Orlistat

Novel Weight Loss Lipid-lowering Drugs Orlistat CAS 96829-58-2

 

Quick Details for Orlistat

Product Name: Orlistat
Synonyms: (S)-2-FORMYLAMINO-4-METHYL-PENTANOIC ACID (S)-1-[[(2S,3S)-3-HEXYL-4-OXO-2-OXETANYL]METHYL]-DODECYL ESTER;RO-18-0647;(-)-TETRAHYDROLIPSTATIN;ORLISTAT;N-FORMYL-L-LEUCINE (1S)-1-[[(2S,3S)-3-HEXYL-4-OXO-2-OXETANYL]METHYL]DODECYL ESTER;XENICAL;(-)-Tetrahydrolipstatin(EquivalentToOrlistat);Orlipastat
CAS: 96829-58-2
MF: C29H53NO5
MW: 495.73
Product Categories: Pharmaceutical Raw Materials;Miscellaneous Biochemicals;API;Antiobesity Agent;Chiral Reagents;Intermediates & Fine Chemicals;Pharmaceuticals;Amino Acids & Derivatives;Heterocycles;ACTOS;Other APIs;Lipid-lowering medicine reducing weight
Melting point : <50 °C
Storage temp. : 2-8°C
Chemical Properties : Off-White Solid
Usage : An antiobesity agent. A pancreatic lipase inhibitor. Antiobesity agent.
Usage : antidiabetic
Usage : Orlistat is an antiobesity agent. Orlistat is an pancreatic lipase inhibitor.
Usage : Tetrahydrolipstatin (orlistat) is a semi-synthetic derivative of lipstatin, a metabolite isolated from Streptomyces toxytricini. Tetrahydrolipstatin acts as a potent, irreversible inhibitor of pancreatic lipase. In vivo, it blocks the absorption of triglycerides while allowing fatty acid absorption. Tetrahydrolipstatin is widely used for the treatment of obesity.

 

Orlistat Pharmacological effects

Orlistat belongs to lipase inhibitor class weight-loss drugs, which is the hydration derivatives of lipstatin, being able to reduce the absorption of food fats so that the weight will get lost. This product has a potent and selective inhibitory effect on gastric lipase and pancreatic lipase with no influence on other kinds of digestive enzymes (amylase, trypsin, and chymotrypsin) and phospholipase without affecting the absorption of carbohydrates, protein and phospholipids. The drug is not absorbed by the gastrointestinal tract with its inhibition on lipase being reversible.

Orlistat can form covalent bonds with the active serine sites of the gastric lipase and the pancreatic lipase in the stomach and small intestine cavity, resulting in inactivation of the enzymes, inhibiting the triglyceride hydrolysis so that the monoglyceride and free fatty acid intake will decrease, thereby controlling the body weight. The pharmacological activity of orlistat is dose-dependent with a therapeutic dose of orlistat (120 mg / day, taken at mealtime) in combination with a low-calorie balanced diet being capable of reducing 30% of fat absorption in the diet. Studies on normal-weight and obese volunteers have shown that orlistat is not substantially absorbed by the body and that the concentration of the drug in the plasma is very low. After oral administration of a single dose (maximal dose of 800 mg), the plasma concentration of orlistat within 8 hours is lower than 5 ng / ml.

Generally under the treatment dose, the body has a low systemic absorption of the orlistat without accumulation during short-term treatment. In vitro experiments, orlistat has an as high as over 99% binding rate to the plasma protein (lipoprotein, albumin as the major binding protein). Orlistat can rarely bind to red blood cells. Studies in obese patients show that orlistat, which is seldom absorbed, has two major metabolites in plasma, M1 (hydrolyzate of the 4-lactone ring) and M3 (M1 attached with a N-formyl-l Lysine lysis product) account for 42% of the total plasma concentration. M1 and M3 have extremely week inhibitory effect on lipase. The unabsorbed orlistat was mainly excreted from the feces, accounting for 97% of the dose taken, 83% of which were prototype drugs, and the cumulative renal excretion amount of orlistat and its metabolites was less than 2%. It needs 3 to 5 days for thorough excretion (feces and urine) of drugs. Both M1 and M3 can be excreted through bile.
This product also has an effect of regulating blood lipids: being able to reduce serum triglyceride (TG) and the low density lipoprotein cholesterol (LDL-C) and increase the proportion of high-density lipoprotein and low-density lipoprotein in the serum of obesity patients.

 

Dosage and Usage

This combination of Xenical (orlistat) with mild low-calorie diet is applicable to obese and overweight patients, including for the long-term treatment of patients who have been associated with obesity-related risk factors. This product has long-term effects of weight control (weight loss, weight maintenance and prevention of rebound). Administration of orlistat can reduce the incidence of obesity-related risk factors and other obesity-related diseases, including hypercholesterolemia and type II diabetes.

Adults: The recommended dose is taking a 120 mg capsule during meal or within one hour after meal. If a meal is not into the food or no fat, you can omit a medication. Long-term use of treatment (including weight control and risk factors for improvement) is sustainable.

The patient’s diet should be nutritionally balanced with slightly low heat. There is about 30% of heat coming from fat. The food should be rich in fruits and vegetables. The intake of fats, carbohydrates and protein should be distributed in three meals a day. There is no evidence that over three times daily /120mg per time can enhance the efficacy. No dose adjustment is required for the elderly.

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