Drug information of orlistat

Mechanism of effect

A reversible inhibitor of gastric and pancreatic lipases, thus inhibiting absorption of dietary fats by 30%.

Pharmacodynamic

Orlistat is a lipase inhibitor for obesity management that acts by inhibiting the absorption of dietary fats

Pharmacokinetics

Absorption:
Minimal. Metabolized within the gastrointestinal wall; forms inactive metabolites.
Excretion:Feces (~97%, 83% as unchanged drug); urine (<2%).
Half-Life Elimination:1-2 hours. Protein Binding:>99% (lipoproteins and albumin).

Drug indications

Obesity management

Dosage

Usual Adult Dose for Obesity
120 mg orally three times a day with each main meal containing fat. The dose may be taken during the meal or within 1 hour of completing the meal.
Usual Pediatric Dose for Obesity
12 years or older:
120 mg orally three times a day with each main meal containing fat. The dose may be taken during the meal or within 1 hour of completing the meal.

Drug contraindications

Pregnancy , hypersensitivity to drug or its components. , chronic malabsorption syndrome , cholestasis

Side effects

Headache , fatigue , Urinary tract infection , edema , myalgia , anxiety , Otitis media , back pain , Upper respiratory tract infection , vaginitis

Interactions

Ethosuximide , Cod liver oil , Cyclosporine , Propafenone , Tenofovir , Levothyroxine , Warfarin , Vitamin D3 , Calcipotriol , Calcitriol , Vitamin A , Vitamin E , Vitamin K1 , saquinavir , Phenindione , Felbamate , Isoetarine , Doravirine , raltegravir , Paricalcitol , Entecavir , rilpivirine , Remdesivir , Bictegravir , ethotoin

Alerts

1-Orlistat is indicated for obese patients with an initial body mass index of ≥30 kg/m2 or ≥27 kg/m2 in the presence of other risk factors (eg, hypertension, diabetes, dyslipidemia)
2-Administer cyclosporine 3 hours after orlistat.
3- Administer levothyroxine and orlistat at least 4 hours apart and monitor for changes in thyroid function.

Points of recommendation

1-Administer during or up to 1 hour after each main meal containing fat; separate dose by at least 2 hours from multivitamin daily supplement. Omit dose if a meal is missed or contains no fat.
2-BMI; diet (calorie and fat intake); serum glucose in patients with diabetes; thyroid function in patient with thyroid disease; liver function tests in patients exhibiting symptoms of hepatic impairment; renal function in patients at risk for renal impairment

Pregnancy level

X