Naltrexone

Indications
 Oral
Opioid dependence
Adult: As hydrochloride: Initially, 25 mg; increase to 50 mg daily if no withdrawal signs occur. Maintenance: 350 mg wkly given as 50 mg daily or divided in 3 doses (given on 3 days of the wk) for improved compliance.
Oral
Adjunct in alcohol dependence
Adult: As hydrochloride: 50 mg daily.
Intramuscular
Adjunct in alcohol dependence
Adult: 380 mg once every 4 wk.
Contraindications
 Patients concurrently dependent on opioids; acute hepatitis or hepatic failure; acute opioid withdrawal; patients on therapeutic opioid analgesics.
Warnings / Precautions
 Hepatic or renal impairment. Monitor LFTs regularly. Patients should be opioid-free for at least 7-10 days prior to initiating naltrexone therapy. Strictly warn patients against the use of opioids while on naltrexone. Monitor for inj-site reactions. Pregnancy, lactation. History of bleeding disorders (including thrombocytopenia).
Adverse Reactions
 Abdominal pain, nausea, vomiting; anxiety, insomnia, lethargy, headache, musculoskeletal pain; anorexia, diarrhoea, constipation; increased thirst; chest pain; chills, dizziness; sexual dysfunction; rash, liver function abnormalities and reversible idiopathic thrombocytopenia. Inj-site reactions.
Overdose Reactions
 Symptoms: Clonic-tonic convulsions and respiratory failure. Management: Supportive and symptomatic.
Drug Interactions
 May reduce effects of opiate-containing preparations e.g. those used for cough and cold, diarrhoea and pain. Increased or decreased serum levels with drugs that alter hepatic metabolism. Potentially increased hepatotoxic effects with disulfiram. Increased risk of naltrexone-induced lethargy and somnolence with thioridazine. May increase insulin requirements.
See Below for More naltrexone Drug Interactions
Lab Interactions
 May interfere in the detection of urinary opiates using some immunoassay or enzymatic methods.
Mechanism of Actions
 Naltrexone acts as a competitive antagonist at opioid receptor sites. It blocks the action of opioids and precipitates withdrawal symptoms in opioid-dependent individuals.
Absorption: Well absorbed from the GI tract. Peak plasma concentrations after about 1 hr.
Distribution: 20% bound to plasma proteins.
Metabolism: Extensively metabolised in the lvier. Undergoes considerable 1st-pass metabolism and may undergo enterohepatic recycling.
Excretion: Via urine (as <1% unchanged drug and as metabolites). Elimination half-life: Approx 4 hr.
Administration
 May be taken with or without food.
Storage Conditions
 Intramuscular: Store at 2-8°C (36-46°F); do not freeze. Oral: Store at 20-25°C (68-77°F).
ATC Classification
 N07BB04 - naltrexone ; Belongs to the class of drugs used in the management of alcohol dependence.
Storage
 Intramuscular: Store at 2-8°C (36-46°F); do not freeze. Oral: Store at 20-25°C (68-77°F).
Available As
  • Naltrexone 50 mg

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