Naltrexone

Aka: Naltrexone, Trexan, Revia, Vivitrol

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II. Indications

  1. Substance Dependence (especially with history of relapse)
    1. Alcoholism
    2. Opioid Dependence
    3. Must be used with an aftercare program
  2. Low dose Naltrexone (0.5 mg to 4.5 mg/day) has also been proprosed for various conditions including Chronic Pain
    1. No rigorous evidence of benefit at these low doses and for these varied conditions, but unlikely to cause harm
    2. Postulated to up-regulate Opioid receptors, increas endorphin production and act as Analgesic and antiinflammatory
    3. May cause Opioid Withdrawal if used soon after last use of Opioids
    4. (2020) Presc Lett 27(4): 22
    5. Toljan (2018) Med Sci 6(4): 82 [PubMed]

III. Contraindications

  1. Long-term Opioid use or Heroin dependence (until off Opioids for at least 7-10 days)
    1. Risk of severe withdrawal
  2. Opioids needed for pain control
  3. Hepatitis or Liver failure

IV. Adverse effects

  1. Hepatotoxicity (dose dependent)
  2. Nausea (10%)
  3. Headache
  4. Anxiety
  5. Sedation

V. Mechanism

  1. Reduces Alcohol craving
  2. Decreases impulsive use of Opioids

VI. Efficacy

  1. Initial studies showed relapse reduction by 50%
  2. Recent large DBPCT showed no benefit with Naltrexone
    1. Relapse rate: 38% at 13 weeks (44% with Placebo)
    2. Compliance rate low: 42-44% in all groups
    3. Krystal (2001) N Engl J Med 345:1734-9 [PubMed]

VII. Adverse effects

  1. Nausea or Vomiting
  2. Abominal pain or cramping
  3. Headache
  4. Dizziness
  5. Fatigue
  6. Insomnia
  7. Anxiety
  8. Arthralgias or myalgias
  9. Risk of lethal Opioid Overdose on relapse
    1. Decreased Opioid tolerance after use
  10. No toxicity if drinking with Naltrexone
    1. Not indicated to make them social drinkers
    2. Alcoholics tend to get less drunk on Naltrexone
  11. Very broad safety profile with minimal adverse effects
    1. However, Opioid use is a contraindication
    2. Hepatotoxicity, however is a risk
    3. Croop (1997) Arch Gen Psych 54:1130-5 [PubMed]

VIII. Monitoring

  1. Obtain serum liver transaminases periodically
    1. Baseline
    2. Repeat at 3 months, then every 3-6 months

IX. Dosage

  1. Frequency options
    1. Daily
      1. Naltrexone 50 mg orally daily
    2. Alternate days
      1. Naltrexone 100 mg orally on Monday, Wednesday and Friday
    3. Monthly (expensive - as much as $1300 per month in 2017)
      1. Vivitrol 380 mg injection every 4 weeks (appears less effective than oral dosing)
  2. Duration
    1. May need to be used for 1 year or longer

X. Safety

  1. Pregnancy Category C
  2. Lactation: Unknown

XI. References

  1. (2018) Presc Lett 25(1):5
  2. Hartmann (1997) Am Fam Physician 55(5):1877-9 [PubMed]
  3. Williams (2005) Am Fam Physician 72(9):1775-80 [PubMed]
  4. Winslow (2016) Am Fam Physician 93(6): 457-65 [PubMed]

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Related Studies

Cost: Medications

naltrexone (on 5/17/2017 at Medicaid.Gov Survey of pharmacy drug pricing)
NALTREXONE 50 MG TABLET Generic $0.80 each
vivitrol (on 4/19/2017 at Medicaid.Gov Survey of pharmacy drug pricing)
VIVITROL 380 MG VIAL + DILUENT $1,251.46 each
FPNotebook does not benefit financially from showing this medication data or their pharmacy links. This information is provided only to help medical providers and their patients see relative costs. Insurance plans negotiate lower medication prices with suppliers. Prices shown here are out of pocket, non-negotiated rates. See Needy Meds for financial assistance information.

Ontology: Naltrexone (C0027360)

Definition (CHV) a drug used to help people who have a narcotic or alcohol addiction stay drug free
Definition (NCI_NCI-GLOSS) A drug that blocks the action of opiates (drugs used to treat pain). It may be used in the treatment of intravenous opiate addiction or alcohol dependence. Naltrexone is also being studied in the treatment of breast cancer. It may block the effects of the hormone estrogen, which causes some breast cancer cells to grow, or block the blood flow to tumors. It is a type of opiate antagonist.
Definition (NCI) A noroxymorphone derivative with competitive opioid antagonistic property. Naltrexone reverses the effects of opioid analgesics by binding to the various opioid receptors in the central nervous system, including the mu-, kappa- and gamma-opioid receptors. This leads to an inhibition of the typical actions of opioid analgesics, including analgesia, euphoria, sedation, respiratory depression, miosis, bradycardia, and physical dependence. Naltrexone is longer-acting and more potent compared to naloxone.
Definition (MSH) Derivative of noroxymorphone that is the N-cyclopropylmethyl congener of NALOXONE. It is a narcotic antagonist that is effective orally, longer lasting and more potent than naloxone, and has been proposed for the treatment of heroin addiction. The FDA has approved naltrexone for the treatment of alcohol dependence.
Definition (CSP) synthetic congener of oxymorphone, chemically related to naloxone; a narcotic antagonist that is effective orally, longer lasting and more potent than naloxone, and has been proposed for the treatment of heroin addiction and alcohol dependence.
Concepts Pharmacologic Substance (T121) , Organic Chemical (T109)
MSH D009271
SnomedCT 373546002, 87617007
LNC LP15000-0, MTHU002303
English Naltrexone, Morphinan-6-one, 17-(cyclopropylmethyl)-4,5-epoxy-3,14-dihydroxy-, (5alpha)-, naltrexone, Naltrexone [Chemical/Ingredient], NALTREXONE, Naltrexone (product), Naltrexone (substance)
Swedish Naltrexon
Czech naltrexon
Finnish Naltreksoni
Russian NALTREKSON, НАЛТРЕКСОН
Japanese ナルトレキソン
Polish Naltrekson
Croatian NALTREKSON
Spanish naltrexona (producto), naltrexona (sustancia), naltrexona, Naltrexona
French Naltrexone
German Naltrexon
Italian Naltressone
Portuguese Naltrexona
Derived from the NIH UMLS (Unified Medical Language System)

Ontology: ReVia (C0591842)

Concepts Pharmacologic Substance (T121) , Organic Chemical (T109)
MSH D009271
English naltrexone hydrochloride (Revia), revia, Nalorex, Bristol Myers Squibb Brand of Naltrexone Hydrochloride, Bristol-Myers Squibb Brand of Naltrexone Hydrochloride, Du Pont Brand of Naltrexone Hydrochloride, Lamepro Brand of Naltrexone Hydrochloride, Nemexin, Orphan Brand of Naltrexone Hydrochloride, Schering Plough Brand of Naltrexone Hydrochloride, Schering-Plough Brand of Naltrexone Hydrochloride, United Drug Brand of Naltrexone Hydrochloride, ReVia, Revia
Derived from the NIH UMLS (Unified Medical Language System)

Ontology: Trexan (C0729157)

Concepts Pharmacologic Substance (T121) , Organic Chemical (T109)
MSH D009271
English Trexan
Derived from the NIH UMLS (Unified Medical Language System)

Related Topics in Pharmacology

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