Clinical Pharmacokinetics
Dr.Justin Kurian
Lecturer
JSS College of Pharmacy
• Clinical pharmacokinetics is the application of
pharmacokinetic methods to drug therapy.
• Clinical pharmacokinetics involves a
multidisciplinary approach to individually
optimized dosing strategies based on the
patient's disease state and patient-specific
considerations.
• Clinical pharmacokinetics is the study of the
relationships between drug dosage regimens
and concentration–time profiles
The three fundamental parameters - control
these relationships are:
• Clearance
• Volume of distribution
• Elimination half-life
• Volume of distribution - Loading Dose
• Clearance - the dose rate required to
maintain a target concentration
• Elimination half-life - dosage interval
• Age, gender, genetic, and ethnic differences
can also result in pharmacokinetic differences
that may affect the outcome of drug therapy.
• The study of pharmacokinetic differences of
drugs in various population groups is termed
as Population Pharmacokinetics
• Pharmacokinetics is also applied to therapeutic drug
monitoring (TDM) for very potent drugs such as
those with a narrow therapeutic range, in order to
optimize efficacy and to prevent any adverse toxicity.
Toxicokinetics and Clinical Toxicology
• Toxicokinetics is the application of pharmacokinetic
principles to the design, conduct, and interpretation
of drug safety evaluation studies and in validating
dose-related exposure in animals.
• Clinical toxicology is the study of adverse effects of
drugs and toxic substances (poisons) in the body.
Pharmacodynamics
• Pharmacodynamics refers to the relationship
between the drug concentration at the site of action
(receptor) and pharmacologic response, including
biochemical and physiologic effects that influence
the interaction of drug with the receptor.
Application of Clinical Pharmacokinetics
• Individualization of Drug Dosage Regimens
• Therapeutic Drug Monitoring
• Dosage Adjustment in renal and hepatic failure
• Design of Dosage Regimens
• Conversion from Intravenous Infusion to Oral
Dosing.
• Dosing of Drugs in Infants and Children
• Drug drug interaction
Pharmacokinetic Model
• A model is a hypothesis using mathematical terms
to describe quantitative relationships concisely.
• Pharmacokinetic parameters
• Simulate the rate processes of drug absorption,
distribution, and elimination to describe and
predict drug concentrations in the body as a
function of time.
Pharmacokinetic models are used to
• Predict plasma, tissue, and urine drug levels
with any dosage regimen
• Calculate the optimum dosage regimen for
each patient individually
• Estimate the possible accumulation of drugs
and/or metabolites
• Correlate drug concentrations with
pharmacologic or toxicologic activity
• Evaluate differences in the rate or extent of
availability between formulations
(bioequivalence)
• Describe how changes in physiology or disease
affect the absorption, distribution, or
elimination of the drug
• Explain drug interactions
Pharmacokinetic Model
1. Compartment Models
Mammillary Model
Catenary Model
2. Physiologic Pharmacokinetic Model (Flow Model)
Significance of Measuring Plasma Drug
Concentrations
• Intensity of the pharmacologic or toxic effect
of a drug – PDC
• Individual variations in the pharmacokinetics
of drugs are quite common
• Ascertains that the calculated dose actually
delivers the plasma level required for
therapeutic effect.
• Patient's physiologic functions may be affected
by disease, nutrition, environment, concurrent
drug therapy.
• Adjustment of the drug dosage in order to
individualize and optimize therapeutic drug
regimens
• Pharmacodynamic response – Importance
