Cetilistat is a medication developed for the management of obesity. It functions as a lipase inhibitor, a type of drug that works within the digestive system. The medication aims to support weight loss efforts, particularly when combined with dietary modifications and increased physical activity.
How Cetilistat Works
Cetilistat targets and inhibits an enzyme in the digestive system called pancreatic lipase. This enzyme, produced by the pancreas, breaks down dietary fats (triglycerides) into smaller, absorbable components like free fatty acids and monoglycerides. Without its action, these fats cannot be properly absorbed by the body.
When cetilistat is taken orally, it binds to the active site of pancreatic lipase within the gastrointestinal tract. This prevents the enzyme from interacting with and breaking down fats consumed in meals. A substantial portion of dietary fat passes through the digestive system undigested and is eliminated from the body through feces. This reduces the amount of calories the body absorbs from fat, decreasing overall caloric intake.
Unlike some other weight-loss medications that influence appetite by acting on the brain, cetilistat’s action is peripheral, meaning it works directly in the digestive system. This localized action helps in reducing fat absorption, which can lead to weight loss. The reduced absorption of fats may also contribute to improvements in lipid profiles by lowering levels of low-density lipoprotein (LDL) cholesterol and triglycerides in the blood.
Conditions Treated by Cetilistat
Cetilistat is primarily developed and studied for the treatment of obesity. Obesity is a condition characterized by excessive body fat accumulation, which can increase the risk of various health problems. When used in conjunction with a reduced-calorie diet and regular physical activity, cetilistat assists individuals in managing their weight.
Beyond its direct application in weight management, cetilistat has also been investigated for its potential in addressing related health conditions often associated with obesity. These include type 2 diabetes and dyslipidemia. Clinical trials have indicated that cetilistat can significantly enhance weight loss and improve these comorbid conditions.
For instance, studies have shown that cetilistat can lead to reductions in glycosylated hemoglobin (HbA1c) levels, a marker for blood sugar control in individuals with type 2 diabetes. It has also been observed to reduce levels of total cholesterol and LDL cholesterol, which are factors in dyslipidemia. Cetilistat is approved in Japan for the treatment of obesity, sometimes with complications.
Important Considerations for Use
The medication is typically taken orally, often in capsule form, and is recommended to be taken during or up to one hour after each main meal. This timing ensures the drug is present in the gut when dietary fats are being digested, maximizing its effectiveness. If a meal is skipped or does not contain fat, the dose for that meal can be omitted.
Common side effects associated with cetilistat are primarily gastrointestinal in nature, which is expected given its mechanism of action. These can include oily or fatty stools, increased frequency of bowel movements, flatulence, and abdominal discomfort. These effects are generally mild, but they can become more noticeable if a high-fat diet is consumed. Other less common side effects reported include headache, fatigue, nausea, and respiratory tract infections.
Cetilistat can affect the absorption of fat-soluble vitamins (A, D, E, and K) because it reduces dietary fat absorption. To help prevent potential deficiencies, it is often advised to take multivitamins containing these vitamins at bedtime, at least two hours before or after taking cetilistat. Certain medical conditions and medications may also interact with cetilistat. Individuals with chronic malabsorption syndrome or cholestasis should not use cetilistat.
Additionally, cetilistat may interact with medications such as immunosuppressants (like cyclosporine), blood thinners (like warfarin), antidiabetic drugs, and thyroid medications. Individuals should inform their healthcare providers about all medications and supplements they are taking to avoid harmful interactions. Pregnant or breastfeeding women are generally advised against using cetilistat, as its safety in these populations has not been established.