Lecture 4-5 Kahoot

Question 1

TRUE OR FALSE

An antagonist with a high affinity for a receptor will typically have a high efficacy as well.

Answer 1

false

an antagonist with a high affinity for a receptor will typically have a lower(?) efficacy as well.

Question 2

Antagonists have affinity but _____ efficacy

Answer 2

zero/low

Antagonists have affinity but zero intrinsic efficacy; they bind to target receptor but produce no response.

Question 3

A drug with a large dissociation constant (kd) value for a receptor has _______ affinity for the receptor.

Answer 3

low

a drug with a large dissociation constant (kd) value for a receptor has LOW affinity for the receptor.

Question 4

which of the following drugs has the highest potency?

Answer 4

curve C

Question 5

What determines a drug having high potency?

Answer 5

a more potent drug requires a lower concentration to give a specified percentage response

Question 6

A _________ dose-response curve measures the effectiveness of a drug within a population.

Answer 6

quantal

a quantal-dose response curve plots fraction of a population that responds to a given dose of a drug…

is the effect present/not present

frequency of effect

Question 7

what is ED50?

Answer 7

dose required to produce a therapeutic effect in 50% of the population

Question 8

Which of the following drugs is the safest with the greatest difference between its effect and toxic dose?

TI = 100
TI= 4
TI= 1,000
TI= 80

Answer 8

TI = 1,000

TI (therapeutic window) is plasma concentration range of a drug where
1. efficacy is high
2. adverse effects is low

Higher TI = safest drug

Question 9

If given a graph and shows ED50(left of graph) and TD50(always to the right of the graph), know how to calculate TI = TD50/ED50

Question 10

Which of the following types of drug would cause inactivation of a receptor with basal activity?

Answer 10

inverse agonist

an inverse agonist decreases response below basal activity (curve drops below 100)

Question 11

Which of the following types of antagonist inactivates the drug itself, not the receptor?

Answer 11

chemical antagonist

one drug binds to another drug making it unavailable to bind to its receptor

Question 12

Assuming no spare receptors exist, a noncompetitive antagonist will reduce ______________ of an agonist response.

Answer 12

efficacy

Question 13

Noncompetitive antagonist

Answer 13

reduces agonist efficacy

Question 14

Competitive antagonist

Answer 14

reduces agonist potency

Question 15

physiological antagonist

Answer 15

the effect of one drug causes physiological effect opposite to action of another drug

opposing effects cancel each other out

e.g salbutamol is physiological antagonist of histamine

Question 16

Assuming spare receptors EXIST, a noncompetitive antagonist will reduce ____________ of an agonist response.

Answer 16

the efficacy and potency

when spare receptors exist with noncompetitive antagonist, at high concentrations, both efficacy and potency decrease.

Question 17

TRUE OR FALSE

A positive allosteric modulator activates a receptor regardless of whether an agonist is bound to the orthosteric site.

Answer 17

FALSE

PAMs differentiate/discriminate between activated and non-activated receptor states

PAMs may have a broader therapeutic window and a reduced liability for receptor desensitization and/or tolerance.

Question 18

What do agonists do?

Answer 18

activate all receptors