BASIC PHARMACOKINETICS:

AHS
Dr. Ramanujam Narayanan, MBBS, MD (Pharmacology), PhD,
Professor (Pharmacology),
Department of Pharmacology,
PSG Institute of Medical Sciences & Research,
Coimbatore
 Contents…
• Pharmacokinetics: definition

• Pharmacokinetic processes

• Pharmacokinetic parameters

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 Pharmacokinetics: definition
• The branch of Pharmacology that deals with
the study of physical, chemical and biological
processes of drug disposition from the site of
administration to the site of action(s) for
therapeutic and adverse / toxic effects
– What the body does to the drug

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 Pharmacokinetic processes
• Absorption
• Distribution & Binding
• Metabolism / Biotransformation*
• Excretion*
– Elimination *

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 Pharmacokinetic parameters
PROCESS ABBREVIATION PARAMETER
ABSORPTION F Bioavailability &
Bioequivalence
Cmax Maximum concentration attained
Tmax Time to Cmax
DISTRIBUTION Vd Volume of distribution
Vss Vd at steady state
METABOLISM & EXCRETION T½ Half-life
= ELIMINATION

EXCRETION CL Clearance

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 BIOAVAILABILITY
• The fraction of drug administered by a route
that reaches the systemic circulation in the
unchanged form

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 BIOEQUIVALENCE
• Two formulations of a drug are said to be
bioequivalent when the rates and extent of
their absorption do not differ significantly
under standard / suitable test conditions

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 Cmax & Tmax

• Cmax  Extent of drug absorption

• Tmax  Rate of drug absorption

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 Volume of distribution
• The apparent volume which could
accommodate the amount of drug
administered if its concentration were similar
to that in the plasma compartment

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 Half-life
• The time taken to excrete fifty percent of total
drug dose administered in the body by a
particular route of elimination

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 Clearance
• The rate of elimination of drug from the body
after a specified time interval by a particular
route of excretion

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 Clinical relevance
PARAMETER SIGNIFICANCE
Bioavailability Extent & rate of absorption
Formulation choice
Route of administration
Onset & duration of action
Volume of distribution Tissue & Plasma protein binding
Cumulation
Removal by extracorporeal methods (dialysis)
Half-life Adverse effects
Toxicity (therapeutic versus toxic margin)
Dosing strategy
Clearance Target organ toxicity
Dosing modification
Cumulative effects
Metabolic efficiency (detoxification)

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