modelPyrimethamine
Extends from Pharmacolibrary.Drugs.ATC.P.P01BD01.
Information
| name: | Pyrimethamine | |
| ATC code: | P01BD01 | route: | oral |
| compartments: | 1 | |
| dosage: | 75 | mg |
| volume of distribution: | 2.3 | L |
| clearance: | 0.024 | L/h/kg |
| other parameters in model implementation | ||
Pyrimethamine is an antiparasitic compound primarily used in combination therapy for the treatment and prevention of malaria, particularly due to its activity against Plasmodium falciparum. It has also been used to treat toxoplasmosis, in combination with a sulfonamide. The drug acts by inhibiting dihydrofolate reductase, disrupting folic acid metabolism in parasites. Pyrimethamine remains in clinical use today.
Pharmacokinetics
Pharmacokinetic parameters reported in healthy adult volunteers following oral administration.
References
Iida, T, et al., & Gross, AS (2020). Evaluation of the Pharmacokinetics, Safety, and Tolerability of a Single Oral Dose of Pyrimethamine in Healthy Male Subjects of Japanese and European Ancestry. Clinical pharmacology in drug development 9(6) 768–773. DOI:10.1002/cpdd.771 PUBMED:https://pubmed.ncbi.nlm.nih.gov/31950646
Hussein, Z, et al., & Canfield, CJ (1997). Population pharmacokinetics of atovaquone in patients with acute malaria caused by Plasmodium falciparum. Clinical pharmacology and therapeutics 61(5) 518–530. DOI:10.1016/S0009-9236(97)90132-6 PUBMED:https://pubmed.ncbi.nlm.nih.gov/9164414
Wang, NS, et al., & Arnold, K (1990). Pharmacokinetics of the combination pyrimethamine with sulfadoxine and mefloquine (FANSIMEF) in Chinese volunteers and the relative bioavailability of a lacquered tablet. Chemotherapy 36(3) 177–184. DOI:10.1159/000238764 PUBMED:https://pubmed.ncbi.nlm.nih.gov/2338028
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.TransferRate | ka (from PK_1C_enteral) | 0.016666666666666666 | first order absorption rate |
| Modelica.Units.SI.Time | Tlag (from PK_1C_enteral) | 600 | delay between oral administration and absorption (default 10min) |
Connectors
| Type | Name | Default | Description |
|---|---|---|---|
| Types.ConcentrationOutput | C_central (from PK_1C) | ||
| Interfaces.ConcentrationPort_b | centralCPort (from PK_1C) |
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 |
Revisions
- 06/2025 Tomas Kulhanek, generated model from data extracted from PUBMED, DrugBank and LLM(GPT4.1)