Naltrexone hydrochloride is a potent, long-acting, orally-effective narcotic
antagonist useful in the management of narcotic addiction.
Narcotic antagonist, In treatment of?alcoholism
sulfonamide, carbonic anhydrase inhibitor, anti-glaucoma agent
Nonselective opioid receptor antagonist; congener of naloxone
Naltrexone hydrochloride has been used:
as an opioid antagonist, to analyse its effect on ethanol preference using Caenorhabditis elegans as a model.
to determine its effectiveness in reducing the preference for substance of abuse (SOA) like nicotine and cocaine using Caenorhabditis elegans as a model.
in the preparation of combinatorial drug, PXT3003 for treating Charcot-Marie-Tooth disease 1A (CMT1A) transgenic rat model Pmp22.
ChEBI: Naltrexone hydrochloride is a hydrochloride obtained by reaction of oxycodone with one molar equivalent of hydrochloric acid. it is a mu-opioid receptor antagonist that is used to treat alcohol dependence. It has a role as a mu-opioid receptor antagonist, an antidote to opioid poisoning and a central nervous system depressant. It contains a naltrexone(1+).
Competitive antagonist for μ, κ, δ, and σ-opioid receptors; has greater oral efficacy and longer duration of action than naloxone.
Opioid antagonist:
Adjunctive prophylactic treatment in patient’s
previously opioid dependant
Treatment of alcohol dependence
Potentially hazardous interactions with other drugs
Opioids: Avoid concomitant use.
Naltrexone is well absorbed from the gastrointestinal
tract but is subject to considerable first-pass metabolism
and may undergo enterohepatic recycling. It is extensively
metabolised in the liver and the major metabolite,
6-β-naltrexol, may also possess weak opioid antagonist
activity.
It is excreted mainly in the urine, <5% is excreted in the
faeces.
The renal clearance for naltrexone ranges from 30-127
mL/min and suggests that renal elimination is primarily
by glomerular filtration
This narcotic antagonist has been purified by recrystallisation from MeOH and dried in air. The free base has m 168-170o after recrystallisation from Me2CO. [Cone et al. J Pharm Sci 64 618 1975, Gold et al. Med Res Rev 2 211 1982.]
