Orlistat (Xenical)

The anti-obesity agent orlistat is really a potent and selective inhibitor of gastrointestinal lipases which promotes weight loss by inhibiting the hydrolysis and absorption of ingested fat. When administered in the recommended dosage, orlistat can block as much as 30% of ingested fat calories, without disrupting the standard physiological functioning of the digestive tract.

Orlistat is indicated in obese adult patients having a body mass index (BMI) of equal to or more than 30 kg/m2 or equal to or more than 28 kg/m2 with concomitant risk factors (e.g. type 2 diabetes, hypertension and hypercholesterolemia).

Patients should also be asked to adopt changes for their lifestyle and diet along with orlistat to be able to maximise treatment success. Orlistat works well and effectively tolerated in patients with type 2 diabetes, hypertension or hypercholesterolaemia and may even slow concomitant disease progression in some instances, probably as a result of fat loss. It's been proven to delay the start of type 2 diabetes in obese impaired glucose tolerance patients inside a 4-year trial.

The adverse event profile of orlistat is usually mild-to-moderate in intensity, even though incidence of gastrointestinal side-effects is generally elevated within the early stages of treatment since the patient learns which foods are full of fat.This may impede patient concordance unless the right support and advice is received.

Responding to past experiences with anti-obesity agents, current expectations of weight loss medicine is limited. The costly cardiac events linked to the serotonergic agents (e.g. fenfluramine, dexfenfluramine) and also the increased risk of haemorrhagic stroke following phenylpropanolamine, have resulted in the strict unsafe effects of new compounds for obesity. For many physicians, pharmacological intervention can be considered a final resort within the management of obese patients, with controlled diet and workout the most well-liked first-line treatment approaches.

Lipases play a vital role within the digestion of long-chain triglycerides; which take into account over 95% of the 50-120 g daily lipid intake of western adults. Of the lipases, pancreatic lipase is paramount enzyme active in the digestion of lipids in both animals and man.

Pancreatic lipases cleave essential fatty acids in the triglyceride chain and also the resultant free essential fatty acids are then readily available for incorporation into micelles, that are consequently absorbed with the small intestine in the level of the brush border. Addititionally there is evidence to claim that pancreatic lipases may be indirectly responsible for the absorption of cholesterol. Thus, the inhibition of triglyceride digestion by lipases represents a legitimate target forming part of the overall weight loss strategy.

Orlistat is definitely an anti-obesity agent having a novel mechanism of action. By inhibiting the game of gastric, carboxylester and pancreatic lipases, it cuts down on the absorption of dietary fat within the gastrointestinal tract, thus promoting weight loss. Additionally, patients are further motivated to lower their fat intake to prevent the relatively unpleasant gastrointestinal side-effects sometimes linked to the drug when an excessive amount of dietary fat is consumed.

Orlistat is indicated for the treating obesity, along with a mildly hypocalorific diet and behavioural and use strategies, in those people with a BMI of 30 kg/m2 or more, or having a BMI of 28 kg/m2 and other risk factors including type 2 diabetes, hypertension and hypercholesterolaemia.

Patients have to lose a minimum of 2.5 kg in weight through adequate dieting and exercise within the month prior to the first prescription of orlistat.7 This short article looks at the properties of orlistat and it is efficacy in controlled clinical trials conducted in many patient populations.