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Product Information

  • Indications

  • Efficacy

  • Contraindications and Warnings

  • Precautions

  • Adverse Events

  • Dosage and Administration


    Indications

    XENICAL acts locally to inhibit GI lipases, blocking the absorption of approximately 30% of dietary fat. XENICAL is indicated for obesity management, including weight loss and weight maintenance, when used in conjunction with a reduced-calorie diet. XENICAL is also indicated to reduce the risk of weight regain after prior weight loss. XENICAL is indicated for obese patients with an initial BMI of >30 kg/m2 or >27 kg/m2 in the presence of other risk factors, such as type 2 diabetes, hypertension and dyslipidemia.

    How XENICAL Works
    How XENICAL Works

    How fat blocking works
    • XENICAL acts locally to inhibit the fat-digesting action of lipases in the GI tract.
    • Intact triglycerides pass through the intestines unabsorbed, creating a caloric deficit.
    • Absorption of carbohydrates and proteins is not affected.


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    Efficacy

    In clinical trials, XENICAL plus diet:
    • Provided twice the mean weight loss as placebo plus diet
    • Maintained mean weight loss better than placebo plus diet20,57
    • Improved cardiovascular and metabolic risk factors better than placebo plus diet20,28,57
    XENICAL was evaluated in seven long-term studies (1 to 2 years' duration) involving more than 4000 patients. XENICAL has proven safety and tolerability profiles.

    Year 1: Faster and greater weight loss 57

    Year 1: Faster and greater weight loss

    In one study, three times as many patients (25% on XENICAL plus diet versus 8% on placebo plus diet, P<0.001) lost>10% of their body weight from randomization (mean: 31 lbs; range: 18 to 67 lbs).18

    In five studies:
    • Two to five times as many patients on XENICAL plus diet lost >10% of their body weight from randomization versus those on placebo plus diet.
    • Pooled data showed overall mean weight loss from randomization was 13.4 lbs for XENICAL plus diet versus 5.8 lbs for placebo plus diet.
    Year 2: Significant weight loss maintained

    Year 2: Percentage of patients losing >=10% and >=5% of body weight from randomization

    In one study, almost four times as many patients on XENICAL plus diet maintained a weight loss of >10% of their body weight from randomization versus those on placebo plus diet.

    In four studies:
    • Two to five times as many patients on XENICAL plus diet maintained a weight loss of >10% of their body weight from randomization versus those on placebo plus diet.

    Dyslipidemia

    Sustained weight loss with improvement in cardiovascular risk factors


    LDL cholesterol: patients with LDL of >130 mg/dL at randomization
    • At year 1, XENICAL plus diet was more effective in reducing LDL cholesterol than placebo plus diet for any weight-loss category.
    Year 1: Mean change in LDL cholesterol in patients with LDL cholesterol >=130 mg/dL
    • At year 1, the mean change from randomization in LDL cholesterol was -7.8% for XENICAL plus diet versus +1.1% for placebo plus diet (P<0.001).15
    • For XENICAL plus diet, there was a consistent decline in LDL cholesterol for 12 weeks following randomization, an improvement that was maintained through week 52.
    • In contrast, for placebo plus diet, mean LDL cholesterol levels generally remained close to levels at randomization.
    • At year 2, the improvements seen with XENICAL plus diet were maintained (P<0.001).
    In the population as a whole, including patients with normal LDL at randomization:
    • The mean change in LDL cholesterol at year 1 was -4.0% for XENICAL plus diet and +5.0% for placebo plus diet (P<0.001).
    The long-term effects of orlistat on morbidity and mortality associated with obesity have not been established.

    Hypertension

    XENICAL plus diet improved both systolic and diastolic blood pressures versus placebo plus diet.

    Year 1: Mean change from randomization in patients with abnormal blood pressure

    The long-term effects of orlistat on morbidity and mortality associated with obesity have not been established.

    Type 2 Diabetes

    Efficacy and safety demonstrated in a 1-year study of obese type 2 diabetics on sulfonylureas (n=321) 28

    Improved Glycemic Control -Year 1: Mean changes from randomization in sulfonylurea usage in type 2 diabetes patients

    Significantly more patients on XENICAL plus diet reduced or discontinued sulfonylurea usage versus those on placebo plus diet (43.2% vs. 28.9%, P<0.05), with significantly greater reductions in mean dosage (P<0.05).

    Decrease in HbA1c in patients with HbA1c greater than 8%

    The long-term effects of orlistat on morbidity and mortality associated with obesity have not been established.

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    Contraindications and Warnings
    • XENICAL is contraindicated in patients with chronic malabsorption syndrome or cholestasis (impaired bile flow), and in patients with known hypersensitivity to XENICAL or to any component of this product.
    • Organic causes of obesity, such as hypothyroidism, should be excluded before prescribing XENICAL.
    • To reduce the chance of drug-drug interaction resulting in reduced levels of cyclosporine, XENICAL and cyclosporine should not be taken within 2 hours of each other. More-frequent monitoring of cyclosporine levels should be considered in patients taking both drugs.

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    Precautions

    Fat-Soluble Vitamins

    When taking XENICAL, patients should be advised to take a multivitamin supplement containing fat-soluble vitamins to ensure adequate nutrition, because XENICAL has been shown to reduce the absorption of some fat-soluble vitamins, including beta-carotene, and because the status of obese patients in general and patients on weight-control diets may be low. The supplement should be taken once a day at least 2 hours before or after administration of XENICAL, such as bedtime.

    Toxicology

    No evidence of bacterial or mammalian mutagenicity, unscheduled DNA synthesis, chromosome aberrations or mouse micronuclei was seen in bacterial and animal studies. No evidence of carcinogenicity existed in animals with systemic exposure to orlistat many times higher than that used in human studies.

    Inappropriate Use

    As with any weight-loss agent, the potential exists for misuse of XENICAL in inappropriate patient populations (e.g., patients with anorexia nervosa or bulimia). See recommended prescribing guidelines for more detail.

    Pregnancy Category B

    XENICAL is not recommended for use during pregnancy.

    Nursing Mothers

    XENICAL should not be taken by nursing mothers.

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    Adverse Events

    Gastrointestinal symptoms are the most commonly observed (incidence of 5% of more, and twice that of placebo) adverse events associated with the use of XENICAL in the double-blind, placebo-controlled clinical trials, and are primarily a manifestation of the mechanism of action. The most common of these adverse events were oily spotting, flatus with discharge, fecal urgency, fatty/oily stool, oily evacuation, increased defecation and fecal incontinence.

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    Dosage and Administration
    • The recommended dose of XENICAL is one 120-mg capsule 3 times a day, once with each main meal containing fat (during or up to 1 hour after the meal).
    • The patient should be on a nutritionally balanced, reduced-calorie diet that contains approximately 30% of calories from fat. The daily intake of fat, carbohydrate and protein should be distributed over three main meals. If a meal is occasionally missed or contains no fat, the dose of XENICAL can be omitted.
    • Doses above 120 mg 3 times a day have not been shown to provide additional benefit.
    • The safety and effectiveness of XENICAL beyond 2 years have not been determined at this time.

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    Mechanism of Action

    Physicians' FAQ

    Managing Patients with Obesity-Related Comorbidities