Naltrexone

Naltrexone is used to prevent people who have been addicted to certain drugs (opiates) from taking them again. It is used as part of a complete treatment program for drug abuse (e.g., compliance monitoring, counseling, behavioral contract, lifestyle changes). This medication must not be used in people currently taking opiates, including methadone. Doing so can cause sudden withdrawal symptoms.

Naltrexone belongs to a class of drugs known as opiate antagonists. It works in the brain to prevent opiate effects (e.g., feelings of well-being, pain relief).

It also decreases the desire to take opiates.

Naltrexone is also used to treat alcohol abuse. It can help people drink less alcohol or stop drinking altogether. It also decreases the desire to drink alcohol when used with a treatment program that includes counseling, support, and lifestyle changes.

Naltrexone is available under the following different brand names: ReVia, Vivitrol, and Depade.

Dosage Forms & Strengths

Tablet

• 50 mg

Microspheres for IM injection

• 380 mg

Oral granules

• 4 mg//packet

Dosage Considerations – Should be Given as Follows:

Asthma

• Adult: 10 mg (single 10-mg tablet) orally once daily in evening
• Children under 12 months: Safety and efficacy not established
• Children 12-24 months: 4 mg (granules) orally once daily in evening
• Children 2-6 years: 4 mg (chewable tablet or granules) orally once daily in evening
• Children 6-15 years: 5 mg (chewable tablet) orally once daily in evening
• Children over 15 years: 10 mg (conventional tablet) orally once daily in evening

Exercise-Induced Bronchospasm

• 7.5 mg/day orally at bedtime; increase by 7.5-15 mg/day no more frequently than every 1-2 weeks; not to exceed 60 mg/day

Post-traumatic Stress Disorder (Off-label)

Prophylaxis

• Adult: 10 mg orally 2 hours before exercise; do not take additional dose within 24 hours
• Children 6-15 years: 5 mg (chewable tablet) orally 2 hours before exercise; do not take additional dose within 24 hours
• Children over 15 years: 10 mg orally 2 hours before exercise; do not take additional dose within 24 hours
• If taking drug for another indication, do not take additional dose to prevent EIB

Allergic or Perennial Rhinitis

• Adult: 10 mg (single 10-mg tablet) orally once daily
• Children under 6 months: Safety and efficacy not established
• Children 6-24 months: 4 mg (granules) orally once daily
• Children 2-6 years: 4 mg (chewable tablet or granules) orally once daily
• Children 6-15 years: 5 mg (chewable tablet) orally once daily
• Children over 15 years: 10 mg (conventional tablet) orally once daily

Seasonal Allergic Rhinitis, Pediatric

• Children under 2 years: Safety and efficacy not established
• Children 2-6 years: 5 mg (chewable tablet) or 4 mg (granules) orally once daily
• Children 6-15 years: 5 mg (chewable tablet) orally once daily
• Children over 15 years: 10 mg (conventional tablet) orally once daily

Administration

• Patients aged 12 years and older with both asthma and allergic rhinitis: 1 dose orally at bedtime
• Patients with allergic rhinitis: Dosing time may be individualized to patient needs
• Granules may be taken directly; mixed in applesauce, carrots, rice, or ice cream; or dissolved in 5 mL of breast milk or baby formula (administer within 15 minutes of opening)

Some adverse drug reactions vary by age group

Common side effects of naltrexone include:

• Headache (similar incidence to placebo)
• Abdominal pain
• Eczema
• Influenza
• Laryngitis
• Sore throat
• Viral infection
• Wheezing
• Dental pain
• Dizziness
• Indigestion
• Elevated liver function tests
• Fever
• Gastroenteritis
• Nasal congestion
• Ear infection
• Rash
• Hives
• Bronchitis
• Cough
• Sinus infection (sinusitis)
• Upper respiratory tract infection

Less common side effects of naltrexone include:

• Allergic granulomatous angiitis (Churg-Strauss syndrome; rare)
• Cholestatic hepatitis (rare)
• Aggressive behavior, altered behavior, suicidal thoughts

Postmarketing side effects of naltrexone reported include:

• Hematologic: Increased bleeding tendency, thrombocytopenia
• Immunologic: Hypersensitivity reactions (e.g., anaphylaxis, hepatic eosinophilic infiltration)
• Psychiatric: Agitation, including aggressive behavior or hostility, anxiousness, depression, disorientation, dream abnormalities, hallucinations, insomnia, irritability, restlessness, sleepwalking, suicidal thinking and behavior (including suicide), tremor
• Neurologic: Drowsiness, numbness and tingling, reduced sense of touch, seizures
• Cardiac: Palpitations
• Respiratory, thoracic, mediastinal: nosebleed, pulmonary eosinophilia
• Gastrointestinal: Diarrhea, indigestion, nausea, pancreatitis, vomiting
• Hepatobiliary: Cases of cholestatic hepatitis, hepatocellular liver injury, and mixed-pattern liver injury have been reported, mostly occurring in combination with other confounding factors (e.g., use of other medications, administration to patients who had underlying potential for liver disease [e.g., alcohol use or other forms of hepatitis])
• Dermatologic: Skin swelling, bruising, erythema multiforme, erythema nodosum, itching, hives
• Musculoskeletal: Joint pain, muscle pain (including muscle cramps)
• General: Swelling (edema)

This document does not contain all possible side effects and others may occur. Check with your physician for additional information about side effects.

If your doctor has directed you to use this medication, your doctor or pharmacist may already be aware of any possible drug interactions and may be monitoring you for them. Do not start, stop, or change the dosage of any medicine before checking with your doctor, health care provider or pharmacist first.

• Severe Interactions of naltrexone include:
  • None
• Serious Interactions of naltrexone include:
  • alfentanil
  • belladonna and opium
  • butorphanol
  • codeine
  • difenoxin hcl
  • diphenoxylate hcl
  • hydrocodone
  • hydromorphone
  • levorphanol
  • meperidine
  • methadone
  • morphine
  • nalbuphine
  • naloxegol
  • opium tincture
  • oxycodone
  • oxymorphone
  • pentazocine
  • sufentanil
  • tapentadol
• Moderate interactions of naltrexone include:
  • acamprosate
  • buprenorphine
  • buprenorphine buccal
  • dronabinol
  • nabilone
  • tramadol
• Mild Interactions of naltrexone include:
  • None.

This information does not contain all possible interactions or adverse effects. Therefore, before using this product, tell your doctor or pharmacist of all the products you use. Keep a list of all your medications with you, and share this information with your doctor and pharmacist. Check with your health care professional or doctor for additional medical advice, or if you have health questions, concerns or for more information about this medicine.

Warnings

• This medication contains naltrexone. Do not take ReVia, Vivitrol, or Depade if you are allergic to naltrexone or any ingredients contained in this drug
• Keep out of reach of children. In case of overdose, get medical help or contact a Poison Control Center immediately

Contraindications

• Patients who are on opioid analgesics, are opioid-dependent (e.g., opioid agonists [methadone], opioid partial agonists [buprenorphine]), are in acute opioid withdrawal, have positive urine test for opioids, or fail to pass naloxone challenge
• Hypersensitivity

Effects of Drug Abuse

• No information available

Short-Term Effects

• Injection may cause severe injection-site reactions (e.g., cellulitis, necrosis, hematoma)
• See "What Are Side Effects Associated with Using Naltrexone?"

Long-Term Effects

• See "What Are Side Effects Associated with Using Naltrexone?"

Cautions

• Depression, suicide, and suicidality cited in postmarketing reports; causal relation not demonstrated
• Vulnerability to opioid overdose: Patients should be alerted that they may be more sensitive to opioids, even at lower doses, after discontinuance of naltrexone
• Opioid withdrawal precipitated abruptly by administration of opioid antagonist to opioid-dependent patient may result in withdrawal syndrome severe enough to necessitate hospitalization
• Risk of hepatotoxicity with increasing doses; dose related hepatocellular injury; discontinue therapy if signs/symptoms of acute hepatitis develop
• Injection may cause severe injection-site reactions (e.g., cellulitis, necrosis, hematoma)
• Injectable microspheres are for intramuscular (IM) use only; inadvertent subcutaneous/intravenous (SC/IV) administration may increase risk of severe injection-site reactions
• Cases of eosinophilic pneumonia reported; consider in patients with symptoms of progressive hypoxia and dyspnea
• Use caution in patients with hepatic failure or with bleeding disorder including thrombocytopenia and hemophilia, or patients taking anticoagulant therapy; bleeding hematoma may occur from intramuscular (IM) administration
• Use caution in renal impairment or hepatic impairment
• Patients should be opioid free for a minimum of 7-10 days before initiating therapy; a naltrexone challenge test recommended to confirm opioid-free status

Pregnancy and Lactation

• Use naltrexone with caution during pregnancy if benefits outweigh risks
• Animal studies show risk and human studies are not available, or neither animal nor human studies were done
• Naltrexone is excreted in breast milk; consult your doctor before breastfeeding