orlistat (Xenical, Alli)
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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
* no long-term effectiveness[14]
Contraindications
malabsorption syndrome
Dosage
- 120 mg with meals
- in combination with American Heart Association 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)
- lower gastrointestinal distress
- oily spotting (4-25%)
- flatus with discharge (2-21%)
- fecal urgency (1-15%)
- fatty/oily stools (5-17%), steatorrhea
- increased defecation (2-6%)
- fecal incontinence (2-9%)[5]
- diarrhea[14]
- reports of serious liver injury, including 6 cases of liver failure[9]
- probably not hepatotoxic[11]
- urinary calculi (hyperoxaluria, calcium oxalate stones)[10][13]
- malnutrition[14]
- diminishes absorption of fat-soluble vitamins
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
References
- ↑ Roche product information
- ↑ Kaiser Permanente Northern California Regional Drug Formulary, Update 9/99
- ↑ Jump up to: 3.0 3.1 Prescriber's Letter 8(9):50, 2001
- ↑ Journal Watch 22(17):132, 2002 Miles JM et al, Diabetes Care 25:1123, 2002
- ↑ Jump up to: 5.0 5.1 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: https://www.ncbi.nlm.nih.gov/pubmed/15956632
Joffe A. Pharmacotherapy for adolescent obesity: a weighty issue. JAMA. 2005 Jun 15;293(23):2932-4. No abstract available. PMID: https://www.ncbi.nlm.nih.gov/pubmed/15956639 - ↑ Jump up to: 6.0 6.1 6.2 Prescriber's Letter 13(3): 2006 Acomplia (Rimonabant) and OTC Orlistat for Weight Loss Detail-Document#: http://prescribersletter.com/(5bhgn1a4ni4cyp2tvybwfh55)/pl/ArticleDD.aspx?li=1&st=1&cs=&s=PRL&pt=3&fpt=25&dd=220313&pb=PRL (subscription needed) http://www.prescribersletter.com
- ↑ Jump up to: 7.0 7.1 Prescriber's Letter 14(3): 2007 FDA Approves Orlistat for Over-the-Counter Use Detail-Document#: http://prescribersletter.com/(5bhgn1a4ni4cyp2tvybwfh55)/pl/ArticleDD.aspx?li=1&st=1&cs=&s=PRL&pt=3&fpt=25&dd=230310&pb=PRL (subscription needed) http://www.prescribersletter.com
- ↑ Prescriber's Letter 14(7): 2007 OTC Orlistat (Alli) for Weight Loss: An Update Detail-Document#: http://prescribersletter.com/(5bhgn1a4ni4cyp2tvybwfh55)/pl/ArticleDD.aspx?li=1&st=1&cs=&s=PRL&pt=3&fpt=25&dd=230702&pb=PRL (subscription needed) http://www.prescribersletter.com
- ↑ Jump up to: 9.0 9.1 FDA MedWatch http://www.fda.gov/Safety/MedWatch/SafetyInformation/SafetyAlertsforHumanMedicalProducts/ucm180025.htm http://www.fda.gov/Safety/MedWatch/SafetyInformation/SafetyAlertsforHumanMedicalProducts/ucm213448.htm
- ↑ Jump up to: 10.0 10.1 Medical Knowledge Self Assessment Program (MKSAP) 15, American College of Physicians, Philadelphia 2009
- ↑ Jump up to: 11.0 11.1 Douglas IJ et al. Orlistat and the risk of acute liver injury: Self controlled case series study in UK Clinical Practice Research Datalink. BMJ 2013 Apr 12; 346:f1936. PMID: https://www.ncbi.nlm.nih.gov/pubmed/23585064
- ↑ Hong J-L et al. Risk of colorectal cancer after initiation of orlistat: Matched cohort study. BMJ 2013 Aug 27; 347:f5039. <PubMed> PMID: https://www.ncbi.nlm.nih.gov/pubmed/23982291 <Internet> http://www.bmj.com/content/347/bmj.f5039
- ↑ Jump up to: 13.0 13.1 Weir MA, Beyea MM, Gomes T et al Orlistat and acute kidney injury: an analysis of 953 patients. Arch Intern Med. 2011 Apr 11;171(7):703-4. PMID: https://www.ncbi.nlm.nih.gov/pubmed/21482850
- ↑ Jump up to: 14.0 14.1 14.2 14.3 Therapeutics Letter #108. Therapeutics Initiative Drugs to Avoid. http://www.ti.ubc.ca/2018/01/04/108-drugs-avoid/