Brand and Other Names:Alli, Xenical
- Classes: Gastrointestinal Agents, Other
Dosing & Uses
Dosage Forms & Strengths
Rx (Xenical): 120 mg PO q8hr with each fat-containing meal (during or up to 1 hr after the meal), dose >360 mg/day shows no additional benefit
OTC (Alli): Up to 60 mg PO q8hr with each fat containing meal
Only effective as an adjunct to caloric restriction, increased physical activity, and behavioral modification
Indicated in patients with pretreatment BMI >30 kg/m², or BMI >27 kg/m² in presence of other risk factors or diseases (eg, HTN, DM, hyperlipidemia)
Take vitamin supplement at least 2 hr before or after taking orlistat, such as bedtime
If patient receiving cyclosporine, administer cyclosporine 3 hr after orlistat
For patients receiving levothyroxine, administer orlistat 4 hr apart
Dosage Forms & Strengths
- Safety and efficacy not established
- Administer as in adults
- Rx (Xenical): 120 mg PO q8hr with each fat-containing meal (during or up to 1 hr after the meal), dose >360 mg/day shows no additional benefit
- OTC (Alli): Up to 60 mg PO q8hr with each fat containing meal
- Only effective as an adjunct to caloric restriction, increased physical activity, and behavioral modification
- Indicated in patients with pretreatment BMI >30 kg/m², or BMI >27 kg/m² in presence of other risk factors or diseases (eg, HTN, DM, hyperlipidemia)
Serious - Use Alternative
Significant - Monitor Closely
Oily spotting (5%)
Frequency Not Defined
Reduced absorption of fat soluble vitamins and beta-carotene
Chronic malabsorption syndrome
If a meal is missed or contains no fat, dose should be omitted
Daily fat intake (30% of calories), carbohydrate, and protein should be evenly distributed over 3 main meals
Note: Multivitamin supplement (including vit A, D, E, K) is recommended
Postmarketing reports of severe liver injury with hepatocellular necrosis or acute hepatic failure with some cases resulting in liver transplant or death
History of hyperoxaluria or calcium oxalate nephrolithiasis; cases of oxalate nephrolithiasis and oxalate nephropathy with renal failure have been reported
Substantial weight loss can increase risk of cholelithiasis
Exclude organic causes of obesisty (eg, hypothyroidism), before prescribing therapy
May increase gastrointestinal events when taking a diet high on fat (>30% total daily calories from fat)
Avoid with anorexia nervosa or bulimia
Pregnancy & Lactation
Pregnancy Category: X; weight loss offers no potential benefit to a pregnant woman and may result in fetal harm; a minimum weight gain, and no weight loss, is currently recommended for all pregnant women, including those who are already overweight or obese
Lactation: Not recommended; not known if orlistat is distributed in breast milk
A:Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B:May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.
C:Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.
D:Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.
X:Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.
NA:Information not available.
Mechanism of Action
Inhibits gastric and pancreatic lipases, prevents triglyceride hydrolysis resulting in decreased absorption of dietary fats
Bioavailability: 5%; absorption is very low and systemic absorption of orlistat is not required for clinical efficacy
Onset: 24-48 hr
Duration: 48-72 hr
Peak Plasma Time: 6-8 hr
Protein Bound: 99%
Metabolized in intestinal wall
Metabolites: M1 & M3 (both probably inactive)
Half-Life: 1-2 hr
Renal Clearance: 0.1% of dose/hr
Excretion: Feces 95-97% (including biliary); urine < 3%
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