99% Purity Weight loss API Orlistat CAS 96829-58-2 white powder

Orlistat More Info

Orlistat is a reversible inhibitor of gastrointestinal lipases indicated for weight loss and weight maintenance. It was first approved by the FDA in 1999 and is marketed under brand names such as Xenical and Alli.

Mechanism of Action

Orlistat functions as a lipase inhibitor, specifically targeting gastric and pancreatic lipases. By binding covalently to the serine residue at the active site of these enzymes, orlistat inhibits their activity, preventing the hydrolysis of dietary triglycerides into absorbable free fatty acids and monoglycerides. Consequently, approximately 30% of dietary fat is not absorbed and is excreted unchanged in the feces. This mechanism results in a caloric deficit that can aid in weight loss when combined with a reduced-calorie diet

Applications

Orlistat is indicated for:
1. Weight Loss: It helps individuals lose weight when used alongside lifestyle modifications such as diet and exercise.
2. Weight Maintenance: After achieving weight loss, orlistat can assist in maintaining the new weight.
3. Prevention of Type 2 Diabetes: Studies suggest that orlistat may help reduce the incidence of type 2 diabetes, particularly in obese individuals

Routes of Administration

Orlistat is administered orally, typically in capsule form. The standard dosage for weight loss is 120 mg taken three times daily with meals that contain fat. Over-the-counter versions (e.g., Alli) are available at lower doses (60 mg) without a prescription

Safety and Side Effects

While orlistat is generally well-tolerated, it is associated with several gastrointestinal side effects, commonly referred to as "treatment effects." These include:
1. Steatorrhea: Oily, loose stools resulting from unabsorbed fats.
2. Flatulence: Increased gas production.
3. Abdominal pain: Discomfort in the stomach area.
These side effects typically diminish over time as the body adjusts to the medication. Serious adverse effects are rare but can include liver injury and allergic reactions. Due to its mechanism, orlistat does not significantly affect other physiological processes such as gastric emptying or bile composition

Pharmacokinetics

Orlistat exhibits minimal systemic absorption; less than 1% of an oral dose enters systemic circulation. The drug's pharmacokinetics are characterized by:
1. Peak Plasma Concentration: Achieved approximately 8 hours post-administration.
2. Protein Binding: Over 99% bound to plasma proteins, mainly lipoproteins and albumin.
3. Metabolism: Primarily occurs in the gastrointestinal tract, producing inactive metabolites that do not contribute to its therapeutic effects