Orlistat - Xenical
25 Oct 2016
Orlistat (Xenical) is a medicine, a specific inhibitor of gastrointestinal lipases which carry out digestion of fats. "Xenical", Roche (company) and Orsoten is most known under trade names. It is used, including and as an agent for weight reduction.
The mechanism of action
Drug possesses a high lipofilnost and is admixed with fat drops. Orlistat is covalently bound to the active center of pancreatic and gastric lipases, thereby inactivating them. In view of inhibition digestive lipases triglycerides can't get into a blood. At the same time deficiency of energy is framed that leads to mobilization of fat from depot. Under the influence of Xenical the mass of vistsero-abdominal fat decreases generally. Also orlistat promotes depression of a hypercholesterinemia – in view of depression of quantity free fat acids and monoglycerides in an intestine lumen – solubility of a cholesterin decreases that reduces its ability to get into a blood. Owing to normalization of lipide structure of a blood sensitivity of tissues to insulin increases, the hyperinsulinemia decreases that also promotes decrease of mass of vistsero-abdominal fat. Pay attention to Mildronate, active components Meldonium.
Researches
According to multicenter the placebo-controlled of researches, in 52 weeks of use of Xenical in standard doses body weight decreased by 6,2% from initial, the level of insulin decreased by 18%.
At 60% of patients with an obesity orlistat lost weight more than for 10%, authentically reduced waist volume. Reliable decrease of body weight was reached as at patients with the normal state of carbohydrate metabolism, and at patients with a diabetes mellitus 2 types. Orlistat confirmed the high efficiency and safety in a large amount of randomized placebos - controlled researches, the most long of which was a research XENDOS (4 years of continuous treatment with Xenical).
When carrying out the 3rd phase of clinical tests of an orlistat it is established that it reduces the level of triglycerides, the general cholesterin, lipoproteins of low density, glycated hemoglobin, reduces arterial pressure.
Use for weight loss
Xenical is prescribed on 120 mg by 3 times a day during food or during 1 h after meal.
Side effect
From digestive tract:
- defecation acceleration - 20,4%
- oily allocations from an anus – 17,5%
- meteorism – 23,9%
- incontience of a feces of 7,7%
Side effects from a GIT are caused by the high content of fat in a nutrition. On statistical data, from – for this side effects stop administration of drug of 8,8% of patients. For prophylaxis of emergence of these phenomena it is necessary to adhere to the moderate hypohigh-calorie diet containing no more than 30% of fat (from the general daily calorage). At the same time these side effects aren't observed. Also within the first 1-4 weeks of administration of drug side effects from a nervous system are observed:
- headache – 30%
- giddiness – 5%
- sleep disorder - 3,9%
- alarming state – 4,7%