Contrave (Bupropion/Naltrexone)
Mysimba
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| Formula | C20H23NO4·HCl (naltrexone hydrochloride); C13H18ClNO·HCl (bupropion hydrochloride) |
| License | FDA approved (NDA 200063; initial U.S. approval 2014); EMA authorized as Mysimba on 26 March 2015 |
| Bioavailability | Absolute bioavailability not stated for the fixed-dose ER product; high-fat meals significantly increase naltrexone and bupropion exposure and should be avoided |
| Legal status | Prescription only (Rx-only); not a controlled substance |
| Chemical Name | Naltrexone HCl: morphinan-6-one, 17-(cyclopropylmethyl)-4,5-epoxy-3,14-dihydroxy-, hydrochloride, (5a)-; Bupropion HCl: (±)-1-(3-chlorophenyl)-2-[(1,1-dimethylethyl)amino]-1-propanone hydrochloride |
| Elimination half-life | Naltrexone ~5 hours; bupropion ~21 hours |
| Dosage (Strength) | Extended-release tablets: 8 mg naltrexone HCl / 90 mg bupropion HCl; titrate to 2 tablets twice daily by Week 4, total daily dose 32 mg/360 mg |
| Pregnancy | Pregnancy Category X; contraindicated during pregnancy because weight loss offers no potential benefit and may result in fetal harm |
| Brands | Contrave; Mysimba |
| Protein binding | Naltrexone 21%; bupropion 84% |
| PubChem CID | 5485201 (naltrexone hydrochloride); 5360515 (naltrexone); 62884 (bupropion hydrochloride); 444 (bupropion); 73005609 (bupropion+naltrexone) |
| MedlinePlus | a619020 |
| ChEBI | 7465 (naltrexone); 3219 (bupropion) |
| ATC code | A08AA62 |
| DrugBank | DB00704 (naltrexone); DB01156 (bupropion) |
| KEGG | D10751 (naltrexone and bupropion); D02095 (naltrexone hydrochloride); D05113 (naltrexone); D00817 (bupropion hydrochloride); D07591 (bupropion) |
| Routes of administration | By mouth (oral extended-release tablets) |
Contrave (naltrexone/bupropion) is a prescription tablet used for chronic weight management in adults who are overweight or obese with at least one weight-related condition, such as high blood pressure, type 2 diabetes, or high cholesterol. It combines two medications that work on areas of the brain involved in appetite and food cravings. It comes as an extended-release tablet plan that should be taken alongside a reduced-calorie diet and increased physical activity.
Directions
Contrave is started at a low dose and increased over four weeks. In Week 1, take one tablet each morning. In Week 2, take one tablet in the morning and one in the evening. In Week 3, take two tablets in the morning and one in the evening. By Week 4 and beyond, take two tablets in the morning and two in the evening (the full maintenance dose of 32 mg/360 mg daily).
Swallow tablets whole. Do not cut, crush, or chew them. Do not take this medication with a high-fat meal, as this can increase the amount of medication absorbed. After 12 weeks on the full dose, treatment may be stopped if at least 5% of body weight has not been lost.
Ingredients
The active ingredients in Contrave are naltrexone hydrochloride and bupropion hydrochloride. Inactive ingredients include microcrystalline cellulose, hydroxypropyl cellulose, lactose anhydrous, L-cysteine hydrochloride, crospovidone, magnesium stearate, hypromellose, edetate disodium, lactose monohydrate, colloidal silicon dioxide, Opadry II Blue, and FD and C Blue #2 aluminum lake.
Cautions
Before using this medication, you may want to consult a healthcare provider about the following:
- Any existing health conditions
- Any allergies
- A list of all medications currently being taken
Like other antidepressants, bupropion carries a boxed warning for increased risk of suicidal thinking and behavior, particularly in young adults under 25. Monitor for worsening mood or unusual behavior.
Contrave can lower the seizure threshold. The risk is higher with alcohol use, eating disorders, and certain medications.
Contrave may raise blood pressure or heart rate. Monitor regularly, especially during the first few months of treatment.
Cases of liver damage have been reported. Contact a healthcare provider if signs of liver problems develop, such as yellowing of the skin or eyes, dark urine, or stomach pain.
Bupropion can trigger acute narrow-angle glaucoma in susceptible individuals.
Patients with type 2 diabetes who use insulin or diabetes medications may experience low blood sugar. Adjustments to diabetes medications may be needed.
Do not drink alcohol while taking Contrave. Alcohol can increase seizure risk and cause serious reactions.
Contraindications
Avoid taking or using this medication if any of the following apply:
- Uncontrolled high blood pressure
- Personal history of seizure disorders
- History of anorexia nervosa or bulimia nervosa
- Currently taking other medications containing bupropion, such as Wellbutrin or Zyban
- Currently taking or recently stopped taking monoamine oxidase inhibitors (MAOIs); at least 14 days must pass between stopping an MAOI and starting Contrave
- Currently using opioid medications or going through opioid withdrawal
- Currently undergoing abrupt discontinuation of alcohol, benzodiazepines, barbiturates, or antiepileptic drugs
- Known allergy to any ingredients in the medication
Side Effects
Common side effects of Contrave include:
- Nausea
- Constipation
- Headache
- Vomiting
- Dizziness
- Insomnia
- Dry mouth
- Diarrhea
Serious side effects can include seizures, severe high blood pressure, and changes in mood or behavior, including thoughts of suicide or self-harm.
Liver injury, serious skin reactions such as Stevens-Johnson syndrome, and severe allergic reactions have also been reported.
Patients taking Contrave may also experience neuropsychiatric symptoms, including agitation, hostility, and unusual changes in thinking.
If any of these occur, stop taking Contrave and seek medical attention.
Frequently Asked Questions about Contrave
What is Contrave used for?
Contrave is a prescription extended-release tablet used with a reduced-calorie diet and increased physical activity to reduce excess body weight and help maintain weight loss in adults with obesity, or in adults with overweight who also have at least one weight-related medical condition. Its effect on cardiovascular morbidity and mortality has not been established.
What is in Contrave, and how does it work?
Contrave combines naltrexone, an opioid antagonist, with bupropion, a dopamine and norepinephrine reuptake inhibitor. Nonclinical data suggest the combination affects brain pathways involved in appetite and reward, but the exact neurochemical effects leading to weight loss are not fully understood.
How is Contrave taken?
Treatment is started gradually: 1 tablet each morning in Week 1, 1 tablet twice daily in Week 2, 2 tablets in the morning and 1 in the evening in Week 3, and then 2 tablets twice daily from Week 4 onward. Tablets should be swallowed whole, not cut, chewed, or crushed, and they should not be taken with a high-fat meal.
How do you know whether Contrave is working well enough?
The label says response should be checked after 12 weeks on the maintenance dose. If the patient has not lost at least 5% of baseline body weight by then, Contrave should be discontinued because meaningful long-term benefit is unlikely.
What are the most common side effects?
The most common side effects are nausea, constipation, headache, vomiting, dizziness, insomnia, dry mouth, and diarrhea. Nausea is the most frequently reported and is also the most common reason people stop treatment in trials.
What are the most important serious warnings?
Contrave carries a boxed warning about suicidal thoughts and behaviors because it contains bupropion. Other important risks include seizures, increased blood pressure or heart rate, opioid overdose risk and precipitated opioid withdrawal, liver injury, and serious allergic reactions; postmarketing reports also include DRESS, AGEP, and aseptic meningitis.
Who should not take Contrave?
It is contraindicated in people with uncontrolled hypertension, seizure disorder or past seizures, anorexia nervosa or bulimia, chronic opioid use or acute opioid withdrawal, abrupt discontinuation of alcohol, benzodiazepines, barbiturates, or antiepileptic drugs, use of other bupropion-containing products, MAOI use within 14 days, or allergy to its ingredients. People previously dependent on short-acting opioids should generally be opioid-free for at least 7 to 10 days before starting, and transitions from methadone or buprenorphine may require up to 2 weeks.
Are there important drug interactions?
Yes. Contrave should not be used with MAOIs, other bupropion-containing products, and generally not with other naltrexone-containing products. Opioid-containing pain, cough, cold, or diarrhea medicines may not work properly and can raise overdose or withdrawal risks, and Contrave can increase exposure to some CYP2D6-metabolized medicines such as certain antidepressants, antipsychotics, beta-blockers, and type 1C antiarrhythmics.
What if a dose is missed, and how should it be stored?
If a dose is missed, skip it and wait until the next regular dosing time; do not take more than one dose at a time. Store Contrave at room temperature, about 68°F to 77°F (20°C to 25°C), and keep it out of reach of children.
What should patients know about pregnancy, breastfeeding, children, and older adults?
Contrave is not recommended in pregnancy, and it should be stopped if pregnancy occurs because weight loss during pregnancy may cause fetal harm. Bupropion and naltrexone or their metabolites are present in human milk, so breastfeeding needs careful discussion. It is not recommended for patients under 18, and adults over 65 may be more sensitive to central nervous system effects and may need extra caution, especially if kidney function is reduced.
