Alli (orlistat)
Last reviewed · Source: First Databank (FDB) drug data
Overview
Orlistat, a reversible inhibitor of gastric and pancreatic lipases, exhibits antiobesity and antilipemic activity.
Orlistat, a reversible inhibitor of gastric and pancreatic lipases, exhibits antiobesity and antilipemic activity. The drug also inhibits certain other (e.g., microbial, carboxylester (for hydrolysis of vitamin esters)) lipases. Orlistat is a synthetic derivative of naturally occurring lipstatin.
Unlike most other currently available antiobesity agents, orlistat does not exert anorexigenic (appetite suppressant) effects. Instead, orlistat exerts its antiobesity effect by decreasing the absorption of dietary fats (triacylglycerols) in the gastric and intestinal lumen via inhibition of triglyceride hydrolysis; at recommended dosages, approximately one-fourth to one-third of dietary fat will not be absorbed. By preventing triglyceride hydrolysis, the drug decreases intestinal concentrations of absorbable free fatty acids and monoglycerides.
Effects of orlistat on serum lipoproteins include decreased concentrations of LDL and total cholesterol; effects on serum triglyceride concentrations are variable, despite reductions in postprandial serum concentrations, as are those on HDL cholesterol. In obese patients, with or without diagnosed diabetes mellitus, improved glucose tolerance and glycemic control can occur. Short-term orlistat use does not affect gallbladder motility or bile composition or lithogenicity in obese or normal-weight individuals; whether long-term therapy reduces the risk of gallstones is unknown.
Orlistat works locally within the GI tract. Following oral administration, systemic exposure to orlistat is minimal. In vitro, orlistat was more than 99% bound to plasma proteins, mainly lipoproteins and albumin.
The drug is metabolized to clinically unimportant metabolites, mainly M1 and M3. Limited data suggest that the elimination half-life of absorbed orlistat ranges from 1-2 hours. Fecal excretion of unabsorbed drug is the major route of elimination.
USES: This medication is used with a doctor-approved exercise, behavior change, and reduced-calorie diet program to help you lose weight. It is used by certain overweight people, such as those who are obese or have weight-related medical problems. Taking orlistat can also help keep you from gaining back weight you have lost.
Losing weight and keeping it off can lessen the many health risks that come with obesity, including heart disease, diabetes, high blood pressure, and a shorter life. Dietary fats need to be broken down into smaller pieces before the body can absorb them. Orlistat works by blocking the enzyme that breaks down fats in your diet.
This undigested fat then passes out of your body in your bowel movement. Orlistat does not block the absorption of calories from sugar and other non-fat foods, so you still need to restrict your total intake of calories.
Generic name: orlistat
Pronunciation: (OR-li-stat)
Reference product & biosimilars
No reference, biosimilar or interchangeable associated with this drug.
Today’s intelligence on Alli
Indications
The following indications are listed for Alli:
- Weight Loss Management For Overweight Or Obese Patient (Body Mass Index 27 Or Greater)
Dosing
The recommended dosage of prescription orlistat (e.g., Xenical(R)) for the management of obesity and weight regain in adults and adolescents 12 years of age and older is 120 mg 3 times daily with each main meal containing fat. Patients should be on a nutritionally balanced, reduced-calorie diet that contains approximately 30% of calories from fat. Daily intake of fat, carbohydrate, and protein should be distributed over 3 main meals. If a meal occasionally is missed or contains no fat, the dose of orlistat may be omitted. Dosages exceeding 120 mg 3 times daily have not been shown to provide additional benefit.
For self-medication for weight loss, the usual dosage of orlistat (Alli(R)) in overweight adults 18 years of age and older is 60 mg 3 times daily with each meal containing fat. If a meal occasionally is missed or contains no fat, the dose of orlistat may be omitted. Dosage for self-medication should not exceed three 60-mg capsules daily.
Orlistat is administered orally 3 times daily, during (or up to 1 hour after) each main meal containing fat. However, administering the drug up to 2 hours after midmeal does not appear to affect efficacy.
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No dosing information is available for this tab.
Drug interactions
There is no enhanced messaging for this drug.
There are no contraindication interactions for this drug.
There are no severe interactions for this drug.
There are no moderate interactions for this drug.
Contraindications
Orlistat is contraindicated in women who are pregnant. (See Pregnancy under Warnings/Precautions: Specific Populations, in Cautions.)
Patients with chronic malabsorption syndrome.
Patients with cholestasis.
Patients with known hypersensitivity to orlistat or any ingredient in the formulations. (See Sensitivity Reactions under Cautions: Warnings/Precautions.)
There are no contraindication contraindications for this drug.
There are no severe contraindications for this drug.
There are no moderate contraindications for this drug.
Adverse reactions
Adverse effects of orlistat occurring in 5% or more of patients and with an incidence at least twice that of placebo include oily spotting, flatus with discharge, fecal urgency, fatty/oily stool, oily evacuation, increased defecation, and fecal incontinence. Such effects usually develop within 3 months of starting therapy and persist for less than one to no more than 4 weeks; occasionally adverse GI effects may occur over a 6-month period or longer. In controlled clinical trials that evaluated orlistat 120 mg three times daily, 8.8% of patients discontinued orlistat because of adverse effects, compared with 5% for placebo. In trials that evaluated orlistat 60 mg three times daily, 3.2% of patients discontinued orlistat because of adverse effects. The most common adverse effects resulting in discontinuance were GI effects.
In clinical studies, adverse effects reported in individuals receiving orlistat 60 mg 3 times daily were similar to those reported in patients receiving 120 mg 3 times daily, and were primarily GI related.
Adverse effects reported in the long-term 4-year study were similar to those reported for the 1- and 2-year studies; the total incidence of GI effects decreased each year over the 4-year study period.
There are no severe adverse reactions for this drug.
There are no less severe adverse reactions for this drug.
Precautions
No enhanced messaging available.
Safety and efficacy of prescription orlistat (Xenical(R)) in children younger than 12 years of age have not been established.
Use of orlistat in obese adolescents 12-16 years of age is supported by safety and efficacy data from studies in obese adolescents, evidence from well-controlled studies in adults, and a 21-day mineral balance study in obese adolescents.
The effects of orlistat (120 mg 3 times daily) on body mass index (BMI) and weight loss have been evaluated in a 54-week, double-blind, placebo-controlled trial in 539 obese adolescents (BMI 2 kg/m2 above 95% percentile based on age and gender) 12-16 years of age. All participants received behavioral therapy and were offered exercise counseling, were instructed to consume a reduced-calorie diet intended to provide 30% of calories from fat, and to take a multivitamin containing fat-soluble vitamins (A, D, E, and K) at least 2 hours before or after orlistat ingestion. After 1 year of treatment, BMI decreased by an average of 0.55 kg/m2 in orlistat-treated patients and increased an average of 0.31 kg/m2 in placebo recipients. More orlistat-treated patients than placebo-treated patients lost at least 5 and 10% of baseline BMI (26.5 versus 15.7%, respectively; 13.3 versus 4.5%, respectively). Additionally, 19% of orlistat-treated patients versus 11.7% of placebo recipients lost at least 5% of baseline weight, with 9.5% of orlistat-treated patients versus 3.3% of placebo recipients achieving at least a 10% weight loss. Adverse effects of orlistat in adolescent patients were similar to those observed in adults.
Administration of orlistat (120 mg 3 times daily) did not result in clinically important changes in calcium, magnesium, phosphorus, zinc, or copper balance in a 21-day study in obese adolescents 12-16 years of age. A decrease in iron balance was observed in orlistat-treated patients and placebo recipients (64.7 versus 40.4 mcmol/24 hours, respectively).
Plasma concentrations of orlistat and its metabolites M1 and M3 in adolescents were similar to those observed in adults receiving an equivalent dosage. Daily fecal fat excretion was 27% of dietary intake in orlistat-treated pediatric patients compared with 7% in those receiving placebo.
Orlistat should not be used for self-medication in children younger than 18 years of age.
Category X. (See Users Guide.)
Orlistat is contraindicated during pregnancy because weight loss offers no potential benefit to a pregnant woman and may result in fetal harm. Because of the obligatory weight gain that occurs in maternal tissues during pregnancy, a minimum weight gain and no weight loss is currently recommended for all pregnant women, including those who are already overweight or obese.
Embryotoxicity and teratogenicity have not been observed in animals at dosages substantially higher than the recommended human dosage. If orlistat is used during pregnancy or if the patient becomes pregnant while receiving the drug, the patient should be apprised of the potential hazard of maternal weight loss to the fetus.
It is not known if orlistat is distributed in breast milk; therefore, the drug should be used with caution in nursing women.
Clinical trial experience with orlistat in geriatric patients 65 years of age and older is insufficient to determine whether they respond differently than younger adults.
The pharmacokinetics of orlistat have not been specifically studied in geriatric patients to date.
ICD codes
No ICD codes are available for this drug.
Formulary status
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Last reviewed · Source: First Databank (FDB) drug data
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