Pharmacodynamic models

When pharmacological effects are seen immediately and are directly related to the drug concentra­tion, a pharmacodynamic model is applied to characterize the relationship between drug concentra­tions and effect. Phoenix includes the following PD models:

Model

Description

Effect at C=0

Effect at C=infinity

Model 101 

Simple Emax Model

0

Emax

Model 102 

Simple Emax Model

E0

Emax+E0

Model 103 

Inhibitory Effect E0 Model

E0

0

Model 104 

Inhibitory Effect Imax Model

E0

E0 – Imax

Model 105 

Sigmoid Emax Model

0

Emax

Model 106 

Sigmoid Emax Model

E0

Emax+E0

Model 107 

Inhibitory Effect Sigmoid E0 Model

E0

0

Model 108 

Inhibitory Effect Sigmoid Imax Model

E0

E0 – Imax

Notation definitions

Term

Definition

Emax

Maximum drug effect.

Imax

Maximum drug inhibition.

E0 

Baseline effect (effect at C=0).

EC50 

Concentration in plasma that achieves 50% of pre­dicted maximum effect in an Emax model.

IC50 

Drug concentration required to produce 50% of the maximal inhibition.

Rmax

Effect at infinity (includes maximum drug effect/inhibi­tion and baseline).

F_Emax

Fractional change in effect from baseline E0 

Gamma

Shape parameter

Model 101

Simple Emax model.

PD101.png 

E=(Emax*C)/(C+EC50)

Estimated parameters: Emax, EC50 

Model 102

Simple Emax model with a baseline effect parameter.

PD102.png 

E=E0+(Emax*C)/(C+EC50)

Estimated parameters: Emax, EC50, E0 
Secondary parameters: Rmax=Emax+E0,  F_Emax=Emax/E0 

Model 103

Inhibitory effect model.

PD103_1.png 

E=E0*(1 – (C/(C+IC50)))

Estimated parameters: E0, IC50 

Model 104

Inhibitory effect model with a baseline effect parameter.

PD104.png 

E=E0 – (Imax*C)/(C+IC50)

Estimated parameters: Imax, IC50, E0 
Secondary parameters: Rmax=E0 – Imax, F_Imax=Imax/E0 

Model 105

Sigmoid Emax model.

PD105.png 

E=(Emax*Cg)/(Cg+EC50g)

Estimated parameters: Emax, EC50, Gamma

Model 106

Sigmoid Emax model with a baseline effect parameter.

PD106.png 

E=E0+(Emax*Cy)/(Cg+EC50g)

Estimated parameters: Emax, EC50, E0, Gamma
Secondary parameters: Rmax=Emax+E0, F_E­max=Emax/E0 

Model 107

Sigmoid inhibitory effect model.

PD107.png 

E=E0*(1 – (Cg/(Cg+IC50g)))

Estimated parameters: E0, IC50, Gamma

Model 108

Sigmoid inhibitory effect model with a baseline effect parameter.

PD108.png 

E=E0 – (Imax*Cg)/(Cg+IC50g)

Estimated parameters: Imax, IC50, E0, Gamma
Secondary parameters: Rmax=E0 – Imax, F_I­max=Imax/E0 

 


Last modified date:6/26/19
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