General MedicinePrescription OnlyPregnancy Cat. Not classifiedFDA Yes
Contrave Extended-Release
NALTREXONE HYDROCHLORIDE AND BUPROPION HYDROCHLORIDE
1 INDICATIONS AND USAGE CONTRAVE is 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. 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 ex...
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Brand names:Contrave Extended-Release
Quick Reference
Medicine ClassGeneral Medicine
FDA ApprovedYes
PregnancyCategory Not classified
Quick Facts
- Active ingredient
- NALTREXONE HYDROCHLORIDE AND BUPROPION HYDROCHLORIDE
- Medicine class
- General Medicine
- Brand names
- Contrave Extended-Release
- Availability
- Prescription only (Rx)
- Pregnancy category
- Not classified
- Half-life
- half-life (T 1/2 ) was approximately 5 hours for naltrexone
- FDA approved
- Yes
What Is Contrave Extended-Release?
1 INDICATIONS AND USAGE CONTRAVE is 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. 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 ex...
Contrave Extended-Release (NALTREXONE HYDROCHLORIDE AND BUPROPION HYDROCHLORIDE) belongs to the General Medicine class of medications. It was first approved by the FDA in Yes. This medication requires a prescription from a licensed healthcare provider.
Key Safety Information
- •Always follow the dose recommended by your healthcare professional. Taking more than prescribed increases the risk of side effects including serious complications.
- •Seek emergency care if you experience signs of an allergic reaction — hives, swelling, difficulty breathing, or rash. Stop the medication and call your doctor immediately.
- •Some medications can increase the risk of cardiovascular events. Tell your doctor if you have high blood pressure, a history of heart attack or stroke, or any pre-existing health condition.
- •Avoid or limit alcohol while taking Contrave Extended-Release. Do not drink alcohol without first discussing it with your healthcare provider as it may increase adverse effects.
- •Take Contrave Extended-Release with food or a full glass of water if stomach upset occurs. Stop use and talk to your doctor if you experience persistent stomach pain or GI symptoms.
- •Tell your doctor about all medications, supplements, and vitamins you take. Some combinations significantly increase the risk of harm.
This is a summary only. Always read the full prescribing information and consult your healthcare provider for personalized medical advice.
Uses & Indications
Contrave Extended-Release is prescribed for the following conditions. Some uses are FDA-approved indications; others may be evidence-based off-label uses. Consult your healthcare provider for personalized guidance.
1 INDICATIONS AND USAGE CONTRAVE is 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.
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.
( 1 ) Limitations of Use: The effect of CONTRAVE on cardiovascular morbidity and mortality has not been established.
( 1 ) Coadministration with other naltrexone-containing products is not recommended.
Coadministration with other bupropion-containing products is contraindicated.
( 1 , 4 ) Limitations of Use: The effect of CONTRAVE on cardiovascular morbidity and mortality has not been established.
CONTRAVE contains naltrexone and bupropion.
Coadministration with other naltrexone-containing products is not recommended.
Dosage Guide
The following are general dosing guidelines only. Your actual dose should be determined by your healthcare provider based on your condition, renal/hepatic function, and other medications.
AD
Adult Dosage
2 DOSAGE AND ADMINISTRATION CONTRAVE dose escalation schedule ( 2.1 ): 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 2.1 Recommended Dosage Initiate and escalate the dosage of CONTRAVE according to the schedule in Table 1: Table 1. Dosage Initiation and Escalation Schedule for CONTRAVE 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 A total daily dosage of 32 mg of naltrexone hydrochloride (HCl) and 360 mg bupropion HCl (two CONTRAVE 8 mg/90 mg tablets twice daily) is reached at the start of Week 4. CONTRAVE should be taken by mouth in the morning and in the evening. The tablets should not be cut, chewed, or crushed. Total daily doses greater than 32 mg/360 mg per day (two tablets twice daily) are not recommended. In clinical trials, CONTRAVE was administered with meals. However, CONTRAVE should not be taken with a
Available Forms
Available Strengths
Side Effects
Common
- 6 ADVERSE REACTIONS The following adverse reactions are discussed in other sections of the labeling: Suicidal Behavior and Ideation [see Boxed Warning , Warnings and Precautions (5.1) ] Neuropsychiatric Adverse Events [see Warnings and Precautions (5.2) ] Seizures [see Contraindications (4) , Warnings and Precautions (5.3) ] Increase in Blood Pressure and Heart Rate [see Warnings and Precautions (5.5) ] Allergic Reactions [see Warnings and Precautions (5.6) ] Angle-Closure Glaucoma [see Warnings and Precautions (5.9) ] Most common adverse reactions (greater than or equal to 5%): nausea, constipation, headache, vomiting, dizziness, insomnia, dry mouth and diarrhea.
- ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Currax Pharmaceuticals LLC at 1-800-793-2145 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch .
- 6.1 Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, the adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice.
- CONTRAVE was evaluated for safety in five double-blind placebo-controlled trials in 4,754 overweight or obese patients (3,239 patients treated with CONTRAVE and 1,515 patients treated with placebo) for a treatment period up to 56 weeks.
- The majority of patients were treated with CONTRAVE 32 mg/360 mg total daily dose.
- In addition, some patients were treated with other combination daily doses including naltrexone up to 50 mg and bupropion up to 400 mg.
- All subjects received study drug in addition to diet and exercise counseling.
Serious
- 5 WARNINGS AND PRECAUTIONS Suicidal Behavior and Ideation: Monitor for depression or suicidal thoughts.
- Discontinue CONTRAVE if symptoms develop.
- ( 5.1 ) 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 suicide.
- Observe patients taking CONTRAVE for the occurrence of such symptoms and instruct them to discontinue CONTRAVE and contact a healthcare provider if they experience such adverse events.
- ( 5.2 ) Risk of seizure may be minimized by adhering to the recommended dosing schedule and avoiding coadministration with high-fat meal.
Rare
Medicine Interactions
Always inform your healthcare provider and pharmacist about ALL medications you take, including prescriptions, OTC medicines, vitamins, and supplements.
MajorModerateMinor
Warnings & Contraindications
5 WARNINGS AND PRECAUTIONS Suicidal Behavior and Ideation: Monitor for depression or suicidal thoughts. Discontinue CONTRAVE if symptoms develop. ( 5.1 ) 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, parano
How Contrave Extended-Release Works
12.1 Mechanism of 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.
Pharmacokinetics
Absorption
Absorption Naltrexone Following single oral administration of CONTRAVE (two 8 mg naltrexone/90 mg bupropion tablets) to healthy subjects, mean peak naltrexone concentration (C max ) was 1
Half-Life
half-life (T 1/2 ) was approximately 5 hours for naltrexone
Metabolism
Metabolism and Excretion Naltrexone The major metabolite of naltrexone is 6-beta-naltrexol
Excretion
Excretion Naltrexone The major metabolite of naltrexone is 6-beta-naltrexol
Pregnancy & Breastfeeding Safety
Not classified
Breastfeeding
Many medications pass into breast milk in varying amounts. Before using Contrave Extended-Releasewhile breastfeeding, discuss the benefits and risks with your healthcare provider or pharmacist — they can weigh your dose, your infant's age, and available lactation safety data to find the safest option for you and your baby.
Storage & Handling
Storage Store at 25°C (77°F); excursions permitted to 15° to 30°C (59° to 86°F) [see USP Controlled Room Temperature].
Frequently Asked Questions
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Contrave Extended-Release dosage guide
Adult, pediatric, renal, and hepatic dosing for Contrave Extended-Release
- Detail
Contrave Extended-Release side effects
Complete adverse effect profile including common, serious, and rare reactions
Sources & References
- • FDA Prescribing Information — Official labeling and package insert for Contrave Extended-Release
- • U.S. National Library of Medicine — MedlinePlus drug information
- • American Hospital Formulary Service (AHFS) — Clinical pharmacology monograph
- • PubMed / MEDLINE — View clinical studies
Last reviewed by MedCentralHub Medical Review Board · MedCentralHub Editorial Policy
Medical Disclaimer
The information on this page is for educational purposes only and is not intended as medical advice, diagnosis, or treatment. Always consult your doctor, pharmacist, or qualified healthcare provider before starting, stopping, or changing any medication.