orlistat (Rx, OTC)

Brand and Other Names:Alli, Xenical
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Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

capsule

  • 60mg (Alli)
  • 120mg (Xenical)
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Obesity Management

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)

Rx (Xenical): 120 mg PO q8hr with each fat-containing meal (during or up to 1 hr after the meal), doses >120 mg TID show 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

Also see Administration and Cautions (drug interaction overview)

Dosage Forms & Strengths

capsule

  • 60mg
  • 120mg
more...

Obesity Management

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)

<12 years: Safety and efficacy not established

≥12 years

  • Rx (Xenical): 120 mg PO q8hr with each fat-containing meal (during or up to 1 hr after the meal), doses >120 mg TID show 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
  • Also see Administration and Cautions (drug interaction overview)
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Interactions

Interaction Checker

and orlistat

No Results

     activity indicator 
    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

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            Adverse Effects

            1-10%

            Oily spotting (5%)

            Frequency Not Defined

            Flatulence

            Fatty/oily stool

            Increased defecation

            Fecal incontinence

            Nausea

            Vomiting

            Reduced absorption of fat soluble vitamins and beta-carotene

            Liver failure

            Oxalate nephropathy

            Leukocytoclastic vasculitis

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            Warnings

            Contraindications

            Pregnancy

            Chronic malabsorption syndrome

            Cholestasis

            Hypersensitivity

            Cautions

            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)

            Diabetes mellitus

            Avoid with anorexia nervosa or bulimia

            Drug interaction overview

            • Cyclosporine: Administer cyclosporine 3 hr after orlistat
            • Levothyroxine: Administer 4 hr apart; monitored for changes in thyroid function
            • Amiodarone PO: A pharmacokinetic study showed reduced amiodarone and desethylamiodarone systemic exposure when coadministered with orlistat
            • Antiepileptic drugs (AEDs): Convulsions reported with coadministration of AEDs and orlistat; monitor serum AED levels
            • Antiretroviral drugs: Loss of virological control has been reported in HIV-infected patients taking orlistat concomitantly with antiretroviral drugs; HIV RNA levels should be frequently monitored in patients taking orlistat and antiretrovirals drugs; if HIV viral load increases, discontinue orlistat
            • Warfarin
              • Vitamin K absorption may be decreased with orlistat
              • Reports of decreased prothrombin, increased INR, and unbalanced anticoagulant treatment resulting in change of hemostatic parameters have been with coadministration of orlistat and anticoagulants
              • Patients on chronic stable doses of warfarin or other anticoagulants who are prescribed orlistat should be monitored closely for coagulation parameters changes
            • Vitamin supplements
              • Orlistat may reduce absorption of some fat-soluble vitamins and beta-carotene
              • Instruct patient to take a multivitamin containing fat-soluble vitamins to ensure adequate nutrition
              • Take vitamin supplement at least 2 hr before or after taking orlistat, such as at bedtime
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            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

            Pregnancy Categories

            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.

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            Pharmacology

            Mechanism of Action

            Inhibits gastric and pancreatic lipases, prevents triglyceride hydrolysis resulting in decreased absorption of dietary fats

            Absorption

            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

            Distribution

            Protein Bound: 99%

            Metabolism

            Metabolized in intestinal wall

            Metabolites: M1 & M3 (both probably inactive)

            Elimination

            Half-Life: 1-2 hr

            Renal Clearance: 0.1% of dose/hr

            Excretion: Feces 95-97% (including biliary); urine < 3%

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            Administration

            Oral Administration

            Take with each fat-containing meal (during or up to 1 hr after the meal)

            The patient should be on a nutritionally balanced, reduced-calorie diet that contains ~30% of calories from fat

            Daily intake of fat, carbohydrate, and protein should be distributed over 3 main meals

            If a meal is occasionally missed or contains no fat, omit the orlistat dose

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            Images

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            Formulary

            FormularyPatient Discounts

            Adding plans allows you to compare formulary status to other drugs in the same class.

            To view formulary information first create a list of plans. Your list will be saved and can be edited at any time.

            Adding plans allows you to:

            • View the formulary and any restrictions for each plan.
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            • Compare formulary status to other drugs in the same class.
            • Access your plan list on any device – mobile or desktop.

            The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

            Tier Description
            1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
            2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
            3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
            4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            NC NOT COVERED – Drugs that are not covered by the plan.
            Code Definition
            PA Prior Authorization
            Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
            QL Quantity Limits
            Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
            ST Step Therapy
            Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
            OR Other Restrictions
            Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
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            Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.