Contrave
Combination product
Pronunciation: nal-TREX-oen and byoo-PROE-pee-on (KON-trayv)
What it isOpioid antagonist plus norepinephrine-dopamine reuptake inhibitor; chronic weight management in obesity or overweight with comorbidity.
Why this oneOral, non-injectable option that may suit patients also quitting smoking or living with depression.
What limits itModest loss and more adverse-effect dropouts than other weight drugs; raises BP and heart rate; contraindicated with opioids and seizures.
Pearls
- Stop if <5% weight loss after 12 weeks at maintenance dose.
- Titrate over 4 weeks to two tablets twice daily.
- Naltrexone can raise aminotransferases; adjust for renal and hepatic impairment.
- Avoid high-fat meals, which sharply raise drug exposure.
Count Rave
Components (2)
FDA label
Read the full label on DailyMed ↗
| FDA dosing | Population | Start | Target | Max |
|---|---|---|---|---|
| Chronic weight management (obesity, or overweight with ≥1 weight-related comorbidity), with reduced-calorie diet and increased activity | Adults | 1 tablet (8 mg/90 mg) QAM week 1, escalate weekly | 2 tablets BID (32 mg/360 mg per day) from week 4 | 32 mg/360 mg per day (2 tablets twice daily) |
Titration Escalate one tablet per week to reach maintenance at the start of Week 4
Renal Moderate or severe impairment: max 2 tablets/day (1 each morning and evening); not recommended in end-stage renal disease
Hepatic Moderate impairment: max 2 tablets/day (1 each morning and evening); not recommended in severe hepatic impairment
Total daily dose should not exceed 32 mg/360 mg (two tablets twice daily); no more than two tablets at one time
Instructions
- Take in the morning and evening; do not cut, chew, or crush
- Do not take with a high-fat meal (increases exposure and seizure risk)
- Allow at least 14 days between an MAOI and Contrave in either direction
- Max 2 tablets/day with CYP2B6 inhibitors (e.g., ticlopidine, clopidogrel)
- Evaluate response after 12 weeks at maintenance; discontinue if <5% baseline weight lost
Available strengths
- ER tab 8/90 mg
Contraindications
- Uncontrolled hypertension
- Seizure disorder or a history of seizures
- Use of other bupropion-containing products
- Bulimia or anorexia nervosa, which increase the risk for seizure
- Chronic opioid or opiate agonist (e.g., methadone) or partial agonist (e.g., buprenorphine) use, or acute opiate withdrawal
- Patients undergoing an abrupt discontinuation of alcohol, benzodiazepines, barbiturates, and antiepileptic drugs
- Concomitant administration of monoamine oxidase inhibitors (MAOIs), or within 14 days of stopping an MAOI (including linezolid or intravenous methylene blue), because of increased risk of hypertensive reactions
Cautions
- Suicidal behavior and ideation — monitor for depression/suicidal thoughts
- Neuropsychiatric adverse events
- Seizures (dose-related)
- Increase in blood pressure and heart rate — monitor
- Hepatotoxicity (naltrexone component)
- Angle-closure glaucoma
- Risk of hypoglycemia in type 2 diabetes on antidiabetic therapy — monitor glucose
- Vulnerability to opioid overdose
Adverse reactions
- Nausea
- Constipation
- Headache
- Vomiting
- Dizziness
- Insomnia
- Dry mouth
- Diarrhea
Pregnancy Weight loss offers no benefit in pregnancy and may cause fetal harm — discontinue when pregnancy recognized; individual components not shown to increase major birth defect risk
Lactation Bupropion, naltrexone, and metabolites present in human milk; seizures reported in breastfed infants (bupropion); weigh benefits vs. risk
Cost
| Strength | #/mo | generic $/mo | CostPlus | |
|---|---|---|---|---|
| 8/90 mg | ER tab | 4 q-wk | not offered |
Clinical profile
Defining liabilitySeizures, hypertension and opioid-antagonist interactions
Part D rank #325.
Self-check
- Which drugs make up Contrave?
Naltrexone and bupropion. - What psychiatric risk is boxed for Contrave?
Suicidal thoughts and behaviors.