Orlistat

Generic Name: orlistat

Intestinal Lipase Inhibitor [EPC]Over-the-Counter (OTC)

Brand Names:

Xenical

11 DESCRIPTION XENICAL (orlistat) is a gastrointestinal lipase inhibitor for obesity management that acts by inhibiting the absorption of dietary fats. Orlistat is (S)-2-formylamino-4-methyl-pentanoic acid (S)-1-[[(2S, 3S)-3-hexyl-4-oxo-2-oxetanyl] methyl]-dodecyl ester. Its empirical formula is C 29 H 53 NO 5 , and its molecular weight is 495.7. It is a single diastereomeric molecule that contains four chiral centers, with a negative optical rotation in ethanol at 529 nm.

Overview

11 DESCRIPTION XENICAL (orlistat) is a gastrointestinal lipase inhibitor for obesity management that acts by inhibiting the absorption of dietary fats. Orlistat is (S)-2-formylamino-4-methyl-pentanoic acid (S)-1-[[(2S, 3S)-3-hexyl-4-oxo-2-oxetanyl] methyl]-dodecyl ester. Its empirical formula is C 29 H 53 NO 5 , and its molecular weight is 495.7. It is a single diastereomeric molecule that contains four chiral centers, with a negative optical rotation in ethanol at 529 nm.

Uses

1 INDICATIONS AND USAGE 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 for weight regain after prior weight loss. XENICAL is indicated for obese patients with an initial body mass index (BMI) ≥30 kg/m 2 or ≥27 kg/m 2 in the presence of other risk factors (e.g., hypertension, diabetes, dyslipidemia). Table 1 illustrates body mass index (BMI) according to a variety of weights and heights. The BMI is calculated by dividing weight in kilograms by height in meters squared. For example, a person who weighs 180 lbs and is 5 ' 5 " would have a BMI of 30.

Dosage

2 DOSAGE AND ADMINISTRATION One 120-mg capsule three times a day with each main meal containing fat (during or up to 1 hour after the meal). ( 2 ) Advise patients to take a nutritionally balanced, reduced-calorie diet that contains approximately 30% of calories from fat. ( 2 ) Distribute the daily intake of fat, carbohydrate, and protein over three main meals. ( 2 ) Advise patients to take a multivitamin containing fat-soluble vitamins to ensure adequate nutrition. ( 2 ) Take the vitamin supplement at least 2 hours before or after the administration of XENICAL, such as at bedtime. ( 2 ) For patients receiving both XENICAL and cyclosporine therapy, administer cyclosporine 3 hours after XENICAL.

Side Effects

6 ADVERSE REACTIONS Most common treatment emergent adverse reactions (≥5% and at least twice that of placebo) include oily spotting, flatus with discharge, fecal urgency, fatty/oily stool, oily evacuation, increased defecation and fecal incontinence. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact the Safety Call Center at 1-888-236-5445 or FDA at 1‑800‑FDA‑1088 (1-800-332-1088) or www.fda.gov/medwatch. 6.1 Clinical Trials Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in patients.

Interactions

7 DRUG INTERACTIONS Cyclosporine: Reduction in cyclosporine plasma levels was observed when XENICAL was coadministered with cyclosporine. ( 7.1 ) Fat-soluble Vitamin Supplements and Analogues: All patients should take a daily multivitamin that contains vitamins A, D, E, K, and beta-carotene. ( 7.2 ) Levothyroxine: Patients treated concomitantly with XENICAL and levothyroxine should be monitored for changes in thyroid function. ( 7.3 ) Warfarin: Patients on chronic stable doses of warfarin who are prescribed XENICAL should be monitored closely for changes in coagulation parameters. ( 7.4 ) Amiodarone: A reduction in exposure to amiodarone was observed when XENICAL was co-administered.

Warnings

5 WARNINGS AND PRECAUTIONS XENICAL has drug interactions and can decrease vitamin absorption. ( 5.1 , 7 ) Take a multivitamin supplement that contains fat-soluble vitamins to ensure adequate nutrition. ( 5.1 ) Rare cases of severe liver injury with hepatocellular necrosis or acute hepatic failure have been reported. ( 5.2 ) Patients may develop oxalate nephrolithiasis and oxalate nephropathy following treatment with XENICAL. Monitor renal function in patients at risk for renal insufficiency. Discontinue XENICAL if oxalate nephropathy develops. ( 5.3 ) Substantial weight loss can increase the risk of cholelithiasis. ( 5.4 ) Exclude organic causes of obesity (eg, hypothyroidism) before prescribing XENICAL. 4 CONTRAINDICATIONS XENICAL is contraindicated in: Pregnancy [see Use in Specific Populations (8.1) ] Patients with chronic malabsorption syndrome Patients with cholestasis Patients with known hypersensitivity to XENICAL or to any component of this product Pregnancy ( 4 , 8.1 ) Chronic malabsorption syndrome ( 4 ) Cholestasis ( 4 ) Known hypersensitivity to XENICAL or to any component of this prod...

Pregnancy

8.1 Pregnancy Pregnancy Category X XENICAL is contraindicated during pregnancy, because 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, due to the obligatory weight gain that occurs in maternal tissues during pregnancy. No embryotoxicity or teratogenicity was seen in animals that received orlistat at doses much higher than the recommended human dose.

Storage

Storage and Handling Store at 25°C (77°F); excursions permitted to 15° to 30°C (59° to 86°F) [see USP Controlled Room Temperature]. Keep bottle tightly closed. XENICAL should not be used after the given expiration date.

Frequently Asked Questions

What is Orlistat used for?

1 INDICATIONS AND USAGE 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 for weight regain after prior weight loss. XENICAL is indicated for obese patients with an initial body mass index (BMI) ≥30 kg/m 2 or ≥27 kg/m 2 in the presence of other risk factors (e.g., hypertension, diabetes, dyslipidemia). Table 1 illustrates body mass index (BMI) according to a variety of weights and heights. The BMI is calculated by dividing weight in kilograms by height in meters squared. For example, a person who weighs 180 lbs and is 5 ' 5 " would have a BMI of 30.

What are the side effects of Orlistat?

6 ADVERSE REACTIONS Most common treatment emergent adverse reactions (≥5% and at least twice that of placebo) include oily spotting, flatus with discharge, fecal urgency, fatty/oily stool, oily evacuation, increased defecation and fecal incontinence. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact the Safety Call Center at 1-888-236-5445 or FDA at 1‑800‑FDA‑1088 (1-800-332-1088) or www.fda.gov/medwatch. 6.1 Clinical Trials Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in patients.

Can I take Orlistat during pregnancy?

8.1 Pregnancy Pregnancy Category X XENICAL is contraindicated during pregnancy, because 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, due to the obligatory weight gain that occurs in maternal tissues during pregnancy. No embryotoxicity or teratogenicity was seen in animals that received orlistat at doses much higher than the recommended human dose.

What are the important warnings for Orlistat?

5 WARNINGS AND PRECAUTIONS XENICAL has drug interactions and can decrease vitamin absorption. ( 5.1 , 7 ) Take a multivitamin supplement that contains fat-soluble vitamins to ensure adequate nutrition. ( 5.1 ) Rare cases of severe liver injury with hepatocellular necrosis or acute hepatic failure have been reported. ( 5.2 ) Patients may develop oxalate nephrolithiasis and oxalate nephropathy following treatment with XENICAL. Monitor renal function in patients at risk for renal insufficiency. Discontinue XENICAL if oxalate nephropathy develops. ( 5.3 ) Substantial weight loss can increase the risk of cholelithiasis. ( 5.4 ) Exclude organic causes of obesity (eg, hypothyroidism) before prescribing XENICAL. 4 CONTRAINDICATIONS XENICAL is contraindicated in: Pregnancy [see Use in Specific Populations (8.1) ] Patients with chronic malabsorption syndrome Patients with cholestasis Patients with known hypersensitivity to XENICAL or to any component of this product Pregnancy ( 4 , 8.1 ) Chronic malabsorption syndrome ( 4 ) Cholestasis ( 4 ) Known hypersensitivity to XENICAL or to any component of this prod...

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Medical Disclaimer

This drug information is for educational purposes only and should not replace professional medical advice. Drug information is sourced from the FDA National Drug Code Directory and Structured Product Labeling. Always consult with a healthcare provider before starting, stopping, or changing any medication.