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 for use 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

Type
Small Molecule
Groups
Approved, Investigational, Withdrawn
Structure
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 initial assessment.7

Nalmefene injection is indicated for the complete or partial reversal of opioid drug effects, including respiratory depression, induced by either natural or synthetic opioids. Nalmefene injection is indicated in the management of known or suspected opioid overdose. It can be used for postoperative opioid overdose reversal.8

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Associated Conditions
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

TargetActionsOrganism
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 Cmax was 16.5 ng/mL and Tmax was approximately 1.5 hours. The exposure (AUC) was 131 ng x h/mL. High-fat meal increased the AUC by 30% and Cmax by 50% and delayed Tmax 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. Tmax 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 (Vc) and at steady-state (Vdss) 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

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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.
DrugInteraction
AbacavirAbacavir may decrease the excretion rate of Nalmefene which could result in a higher serum level.
AceclofenacAceclofenac may decrease the excretion rate of Nalmefene which could result in a higher serum level.
AcemetacinAcemetacin may decrease the excretion rate of Nalmefene which could result in a higher serum level.
AcetaminophenAcetaminophen may decrease the excretion rate of Nalmefene which could result in a higher serum level.
AcetazolamideAcetazolamide may increase the excretion rate of Nalmefene which could result in a lower serum level and potentially a reduction in efficacy.
Acetylsalicylic acidAcetylsalicylic acid may decrease the excretion rate of Nalmefene which could result in a higher serum level.
AclidiniumNalmefene may decrease the excretion rate of Aclidinium which could result in a higher serum level.
AcrivastineNalmefene may decrease the excretion rate of Acrivastine which could result in a higher serum level.
AcyclovirAcyclovir may decrease the excretion rate of Nalmefene which could result in a higher serum level.
Adefovir dipivoxilAdefovir 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.

Products

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Product Ingredients
IngredientUNIICASInChI Key
Nalmefene hydrochlorideK7K69QC05X58895-64-0GYWMRGWFQPSQLK-OPHZJPRHSA-N
Nalmefene hydrochloride dihydrate52Z0G7QVJX1228646-70-5XOBQQQVDLSMXCE-JVRGSUDVSA-N
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
RevexInjection, solution1 mg/1mLIntravenousBaxter Laboratories2006-06-19Not applicableUS flag
RevexInjection, solution0.1 mg/1mLIntravenousBaxter Laboratories2006-06-19Not applicableUS flag
SelincroTablet, film coated18 mgOralH. Lundbeck A/S2016-09-08Not applicableEU flag
SelincroTablet, film coated18 mgOralH. Lundbeck A/S2016-09-08Not applicableEU flag
SelincroTablet, film coated18 mgOralH. Lundbeck A/S2016-09-08Not applicableEU flag
SelincroTablet, film coated18 mgOralH. Lundbeck A/S2016-09-08Not applicableEU flag
SelincroTablet, film coated18 mgOralH. Lundbeck A/S2016-09-08Not applicableEU flag
SelincroTablet, film coated18 mgOralH. Lundbeck A/S2016-09-08Not applicableEU flag
SelincroTablet, film coated18 mgOralH. Lundbeck A/S2016-09-08Not applicableEU flag
SelincroTablet, film coated18 mgOralH. Lundbeck A/S2016-09-08Not applicableEU flag
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
Nalmefene HydrochlorideInjection, solution1 mg/1mLIntramuscular; Intravenous; SubcutaneousPurdue Pharma L.P.2022-02-08Not applicableUS flag

Categories

ATC Codes
N07BB05 — Nalmefene
Drug Categories
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
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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
show 15 more
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]
KEGG Drug
D05111
KEGG Compound
C08027
ChemSpider
4447642
BindingDB
50045776
RxNav
31479
ChEBI
7457
ChEMBL
CHEMBL982
ZINC
ZINC000000403529
Wikipedia
Nalmefene

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4CompletedTreatmentAlcohol Dependency1
4RecruitingTreatmentResuscitations1
4TerminatedTreatmentAlcohol Dependency1
3CompletedTreatmentAlcohol Dependency5
3Unknown StatusTreatmentAlcohol Dependency / Cirrhosis of the Liver / Nalmefene1
2CompletedTreatmentAlcohol Use Disorders (AUD)1
2CompletedTreatmentPruritus, Atopic Dermatitis1
2CompletedTreatmentSmoking, Cessation1
2Unknown StatusTreatmentImpulse-control disorder / Parkinson's Disease (PD)1
2, 3CompletedTreatmentPathological Gambling Disorder1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
FormRouteStrength
Injection, solutionIntramuscular; Intravenous; Subcutaneous1 mg/1mL
Injection, solutionIntravenous0.1 mg/1mL
Injection, solutionIntravenous1 mg/1mL
TabletOral18 MG
Tablet, coatedOral18 MG
Tablet, film coatedOral18 MG
Tablet, film coatedOral
Prices
Not Available
Patents
Not Available

Properties

State
Solid
Experimental Properties
PropertyValueSource
pKa7.6https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=3abfbffc-9e52-4fc6-ae92-6e0a97f4afe7
Predicted Properties
PropertyValueSource
Water Solubility0.839 mg/mLALOGPS
logP2.24ALOGPS
logP1.95ChemAxon
logS-2.6ALOGPS
pKa (Strongest Acidic)10.35ChemAxon
pKa (Strongest Basic)9.57ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count4ChemAxon
Hydrogen Donor Count2ChemAxon
Polar Surface Area52.93 Å2ChemAxon
Rotatable Bond Count2ChemAxon
Refractivity95.21 m3·mol-1ChemAxon
Polarizability37.04 Å3ChemAxon
Number of Rings6ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET Features
Not Available

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available

Targets

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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]
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]
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]

Enzymes

Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Substrate
General Function
Glucuronosyltransferase activity
Specific Function
UDPGT is of major importance in the conjugation and subsequent elimination of potentially toxic xenobiotics and endogenous compounds.Its unique specificity for 3,4-catechol estrogens and estriol su...
Gene Name
UGT2B7
Uniprot ID
P16662
Uniprot Name
UDP-glucuronosyltransferase 2B7
Molecular Weight
60694.12 Da
References
  1. European Medicines Agency (EMA) Summary of product characteristics: Selincro (nalmefene) oral tablets [Link]
Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Substrate
General Function
Retinoic acid binding
Specific Function
UDPGT is of major importance in the conjugation and subsequent elimination of potentially toxic xenobiotics and endogenous compounds. Isoform 2 lacks transferase activity but acts as a negative reg...
Gene Name
UGT1A3
Uniprot ID
P35503
Uniprot Name
UDP-glucuronosyltransferase 1-3
Molecular Weight
60337.835 Da
References
  1. European Medicines Agency (EMA) Summary of product characteristics: Selincro (nalmefene) oral tablets [Link]
Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Substrate
General Function
Steroid binding
Specific Function
UDPGT is of major importance in the conjugation and subsequent elimination of potentially toxic xenobiotics and endogenous compounds. Isoform 2 lacks transferase activity but acts as a negative reg...
Gene Name
UGT1A8
Uniprot ID
Q9HAW9
Uniprot Name
UDP-glucuronosyltransferase 1-8
Molecular Weight
59741.035 Da
References
  1. European Medicines Agency (EMA) Summary of product characteristics: Selincro (nalmefene) oral tablets [Link]
Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Substrate
General Function
Vitamin d3 25-hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
Gene Name
CYP3A4
Uniprot ID
P08684
Uniprot Name
Cytochrome P450 3A4
Molecular Weight
57342.67 Da
References
  1. European Medicines Agency (EMA) Summary of product characteristics: Selincro (nalmefene) oral tablets [Link]
Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Substrate
General Function
Oxygen binding
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP3A5
Uniprot ID
P20815
Uniprot Name
Cytochrome P450 3A5
Molecular Weight
57108.065 Da
References
  1. European Medicines Agency (EMA) Summary of product characteristics: Selincro (nalmefene) oral tablets [Link]

Drug created at March 19, 2008 16:18 / Updated at July 01, 2022 11:43