9.23 Pharmacodynamics Flashcards Preview

Foundations Exam 3 > 9.23 Pharmacodynamics > Flashcards

Flashcards in 9.23 Pharmacodynamics Deck (36):
1

drugs that block access of an agonist to its receptor. They do not change the receptor conformation or have any transduction.

antagonist

2

does an antagonist have potency?

yes, measure against agonist. if you need less to produce effect, more potent

3

if there are spare receptors for a drug, ____ will be less than ____.

ED50 < Kd

4

G__ acts to inhibit AC, decreasing cAMP levels and deactivating PKA

I

5

kinase receptors usually ____ and cross-________

dimerize, cross-phosphorylate

6

G__ is stimulatory, G__ is inhibitory, G__ acts on PLC

S
I
Q

7

dosage (concentration) required to induce (or block if negative) a response. amount of drug required to bring around a response. ability to get to site of action, etc.

potency

8

additional G proteins can activate ______, which causes release of arachidonic acid from the plasma membrane

PLA2

9

the therapeutic index is between the ____________ curve and the _________ curve

therapeutic effect curve
lethal dose curve

10

A G-protein can alter ion channel activity by the ____ subunit indirectly gating ion channels from the intracellular side

beta-gamma

11

ability of a drug to induce a response by itself

efficacy

12

Taking the chemical message and turning it into a biochemical event within the cell.

signal transduction

13

A graph of the fraction of a population that shows a specified response (either produced or not produced) at progressively increasing doses.

quantal dose-response curves

14

Interacts with receptor at recognition site but cannot produce a maximum response (reduced efficacy).

partial agonist

15

A graph of increasing response to increasing drug concentration or dose

graded dose response curve

16

the therapeutic window is between the ______________ curve, and the ______________ curve

therapeutic effect curve
side effect curve

17

equation for therapeutic window:

TW = TD50/ED50
TD - toxic dose
ED - effective dose

18

an agonist has _____ efficacy. A partial agonist has _____ efficacy. An antagonist has _____ efficacy

high
reduced
no

19

in dose response curves, potency is associated with _______ shift, and efficacy is associated with _______ shift

Left/right
up/down

20

antagonists that interact irreversibly with the receptor recognition site, usually by formation of covalent bond. Agonists can’t compete and overcome blocking action.

noncompetitive antagonist

21

____ receptors can imitate a chain reaction of protein phosphorylation

kinase

22

competitive agonists decrease ______, while noncompetitive agonists decrease _______ and or ______

potency
potency, efficacy

23

The concentration of drug that binds 50% of the receptors in the system (total receptors in the system - if this was bound, it would be Emax)

Kd

24

in the Gq pathway, DAG activates _____ and IP3 activates ____, letting Ca++ into the cell from ER, activating _____

PKC
IP3R, CAMk

25

G__ acts on AC, increasing cAMP levels and activating PKA

S

26

the dose on a dose response curve that produces half of the maximal response

ED50

27

G__ acts on PLC, which acts on _____, releasing into two components (____ and ____)

Q
PIP3
IP3 and DAG

28

equation for therapeutic index:

TI = LD50/ED50

LD = lethal dose

29

binds in the same spot on the receptor as the drug, blocking binding of agonist. Can be overcome by increasing drug concentration.

competitive agonist

30

define: drugs that interact with specific receptors and cause a change in conformation of the receptor, transduction, and amplification. Full efficacy

agonist

31

low Kd = _____ affinity

high

32

what are the three main forces between drugs and their receptors?

ionic bonds, H bonds, van der Waals forces

33

a partial agonist can behave as a partial ________ in the presence of a full agonist. This _____ efficacy.

antagonist
decreases

34

what are the three components of a drug receptor system?

1. recognition site
2. transducer mechanism
3. amplification system

35

the higher the therapeutic index, the ______ the drug

safer

36

In graded dose-response curves, the concentration or dose that causes 50% of the maximal effect. In quantal dose-response curves, the concentration or dose that causes a specified response in 50% of the population under study

ED50/EC50