How drugs act L13

Question 1

A drug=

Answer 1

a chemical applied to a physiological system that affects its function in a specific way

Question 2

what do nearly all drugs act on

Answer 2

target proteins

Question 3

what do most drugs work on (specific)

Answer 3

GPCR

Question 4

what is specificity

Answer 4

the degree to which the effects of a drug are due to one pharmacological action

Question 5

specificity is ______

Answer 5

reciprocal (individual drugs bind only to certain targets and individual targets only recognise certain classes of drugs)

Question 6

affinity=

Answer 6

the strength of non-covalent bonds between drug and receptor

Question 7

what is affinity measured by

Answer 7

dissociation constant

Question 8

dissociation constant=

Answer 8

the concentration at which half the drug is bound to the receptor at equilibrium

Question 9

kon=

Answer 9

association constant

Question 10

Koff=

Answer 10

dissociation constant

Question 11

Kd=

Answer 11

equilibrium dissociation constant —>Koff/Kon

Question 12

agonist=

Answer 12

a drug that produces a positive effect when bound

Question 13

antagonist=

Answer 13

a drug that reduces the effect of an agonist

Question 14

what is the relationship between agonist conc and agonist occupancy with a competitive antagonist

Answer 14

increasing agonist conc enough will ensure agonist occupancy

Question 15

what is the relationship between agonist conc and agonist occupancy with a non-competitive antagonist

Answer 15

increasing agonist conc will have no effect on agonist occupancy, if there are enough antagonists present to fill receptors.

Question 16

what is an inverse agonist

Answer 16

a drug that produces a negative effect when bound to a receptor

Question 17

efficacy (Emax)=

Answer 17

the maximum response achievable from a drug

Question 18

potency=

Answer 18

the dose of a drug required to produce a specific effect of a given intensity.