Naltrexone: Effective Opioid and Alcohol Dependence Management
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Synonyms | |||
Naltrexone is an opioid antagonist medication primarily indicated for the management of alcohol dependence and the prevention of relapse to opioid dependence following detoxification. It functions by competitively binding to opioid receptors, thereby blocking the euphoric and sedative effects of opioids. When used as part of a comprehensive treatment program that includes counseling and psychosocial support, naltrexone significantly supports sustained recovery. Available in oral tablet and extended-release injectable formulations, it offers flexible dosing options tailored to individual patient needs and compliance considerations.
Features
- Active ingredient: Naltrexone hydrochloride
- Available formulations: 50 mg oral tablets; 380 mg extended-release intramuscular injection
- Mechanism: Pure opioid antagonist with high affinity for mu-opioid receptors
- Bioavailability: Oral: 5–40% (extensive first-pass metabolism); IM: sustained release over approximately 4 weeks
- Half-life: Oral: 4–13 hours; Extended-release injection: 5–10 days (depending on release kinetics)
- Excretion: Primarily renal (with metabolites)
Benefits
- Reduces craving for alcohol and decreases heavy drinking days in alcohol use disorder
- Blocks the euphoric effects of opioids, discouraging recreational use and supporting abstinence
- Non-addictive with no potential for abuse or dependence
- Available in long-acting formulation to improve adherence and reduce dosing frequency
- Can be integrated into comprehensive treatment plans including behavioral therapy
- Helps restore neurochemical balance disrupted by chronic substance use
Common use
Naltrexone is FDA-approved for the treatment of alcohol dependence in patients who are able to abstain from alcohol in an outpatient setting prior to initiation of therapy. It is also indicated for the prevention of relapse to opioid dependence following opioid detoxification. Off-label uses include the treatment of other impulse control disorders, though evidence is less established. Treatment is typically initiated after a minimum 7–10 day opioid-free period to avoid precipitating withdrawal.
Dosage and direction
For alcohol dependence:
Initiate with 25 mg orally once daily; increase to 50 mg orally once daily after assessing tolerability. Alternatively, 380 mg intramuscular injection every 4 weeks, administered by healthcare professional.
For opioid dependence:
Begin with 25 mg orally; if no withdrawal signs appear, administer 50 mg daily thereafter. Alternatively, 380 mg IM every 4 weeks, only after patient is opioid-free for at least 7–10 days.
Dosing must be individualized based on patient response, tolerability, and treatment setting. Administer oral tablets with food or antacids to minimize gastrointestinal upset.
Precautions
Hepatotoxicity: Monitor liver function tests at baseline and periodically during treatment. Use with caution in patients with hepatic impairment.
Depression and suicidality: Monitor for emergence or worsening of depression or suicidal ideation.
Precipitation of opioid withdrawal: Ensure patient is opioid-free before initiation to avoid acute withdrawal syndrome.
Injection-site reactions: Monitor for nodules, swelling, or other local reactions with extended-release formulation.
Accidental opioid overdose: Patients may have reduced tolerance; overdose risk is increased if opioids are used after naltrexone discontinuation.
Contraindications
- Patients receiving opioid analgesics, currently dependent on opioids, or in acute opioid withdrawal
- Positive urine screen for opioids
- Acute hepatitis or liver failure
- History of hypersensitivity to naltrexone or any component of the formulation
- Failure to pass a naloxone challenge test (if applicable)
Possible side effect
Common (≥5%): Nausea, headache, dizziness, insomnia, anxiety, vomiting
Less common (1–5%): Loss of appetite, muscle cramps, joint pain, increased thirst, drowsiness
Rare (<1%): Hepatotoxicity, allergic reactions, injection site reactions (for IM formulation), depression, suicidal ideation
Side effects are generally dose-related and often diminish with continued therapy. Most are mild to moderate in severity.
Drug interaction
Opioids: Naltrexone blocks therapeutic effects of opioid analgesics; avoid concomitant use.
Opioid-containing medications: Including some cough suppressants and antidiarrheals; effects will be blocked.
Disulfiram: Increased risk of hepatotoxicity; avoid combination.
Thioridazine: May increase drowsiness; monitor closely.
CYP450 inducers/inhibitors: May alter naltrexone metabolism; clinical significance uncertain.
Missed dose
If a dose is missed, take it as soon as remembered unless it is almost time for the next dose. Do not double the dose. For the extended-release injection, contact the healthcare provider to reschedule administration. Consistent dosing is important for maintaining receptor blockade.
Overdose
No specific antidote exists. Symptoms may include nausea, abdominal pain, dizziness, and injection site reactions (for IM formulation). Management is supportive and symptomatic. Hemodialysis is not effective due to high protein binding. In cases of suspected overdose, seek immediate medical attention.
Storage
Store at room temperature (20–25°C/68–77°F). Oral tablets should be kept in a tightly closed container. Protect from light and moisture. Extended-release injection vials should be stored refrigerated (2–8°C/36–46°F); allow to reach room temperature before administration. Keep out of reach of children and pets.
Disclaimer
This information is for educational purposes only and does not constitute medical advice. Always consult a qualified healthcare provider for diagnosis and individualized treatment recommendations. Do not initiate, adjust, or discontinue medication without professional supervision.
Reviews
“Naltrexone has been transformative in our addiction medicine practice. The extended-release formulation particularly improves compliance in patients with unstable living situations.” — Addiction Specialist, 12 years experience
“While effective, careful patient selection and thorough education about precipitated withdrawal are absolutely essential for safe use.” — Clinical Pharmacist, Substance Use Disorder Clinic
“We’ve observed significant reductions in relapse rates when naltrexone is combined with cognitive behavioral therapy. The oral formulation allows for flexible dosing during early recovery.” — Psychiatric Researcher