Orlistat
- Atc Codes:A08AB01
- CAS Codes:96829-58-2
- PHARMGKB ID:96829-58-2
Table of contents
- Brand Names
- Chemistry
- Pharmacologic Category
- Mechanism of Action
- Therapeutic Use
- Pregnancy and Lactation Implications
- Contraindications
- Warnings and Precautions
- Adverse Reactions
- Genes that may be involved
- Drug Interactions
- Nutrition/Nutraceutical Interactions
- Dosage
- Pharmacokinetics and Pharmacodynamics
- Special Considerations
Brand Names
Europe
Austria: Alli, Xenical; Belgium: Alli, Xenical; Cyprus: Alli, Xenical; Czech Republic: Alli, Xenical; Denmark: Alli, Xenical; Estonia: Alli, Xenical; Finland: Alli, Xenical; France: Alli, Xenical; Germany: Alli, Xenical; Greece: Alli, Xenical; Hungary: Alli, Xenical; Ireland: Alli, Xenical; Italy: Alli, Xenical; Latvia: Alli, Xenical; Lithuania: Alli, Xenical; Luxembourg: Alli, Xenical; Malta: Alli, Xenical; Netherlands: Alli, Xenical; Poland: Alli, Xenical; Portugal: Alli, Xenical; Romania: Alli, Xenical; Slovakia: Alli, Xenical; Slovenia: Alli, Xenical; Spain: Alli, Xenical; Sweden: Alli, Xenical; UK: Alli, Xenical.
North America
Canada: Xenical; USA: Alli, Xenical.
Latin America
Argentina: Crisplus, Fingras, Frugal, Liposol, Oleofin, Xenical, Xinplex; Brazil: Xenical; Mexico: Amsafast, Lindeza, Lysthin, Redustat, Ventu, Xenical.
Asia
Japan: Xenical.
Drug combinations
Chemistry
Orlistat: C~29~H~53~NO~5~. Mw: 495.73. (1) L-Leucine, N-formyl-, 1-[(3-hexyl-4-oxo-2-oxetanyl)methyl]dodecyl ester, [2S-[2α(R*),3β]]-; (2) N-Formyl-L-leucine, ester with (3S,4S)-3-hexyl-4-[(2S)-2-hydroxytridecyl]-2-oxetanone. CAS-96829-58-2 (1991).
Pharmacologic Category
GI Drugs, Miscellaneous. Lipase Inhibitor. (ATC-Code: A08AB01).
Mechanism of action
Decreases intestinal lumen absorption of dietary fat (triacylglycerol) by reversibly inhibiting gastric and pancreatic lipase-mediated triglyceride hydrolysis (decreases intestinal concentrations of absorbable free fatty acids and monoglycerides). Decreases concentrations of LDL and total cholesterol. Variable effects on serum triglycerides and HDL-C.
Therapeutic use
Management of obesity (weight loss and weight management) when used in conjunction with reduced-calorie and low-fat diet.
Pregnancy and lactiation implications
There are no adequate studies in pregnant women. Not recommended for use during pregnancy. Excretion in breast milk unknown. Nursing not recommended.
Unlabeled use
Contraindications
Hypersensitivity to orlistat or any component of the formulation. Chronic malabsorption syndrome or cholestasis.
Warnings and precautions
Some patients may develop increased levels of urinary oxalate following treatment (caution if history of hyperoxaluria or calcium oxalate nephrolithiasis). Gastrointestinal adverse events may increase if taken with high-fat diet (>30% total daily calories from fat). If taken with any one very high-fat meal, possibility of gastrointestinal effects increases (daily intake of fat should be distributed over three main meals). Orlistat shown to reduce absorption of some fat-soluble vitamins and β-carotene. Patients who have had an organ transplant should not use orlistat. As with any weight-loss agent, potential exists for misuse in appropriate patient populations (e.g. patients with anorexia nervosa or bulimia).