Naltrexone et bupropion

Contrave

Usages autorisés

• CONTRAVE is a combination of naltrexone, an opioid antagonist, and bupropion, an aminoketone antidepressant, indicated in combination with a reduced-calorie diet and increased physical activity to reduce excess body weight and maintain weight reduction long term in adults with obesity or overweight in the presence of at least one weight-related comorbid condition.
• Limitations of Use: The effect of CONTRAVE on cardiovascular morbidity and mortality has not been established.
• Coadministration with other naltrexone-containing products is not recommended.

Formes et dosages

• CONTRAVE extended-release tablets: 8 mg/90 mg are blue, round, bi-convex, film-coated, and debossed with "NB-890" on one side.
• Extended-Release Tablets: 8 mg naltrexone hydrochloride (HCl) /90 mg bupropion HCl

Comment il se prend

• CONTRAVE dose escalation schedule: Morning Dose Evening Dose Week 1 1 tablet None Week 2 1 tablet 1 tablet Week 3 2 tablets 1 tablet Week 4 - Onward 2 tablets 2 tablets

Ne doit pas être utilisé en cas de

• CONTRAVE is contraindicated in Uncontrolled hypertension Seizure disorder or a history of seizures Use of other bupropion-containing products (including, but not limited to, WELLBUTRIN, WELLBUTRIN SR, WELLBUTRIN XL, APLENZIN and ZYBAN) Bulimia or anorexia nervosa, which increase the risk for seizure Chronic opioid or opiate agonist (e.g., methadone) or partial agonists (e.g., buprenorphine) use,...
• At least 14 days should elapse between discontinuation of MAOI and initiation of treatment with CONTRAVE.
• There is an increased risk of hypertensive reactions when CONTRAVE is used concomitantly with MAOIs.
• Starting CONTRAVE in a patient treated with reversible MAOIs such as linezolid or intravenous methylene blue is also contraindicated Known allergy to bupropion, naltrexone or any other component of CONTRAVE.

Interactions

• MAOIs: Increased risk of hypertensive reactions can occur when used concomitantly.
• Drugs Metabolized by CYP2D6: Bupropion inhibits CYP2D6 and can increase concentrations of antidepressants, (e.g., selective serotonin reuptake inhibitors and many tricyclics), antipsychotics (e.g., haloperidol, risperidone and thioridazine), beta-blockers (e.g., metoprolol) and Type 1C antiarrhythmics (e.g., propafenone and flecainide). Consider dose reduction when using with CONTRAVE.
• Digoxin: May decrease plasma digoxin levels. Monitor digoxin levels.
• Concomitant Treatment with CYP2B6 Inhibitors (e.g., ticlopidine or clopidogrel) can increase bupropion exposure. Do not exceed one tablet twice daily when taken with CYP2B6 inhibitors.
• CYP2B6 Inducers (e.g., ritonavir, lopinavir, efavirenz, carbamazepine, phenobarbital, and phenytoin) may reduce efficacy by reducing bupropion exposure, avoid concomitant use.
• Drugs that Lower Seizure Threshold: Dose CONTRAVE with caution.

Mises en garde et précautions

• Suicidal Behavior and Ideation: Monitor for depression or suicidal thoughts. Discontinue CONTRAVE if symptoms develop.
• Neuropsychiatric Adverse Events During Smoking Cessation: Postmarketing reports of serious or clinically significant neuropsychiatric adverse events have included changes in mood (including depression and mania), psychosis, hallucinations, paranoia, delusions, homicidal ideation, aggression, hostility, agitation, anxiety, and panic, as well as suicidal ideation, suicide attempt, and completed...
• Risk of seizure may be minimized by adhering to the recommended dosing schedule and avoiding coadministration with high-fat meal.
• Increase in Blood Pressure and Heart Rate: Monitor blood pressure and heart rate in all patients, especially those with cardiac or cerebrovascular disease.
• Hepatotoxicity: Cases of hepatitis and clinically significant liver dysfunction observed with naltrexone exposure.
• Angle-closure glaucoma: Angle-closure glaucoma has occurred in patients with untreated anatomically narrow angles treated with antidepressants.
• Use of Antidiabetic Medications: Weight loss may cause hypoglycemia. Monitor blood glucose.

Effets indésirables fréquents

• Most common adverse reactions (greater than or equal to 5%): nausea, constipation, headache, vomiting, dizziness, insomnia, dry mouth and diarrhea.

Grossesse

Weight loss offers no benefit to a pregnant patient and may cause fetal harm. When a pregnancy is recognized, advise the pregnant patient of the risk to the fetus, and discontinue CONTRAVE (see Clinical Considerations). Available pharmacovigilance data and data from clinical trials with the individual components of CONTRAVE use in pregnant patients have not demonstrated a drug-associated risk of major birth defects, miscarriage or adverse maternal or fetal outcomes.

Mécanisme d'action

CONTRAVE has two 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 two 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.

Titulaire de l'autorisation:

Nalpropion Pharmaceuticals LLC

Version de la notice:

10 novembre 2025

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