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Nalmefene hydrochloride

Nalmefene hydrochloride structure

CAS No:
58895-64-0
Formula:
C21H26ClNO3
Chemical Name:
Nalmefene hydrochloride
Synonyms:
Morphinan-3,14-diol, 17-(cyclopropylmethyl)-4,5-epoxy-6-methylene-, hydrochloride, (5alpha)-;Revex;Unii-K7K69qc05x;(5α)-17-(Cyclopropylmethyl)-4,5-epoxy-6-methylenemorphinan-3,14-diolhydrochloride;(5a)-17-(CyclopropylMethyl)-6-Methylene-4,5-epoxyMorphinan-3,14-diol;Morphinan-3,14-diol,17-(cyclopropylMethyl)-4,5-epoxy-6-Methylene-, hydrochloride (1:1), (5a)-;(4R,4aS,7aS,12bS)-3-(cyclopropylmethyl)-7-methylidene-2,4,5,6,7a,13-hexahydro-1H-4,12-methanobenzofuro[3,2-e]isoquinoline-4a,9-diol,hydrochloride;Nalmefene Impurity 2
Categories:
Pharmaceutical Intermediates > Bulk Drug Intermediates

Description

Nalmefene hydrochloride has been introduced in the U.S.A. for opioid reversal following surgery, and in the reversal of opioid overdoses and epidurally administered narcotics. Nalmefene is an opioid antagonist that inhibits respiratory, analgesic and subjective effects of opioids. It has a higher potency, a longer duration of action, and superior bioavailability than the structurally related naltrexone. Nalmefene has a wide spectrum of biological activity and is in clinical trials for the treatment of interstitial cystitis, recalcitrant pruritus of cholestasis, stroke, rheumatoid arthritis, shock, CNS trauma, and alcoholism. Studies indicate that nalmefene does not induce morphine-like effects and has no apparent abuse potential.

Nalmefene hydrochloride Basic Attributes

Molecular Weight：

375.89

EC Number：

232-572-4

Color/Form：

White

Characteristics

Melting Point：

180-185°

PKA：

7.63(at 25℃)

Critical Temperature & Pressure：

Desiccate at RT

Safety Information

Storage features：

Desiccate at RT

Nalmefene hydrochloride Use and Manufacturing

Nalmefene Hydrochloride is a structural analog of Naltrexone (N285780) with opiate antagonist activity used in pharmaceutical treatment of alcoholism. Other pharmacological applications of this compound aim to reduce food cravings, drug abuse and pulmonary disease in affected individuals. Used as an opioid-induced tranquilizer on large animals in the veterinary industry. Narcotic antagonist

Drug Function and Efficacy

Nalmefene is an opioid antagonist that can inhibit or reverse the respiratory depression, sedation, and hypotension effects of opioid drugs. Pharmacodynamic studies have shown that the duration of action of nalmefene is longer than that of naloxone at a complete reversal dose. Nalmefene has no opioid agonist activity and does not produce respiratory depression, hallucinogenic effects, or mydriasis. No pharmacological effects were observed when nalmefene was administered in the absence of an opioid agonist. No tolerance, physical dependence, or abuse liability of nalmefene was observed in the study. In opioid-dependent individuals, nalmefene can produce acute withdrawal symptoms.

This ingredient has been used in drugs with the following functions (note: it does not mean that the ingredient itself has the following health functions)

Related Drugs

Nalmefene Hydrochloride Injection
Ingredients	The main ingredient of this product is nalmefene hydrochloride, and its chemical name is: 17-cyclopropylmethyl-4,5α-epoxy-6-methylenemorphinan-3,14-diol hydrochloride. The chemical structural formula is: Molecular formula: C21H25NO3·HCl Molecular weight: 375.90 Excipients are sodium chloride, hydrochloric acid, and water for injection.
Indication	Nalmefene can cause anesthesia when used after benzodiazepines, inhaled anesthetics, muscle relaxants, and muscle relaxant antagonists. This product can also be used in outpatient settings for conscious sedated patients and in emergency situations of multiple drug overdoses. No harmful drug interactions have been observed. Preclinical studies have shown that flumazenil and nalmefene can induce seizures in animals. Combining flumazenil and nalmefene produces fewer seizures than expected in rodent studies because the drugs alone can achieve the expected effects. Based on these data, adverse reactions cannot be expected from the combination of these two drugs, but it should be known that nalmefene may cause epilepsy when used in combination with these drugs.
Specifications	1ml: 0.1mg (calculated as nalmefene)
Manufacturer	Liaoning Haisco Pharmaceutical Co., Ltd.

Nalmefene Hydrochloride Injection
Specifications	1ml:0.1mg
Manufacturer	Xi'an Lijun Pharmaceutical Co.Limited

Nalmefene hydrochloride
Ingredients	Nalmefene hydrochloride, the excipients are sodium chloride, hydrochloric acid and water for injection.

See More Related Drugs

Registered Holders

SpecGx LLC

United States
Active
Biobetta Pharmaceuticals (Shanghai) Co., Ltd.

China
Active
Chongqing Unger Dragon Pharmaceutical Co., Ltd.

China
Active

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