Naltrexone hydrochloride Chemical Properties

Melting point:

274-2760C

storage temp. 

2-8°C

solubility 

H₂O: 50 mg/mL, clear, colorless

color 

White to Off-White

Water Solubility 

Soluble in water at 50mg/ml.

Sensitive 

Light Sensitive

Merck 

13,6389

BRN 

3580333

CAS DataBase Reference

16676-29-2(CAS DataBase Reference)

Safety Information

Hazard Codes 

Xn

Risk Statements 

22

Safety Statements 

22-36

WGK Germany 

3

RTECS 

QD2160000

F 

8-10

HS Code 

2932.99.7000

Toxicity

guinea pig,LD50,oral,1490mg/kg (1490mg/kg),Medicamentos de Actualidad. Vol. 21, Pg. 264, 1985.

Naltrexone hydrochloride Usage And Synthesis

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)

Uses

Nonselective opioid receptor antagonist; congener of naloxone

Uses

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.

Uses

sulfonamide, carbonic anhydrase inhibitor, anti-glaucoma agent

Uses

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.]

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