Orlistat is a widely used over-the-counter weight loss medication for obesity management. Its core mechanism of action is to inhibit the activity of gastrointestinal lipase, reducing the absorption of about 30% of dietary fat by the body. Undigested fat is directly excreted with feces, reducing calorie intake and achieving the effect of assisting weight loss.

1、 Drug name

1. Common name: Orlistat

2. Product Name: XENICAL ®

2、 Indications

1. Used for obesity management, including weight loss and maintenance in combination with a low calorie diet.

2. Used to reduce the risk of weight rebound after previous weight loss.

3. It is applicable to patients with initial body mass index (BMI) ≥ 30kg/m ², or patients with BMI ≥ 27kg/m ² and other risk factors (such as hypertension, diabetes, dyslipidemia).

3、 Specifications and characteristics

Specification: Capsules, each containing 120 milligrams of orlistat.

4、 Main components

Active ingredient: Orestat.

5、 Usage and dosage

1. Recommended dosage: 1 capsule (120mg) each time, 3 times a day, taken with a high-fat main meal (within 1 hour after or during meals).

2. Dietary requirements: It is necessary to follow a nutritionally balanced low calorie diet, with approximately 30% of daily calories coming from fat. Daily intake of fat, carbohydrates, and protein should be distributed among three meals.

3. Omission treatment: If there are occasional missed meals or if the meal does not contain fat, the dose can be omitted.

4. Vitamin supplementation: As this product may reduce the absorption of certain fat soluble vitamins, patients should take a daily multivitamin containing fat soluble vitamins (vitamins A, D, E, K, and beta carotene). Supplements should be taken at least 2 hours before or after taking this product (such as before bedtime).

6、 Dose adjustment

1. Doses higher than 120 milligrams per dose, three times a day, did not show any additional benefits.

2. For patients with diabetes, weight loss may affect blood glucose control, and it may be necessary to reduce the dosage of oral hypoglycemic drugs (such as sulfonylureas) or insulin.

7、 Medication precautions

1. Before and after meals: Take with meals or within 1 hour after meals.

2. Taken together with other medications:

(1) Cyclosporine: Cyclosporine should be taken at least 3 hours after taking this product.

(2) Left thyroid hormone: It should be taken at least 4 hours apart from this product and monitored for thyroid function.

(3) Antiepileptic drugs: It is necessary to monitor possible changes in the frequency or severity of epileptic seizures.

(4) Antiretroviral drugs: HIV RNA levels should be monitored frequently, and if an increase in viral load is confirmed, this product should be discontinued.

(5) Warfarin: Close monitoring of coagulation parameters is required.

3. Adverse reaction response: The most common adverse reactions are related to the gastrointestinal tract and are manifestations of the mechanism of action. If the dietary fat content is too high (>30% of total daily calories), gastrointestinal events may increase.

8、 Medication for special populations

1. Pregnant women: Do not use. It is not recommended to lose weight during pregnancy.

2. Breastfeeding women: Use with caution, it is unclear whether orlistat is secreted through human milk.

3. Children: The safety and efficacy of patients under 12 years old have not been established. The use of 12-16 year old adolescents is based on adult studies and additional data for this age group, and adverse reactions are similar to those in adults.

4. Elderly: Clinical studies did not include a sufficient number of patients aged 65 and above to determine whether their responses were different.

9、 Adverse reactions

1. The most common adverse reactions (with an incidence rate of ≥ 5% and at least twice that of the placebo group) are: oily spots, gastrointestinal bloating with excrement, urgency, fatty/oily stools, oily excretion, increased frequency of bowel movements, and fecal incontinence.

2. Other common adverse reactions include abdominal pain/discomfort, nausea, infectious diarrhea, upper respiratory tract infection, headache, fatigue, etc.

3. Serious adverse reactions (to be cautious):

(1) Severe liver injury: Rare case reports may present with hepatocyte necrosis or acute liver failure. If symptoms such as loss of appetite, itching, jaundice, dark urine color, light stool color, and pain in the upper right abdomen occur, the medication should be stopped immediately and medical attention should be sought.

(2) Oxalate nephrolithiasis and kidney disease: case reports available. Patients at increased risk of renal insufficiency should have their renal function monitored.

(3) Gallstones: Significant weight loss may increase the risk.

(4) Allergic reactions: Rare reports include itching, rash, urticaria, angioedema, bronchospasm, and allergic reactions.

10、 Contraindications

1. Pregnancy.

2. Chronic malabsorption syndrome.

3. Cholestasis.

4. Known to be allergic to XENICAL or any of its ingredients.

11、 Drug interactions

1. Cyclosporine: Combination use can reduce the blood concentration of cyclosporine. Simultaneous use is prohibited and should be taken at least 3 hours apart.

2. Fat soluble vitamins and analogues: reduce the absorption of beta carotene and vitamin E acetate supplements. It is recommended to supplement with multivitamins daily (at least 2 hours apart).

3. Levothyroxine: Co administration may lead to hypothyroidism, and thyroid function should be monitored with at least a 4-hour interval between medication.

4. Warfarin and other anticoagulants: may reduce vitamin K absorption, affect coagulation parameters, and require close monitoring.

5. Amiodarone: Co administration may reduce the exposure of amiodarone and its metabolites, which may weaken the therapeutic effect.

6. Antiepileptic drugs: There have been reports of seizures occurring in combination, and changes in seizures need to be monitored.

7. Antiretroviral drugs: may lead to virological control failure in HIV infected individuals, requiring frequent monitoring of HIV RNA levels.

12、 Storage method

1. Stored at 25 ° C (77 ° F), allowing fluctuations between 15 ° C and 30 ° C (59 ° F and 86 ° F).

2. Do not use after the expiration date indicated on the packaging.

Orlistatinformation