. 

Sibutramine is medically useful as an oral weight loss drug, usually using sibutramine hydrochloride to produce medicines. The drug was developed by Abbott Laboratories, USA, under the trade names Reductil, Meridia, and has been discontinued in many countries.


Until 2010, it was widely sold and prescribed as an adjunct to obesity treatment with diet and exercise. It has been associated with increased cardiovascular events and strokes and has been withdrawn from several countries and regions on the market, including Australia, Canada, China, the European Union, Hong Kong, India, Mexico, New Zealand, the Philippines, Thailand, the United Kingdom, and the United States. However, this drug is still available in some countries.

 

Function

Sibutramine is a non-amphetamine appetite suppressant with antidepressant properties.

Sibutramine acts primarily through its secondary (M1) and primary (M2) amine metabolites, Its mechanism of action is to inhibit the reuptake of norepinephrine, serotonin and dopamine, increase satiety and accelerate energy expenditure while releasing norepinephrine, serotonin, and dopamine No significant impact.

Studies have also shown that sibutramine and its amine active metabolites have no significant anticholinergic, antihistamine and monoamine oxidase inhibitory effects.

Sibutramine is a monoamine reuptake inhibitor (MRI) that, in humans, reduces reuptake of norepinephrine (via ~73%), serotonin (from ~54%), and dopamine (by ~ 16%), thus increasing the levels of these substances in synaptic cracks help to enhance satiety; in particular, serotoninergic effects are thought to affect appetite. Older anorexia agents such as amphetamine and fenfluramine force these neurotransmitters to be released rather than affecting their reuptake.

 

Application

Sibutramine is an oral central weight-loss drug. It is a non-amphetamine appetite suppressant. Its metabolites in the body can inhibit the reuptake of norepinephrine, serotonin and dopamine, reduce appetite and increase satiety. energy consumption and speed up the body, thus reducing the weight. Its degree of weight loss was positively correlated with the dose. In addition, this product has a mild anti-depressant effect. Oral absorbable, bioavailability is 77%; peak plasma concentration after 1.2 hours, protein binding rate of 97%, the highest concentration in the liver and kidney. In the liver metabolism of the two active metabolites: single norepinephrine sibutramine dual norepinephrine and sibutramine.

1.5-HT reuptake inhibitor for the treatment of obesity.
2. As a norepinephrine and 5-HT reuptake inhibitor, sibutramine acts primarily through its metabolites. It inhibits the reuptake of 5-HT, norepinephrine and other monoamine signaling factors, increases physiological satiety, reduces appetite, induces heat production, increases energy consumption, and reduces fat accumulation. Obesity treatment for diet control, exercise inability to reduce and weight control.

 

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