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Pharmacology & Anesthesiology > Pharmacodynamics > Flashcards

Pharmacodynamics Flashcards

1
Q

what type of name should a veterinarian be familiar with
1) chemical name
2) generic name
3) commercial/trade/brand name

A

generic name (2)

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2
Q

most drugs act by doing what

A

stimulating or inhibiting membrane receptors

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3
Q

more than ________ plasma membrane receptors are known, in more than ____ families

A

1000; 20

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4
Q

in order for a drug to interact with a receptor, it needs to possess adequate (3)

A

size, charge, shape/anatomic composition

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5
Q

what is the signal transduction pathway

A

the receptor, cellular target and any intermediary molecules

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6
Q

what is the size range of drugs and why

A

100-1000
100 MV minimum size for specificity of action
1000 MV maximum size for reasonable movement to sites of action

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7
Q

drugs that interact with receptors through weak bonds are (more/less) selective

A

more

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8
Q

what is affinity

A

relative ability to bind to a receptor

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9
Q

the strongest type of bond is _________ which is (more/less) common; the weakest type of bond is _____________, which is (more/less) common; an intermediate type of bond is ___________, which is (more/less) common

A

covalent, less; hydrophobic, more; electrostatic, more

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10
Q

hydrogen bonds and van der waals bonds are what type of bond

A

electrostatic

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11
Q

what is the important consequence of enantiomers

A

one enantiomer is often more potent as it fits the receptor better

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12
Q

drug effect is generally proportional to ____________, which in turn is dependent on ____________

A

percentage of receptors occupied by the drug; concentration of drug in the ECF

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13
Q

how many mechanisms of transmembrane signalling exist

A

5

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14
Q

what are the 5 transmembrane signalling mechanisms

A

1) cytoplasmic receptor (steroids)
2) transmembrane enzyme (tyrosine kinase)
3) transmembrane no enzyme (JAK STAT)
4) ion channel
5) GPCR

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15
Q

what is the most abundant receptor type

A

GPCR

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16
Q

what is one important GPCR

A

beta adrenergic receptors

17
Q

what is the role of second messengers

A

translate D-R interactions into a change in cellular activity; amplification of signals

18
Q

T/F most drugs act on receptors that have an endogenous ligand

A

T

19
Q

describe the following:
1) agonist
2) partial agonist
3) antagonist
4) inverse agonist

A

1) fully stimulates the receptor
2) partially stimulates the receptor
3) does not activate receptor; blocks agonists
4) lowers basal activity of receptor

20
Q

what is the dose response curve

A

depiction of drug effect as a function of drug concentration

21
Q

what is potency? what is it defined by

A

the concentration of drug required to produce a certain effect; half-maximal effective concentration or EC50

22
Q

what is efficacy? what is it defined by

A

the magnitude of the cellular response when all receptors of a given type are occupied by the ligand; Emax

23
Q

T/F the most potent drug is not necessarily the most efficacious

A

T

24
Q

is efficacy or potency more important to a clinician

A

efficacy

25
Q

what happens to efficacy/potency during competitive receptor antagonism

A

efficacy does not change (no change in Emax) but potency decreases (EC50 value larger)

26
Q

what happens to efficacy and potency during non-competitive receptor antagonism

A

efficacy decreases (Emax is reduced); may or may not see a change in potency (EC50)

27
Q

what is allosteric antagonism an example of

A

non-competitive antagonism (will decrease efficacy and may/may not change potency)

28
Q

what is an example of a positive allosteric modulator

A

benzodiazepines (increase affinity of GABA receptors for GABA -> muscle relaxation)

29
Q

what is tolerance

A

the gradual decrease in responsiveness to chronic drug administration

30
Q

how does desensitization/tolerance/down-regulation manifest

A

1) decreased production of receptors
2) phosphorylation of receptor to inactivate
3) sequestration of receptors in the cell

31
Q

what can happen when a receptor antagonist is used chronically and is suddenly withdrawn

A

supersensitivity

32
Q

what is tachyphylaxis

A

more rapid form of tolerance that can happen on the second dose with some drugs

Pharmacology & Anesthesiology (22 decks)

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