- Scientifically proven to block the absorption of 30% of the fat you eat
- The only FDA approved medication to block the absorption of fat
- Boosts weight loss by 50%
- Take one with every meal you eat
Directions for use: Start with one tablet with each meal until sensitivity to side effects can be guaged. Then raise to 2 tablets with every meal.
Orlistat is a drug designed to treat obesity. It is marketed as a prescription drug 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 at twice the price Enhanced Athlete charges. 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 is the saturated derivative of lipstatin, a potent natural inhibitor of pancreatic lipases isolated from the bacteriumStreptomyces toxytricini. However, due to its relative simplicity and stability, orlistat was chosen over lipstatin for development as an anti-obesity drug.
The effectiveness of orlistat in promoting weight loss is definite but modest. Pooled data from clinical trials suggest that people given orlistat in addition to lifestyle modifications, such as diet and exercise, lose about 2–3 kilograms (4.4–6.6 lb) more than those not taking the drug over the course of a year. Orlistat also modestly reduces blood pressure and appears to prevent the onset of type 2 diabetes, whether from the weight loss itself or to other effects. In a large randomized controlled trial, orlistat was found to reduce the incidence of diabetes by nearly 40% in obese people.
Benefits aside, however, orlistat is notorious for its gastrointestinal side effects (sometimes referred to as treatment effects), which can include steatorrhea (oily, loose stools). They decrease with time, however, and are the most frequently reported adverse effects of the drug. In the United States and the European Union, orlistat is available for sale without a prescription. Over-the-counter approval was controversial in the United States, with consumer advocacy group Public Citizen repeatedly opposing it on safety and efficacy grounds. Generic formulations of orlistat are available in some countries. In Australia it is listed as an S3 medication and so is available over the counter in pharmacies.
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, asignificant 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 mmHgin systolic and diastolic blood pressure respectively).[needs update]
The primary side effects of the drug are gastrointestinal-related, and include steatorrhea (oily, loose stools with excessive flatus due to unabsorbed fats reaching the large intestine), fecal incontinence and frequent or urgent bowel movements. GlaxoSmithKline recommends that all users be cautious of the possible side effects until they “have a sense of any treatment effects”. To minimize these effects, foods with high fat content should be avoided; the manufacturer advises consumers to follow a low-fat, reduced-calorie diet. Oily stools and flatulence can be controlled by reducing the dietary fat content to somewhere in the region of 15 grams per meal. The manual for Alli makes it clear that orlistat treatment involves aversion therapy, encouraging the user to associate eating fat with unpleasant treatment effects.
According to Roche, side effects are most severe when beginning therapy and may decrease in frequency with time; this is supported by the results of the XENDOS study, which found that 36% of people had gastrointestinal adverse effects during their fourth year of taking orlistat, whereas 91% of study subjects had experienced at least one GI-related side effect during the first year of treatment. It has also been suggested that the decrease in side effects over time may be associated with long-term compliance with alow-fat diet.
Absorption of fat-soluble vitamins and other fat-soluble nutrients is slightly inhibited by the use of orlistat. A multivitamin tablet containing vitamins A, D, E, K, and beta-carotene should be taken once a day, at bedtime, when using orlistat.
Mechanism of action
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.
Orlistat has historically been available by prescription only, and this situation continues in Canada. In Australia, the European Union,and the United States, certain formulations of orlistat have been approved for sale without a prescription.
Australia and New Zealand
In Australia and New Zealand, orlistat is currently available over-the-counter in 120 mg size (84 capsules to the pack). Initially available only with a prescription, it was reclassified as a “Pharmacist Only Medicine” in October 2003. In 2007 the Committee decided to keep orlistat as a Schedule 3 drug, but withdrew its authorization of direct-to-consumer Xenical advertising, stating this “increased pressure on pharmacists to provide orlistat to consumers…this in turn had the potential to result in inappropriate patterns of use”. Xenical has recently[when?] began being advertised direct-to-customers again.
On 23 January 2006, a U.S. Food and Drug Administration advisory panel voted 11 to 3 to recommend the approval of an OTC formulation of orlistat, to be marketed under the name alli /ˈælaɪ/ by GlaxoSmithKline. Approval was granted on 7 February 2007, and alli became the first weight loss drug officially sanctioned by the U.S. government for over-the-counter use. Consumer advocacy organization Public Citizen opposed over-the-counter approval for orlistat.