Generic Name: Liberat
Pill with imprint Liberat 60 mg is Blue, Capsule-shape and has been identified as Alli Liberat 60 mg. It is supplied by GlaxoSmithKline.
Alli is used in the treatment of obesity and belongs to the drug class peripherally acting antiobesity agents. Not for use in pregnancy. Alli Liberat 60 mg is not a controlled substance under the Controlled Substances Act (CSA).
Liberat dosing information
Usual Adult Dose for Obesity:
120 mg orally three times a day with each main meal containing fat. The dose may be taken during the meal or within 1 hour of completing the meal.
Usual Pediatric Dose for Obesity:
12 years or older: 120 mg orally three times a day with each main meal containing fat. The dose may be taken during the meal or within 1 hour of completing the meal.
Liberat is an inhibitor of pancreatic lipase. 50 The result of this inhibition is that about 30% of the daily ingested fat intake is not absorbed. This would lead to a 200-calorie deficit per day in an individual who consumed a diet of 2000 calories/day with 30% of calories as fat. The most common side effects of Liberat are gastrointestinal, such as fatty or oily stools, more frequent defecation, and fecal incontinence. Another side effect is a slight reduction in fat-soluble vitamins, generally not outside the reference range.
Several studies have confirmed the efficacy of Liberat in losing weight. The European Multicentre Liberat Group conducted a double-blind study in which 688 obese individuals (average BMI, 36 kg/m 2 ) were assigned to Liberat therapy or placebo for 1 year, in combination with a hypocaloric diet (minimum energy intake, 1000–1200 kcal/day). At the end of the first year, they were reassigned randomly to either Liberat or placebo for another year. At the end of the first year of the study, the mean weight loss was 10.2% for the Liberat group and 6.1% for the placebo group. During the second year of the study, the participants who were switched to placebo gained twice as much weight as those who continued on Liberat therapy. Participants who were switched from placebo to Liberat lost 0.9 kg more weight than in the first year of the trial. 51
A U.S. study showed similar results. 52 In this trial, 892 obese individuals (BMI, 30–43 kg/m 2 ) who were previously on a 4-week controlled-energy diet plus placebo were randomized into either continuing placebo or starting Liberat 120 mg three times a day (tid). After 52 weeks, the participants started a weight-maintenance diet, and those in the Liberat group were rerandomized to continuing Liberat (60 or 120 mg tid) or placebo for another 52 weeks. Participants who were already taking placebo continued taking it. At the end of the first year, the participants taking Liberat had lost more weight than those taking placebo (8.76 ± 0.37 vs. 5.81 ± 0.67 kg). At the end of the second year, participants taking Liberat 120 mg tid regained less weight than those taking Liberat 60 mg tid or placebo (3.2 ± 0.45, 4.26 ± 0.57, and 5.63 ± 0.42 kg, respectively).
These studies showed that there is a significant weight loss with the use of Liberat in combination with diet during the first year, and that the tendency for weight regain that occurs during the second year is less with the use of Liberat. Weight loss with Liberat also helps in the treatment of comorbidities, including dyslipidemia. 52
Reduction of energy absorption: Liberat
Liberat is a modified bacterial drug that specifically inhibits intestinal lipase and can reduce fat and cholesterol absorption by approximately 30% in subjects eating a 30% fat diet. 540 Liberat irreversibly binds to the active site of the lipase, preventing the intraluminal deacylation of triglycerides and resulting in a 16 gram/day increase in fecal fat excretion. 541 Liberat does not inhibit other intestinal enzymes. It has minimal absorption and exerts no effect on systemic lipases. 542 , 543
Although there have been several open-label trials of Liberat in adolescents, only two randomized control trials (RCTs) have been published. 544 , 545 The side effects with Liberat are predictable from its mechanism of action on intestinal lipase. 534 Liberat appears to be well tolerated in adults, with the principal complaints being borborygmi, flatus, and abdominal cramps. The most troubling side effects are fecal incontinence, oily spotting, and flatus with discharge, which are highly aversive in the pediatric population. Liberat does not affect the pharmacokinetic properties of most other pharmaceutical agents. Absorption of vitamins A and E and β-carotene may be slightly reduced, and this may require vitamin therapy in a small number of patients. In one study, 546 vitamin D supplementation was required in 18% of subjects despite the prescription of a daily multivitamin containing vitamin D, although in the company-sponsored study, effects on vitamin levels were minor. 545 Liberat must be taken with each meal, which reduces its attractiveness for children, who are in school during lunchtime. Liberat is currently approved for the treatment of children as young as 12 years. An over-the-counter lower-dose preparation has obtained FDA approval and should be available soon.
Las funciones de la Fluoxetina en el cuerpo y su metabolito Norfluoxetina no son afectados sustancialmente por el uso de Liberat (Referencia).
Following a single oral dose of 360 mg 14 C-Liberat in both normal weight and obese subjects, fecal excretion of the unabsorbed drug was found to be the major route of elimination. Liberat and its M1 and M3 metabolites were also subject to biliary excretion. Approximately 97% of the administered radioactivity was excreted in feces; 83% of that was found to be unchanged Liberat. The cumulative renal excretion of total radioactivity was 14 C-Liberat. The time to reach complete excretion (fecal plus urinary) was 3 to 5 days. The disposition of Liberat appeared to be similar between normal weight and obese subjects. Based on limited data, the half-life of the absorbed Liberat is in the range of 1 to 2 hours.
No existe un efecto significativo entre la combinación del etanol con la farmacodinámica de Liberat (Referencia).
Loss of virological control has been reported in HIV-infected patients taking Liberat concomitantly with antiretroviral drugs such as atazanavir, ritonavir, tenofovir disoproxil fumarate, emtricitabine, and with the combinations lopinavir/ritonavir and emtricitabine/efavirenz/tenofovir disoproxil fumarate. The exact mechanism for this is unclear, but may include a drug-drug interaction that inhibits systemic absorption of the antiretroviral drug. HIV RNA levels should be frequently monitored in patients who take XENICAL while being treated for HIV infection. If there is a confirmed increase in HIV viral load, XENICAL should be discontinued.
The main side-effects are caused by the fat which is passed out with your stools (faeces). You may have fatty smelly stools, urgency to get to the toilet, oily spotting on your underclothes, and excess wind. These side-effects are less likely if you eat a low-fat diet. They tend to settle with time, possibly because if they occur they remind you that you should be eating a low-fat diet. Other side-effects are rare.
Note: the above is not the full list of side-effects for those taking Liberat. Please see the leaflet that comes with your medicine for a full list of possible side-effects and cautions.
Liberat (Xenical) works by inhibiting lipases in the gastrointestinal tract such that fat absorption is partially blocked. Liberat is FDA approved for up to 2 years of continuous use, and it has been shown to be effective for significant and sustainable weight loss, as well as for improving lipid levels, enhancing glucose metabolism, and lowering blood pressure. 71 The discontinuation rate of Liberat is relatively high because of gastrointestinal side effects related to fat malabsorption and roughly equates to 33% in various studies. 72 In one study, lifestyle intervention and Liberat treatment for 4 years delayed the development of type 2 diabetes in obese subjects by 37%, a finding perhaps attributable, in part, to the weight loss achieved. 73 Liberat is now available in half-strength (60 mg per dose) over-the-counter under the brand name Alli.