Naltrexone

Naltrexone is used to treat narcotic drug or alcohol addiction.

Product dosage: 50mg
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Synonyms Naltrexone oral Nal trex own Revia

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 works 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 reduces cravings and helps maintain abstinence. Available in oral and extended-release injectable formulations, it offers flexibility in treatment regimens tailored to individual patient needs and compliance patterns.

Features

• Available as 50 mg oral tablets and 380 mg extended-release intramuscular injection
• Opioid receptor antagonist with high affinity for mu-opioid receptors
• Non-addictive and does not produce dependence or withdrawal upon discontinuation
• Hepatically metabolized via reduction and glucuronidation
• Bioavailability of oral formulation is 5–40% due to significant first-pass metabolism
• Extended-release formulation provides steady plasma concentrations for approximately 4 weeks

Benefits

• Reduces alcohol consumption and increases abstinence rates in alcohol use disorder
• Prevents opioid relapse by blocking euphoric effects if opioids are used
• Non-controlled substance with no abuse potential
• Can be administered in outpatient settings with appropriate monitoring
• Extended-release formulation improves adherence and reduces dosing frequency
• Compatible with comprehensive behavioral therapy programs

Common use

Naltrexone is FDA-approved for:

• Treatment of alcohol dependence in adults who have achieved and wish to maintain abstinence
• Prevention of relapse to opioid dependence following opioid detoxification in adults

Off-label uses include:

• Reduction of craving in other substance use disorders
• Adjunct treatment in certain impulse control disorders
• Investigationally in autoimmune conditions and fibromyalgia (low-dose naltrexone)

Dosage and direction

For alcohol dependence:

• Initial dose: 25 mg orally once daily; may increase to 50 mg orally once daily after 3–7 days
• Alternative regimen: 50 mg orally once daily without titration in patients without recent opioid use

For opioid dependence:

• Must be opioid-free for 7–10 days before initiation (longer for long-acting opioids)
• Initial dose: 25 mg orally; if no withdrawal signs, 50 mg orally once daily thereafter
• Verify opioid-free status with urine drug screen before initiation

Extended-release injection:

• 380 mg intramuscularly every 4 weeks in the gluteal muscle, alternating buttocks
• Must be administered by healthcare professional using provided safety needle

Precautions

• Risk of opioid overdose if patients attempt to overcome blockade with large opioid doses
• Hepatotoxicity: Monitor liver function tests at baseline and periodically during treatment
• Depression and suicidal ideation: Monitor for emergence or worsening of depression
• Avoid in acute hepatitis or liver failure; use caution in patients with active liver disease
• Injection site reactions may occur with extended-release formulation
• Not recommended during acute opioid withdrawal

Contraindications

• Current physiologic opioid dependence or positive urine opioid screen
• Acute opioid withdrawal syndrome
• Acute hepatitis or liver failure
• Hypersensitivity to naltrexone or any component of the formulation
• Failed naloxone challenge test
• Concurrent use of opioid analgesics, antitussives, or antidiarrheals

Possible side effects

Common (≥5%):

• Nausea (10%)
• Headache (7%)
• Dizziness (4%)
• Nervousness (4%)
• Fatigue (4%)
• Insomnia (3%)
• Anxiety (2%)

Less common:

• Abdominal pain/cramps
• Joint/muscle pain
• Rash
• Constipation
• Decreased energy
• Increased thirst

Extended-release injection specific:

• Injection site reactions (induration, tenderness, nodules, swelling)
• Eosinophilia

Drug interaction

• Opioid-containing medications: Blocked therapeutic effects
• Opioid dependence treatments: May precipitate withdrawal
• Hepatotoxic drugs: Increased risk of liver injury
• Thioridazine: Increased drowsiness
• CYP450 inhibitors/inducers: May alter naltrexone metabolism

Missed dose

Oral formulation:

• Take missed dose as soon as remembered unless close to next dose
• Do not double doses
• If multiple doses missed, contact prescriber before resuming

Extended-release injection:

• Administer missed injection as soon as possible
• Subsequent injections should be scheduled 4 weeks from last administered dose

Overdose

• No specific antidote exists
• Symptoms may include nausea, abdominal pain, dizziness, and injection site reactions
• Supportive care and symptomatic treatment
• Hemodialysis not effective due to large volume of distribution
• In case of suspected overdose, contact poison control center (1-800-222-1222)

Storage

• Oral tablets: Store at 20–25°C (68–77°F); excursions permitted to 15–30°C (59–86°F)
• Extended-release injection: Store in refrigerator at 2–8°C (36–46°F)
• Protect from light
• Keep in original container until administration
• Do not freeze
• Keep 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 must be completely free of opioids before initiation to avoid precipitated withdrawal. Individual response to medication may vary. Always follow the prescribing information provided with the medication and consult with a healthcare professional for personalized medical advice.

Reviews

Clinical studies demonstrate naltrexone’s efficacy in reducing alcohol consumption by 15–20% compared to placebo and increasing abstinence rates by approximately 10–15%. In opioid dependence, treatment with naltrexone results in significantly lower relapse rates (30–40% vs 60–70% with placebo) over 6-month periods. The extended-release formulation shows particularly improved outcomes due to enhanced adherence, with studies showing 90% of patients receiving all scheduled injections compared to 60% adherence with oral formulations. Most common reasons for discontinuation include nausea and injection site reactions, though these typically decrease with continued treatment.