Daily Medication Pearl: Naltrexone HCl and Bupropion HCl (Contrave)

Medication Pearl of the Day: Naltrexone HCl and Bupropion HCl (Contrave)

Indication: Contrave is a combination of naltrexone, an opioid antagonist, and bupropion, an aminoketone antidepressant, indicated as an adjunct to a reduced-calorie diet and increased physical activity for chronic weight management in adults with an initial body mass index (BMI) of 30 kg/m2 or greater (obese) or 27 kg/m2 or greater (overweight) in the presence of at least 1 weight-related comorbidity (e.g., hypertension, type 2 diabetes mellitus, or dyslipidemia).

Insight:

• Dosing: Take 1 tablet to start then to 2 tablets as weeks progress, per directions.
• Dosage forms: Extended-release tablets 8 mg naltrexone HCl/90 mg bupropion HCl.
• Adverse events: Most common adverse reactions (greater than or equal to 5%): nausea, constipation, headache, vomiting, dizziness, insomnia, dry mouth, and diarrhea.
• Mechanism of action: Contrave has 2 components: naltrexone, an opioid antagonist, and bupropion, a relatively weak inhibitor of the neuronal reuptake of dopamine and norepinephrine. Nonclinical studies suggest that naltrexone and bupropion have effects on 2 separate areas of the brain involved in the regulation of food intake—the hypothalamus (appetite regulatory center) and the mesolimbic dopamine circuit (reward system). The exact neurochemical effects of Contrave leading to weight loss are not fully understood.

Reference: LABEL (fda.gov)