Pharmacokinetics
Philip Rowe
Description
Content
- ADME and Pharmacokinetics
- ADME – Absorption Distribution, Metabolism and Excretion
- Pharmacokinetics
- Absorption: Absorption rate constant, Bioavailability and Salt factor
- Passive diffusion and other mechanisms by which drugs may cross biological membranes
- Rate of drug absorption and the Absorption rate constant (Ka)
- Bioavailability
- Salt factor
- Distribution: Compartments and Volume of Distribution
- The rate of distribution and compartments
- One compartment model
- Two compartment model
- The extent of distribution
- Volume of distribution
- Using the volume of distribution to calculate dose size
- Practice calculations
- Elimination: Elimination rate constant, half-life and clearance
- Elimination rate constant and half-life
- Clearance
- Practice calculations
- Single intravenous bolus injection into one compartment
- Concentration versus time graph
- Relationship between time and concentration
- Area Under the Curve (AUC)
- Practice calculations
- Appendix 1
- Appendix 2
- Analysis of experimental data from a bolus i.v
- injection into one compartment
- Analysis of clinical trials data
- Analysis of data arising in a clinical setting
- Practice calculations
- Appendix 1
- Appendix 2
- Single intravenous bolus injection into two compartments
- The model to be considered
- Drug concentrations in blood and the rest of the first compartment
- Determining how many compartments a drug occupies
- Drug concentration in the second compartment
- Two compartment systems and therapeutic drug monitoring for digoxin
- Constant intravenous infusion
- The model to be considered
- Concentration versus time curve during infusion
- Relationship between rate of infusion and concentration at steady state
- Loading doses
- The accumulation period
- Practice questions
- Appendix
- Extravascular administration
- The situation to be considered
- Concentration versus time curve
- Changing the rate of absorption
- Cmax and Tmax
- Determination of bioavailability for extravascular doses
- Trapezoidal rule – A practical method to measure AUC
- Practice question
- Appendix
- Multiple dosing
- Pharmacokinetic accumulation and steady state
- Multiple extravascular doses
- Concentrations at steady state
- Loading dose
- Accumulation stage
- Extent of fluctuation in drug concentrations
- Practice questions
- Appendix
- Non-linear pharmacokinetics
- Considering drug metabolism as an enzyme catalysed reaction
- Exceptions to linearity
- Effect of non-linearity on the relationship between dose and drug concentration
- Clinical significance of non-linear kinetics
- Non-linear kinetics and drug development
- Non-compartmental pharmacokinetics
- The case for non-compartmental methods
- Calculation methods
- More complex situations
- Computerized analysis of pharmacokinetic data
- Least squares fitting
- Practice question
- Creatinine clearance
- Clearance of creatinine and various drugs
- Digoxin dosing
- Practice questions
- Pharmacokinetic symbols and equations
- Symbols
- Cockcroft and Gault equations
- Additional material available from the internet
- Answers to practice questions
Download
 are described, with an emphasis...){kind=link}