Kinetics of drugs and their metabolites and dosage regimen design

Learning Objectives:

At the end of the course, the student is expected to understand the biologic fate of drugs and apply this in drug development. Specifically the student should be able to: 

  • To evaluate the important pharmacokinetic parameters for different compartmental models; 
  • To design the appropriate dosage regimen for the drug product

  1. Define pharmacodynamics and pharmacokinetics 

  1. Understand the processes that control the dose-response relationships 

  1. Appreciate in a general way how mathematical expressions in pharmacodynamics and pharmacokinetics can be used for the rational determination of optimum dosing regimens 

  2. Distinguish diffusion and transporter-mediated passage

  1. Distinguish transcellular and paracellular transport 

  1. Identify membrane and drug factors that control passive diffusion 

  1. Distinguish uptake and efflux transporters 

  1. Become familiar with members of the SLC and ABC superfamilies 

  1. Understand how transporters affect pharmacokinetics and pharmacodynamics 


  1. Define local and systemic drug administration 

  1. Describe common routes of drug administration and their characteristics 

  1. Characterize the steps involved in oral absorption 

  1. Define the bioavailability factor 

  1. Categorize the components of F: Fa, Fg and Fh 

  1. Identify the drug formulation, and biological determinants of bioavailability 

  1. Understand the determinants of the rate of drug absorption 

  1. Define the biopharmaceutical classification system 

  1. Understand how the BCS and BDDCS can be applied 


  1. Understand the factors that control a drug’s distribution from the plasma to the tissues 

  1. Know the main physiological volumes that a drug may access 

  1. Understand the influence of plasma protein and tissue binding on the distribution profile 

  1. Understand how the apparent volume of distribution expresses the distribution of a drug between plasm and the rest of the body 

  1. Understand the factors that control plasma protein binding 

  1. Appreciate the clinical significance of altered protein binding 

  1. Understand the factors that control the rate of drug distribution 

  1. Appreciate some unique aspects of drug distribution to the central nervous system 


  1. Identify the major routes of drug elimination 

  1. Apply first-order kinetics to drug elimination 

  1. Understand how clearance is used to express drug elimination 

  1. Understand the relationships, among clearance, volume of distribution and the rate of elimination 

  1. Understand the factors that control renal clearance: glomerular filtration, tubular secretion and tubular reabsorption 

  1. Identify the major enzymes involved in drug metabolism 

  1. Identify the characteristics of metabolism-based drug-drug interactions 

  1. Know the role of the major drug transporters in hepatic clearance 

  1. Understand the factors that control hepatic clearance 

  1. Distinguish the effects of modifiers of drug metabolism on the pharmacokinetics of nonrestrictively and restrictively cleared dugs 

  1. Determine total body and renal clearance from clinical data


Basic pharmacokinetics and pharmacodynamics

by Sara E. Rosenbaum

Applied biopharmaceutics and pharmacokinetics

by Leon Shargel

Drug disposition and pharmacokinetics principles to applications

by Stephen Curry and Robin Whelpton