A Complete Guide to Weight Loss Pill Orlistat

By Ayesha Gulzar

Orlistat is an anti-obesity (weight loss pill) medications approved by the US Food and Drug Administration (FDA). It is commonly used to manage obesity by reversibly inhibiting the gut enzymes.
Weight loss pill orlistat gives maximum benefit when used with balanced diet and exercise. Orlistat is available as a prescription drug, Xenical (orlistat 120mg), and an over-the-counter use brand, Alli (orlistat 60mg).1
The article provides a comprehensive overview of how orlistat works, how to use it, dosage, and side effects.

FDA Approval Dates

  • Xenical (orlistat 120mg) was approved by the FDA as a prescription product in 1999.
  • In 2007, Alli (orlistat 60mg) was approved for OTC use for weight loss in overweight adults aged 18 and older.

How Orlistat Works?

Weight loss pill orlistat works to manage obesity by reversibly inhibiting gastric and pancreatic enzymes (lipase) within the gut. These lipases play a crucial role in the digestion of dietary fat. It by breaks down triglycerides into absorbable free fatty acids and monoglycerides.
2Inactivating lipase prevents the hydrolysis of triglycerides, thereby reducing the absorption of free fatty acids.

In simple words, orlistat helps with weight control by reducing the absorption of 20-30% of dietary fat. However, it does not act on the fats already present in the body.

weight loss

Indications:

The FDA-approved indication of orlistat includes:

  • People with obesity have a body mass index (BMI) of 30 kg/m2 or higher.
  • People with a BMI greater than 27 kg/m2 and the presence of risk factors, including hypertension, diabetes, and dyslipidemias(abnormal amount of fats in the blood).
  • Individuals seeking to reduce the risk of weight regain following previous weight loss efforts.

Off-Label Uses

It is also used off-label (indications not approved by the FDA, but the drug is effective in treating them). According to the American Heart Association (AHA) in 2021, orlistat is deemed safe and effective:

  • For treating obesity in individuals with heart failure
  • Lowering serum triglycerides in children with type 1 hyperlipoproteinemia.
  • Efficacy in people with non-alcoholic fatty liver disease

How Long Will It Take To Show Weight Loss By Orlistat?

It is essential to take orlistat with diet control and exercise for maximum benefits.
You will begin to see results in two weeks of taking the medicine. However, noticeable results will appear after continuos intake of orlistat for nearly six months.

How To Take Orlistat?

  • Orlistat is available as oral tablets in 60 mg (over-the-counter) and 120 mg (prescription) strengths.
  • The recommended orlistat dosage is 120 mg orally, taken three times daily.
  • The administration is during or within one hour after the fat-containing meal. The dosage of more than 120 mg/d has no additional benefit.
  • Take a low-fat diet for additional benefits and enhanced results.
  • If you miss the meal, you can skip the orlistat dose.
  • Take the tablet with a meal or within two hours of a meal. Later intake will be of no use, as most fat absorption occurs within three hours.
  • Take multivitamin supplements (containing fat-soluble vitamins) daily. Take multivitamin supplements at least two hours after orlistat administration.

Use In Specific Populations:

  • Renal impairment: Orlistat is considered safe for use in people with renal impairment. 
  • Hepatic impairment: Prescribe with caution to people with obstructed bile ducts and abnormal liver function tests.
  • Pregnancy: Orlistat is contraindicated during pregnancy.
  • Breastfeeding considerations: Weight loss medications are not recommended during breastfeeding.
  • Pediatric: Orlistat is FDA-approved for long-term treatment of obesity in children aged 12 and older. However, the safety and efficacy of orlistat have not been established in children aged 12 or younger.
  • Older patients: Studies have shown orlistat’s efficacy in the older population.

Side Effects of Orlistat

The adverse effects of orlistat include the following:

  • The most common adverse effect of orlistat use is steatorrhea(the presence of excess fat in feces). It occurs due to impaired absorption of dietary fat.
  • Other adverse effects include fecal spotting, diarrhea, abdominal pain, and anal fissures(a tear in the mucosal lining of the anal canal).
  • Orlistat may inhibit the absorption of fat-soluble vitamins and other fat-soluble nutrients. You should use a multivitamin tablet containing vitamins A, D, E, K, and beta-carotene once daily.
  • Orlistat can increase the risk of osteoporosis (weak bones) by impairing the absorption of calcium and vitamin D.

Drug Drug Interactions

Orlistat can reduce the efficacy of some drugs when you take them together.3 These include:

  • Antiepileptics like lamotrigine, valproate, vigabatrin, and gabapentin.
  • Amiodarone
  • Cyclosporine
  • Levothyroxine
  • Warfarin
  • Antiretroviral medications such as HIV medications

Warning And Precations

Orlistat is contraindicated in individuals with4:

  • Hypersensitivity to orlistat or its constituents
  • Cholestasis (reduced flow of bile from liver)
  • Pregnancy
  • Chronic malabsorption

Prec5autions

  • Orlistat can increase the risk of acute kidney injury or increases the risk of renal stones.
  • Used with caution in people with anorexia or bulimia nervosa (an eating disorder).

Ask your healthcare professionals to rule out organic causes of obesity like hypothyroidism or Cushing syndrome before initiating orlistat therapy.

A Word From Writer:

Always ask your healthcare professional before using any drug to get maximum therapeutic effects and minimum adverse effects. The article is for information purpose that does not rule out the need of a professional advice.

Sorurces
  1. Food and Drug Administration. Orlistat (marketed as Alli and Xenical) Information. ↩︎
  2. Guerciolini R. Mode of action of orlistat. Int J Obes Relat Metab Disord. 1997 Jun;21 Suppl 3:S12-23. ↩︎
  3. Heck AM, Yanovski JA, Calis KA. Orlistat, a new lipase inhibitor for the management of obesity. Pharmacotherapy. 2000 Mar;20(3):270-9. ↩︎
  4. MacMillan M, Cummins K, Fujioka K. What weight loss treatment options do geriatric patients with overweight and obesity want to consider? Obes Sci Pract. 2016 Dec;2(4):477-482. ↩︎
  5. Chao AM, Wadden TA, Berkowitz RI. The safety of pharmacologic treatment for pediatric obesity. Expert Opin Drug Saf. 2018 Apr;17(4):379-385. ↩︎