Block 1 Lecture 3 -- Pharmacodynamics I Flashcards Preview

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Flashcards in Block 1 Lecture 3 -- Pharmacodynamics I Deck (41):
1

ligand:

molecules that binds to some other type of biological entity

2

receptor:

protein that interacts with a ligand resulting in a change in physiological activity

3

drug mechanism of action:

the physicochemical relationship between a drug and its specific target, and the cascade of biochemical signaling that ensues

4

placebo response:

inert substance given to a patient that leads to clinical improvement

5

nocebo response:

inert substance that causes a worsening of Sxs or development of ADRs

6

adverse drug response:

undesirable drug response

7

idiosyncratic drug response:

a quantitatively abnormal drug response

8

drug allergy:

an adverse immunologic reaction to a drug

9

agonist:

ligand that binds receptor and activates it

10

partial agonist:

a drug with less than maximal effect in comparison to a full agonist

11

indirect-acting agonist:

drug that increases synaptic concentration of endogenous neurotransmitter

12

allosterically-acting ligand:

ligand that interacts at a non-orthosteric site where it can potentiate functional response to an endogenous ligand

13

chemical antagonist:

a compound that chemically combines with a xenobiotic to prevent delivery of that substance to its normal site of action

14

physiologic antagonist:

a drug that blocks a physiological response related to a particular condition without actually affecting the state of that condition

15

receptor (pharmacological) antagonist:

drug that prevents formation of agonist-receptor complexes

16

competitive antagonist:

drug that competes with NTs for access to orthosteric binding sites

17

non-competitive antagonist:

drug that binds receptor at a non-orthosteric site

18

irreversible antagonist:

drug that binds covalently to a receptor

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indirect antagonist:

drug that decreases synaptic concentration of NT

20

inverse agonist:

drug that produces physiological effects opposite to those of an agonist

21

potency:

the relationship between a drug concentration and its biological response in comparison to another drug

22

Quantal Dose Response Curve:

graph used to plot "all or nothing" drug responses; commonly used to assess responses across large patient population

23

efficacy

the ability of a drug to produce a desired effect

24

constitutive activity:

activity present in the GPCRs of some systems to produce physiologically active effects even in the absence of agonist

25

on-target ADR:

drug hits intended target excessively or in the wrong location

26

off-target ADR:

drug interacts with unintended targets

27

direct-acting agonist:

drug with enough structural similarity to an endogenous ligand to bind to and directly activate NT receptors

28

Partial agonists are aka...

functional antagonists

29

What are the mechanisms by which indirect-acting agonists might work?

1) block NT degradation
2) block re-uptake transporters
3) increase pre-synaptic release

30

What are the types of antagonism?

1) PK
2) chemical
3) physiologic
4) receptor (pharmacological)

31

Describe the structure of the nAChR

5 subunits like GABAa but excitatory

32

Describe structure of the GABAa receptor

5 subunits surrounding inhibitory Cl- channel
- 2 orthosteric GABA sites
- allosteric: EtOH, BZDs, neurosteroids, barbiturates

33

Axes of a DRC:

% response vs. [drug]

34

ED50:

[agonist] that produces a 50% maximal response

35

IC50

ED50 for antagonist--
[antagonist] to decrease agonist response by 50%

36

examples of irreversible antagonists:

organophosphates
snake toxins

37

examples of chemical antagonism:

1) mercury + dimercaprol
2) anti-venoms
3) immunotherapy for addiction

38

examples of physiologic antagonism:

1) epinephrine + histamine
2) beta-blockers in hyperthyroidism

39

example of receptor antagonism:

propranolol + NE

40

What are the mechanisms by which indirect antagonists might work?

1) block NT synthesis
2) decrease pre-synaptic NT release

41

What factors could cause an idiosyncratic drug response?

1) reactive metabolites
2) non-allergic changes in pt immune system
3) specific gene mutations in receptor