Naltrexone
- Atc Codes:N07BB04
- CAS Codes:16676-29-2
- PHARMGKB ID:16676-29-2
Table of contents
- Brand Names
- Drug Combinations
- Chemistry
- Pharmacologic Category
- Mechanism of Action
- Therapeutic Use
- Pregnancy and Lactation Implications
- Contraindications
- Warnings and Precautions
- Adverse Reactions
- Caution and personalized dose adjustment in patients with the following genotypes
- Other genes that may be involved
- Drug Interactions
- Dosage
- Pharmacokinetics and Pharmacodynamics
- Special Considerations
Brand Names
Europe
Austria: Dependex, Ethylex, Naltrexin, Naltrexon, Nemexin, Revia; Belgium: Nalorex; Bulgaria: Adepend, Ethylex, Revia; Cyprus: Abernil; Czech Republic: Naltrexone, Nemexin, Revia; Denmark: Naltrexon; Estonia: Revia; Finland: Naltrexon, Revia; France: Nalorex, Naltrexone, Revia; Germany: Nalorex, Naltrexon, Nemexin; Greece: Nalorex; Hungary: Antaxon, Naltrexone; Ireland: Ethylex, Nalorex, Revia; Italy: Antaxone, Nalorex, Narcoral; Latvia: Naltrexone, Revia; Lithuania: Naltrexone, Revia; Malta: Abernil, Nalorex, Opizone; Netherlands: Naltrexon, Revia; Portugal: Antaxone, Basinal, Destoxicam, Nalorex, Naltrexona; Romania: Revia; Slovenia: Naltrekson, Revia; Spain: Antaxone, Revia; UK: Nalorex, Opizone.
North America
Canada: Revia; USA: Revia, Vivitrol.
Latin America
Argentina: Revez; Brazil: Revia.
Drug combinations
Naltrexone and Morphine
Chemistry
Naltrexone Hydrochloride: C~20~H~23~NO~4~ HCl. Mw: 377.86. (1) Morphinan-6-one, 17-(cyclopropylmethyl)-4,5-epoxy-3,14-dihydroxy-, hydrochloride, (5α)-; (2) 17-Cyclopropylmethyl)-4,5α-epoxy-3,14-dihydroxymorphinan-6-one hydrochloride. CAS-16676-29-2.
Pharmacologic Category
Opiate Antagonists. Alcohol Deterrents. Antidotes. (ATC-Code: N07BB04).
Mechanism of action
Naltrexone acts as competitive antagonist at opioid receptor sites, showing highest affinity for μ-receptors.
Therapeutic use
Treatment of ethanol dependence. Blockade of effects of exogenously administered opioids.
Pregnancy and lactiation implications
Evidence of early fetal loss observed with oral naltrexone in animal studies. There are no adequate, well-controlled studies in pregnant women and drug should be used during pregnancy only when potential benefits justify possible risks to fetus. Unknown whether naltrexone affects duration of labor and delivery. Naltrexone and active metabolite (6-β-naltrexol) distributed into human milk (not recommended in nursing women).
Unlabeled use
Contraindications
Hypersensitivity to naltrexone or any component of the formulation. Narcotic dependence or current use of opioid analgesics. Acute opioid withdrawal. Positive urine screen for opioids. Acute hepatitis. Liver failure.
Warnings and precautions
Patients treated with naltrexone may respond to lower opioid doses than previously used. May precipitate symptoms of acute withdrawal in opioid-dependent patients. Cases of eosinophilic pneumonia reported. Dose-related hepatocellular injury possible. Suicidal thoughts and depression reported. Use with caution in history of bleeding disorders and/or patients on anticoagulant therapy (bleeding/hematoma may occur from I.M. administration); also in hepatic and/or renal impairment. Use of naltrexone does not eliminate or diminish withdrawal symptoms. Vehicle used in injectable (polylactide-co-glycolide microspheres) rarely associated with retinal artery occlusion in abnormal arteriovenous anastomosis (e.g. patent foramen ovale).