modelMethylnaltrexoneBromide
Extends from Pharmacolibrary.Drugs.ATC.A.A06AH01.
Information
| name: | MethylnaltrexoneBromide | |
| ATC code: | A06AH01 | route: | subcutaneous |
| compartments: | 2 | |
| dosage: | 12 | mg |
| volume of distribution: | 20 | L |
| clearance: | 15 | L/h |
| other parameters in model implementation | ||
Methylnaltrexone bromide is a peripherally-acting μ-opioid receptor antagonist (PAMORA) used to treat opioid-induced constipation in adult patients with chronic non-cancer pain or advanced illness. It is approved for clinical use and marketed under several names, including Relistor.
Pharmacokinetics
Pharmacokinetic parameters reported in healthy adult subjects after a single subcutaneous injection.
References
Rotshteyn, Y, et al., & Yuan, CS (2011). Methylnaltrexone bromide: research update of pharmacokinetics following parenteral administration. Expert opinion on drug metabolism & toxicology 7(2) 227–235. DOI:10.1517/17425255.2011.549824 PUBMED:https://pubmed.ncbi.nlm.nih.gov/21222554
Mozaffari, S, et al., & Abdollahi, M (2018). Methylnaltrexone bromide for the treatment of opioid-induced constipation. Expert opinion on pharmacotherapy 19(10) 1127–1135. DOI:10.1080/14656566.2018.1491549 PUBMED:https://pubmed.ncbi.nlm.nih.gov/29979903
Zhang, D, et al., & Liu, H (2018). Pharmacokinetic study of methylnaltrexone after single and multiple subcutaneous administrations in healthy Chinese subjects. Xenobiotica; the fate of foreign compounds in biological systems 48(8) 804–808. DOI:10.1080/00498254.2017.1364449 PUBMED:https://pubmed.ncbi.nlm.nih.gov/28776489
Parameters
| Type | Name | Default | Description |
|---|---|---|---|
| Modelica.Units.SI.Mass | weight (from PK_1C) | 75 | patient weight (kg) |
| Modelica.Units.SI.SpecificVolume | VdPerKg (from PK_1C) | 0.9 | Volume of distribution (L/kg) |
| Modelica.Units.SI.MassFraction | F (from PK_1C) | 0.8 | bioavailiability (0-1) |
| Pharmacolibrary.Types.Clearance | Cl (from PK_1C) | 20 | clearance |
| Modelica.Units.SI.Time | adminTime (from PK_1C) | 60 | first administration time (s) |
| Modelica.Units.SI.Time | adminDuration (from PK_1C) | 600 | administration duration (s) |
| Modelica.Units.SI.Time | adminPeriod (from PK_1C) | 8*60*60 | period of administration (default 8 hours)(s) |
| Pharmacolibrary.Types.Mass | adminMass (from PK_1C) | 1000 | administration mass (mg) |
| Integer | adminCount (from PK_1C) | 8 | number of dose administered (1) |
| Pharmacolibrary.Types.Volume | Vd (from PK_1C) | VdPerKg*weight | Volume of distribution (m3) |
| Pharmacolibrary.Types.MassConcentration | Cmin (from PK_1C) | 0.004 | minimal therapeutic range |
| Pharmacolibrary.Types.MassConcentration | Cmax (from PK_1C) | 0.008 | minimal therapeutic range |
| Pharmacolibrary.Types.MassConcentration | Ctox_peak (from PK_1C) | 0.012 | toxicity peak level |
| Pharmacolibrary.Types.MassConcentration | Ctox_trough (from PK_1C) | 0.006 | toxicity trough level |
| Pharmacolibrary.Types.Volume | Vdp (from PK_2C) | VdpPerKg*weight | Volume of distribution (m3) |
| Modelica.Units.SI.SpecificVolume | VdpPerKg (from PK_2C) | 0.9 | Volume of distribution peripheral(l/kg) |
| Pharmacolibrary.Types.Clearance | k12 (from PK_2C) | 1 | intercompartmental C-P clearance |
| Pharmacolibrary.Types.Clearance | k21 (from PK_2C) | 1 | intercompartmental P-C clearance |
Connectors
| Type | Name | Default | Description |
|---|---|---|---|
| Types.ConcentrationOutput | C_central (from PK_1C) | ||
| Interfaces.ConcentrationPort_b | centralCPort (from PK_1C) | ||
| Interfaces.ConcentrationPort_b | peripheralCPort (from PK_2C) | ||
| Pharmacolibrary.Types.ConcentrationOutput | C_peripheral1 (from PK_2C) |
Components
| Type | Name | Default | Description |
|---|---|---|---|
| Pharmacokinetic.NoPerfusedTissueCompartment | central (from PK_1C) | ||
| Pharmacokinetic.ClearanceDrivenElimination | elim (from PK_1C) | ||
| Sources.PeriodicDose | periodicDose (from PK_1C) | ||
| Modelica.Units.SI.Time | t1_2 (from PK_1C) | elimination half-life | |
| Pharmacolibrary.Pharmacokinetic.TransferFirstOrderNonSym | transfer (from PK_2C) | ||
| Pharmacolibrary.Pharmacokinetic.NoPerfusedTissueCompartment | peripheral (from PK_2C) |
Revisions
- 06/2025 Tomas Kulhanek, generated model from data extracted from PUBMED, DrugBank and LLM(GPT4.1)