PHARMACODYNAMICS

THE ACTION OF THE DRUG

ON THE BODY

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 Cont...
Pharmacodynamics is the study of the biochemical
and physiological effects of drugs on the body or on
microorganisms or parasites within or on the body and the
mechanisms of drug action and the relationship between
drug concentration and effect.

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 Plasma Site of
Dosage Effects
Concen. Action

Pharmacokinetics Pharmacodynamics

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 Definition…
Drug Action: Drug action is the initial
interaction of a drug with cells at the
site of action & the resultant
physiological & biochemical
consequences are the drug effect.

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 Receptor binding..

Agonist.

Drug-Receptor
Antagonist
interaction

Partial Agonist.
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 AGONIST : which produces a stimulation type
response. The agonist is a very close mimic and "fits"
with the receptor site and is thus able to initiate a
response.
 ANTAGONIST : interacts with the receptor site and
blocks or depresses the normal response for that
receptor because it only partially fits the receptor site
and can not produce an effect. However, it does block
the site preventing any other agonist or the normal
neurotransmitter from interacting with the receptor
site.

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 PARTIAL AGONISTS are drugs that bind to and
activate a given receptor, but have only
partial efficacy at the receptor relative to a full
agonist. when both a full agonist and partial agonist
are present, the partial agonist actually acts as
a competitive antagonist, competing with the full
agonist for receptor occupancy and producing a net
decrease in the receptor activation observed with the
full agonist alone.

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 INVERSE AGONIST is an agent that binds to
the same receptor as an agonist but induces a
pharmacological response opposite to that
agonist.

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 Dose response curves of a full agonist, partial agonist,
neutral antagonist and inverse agonist
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POTENCY is the relationship between the dose of a drug
and the therapeutic effect. It refers to the drug's
strength. A drug is considered potent when a small
amount of the drug achieves the intended effect. or
 Amount of a drug needed to produce a given effect
 Determined mainly by the affinity of the receptor for
the drug
 Potency affects drug dosage
 Relatively unimportant in clinical use of drugs
 Are more potent drugs superior therapeutic agent?

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 EFFICACY is the ability of a drug to produce the desired
therapeutic effect. Efficacy means that the drug is
effective. When comparing two drugs that work
equally, the one with the lower dose has a higher
potency. They have equal efficacy. Or
The maximal effect that can be produced by a drug
determined mainly by the properties of the drug and
its receptor-effector system
 Important clinical measure
 Partial agonist have lower maximal efficacy than full
agonist

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 Dose response curves
 The relationship of dose to response can be
illustrated as a graph called as dose response curve.
• Dose-response curves can be used to plot the
results of many kinds of experiments.

• The X-axis plots concentration of a drug

• The Y-axis plots response

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 Used to measure
• Drug potency

• Drug efficacy

• Drug safety

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 Potency
HI B
A
Average
Response
Magnitude

0 X
DRUG DOSE
A is more potent than B

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Maximum Efficacy
HI B

A
Average
Response
Magnitude

LO
0 X
DRUG DOSE

B has greater max efficacy than A

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 Type of Dose-Response Curves
 Graded
•Measured in a single biologic unit
• Continuous scale (↑dose →↑effect)
• Relates dose to intensity of effect
 Quantal
• Population studies
• All-or-none pharmacologic effect
• Relates dose to frequency of effect

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 Therapeutic Index - TI
• Ratio of dose to produce toxic effect to dose to
produce desired effect
• TI = LD50/ED50
• The larger the ratio, the greater the safety (e.g. 10)

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 Therapeutic Index and Margin of Safety
• The Therapeutic Index (TI) is used to compare the
therapeutically effective dose to the toxic dose. The
TI is a statement of relative safety of a drug. It is the
ratio of the dose producing toxicity to the dose
needed to produce the desired therapeutic response.
• The common method used to derive the TI is to use
the 50% dose-response points. For example, if the
LD50 is 200 and the ED50 is 20 mg, the TI would be
10 (200/20). A clinician would consider a drug safer
if it had a TI of 10 than if it had a TI of 3.

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 TI = LD50/ ED50
ED LD
100

% subjects 50

0
0 X
DRUG DOSE
• Relatively safe ~
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 TI = LD50/ ED50
ED LD
100

% subjects 50

0
0 X
DRUG DOSE
• Less safe drug ~
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 Agonist and Antagonist
Affinity Efficacy
• Agonist yes high
• Partial agonist yes low
• Antagonist
– Competitive low-medium no
– Non-competitive high no

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