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Posted by Reductil on Tue Jul 13 06:40:53 2004: IP Address: 195.166.60.200

In Reply to: Re: Smiling posted by Renee on Fri Apr 7 21:49:26 2000:

REDUCTIL

Presentation

Sibutramine hydrochloride

REDUCTIL 10mg is a blue/yellow capsule with 'Reductil' and '10' printed on the capsule.

REDUCTIL 15mg is a blue/white capsule with 'Reductil' and '15' printed on the capsule.

Uses

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REDUCTIL (sibutramine hydrochloride ) is the first orally administered serotonin (5-hydroxytryptamine, 5-HT) and noradrenaline reuptake inhibitor (SNRI) to be used for the management of obesity.

Sibutramine produces its therapeutic effects predominantly via its active secondary and primary amine metabolites (metabolites 1 and 2 respectively) which are inhibitors of noradrenaline, serotonin (5-hydroxytryptamine; 5-HT) and dopamine reuptake. In human brain tissue, metabolites 1 and 2 are ~3-fold more potent as in vitro inhibitors of noradrenaline and serotonin reuptake than of dopamine. Plasma samples taken from sibutramine-treated volunteers caused significant inhibition of both noradrenaline reuptake (73%) and serotonin reuptake (54%) with no significant inhibition of dopamine reuptake (16%). Sibutramine and its metabolites are neither monoamine-releasing agents nor are they monoamine oxidase inhibitors. They have no affinity with a large number of neurotransmitter receptors, including serotonergic (5-HT₁, 5-HT_1A, 5-HT_1B, 5-HT_2A, 5-HT_2C), adrenergic (β₁, β₂, β₃,α₁, α₂), dopaminergic (D₁-like, D₂-like), muscarinic, histaminergic (H₁), benzodiazepine and NMDA receptors.

In animal models, it potently reduces body weight gain by a dual action to decrease calorie intake through enhancement of post-ingestive satiety responses and to increase energy expenditure by enhancing resting metabolic rate. It is postulated that sibutramine decreases food intake by enhancing central noradrenaline and 5-HT function mediated through α-1 and 5-HT_2A/2C receptors, respectively, and increases metabolic rate by enhancing peripheral noradrenaline function through α-3 adrenoreceptors. In man dose-dependant reductions in bodyweight are seen following treatment with sibutramine.

Pharmacodynamics/Clinical Studies

Observational epidemiologic studies have established a relationship between obesity and the risks for cardiovascular disease, non-insulin dependent diabetes mellitus (NIDDM), certain forms of cancer, gallstones, certain respiratory disorders, and an increase in overall mortality. These studies suggest that weight loss, if maintained, may produce health benefits for some patients with chronic obesity who may also be at risk for other diseases.

The long-term effects of REDUCTIL on the morbidity and mortality associated with obesity have not been established. Sibutramine's effect on weight loss was examined in double-blind, placebo-controlled obesity trials with study durations of 8 weeks to 18 months and doses ranging from 1 to 30mg once daily.

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: <H1><FONT size=3>REDUCTIL</FONT></H1><P><STRONG>Presentation</STRONG></P><P>Sibutramine hydrochloride </P><P>REDUCTIL 10mg is a blue/yellow capsule with 'Reductil' and '10' printed on the capsule.</P><P>REDUCTIL 15mg is a blue/white capsule with 'Reductil' and '15' printed on the capsule.</P><P><STRONG>Uses</STRONG></P><P><STRONG>Actions</STRONG></P><P>REDUCTIL (sibutramine hydrochloride ) is the first orally administered serotonin (5-hydroxytryptamine, 5-HT) and noradrenaline reuptake inhibitor (SNRI) to be used for the management of obesity.</P><P>Sibutramine produces its therapeutic effects predominantly via its active secondary and primary amine metabolites (metabolites 1 and 2 respectively) which are inhibitors of noradrenaline, serotonin (5-hydroxytryptamine; 5-HT) and dopamine reuptake. In human brain tissue, metabolites 1 and 2 are ~3-fold more potent as in vitro inhibitors of noradrenaline and serotonin reuptake than of dopamine. Plasma samples taken from sibutramine-treated volunteers caused significant inhibition of both noradrenaline reuptake (73%) and serotonin reuptake (54%) with no significant inhibition of dopamine reuptake (16%). Sibutramine and its metabolites are neither monoamine-releasing agents nor are they monoamine oxidase inhibitors. They have no affinity with a large number of neurotransmitter receptors, including serotonergic (5-HT<SUB>1</SUB>, 5-HT<SUB>1A</SUB>, 5-HT<SUB>1B</SUB>, 5-HT<SUB>2A</SUB>, 5-HT<SUB>2C</SUB>), adrenergic (β<SUB>1</SUB>, β<SUB>2</SUB>, β<SUB>3</SUB>,α<SUB>1</SUB>, α<SUB>2</SUB>), dopaminergic (D<SUB>1</SUB>-like, D<SUB>2</SUB>-like), muscarinic, histaminergic (H<SUB>1</SUB>), benzodiazepine and NMDA receptors.</P><P>In animal models, it potently reduces body weight gain by a dual action to decrease calorie intake through enhancement of post-ingestive satiety responses and to increase energy expenditure by enhancing resting metabolic rate. It is postulated that sibutramine decreases food intake by enhancing central noradrenaline and 5-HT function mediated through α-1 and 5-HT<SUB>2A/2C</SUB> receptors, respectively, and increases metabolic rate by enhancing peripheral noradrenaline function through α-3 adrenoreceptors. In man dose-dependant reductions in bodyweight are seen following treatment with sibutramine.</P><P><STRONG>Pharmacodynamics/Clinical Studies</STRONG></P><P>Observational epidemiologic studies have established a relationship between obesity and the risks for cardiovascular disease, non-insulin dependent diabetes mellitus (NIDDM), certain forms of cancer, gallstones, certain respiratory disorders, and an increase in overall mortality. These studies suggest that weight loss, if maintained, may produce health benefits for some patients with chronic obesity who may also be at risk for other diseases.</P><P>The long-term effects of REDUCTIL on the morbidity and mortality associated with obesity have not been established. Sibutramine's effect on weight loss was examined in double-blind, placebo-controlled obesity trials with study durations of 8 weeks to 18 months and doses ranging from 1 to 30mg once daily.

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