modelR06AX19

Extends from Pharmacokinetic.Models.PK_1C.

Information

name:Azelastine
ATC code:R06AX19
route:intranasal
compartments:1
dosage:0.14mg
volume of distribution:14.5L
clearance:0.5L/h/kg
other parameters in model implementation

Azelastine is a selective histamine H1 receptor antagonist with additional anti-inflammatory and mast cell stabilizing properties. It is primarily used for the symptomatic relief of allergic rhinitis and conjunctivitis. It is available as a nasal spray and ophthalmic solution, and is approved for use in many countries, including for prescription and over-the-counter use.

Pharmacokinetics

PK parameters reported for healthy adult volunteers after single and multiple intranasal administrations.

References

  1. Wolthers, OD (2013). New patents of fixed combinations of nasal antihistamines and corticosteroids in allergic rhinitis. Recent patents on inflammation & allergy drug discovery 7(3) 223–228. DOI:10.2174/1872213x113079990019 PUBMED:https://pubmed.ncbi.nlm.nih.gov/23862774

  2. Simons, FE, & Simons, KJ (1999). Clinical pharmacology of new histamine H1 receptor antagonists. Clinical pharmacokinetics 36(5) 329–352. DOI:10.2165/00003088-199936050-00003 PUBMED:https://pubmed.ncbi.nlm.nih.gov/10384858

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

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)