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Psychopharmacology > Lecture 6: Pharmacodynamics > Flashcards

Lecture 6: Pharmacodynamics Flashcards

1
Q

pharmacodynamics

A

the study of what drugs do to the body

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2
Q

dissociation constant

A

Kd; equilibrium constant that measures propensity of larger object to separate (dissociate) reversibly into smaller components. the drug concentration (in moles) at which half of the receptors are bound to the drug

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3
Q

dissociation constants for drug-receptor or transmitter-receptor interactions can be in ___

A

nM to muM range

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4
Q

definition of receptor

A

large molecule; site where naturally-ocurring signaling molecules produce biological effect

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5
Q

agonistic action

A

binding to the site of the normal endogenous neurotransmitter which initiates a similar cellular response

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6
Q

allosteric action

A

binding to nearby site can facilitate transmitter binding

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7
Q

antagonistic action

A

binding to receptor site can block access of transmitter to normal binding site

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8
Q

4 types of receptor structure

A
  1. ionotropic
  2. metabotropic
  3. carrier proteins (transporters)
  4. degradative enzymes
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9
Q

3 steps of ionotropic receptor binding

A
  1. NT molecules bind to protein sites in receptor channel
  2. binding causes channel to open immediately
  3. when channel opens, ions are able to move into or out of the neuron
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10
Q

what does GABA stand for?

A

gamma aminobutyric acid

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11
Q

two broad classes of GABA receptors and types

A

GABAa (ionotropic)

GABAb (metabotropic)

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12
Q

how many protein subunits does the GABAa receptor have?

A

5

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13
Q

names of GABAa receptor subunits

A

gamma2
beta2 (2)
alpha1 (2)

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14
Q

how many membrane spanning domains does a subunit have?

A

4 - helices

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15
Q

polypeptides

A

amino acids linked by peptide bonds

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16
Q

4 important parts of GABAa receptor

A
  1. chloride channel
  2. GABA site
  3. barbiturate site
  4. benzodiazepine site
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17
Q

metabotropic receptors

A

G protein-coupled receptors (GPCRs)

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18
Q

metabotropic receptors induce the release of ___ which can trigger ___

A

intracellular protein

second messengers

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19
Q

what are 3 of the 5 examples of processes metabotropic receptors control?

A
  1. ion channel function
  2. energy metabolism
  3. cell division/differentiation
  4. neuron excitability
  5. gene expression
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20
Q

when G proteins bind ___ they are on, and when they bind ___ they are off

A 
guanosine triphosphate (GTP)
guanosine diphosphate (GDP)
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21
Q

4 steps in G protein activation of an ion channel

A
  1. NT molecule binds to GPCR
  2. transmitter binding activates GPCR
  3. activated subunit of GPCR moves to nearby ion channel
  4. when G protein subunit attaches to ion channel, it opens, allowing ion flow
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22
Q

two major processes/enzymes triggered by G protein activation

A
  1. phospholipid hydrolysis

2. adenylyl cyclase

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23
Q

phospholipid hydrolysis second messengers

A
  1. DG

2. IP3

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24
Q

major adenylyl cyclase 2nd messenger

A

cAMP (cyclic adenosine monophosphate)

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25
Q

consequence of presynaptic change in channel activity

A

change in amt of NT released

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26
Q

consequence of postsynaptic change in channel activity

A

change in firing pattern of neuron or cell

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27
Q

drugs can be ___ specific than endogenous ligands

A

more

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28
Q

carrier proteins

A

transporters; bind to NTs to transport them back to presynaptic neurons

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29
Q

2 drugs that block carrier proteins

A

SSRIs (block 5HT)

cocaine (blocks DA and NE)

30
Q

net effect of transporter blockage

A

increase amount of NT available in synaptic cleft

31
Q

two gradients affecting ion flow

A
  1. voltage gradient

2. concentration gradient

32
Q

degradative enzymes

A

function to break down NTs

33
Q

___ are used as pesticides and nerve gases

A

irreversible acetylcholine esterase inhibitors

34
Q

___ are used as cognitive enhancers in alzheimer’s disease and to increase muscle contractions in myasthenia gravis

A

reversible AChE inhibitors

35
Q

monoamine oxidase inhibitors inhibit ___ breakdown of ___ and ___

A

presynaptic

NE & DA

36
Q

optical isomers

A

molecular optical images, like left and right hand

37
Q

+ or D isomer rotates ___, and - or L isomer rotates ___

A

clockwise

counterclockwise

38
Q

50/50 combination of D and L is called a ___

A

racemic mixture

39
Q

___ can occur if ligand activation is chronically blocked. example of drug type that causes this?

A
  1. up regulation/supersensitivity

2. antipsychotics that block DA receptors

40
Q

dose response curves (37); what are the two x axes used?

A
  1. percentage of subjects responding

2. intensity of response

41
Q

4 variables DRCs give info about

A
  1. potency
  2. slope
  3. efficacy
  4. variability
42
Q

potency

A

concentration at which drug produces desired effect; usually attach more tightly than less potent drugs. high affinity does not equal high potency

43
Q

what is the difference between potency and affinity?

A

potency is a function of both efficacy and affinity; for a drug to be potent, it must both bind strongly and initiate a strong response. an antagonist can have high affinity but no potency

44
Q

slope

A

linear central part of curve which indicates how sharply effect changes with each change in dose

45
Q

if a small change in dose produces a large change in effective, slope is ___

A

steep

46
Q

if a large change in dose produces small changes in effect, the slope is ___

A

shallow

47
Q

efficacy

A

the maximum effect obtainable with higher doses producing no additional effect

48
Q

what is the difference between potency and efficacy?

A

some drugs may be potent, but might never be able to produce a peak response no matter how much is given

49
Q

a drug that is more efficacious produces a ___ peak than a less efficacious drug

A

higher/greater maximum

50
Q

spare receptors

A

maximum effect obtainable with a drug can occur when not all of the receptors have been bound by ligand

51
Q

variability

A

individ difference in drug response can include potency, max effect, or slope

52
Q

4 types of DRCs

A
  1. full agonistic
  2. partial agonistic
  3. antagonistic
  4. inverse agonistic
53
Q

a partial agonist has a similar action to a full agonist, but is less ___

A

efficacious

54
Q

antagonist

A

blocks or limits action of ligand, but has no effect of its own (no potency)

55
Q

inverse agonist

A

binding to receptor site produces effect opposite to that of the endogenous ligand

56
Q

allosteric modulators

A

affect receptor response by binding to site that is diff from site to which endogenous ligand binds

57
Q

positive allosteric modulators ___ response to endogenous ligand

A

increase

58
Q

negative allosteric modulators ___ effect of endogenous ligand

A

diminish

59
Q

ED50

A

drug dose that produces desired effect in 50% of subjects

60
Q

LD50

A

lethal dose for 50% of test subjects

61
Q

TI

A

therapeutic index; ratio of LD50 to ED50

62
Q

TR

A

therapeutic ratio; dose that causes adverse fx in 50% of pop to dose that causes therapeutic effect in 50%

63
Q

the greater the TI, the ____ the drug

A

safer

64
Q

TI =

A

LD50/ED50

65
Q

The lower the ED50, the ___ the potency. the lower the TI, the ____ the safety

A

potency

safety

66
Q

double-blind tests with placebo run-in period

A

every patient given a placebo for a week; those who respond positively removed

67
Q

nocebo effect

A

negative expectation of phenom causes it to have more negative effect

68
Q

polypharmacy

A

combining meds to improve outcome

69
Q

pharmacodynamic redundancy

A

two drugs have same or overlapping mechanisms of action

70
Q

pharmacodynamic interaction

A

two drugs may oppose each other. e.g. antipsychotic blocks DA type 2 receptors, while ADHD stimulant increases DA levels

71
Q

pharmacokinetic interactions

A

one drug may affect another drug’s ADME

72
Q

axes of a graph of PK
axes of a graph of PD
combination graph?

A
  1. concentration vs. time
  2. effect vs. conc(log)
  3. PK/PD - effect vs. time

Psychopharmacology (22 decks)

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