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ALIMENTARY TRACT AND METABOLISM › ANTIOBESITY PREPARATIONS, EXCL. DIET PRODUCTS › ANTIOBESITY PREPARATIONS, EXCL. DIET PRODUCTS › Centrally acting antiobesity products
bupropion and naltrexone
A08AA62
Forms & Strengths
- Extended-release tablets: 90 mg naltrexone hydrochloride / 8 mg bupropion hydrochloride
Adult Dosing
- Initial: 1 tablet (90 mg/8 mg) PO once daily in the morning for 1 week
- Week 2: 1 tablet PO twice daily (morning and evening)
- Week 3: 2 tablets PO in the morning and 1 tablet PO in the evening
- Maintenance (Week 4 onwards): 2 tablets PO twice daily (maximum daily dose: 360 mg naltrexone / 32 mg bupropion)
- Evaluate efficacy and tolerance at 12 weeks; discontinue if weight loss is < 5% of baseline
Pediatric Dosing
- Safety and efficacy have not been established in pediatric patients < 18 years of age
Indications
- 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 one weight-related comorbid condition (e.g., hypertension, type 2 diabetes mellitus, dyslipidemia)
Mechanism of Action
- Combines bupropion (a relatively weak inhibitor of neuronal reuptake of dopamine and norepinephrine) and naltrexone (an opioid receptor antagonist)
- Acts on the hypothalamus (pro-opiomelanocortin [POMC] neurons) and the mesolimbic dopamine circuit to reduce appetite and reward pathways associated with food
Contraindications
- Uncontrolled hypertension
- Seizure disorder or history of seizures
- Current or prior diagnosis of anorexia nervosa or bulimia
- Abrupt discontinuation of alcohol, benzodiazepines, barbiturates, and antiepileptic drugs
- Use of other bupropion-containing products
- Chronic opioid use or acute opioid withdrawal
- Concomitant use of monoamine oxidase inhibitors (MAOIs) or use within 14 days
Adverse Reactions
- Nausea
- Constipation
- Headache
- Vomiting
- Insomnia
- Dry mouth
- Diarrhea
- Dizziness
- Increased blood pressure and heart rate
- Anxiety
Drug Interactions
- MAOIs: May cause acute hypertensive reactions; contraindicated
- Opioids: Naltrexone blocks opioid effects and may precipitate acute withdrawal
- CYP2B6 inhibitors (e.g., ticlopidine, clopidogrel): May increase bupropion exposure
- CYP2B6 inducers (e.g., ritonavir, lopinavir, efavirenz): May decrease bupropion efficacy
- Drugs lowering seizure threshold (e.g., antipsychotics, antidepressants, theophylline, systemic steroids): Increases risk of seizures
- Dopaminergic drugs (levodopa, amantadine): May increase adverse central nervous system effects
Curated Content: Needs Vetting Before Put to Clinical Use