Drug treatments for obesity/Bibliography

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A list of key readings about Drug treatments for obesity.
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Review Articles

[1] Magni P. et al. (2009) Feeding behavior in mammals including humans. Ann.N.Y.Acad.Sci. 1163:221-232. PMID 19456343

[2] 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. 53:262-270 (The most widely used anti-obesity agents are sibutramine and orlistat, both available in clinical practice for about a decade.)

[3] Elangbam C.S (2009) Current Strategies in the Development of Anti-obesity Drugs and Their Safety Concerns. vet pathol. 26:10-24 (This review covers the current state of antiobesity drugs and their safety concerns, and highlights new therapeutic targets and scientific advances toward the development of appropriate animal models by using novel techniques that will aid in understanding pathogenesis and pathophysiology of anorexigen-related safety issues.)

[4] Bray G (2008) Lifestyle and Pharmacological Approaches to Weight Loss: Efficacy and Safety. J Clin Endocrinol metab. 93: S81–S88 (There is currently no evidence that clearly supports a superiority of one macronutrient composition for diets used for weight loss...Physical activity is particularly important in helping patients maintain a weight loss once achieved and is less valuable for weight loss itself...but only a few drugs have been developed that tap these mechanisms. Orlistat, which blocks intestinal lipase, is one; sibutramine, a serotoninnorepinephrine reuptake inhibitor, is a second.)

[5] Zanella M, Filho F (2009) Emerging drugs for obesity therapy. Arq Bras Endocrinol Metab. 53(2):271-280 (Fortunately, recent fundamental insights into the neuroendocrine mechanisms regulating body weight provide an expanding list of molecular targets for novel, rationally designed antiobesity drugs. In this review, the therapeutic potential of some antiobesity molecules in the development will be analyzed based on an understanding of energy homeostasis.)

[6] Desilets AR, Dhakal-Karki S, Dunican KC. (2008). Role of metformin for weight management in patients without type 2 diabetes. Ann Pharmacotherapy. 42(6):817-26. "The weight loss effects of metformin in overweight or obese adults and adolescents without diabetes appear promising; however, trials have been limited by small patient populations and weak design."

[7] Siraj ES. (2003). Is there a role for metformin or acarbose as a weight-loss agent in the absence of diabetes? Cleve Clin J Med. 70(8):702-4. "several studies found that patients with type 2 diabetes lost weight while taking metformin, with significant reductions in total body fat and visceral fat in those with preexisting abdominal or visceral obesity."

[8] Knowler WC et al. (2002). Reduction in the incidence of type 2 diabetes with lifestyle intervention or metformin.N Engl J Med. 346(6):393-403. "as compared with placebo; the lifestyle intervention was significantly more effective than metformin."

[9] Bulik C, et al(1992) Abuse of Drugs Associated with Eating Disorders.

[10] Wagner J, et al(1991) Enhancement of athletic performance with drugs. An overview.

[11] Krotkiewski M, et al. Thyroid hormones in the pathogenesis and treatment of obesity.

[12] Aronne LJ, et al. New Targets for Obesity Pharmacotherapy.

[13] Greenaway, et al. The safety and efficacy of pharmaceutical and herbal caffeine and ephedrine use as a weight loss agent.

[14] Diepvens, et al. Obesity and thermogenesis related to the consumption of caffeine, ephedrine, capsaicin, and green tea

[15] - Tziomalos K et al. (2009) The use of sibutramine in the management of obesity and related disorders: An update. Vascular Health and Risk Management 5:1 pp. 441-452. (Sibutramine, in conjunction with lifestyle measures, is a useful drug for reducing body weight and improving associated cardiometabolic risk factors and obesity-related disorders. Studies of longer duration are required to determine the precise indications of the drug, to evaluate safety issues and to assess its efficacy on cardiovascular mortality. )

[16] - Woo T (2009) Pharmacotherapy and Surgery Treatment for the Severely Obese Adolescent. Journal of Paediatric Health Care 23:4 pp.206-212 (Originally studied as an antidepressant, sibutramine is a serotonin and norepinephrine re-uptake inhibitor, with metabolites (M1 and M2) that weakly inhibit dopamine, causing satiety when taken at therapeutic doses. Multiple trials in adults have demonstrated that the appetite suppressant effects of sibutramine lead to weight loss, including the Sibutramine Trial of Obesity Reduction and Maintenance (STORM) trial, a long-term trial demonstrating a sustained weight loss while taking sibutramine for up to 2 years.)


  1. Aronne LJ, et al. New Targets for Obesity Pharmacotherapy.
  2. Bray G (2008) Lifestyle and Pharmacological Approaches to Weight Loss: Efficacy and Safety. J Clin Endocrinol metab. 93: S81–S88 (There is currently no evidence that clearly supports a superiority of one macronutrient composition for diets used for weight loss...Physical activity is particularly important in helping patients maintain a weight loss once achieved and is less valuable for weight loss itself...but only a few drugs have been developed that tap these mechanisms. Orlistat, which blocks intestinal lipase, is one; sibutramine, a serotoninnorepinephrine reuptake inhibitor, is a second.)
  3. Bulik C, et al(1992) Abuse of Drugs Associated with Eating Disorders.
  4. 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. 53:262-270 (The most widely used anti-obesity agents are sibutramine and orlistat, both available in clinical practice for about a decade.)
  5. Diepvens, et al. Obesity and thermogenesis related to the consumption of caffeine, ephedrine, capsaicin, and green tea.
  6. Desilets AR, Dhakal-Karki S, Dunican KC. (2008). Role of metformin for weight management in patients without type 2 diabetes. Ann Pharmacotherapy. 42(6):817-26. "The weight loss effects of metformin in overweight or obese adults and adolescents without diabetes appear promising; however, trials have been limited by small patient populations and weak design."
  7. Elangbam C.S (2009) Current Strategies in the Development of Anti-obesity Drugs and Their Safety Concerns. vet pathol. 26:10-24 (This review covers the current state of antiobesity drugs and their safety concerns, and highlights new therapeutic targets and scientific advances toward the development of appropriate animal models by using novel techniques that will aid in understanding pathogenesis and pathophysiology of anorexigen-related safety issues.)
  8. Greenaway, et al. The safety and efficacy of pharmaceutical and herbal caffeine and ephedrine use as a weight loss agent.
  9. Knowler WC et al. (2002). Reduction in the incidence of type 2 diabetes with lifestyle intervention or metformin.N Engl J Med. 346(6):393-403. "as compared with placebo; the lifestyle intervention was significantly more effective than metformin."
  10. Krotkiewski M, et al. Thyroid hormones in the pathogenesis and treatment of obesity.
  11. Magni P. et al. (2009) Feeding behavior in mammals including humans. Ann.N.Y.Acad.Sci. 1163:221-232. PMID 19456343
  12. Siraj ES. (2003). Is there a role for metformin or acarbose as a weight-loss agent in the absence of diabetes? Cleve Clin J Med. 70(8):702-4. "several studies found that patients with type 2 diabetes lost weight while taking metformin, with significant reductions in total body fat and visceral fat in those with preexisting abdominal or visceral obesity."
  13. Tziomalos K et al. (2009) The use of sibutramine in the management of obesity and related disorders: An update. Vascular Health and Risk Management 5:1 pp. 441-452. (Sibutramine, in conjunction with lifestyle measures, is a useful drug for reducing body weight and improving associated cardiometabolic risk factors and obesity-related disorders. Studies of longer duration are required to determine the precise indications of the drug, to evaluate safety issues and to assess its efficacy on cardiovascular mortality. )
  14. Wagner J, et al(1991) Enhancement of athletic performance with drugs. An overview.
  15. Woo T (2009) Pharmacotherapy and Surgery Treatment for the Severely Obese Adolescent. Journal of Paediatric Health Care 23:4 pp.206-212 (Originally studied as an antidepressant, sibutramine is a serotonin and norepinephrine re-uptake inhibitor, with metabolites (M1 and M2) that weakly inhibit dopamine, causing satiety when taken at therapeutic doses. Multiple trials in adults have demonstrated that the appetite suppressant effects of sibutramine lead to weight loss, including the Sibutramine Trial of Obesity Reduction and Maintenance (STORM) trial, a long-term trial demonstrating a sustained weight loss while taking sibutramine for up to 2 years.)
  16. Zanella M, Filho F (2009) Emerging drugs for obesity therapy. Arq Bras Endocrinol Metab. 53(2):271-280 (Fortunately, recent fundamental insights into the neuroendocrine mechanisms regulating body weight provide an expanding list of molecular targets for novel, rationally designed antiobesity drugs. In this review, the therapeutic potential of some antiobesity molecules in the development will be analyzed based on an understanding of energy homeostasis.)
  17. 'The prevalence of obesity and associated metabolic/cardiovascular disease has reached epidemic proportions in industrialized and developing countries. Dietary and behavioural approaches are insufficient to maintain weight loss and to fight this trend... One promising new strategy is the blockade of the endocannabinoid system which is involved in the regulation of energy balance, food intake, and lipid/glucose metabolism.'
  18. 'Many different diets have been tried to treat obesity, and weight loss occurs with all of them.... Food intake is controlled through many different mechanisms, but only a few drugs have been developed that tap these mechanisms. Orlistat, which blocks intestinal lipase, is one; sibutramine, a serotoninnorepinephrine reuptake inhibitor, is a second. Surgical approaches provide the most dramatic weight loss and have been demonstrated to reduce long-term mortality and reduce the incidence of diabetes.'

Primary Research Papers

[19] Lee A, Morley JE. (1998). Metformin decreases food consumption and induces weight loss in subjects with obesity with type II non-insulin-dependent diabetes. Obes Res. 6(1):47-53. "metformin decreases calorie intake in a dose-dependent manner and leads to a reduction in bodyweight in NIDDM patients with obesity."

[20] Rossner S, Sjostrom L, Noack R, Meinders A, Noseda G (2000) Weight loss, weight maintenance, and improved cardiovascular risk factors after 2 years treatment with orlistat for obesity. Obesity Research.8:41-61 "Orlistat administered for 2 years promotes weight loss and minimizes weight regain. Additionally, orlistat therapy improves lipid profile, blood pressure, and quality of life."

[21] Hauptman J, Lucas C, Boldrin M, Collins H (2000) Orlistat in the Long-term Treatment of Obesity in Primary Care Settings. Arch Fam Med 9:160–167 "More patients treated with orlistat lost 5% or more of their initial weight in year 1 (48.8% and 50.5% of patients in the 60-mg and 120-mg groups, respectively) compared with placebo (30.7%; P,.001), and approximately 34% of patients in the orlistat groups sustained weight loss of 5% or greater over 2 years compared with 24% in the placebo group (P,.001)."

[22] Kristensen, et al. Hypothalamic CART is a new anorectic peptide regulated by leptin.



  • Hauptman J, Lucas C, Boldrin M, Collins H (2000) Orlistat in the Long-term Treatment of Obesity in Primary Care Settings. Arch Fam Med 9:160–167 "More patients treated with orlistat lost 5% or more of their initial weight in year 1 (48.8% and 50.5% of patients in the 60-mg and 120-mg groups, respectively) compared with placebo (30.7%; P,.001), and approximately 34% of patients in the orlistat groups sustained weight loss of 5% or greater over 2 years compared with 24% in the placebo group (P,.001)."
  • Kristensen, et al. Hypothalamic CART is a new anorectic peptide regulated by leptin.
  • Lee A, Morley JE. (1998). Metformin decreases food consumption and induces weight loss in subjects with obesity with type II non-insulin-dependent diabetes. Obes Res. 6(1):47-53. "metformin decreases calorie intake in a dose-dependent manner and leads to a reduction in bodyweight in NIDDM patients with obesity."
  • Rossner S, Sjostrom L, Noack R, Meinders A, Noseda G (2000) Weight loss, weight maintenance, and improved cardiovascular risk factors after 2 years treatment with orlistat for obesity. Obesity Research.8:41-61 "Orlistat administered for 2 years promotes weight loss and minimizes weight regain. Additionally, orlistat therapy improves lipid profile, blood pressure, and quality of life."
  • (2009) Effects of liraglutide in the treatment of obesity: a randomised, double-blind, placebo-controlled study. Lancet

Books

[24] Rang H, Dale M, Ritter J, Moore P (2007) Pharmacology. Churchill Livingstone, Elsevier. 417-418.

[25] Boon NA, Colledge NR, Walker BR, Hunter JAA (2006) Davidson's Principles & Practice of Medicine 111-117.

Websites

[26] NHS National Institute for Health and Clinical Excellence: Press release (2001), Viewed 7 October 2009, http://www.nice.org.uk/search/guidancesearchresults.jsp?keywords=orlistat&currentpage=2&paginatedpage=1&searchType=All&sort=&pageSize=&startYearMonth=&endYearMonth=&refId=&fromSearch=true

[27] 'The European Medicines Agency (EMEA), the European Union (EU) body which is responsible for monitoring the safety of medicines, has recommended the suspension of the marketing authorisation for rimonabant (acomplia) from Sanofi-Aventis. The EMEA has concluded that the benefits of rimonabant no longer outweigh its risks and the marketing authorisation should be suspended across the EU. The EMEA has advised that patients who are currently taking rimonabant should consult their doctor or pharmacist at a convenient time to discuss their treatment. The EMEA has advised that there is no need for patients to stop treatment with rimonabant immediately, but patients who wish to stop can do so at any time.' [N3]

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