II. Indications
- Substance Dependence (especially with history of relapse)
- Alcoholism
- Best used with an aftercare program
- However, may be started in patients who are continuing to drink
- Opioid Dependence
- Patients must abstain from Opioids for at least 7-10 days before starting
- Alcoholism
- Low dose Naltrexone (0.5 mg to 4.5 mg/day) has also been proprosed for various conditions including Chronic Pain
- No rigorous evidence of benefit at these low doses and for these varied conditions, but unlikely to cause harm
- Postulated to up-regulate Opioid receptors, increas endorphin production and act as Analgesic and antiinflammatory
- May cause Opioid Withdrawal if used soon after last use of Opioids
- (2020) Presc Lett 27(4): 22
- Toljan (2018) Med Sci 6(4): 82 [PubMed]
III. Contraindications
IV. Mechanism
- Very long acting opioid Antagonist (duration >24 hours)
- Reduces Alcohol craving
- Decreases impulsive use of Opioids
V. Medications
- Naltrexone Oral Tablet (Revia)
- Naltrexone Extended Release IM (Vivitrol)
VI. Dosing
- Frequency options
- Oral Daily
- Naltrexone 50 mg orally daily (dosing range 25 to 100 mg orally daily)
- Oral Alternate days
- Naltrexone 100 mg orally on Monday, Wednesday and Friday
- IM Monthly (expensive - as much as $1300 per month in 2017)
- Vivitrol 380 mg injection every 4 weeks (appears less effective than oral dosing)
- Oral Daily
- Duration
- May need to be used for 1 year or longer
VII. Adverse Effects
- Adverse Effects decreased with IM formulation
- Hepatotoxicity (dose dependent)
- Nausea or Vomiting (10%)
- Abominal pain or cramping
- Headache
- Dizziness
- Fatigue
- Insomnia
- Sedation
- Anxiety
- Arthralgias or myalgias
- Injection Site Reaction (IM, Vivitrol)
- Risk of lethal Opioid Overdose on relapse
- Decreased Opioid tolerance after use
- No toxicity if drinking with Naltrexone
- Not indicated to make them social drinkers
- Alcoholics tend to get less drunk on Naltrexone
- Very broad safety profile with minimal adverse effects
- However, Opioid use is a contraindication
- Hepatotoxicity, however is a risk
- Croop (1997) Arch Gen Psych 54:1130-5 [PubMed]
VIII. Safety
- Pregnancy Category C
- Lactation: Unknown
IX. Efficacy
- Initial studies showed relapse reduction by 50%
- IM monthly Naltrexone injection (Vivitrol) appears more effective and with fewer adverse effects than oral daily (Revia)
- Return to Alcohol use 150 days for IM (50 days for oral)
- Leighty (2019) Mental Health Clin 9(6): 392-6 [PubMed]
- Decreases heavy drinking days
- Some studies have shown marginal benefit with Naltrexone
- Relapse rate: 38% at 13 weeks (44% with Placebo)
- Compliance rate low: 42-44% in all groups
- Krystal (2001) N Engl J Med 345:1734-9 [PubMed]
X. Monitoring
- IM Naltrexone patients should have a medic alert card
- Consult pain management in patients with Acute Severe Pain
- Obtain serum liver transaminases periodically
- Baseline
- Repeat at 3 months, then every 3-6 months
XI. Drug Interactions
- May be used in combination with other agents used in Substance Abuse
- Examples: Acomprosate, Topiramate, Gabapentin
-
Opioids
- Severe withdrawal risk (see contraindications as above)
XII. Resources
- Naltrexone Tablet (DailyMed)
- Naltrexone IM Injection (DailyMed)
Images: Related links to external sites (from Bing)
Related Studies
naltrexone (on 12/21/2022 at Medicaid.Gov Survey of pharmacy drug pricing) | ||
NALTREXONE 50 MG TABLET | Generic | $0.65 each |
vivitrol (on 4/1/2022 at Medicaid.Gov Survey of pharmacy drug pricing) | ||
VIVITROL 380 MG VIAL | $1,446.85 each | |
VIVITROL 380 MG VIAL-DILUENT | $1,446.85 each |
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 |
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 |
Ontology: Trexan (C0729157)
Concepts | Pharmacologic Substance (T121) , Organic Chemical (T109) |
MSH | D009271 |
English | Trexan |