Term
| fundamental principles of pharmacodynamics |
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Definition
drugs can only modify underlying biochemical or phys processes
drugs can NOT create effects
receptor occupancy theory |
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Term
| receptor occupancy theory |
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Definition
| drug action requires a physical interaction with a receptor |
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Term
| receptors (Target macromolecules) |
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Definition
enzyme
nucleic acid
membrane receptors |
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Term
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Definition
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Definition
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Term
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Definition
cellular surfaces
intracellular |
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Term
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Definition
ligand-gated ion channels
GPCR
enzyme-linked receptors
intracellular receptors |
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Term
spare receptors
rat heart vs human heart |
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Definition
95% rat
5-10% human heart |
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Term
| the magnitide of the effect is assumed to be directly proportional to |
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Definition
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Term
| drug effect is dependent upon |
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Definition
drug concentration
Effect=Rtotal x [D] / Kd + [D]
Remembrer Michaelis-Menton |
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Term
| Drug-receptor interaction not static rather |
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Definition
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Term
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Definition
a continuous change in effect with change in dose
change in effect over a wide range of doses may be plotted |
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Term
| Plot of dose vs effect with arithmetic dose scaled yields a |
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Definition
curved line
simple rectangular hyperbola |
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Term
| A typical D-R curve shows |
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Definition
| potency, efficacy, and slope |
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Term
| Drugs are classified according to the magnitude of their 2 molecular properties |
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Definition
affinity for the receptor (potency)
efficacy once bound to the receptor |
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Term
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Definition
| has affinity for receptor and efficacy |
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Term
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Definition
has affinity but no efficacy
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Term
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Definition
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Term
| Noncompetitive Antagonist |
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Definition
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Term
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Definition
| has affinity and low efficacy |
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Term
Magnitude to drug effect
Agonist |
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Definition
concentration @ receptor site= plasma conc
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Term
Concentration at receptor site-plasma concentration
for agonist depends on |
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Definition
dose of drug administered
absorption
distribution
metabolism |
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Term
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Definition
| maximum response produced by drug |
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Term
potency
effective dose concentration |
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Definition
how much drug is required to elicit desired response
usually the ED50 |
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Term
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Definition
competes for binding w/ agonist
agonist behaves as if less potent
max response can always be achieved agonist is given @ high enough dose |
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Term
| noncompetitive antagonist |
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Definition
prevents agonist binding with receptor
OR
prevents agonist from activating receptor |
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Term
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Definition
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Term
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Definition
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Term
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Definition
| block agonist but cause less response (than full agonist) |
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Term
| Factors affecting drug response |
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Definition
resistance
tolerance
tachyphylaxis |
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Term
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Definition
| usually refers to antimicrobial drugs |
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Term
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Definition
| decrease in drug response during repeated administration |
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Term
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Definition
| acute development of tolerance due to rapid repeated admin. of some drugs |
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Term
| Pharmacokinetic Tolerance |
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Definition
drug disposition tolerance
due to a decrease in drug conc @ its site of action
barbiturates, alcohol, phenylbutazone |
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Term
| reduced responsiveness to the drug @ its site of action |
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Definition
amphetamine
caffeine
nicotine
morphine, barbiturates, alcohol |
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Term
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Definition
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Term
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Definition
frequency with which a defined effect occurs in a population @ a given dose
cumulative frequency with which an effect occurs in a pop @ a given dose and all lower doses |
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Term
| therapeutic index equation |
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Definition
| toxic dose/effective dose |
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Term
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Definition
| small increase in dose is more likely to produce toxic effect |
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Term
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Definition
| large increases in dose are less likely to produce toxic effect |
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Term
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Definition
preclinical= LD50/ED50
clinical TD50/ED50 |
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