Xenical 120mg Capsule (Orlistat 120mg)

# Additional Information

Uses for Xenical

Xenical 120mg Capsule Orlistat (120mg) is widely indicated for obesity management, focusing on weight loss and its maintenance in conjunction with a reduced-calorie diet. This medication is particularly beneficial for:

• Obese patients with an initial Body Mass Index (BMI) ≥30 kg/m²
• Patients with a BMI ≥27 kg/m² who have additional risk factors, like hypertension, diabetes, or dyslipidemia
• Reducing the risk of weight regain after significant weight loss

Consultation with healthcare providers is critical to ensure Xenical’s appropriateness based on individual health conditions.

Dosage for Xenical

The recommended dosage for Xenical 120mg Capsule Orlistat (120mg) is one capsule three times a day with each main meal containing fat. However, it’s crucial to adhere to specific considerations:

• If a meal is missed or contains no fat, the Xenical dose can be omitted
• A balanced, reduced-calorie diet with about 30% calories from fat should complement the medication
• Distribute the daily intake of fat, carbohydrate, and protein over three main meals
• Use multivitamin supplements containing fat-soluble vitamins at least 2 hours before or after taking Xenical

Below is a table summarizing the recommended daily grams of fat for various daily caloric intakes in a 30% fat diet:

How Supplied

Each Xenical 120mg Capsule Orlistat (120mg) is supplied in a turquoise, hard-gelatin capsule form containing pellets. Here’s a brief on how it is packaged:

• Turquoise, two-piece, No. 1 opaque hard-gelatin capsule imprinted with XENICAL 120 in black ink
• Bottle of 90 Capsules (NDC 61269-460-90)

Storage and Handling

Proper storage conditions for Xenical are paramount:

• Store at 25°C (77°F), with permitted excursions between 15° to 30°C (59° to 86°F)
• Keep the bottle tightly closed to prevent moisture ingress
• Do not use the medication after the expiration date

Distribution information:

• Distributed by: Genentech USA, Inc. A Member of the Roche Group 1 DNA Way South San Francisco, CA 94080-4990.
• Revised: Nov 2022

Clinical Pharmacology for Xenical

Mechanism of Action

Orlistat, the active ingredient in Xenical 120mg Capsule Orlistat (120mg), is a reversible inhibitor of gastrointestinal lipases. By forming a covalent bond with the active serine residue site of gastric and pancreatic lipases, it renders these enzymes inactive, thereby hindering the absorption of dietary fats.

Pharmacodynamics

At the therapeutic dose of 120 mg three times daily, orlistat inhibits fat absorption by approximately 30%. Figure 1 illustrates the dose-response relationship:

Pharmacokinetics

Insights into the pharmacokinetics of Xenical 120mg Capsule Orlistat (120mg) reveal minimal systemic exposure:

• Absorption: Systemic absorption is negligible, with low plasma concentrations (<10 ng/mL)
• Distribution: >99% bound to plasma proteins, with minimal partition into erythrocytes
• Metabolism: Produces two metabolites, M1 and M3, which have much weaker lipase inhibitory activities
• Elimination: Major route is fecal excretion, contributing to approximately 97% of the administered dose

Table 2 outlines the pharmacokinetic data for specific populations and drugs:

Clinical Studies

Weight Management and Risk Factors

The long-term impact of Xenical on weight loss, weight maintenance, and the risk factors associated with obesity has been extensively studied.

One-Year Results

Weight Loss and Weight Maintenance

Data from five trials revealed an average weight loss of 13.4 lbs among Xenical-treated patients compared to 5.8 lbs among placebo-treated patients:

Improvements in Risk Factors

Significant improvements were noted in several risk factors, including a reduction in cholesterol and insulin levels:

Effect on Weight Regain

Several studies assessed the effects of Xenical on reducing weight regain. Patients treated with Xenical regained significantly less weight compared to those on placebo:

Two-Year Results

Long-Term Weight Control and Risk Factors

Pooled data indicate sustained benefits in weight management over two years. The percentage of patients losing ≥5% and ≥10% of body weight after 2-year treatment is summarized below:

Table 8 outlines relative changes in risk factors associated with long-term obesity treatment:

Four-Year Results

Long-Term Weight Control and Risk Factors

The XENDOS study, which spanned four years, provided a comprehensive exploration of Xenical’s efficacy. The mean percent weight loss at the end of four years favored Xenical:

Risk factors associated with obesity were again evaluated over this extended period:

Pediatric Clinical Studies

Studies extended to pediatric populations have also shown promise, with significant weight control measures recorded among obese adolescents:

Xenical 120mg Capsule Orlistat (120mg) has demonstrated an ability to support weight loss and maintenance over extended periods. These findings underscore the importance of integrating pharmacological support alongside lifestyle adjustments to achieve sustained obesity management. For detailed investigations and data points, refer to the respective clinical trial documents cited.

Drug Interactions

Xenical’s interactions with other medications necessitate careful consideration. Significant interactions include:

• Cyclosporine: Avoid simultaneous administration. Administer cyclosporine three hours after Xenical
• Fat-Soluble Vitamins: Orlistat reduces absorption; patients should take multivitamins two hours before or after Xenical
• Levothyroxine: Administer at least four hours apart. Monitor thyroid function
• Warfarin: Monitor coagulation parameters closely as Vitamin K absorption may decrease
• Amiodarone: Monitor therapeutic effect due to the reduced exposure to the drug
• Antiepileptic Drugs: Monitor changes in seizure frequency and severity
• Antiretroviral Drugs: Regular HIV RNA level monitoring is recommended

Further guidance and monitoring are crucial in patients using Xenical alongside these medications.

Conclusion

Xenical 120mg Capsule Orlistat (120mg) offers a potent approach for managing obesity and its related complications. The rigorous clinical studies affirm its efficacy in aiding weight loss and maintaining this reduction, fostering improvements in several obesity-associated risk factors. However, the importance of accompanying lifestyle changes, adherence to dosing schedules, and awareness of potential drug interactions cannot be overstated. Continuous patient education and medical guidance will maximize the therapeutic benefits of this medication.

For more comprehensive information, please consult your healthcare provider or refer to the detailed clinical data provided in the mentioned studies.

[References]
– Drugs.com. (n.d.). Xenical (Orlistat): Uses, Dosage, Side Effects, Interactions, Warning.
– Genentech USA, Inc. Xenical (Orlistat) Full Prescribing Information. Revised: Nov 2022.