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Pharmacology > Pharmacodynamics > Flashcards

Pharmacodynamics Flashcards

1
Q

which one of Paul Ehrlich’s theories used the analogy of a lock & key?

A

the side chain theory & concept of the receptor

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2
Q

what was the lock and key analogy implying relating to a ligand & a receptor?

A
  1. key goes in and out (reversible binding)
  2. key must fit lock (selective binding)
  3. only certain keys turn the lock (selectivity of action)
  4. thermodynamic (energetically favorable to obtain binding/action)
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3
Q

most receptors have endogenous naturally occurring molecule that

A

bind to them

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4
Q

exogenous drugs have to be designed to

A

bind and mimic the endogenous substance at the same receptor

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5
Q

give an example of an endogenous molecule and exogenous drug acting through the same receptor class

A

endorphins & morphine bind to opiate receptors in the brain

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6
Q

what chemical bond determines if a drug-receptor complex is irreversible

A

covalent

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7
Q

what chemical bond determines if a drug-receptor complex is reversible by altering pH

A

ionic

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8
Q

what chemical bond determines if a drug-receptor complex is readily reversible

A
  • hydrogen
  • hydrophobic
  • van der Waals
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9
Q

define stereoisomers

A

chemical structures that are chemically identical but have different orientations around the single bond

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10
Q

what effect can stereoisomers have on drug affinity?

A

it can alter affinity of a drug to its receptor therefore affecting its potency

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11
Q

define hydrophobic

A
  • water hating
  • fat loving
  • nonpolar
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12
Q

define hydrophilic

A
  • water loving
  • fat hating
  • polar
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13
Q

define lipophilicity

A

allows drugs to move among body compartments and bind to receptors

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14
Q

what are the 4 requirements for good drug binding

A
  1. receptor specificity
  2. type of bond formed
  3. stereoselectivity
  4. solubility characteristic
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15
Q

define agonists

A

bind to produce and elicit
- max. activation of receptor
- max response from the tissue

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16
Q

define antagonists

A

bind but produce
- NO activation of receptor
- block response from tissue

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17
Q

define partial agonists

A

produce weaker activation of receptor than full agonists or endogenous ligands

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18
Q

define inverse agonists

A

inhibit rather than activate the receptor

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19
Q

define allosteric modulators

A

bind to receptors at alternate binding site

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20
Q

define potency

A

the measure of the amount of drug necessary to produce an effect of a given magnitude

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21
Q

what is EC50

A

the [] of a drug needed to produce 50% of the maximum effect

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22
Q

what is ED50

A

dose that produces 50% of maximal response

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23
Q

define efficacy

A

ability of a bound drug to change the receptor in a way that produces an effect

24
Q

what is Emax

A

the maximal efficacy of a drug

25
Q

define therapeutic index (TI)

A

ratio of LD50/TD50 and ED50

26
Q

which if the 2, efficacy or potency, is a more useful value?

A

efficacy

27
Q

why is the efficacy a more clinically useful value than potency?

A

b/c a drug with greater efficacy is more therapeutically beneficial that one that is more potent

28
Q

what is LD50

A

the dose at which 50% of patients die

29
Q

what is TD50%

A

the dose at which toxicity occurs in 50% of patients

30
Q

drugs with which type of therapeutic window are more desirable?

A

those with a greater/wider therapeutic window

31
Q

drug binding specificity involves

A

molecular recognition between ligand and receptor

32
Q

drug binding specificity requires

A

spatially & energetically complementary domains

33
Q

explain the concept of binding affinity/ binding energy

A
  • recognition between receptor and ligand
  • spatially/ energetically complementary domains
34
Q

equilibrium binding constant KD represents…

A

rate of dissociation/ rate of association

35
Q

what information does KD provide about a drug?

A

drugs w/ a high affinity display a small KD value

36
Q

KD= the drug concentration that gives

A

50% bound receptors

37
Q

KD is inversely related to

A

drug binding affinity

38
Q

receptor classifications are named after an

A

endogenous ligand w/ various subtypes of receptors named for exogenous agents

39
Q

what is an example of a ligand gated ion channel?

A

in skeletal muscles for movement of NA+ and Ca2+

  • nicotinic cholinergic receptors
  • endogenous ligand acetylcholine
40
Q

explain GPCRs

G-protein coupled receptors

A

7 transmembrane domains spanning region of the receptor w/ few allosteric modulator binding sites

41
Q

GPCRs activate

A

2nd messenger systems within the intracellular space

42
Q

which receptors represent the largest protein class of receptors in the human genome?

A

GPCRs

43
Q

gives examples of GCPR receptors

A
  • muscarinic cholinergic receptors
  • adrenergic (a & b )
  • dopaminergic
  • serotonergic
44
Q

give examples of endogenous ligands that bind to GCPRs

A
  • acetylcholine
  • epinephrine
  • norepinephrine
  • dopamine
  • serotonin
  • GABA
  • glucagon
45
Q

the GCPR are found in the

A
  • heart
  • respiratory system
  • digestive system
  • blood vessels
46
Q

what are RTKS

receptor tyrosine kinases

A

single transmembrane spanning regions

47
Q

describe the mechanism of RTKs

A

binding of ligand causes dimerization of the kinases following phosphorylation by ATP

48
Q

give examples of ligands that bind to RTKs

A
  • insulin
  • GF
    GH
49
Q

ligand binding occurs on what side of the cell?

A

on the extracellular side

50
Q

nuclear receptors are ..

A

receptor residues that are on the inside of the cell or within the nucleus

51
Q

in nuclear receptors the ligand-receptor complex binds to

A

DNA segment for transcription

52
Q

what is a unique characteristic of nuclear receptors?

A

they have longer lasting effects than other ligand-binding receptors

53
Q

what are some examples of endogenous receptors that bind to nuclear receptors?

A
  • corticosteroids
  • mineralocorticoids
  • sex steroids (estrogen & testosterone)
  • vit. A and D
54
Q

what are the 4 known changes that can occur in receptor quantities?

A
  • receptor quantities are not constant
  • internalization & degradation
  • change in receptor synthesis rate
  • can be unregulated or downregulated
55
Q

describe upregulation

A

receptor number increase due to a decrease of activity in the receptor

56
Q

describe downregulation

A

receptor number decreases due to an increase making the cell less sensitive to the ligand

57
Q

describe desensitization/tolerance

A

continued stimulation of a receptor system will depress the effect produced by an administered drug

  • a higher dose is requires to each the same effect

Pharmacology (9 decks)

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