drug response

Question 1

ligands

Answer 1

proteins
peptides
small molecules

Question 2

agonist

Answer 2

conformation changes to active site

Question 3

emax

Answer 3

max response acheived by agonist

drug efficacy/activity

Question 4

ED50

Answer 4

drug concentration 50% emax achieved

drug potency

50% population shows response

Question 5

efficacy

Answer 5

max drug effect (pharm efficacy)

all agonists have some efficacy

partial agnoist lower max eff

Question 6

potency

def, determined by, relation to?

Answer 6

amount of drug to produce effect

affinity of receptor for the drug

determined by affinity of receptor

inverse to EC50

D-R shifts left

Question 7

effective concentration

Answer 7

ed50/EC50 concentration of agonist needed to elicit half of the max bio response of agonist

Question 8

LD50

Answer 8

dose at which 50% population dies

Question 9

therapeutic index

Answer 9

LD50/ED50 safety indication (higher is better)

Question 10

antagonists pharm efficacy

Answer 10

zero

no effect on receptor

dont change activity state

Question 11

antagonists clinical eff

Answer 11

do have clincal eff

therapeutic effect

prevent endogenous agonist

Question 12

competitive antagonist

Answer 12

same site as agonist

reversible: inhib can be overcome ^ [agonist]
irreversable: inhib cannot be overcome

affects potency

Question 13

non-competitive antagonists

Answer 13

binds receptor elsewhere

cant be competed w/ agonist

cannot be overcome by agonist

affects efficacy (decrease)