Sibutramine: Difference between revisions
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'''Sibutramine''' is a | '''Sibutramine''' is a a centrally-acting [[serotonin-norepinephrine reuptake inhibitor]] structurally related to [[amphetamine]]s. Originally used in the treatment of [[depression]], <ref name=Woo2009>Woo T (2009) Pharmacotherapy and surgery treatment for the severely obese adolescent. ''J Paediatric Health Care'' 23:206-12</ref> it is now used to help obese and overweight patients lose weight, and along with [[Orlistat]], in 2008 was the only drug licensed for use in the UK. <ref name=Rang2007>Rang H ''et al.''(2007) ''Pharmacology''. Churchill Livingstone, Elsevier. 417-8</ref> It has been associated with increased cardiovascular events and stroke, and has since been withdrawn from the market. | ||
Sibutramine acts within the [[hypothalamus]] by preventing reuptake of both [[noradrenaline]] and [[serotonin]]. <ref name=Bray2008>Bray G (2008) Lifestyle and pharmacological approaches to weight loss: efficacy and safety. ''J Clin Endocrinol Metab'' 93:S81–8 </ref><ref name=Tziomalos2009>Tziomalos K ''et al.'' (2009) The use of sibutramine in the management of obesity and related disorders: An update. ''Vascular Health and Risk Management'' 5:441-52</ref> This inhibition causes the patient increased feelings of satiety, a decreased appetite, and a corresponding reduced intake of food which results in weight loss. <ref name=Coutinho2009>Coutinho W (2009) The first decade of sibutramine and orlistat: a reappraisal of their expanding roles in the treatment of obesity and associated conditions. ''Arquivos Brasileiros De Endocrinologia E Metabologia'' 53:262-70</ref> Some studies have shown that sibutramine may increase [[thermogenesis]] and as such, contribute to weight loss, but there have also been other studies in which no such effects were shown, and it seems that this action contributes in, at most a minor way to weight loss. It is also thought that sibutramine may effect levels of the hormones [[leptin]] and [[ghrelin]], as well as central [[neuropeptide Y]] (NPY), and [[proopiomelanocortin]] (POMC) mRNA. Sibutramine treatment differs to orlistat in relation to leptin, as, when using sibutramine, transfer of leptin into the brain is maintained or even increased during weight loss which does not happen when using orlistat. | |||
Sibutramine was first marketed by Knoll Pharmaceuticals and subsequently by [[Abbott Laboratories]] under various brand names including ''Reductil'', ''Meridia'' and ''Sibutrex''. It is classified as a [[Controlled Substances Act#Schedule IV drugs|Schedule IV]] [[controlled substance]] in the U.S.A. | |||
==References== | ==References== | ||
<references/> | <references/> | ||
Revision as of 10:49, 11 October 2010
Sibutramine is a a centrally-acting serotonin-norepinephrine reuptake inhibitor structurally related to amphetamines. Originally used in the treatment of depression, [1] it is now used to help obese and overweight patients lose weight, and along with Orlistat, in 2008 was the only drug licensed for use in the UK. [2] It has been associated with increased cardiovascular events and stroke, and has since been withdrawn from the market.
Sibutramine acts within the hypothalamus by preventing reuptake of both noradrenaline and serotonin. [3][4] This inhibition causes the patient increased feelings of satiety, a decreased appetite, and a corresponding reduced intake of food which results in weight loss. [5] Some studies have shown that sibutramine may increase thermogenesis and as such, contribute to weight loss, but there have also been other studies in which no such effects were shown, and it seems that this action contributes in, at most a minor way to weight loss. It is also thought that sibutramine may effect levels of the hormones leptin and ghrelin, as well as central neuropeptide Y (NPY), and proopiomelanocortin (POMC) mRNA. Sibutramine treatment differs to orlistat in relation to leptin, as, when using sibutramine, transfer of leptin into the brain is maintained or even increased during weight loss which does not happen when using orlistat.
Sibutramine was first marketed by Knoll Pharmaceuticals and subsequently by Abbott Laboratories under various brand names including Reductil, Meridia and Sibutrex. It is classified as a Schedule IV controlled substance in the U.S.A.
References
- ↑ Woo T (2009) Pharmacotherapy and surgery treatment for the severely obese adolescent. J Paediatric Health Care 23:206-12
- ↑ Rang H et al.(2007) Pharmacology. Churchill Livingstone, Elsevier. 417-8
- ↑ Bray G (2008) Lifestyle and pharmacological approaches to weight loss: efficacy and safety. J Clin Endocrinol Metab 93:S81–8
- ↑ Tziomalos K et al. (2009) The use of sibutramine in the management of obesity and related disorders: An update. Vascular Health and Risk Management 5:441-52
- ↑ Coutinho W (2009) The first decade of sibutramine and orlistat: a reappraisal of their expanding roles in the treatment of obesity and associated conditions. Arquivos Brasileiros De Endocrinologia E Metabologia 53:262-70