Naltrexone: Effective Opioid and Alcohol Dependence Management
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Synonyms | |||
Naltrexone is a competitive opioid antagonist medication indicated for the management of alcohol dependence and the prevention of relapse to opioid dependence following opioid detoxification. It works by binding to opioid receptors in the brain, blocking the euphoric and sedative effects of opioids and reducing the craving for alcohol. Available in oral tablet and extended-release injectable formulations, naltrexone represents a cornerstone medication in comprehensive addiction treatment protocols when used as part of a complete treatment program that includes counseling and psychosocial support.
Features
- Competitive opioid receptor antagonist
- Available in 50 mg oral tablets and 380 mg extended-release intramuscular injection
- Blocks euphoric effects of exogenous opioids
- Reduces alcohol craving and consumption
- Non-addictive with no abuse potential
- Multiple administration options for treatment flexibility
Benefits
- Prevents relapse in opioid-dependent individuals by blocking opioid effects
- Reduces alcohol consumption and increases abstinence rates in alcohol use disorder
- Eliminates physiological reinforcement from substance use
- Facilitates engagement in psychosocial therapies
- Provides extended protection with monthly injection formulation
- Non-controlled medication with minimal abuse liability
Common use
Naltrexone is primarily prescribed for two FDA-approved indications: treatment of alcohol dependence in adults who have achieved abstinence and prevention of relapse to opioid dependence following opioid detoxification. Off-label uses include treatment of other impulse control disorders, though evidence supporting these applications is more limited. The medication is typically initiated after complete opioid detoxification and a 7-10 day opioid-free period to prevent precipitated withdrawal. For alcohol dependence treatment, naltrexone may be started once abstinence is achieved.
Dosage and direction
Oral formulation: The recommended dose for both alcohol dependence and opioid dependence is 50 mg once daily. Treatment may be initiated with 25 mg for the first dose to assess tolerability. Some protocols utilize 100 mg every other day or 150 mg every third day for improved adherence.
Extended-release injection: 380 mg delivered intramuscularly in the gluteal muscle every 4 weeks or once monthly. The injection must be administered by a healthcare professional using the provided specific needles.
Dosing should be consistent whether taken with or without food. Treatment duration typically ranges from 3 to 12 months based on individual response and treatment goals.
Precautions
Patients must be completely free of opioids for 7-10 days before initiating naltrexone to avoid precipitated withdrawal. Liver function tests should be performed before initiation and periodically during treatment due to dose-related hepatotoxicity risk. Use with caution in patients with renal impairment. Naltrexone may increase sensitivity to opioids if attempted after discontinuation. Patients should carry medical identification indicating they are taking naltrexone. Emergency personnel should be informed that larger than usual opioid doses may be needed for pain management.
Contraindications
Patients receiving opioid analgesics, currently dependent on opioids, in acute opioid withdrawal, or with positive urine screen for opioids. Patients with acute hepatitis or liver failure. History of hypersensitivity to naltrexone or any component of the formulation. The extended-release formulation is additionally contraindicated in patients with thrombocytopenia or any coagulation disorder.
Possible side effects
Common (≥5%): Nausea (10%), headache (7%), dizziness (4-10%), nervousness (4-10%), fatigue (4-10%), insomnia (3-10%), anxiety (2-10%), abdominal pain/cramps (3-10%)
Less common (1-5%): vomiting, decreased appetite, joint/muscle pain, increased thirst, constipation, rhinorrhea, sneezing
Rare (<1%): hepatotoxicity (dose-related), eosinophilic pneumonia, depression, suicidal ideation, injection site reactions (with depot formulation)
Most side effects are dose-related and tend to diminish within a few days to weeks of continued therapy.
Drug interaction
Naltrexone may precipitate acute withdrawal in patients receiving opioid agonists including methadone, buprenorphine, codeine, hydrocodone, oxycodone, and morphine. May diminish efficacy of opioid-containing medications, including antitussives and antidiarrheals. Theoretical interaction with opioid-like medications such as dextromethorphan. Potential pharmacodynamic interaction with other centrally-acting medications. No clinically significant pharmacokinetic interactions with disulfiram or acamprosate.
Missed dose
If a dose is missed, it should be taken as soon as remembered. However, if it is almost time for the next dose, the missed dose should be skipped and the regular dosing schedule resumed. Patients should not take double or extra doses. For the extended-release injection, contact the healthcare provider to reschedule the injection as soon as possible.
Overdose
No specific antidote exists for naltrexone overdose. Symptoms may include nausea, abdominal pain, dizziness, and sedation. In cases of massive overdose, injection site necrosis may occur with the depot formulation. Management is supportive and symptomatic. Hemodialysis is not effective due to high protein binding and large volume of distribution. Because naltrexone blocks opioid receptors, higher than usual doses of opioids may be required for pain management in emergency situations.
Storage
Store at room temperature (20-25°C or 68-77°F). Oral tablets should be kept in their original container with the lid tightly closed. Protect from light and moisture. The extended-release injection should be stored refrigerated at 2-8°C (36-46°F) and protected from light. The suspension should be brought to room temperature for approximately 45 minutes before administration. Do not freeze. Keep all medications out of reach of children and pets.
Disclaimer
This information is for educational purposes only and does not constitute medical advice. Naltrexone should only be used under the supervision of a qualified healthcare provider. Patients should not initiate or discontinue naltrexone without medical consultation. Individual response to medication may vary. Always follow the prescribed dosage and instructions provided by your healthcare provider.
Reviews
Clinical studies demonstrate naltrexone’s efficacy in reducing relapse rates in opioid dependence by approximately 50% compared to placebo when combined with psychosocial support. Meta-analyses show naltrexone reduces risk of heavy drinking by 83% and increases abstinence rates by 50% in alcohol use disorder. The extended-release formulation shows superior adherence rates compared to oral administration. Patient-reported outcomes indicate improved quality of life measures and treatment satisfaction scores. Real-world evidence supports naltrexone’s role as an effective component of comprehensive addiction treatment programs.