modelProguanil

Extends from Pharmacolibrary.Drugs.ATC.P.P01BB01.

Information

name:Proguanil
ATC code:P01BB01
route:oral
compartments:1
dosage:200mg
volume of distribution:342L
clearance:23L/h
other parameters in model implementation

Proguanil is an antimalarial drug, primarily used for the prevention and treatment of malaria, often in combination with atovaquone. It acts by inhibiting dihydrofolate reductase in the malaria parasite. Proguanil is still approved and in clinical use for malaria prophylaxis.

Pharmacokinetics

Pharmacokinetic parameters reported in healthy adult volunteers following a single oral dose of proguanil.

References

  1. Hussein, Z, et al., & Canfield, CJ (1996). Population pharmacokinetics of proguanil in patients with acute P. falciparum malaria after combined therapy with atovaquone. British journal of clinical pharmacology 42(5) 589–597. DOI:10.1111/j.1365-2125.1996.tb00114.x PUBMED:https://pubmed.ncbi.nlm.nih.gov/8951190

  2. Helsby, NA, et al., & Breckenridge, AM (1990). The pharmacokinetics and activation of proguanil in man: consequences of variability in drug metabolism. British journal of clinical pharmacology 30(4) 593–598. DOI:10.1111/j.1365-2125.1990.tb03818.x PUBMED:https://pubmed.ncbi.nlm.nih.gov/2291871

  3. McGready, R, et al., & Nosten, F (2003). The pharmacokinetics of atovaquone and proguanil in pregnant women with acute falciparum malaria. European journal of clinical pharmacology 59(7) 545–552. DOI:10.1007/s00228-003-0652-9 PUBMED:https://pubmed.ncbi.nlm.nih.gov/12955371

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.TransferRateka (from PK_1C_enteral)0.016666666666666666first order absorption rate
Modelica.Units.SI.TimeTlag (from PK_1C_enteral)600delay between oral administration and absorption (default 10min)

Connectors

TypeNameDefaultDescription
Types.ConcentrationOutputC_central (from PK_1C)
Interfaces.ConcentrationPort_bcentralCPort (from PK_1C)

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

Revisions

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