Clinical Overview
Naltrexone-Bupropion is a combination medication indicated as an adjunct to a reduced-calorie diet and increased physical activity for chronic weight management in adults with obesity (BMI ≥30) or overweight (BMI ≥27) with at least one weight-related comorbidity. This unique combination targets both appetite and cravings through complementary mechanisms.
Primary Clinical Applications
Contrave is indicated for chronic weight management in adults with obesity or overweight with weight-related medical conditions such as hypertension, type 2 diabetes, or dyslipidemia. It is designed for long-term use as part of a comprehensive weight management program.
Mechanism and Clinical Benefits
The combination works synergistically: naltrexone blocks opioid receptors affecting food reward pathways, while bupropion inhibits dopamine and norepinephrine reuptake. Together, they reduce food cravings and appetite while potentially increasing energy expenditure.
Treatment Considerations
The medication requires gradual dose escalation over 4 weeks to minimize side effects. Patients should be evaluated at 12 weeks, and treatment should be discontinued if 5% weight loss has not been achieved. Regular monitoring for mood changes and cardiovascular effects is essential.
Prescribing Information
Dosing & Administration
Weight Management – Dose Escalation:
- Week 1: 1 tablet (8 mg/90 mg) in morning
- Week 2: 1 tablet morning and evening
- Week 3: 2 tablets morning, 1 tablet evening
- Week 4+: 2 tablets morning and evening (maintenance)
Maintenance Dose:
- Target: 32 mg naltrexone/360 mg bupropion daily
- Administration: With food to reduce nausea
Indications
- Chronic weight management in adults with BMI ≥30
- Chronic weight management in adults with BMI ≥27 plus weight-related comorbidity
- Used as adjunct to reduced-calorie diet and increased physical activity
Contraindications
- Uncontrolled hypertension
- Seizure disorder or history of seizures
- Use of other bupropion-containing products
- Bulimia or anorexia nervosa
- Chronic opioid or opiate agonist use
- Acute opiate withdrawal
- MAOI use within 14 days
Warnings & Precautions
- Boxed Warning: Increased suicidal thoughts and behaviors with bupropion
- Neuropsychiatric events: Monitor for mood changes, depression, suicidal ideation
- Seizure risk: Dose-dependent risk, especially with predisposing factors
- Hypertension: Monitor blood pressure and heart rate
- Hepatotoxicity: Monitor liver function
- Angle-closure glaucoma: Risk of acute attacks
Drug Interactions
- MAOIs: Contraindicated – increased seizure risk
- Opioids: Naltrexone blocks opioid effects
- CYP2D6 substrates: Bupropion inhibits CYP2D6
- Drugs lowering seizure threshold: Increased seizure risk
Adverse Reactions
Common (≥5%):
- Nausea, constipation, headache, vomiting, dizziness, insomnia
Serious:
- Seizures, hypertension, hepatotoxicity, suicidal ideation
Special Populations
- Renal Impairment: Use with caution in moderate-severe impairment
- Hepatic Impairment: Not recommended in moderate-severe impairment
- Pregnancy: Category X – contraindicated
- Elderly: Limited experience, use with caution
Medical Disclaimer: This information is for educational purposes only and is not intended as medical advice. Always consult with qualified healthcare professionals before making any treatment decisions. Individual patient circumstances may vary significantly.
