Molecule
Orlistat
Class
GI Drugs, Miscellaneous
VA Class
GA900
Chemical Name
[2S-[2α(R*),3β]]-1-[(3-hexyl-4-oxo-2-oxetanyl)-methyl]dodecyl-N-formyl-lLeucine
Molecular Formula
C29H53O5
CAS Number
96829-58-2
Brands
Reesize 60 and 120 mg
Status
Drug. Reesize is a medication used for weight loss that contain different strengths of the same active ingredient, orlistat. Reesize 60 and 120 mg are available by prescription only.
Special Alert
Healthcare professionals should weigh the benefits of weight loss with the potential risks associated with orlistat before prescribing or recommending these medications to their patients; patients should stop use of orlistat and contact their healthcare professional if they develop any signs and symptoms of liver injury, including itching, yellow eyes or skin, dark urine, light-colored stools, or loss of appetite. The most commonly reported adverse events described in the 32 reports of serious liver injury were jaundice, weakness, and abdominal pain.
FDA Approval
FDA is reviewing data on suspected cases of liver injury submitted by the manufacturers of Orlistat. Analysis of these data is ongoing, and no definite association between liver injury and orlistat has been established at this time. FDA has not advised healthcare professionals to change their prescribing practices with orlistat. Consumers currently taking Orlistat should continue to take it as prescribed and should continue to use the product as directed.
Mechanism of Action
Reversible inhibitor of gastric and pancreatic lipases; exhibits antiobesity and antilipemic activity.
Usage of Reesize
Obesity
Adjunct to caloric restriction, increased physical activity, and behavioral modification in the treatment of exogenous obesity; also used to reduce the risk of weight regain after initial loss.
Use in patients with initial body mass index (BMI) of ≥29 kg/m2; also use in those with BMI of ≥25 kg/m2 in the presence of risk factor or disease (e.g., hypertension, diabetes mellitus, hyperlipidemia).
Reesize Administration
Administration
Reesize Oral Administration
Administer orally 3 times daily, during (or up to 1 hour after) each main meal containing fat. However, efficacy apparently not affected by administering the drug up to 2 hours after midmeal. Omit Reesize dose if a meal occasionally is missed or contains no fat.
Distribute daily fat (30% of calories), carbohydrate, and protein intake evenly over 3 main meals; administration of orlisatat with any one very high-fat meal increases potential for adverse GI effects. Manufacturer recommends use of vitamin supplement containing fat-soluble vitamins. Administer multivitamin ≥2 hours before or after Reesize; administer vitamin supplement at bedtime for convenience.
Reesize Dosage
Adults
Obesity
Oral
120 mg 3 times daily with each main meal containing fat. No additional benefit with dosages >120 mg 3 times daily.
60 mg 3 times daily with each main meal containing fat for those who need therapeutic assistance to maintain weight loss.
Reassess weight management and therapy periodically. Safety and efficacy beyond 2 years not established in clinical studies. However, if effective for weight loss or maintenance and no serious adverse effects occur, may continue orlistat as long as clinically indicated.
Cautions for Orlistat
Contraindications
Chronic malabsorption syndrome or cholestasis. Known hypersensitivity to orlistat or any ingredient in the formulation.
Warnings/Precautions
Warnings
Obesity Evaluation
Rule out organic causes of obesity (e.g., hypothyroidism) before initiating orlistat therapy.
Cyclosporine Interaction
Do not administer concomitantly with cyclosporine; administer cyclosporine 2 hours before or after orlistat. (See Specific Drugs under Interactions.)
General Precautions
Pending revision, the material in this section should be considered in light of more recently available information.
Hyperoxaluria
Possible increased concentrations of urinary oxalate. Caution in patients with a history of hyperoxaluria or calcium oxalate nephrolithiasis.
Misuse Potential
Avoid use in inappropriate patient populations (e.g., those with anorexia nervosa or bulimia).
Diabetes Mellitus
Weight loss may improve glycemic control; dose reductions or discontinuance of concomitant antidiabetic therapy (e.g., insulin, sulfonylureas, metformin) may be necessary.
Dietary Guidelines
Adherence to dietary recommendations minimizes adverse GI effects related to fat intake, as well as contributing to weight loss.
Vitamin Supplementation
Fat-soluble vitamin deficiency is unlikely but possible (see Specific Drugs under Interactions). Manufacturer considers routine (once daily) supplementation with fat-soluble vitamins (A, D, E, K) a prudent precaution (see Oral Administration under Dosage and Administration).
Specific Populations
Pregnancy
Category B; use NOT recommended.
Lactation
Not known whether orlistat is distributed into milk; use NOT recommended.
Pediatric Use
Safety and efficacy not established in children <18 years of age.
Geriatric Use
Insufficient experience in patients ≥65 years of age to determine whether geriatric patients respond differently than younger adults.
Common Adverse Effects
Oily spotting, flatus with discharge, fecal urgency, fatty/oily stool, oily evacuation, increased defecation, fecal incontinence.
Interactions for Orlistat
Specific Drugs
Orlistat Pharmacokinetics
Absorption
Bioavailability
Systemic absorption of orlistat is minimal. Reesize hardly passes beyond intestine to enter the blood stream, which is why it is claimed to have local action and is virtually free of side effects.
Distribution
Plasma Protein Binding
>99% in vitro (lipoproteins and albumin).
Metabolism
Metabolized principally in intestinal wall to clinically unimportant metabolites.
Elimination Route
Excreted principally in the feces (97%), mainly as unchanged drug (about 80%).
Stability
With prescribed storage condition stable through the shelf-life period indicated in the pack
Oral
Capsules
Actions
Decreases intestinal lumen absorption of dietary fat (triacylglycerol) by reversibly inhibiting gastric and pancreatic lipase-mediated triglyceride hydrolysis, thereby decreasing intestinal concentrations of absorbable free fatty acids and monoglycerides.
About one-third of dietary fat will not be absorbed at recommended dosages.
Decreases concentrations of LDL and total cholesterol; variable effects on serum triglycerides and HDL cholesterol.
Advice to Patients
Provide patient a copy of manufacturer’s patient information. Importance of adherence to clinician’s dietary and, if applicable, exercise recommendations (Available in the Patient Conseling Section).
Importance of distributing daily fat (30% of total daily calories), carbohydrate, and protein intake evenly over 3 main meals.
Importance of omitting orlistat dose if meal contains no fat or is skipped.
Importance of informing clinicians of any consistent problems absorbing food (chronic malabsorption), gallbladder problems, anorexia, or bulimia. Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs and dietary supplements (including herbal preparations), particularly cyclosporine.
Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed.
Importance of informing patients of other precautionary information. (See Cautions.)
Preparations
Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.
Orlistat : Routes Oral
Dosage Forms : Capsules
Strengths : 60 and 120 mg
Brand Name : Reesize
Manufacturer : Chimak
Pricing : As Indicated in the Pack
Disclaimer
This report on medications is for your information only, and is not considered individual patient advice. Because of the changing nature of drug information, please consult your physician or pharmacist about specific clinical use.
