How to take Orlistat

Orlistat (also known as tetrahydrolipstatin) is a drug designed to treat obesity. It is marketed as a prescription under the trade name Xenical by Roche in most countries, and is sold over-the-counter as Alli by GlaxoSmithKline in the United Kingdom and the United States. Its primary function is preventing the absorption of fats from the human diet by acting as a lipase inhibitor, thereby reducing caloric intake. It is intended for use in conjunction with a healthcare provider-supervised reduced-calorie diet.

Orlistat (prescription and nonprescription) is used with an individualized low-calorie, low-fat diet and exercise program to help people lose weight. Prescription Orlistat(CAS NO:96829-58-2) is used in overweight people who may also have high blood pressure, diabetes, high cholesterol, or heart disease. It is also used after weight-loss to help people keep from gaining back that weight. It is in a class of medications called lipase inhibitors. It works by preventing some of the fat in foods eaten from being absorbed in the intestines. This unabsorbed fat is then removed from the body in the stool.

Orlistat comes as a capsule and a nonprescription capsule to take by mouth. It is usually taken three times a day with each main meal that contains fat. Take this medicine during a meal or up to 1 hour after a meal. If a meal is missed or does not have fat, you may skip your dose. Follow the directions on your prescription label or the package label carefully, and ask your doctor or pharmacist to explain any part you do not understand. Take this medicine exactly as directed. Do not take more or less of it or take it more often than prescribed by your doctor or stated on the package.

Orlistat works by inhibiting gastric and pancreatic lipases, the enzymes that break down triglycerides in the intestine. When lipase activity is blocked, triglycerides from the diet are not hydrolyzed into absorbable free fatty acids, and are excreted undigested instead. Only trace amounts of this medicine are absorbed systemically; the primary effect is local lipase inhibition within the GI tract after an oral dose. The primary route of elimination is through the feces.

Orlistat was also recently found to inhibit the thioesterase domain of fatty acid synthase (FAS), an enzyme involved in the proliferation of cancer cells but not normal cells. However, potential side effects of this medicine, such as inhibition of other cellular off-targets or poor bioavailability, might hamper its application as an effective antitumor agent. 

One profiling study undertook a chemical proteomics approach to look for new cellular targets of Orlistat, including its off-targets. Orlistat also show potential activities mycobacteria and Trypanosoma brucei parasite (See further reading).

At the standard prescription dose of 120 mg three times daily before meals, orlistat prevents approximately 30% of dietary fat from being absorbed, and about 25% at the standard over-the-counter dose of 60 mg. Higher doses do not produce more potent effects.

Keep Orlistat in the container it came in, tightly closed, and out of reach of children. Store it at room temperature and away from excess heat, moisture (not in the bathroom), and light. Throw away any medication that is outdated or no longer needed. Talk to your pharmacist about the proper disposal of your medication.

It is important for you to keep a written list of all of the prescription and nonprescription (over-the-counter) medicines you are taking, as well as any products such as vitamins, minerals, or other dietary supplements. You should bring this list with you each time you visit a doctor or if you are admitted to a hospital. It is also important information to carry with you in case of emergencies.

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