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Orlistat Capsules

Capitalizing on our strong medical experience, we bring forth with 120 mg. It is used to reduce the weight as its functions to block the fat available in our routine diet. Its formulation is done to treat the obesity problems. It is a saturated derivative of lipstatin and is a natural inhibitor of pancreatic lipases. Orlistat is clinically tested and is offered in capsules

Remedy:	Treatment of obesity
Composition:	Each hard gelatin capsule contains: orlistat 120 mg, excipients Q S, approved colour used in empty capsule shells
Therapeutic group:	Peripherally acting antiobesity agent, ATC CODE: A08AB01
Mechanism of action:	Orlistat is a reversible inhibitor of lipases. It exerts its therapeutic activity in the lumen of the stomach and small intestine by forming a covalent bond with the active serine residue site of gastric and pancreatic lipases. The inactivated enzymes are thus unavailable to hydrolyze dietary fat in the form of triglycerides into absorbable free fatty acids and monoglycerides. As undigested triglycerides are not absorbed, the resulting caloric deficit may have a positive effect on weight control. Systemic absorption of the drug is therefore not needed for activity.
Pharmacokinetic properties:	Absorption: Studies in normal weight and obese volunteers have shown that the extent of absorption of orlistat was minimal. Plasma concentrations of intact orlistat were non-measurable (< 5ng/mL) eight hours following oral administration of orlistat. In general, at therapeutic doses, detection of intact orlistat in plasma was sporadic and concentrations were extremely low (< 10ng/mL or 0.02μmol), with no evidence of accumulation, which is consistent with minimal absorption. Distribution: The volume of distribution cannot be determined because the drug is minimally absorbed and has no defined systemic pharmacokinetics. In vitro orlistat is > 99% bound to plasma proteins (lipoproteins and albumin were the major binding proteins). Orlistat minimally partitions into erythrocytes Metabolism: Based on animal data, it is likely that the metabolism of orlistat occurs mainly within the gastrointestinal wall. Based on a study in obese patients, of the minimal fraction of the dose that was absorbed systemically, two major metabolites, M1 (4-member lactone ring hydrolysed) and M3 (M1 with N-formyl leucine moiety cleaved), accounted for approximately 42% of the total plasma concentration. M1 and M3 have an open beta-lactone ring and extremely weak lipase inhibitory activity (1000 and 2500 fold less than orlistat respectively). In view of this low inhibitory activity and the low plasma levels at therapeutic doses (average of 26ng/mL and 108ng/mL respectively), these metabolites are considered to be pharmacologically inconsequential. Elimination: Studies in normal weight and obese subjects have shown that faecal excretion of the unabsorbed drug was the major route of elimination. Approximately 97% of the administered dose was excreted in faeces and 83% of that as unchanged orlistat. The cumulative renal excretion of total orlistat-related materials was < 2% of the given dose. The time to reach complete excretion (faecal plus urinary) was 3 to 5 days. The disposition of orlistat appeared to be similar between normal weight and obese volunteers. Orlistat, M1 and M3 are all subject to biliary excretion.

Therapeutic indications:
Orlistat is indicated:	In conjunction with a mildly hypocaloric diet for the treatment of obese patients with a body mass index (BMI) greater or equal to 30 kg/m², or overweight patients (BMI > 28 kg/m²) with associated risk factors. For the treatment of obesity to inhibits absorption of dietary fats in stomach and small intestine To reduce risk of regaining after weight loss For treatment of obese patients who are obese with a body mass index (a measure of obesity) of more than 30 kg/m2.
Posology and method of administration	The recommended dose is one capsule (120 mg) three times daily. Orlistat should be taken one hour after or during a meal containing about 15 mg of fat. Meals without fat do not require orlistat. Patients should eat a nutritionally balanced, reduced calorie diet that contains approximately 30% of calories from fat.
Side effects:	The primary side effects of the drug are gastrointestinal-related and include steatorrhea (oily, loose stools with excessive flatus due to unabsorbed fats reaching the large intestine), fecal incontinence and frequent or urgent bowel movements.
Composition:	Orlistat is contraindicated in:malabsorption, hypersensitivity to orlistat, reduced gallbladder function (e.g. after cholecystectomy), pregnancy and breastfeeding Use with caution:obstructed bile duct, impaired liver function and pancreatic disease.
Warning & precautions:	Caution should be exercised in patients with history of gallbladder, liver, pancreas or thyroid problems, sugar, kidney stones, received an organ transplant, any allergy, who is taking other medications, during pregnancy and breast feeding. It should not be used in children. Follow proper diet and exercise program as directed by your physician. It may affect blood sugar level; monitoring of sugar level regularly is recommended while taking this medication. Absorption of fat-soluble vitamins and other fat-soluble nutrients is inhibited by the use of orlistat. A multivitamin tablet containing vitamins A, D, E, K and beta-carotene should be taken once a day, at bedtime, when using orlista
Drug interactions:	Orlistat may reduce plasma levels of ciclosporin (cyclosporin), therefore, the two drugs should not be administered concomitantly. Cyclosporine should be administered two hours before or after orlistat. Orlistat can impair absorption of the antiarrhythmic amiodarone. The blood thinning effect of warfarin (Coumadin) depends on the amount of vitamin K in the body and vitamin K is one of the vitamins that bind to fat. Patients receiving warfarin who begin orlistat should have their blood clotting monitored closely because orlistat may cause levels of vitamin K to decline. This will increase the effects of warfarin and lead to abnormal bleeding from the warfarin. The evidence for deficiency of vitamin K in patients who are taking orlistat is not noted yet. Hypothyroidism may occur when orlistat and levothyroxine (synthroid, levoxyl, levothroid, unithroid) are combined. Patients treated with both orlistat and levothyroxine should be monitored for changes in thyroid function. The orlistat and levothyroxine should be taken at least four hours apart. Fat-soluble vitamin supplements and analogues:Upto 30% reduction in beta-carotene supplement absorption may occur when concomitantly administered with orlistat. Orlistat may inhibit absorption of a vitamin E acetate supplement by approximately 60%. The effect of orlistat on the absorption of supplemental vitamin D, vitamin A and nutritionally-derived vitamin K is not known yet. Orlistat do not alter the pharmacokinetics or pharmacodynamics of glyburide, digoxin, phenytoin, pravastatin.
Oral Contraceptives:	The treatment of orlistat 120 mg three times a day does not change the ovulation-suppressing action of oral contraceptives.
Storage:	Do not store above 25℃. Store in original package in order to protect from moisture. Keep the container tightly closed in order to protect from moisture.
Packaging:	10 capsules packed in alu-alu blister in a printed carton.

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