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PMID: 16956313 Published · ppublish English Journal Article Research Support, Non-U.S. Gov't Review

Orlistat: a review of its use in the management of obesity.

Drugs ·Vol. 66 ·No. 12 ·2006-00-00 ·Pages 1625-56

Henness S, Perry CM

Abstract

Orlistat (Xenical) is a reversible inhibitor of gastric and pancreatic lipases. In conjunction with a hypocaloric diet and moderate exercise, orlistat is an effective drug for use in the management of obesity in adults with or without comorbidities. Recent data have shown that orlistat is also effective as a component of weight management strategies in obese adolescents. In addition to its well established efficacy in achieving modest weight loss, orlistat has been shown to improve glycaemic parameters in obese adults with type 2 diabetes mellitus as well as some features of the metabolic syndrome. Orlistat is generally well tolerated. Thus, orlistat is an option for the treatment of obese patients with or without type 2 diabetes and also has a role in the management of obese patients with the metabolic syndrome, associated comorbidities or concomitant disorders.

MeSH Terms
Adolescent Adult Anti-Obesity Agents/pharmacokinetics,pharmacology,therapeutic use Biological Availability Blood Glucose/drug effects Blood Pressure/drug effects Diabetes Mellitus, Type 2/complications Female Humans Lactones/pharmacokinetics,pharmacology,therapeutic use Male Obesity/complications,drug therapy Orlistat Overweight Randomized Controlled Trials as Topic Weight Loss/drug effects
Chemicals
Anti-Obesity Agents Blood Glucose Lactones Orlistat
Authors & Affiliations
2 authors, click to expand affiliations / ORCID
Henness Sheridan
Adis International Limited, Mairangi Bay, Auckland, New Zealand. [email protected]
Perry Caroline M
References (97)
97 references, click to expand
  1. Randomized, double-blind, placebo-controlled trial of orlistat for weight loss in adolescents.
    Endocr Pract. 2006 Jan-Feb;12(1):18-28 PMID: 16524859
  2. Weight control and risk factor reduction in obese subjects treated for 2 years with orlistat: a randomized controlled trial.
    JAMA. 1999 Jan 20;281(3):235-42 PMID: 9918478
  3. Coronary heart disease incidence in NIDDM patients in the Helsinki Heart Study.
    Diabetes Care. 1992 Jul;15(7):820-5 PMID: 1516498
  4. The influence of orlistat on the pharmacokinetics and pharmacodynamics of glyburide in healthy volunteers.
    J Clin Pharmacol. 1995 May;35(5):521-5 PMID: 7657854
  5. The effect of orlistat on the pharmacokinetics and pharmacodynamics of warfarin in healthy volunteers.
    J Clin Pharmacol. 1996 Jul;36(7):659-66 PMID: 8844450
  6. The effect of orlistat, an inhibitor of dietary fat absorption, on the absorption of vitamins A and E in healthy volunteers.
    J Clin Pharmacol. 1996 Jul;36(7):647-53 PMID: 8844448
  7. Effects of orlistat on obesity-related diseases - a six-month randomized trial.
    Diabetes Obes Metab. 2004 Sep;6(5):375-83 PMID: 15287931
  8. Efficacy of orlistat as an adjunct to behavioral treatment in overweight African American and Caucasian adolescents with obesity-related co-morbid conditions.
    J Pediatr Endocrinol Metab. 2004 Mar;17(3):307-19 PMID: 15112907
  9. Effect of orlistat treatment on body composition and resting energy expenditure during a two-year weight-reduction programme in obese Finns.
    Int J Obes Relat Metab Disord. 2000 Dec;24(12):1567-72 PMID: 11126207
  10. A health economic model to assess the long-term effects and cost-effectiveness of orlistat in obese type 2 diabetic patients.
    Diabetes Care. 2002 Feb;25(2):303-8 PMID: 11815500
  11. Effect of orlistat in overweight and obese patients with type 2 diabetes treated with metformin.
    Diabetes Care. 2002 Jul;25(7):1123-8 PMID: 12087008
  12. Three-month tolerability of orlistat in adolescents with obesity-related comorbid conditions.
    Obes Res. 2002 Jul;10(7):642-50 PMID: 12105286
  13. The cost effectiveness of orlistat in a 1-year weight-management programme for treating overweight and obese patients in Sweden : a treatment responder approach.
    Pharmacoeconomics. 2005;23(10):1007-20 PMID: 16235974
  14. Influence of intense multidisciplinary follow-up and orlistat on weight reduction in a primary care setting.
    BMC Fam Pract. 2005 Jan 29;6(1):5 PMID: 15679893
  15. Clinical efficacy of orlistat therapy in overweight and obese patients with insulin-treated type 2 diabetes: A 1-year randomized controlled trial.
    Diabetes Care. 2002 Jun;25(6):1033-41 PMID: 12032111
  16. Economic evaluation of orlistat in overweight and obese patients with type 2 diabetes mellitus.
    Pharmacoeconomics. 2003;21(7):501-12 PMID: 12696990
  17. The effect of orlistat on the pharmacokinetics of phenytoin in healthy volunteers.
    J Clin Pharmacol. 1996 Jul;36(7):654-8 PMID: 8844449
  18. Effect of orlistat on cardiovascular disease risk in obese adults.
    Diabetes Obes Metab. 2005 May;7(3):254-62 PMID: 15811142
  19. Weight change and blood coagulability and fibrinolysis in healthy obese women.
    Int J Obes Relat Metab Disord. 2001 Feb;25(2):212-8 PMID: 11410822
  20. Orlistat in the long-term treatment of obesity in primary care settings.
    Arch Fam Med. 2000 Feb;9(2):160-7 PMID: 10693734
  21. Effect of orlistat on weight and body composition in obese adolescents: a randomized controlled trial.
    JAMA. 2005 Jun 15;293(23):2873-83 PMID: 15956632
  22. Long-term systemic exposure of orlistat, a lipase inhibitor, and its metabolites in obese patients.
    J Clin Pharmacol. 1999 Jan;39(1):41-6 PMID: 9987699
  23. A pilot study of orlistat treatment in obese, non-alcoholic steatohepatitis patients.
    Aliment Pharmacol Ther. 2004 Sep 15;20(6):623-8 PMID: 15352910
  24. Role of orlistat in the treatment of obese patients with type 2 diabetes. A 1-year randomized double-blind study.
    Diabetes Care. 1998 Aug;21(8):1288-94 PMID: 9702435
  25. Effect of Orlistat in obese patients with heart failure: a pilot study.
    Congest Heart Fail. 2005 May-Jun;11(3):118-23 PMID: 15947531
  26. Reduction of body weight and co-morbidities by orlistat: The XXL--Primary Health Care Trial.
    Diabetes Obes Metab. 2005 Jan;7(1):21-7 PMID: 15642072
  27. Diabesity: are weight loss medications effective?
    Treat Endocrinol. 2005;4(2):65-74 PMID: 15783244
  28. Effect of intensive blood-glucose control with metformin on complications in overweight patients with type 2 diabetes (UKPDS 34). UK Prospective Diabetes Study (UKPDS) Group.
    Lancet. 1998 Sep 12;352(9131):854-65 PMID: 9742977
  29. Orlistat for obesity: benefits beyond weight loss.
    Diabetes Res Clin Pract. 2005 Jan;67(1):78-83 PMID: 15620437
  30. Review of limited systemic absorption of orlistat, a lipase inhibitor, in healthy human volunteers.
    J Clin Pharmacol. 1995 Nov;35(11):1103-8 PMID: 8626884
  31. Lipid peroxides in obese patients and effects of weight loss with orlistat on lipid peroxides levels.
    Int J Obes (Lond). 2005 Jan;29(1):142-5 PMID: 15467775
  32. Effect of orlistat, micronised fenofibrate and their combination on metabolic parameters in overweight and obese patients with the metabolic syndrome: the FenOrli study.
    Curr Med Res Opin. 2005 Dec;21(12):1997-2006 PMID: 16368051
  33. Intensive blood-glucose control with sulphonylureas or insulin compared with conventional treatment and risk of complications in patients with type 2 diabetes (UKPDS 33). UK Prospective Diabetes Study (UKPDS) Group.
    Lancet. 1998 Sep 12;352(9131):837-53 PMID: 9742976
  34. Latin-American trial of orlistat for weight loss and improvement in glycaemic profile in obese diabetic patients.
    Diabetes Obes Metab. 2003 May;5(3):180-8 PMID: 12681025
  35. A randomized study of orlistat in combination with a weight management programme in obese patients with Type 2 diabetes treated with metformin.
    Diabet Med. 2005 May;22(5):612-8 PMID: 15842517
  36. Orlistat: in the prevention and treatment of type 2 diabetes mellitus.
    Drugs. 2001;61(14):2107-19; discussion 2120-1 PMID: 11735640
  37. The burden of chronic hyperglycemia.
    Diabetes Care. 1998 Dec;21 Suppl 3:C32-4 PMID: 9850486
  38. The ORLIstat and CArdiovascular risk profile in patients with metabolic syndrome and type 2 DIAbetes (ORLICARDIA) Study.
    Curr Med Res Opin. 2004 Sep;20(9):1393-401 PMID: 15383188
  39. Pharmacologic and surgical management of obesity in primary care: a clinical practice guideline from the American College of Physicians.
    Ann Intern Med. 2005 Apr 5;142(7):525-31 PMID: 15809464
  40. XENical in the prevention of diabetes in obese subjects (XENDOS) study: a randomized study of orlistat as an adjunct to lifestyle changes for the prevention of type 2 diabetes in obese patients.
    Diabetes Care. 2004 Jan;27(1):155-61 PMID: 14693982
  41. Orlistat: a review of its use in the management of obesity.
    Drugs. 1999 Oct;58(4):743-60 PMID: 10551441
  42. Pharmacokinetic evaluation of the possible interaction between selected concomitant medications and orlistat at steady state in healthy subjects.
    J Clin Pharmacol. 2002 Sep;42(9):1011-9 PMID: 12211217
  43. Analysis of the XENDOS study (Xenical in the Prevention of Diabetes in Obese Subjects).
    Endocr Pract. 2006 Jan-Feb;12 Suppl 1:31-3 PMID: 16627377
  44. Cognitive behavioral therapy guided self-help and orlistat for the treatment of binge eating disorder: a randomized, double-blind, placebo-controlled trial.
    Biol Psychiatry. 2005 May 15;57(10):1193-201 PMID: 15866560
  45. Orlistat: a review of its use in the management of patients with obesity.
    Drugs. 2004;64(24):2845-64 PMID: 15563254
  46. Influence of weight loss on myocardial performance index.
    Heart Vessels. 2006 Mar;21(2):84-8 PMID: 16550308
  47. Executive Summary of The Third Report of The National Cholesterol Education Program (NCEP) Expert Panel on Detection, Evaluation, And Treatment of High Blood Cholesterol In Adults (Adult Treatment Panel III).
    JAMA. 2001 May 16;285(19):2486-97 PMID: 11368702
  48. X-PERT: weight reduction with orlistat in obese subjects receiving a mildly or moderately reduced-energy diet: early response to treatment predicts weight maintenance.
    Diabetes Obes Metab. 2005 Nov;7(6):699-708 PMID: 16219013
  49. Orlistat for the treatment of obesity: cost utility model.
    Obes Rev. 2005 Nov;6(4):323-8 PMID: 16246217
  50. The interaction of the lipase inhibitor orlistat with ethanol in healthy volunteers.
    Eur J Clin Pharmacol. 1998 Nov-Dec;54(9-10):773-7 PMID: 9923583
  51. Effects of equal weight loss with orlistat and placebo on body fat and serum fatty acid composition and insulin resistance in obese women.
    Am J Clin Nutr. 2004 Jan;79(1):22-30 PMID: 14684393
  52. Randomised trial of the effect of orlistat on body weight and cardiovascular disease risk profile in obese patients: UK Multimorbidity Study.
    Int J Clin Pract. 2002 Sep;56(7):494-9 PMID: 12296610
  53. Reduction in blood cyclosporine concentration by orlistat in two renal transplant patients.
    Transplant Proc. 2002 Feb;34(1):137-9 PMID: 11959223
  54. The effect of orlistat, an inhibitor of dietary fat absorption, on the pharmacokinetics of beta-carotene in healthy volunteers.
    J Clin Pharmacol. 1996 Feb;36(2):152-9 PMID: 8852391
  55. Effect of orlistat in obese patients with binge eating disorder.
    Obes Res. 2005 Oct;13(10):1701-8 PMID: 16286517
  56. Human leptin: from an adipocyte hormone to an endocrine mediator.
    Eur J Endocrinol. 2000 Sep;143(3):293-311 PMID: 11022169
  57. The effects of orlistat in patients with diabetes: improvement in glycaemic control and weight loss.
    Curr Med Res Opin. 2005 Nov;21(11):1885-90 PMID: 16307710
  58. Clinical guidelines on the identification, evaluation, and treatment of overweight and obesity in adults: executive summary. Expert Panel on the Identification, Evaluation, and Treatment of Overweight in Adults.
    Am J Clin Nutr. 1998 Oct;68(4):899-917 PMID: 9771869
  59. Effects of orlistat on fat-soluble vitamins in obese adolescents.
    Pharmacotherapy. 2002 Jul;22(7):814-22 PMID: 12126214
  60. Association of glycaemia with macrovascular and microvascular complications of type 2 diabetes (UKPDS 35): prospective observational study.
    BMJ. 2000 Aug 12;321(7258):405-12 PMID: 10938048
  61. Efficacy and safety comparative evaluation of orlistat and sibutramine treatment in hypertensive obese patients.
    Diabetes Obes Metab. 2005 Jan;7(1):47-55 PMID: 15642075
  62. Weight loss, weight maintenance, and improved cardiovascular risk factors after 2 years treatment with orlistat for obesity. European Orlistat Obesity Study Group.
    Obes Res. 2000 Jan;8(1):49-61 PMID: 10678259
  63. Lack of effect of orlistat on the bioavailability of a single dose of nifedipine extended-release tablets (Procardia XL) in healthy volunteers.
    J Clin Pharmacol. 1996 Apr;36(4):352-5 PMID: 8728349
  64. Orlistat in the treatment of overweight or obese Chinese patients with newly diagnosed Type 2 diabetes.
    Diabet Med. 2005 Dec;22(12):1737-43 PMID: 16401321
  65. Cholesterol lowering effect of dietary weight loss and orlistat treatment--efficacy and limitations.
    Aliment Pharmacol Ther. 2004 Jun 1;19(11):1173-9 PMID: 15153170
  66. Effect of orlistat on plasma leptin levels and risk factors for the metabolic syndrome.
    Metab Syndr Relat Disord. 2005 Summer;3(2):122-9 PMID: 18370719
  67. Randomised placebo-controlled trial of orlistat for weight loss and prevention of weight regain in obese patients. European Multicentre Orlistat Study Group.
    Lancet. 1998 Jul 18;352(9123):167-72 PMID: 9683204
  68. Comparison of metabolic effects of orlistat and sibutramine treatment in Type 2 diabetic obese patients.
    Diabetes Nutr Metab. 2004 Aug;17(4):222-9 PMID: 15575343
  69. The effect of short-term (21-day) orlistat treatment on the physiologic balance of six selected macrominerals and microminerals in obese adolescents.
    J Am Coll Nutr. 2003 Oct;22(5):357-62 PMID: 14559927
  70. Effect of orlistat on postprandial lipemia, NMR lipoprotein subclass profiles and particle size.
    Atherosclerosis. 2005 May;180(1):127-35 PMID: 15823285
  71. Prevention of type 2 diabetes mellitus by changes in lifestyle among subjects with impaired glucose tolerance.
    N Engl J Med. 2001 May 3;344(18):1343-50 PMID: 11333990
  72. Orlistat in responding obese type 2 diabetic patients: meta-analysis findings and cost-effectiveness as rationales for reimbursement in Sweden and Switzerland.
    Int J Obes (Lond). 2005 May;29(5):517-23 PMID: 15738932
  73. Lack of interaction between orlistat and oral contraceptives.
    Eur J Clin Pharmacol. 1996;50(5):421-4 PMID: 8839667
  74. A double-blind randomized placebo-controlled trial of orlistat for the treatment of nonalcoholic fatty liver disease.
    Clin Gastroenterol Hepatol. 2006 May;4(5):639-44 PMID: 16630771
  75. Obesity in transplant patients: case report showing interference of orlistat with absorption of cyclosporine and review of literature.
    Endocr Pract. 2002 Mar-Apr;8(2):124-6 PMID: 11942778
  76. The effect of orlistat-induced weight loss on interleukin-6 and C-reactive protein levels in obese subjects.
    Acta Cardiol. 2005 Jun;60(3):265-9 PMID: 15999465
  77. Addition of orlistat to conventional treatment in adolescents with severe obesity.
    Eur J Pediatr. 2004 Dec;163(12):738-41 PMID: 15378354
  78. Effect of orlistat added to diet (30% of calories from fat) on plasma lipids, glucose, and insulin in obese patients with hypercholesterolemia.
    Am J Cardiol. 2003 Apr 15;91(8):961-4 PMID: 12686336
  79. Effects of orlistat, a lipase inhibitor, on the pharmacokinetics of three highly lipophilic drugs (amiodarone, fluoxetine, and simvastatin) in healthy volunteers.
    J Clin Pharmacol. 2003 Apr;43(4):428-35 PMID: 12723464
  80. The effects of orlistat on body weight and glycaemic control in overweight patients with type 2 diabetes: a randomized, placebo-controlled trial.
    Diabetes Obes Metab. 2002 Nov;4(6):415-23 PMID: 12406041
  81. Short-term effect of orlistat on dietary glycotoxins in healthy women and women with polycystic ovary syndrome.
    Metabolism. 2006 Apr;55(4):494-500 PMID: 16546480
  82. Reduction in the incidence of type 2 diabetes with lifestyle intervention or metformin.
    N Engl J Med. 2002 Feb 7;346(6):393-403 PMID: 11832527
  83. Orlistat improves blood pressure control in obese subjects with treated but inadequately controlled hypertension.
    J Hypertens. 2002 Nov;20(11):2257-67 PMID: 12409965
  84. Pharmacotherapy for obesity.
    Drugs. 2005;65(10):1391-418 PMID: 15977970
  85. Safety of drug therapies used for weight loss and treatment of obesity.
    Drug Saf. 2006;29(4):277-302 PMID: 16569079
  86. Efficacy of sibutramine, orlistat and combination therapy on short-term weight management in obese patients.
    Biomed Pharmacother. 2004 Dec;58(10):582-7 PMID: 15589067
  87. Orlistat inhibits dietary cholesterol absorption.
    Obes Res. 2001 Oct;9(10):599-604 PMID: 11595776
  88. The effects of orlistat on weight and on serum lipids in obese patients with hypercholesterolemia: a randomized, double-blind, placebo-controlled, multicentre study.
    Int J Obes Relat Metab Disord. 2001 Nov;25(11):1713-21 PMID: 11753595
  89. The effect of orlistat on body weight and coronary heart disease risk profile in obese patients: the Swedish Multimorbidity Study.
    J Intern Med. 2000 Sep;248(3):245-54 PMID: 10971792
  90. Weight reduction and long-term maintenance after 18 months treatment with orlistat for obesity.
    Int J Obes Relat Metab Disord. 2003 May;27(5):591-7 PMID: 12704403
  91. Drug interaction in a renal transplant patient: cyclosporin-Neoral and orlistat.
    Am J Kidney Dis. 2003 Feb;41(2):493-6 PMID: 12552515
  92. Comparison of efficacy of sibutramine or orlistat versus their combination in obese women.
    Endocr Res. 2004 May;30(2):159-67 PMID: 15473126
  93. Orlistat for the treatment of obesity: rapid review and cost-effectiveness model.
    Obes Rev. 2000 Oct;1(2):121-6 PMID: 12119985
  94. Metabolic profiles of minimally absorbed orlistat in obese/overweight volunteers.
    J Clin Pharmacol. 1996 Nov;36(11):1006-11 PMID: 8973989
  95. Cost-effectiveness of orlistat for the treatment of overweight and obese patients in Ireland.
    Int J Obes (Lond). 2005 Aug;29(8):975-82 PMID: 15852050
  96. The influence of reduced dietary fat absorption induced by orlistat on the pharmacokinetics of digoxin in healthy volunteers.
    J Clin Pharmacol. 1995 Aug;35(8):840-3 PMID: 8522642
  97. Effects of a weight-reduction program with orlistat on serum leptin levels in obese women: A 12-week, randomized, placebo-controlled study.
    Curr Ther Res Clin Exp. 2004 Mar;65(2):127-37 PMID: 24936112
Article Info
Journal
Drugs
Abbr.
Drugs
ISSN
0012-6667
Published
2006-00-00
Pages
1625-56
Language
English
Region
New Zealand
NLM ID
7600076
Subset
IM
Analysis Services
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