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Table 1 Pharmacokinetic and pharmacodynamic models for donepezil.

From: Compliance assessment of ambulatory Alzheimer patients to aid therapeutic decisions by healthcare professionals

Model type (name) & equation

Variables and parameters

Reference

Pharmacokinetic model

(two compartment model)

   

C = D ⋅ [ A ⋅ e − α ( t − l a g t i m e ) + B ⋅ e − β ( t − l a g t i m e ) − ( A + B ) ⋅ e − k a ⋅ ( t − l a g t i m e ) ]

for D = 5 mg:

A = 3.502 ng/mL

B = 1.209 ng/mL

α = 0.445 h-1

β = 0.014 h

ka = 1.319 h-1

lag time = 0.96 h

for D = 10 mg:

A = 4.536 ng/mL

B = 1.234 ng/mL

α = 0.542 h-1

β = 0.015 h-1

ka = 1.696 h-1

lag time = 0.68 h

[32]

Pharmacodynamic model

(Emax model)

Emax = 100.8%

EC50 = 15.6 ng/mL

 

[34]

E = E max â‹… C E C 50 + C

   
  1. Parameter values and reference to literature, utilised for the in silico simulation.
  2. C = total plasma drug concentration [ng/mL]
  3. t = time [h]
  4. D = dose
  5. A, B = intercepts of the two exponential terms
  6. α, β = macro (hybrid) rate constants
  7. ka = absorption rate constant
  8. E = effect, i.e. inhibition of peripheral cholinesterase, %
  9. Emax = maximum effect
  10. EC50 = drug concentration at half of maximum effect