Pharmacokinetics, Pharmacodynamics, and Dose Optimization ...
Pharmacokinetics a. route of administration b. absorption and elimination Pharmacodynamics a....
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Transcript of Pharmacokinetics a. route of administration b. absorption and elimination Pharmacodynamics a....
Pharmacokineticsa. route of administrationb. absorption and elimination
Pharmacodynamicsa. dose-effect curveb. therapeutic indexc. ligand bindingd. agonist vs. antagoniste. neurotransmitter systems
Pharmacokineticsa. route of administrationb. absorption and elimination
Pharmacodynamicsa. dose-effect curveb. therapeutic indexc. ligand bindingd. agonist vs. antagoniste. neurotransmitter systems
Routes of Administration
a. oral easy self-administration prolonged effect stomach distress some drugs not orally effective
b. topical applied only to needed area poor absorption
c. rectal infants and unconscious adults variable absorption
d. inhalation rapid onset/offset irritation
e. injection rapid onset good control of dosage requires sterile conditions
Injection Route
a. Intravenous (i.v.)- into vein
b. Subcutaneous (s.c.)- under skin c. Intraperitoneal (i.p.)- into peritoneal cavity d. Intracerebroventricular (i.c.v.)- into cerebral ventricle e. Intrathecal- into spinal fluid
f. Epidural- into space that surrounds the dura of spinal cord
g. Intramuscular (i.m.)- into muscle
Pharmacokineticsa. route of administrationb. absorption and elimination
Pharmacodynamicsa. dose-effect curveb. therapeutic indexc. ligand bindingd. agonist vs. antagoniste. neurotransmitter systems
Pharmacokineticsa. route of administrationb. absorption and elimination
Pharmacodynamicsa. dose-effect curveb. therapeutic indexc. ligand bindingd. agonist vs. antagoniste. neurotransmitter systems
Comparing Dose-Effect CurvesComparing Dose-Effect Curves
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1 10 100 10000
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% of Maximal % of Maximal EffectEffect
[Drug][Drug]
Drug ADrug A
Drug CDrug C
Drug BDrug B
Pharmacokineticsa. route of administrationb. absorption and elimination
Pharmacodynamicsa. dose-effect curveb. therapeutic indexc. ligand bindingd. agonist vs. antagoniste. neurotransmitter systems
Pharmacokineticsa. route of administrationb. absorption and elimination
Pharmacodynamicsa. dose-effect curveb. therapeutic indexc. ligand bindingd. agonist vs. antagoniste. neurotransmitter systems
Saturation
Scatchard plot
RECEPTOR-LIGAND BINDING
•Must be saturable
•Must be reversible
•Must be specific
•If it is a receptor, there must be a biological effect
Pharmacokineticsa. route of administrationb. absorption and elimination
Pharmacodynamicsa. dose-effect curveb. therapeutic indexc. ligand bindingd. agonist vs. antagoniste. neurotransmitter systems
% Maximum % Maximum EffectEffect
[Drug][Drug]
Agonist
Antagonist
Partial agonist
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1 10010 1000
Agonist
Antagonist
Partial agonist
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80
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1 10010 1000
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1 10 100 10000
20
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1 10 100 1000
% of Maximal % of Maximal EffectEffect
[Drug][Drug]
AgonistAgonist
Agonist + competitive Agonist + competitive antagonistantagonist
Agonist + non-competitive Agonist + non-competitive antagonistantagonist
Pharmacokineticsa. route of administrationb. absorption and elimination
Pharmacodynamicsa. dose-effect curveb. therapeutic indexc. ligand bindingd. agonist vs. antagoniste. neurotransmitter systems
NEUROTRANSMITTER CRITERIA
•Must be localized in neuron
•Must be released with stimulation
•Must be mimicked with exogenous application
•Must be pharmacologically active at receptor
