Naltrexone/bupropion Research Reference

Catalog classification, reference sizes, lab math links, and source-backed data. Educational use only — not medical advice.

Researched for: PepTools vendor-neutral scientific reference catalog

Prescription anti-obesity fixed-dose combination; opioid antagonist and aminoketone antidepressant compound Reference approved

Also known as: Contrave, naltrexone hydrochloride/bupropion hydrochloride, naltrexone HCl/bupropion HCl, naltrexone-bupropion extended-release

Quick Facts

Reference Sizes
8 mg naltrexone hydrochloride / 90 mg bupropion hydrochloride extended-release tablet, 7-tablet bottle, 120-tablet bottle
Components
Naltrexone hydrochloride 8 mg per extended-release tablet + Bupropion hydrochloride 90 mg per extended-release tablet
Storage
Store at 25 °C (77 °F); excursions permitted to 15–30 °C (59–86 °F) under USP controlled-room-temperature conditions.
Solubility
Naltrexone hydrochloride is soluble in water at approximately 100 mg/mL; bupropion hydrochloride is described in the FDA labeling as highly soluble in water. The finished extended-release tablet is a formulated solid dosage form, and these component solubility values should not be interpreted as a solubility value for the intact tablet.

Blend Components

This entry is a multi-compound blend. Each component can be opened individually in the reconstitution calculator.

Component
Naltrexone hydrochloride 8 mg per extended-release tablet
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Component
Bupropion hydrochloride 90 mg per extended-release tablet
Calculator Profile
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Component amounts shown are arithmetic starters based on equal distribution. Edit values in the calculator before saving.

Catalog Description

Naltrexone/bupropion is an oral extended-release tablet formulation containing the opioid antagonist naltrexone and the aminoketone antidepressant bupropion. U.S. labeling indicates use with a reduced-calorie diet and increased physical activity for long-term weight reduction and maintenance in adults with obesity or adults with overweight plus at least one weight-related comorbid condition. The exact neurochemical basis of the weight-loss effect is not fully understood; labeling describes effects involving hypothalamic appetite-regulation pathways and mesolimbic reward pathways.

Catalog descriptions reflect research context only. Not a medical claim or treatment recommendation.

Research Profile

Half-Life
Following single oral administration of the extended-release combination, mean elimination half-life is approximately 5 hours for naltrexone and approximately 21 hours for bupropion. The active naltrexone metabolite 6-beta-naltrexol and active bupropion metabolites have different and generally longer accumulation characteristics; bupropion metabolites reach steady-state concentrations at approximately one week with twice-daily administration.
Onset
After a single oral administration of two tablets, mean time to peak plasma concentration is approximately 2 hours for naltrexone and 3 hours for bupropion. The clinical weight-management response is evaluated over weeks; U.S. labeling specifies assessment after 12 weeks at the maintenance dosage, corresponding to approximately 16 weeks from treatment initiation.
Administration Routes (Research)
oral

Reported Research Effects

Data source: Primary literature, regulator records, trial registries, and identity-specific evidence search

Reflects preclinical/research literature context only. Not a medical claim, dosing instruction, or treatment recommendation.

Research Notes

The FDA-approved strength is 8 mg naltrexone hydrochloride/90 mg bupropion hydrochloride per extended-release tablet. The labeled dose-escalation regimen progresses over four weeks to a maximum of four tablets per day, divided into morning and evening doses; this is recorded here as regulatory reference information, not individualized dosing guidance. Tablets should be swallowed whole and not cut, chewed, or crushed. The product should not be taken with high-fat meals because systemic exposure to both components increases. Coadministration with other bupropion-containing products is contraindicated, and coadministration with other naltrexone-containing products is not recommended. The cardiovascular morbidity and mortality effect has not been established. Initial U.S. approval was in 2014; the FDA label used for this record was revised in November 2025.

Supplementary research context only. Not medical advice or a treatment recommendation.

Registry Identifiers

FDA NDA 200063; RxCUI 1551468 for naltrexone HCl 8 mg/bupropion HCl 90 mg 12-hour extended-release oral tablet; RxCUI 1551474 for Contrave 8 mg/90 mg 12-hour extended-release oral tablet; NDC 51267-890-07 and 51267-890-99; UNII naltrexone hydrochloride Z6375YW9SF; UNII bupropion hydrochloride ZG7E5POY8O

Source-Backed Observations

The product is a fixed-dose combination rather than a single discrete molecular entity. Each tablet is a trilayer, film-coated, extended-release tablet containing 8 mg naltrexone hydrochloride and 90 mg bupropion hydrochloride. The current U.S. label identifies oral administration only. Common labeled adverse reactions include nausea, constipation, headache, vomiting, dizziness, insomnia, dry mouth, and diarrhea. Important labeled risks include seizures, increases in blood pressure or heart rate, hepatotoxicity, and suicidal thoughts or behaviors associated with the bupropion component.

Reflects published research. Educational reference — not a recommendation for use.

Sources

CONTRAVE (naltrexone hydrochloride and bupropion hydrochloride) extended-release tablets: U.S. Prescribing Information, revised November 2025
https://www.accessdata.fda.gov/drugsatfda_docs/label/2025/200063s024s026lbl.pdf (accessed 2026-09-12)
DailyMed: CONTRAVE extended-release naltrexone hydrochloride and bupropion hydrochloride tablet
https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=485ff360-32c8-11df-928b-0002a5d5c51b (accessed 2026-09-12)
NaltrexoneBupropion: PubChem Reference Collection
https://pubchem.ncbi.nlm.nih.gov/compound/NaltrexoneBupropion (accessed 2026-09-12)

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Research Use Only. All content is for educational and research reference only. Not medical advice, a treatment recommendation, or guidance on human use. Compounds are not FDA-approved drugs unless specifically noted.

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