week 4

Question 1

potency

Answer 1

an index of the concentration required for a given effect = EC50 = mix function of both affinity & efficacy

Question 2

drugs that are highly potent only require ___ doses

Answer 2

small dose (concentration) to achieve their effects

Question 3

what are the four protein targets

Answer 3

1. receptors
2. ion channels
3. enzymes
4. transporters

Question 4

define agonists

Answer 4

drugs that occupy receptors & activate them

Question 5

define antagonists

Answer 5

drugs that occupy receptors but do not activate them, they block receptor activation by agonist

Question 6

two types of antagonists

Answer 6

irreversible antagonist

competitive antagonist

Question 7

three types of agonists

Answer 7

partial vs full agonist & inverse agonist

Question 8

define partial compared to full agonist

Answer 8

full agonist has a higher efficacy (produces a full response) whilst not fully occupying all the receptors. partial agonist has a lower efficacy whilst occupying all receptors still cannot produce maximum response (despite concentration).

Question 9

define inverse agonist

Answer 9

produce effect opposite to agonist & binds to same binding site = negative efficacy

Question 10

define efficacy

Answer 10

the capacity of a drug to activate a receptor & generate a response = maximal response a drug can produce

Question 11

define ec50

Answer 11

concentration needed to produce a 50% max response

Question 12

if curve B has the same efficacy as curve A but is more the the right then what is the difference

Answer 12

Curve B has a lower potency

Question 13

define competitive antagonist

Answer 13

competes with agonist for binding site = zero efficacy

Question 14

what does competitive antagonist do to the curve if it is added with the agonist

Answer 14

shift of the curve to the right without affecting the slope or max response

Question 15

what looks similar to competitive antagonist

Answer 15

a partial agonist with a full agonist also cause a shift to the right but look for the initial response

Question 16

what does full agonist mixed with partial agonist look like on concentration curve

Answer 16

it competes with the full agonist for binding site therefore, it delays the efficacy but eventually reaches the efficacy

Question 17

what does the partial agonist look like by self

Answer 17

starts from zero but reaches half the efficacy of the full agonist and slightly more to the right because it is slower

Question 18

define irreversible antagonist & affect on concentration curve

Answer 18

drug forms covalent bonds with the receptor

shift of the curve to the right & also affect slope & max response

Question 19

can the concentration curve be used to calculate affinity if there are spare receptors

Answer 19

no

Question 20

define allosteric modulation & the two types

Answer 20

drugs that bind to an alternate site to the orthosteric site, they can be antagonism (lower the efficacy) = negative allosteric modulator or potentiation (increase the efficacy) = postive allosteric modulator

Question 21

define pharmacokinetics

Answer 21

the study of how the body handles drugs

Question 22

define pharmacodynamics

Answer 22

what the drugs do to the body & how they do it

Question 23

what is studied in pharmacodynamics

Answer 23

the association of a drug molecule with its target leads to a physiological response

Question 24

are most drug targets proteins

Answer 24

yes

Question 25

define specificity

Answer 25

when a drug interacts with only one molecular target at one site & has one effect

Drugs bind to a specific site on the protein

Question 26

define selectivity

Answer 26

preference for a molecular target at a particular cell & issue

one protein might bind better to one protein over another

Question 27

define affinity & its measurement

Answer 27

tendency of a drug to bind to the receptor & measured by dissociation constant (Kd)

Question 28

the higher the Kd ….

Answer 28

the lower the affinity

Question 29

define Emax

Answer 29

the maximum effect & in percentage