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Orlistat Orlipastat 96829-58-2 obesity type 2 diabetes weight loss
Alias:N-Formyl-L-leucine (1S)-1-[[(2S,3S)-3-hexyl-4-oxo-2-oxetanyl]methyl]dodecyl ester;(-)-Tetrahydrolipstatin
Orlistat is used for the treatment of obesity. The amount of weight loss achieved with orlistat varies. In one-year clinical trials, between 35.5% and 54.8% of subjects achieved a 5% or greater decrease in body mass, although not all of this mass was necessarily fat. Between 16.4% and 24.8% achieved at least a 10% decrease in body fat. After orlistat was stopped, a significant number of subjects regained weight-up to 35% of the weight they had lost.
The incidence of type 2 diabetes in an obese population over four years is decreased with orlistat (6.2%) compared to placebo (9.0%).Long-term use of orlistat also leads to a modest reduction in blood pressure (mean reductions of 2.5 and 1.9 mmHg in systolic and diastolic blood pressure respectively).
|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|
Orlistat is currently internationally recognized as a new type of weight loss lipid-lowering drugs with the marketed product being under the name of Xenical. It was first listed in New Zealand in 1998 with annual sale of $ 146 million at that time. In 2007, the sale reaches $ 538 million, Orlistat occupy 80% of the market share of the global weight-loss market with the annual sale of only China Hong Kong year reaching 80 million US dollars.
Orlistat is a long-acting and potent specific inhibitor of gastrointestinal tract lipase, appearing as white or white-like powder at room temperature and being insoluble in water, soluble in chloroform and easily soluble in ethanol. It 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. Fat in food can’t be broken down into free fatty acids and monoacylglycerols so that the fat can’t be absorbed and utilized, thereby having reduced the body's calorie intake to control the body weight.
The drug does not need to be absorbed through the body. At normal doses, the absorption of fat can be inhibited by 30%. There is little absorption after oral administration. It can be subject to metabolic inactivation in the intestine with the metabolic sites located in the gastrointestinal wall. The elimination half-life is about 14 to 19 hours. About 97% of the goods are excreted with the feces, of which 83% are in the prototype.
Clinically orlistat can be applied to the treatment of obesity and hyperlipidemia. Under normal circumstances, it can be subject to oral administration at a dose of 120 mg for three times per day. Take it during the meal or 1 hour after a meal. After 2 weeks of administration, the body weight can begin to decline. It can be taken continuously for 6 to 12 months. If the dose is increased to above 400 mg daily, the effect will no longer be further enhanced.
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.