[Durgical](https://durgical.com/en/) › [DurgiPedia](https://durgical.com/en/durgipedia/) › [Pharmacology](https://durgical.com/en/pharmacology/) › [Anti-obesity drugs](https://durgical.com/en/pharmacology/classes/anti-obesity-drugs/) › Naltrexone and bupropion

# Naltrexone and bupropion

## Anti-obesity drugs?

Anti-obesity drugs

## Pregnancy: avoid?

Not used in pregnancy; the prescriber is told at once if pregnancy occurs during treatment.

An extended-release combination of an opioid antagonist and an antidepressant that acts on hunger and reward circuits; used with diet and exercise in obesity.

Updated Nov 1, 2026

## Quick facts

**Group**
[Anti-obesity drugs](https://durgical.com/en/pharmacology/classes/anti-obesity-drugs/)

**Target**
Hypothalamic appetite and brain reward circuits (opioid receptors and dopamine/noradrenaline reuptake)

**Used for**
Chronic weight management

**Key effects**
Nausea · Constipation or diarrhoea · Headache

**Monitor**
Weight · Blood pressure and heart rate · Mood

**ATC**
A08AA62

No doses: the clinician sets them by the current guideline.

On this page

- The basics Mechanism of action
- Indications
- Adverse effects
- Pharmacokinetics
- Memory aid

- Clinical What the labels mean

- Safety Contraindications
- Key interactions
- What is monitored
- Administration and safety
- Pregnancy and breastfeeding
- Nursing care

- Study Test yourself

- Connections Connections

## Mechanism of action

Bupropion inhibits the reuptake of dopamine and noradrenaline; naltrexone blocks opioid receptors. Together they are thought to act on the hypothalamic hunger centre and the mesolimbic reward system, reducing appetite and food cravings.

- Bupropion raises dopamine and noradrenaline signalling
- Naltrexone blocks opioid receptors
- Hunger centre and reward system are damped
- Less appetite and fewer food cravings

## Indications

- Chronic weight management with a reduced-calorie diet and exercise in obesity, or overweight with weight-related conditions [Obesity →](https://durgical.com/en/conditions/obesity/)

## Adverse effects

### Common

- Nausea (very common at the start), vomiting
- Constipation or diarrhoea
- Headache, dizziness, insomnia
- Dry mouth, altered taste
- Tremor, sweating, flushing, ringing in the ears

### Serious (rare, important)

- Suicidal thoughts and changes in mood or behaviour (boxed warning for bupropion)
- Seizures
- Raised blood pressure and heart rate
- Angle-closure glaucoma
- Serious allergic and skin reactions
- Precipitated opioid withdrawal, or overdose if opioids are taken to overcome the block

## Contraindications

- Seizure disorder, or anorexia nervosa or bulimia
- Uncontrolled high blood pressure
- Chronic opioid use, opioid agonist treatment or acute opioid withdrawal
- Abrupt stopping of alcohol, benzodiazepines, sedatives or antiseizure drugs
- Use of an MAO inhibitor in the past 14 days
- Other bupropion-containing products

## Key interactions

**Opioid analgesics and opioid-containing cough or antidiarrhoeal medicines**
Blocked by naltrexone; may precipitate withdrawal; avoided.

**MAO inhibitors (including linezolid and methylene blue)**
Contraindicated; at least 14 days are left between them.

**Other bupropion products**
Duplicate bupropion raises seizure risk.

**Alcohol**
Worsens side effects.

## What is monitored

- Weight, to judge whether treatment continues
- Blood pressure and heart rate
- Mood, suicidal thoughts and behaviour, especially early and after dose changes
- Eye pain or vision changes

## Administration and safety

- Oral extended-release tablets, swallowed whole, not split, chewed or crushed.
- Started low and increased weekly over the first weeks; taken twice a day.
- Not taken with a high-fat meal.
- Look-alike risk: not given together with other bupropion products (antidepressant or smoking-cessation forms).

## Pregnancy and breastfeeding

Not used in pregnancy; the prescriber is told at once if pregnancy occurs during treatment.

## Nursing care

- Before: seizure history, eating disorders, blood pressure, opioid use, MAOI use.
- During: blood pressure, pulse, mood and suicidal thinking.
- Teach that opioid pain medicines will not work well and that trying to overcome the block can cause overdose.
- Teach to report seizures, eye pain or rash immediately.

## Pharmacokinetics

**Absorption**
Oral extended-release tablet; it is not taken with a high-fat meal.

## Memory aid

NB = 'No Binge': Naltrexone blocks the opioid 'reward' of eating, Bupropion pushes the hunger centre to stop. Watch the B-side: seizures, BP, blues (mood).

## Test yourself

Think of the answer, then tap the question to see it.

## Why can't a patient on naltrexone-bupropion receive usual opioid analgesia?

Naltrexone blocks opioid receptors, so opioids work poorly and may precipitate withdrawal.

## Which seizure-related conditions contraindicate naltrexone-bupropion?

Seizure disorder, eating disorders (anorexia, bulimia) or abrupt alcohol or benzodiazepine withdrawal.

## Which boxed warning comes from the bupropion component?

Suicidal thoughts and behaviour, especially in young people.

[Add to my cards (3)](https://durgical.app/estudiar/?add=/en/pharmacology/naltrexone-and-bupropion/)

[More Pharmacology questions →](https://durgical.com/en/practice/?f=pharmacology)

## What the labels mean

**Pregnancy: avoid**
Not used in pregnancy; the prescriber is told at once if pregnancy occurs during treatment.

## Connections

## Related drugs 3

- [Naltrexone](https://durgical.com/en/pharmacology/naltrexone/)
- [Bupropion](https://durgical.com/en/pharmacology/bupropion/)
- [Phentermine and topiramate](https://durgical.com/en/pharmacology/phentermine-and-topiramate/)

## Related conditions 1

- [Obesity](https://durgical.com/en/conditions/obesity/)

[← Back to the class: Anti-obesity drugs](https://durgical.com/en/pharmacology/classes/anti-obesity-drugs/)

Educational content on how drugs work; not a prescribing guide and no substitute for a health professional's advice. No doses are given.

Sources: [Naltrexone and Bupropion: MedlinePlus Drug Information](https://medlineplus.gov/druginfo/meds/a619020.html) (MedlinePlus (U.S. National Library of Medicine), 2019); [ATCDDD - ATC/DDD Index](https://atcddd.fhi.no/atc_ddd_index/?code=A08AA62) (WHO Collaborating Centre for Drug Statistics Methodology, 2026).

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Representative model, for educational purposes only.

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License: CC BY 4.0 (https://creativecommons.org/licenses/by/4.0/). Cite as: DurgiPedia (durgical.com), https://durgical.com/en/pharmacology/naltrexone-and-bupropion/
