Orlistat

From Anvita Health Wiki

Contents 1 Introduction 2 Indications 3 Contraindications 4 Dosage 5 Pharmacokinetics 6 Adverse-effects 7 Drug-interactions 8 Mechanism-of-action 9 Notes 10 More General Terms 11 Internet Database 12 References

Introduction

• Tradenames: Xenical, Alli ( OTC). C29H53NO5.

Indications

• weight reduction (> 30 lbs overweight)
• overweight patients with diabetes mellitus type 2

• for use in combination with metformin

• weight reduction in obese adolescents

Contraindications

• malabsorption syndrome

Dosage

• 120 mg with meals
• in combination with diet
• psyllium ( Metamucil) 6 g (1 round tsp) with each dose of orlistat can reduce GI symptoms [3]
• take in combination with multivitamin [6]

• Xenical 120 mg. Alli 60 mg ( OTC) [6]

Pharmacokinetics

• not systemically absorbed

Adverse-effects

• (generally diminish with time)
• oily spotting (4-25%)
• flatus with discharge (2-21%)
• fecal urgency (1-15%)
• fatty/oily stools (5-17%)
• increased defecation (2-6%)
• fecal incontinence (2-9%) [5]
• reports of serious liver injury, including 6 cases of liver failure [9]
• urinary calculi ( oxalate) [10]

Drug-interactions

• not recommended with cyclosporine

Mechanism-of-action

• reversible inhibitor of lipase within the GI tract
• forms covalent bond with active serine residues of gastric & pancreatic lipases
• inhibits dietary fat absorption by about 30%
• systemic absorption is minimal
• diminishes absorption of fat

Notes

• Alli ( OTC) about $2/day (2007) [7]

More General Terms

• ester
• amide
• metabolic agent (metabolic modifier)
• enzyme inhibitor

Internet Database

PubChem: 3034010
PubChem: 5284600
PubChem: 4599

References

1. Roche product information
2. Kaiser Permanente Northern California Regional Drug Formulary, Update 9/99
3. Prescriber's Letter 8(9):50, 2001
4. Journal Watch 22(17):132, 2002 Miles JM et al, Diabetes Care 25:1123, 2002
5. Journal Watch 25(14):111, 2005 Chanoine JP, 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 Jun 15;293(23):2873-83. PMID: [1]
   - Joffe A. Pharmacotherapy for adolescent obesity: a weighty issue. JAMA. 2005 Jun 15;293(23):2932-4. No abstract available. PMID: [2]
6. Prescriber's Letter 13(3): 2006 Acomplia (Rimonabant) and OTC Orlistat for Weight Loss Detail-Document#: [3] (subscription needed) [4]
7. Prescriber's Letter 14(3): 2007 FDA Approves Orlistat for Over-the-Counter Use Detail-Document#: [5] (subscription needed) [6]
8. Prescriber's Letter 14(7): 2007 OTC Orlistat (Alli) for Weight Loss: An Update Detail-Document#: [7] (subscription needed) [8]
9. FDA MedWatch [9] [10]
10. Medical Knowledge Self Assessment Program (MKSAP) 15, American College of Physicians, Philadelphia 2009

orlistat (Xenical, Alli)