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- Approved, Investigational, Withdrawn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
Structure for Nalmefene (DB06230)
- 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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- Contraindications & Blackbox Warnings
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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 agonistHumans ADelta-type opioid receptor antagonistHumans AMu-type opioid receptor antagonistHumans - 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
Improve decision support & research outcomesWith structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates.Improve decision support & research outcomes with our structured adverse effects data.- 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.
Drug Interaction Integrate drug-drug
interactions in your softwareAbacavir 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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- 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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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 US 
Revex Injection, solution 0.1 mg/1mL Intravenous Baxter Laboratories 2006-06-19 Not applicable US Selincro Tablet, film coated 18 mg Oral H. Lundbeck A/S 2016-09-08 Not applicable EU 
Selincro Tablet, film coated 18 mg Oral H. Lundbeck A/S 2016-09-08 Not applicable EU Selincro Tablet, film coated 18 mg Oral H. Lundbeck A/S 2016-09-08 Not applicable EU Selincro Tablet, film coated 18 mg Oral H. Lundbeck A/S 2016-09-08 Not applicable EU Selincro Tablet, film coated 18 mg Oral H. Lundbeck A/S 2016-09-08 Not applicable EU Selincro Tablet, film coated 18 mg Oral H. Lundbeck A/S 2016-09-08 Not applicable EU Selincro Tablet, film coated 18 mg Oral H. Lundbeck A/S 2016-09-08 Not applicable EU Selincro Tablet, film coated 18 mg Oral H. Lundbeck A/S 2016-09-08 Not applicable EU - 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 US
Categories
- ATC Codes
- N07BB05 — Nalmefene
- 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 show 4 more
- 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
- 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]
- 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]
- 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]
- Authors unspecified: Nalmefene . [Article]
- 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]
- 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]
- European Medicines Agency (EMA) Summary of product characteristics: Selincro (nalmefene) oral tablets [Link]
- DailyMed Label: NALMEFENE HYDROCHLORIDE injection, solution for intravenous, intramuscular, or subcutaneous use [Link]
- EMA Assessment Report: Selincro (nalmafene) oral tablets [Link]
- Australian Public Assessment Report: Nalmefene (as hydrochloride dihydrate) [Link]
- External Links
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 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 2, 3 Completed Treatment Pathological Gambling Disorder 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
- 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
- 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]
- 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]
- 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
- 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]
- 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]
- 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]
- 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
- 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]
- 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]
- 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
- 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
- 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
- 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
- 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
- European Medicines Agency (EMA) Summary of product characteristics: Selincro (nalmefene) oral tablets [Link]
Drug created at March 19, 2008 16:18 / Updated at June 24, 2022 07:32