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Pharmacology
Pharmacodynamics
41
Pharmacology
Graduate
06/17/2014

Additional Pharmacology Flashcards

 


 

Cards

Term
fundamental principles of pharmacodynamics
Definition

drugs can only modify underlying biochemical or phys processes

drugs can NOT create effects

receptor occupancy theory

Term
receptor occupancy theory
Definition
drug action requires a physical interaction with a receptor
Term
receptors (Target macromolecules)
Definition

enzyme

nucleic acid

membrane receptors

Term
specificity
Definition
lock and key
Term
drugs are referred to as
Definition
ligands
Term
receptor locations
Definition

cellular surfaces

intracellular

Term
Receptor families
Definition

ligand-gated ion channels

GPCR

enzyme-linked receptors

intracellular receptors

Term

spare receptors

rat heart vs human heart

Definition

95% rat

5-10% human heart

Term
the magnitide of the effect is assumed to be directly proportional to
Definition
the drug concentration
Term
drug effect is dependent upon
Definition

drug concentration

Effect=Rtotal x [D] / Kd + [D]

Remembrer Michaelis-Menton

Term
Drug-receptor interaction not static rather
Definition
on/off interaction
Term
Graded Responses
Definition

a continuous change in effect with change in dose

change in effect over a wide range of doses may be plotted

Term
Plot of dose vs effect with arithmetic dose scaled yields a
Definition

curved line

simple rectangular hyperbola

Term
A typical D-R curve shows
Definition
potency, efficacy, and slope
Term
Drugs are classified according to the magnitude of their 2 molecular properties
Definition

affinity for the receptor (potency)

efficacy once bound to the receptor

Term
Agonist
Definition
has affinity for receptor and efficacy
Term
Antagonist
Definition

has affinity but no efficacy

 

Term
Competitive Antagonist
Definition
Term
Noncompetitive Antagonist
Definition
Term
Partial agonist
Definition
has affinity and low efficacy
Term

Magnitude to drug effect

Agonist

Definition

concentration @ receptor site= plasma conc

 

Term

Concentration at receptor site-plasma concentration

for agonist depends on

Definition

dose of drug administered

absorption

distribution

metabolism

Term
efficacy
Definition
maximum response produced by drug
Term

potency

effective dose concentration

Definition

how much drug is required to elicit desired response

usually the ED50

Term
Competitive antagonist
Definition

competes for binding w/ agonist

agonist behaves as if less potent

max response can always be achieved agonist is given @ high enough dose

Term
noncompetitive antagonist
Definition

prevents agonist binding with receptor 

OR

prevents agonist from activating receptor

Term
Reversible antagonist
Definition
Term
Irreversible antagonist
Definition
Term
Partial agonist
Definition
block agonist but cause less response (than full agonist)
Term
Factors affecting drug response
Definition

resistance

tolerance

tachyphylaxis

Term
resistance
Definition
usually refers to antimicrobial drugs
Term
tolerance
Definition
decrease in drug response during repeated administration
Term
tachyphylaxis
Definition
acute development of tolerance due to rapid repeated admin. of some drugs
Term
Pharmacokinetic Tolerance
Definition

drug disposition tolerance

due to a decrease in drug conc @ its site of action

barbiturates, alcohol, phenylbutazone

Term
reduced responsiveness to the drug @ its site of action
Definition

amphetamine

caffeine

nicotine

morphine, barbiturates, alcohol

Term
drug safety
Definition
therapeutic index
Term
Quantal responses
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

Term
therapeutic index equation
Definition
toxic dose/effective dose
Term
small therapeutic index
Definition
small increase in dose is more likely to produce toxic effect
Term
large therapeutic index
Definition
large increases in dose are less likely to produce toxic effect
Term
TI
Definition

preclinical= LD50/ED50

clinical TD50/ED50

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