The use of orlistat in the treatment of obesity dyslipidaemia and Type 2 diabetes

Expert Opinion on Pharmacotherapy

Volumn 6, Issue 14, 2005, Pages 2483-2491

  Nelson, Robert H ^a   Miles, John M ^a  

^a MAYO CLINIC   (United States)

Author keywords

Dyslipidaemia; Insulin resistance; Obesity; Orlistat; Type 2 diabetes

Indexed keywords

ACARBOSE; ALPHA TOCOPHEROL; ANTICONVULSIVE AGENT; ANTIOBESITY AGENT; BETA CAROTENE; CYCLOSPORIN; DIGITALIS; FATTY ACID DERIVATIVE; GLUCOSE; HEMOGLOBIN A1C; HIGH DENSITY LIPOPROTEIN CHOLESTEROL; HYDROXYMETHYLGLUTARYL COENZYME A REDUCTASE INHIBITOR; INSULIN; ISPAGULA; LIPID; LOW DENSITY LIPOPROTEIN CHOLESTEROL; METFORMIN; ORAL CONTRACEPTIVE AGENT; PLACEBO; SIBUTRAMINE; SULFONYLUREA; TESTOSTERONE; TETRAHYDROLIPSTATIN; TRIACYLGLYCEROL LIPASE; VITAMIN D; VITAMIN K GROUP; WARFARIN;

ABDOMINAL PAIN; ALTERNATIVE MEDICINE; ARTICLE; ATHEROSCLEROSIS; BEHAVIOR MODIFICATION; BLOATING; BODY MASS; CARCINOGENICITY; CARDIOVASCULAR RISK; CLINICAL TRIAL; COMORBIDITY; DIARRHEA; DIET THERAPY; DRUG ABSORPTION; DRUG ELIMINATION; DRUG METABOLISM; DRUG POTENTIATION; DRUG SAFETY; DRUG STRUCTURE; DRUG TOLERABILITY; DYSLIPIDEMIA; ENZYME INHIBITION; EXERCISE; FLATULENCE; GASTROINTESTINAL SYMPTOM; HUMAN; HYPERGLYCEMIA; HYPERTENSION; LIFESTYLE; LONGITUDINAL STUDY; LOW FAT DIET; META ANALYSIS; NON INSULIN DEPENDENT DIABETES MELLITUS; OBESITY; PRESCRIPTION; STRUCTURE ANALYSIS; SYSTEMATIC REVIEW; TREATMENT OUTCOME; VASCULAR DISEASE; WEIGHT REDUCTION;

ANTI-OBESITY AGENTS; CARDIOVASCULAR DISEASES; DIABETES MELLITUS, TYPE 2; DIET, FAT-RESTRICTED; DYSLIPIDEMIAS; ENZYME INHIBITORS; EXERCISE; GASTROINTESTINAL TRACT; HUMANS; LACTONES; LIPASE; MULTICENTER STUDIES; OBESITY; PATIENT COMPLIANCE; RANDOMIZED CONTROLLED TRIALS; WEIGHT LOSS;

EID: 28244502153     PISSN: 14656566     EISSN: None     Source Type: Journal    
DOI: 10.1517/14656566.6.14.2483     Document Type: Article

References (70)

1. WADDEN T, BUTRYN M, BYRNE K: Efficacy of lifestyle modification for long-term weight control. Obes. Res. (2004) 12(Suppl.): 151S-162S.
2. WILLIAMSON D, VINICOR F, BOWMAN B: Primary prevention of Type 2 diabetes mellitus by lifestyle intervention: implications for health policy. Ann. Intern. Med. (2004) 140(11):951-957.
3. FOSTER G, WADDEN T, PHELAN S, SARWER D, SANDERSON R: Obese patients' perceptions of treatment outcomes and the factors that influence them. Arch. Intern. Med. (2001) 161(17):2133-2139.
4. WADDEN T, BUTRYN M: Behavioral treatment of obesity. Endocrinol. Metab. Clin. North Am. (2003) 32(4):981-1003.
5. BUCHWALD H, AVIDOR Y, BRAUNWALD E et al.: Bariatric surgery: a systematic review and meta-analysis. JAMA (2004) 292(14):1724-1737.
6. WADDEN T, STUNKARD A: Psychopathology and obesity. Ann. NY Acad. Sci. (1987) 499:55-65.
7. HEDLEY A, OGDEN C, JOHNSON C et al.: Prevalence of overweight and obesity among US children, adolescents, and adults, 1999-2002. JAMA (2004) 291(23):2847-2850.
8. BLOCK J, DESALVO K, FISHER W: Are physicians equipped to address the obesity epidemic? Knowledge and attitudes of internal medicine residents. Prev. Med. (2003) 36(6):669-675.
9. FINER N: Pharmacotherapy of obesity. Best Pract. Res. Clin. Endocrinol. Metab. (2002) 16(4):717-742.
10. DRENT ML, LARSSON I, WILLIAM-OLSSON T et al.: Orlistat (Ro 18-0647), a lipase inhibitor, in the treatment of human obesity: a multiple dose study. Int. J. Obes. Relat. Metab. Disord. (1995) 19(4):221-226.
11. ZHI J, MULLIGAN TE, HAUPTMAN JB: Long-term systemic exposure of orlistat, a lipase inhibitor, and its metabolites in obese patients. J. Clin. Pharmacol. (1999) 39(1):41-46.
12. ZHI J, MELIA AT, FUNK C et al.: Metabolic profiles of minimally absorbed orlistat in obese/overweight volunteers. J. Clin. Pharmacol. (1996) 36(11):1006-1011.
13. SHEPARD TY, JENSEN DR, BLOTNER S et al.: Orlistat fails to alter postprandial plasma lipid excursions or plasma lipases in normal-weight male volunteers. Int. J. Obes. Relat. Metab. Disord. (2000) 24(2):187-194.
14. CARRIERE F, RENOU C, RANSAC S et al.: Inhibition of gastrointestinal lipolysis by Orlistat during digestion of test meals in healthy volunteers. Am. J. Physiol. Gastrointest. Liver Physiol. (2001) 281(1):G16-28.
15. PADWAL R, LI SK, LAU DC: Long-term pharmacotherapy for overweight and obesity: a systematic review and meta-analysis of randomized controlled trials. Int. J. Obes. Relat. Metab. Disord. (2003) 27(12):1437-1446.
16. DAVIDSON MH, HAUPTMAN J, DIGIROLAMO M et al.: Weight control and risk factor reduction in obese subjects treated for 2 years with orlistat: a randomized controlled trial. JAMA (1999) 281(3):235-242.
17. HILL JO, HAUPTMAN J, ANDERSON JW et al.: Orlistat, a lipase inhibitor, for weight maintenance after conventional dieting: a 1-y study. Am. J. Clin. Nutr. (1999) 69:1108-1116.
18. TORGERSON JS, HAUPTMAN J, BOLDRIN MN, SJOSTROM L: 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) 27(1):155-161.
19. MILES JM, LEITER L, HOLLANDER P et al.: Effect of orlistat in overweight and obese patients with Type 2 diabetes treated with metformin. Diabetes Care (2002) 25(7):1123-1128.
20. HOLLANDER PA, ELBEIN SC, HIRSCH IB et al.: Role of orlistat in the treatment of obese patients with Type 2 diabetes. A 1-year randomized double-blind study. Diabetes Care (1998) 21(8):1288-1294.
21. KELLEY DE, BRAY GA, PI-SUNYER FX et al.: 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) 25(6):1033-1041.
22. STERN J, HIRSCH J, BLAIR S et al.: Weighing the options: criteria for evaluating weight-management programs. The Committee to Develop Criteria for Evaluating the Outcomes of Approaches to Prevent and Treat Obesity. Obes. Res. (1995) 3(6):591-604.
23. ANDERSON JW, KONZ EC: Obesity and disease management: effects of weight loss on comorbid conditions. Obes. Res. (2001) 9(Suppl. 4):326S-334S.
24. WILLIAMSON D, PAMUK E, THUN M et al.: Prospective study of intentional weight loss and mortality in overweight white men aged 40-64 years. Am. J. Epidemiol. (1995) 149(6):491-503.
25. WILLIAMSON D, THOMPSON T, THUN M et al.: Intentional weight loss and mortality among overweight individuals with diabetes. Diabetes Care (2000) 23(10):1499-1504.
26. JAYAGOPAL V, KILPATRICK ES, HOLDING S, JENNINGS PE, SL A: Orlistat is as beneficial as metformin in the treatment of polycystic ovarian syndrome. J. Clin. Endocrinol. Metab. (2005) 90(2):729-733.
27. TAN KC, TSO AW, TAM SC, PANG RW, LAM KS: Acute effect of orlistat on post-prandial lipaemia and free fatty acids in overweight patients with Type 2 diabetes mellitus. Diabet. Med. (2002) 19(11):944-948.
28. TONSTAD S, POMETTA D, ERKELENS DW et al.: The effect of the gastrointestinal lipase inhibitor, orlistat, on serum lipids and lipoproteins in patients with primary hyperlipidaemia. Eur. J. Clin. Pharmacol. (1994) 46(5):405-410.
29. MICIC D, IVKOVIC-LAZAR T, DRAGOJEVIC R et al.: Orlistat, a gastrointestinal lipase inhibitor, in therapy of obesity with concomitant hyperlipidemia. Med. Pregl. (1999) 52(9-10):323-333.
30. LUCAS CP, BOLDRIN MN, REAVEN GM: 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) 91(8):961-964.
31. LUCAS KH, KAPLAN-MACHLIS B: Orlistat-a novel weight loss therapy. Ann. Pharmacother. (2001) 35(3):314-328.
32. ZAVORAL JH: Treatment with orlistat reduces cardiovascular risk in obese patients. J. Hypertens. (1998) 16(12 Pt 2):2013-2017.
33. HUTTON B, FERGUSSON D: Changes in body weight and serum lipid profile in obese patients treated with orlistat in addition to a hypocaloric diet: a systematic review of randomized clinical trials. Am. J. Clin. Nutr. (2004) 80 (6):1461-1468.
34. MULS E, KOLANOWSKI J, SCHEEN A, VAN GAAL L, OBELHYX STUDY G: 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) 25(11):1713-1721.
35. DEROSA G, MUGELLINI A, CICCARELLI L, FOGARI R: Randomized, double-blind, placebo-controlled comparison of the action of orlistat, fluvastatin, or both an anthropometric measurements, blood pressure, and lipid profile in obese patients with hypercholesterolemia prescribed a standardized diet. Clin. Ther. (2003) 25(4):1107-1122.
36. SJOSTROM L, RISSANEN A, ANDERSEN T et al.: Randomised placebo-controlled trial of orlistat for weight loss and prevention of weight regain in obese patients. European Multicentre Orlistat Study Group. Lancet (1998) 352:167-172.
37. MITTENDORFER B, OSTLUND RE JR, PATTERSON BW, KLEIN S: Orlistat inhibits dietary cholesterol absorption. Obes. Res. (2001) 9(10):599-604.
38. STAMLER J, VACCARO O, NEATON J, WENTWORTH D: Diabetes, other risk factors, and 12-yr cardiovascular mortality for men screened in the Multiple Risk Factor Intervention Trial. Diabetes Care. (1993) 16(2):434-444.
39. 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) 352(9131):837-853.
40. 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) 352(9131):854-865.
41. CHIASSON J, JOSSE R, GOMIS R et al.: Acarbose treatment and the risk of cardiovascular disease and hypertension in patients with impaired glucose tolerance: the STOP-NIDDM trial. JAMA (2003) 290(4):486-494.
42. KEATING GM, JARVIS B: Orlistat: in the prevention and treatment of Type 2 diabetes mellitus. Drugs (2001) 61(14):2107-2121.
43. SCHEEN AJ, PH. E: Antiobesity treatment in Type 2 diabetes: results of clinical trials with orlistat and sibutramine. Diabetes Metab. (2002) 28:437-445.
44. NORRIS SL, ZHANG X, AVENELL A et al.: Efficacy of pharmacotherapy for weight loss in adults with Type 2 diabetes mellitus: a meta-analysis. Arch. Intern. Med. (2004) 164(13):1395-1404.
45. KELLEY DE, KULLER LH, MCKOLANIS TM et al.: Effects of moderate weight loss and orlistat on insulin resistance, regional adiposity, and fatty acids in Type 2 diabetes. Diabetes Care (2004) 27(1):33-40.
46. HEYMSFIELD SB, SEGAL KR, HAUPTMAN J et al.: Effects of weight loss with orlistat on glucose tolerance and progression to Type 2 diabetes in obese adults. Arch. Int. Med. (2000) 160(9):1321-1326.
47. SHARMA AM, GOLAY A: Effect of orlistat-induced weight loss on blood pressure and heart rate in obese patients with hypertension. J. Hypertens. (2002) 20(9):1873-1878.
48. DIDANGELOS TP, THANOPOULOU AK, BOUSBOULAS SH et al.: The ORLIstat and CArdiovascular risk profile in patients with metabolic syndrome and Type 2 DIAbetes (ORLICARDIA) Study. Curr. Med. Res. Opin. (2004) 20(9):1393-1401.
49. WADDEN TA, BERKOWITZ RI, WOMBLE LG et al.: Effects of sibutramine plus orlistat in obese women following 1 year of treatment by sibutramine alone: a placebo-controlled trial. Obes. Res. (2000) 8(6):431-437.
50. FERRAZ RR, TISELIUS HG, HEILBERG IP: Fat malabsorption induced by gastrointestinal lipase inhibitor leads to an increase in urinary oxalate excretion. Kidney Int. (2004) 66(2):676-682.
51. MATHUS-VLIEGEN EM, VAN IERLAND-VAN LEEUWEN ML, TERPSTRA A: Lipase inhibition by orlistat: effects on gall-bladder kinetics and cholecystokinin release in obesity. Aliment. Pharmacol. Ther. (2004) 19(5):601-611.
52. TROUILLOT TE, PACE DG, MCKINLEY C et al.: Orlistat maintains biliary lipid composition and hepatobiliary function in obese subjects undergoing moderate weight loss. Am. J. Gastroenterol. (2001) 96(6):1888-1894.
53. CAVALIERE H, FLORIANO I, MEDEIROS-NETO G: Gastrointestinal side effects of orlistat may be prevented by concomitant prescription of natural fibers (psyllium mucilloid). Int. J. Obes. Relat. Metab. Disord. (2001) 25(7):1095-1099.
54. GOTFREDSEN A, WESTERGREN HENDEL H, ANDERSEN T: Influence of orlistat on bone turnover and body composition. Int. J. Obes. Relat. Metab. Disord. (2001) 25(8):1154-1160.
55. PACE DG, BLOTNER S, GUERCIOLINI R: Short-term orlistat treatment does not affect mineral balance and bone turnover in obese men. J. Nutr. (2001) 131(6):1694-1699.
56. CHANOINE J-P, HAMPL S, JENSEN C, BOLDRIN M, HAUPTMAN J: Effect of orlistat on weight and body composition in obese adolescents: a randomized controlled trial. JAMA. (2005) 293(23):2873-2883.
57. EVANS S, MICHAEL R, WELLS H et al.: Drug interaction in a renal transplant patient: cyclosporin-neoral and orlistat. Am. J. Kidney Dis. (2003) 41(2):493-496.
58. ZHI J, MOORE R, KANITRA L, MULLIGAN TE: Pharmacokinetic evaluation of the possible interaction between selected concomitant medications and orlistat at steady state in healthy subjects. J. Clin. Pharmacol. (2002) 42(9):1011-1019.
59. BARBARO D, ORSINI P, PALLINI S, PIAZZA F, PASQUINI C: Obesity in transplant patients: case report showing interference of orlistat with absorption of cyclosporine and review of literature. Endocr. Pract. (2002) 8(2):124-126.
60. NAGELE H, PETERSEN B, BONACKER U, RODIGER W: Effect of orlistat on blood cyclosporin concentration in an obese heart transplant patient. Eur. J. Clin. Pharmacol. (1999) 55(9):667-669.
61. FINER N, JAMES WP, KOPELMAN PG, LEAN ME, WILLIAMS G: One-year treatment of obesity: a randomized, double-blind, placebo-controlled, multicentre study of orlistat, a gastrointestinal lipase inhibitor. Int. J. Obes. Relat. Metab. Disord. (2000) 24(3):306-313.
62. MCDUFFIE JR, CALIS KA, BOOTH SL, UWAIFO GI, YANOVSKI JA: Effects of orlistat on fat-soluble vitamins in obese adolescents. Pharmacotherapy. (2002) 22(7):814-822.
63. MELIA AT, KOSS-TWARDY SG, ZHI J: 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) 36(7):647-653.
64. MACWALTER RS, FRASER HW, ARMSTRONG KM: Orlistat enhances warfarin effect. Ann. Pharmacother. (2003) 37(4):510-512.
65. ZHI J, MELIA AT, GUERCIOLINI R et al.: The effect of orlistat on the pharmacokinetics and pharmacodynamics of warfarin in healthy volunteers. J. Clin. Pharmacol. (1996) 36(7):659-666.
66. ZHI J, MELIA AT, KOSS-TWARDY SG et al.: The influence of orlistat on the pharmacokinetics and pharmacodynamics of glyburide in healthy volunteers. J. Clin. Pharmacol. (1995) 35(5):521-525.
67. ZHI J, MOORE R, KANITRA L, MULLIGAN TE: 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) 43(4):428-435.
68. MELIA AT, ZHI J, KOSS-TWARDY SG et al.: The influence of reduced dietary fat absorption induced by orlistat on the pharmacokinetics of digoxin in healthy volunteers. J. Clin. Pharmacol. (1995) 35(8):840-843.
69. MELIA AT, MULLIGAN TE, ZHI J: The effect of orlistat on the pharmacokinetics of phenytoin in healthy volunteers. J. Clin. Pharmacol. (1996) 36(7):654-658.
70. HARTMANN D, GUZELHAN C, ZUIDERWIJK PB, ODINK J: Lack of interaction between orlistat and oral contraceptives. Eur. J. Clin. Pharmacol. (1996) 50(5):421-424.