9.23 Pharmacodynamics Flashcards

1
Q

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

A

antagonist

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2
Q

does an antagonist have potency?

A

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

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3
Q

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

A

ED50 < Kd

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4
Q

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

A

I

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5
Q

kinase receptors usually ____ and cross-________

A

dimerize, cross-phosphorylate

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6
Q

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

A

S
I
Q

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7
Q

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.

A

potency

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8
Q

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

A

PLA2

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9
Q

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

A

therapeutic effect curve

lethal dose curve

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10
Q

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

A

beta-gamma

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11
Q

ability of a drug to induce a response by itself

A

efficacy

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12
Q

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

A

signal transduction

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13
Q

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

A

quantal dose-response curves

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14
Q

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

A

partial agonist

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15
Q

A graph of increasing response to increasing drug concentration or dose

A

graded dose response curve

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16
Q

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

A

therapeutic effect curve

side effect curve

17
Q

equation for therapeutic window:

A

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

18
Q

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

A

high
reduced
no

19
Q

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

A

Left/right

up/down

20
Q

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

A

noncompetitive antagonist

21
Q

____ receptors can imitate a chain reaction of protein phosphorylation

A

kinase

22
Q

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

A

potency

potency, efficacy

23
Q

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)

A

Kd

24
Q

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

A

PKC

IP3R, CAMk

25
Q

G__ acts on AC, increasing cAMP levels and activating PKA

A

S

26
Q

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

A

ED50

27
Q

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

A

Q
PIP3
IP3 and DAG

28
Q

equation for therapeutic index:

A

TI = LD50/ED50

LD = lethal dose

29
Q

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

A

competitive agonist

30
Q

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

A

agonist

31
Q

low Kd = _____ affinity

A

high

32
Q

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

A

ionic bonds, H bonds, van der Waals forces

33
Q

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

A

antagonist

decreases

34
Q

what are the three components of a drug receptor system?

A
  1. recognition site
  2. transducer mechanism
  3. amplification system
35
Q

the higher the therapeutic index, the ______ the drug

A

safer

36
Q

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

A

ED50/EC50