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The central paradigm of clinical pharmacology: The
dose-concentration-effect relationship
Efficacy
Dose concentration
pharmacokinetics Toxicity
Pharmacodynamic
Introduction
• Pharmacokinetics describes the time course of
a drug in a body fluid, preferably plasma or
blood, that results from the administration of
a certain dosage regimen.
• It comprises all processes affecting drug
absorption, distribution, metabolism, and
excretion.
• Simplified, pharmacokinetics characterizes
what the body does to the drug.
• In contrast, pharmacodynamic characterizes
the intensity of a drug effect or toxicity
resulting from certain drug concentration in a
body fluid, usually at the assumed site of drug
action. It can be simplified to what the drug
does to the body
Protein bound drug Tissue bound drug
Drug Absorption Distribution
s
Plasma concentration Tissue concentration c
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n
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k
Elimination o
c
a
m
r
a
Drug bound h
Metabolism Drug in effect to P
Excretion compartment Receptor/
effector
s
c
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Post-receptor m
events a
n
y
biochemical d
o
events c
a
Pharmacological m
r
response a
h
P
• General pharmacokinetic and pharmacodynamic
principles are to a large extent equally applicable to
protein and peptide drugs as they are to traditional
small molecule-based therapeutics.
• Deviations from some of these principles and additional
challenges with regard to the characterization of the
pharmacokinetics and pharmacodynamics of peptide
and protein therapeutics, however, arise from some of
their specific properties:
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