Composition
Each capsule contains orlistat 120 mg.
Properties
Absorption of orlistat after oral administration is minimal.
99% bound to plasma proteins (lipoproteins and albumin are the major binding proteins).
Half-life of the absorbed orlistat is in the range of 1 to 2 hours.
Metabolism of orlistat occurs mainly within the gastrointestinal wall. Two metabolites, M1 (4-member lactone ring hydrolyzed) and M3 (M1 with N-formyl leucine moiety cleaved) are known.
These metabolites are considered pharmacologically inconsequential.
The primary metabolite M1 has a short half-life (approximately 3 hours) whereas the secondary metabolite M3 disappears at a slower rate (half-life approximately 13.5 hours).
Fecal excretion of the unabsorbed drug was found to be the major route of elimination
Indications
Slim-Safe® is indicated for:
- Obesity management, including weight loss, and weight maintenance, in conjunction with dietary modification.
- Reducing weight for obese diabetic subjects
Precautions
Patients should be advised to adhere to dietary guidelines. If orlistat is taken with a meal very high in fat, the possibility of gastrointestinal side effects increases.
Patients should be counseled to take a multivitamin supplement that contains fat-soluble vitamins to ensure adequate nutrition, because orlistat is shown to reduce the absorption of some fat-soluble vitamins and beta-carotene. The supplement should be taken at least 2 hours before or after an orlistat dose or at bedtime.
Caution should be exercised when prescribing orlistat to patients with a history of hyperoxaluria or calcium oxalate nephrolithiasis.
Weight-loss induction by orlistat may be accompanied by improved metabolic control in diabetics, which might require a reduction in the dose of oral hypoglycemic medication (e.g., sulfonylureas, metformin) or insulin.
Orlistat adds to the lipid-lowering effect of pravastatin.
Dosage and administration
120 mg capsule (one capsule) three times a day with each main meal containing fat (during or up to 1 hour after the meal). If a meal is occasionally missed or contains no fat, the dose of Slim-Safe® can be omitted.
Doses above 120 mg three times a day have not been shown to provide additional benefit.
Adverse effects
Gastrointestinal (GI) symptoms, including fecal urgency, flatulence, and fatty stools are the most frequently reported adverse effects. They could be minimized by limiting the amount of fat in the diet. Those side effects may last for less than 1 week, and the majority may last for not more than 4 weeks.
Upon discontinuation of therapy, fecal fat content usually returns to pretreatment levels within 48 to 72 hours.
Other side effects such as headache, fatigue, anxiety and menstrual irregularities may happen.
Pregnancy & lactation
Pregnancy: Category B.
It is not known if orlistat is secreted in human milk. Therefore, it should not be taken by lactating women.
Contraindications
Orlistat is contraindicated in patients with chronic malabsorption syndrome or cholestasis, and in patients with known hypersensitivity to the product.
How supplied
Packs of one strip, each of 10 capsules.
Keep all medicaments out of reach of children
Product of: AMOUN PHARMACEUTICAL CO. El-Obour City, Cairo, Egypt. ATC Code: A08AB01