Nalmefene

Identification

Summary

Nalmefene is an opioid antagonist used to reduce alcohol consumption in adults with alcohol dependence and treat and prevent opioid overdose.

Brand Names

Revex, Selincro

Generic Name

Nalmefene

DrugBank Accession Number

DB06230

Background

Nalmefene, a 6-methylene analogue of naltrexone, is an opioid receptor antagonist.⁸ It acts as an antagonist at the mu (μ)-opioid and delta (δ)-opioid receptors and a partial agonist at the kappa (κ)-opioid receptor.⁷

In Europe, nalmefene oral tablets are used to reduce alcohol consumption in adults with alcohol dependence.⁷ Nalmefene was approved in the United States in 1995 as an antidote for opioid overdose.⁴ Nalmefene injection is used to manage known or suspected opioid overdose. It is used for complete or partial reversal of opioid drug effects, including respiratory depression, induced by either natural or synthetic opioids.⁸ The nasal spray formulation of nalmefene was approved by the FDA in May 2023.¹¹

Type

Small Molecule

Groups

Approved, Investigational, Withdrawn

Structure

3D

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MOLSDF3D-SDFPDBSMILESInChI

Similar Structures

Structure for Nalmefene (DB06230)

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Weight

Average: 339.435
Monoisotopic: 339.183443669

Chemical Formula

C₂₁H₂₅NO₃

Synonyms

• Nalmefene
• Nalmefeno

External IDs

• JF-1
• ORF 1167
• ORF 11676
• ORF-1167
• ORF-11676
• SRD-174
• SRD174

Pharmacology

Indication

Nalmefene oral tablet is indicated for the reduction of alcohol consumption in adult patients with alcohol dependence who have a high drinking risk level (DRL), without physical withdrawal symptoms and who do not require immediate detoxification. Nalmefene should only be prescribed in conjunction with continuous psychosocial support focused on treatment adherence and reducing alcohol consumption. Nalmefene should be initiated only in patients who continue to have a high DRL two weeks after the initial assessment.⁷

Nalmefene injection and nasal spray are indicated for the complete or partial reversal of opioid drug effects, including respiratory depression, induced by either natural or synthetic opioids. They are also indicated in the management of known or suspected opioid overdose.^8,11 Nalmefene injection can be used for postoperative opioid overdose reversal.⁸

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Associated Conditions

• Alcohol Dependency
• Opioid Overdose

Contraindications & Blackbox Warnings

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Pharmacodynamics

Nalmefene is an opioid antagonist with no agonist activity. It works to prevent or reverse the effects of opioids, including respiratory depression, sedation, and hypotension.⁸ Nalmefene has a longer duration of action than naloxone, another opioid antagonist used to reverse opioid overdose.^2,8 In a study of brain receptor occupancy, a 1 mg dose of nalmefene blocked over 80% of brain opioid receptors within five minutes after administration.⁸

Nalmefene has no opioid agonist activity and it is not associated with drug tolerance, physical dependence, or abuse potential.⁸

Nalmefene is not known to produce respiratory depression, psychotomimetic effects, or pupillary constriction. No pharmacological activity was observed when nalmefene was administered in the absence of opioid agonists. However, as with all opioid antagonists, nalmefene can produce acute withdrawal symptoms in individuals with opioid dependence. These withdrawal symptoms should be managed with symptomatic and supportive treatment: the administration of large amounts of opioids to patients receiving opioid antagonists in an attempt to overcome a full blockade has resulted in adverse respiratory and circulatory reactions.⁸

Mechanism of action

The opioid system consists of three opioid receptors - mu (μ), delta (δ), and kappa (κ) - that are G-protein coupled receptors.⁶ Opioid receptors are activated by endogenous opioid peptides and are expressed throughout the brain to play a critical role in mood regulation, pain, reward, addictive behaviours, and substance use disorders. Opioid receptors are involved in various brain signalling pathways, including the mesolimbic pathway, sometimes referred to as the reward pathway. The mesolimbic pathway plays an important role in the positive reinforcement of natural rewards like food and drugs of abuse like exogenous opioid drugs. Many abused drugs activate mu-opioid receptors, leading to positive reinforcing effects.⁵ Alcohol consumption can also cause the release of endogenous opioids, which bind to mu and delta receptors, thereby increasing the release of dopamine in the nucleus accumbens to induce reward and positive reinforcement effects.¹

Nalmefene is an antagonist at the mu and delta-opioid receptors and a partial agonist at the kappa-opioid receptor. As an antagonist, nalmefene blocks ligands from binding to the opioid receptor.⁷ Animal studies suggest that kappa-opioid receptor signalling blocks acute reward and positive reinforcement effects of drugs with abusive potential by decreasing dopamine in the nucleus accumbens.¹ In vivo studies have demonstrated that nalmefene reduces alcohol consumption, possibly by modulating cortico-mesolimbic functions.⁷ Preclinical studies suggest that nalmefene restores alcohol-induced dysregulations of the MOR/endorphins and the KOR/dynorphin system.³

Target	Actions	Organism
AKappa-type opioid receptor	partial agonist	Humans
ADelta-type opioid receptor	antagonist	Humans
AMu-type opioid receptor	antagonist	Humans

Absorption

Nalmefene is rapidly absorbed after a single oral administration of 18.06 mg with an absolute oral bioavailability of 41%. The C_max was 16.5 ng/mL and T_max was approximately 1.5 hours. The exposure (AUC) was 131 ng x h/mL. High-fat meal increased the AUC by 30% and C_max by 50% and delayed T_max by 30 min; however, this is unlikely of clinical significance.⁷

Nalmefene exhibits dose-proportional pharmacokinetics following intravenous administration of 0.5 mg to 2 mg. T_max was 2.3 ± 1.1 hours following intramuscular administration and 1.5 ± 1.2 hours following subcutaneous administration. Therapeutic plasma concentrations are likely to be reached within 5 to 15 minutes after a 1 mg dose in an emergency. There is variability in the speed of absorption for intramuscular and subcutaneous dosing.⁸

Volume of distribution

Following a 1 mg parenteral dose, nalmefene was rapidly distributed. The apparent volumes of distribution centrally (V_c) and at steady-state (V_dss) are 3.9 ± 1.1 L/kg and 8.6 ± 1.7 L/kg, respectively.⁸ Nalmefene readily crosses the blood-brain barrier.⁷

Protein binding

Protein binding of nalmefene ranges from 30% to 45%.^7,8 In vitro, 67% (CV 8.7%) of nalmefene was distributed into red blood cells and 39% (CV 6.4%) was distributed into plasma. The whole blood to plasma ratio was 1.3 (CV 6.6%) over the nominal concentration range in whole blood from 0.376 to 30 ng/mL.⁸

Metabolism

Nalmefene is extensively metabolized by the liver, primarily by glucuronide conjugation mainly mediated by UGT2B7 and UGT1A3 and UGT1A8 to a lesser extent. The major metabolite is pharmacologically inactive nalmefene 3-O-glucuronide.⁷ Nalmefene is also metabolized to trace amounts of an N-dealkylated metabolite, which has minimal pharmacological activity.⁸

Nalmefene can undergo dealkylation mediated by CYP3A4/5 to form nornalmefene. Nornalmefene can be further converted to nornalmefene 3-O-glucuronide and nornalmefene 3-sulfate, which are generally inactive metabolites.⁷

Nalmefene can also undergo CYP3A4/5-mediated sulfation to form nalmefene 3-O-sulfate, which retains some pharmacological activity. However, nalmefene 3-O-sulfate is present in the circulation in less than 10% of that of nalmefene; thus, it is unlikely to be a major contributor to the pharmacological activity of nalmefene.⁷ The plasma concentration-time profile in some subjects suggests that nalmefene undergoes enterohepatic recycling.⁸

Hover over products below to view reaction partners

• Nalmefene
  • Nalmefene 3-O-glucuronide
  • Nalmefene 3-O-sulfate
  • Nornalmefene
    • Nornalmefene 3-O-sulfate
    • Nornalmefene 3-O-glucuronide

Route of elimination

Renal excretion is the main route of elimination for nalmefene and its metabolites. About 54% of the total dose is excreted in the urine as nalmefene 3-O-glucuronide. Less than 3% of the dose is excreted as nalmefene or other metabolites ⁷. About 17% of the dose is excreted in the feces.⁸

Half-life

The terminal half-life is approximately 12.5 hours following oral administration.⁷ After intravenous administration of 1 mg nalmefene to healthy adult male subjects, plasma concentrations declined biexponentially with redistribution and a terminal elimination half-life of 41 ± 34 minutes and 10.8 ± 5.2 hours, respectively.⁸

Clearance

The oral clearance of nalmefene (CL/F) was estimated as 169 L/h.⁷ Following intravenous administration of 1 mg nalmefene, the systemic clearance of nalmefene was 0.8 ± 0.2 L/hr/kg and the renal clearance was 0.08 ± 0.04 L/hr/kg.⁸

Adverse Effects

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Toxicity

The oral LD₅₀ values were 230 and <200 mg/kg for male and female mice, <300 and 150 mg/kg for male and female rats, and <225 and 225 for male and female rabbits.⁹ In mice, rats, and rabbits, intravenous LD₅₀ values had a range of 15.0-48.5 mg/kg and subcutaneous LD₅₀ values were in the range of 157-1150 mg/kg.¹⁰

Nalmefene was well tolerated and showed no serious toxicity during experimental administration to healthy individuals, even when given at 15 times the highest recommended dose. In a small number of subjects, at doses exceeding the recommended nalmefene injection dose, nalmefene produced symptoms suggestive of reversal of endogenous opioids, such as nausea, chills, myalgia, dysphoria, abdominal cramps, and joint pain. These symptoms can also arise in other narcotic antagonist drugs and they are usually transient in nature and occur at a very low frequency.⁸

Large doses of nalmefene have been used in studies. For example, one study used doses of nalmefene up to 90 mg/day for 16 weeks in patients diagnosed with pathological gambling. In a study in patients with interstitial cystitis, 20 patients received 108 mg/day of nalmefene for more than two years. Intake of a single dose of 450 mg nalmefene has been reported without changes in blood pressure, heart rate, respiration rate, or body temperature. There was no unusual pattern of adverse reactions, but the experience is limited. Management of an overdose should be observational and symptomatic.⁷

Pathways

Not Available

Pharmacogenomic Effects/ADRs

Not Available

Interactions

Drug Interactions

This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.

• Approved
• Vet approved
• Nutraceutical
• Illicit
• Withdrawn
• Investigational
• Experimental
• All Drugs

Drug	Interaction
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Abacavir	Abacavir may decrease the excretion rate of Nalmefene which could result in a higher serum level.
Aceclofenac	Aceclofenac may decrease the excretion rate of Nalmefene which could result in a higher serum level.
Acemetacin	Acemetacin may decrease the excretion rate of Nalmefene which could result in a higher serum level.
Acetaminophen	Acetaminophen may decrease the excretion rate of Nalmefene which could result in a higher serum level.
Acetazolamide	Acetazolamide may increase the excretion rate of Nalmefene which could result in a lower serum level and potentially a reduction in efficacy.
Acetylsalicylic acid	Acetylsalicylic acid may decrease the excretion rate of Nalmefene which could result in a higher serum level.
Aclidinium	Nalmefene may decrease the excretion rate of Aclidinium which could result in a higher serum level.
Acrivastine	Nalmefene may decrease the excretion rate of Acrivastine which could result in a higher serum level.
Acyclovir	Acyclovir may decrease the excretion rate of Nalmefene which could result in a higher serum level.
Adefovir dipivoxil	Adefovir dipivoxil may decrease the excretion rate of Nalmefene which could result in a higher serum level.

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Food Interactions

• Take with or without food. High-fat food increases the AUC by 30% and Cmax by 50% and delays Tmax by 30 min, but this is unlikely of clinical relevance.

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Product Ingredients

Ingredient	UNII	CAS	InChI Key
Nalmefene hydrochloride	K7K69QC05X	58895-64-0	GYWMRGWFQPSQLK-OPHZJPRHSA-N
Nalmefene hydrochloride dihydrate	52Z0G7QVJX	1228646-70-5	XOBQQQVDLSMXCE-JVRGSUDVSA-N

Brand Name Prescription Products

Name	Dosage	Strength	Route	Labeller	Marketing Start	Marketing End	Region	Image
Revex	Injection, solution	1 mg/1mL	Intravenous	Baxter Laboratories	2006-06-19	Not applicable
Revex	Injection, solution	0.1 mg/1mL	Intravenous	Baxter Laboratories	2006-06-19	Not applicable
Selincro	Tablet, film coated	18 mg	Oral	H. Lundbeck A/S	2016-09-08	Not applicable
Selincro	Tablet, film coated	18 mg	Oral	H. Lundbeck A/S	2016-09-08	Not applicable
Selincro	Tablet, film coated	18 mg	Oral	H. Lundbeck A/S	2016-09-08	Not applicable
Selincro	Tablet, film coated	18 mg	Oral	H. Lundbeck A/S	2016-09-08	Not applicable
Selincro	Tablet, film coated	18 mg	Oral	H. Lundbeck A/S	2016-09-08	Not applicable
Selincro	Tablet, film coated	18 mg	Oral	H. Lundbeck A/S	2016-09-08	Not applicable
Selincro	Tablet, film coated	18 mg	Oral	H. Lundbeck A/S	2016-09-08	Not applicable
Selincro	Tablet, film coated	18 mg	Oral	H. Lundbeck A/S	2016-09-08	Not applicable

Generic Prescription Products

Name	Dosage	Strength	Route	Labeller	Marketing Start	Marketing End	Region	Image
Nalmefene Hydrochloride	Injection, solution	1 mg/1mL	Intramuscular; Intravenous; Subcutaneous	Purdue Pharma L.P.	2022-02-08	Not applicable

Categories

ATC Codes

N07BB05 — Nalmefene

• N07BB — Drugs used in alcohol dependence
• N07B — DRUGS USED IN ADDICTIVE DISORDERS
• N07 — OTHER NERVOUS SYSTEM DRUGS
• N — NERVOUS SYSTEM

Drug Categories

• Alkaloids
• Antidotes
• Antipruritics
• Central Nervous System Agents
• Cytochrome P-450 CYP3A Substrates
• Cytochrome P-450 CYP3A4 Substrates
• Cytochrome P-450 CYP3A5 Substrates
• Cytochrome P-450 Substrates
• Drugs that are Mainly Renally Excreted
• Drugs Used in Addictive Disorders
• Drugs Used in Alcohol Dependence
• Heterocyclic Compounds, Fused-Ring
• Morphinans
• Nervous System
• Opiate Alkaloids
• Opioid Antagonists
• Peripheral Nervous System Agents
• Phenanthrenes
• Sensory System Agents
• UGT1A3 substrates
• UGT2B7 substrates

Chemical TaxonomyProvided by Classyfire

Description

This compound belongs to the class of organic compounds known as phenanthrenes and derivatives. These are polycyclic compounds containing a phenanthrene moiety, which is a tricyclic aromatic compound with three non-linearly fused benzene.

Kingdom

Organic compounds

Super Class

Benzenoids

Class

Phenanthrenes and derivatives

Sub Class

Not Available

Direct Parent

Phenanthrenes and derivatives

Alternative Parents

Tetralins / Coumarans / Aralkylamines / Alkyl aryl ethers / 1-hydroxy-2-unsubstituted benzenoids / Piperidines / Tertiary alcohols / Trialkylamines / Cyclic alcohols and derivatives / 1,2-aminoalcohols / Oxacyclic compounds / Azacyclic compounds / Organopnictogen compounds / Hydrocarbon derivatives

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Substituents

1,2-aminoalcohol / 1-hydroxy-2-unsubstituted benzenoid / Alcohol / Alkyl aryl ether / Amine / Aralkylamine / Aromatic heteropolycyclic compound / Azacycle / Coumaran / Cyclic alcohol / Ether / Hydrocarbon derivative / Organic nitrogen compound / Organic oxygen compound / Organoheterocyclic compound / Organonitrogen compound / Organooxygen compound / Organopnictogen compound / Oxacycle / Phenanthrene / Piperidine / Tertiary alcohol / Tertiary aliphatic amine / Tertiary amine / Tetralin

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Molecular Framework

Aromatic heteropolycyclic compounds

External Descriptors

morphinane alkaloid (CHEBI:7457)

Affected organisms

• Humans and other mammals

Chemical Identifiers

UNII

TOV02TDP9I

CAS number

55096-26-9

InChI Key

WJBLNOPPDWQMCH-MBPVOVBZSA-N

InChI

InChI=1S/C21H25NO3/c1-12-6-7-21(24)16-10-14-4-5-15(23)18-17(14)20(21,19(12)25-18)8-9-22(16)11-13-2-3-13/h4-5,13,16,19,23-24H,1-3,6-11H2/t16-,19+,20+,21-/m1/s1

IUPAC Name

(1S,5R,13S,17S)-4-(cyclopropylmethyl)-14-methylidene-12-oxa-4-azapentacyclo[9.6.1.0^{1,13}.0^{5,17}.0^{7,18}]octadeca-7,9,11(18)-triene-10,17-diol

SMILES

OC1=CC=C2C[C@H]3N(CC4CC4)CC[C@@]45[C@@H](OC1=C24)C(=C)CC[C@@]35O

References

General References

1. Paille F, Martini H: Nalmefene: a new approach to the treatment of alcohol dependence. Subst Abuse Rehabil. 2014 Aug 8;5:87-94. doi: 10.2147/SAR.S45666. eCollection 2014. [Article]
2. Glass PS, Jhaveri RM, Smith LR: Comparison of potency and duration of action of nalmefene and naloxone. Anesth Analg. 1994 Mar;78(3):536-41. [Article]
3. Mann K, Torup L, Sorensen P, Gual A, Swift R, Walker B, van den Brink W: Nalmefene for the management of alcohol dependence: review on its pharmacology, mechanism of action and meta-analysis on its clinical efficacy. Eur Neuropsychopharmacol. 2016 Dec;26(12):1941-1949. doi: 10.1016/j.euroneuro.2016.10.008. Epub 2016 Nov 12. [Article]
4. Authors unspecified: Nalmefene . [Article]
5. Le Merrer J, Becker JA, Befort K, Kieffer BL: Reward processing by the opioid system in the brain. Physiol Rev. 2009 Oct;89(4):1379-412. doi: 10.1152/physrev.00005.2009. [Article]
6. Al-Hasani R, Bruchas MR: Molecular mechanisms of opioid receptor-dependent signaling and behavior. Anesthesiology. 2011 Dec;115(6):1363-81. doi: 10.1097/ALN.0b013e318238bba6. [Article]
7. European Medicines Agency (EMA) Summary of product characteristics: Selincro (nalmefene) oral tablets [Link]
8. DailyMed Label: NALMEFENE HYDROCHLORIDE injection, solution for intravenous, intramuscular, or subcutaneous use [Link]
9. EMA Assessment Report: Selincro (nalmafene) oral tablets [Link]
10. Australian Public Assessment Report: Nalmefene (as hydrochloride dihydrate) [Link]
11. FDA Approved Drug Products: OPVEE (nalmefene) nasal spray [Link]

External Links

KEGG Drug

D05111

KEGG Compound

C08027

ChemSpider

4447642

BindingDB

50045776

RxNav

31479

ChEBI

7457

ChEMBL

CHEMBL982

ZINC

ZINC000000403529

Wikipedia

Nalmefene

Clinical Trials

Clinical Trials

Phase	Status	Purpose	Conditions	Count
4	Completed	Treatment	Alcohol Dependency	1
4	Recruiting	Treatment	Resuscitations	1
4	Terminated	Treatment	Alcohol Dependency	1
3	Completed	Treatment	Alcohol Dependency	5
3	Not Yet Recruiting	Treatment	Behavioural Addiction	1
3	Unknown Status	Treatment	Alcohol Dependency / Cirrhosis of the Liver / Nalmefene	1
2	Completed	Treatment	Alcohol Use Disorders (AUD)	1
2	Completed	Treatment	Pruritus, Atopic Dermatitis	1
2	Completed	Treatment	Smoking, Cessation	1
2	Unknown Status	Treatment	Impulse-control disorder / Parkinson's Disease (PD)	1

Pharmacoeconomics

Manufacturers

Not Available

Packagers

Not Available

Dosage Forms

Form	Route	Strength
Injection, solution	Intramuscular; Intravenous; Subcutaneous	1 mg/1mL
Injection, solution	Intravenous	0.1 mg/1mL
Injection, solution	Intravenous	1 mg/1mL
Tablet	Oral	18 MG
Tablet, coated	Oral	18 MG
Tablet, film coated	Oral	18 MG
Tablet, film coated	Oral

Prices

Not Available

Patents

Not Available

Properties

State

Solid

Experimental Properties

Property	Value	Source
pKa	7.6	https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=3abfbffc-9e52-4fc6-ae92-6e0a97f4afe7

Predicted Properties

Property	Value	Source
Water Solubility	0.839 mg/mL	ALOGPS
logP	2.24	ALOGPS
logP	1.95	Chemaxon
logS	-2.6	ALOGPS
pKa (Strongest Acidic)	10.35	Chemaxon
pKa (Strongest Basic)	9.57	Chemaxon
Physiological Charge	1	Chemaxon
Hydrogen Acceptor Count	4	Chemaxon
Hydrogen Donor Count	2	Chemaxon
Polar Surface Area	52.93 Å2	Chemaxon
Rotatable Bond Count	2	Chemaxon
Refractivity	95.21 m3·mol-1	Chemaxon
Polarizability	37.04 Å3	Chemaxon
Number of Rings	6	Chemaxon
Bioavailability	1	Chemaxon
Rule of Five	Yes	Chemaxon
Ghose Filter	Yes	Chemaxon
Veber's Rule	No	Chemaxon
MDDR-like Rule	No	Chemaxon

Predicted ADMET Features

Not Available

Spectra

Mass Spec (NIST)

Not Available

Spectra

Spectrum	Spectrum Type	Splash Key
Predicted MS/MS Spectrum - 10V, Positive (Annotated)	Predicted LC-MS/MS	Not Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)	Predicted LC-MS/MS	Not Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)	Predicted LC-MS/MS	Not Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)	Predicted LC-MS/MS	Not Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)	Predicted LC-MS/MS	Not Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)	Predicted LC-MS/MS	Not Available

Targets

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insights and accelerate drug research.

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Details1. Kappa-type opioid receptor

Kind

Protein

Organism

Humans

Pharmacological action

Yes

Actions

Partial agonist

General Function

Opioid receptor activity

Specific Function

G-protein coupled opioid receptor that functions as receptor for endogenous alpha-neoendorphins and dynorphins, but has low affinity for beta-endorphins. Also functions as receptor for various synt...

Gene Name

OPRK1

Uniprot ID

P41145

Uniprot Name

Kappa-type opioid receptor

Molecular Weight

42644.665 Da

References

1. Kreek MJ, Schluger J, Borg L, Gunduz M, Ho A: Dynorphin A1-13 causes elevation of serum levels of prolactin through an opioid receptor mechanism in humans: gender differences and implications for modulation of dopaminergic tone in the treatment of addictions. J Pharmacol Exp Ther. 1999 Jan;288(1):260-9. [Article]
2. Mann K, Torup L, Sorensen P, Gual A, Swift R, Walker B, van den Brink W: Nalmefene for the management of alcohol dependence: review on its pharmacology, mechanism of action and meta-analysis on its clinical efficacy. Eur Neuropsychopharmacol. 2016 Dec;26(12):1941-1949. doi: 10.1016/j.euroneuro.2016.10.008. Epub 2016 Nov 12. [Article]
3. European Medicines Agency (EMA) Summary of product characteristics: Selincro (nalmefene) oral tablets [Link]

Details2. Delta-type opioid receptor

Kind

Protein

Organism

Humans

Pharmacological action

Yes

Actions

Antagonist

General Function

Opioid receptor activity

Specific Function

G-protein coupled receptor that functions as receptor for endogenous enkephalins and for a subset of other opioids. Ligand binding causes a conformation change that triggers signaling via guanine n...

Gene Name

OPRD1

Uniprot ID

P41143

Uniprot Name

Delta-type opioid receptor

Molecular Weight

40368.235 Da

References

1. Ingman K, Hagelberg N, Aalto S, Nagren K, Juhakoski A, Karhuvaara S, Kallio A, Oikonen V, Hietala J, Scheinin H: Prolonged central mu-opioid receptor occupancy after single and repeated nalmefene dosing. Neuropsychopharmacology. 2005 Dec;30(12):2245-53. [Article]
2. Paille F, Martini H: Nalmefene: a new approach to the treatment of alcohol dependence. Subst Abuse Rehabil. 2014 Aug 8;5:87-94. doi: 10.2147/SAR.S45666. eCollection 2014. [Article]
3. Mann K, Torup L, Sorensen P, Gual A, Swift R, Walker B, van den Brink W: Nalmefene for the management of alcohol dependence: review on its pharmacology, mechanism of action and meta-analysis on its clinical efficacy. Eur Neuropsychopharmacol. 2016 Dec;26(12):1941-1949. doi: 10.1016/j.euroneuro.2016.10.008. Epub 2016 Nov 12. [Article]
4. European Medicines Agency (EMA) Summary of product characteristics: Selincro (nalmefene) oral tablets [Link]

Details3. Mu-type opioid receptor

Kind

Protein

Organism

Humans

Pharmacological action

Yes

Actions

Antagonist

General Function

Voltage-gated calcium channel activity

Specific Function

Receptor for endogenous opioids such as beta-endorphin and endomorphin. Receptor for natural and synthetic opioids including morphine, heroin, DAMGO, fentanyl, etorphine, buprenorphin and methadone...

Gene Name

OPRM1

Uniprot ID

P35372

Uniprot Name

Mu-type opioid receptor

Molecular Weight

44778.855 Da

References

1. Mann K, Torup L, Sorensen P, Gual A, Swift R, Walker B, van den Brink W: Nalmefene for the management of alcohol dependence: review on its pharmacology, mechanism of action and meta-analysis on its clinical efficacy. Eur Neuropsychopharmacol. 2016 Dec;26(12):1941-1949. doi: 10.1016/j.euroneuro.2016.10.008. Epub 2016 Nov 12. [Article]
2. Ingman K, Hagelberg N, Aalto S, Nagren K, Juhakoski A, Karhuvaara S, Kallio A, Oikonen V, Hietala J, Scheinin H: Prolonged central mu-opioid receptor occupancy after single and repeated nalmefene dosing. Neuropsychopharmacology. 2005 Dec;30(12):2245-53. [Article]
3. European Medicines Agency (EMA) Summary of product characteristics: Selincro (nalmefene) oral tablets [Link]

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Drug created at March 19, 2008 16:18 / Updated at June 05, 2023 04:57