modelNalmefene

Diagram of Nalmefene

Extends from Pharmacolibrary.Drugs.ATC.N.N07BB05.

Information

name:Nalmefene
ATC code:N07BB05
route:oral
compartments:2
dosage:18mg
volume of distribution:1.5L
clearance:28L/h
other parameters in model implementation

Nalmefene is an opioid receptor modulator, primarily used to reduce alcohol consumption in adults with alcohol dependence. It acts as an antagonist at the mu and delta opioid receptors and a partial agonist at the kappa opioid receptor. It is approved in several countries (e.g., in the EU) as a prescription medication for the reduction of alcohol consumption in patients with alcohol dependence.

Pharmacokinetics

Pharmacokinetic parameters reported in healthy adult volunteers after single oral administration.

References

  1. Kyhl, LE, et al., & Areberg, J (2016). Population pharmacokinetics of nalmefene in healthy subjects and its relation to μ-opioid receptor occupancy. British journal of clinical pharmacology 81(2) 290–300. DOI:10.1111/bcp.12805 PUBMED:https://pubmed.ncbi.nlm.nih.gov/26483076

  2. Palpacuer, C, et al., & Naudet, F (2015). Risks and Benefits of Nalmefene in the Treatment of Adult Alcohol Dependence: A Systematic Literature Review and Meta-Analysis of Published and Unpublished Double-Blind Randomized Controlled Trials. PLoS medicine 12(12) e1001924–None. DOI:10.1371/journal.pmed.1001924 PUBMED:https://pubmed.ncbi.nlm.nih.gov/26694529

Parameters

TypeNameDefaultDescription
Modelica.Units.SI.Massweight (from PK_1C)75patient weight (kg)
Modelica.Units.SI.SpecificVolumeVdPerKg (from PK_1C)0.9Volume of distribution (L/kg)
Modelica.Units.SI.MassFractionF (from PK_1C)0.8bioavailiability (0-1)
Pharmacolibrary.Types.ClearanceCl (from PK_1C)20clearance
Modelica.Units.SI.TimeadminTime (from PK_1C)60first administration time (s)
Modelica.Units.SI.TimeadminDuration (from PK_1C)600administration duration (s)
Modelica.Units.SI.TimeadminPeriod (from PK_1C)8*60*60period of administration (default 8 hours)(s)
Pharmacolibrary.Types.MassadminMass (from PK_1C)1000administration mass (mg)
IntegeradminCount (from PK_1C)8number of dose administered (1)
Pharmacolibrary.Types.VolumeVd (from PK_1C)VdPerKg*weightVolume of distribution (m3)
Pharmacolibrary.Types.MassConcentrationCmin (from PK_1C)0.004minimal therapeutic range
Pharmacolibrary.Types.MassConcentrationCmax (from PK_1C)0.008minimal therapeutic range
Pharmacolibrary.Types.MassConcentrationCtox_peak (from PK_1C)0.012toxicity peak level
Pharmacolibrary.Types.MassConcentrationCtox_trough (from PK_1C)0.006toxicity trough level
Pharmacolibrary.Types.VolumeVdp (from PK_2C)VdpPerKg*weightVolume of distribution (m3)
Modelica.Units.SI.SpecificVolumeVdpPerKg (from PK_2C)0.9Volume of distribution peripheral(l/kg)
Pharmacolibrary.Types.Clearancek12 (from PK_2C)1intercompartmental C-P clearance
Pharmacolibrary.Types.Clearancek21 (from PK_2C)1intercompartmental P-C clearance
Pharmacolibrary.Types.TransferRateka (from PK_2C_enteral)0.016666666666666666first order absorption rate
Modelica.Units.SI.TimeTlag (from PK_2C_enteral)600delay between oral administration and absorption (default 10min)

Connectors

TypeNameDefaultDescription
Types.ConcentrationOutputC_central (from PK_1C)
Interfaces.ConcentrationPort_bcentralCPort (from PK_1C)
Interfaces.ConcentrationPort_bperipheralCPort (from PK_2C)
Pharmacolibrary.Types.ConcentrationOutputC_peripheral1 (from PK_2C)

Components

TypeNameDefaultDescription
Pharmacokinetic.NoPerfusedTissueCompartmentcentral (from PK_1C)
Pharmacokinetic.ClearanceDrivenEliminationelim (from PK_1C)
Sources.PeriodicDoseperiodicDose (from PK_1C)
Modelica.Units.SI.Timet1_2 (from PK_1C)elimination half-life
Pharmacolibrary.Pharmacokinetic.TransferFirstOrderNonSymtransfer (from PK_2C)
Pharmacolibrary.Pharmacokinetic.NoPerfusedTissueCompartmentperipheral (from PK_2C)

Revisions

  • 06/2025 Tomas Kulhanek, generated model from data extracted from PUBMED, DrugBank and LLM(GPT4.1)