What are the indications for Naltrexone (opioid receptor antagonist)?

From the Guidelines

Naltrexone is indicated for the treatment of alcohol use disorder, opioid use disorder, and certain behavioral addictions, as well as for managing obesity and aiding in smoking cessation, as supported by the most recent evidence from 2022 1.

Indications for Naltrexone

• Alcohol use disorder: reduces cravings and the pleasurable effects of alcohol
• Opioid use disorder: prevents relapse after complete detoxification by blocking the euphoric effects of opioids
• Behavioral addictions: sometimes used off-label for impulse control disorders, eating disorders, and self-injurious behaviors
• Obesity management: naltrexone-bupropion ER is used for weight loss in adults with obesity, with a recommended titration schedule and maintenance dose of 2 tablets twice per day 1
• Smoking cessation: limited data suggests that naltrexone-bupropion ER may be effective in reducing nicotine use and mitigating associated weight gain 1

Important Considerations

• Patients must be opioid-free for 7-10 days before starting naltrexone to avoid precipitating withdrawal
• Naltrexone works by competitively binding to opioid receptors without activating them, thereby blocking the effects of endogenous and exogenous opioids
• Common side effects include nausea, headache, dizziness, and liver enzyme elevations
• Naltrexone is contraindicated in patients with acute hepatitis, liver failure, or those currently taking opioid medications, and requires liver function monitoring during treatment
• The combination of naltrexone and bupropion should be avoided in patients with uncontrolled hypertension, and patients should be observed for neuropsychiatric adverse effects, including suicidal thoughts and behaviors, especially in individuals younger than 24 years 1

From the FDA Drug Label

Naltrexone hydrochloride tablets USP 50 mg is indicated in the treatment of alcohol dependence and for the blockade of the effects of exogenously administered opioids. A dose of 50 mg once daily is recommended for most patients Treatment of Opioid Dependence Treatment should be initiated with an initial dose of 25 mg of naltrexone hydrochloride. If no withdrawal signs occur, the patient may be started on 50 mg a day thereafter

Les indications pour le Naltrexone sont :

• Dépendance à l'alcool : 50 mg par jour
• Dépendance aux opioïdes : 25 mg le premier jour, puis 50 mg par jour si aucun signe de sevrage n'apparaît 2 2

From the Research

Naltrexone Indications

Naltrexone is an opioid receptor antagonist with various indications, including:

• Opioid dependence: Naltrexone blocks the reinforcing effects of opioids and reduces craving 3
• Alcohol dependence: Naltrexone reduces alcohol consumption and craving, although its effectiveness is less evident than in opioid dependence 3, 4
• Eating disorders: Naltrexone has been found useful in the treatment of eating disorders, possibly due to its effect on endogenous opioids 5

Off-Label Uses

Naltrexone may also be used off-label for:

• Pruritus in cholestasis: Naltrexone has been proposed as a possible treatment for pruritus in cholestasis, although its pharmacokinetic behavior in liver disease needs to be considered 6
• Major depression: However, naltrexone may worsen co-morbid major depression in some patients, and its use in this context is not well established 7

Important Considerations

When using naltrexone, it is essential to consider:

• Liver function: Naltrexone's pharmacokinetic behavior is altered in liver cirrhosis, which may affect its systemic availability 6
• Dosing and formulation: Naltrexone is available in various formulations, including oral, implant, and injectable depot formulations, which may affect its efficacy and safety 3