Naltrexone hydrochloride

Description

Naltrexone hydrochloride is a potent, long-acting, orally-effective narcotic antagonist useful in the management of narcotic addiction.

Chemical properties

White Crystalline Powder

Originator

Endo (USA)

The Uses of Naltrexone hydrochloride

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.

The Uses of Naltrexone hydrochloride

Nonselective opioid receptor antagonist; congener of naloxone

The Uses of Naltrexone hydrochloride

sulfonamide, carbonic anhydrase inhibitor, anti-glaucoma agent

The Uses of Naltrexone hydrochloride

Narcotic antagonist, In treatment of?alcoholism

Definition

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+).

brand name

TREXAN

Biological Activity

Opioid antagonist.

Biochem/physiol Actions

Competitive antagonist for μ, κ, δ, and σ-opioid receptors; has greater oral efficacy and longer duration of action than naloxone.

Clinical Use

Opioid antagonist:
Adjunctive prophylactic treatment in patient’s previously opioid dependant
Treatment of alcohol dependence

Drug interactions

Potentially hazardous interactions with other drugs
Opioids: Avoid concomitant use.

Metabolism

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

storage

Room temperature

Purification Methods

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.]