Contrave

Contrave is the other name or brand name for naltrexone hydrochloride/bupropion hydrochloride.

Bupropion and naltrexone

Contrave

Contrave is a prescription medication that combines naltrexone hydrochloride, an opioid antagonist, and bupropion hydrochloride, an aminoketone antidepressant. It is used as an adjunct to a reduced-calorie diet and increased physical activity for chronic weight management in adults.

Indications and Usage

Contrave is indicated for chronic weight management in adults with an initial body mass index (BMI) of:

• 30 kg/m² or greater (obese)
• 27 kg/m² or greater (overweight) in the presence of at least one weight-related comorbidity, such as hypertension, type 2 diabetes mellitus, or dyslipidemia.

Limitations of Use

The effect of Contrave on cardiovascular morbidity and mortality has not been established. Additionally, its safety and effectiveness in combination with other products intended for weight loss, including prescription drugs, over-the-counter drugs, and herbal preparations, have not been established.

Dosage and Administration

Contrave's dose escalation schedule is as follows:

• Week 1: 1 tablet in the morning
• Week 2: 1 tablet in the morning and 1 in the evening
• Week 3: 2 tablets in the morning and 1 in the evening
• Week 4 onwards: 2 tablets in the morning and 2 in the evening

Dosage Forms and Strengths

Contrave is available as extended-release tablets containing 8 mg naltrexone HCl and 90 mg bupropion HCl.

Contraindications

• Uncontrolled hypertension
• Seizure disorders, anorexia nervosa or bulimia, or undergoing abrupt discontinuation of alcohol, benzodiazepines, barbiturates, and antiepileptic drugs
• Use of other bupropion-containing products
• Chronic opioid use
• Use within 14 days of taking monoamine oxidase inhibitors (MAOI)
• Known allergy to any of the ingredients in Contrave

Warnings and Precautions

• Suicidal Behavior and Ideation: Monitor for depression or suicidal thoughts. Discontinue Contrave if symptoms develop.
• Neuropsychiatric Adverse Events During Smoking Cessation: Observe for mood changes, psychosis, hallucinations, paranoia, delusions, homicidal ideation, aggression, hostility, agitation, anxiety, panic, as well as suicidal ideation, suicide attempt, and completed suicide.
• Risk of Seizure: Minimize by adhering to the recommended dosing schedule and avoiding coadministration with high-fat meals.
• Increase in Blood Pressure and Heart Rate: Monitor in all patients, especially those with cardiac or cerebrovascular disease.
• Hepatotoxicity: Cases of hepatitis and clinically significant liver dysfunction observed with naltrexone.
• Angle-Closure Glaucoma: Occurred in patients with untreated anatomically narrow angles treated with antidepressants.
• Use of Antidiabetic Medications: Weight loss may cause hypoglycemia. Monitor blood glucose.

Adverse Reactions

The most common adverse reactions (≥5%) include nausea, constipation, headache, vomiting, dizziness, insomnia, dry mouth, and diarrhea.

Drug Interactions

• MAOIs: Increased risk of hypertensive reactions with concomitant use.
• Drugs Metabolized by CYP2D6: Bupropion inhibits CYP2D6. Consider dose reduction when used with Contrave.
• Digoxin: May decrease plasma digoxin levels. Monitor levels.
• CYP2B6 Inhibitors: Can increase bupropion exposure. Do not exceed one tablet twice daily.
• CYP2B6 Inducers: May reduce efficacy by reducing bupropion exposure.
• Drugs that Lower Seizure Threshold: Use with caution.
• Dopaminergic Drugs: CNS toxicity can occur with concomitant use.
• Drug-Laboratory Test Interactions: Contrave can cause false-positive urine test results for amphetamines.

Use in Specific Populations

• Pregnancy: Weight loss during pregnancy may cause fetal harm. Discontinue when pregnancy is recognized.
• Pediatric Use: Safety and effectiveness not established and use not recommended.

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