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IDT Fall > Depression Medchem > Flashcards

Depression Medchem Flashcards

1
Q

what are common features to identify tricyclic antidepressants (TCAs)?

A

triple ring formation
not aromatic (no double bonds on middle ring)

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2
Q

what do TCAs have at C3 that increases their activity?

A

monohalogenation

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3
Q

the side chain of TCAs do not exceed how many atoms?

A

4

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4
Q

TCAs with tertiary amine groups can be expected to be more ______ and stronger ______

A

sedating (greater H1 antagonism), anticholinergics (M1 antagonism)

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5
Q

what is the major route of metabolism for TCAs? minor route?

A

major: Cyp2D6
minor: Cyp2C19

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6
Q

Imipramine undergoes what metabolism? what are the 2 active metabolites?

A

N-demethylation
Desipramine and 2-hydroxydesipramine

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7
Q

halogenation of TCAs makes them more potent inhibitors of?

A

5-HT reuptake

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8
Q

what drug class is Imipramine?

A

TCA

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9
Q

what drug class is amitriptyline?

A

TCA

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10
Q

amitriptyline undergoes what metabolism? what is the active metabolite?

A

N-demethylation
nortriptyline

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11
Q

which TCA is used as a mixture of Z/E isomers?

A

Doxepin

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12
Q

what drug class is doxepin?

A

TCA

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13
Q

what is the active metabolite of doxepin?

A

N-desmethyldoxepin

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14
Q

why do we make anti-itch creams containing doxepin?

A

it has anti H1 activity

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15
Q

why can doxepin be found in a sleep aid drug?

A

due to its H1 antagonism

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16
Q

which TCA is more selective for inhibiting NET over SERT?

A

Maprotiline

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17
Q

what drug class is maprotiline?

A

TCA

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18
Q

what is the mechanism of action of MAOIs?

A

catalyze the oxidative deamination of beta-arylethyl amines such as NE, DA, 5-HT, and tyramine

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19
Q

what are the 2 characteristics of traditional MAOIs?

A
  1. mechanism-based irreversible inhibitors
  2. lack selectivity between MAO-A and MAO-B
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20
Q

what drug class is tranylcypromine?

A

traditional MAOI

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21
Q

what drug class is phenelzine?

A

traditional MAOI

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22
Q

what route of metabolism does phenelzine inhibit?

A

Cyp2B6

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23
Q

what drug class is isocarboxazid?

A

traditional MAOI prodrug

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24
Q

what is the name of the active version of isocarboxazid? drug class?

A

benzylhydrazine
also a traditional MAOI

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25
Q

what drug class is selegiline?

A

MAO-B inhibitor

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26
Q

what drug formulation does selegiline come in?

A

transderm patch

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27
Q

what drug class is fluoxetine?

A

SSRI

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28
Q

what characteristic do all SSRIs have?

A

an electron withdrawing group consisting of halogens

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29
Q

what route of metabolism does fluoxetine undergo? what is the active metabolite?
what’s significant about fluoxetine’s half-life?

A

N-demethylation into Norfluoxetine
has a very long half-life, 4-16 days

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30
Q

which two routes of metabolism do fluoxetine/norfluoxetine inhibit?

A

Cyp2D6 and 2C19

31
Q

how long does the pt need to wait after stopping MAOI therapy to start fluoxetine therapy?

A

2 weeks

32
Q

how long does the pt need to wait after stopping fluoxetine therapy to start MAOI therapy?

A

5 weeks

33
Q

which SSRI is used as a single 1S,4S, enantiomer?

A

sertraline

34
Q

what drug class is sertraline?

A

SSRI

35
Q

what is the active metabolite of sertraline?

A

N-desmethylsertraline

36
Q

what route of metabolism does sertraline inhibit?

A

Cyp2D6

37
Q

which SSRI is used as the 3S,4R enantiomer?

A

paroxetine

38
Q

what drug class is paroxetine?

A

SSRI

39
Q

what route of metabolism does sertraline undergo? what is its inactive metabolite?

A

Cyp2D6 into catechol metabolite

40
Q

paroxetine is a potent irreversible inhibitor of what route of metabolism?

A

2D6

41
Q

what drug class is fluvoxamine?

A

SSRI

42
Q

what is the active metabolite of fluvoxamine?

A

there is none

43
Q

which 2 routes of metabolism does fluvoxamine inhibit?

A

Cyp1A2 and 2C19

44
Q

which SSRI has the most selectivity for SERT?

A

citalopram

45
Q

what drug class is citalopram?

A

SSRI

46
Q

what is the single active S enantiomer of citalopram?

A

escitalopram

47
Q

what is the active metabolite of citalopram?

A

desmethylcitalopram

48
Q

what drug class is trazodone?

A

serotonin modulator and stimulator

49
Q

what metabolizes trazodone? what is the active metabolite? what is the drug classification of the metabolite?

A

Cyp3A4
m-chlorophenylpiprazine
5HT2A partial agonist

50
Q

what drug class is nefazodone?

A

serotonin modulator and stimulator

51
Q

what metabolizes nefazodone? the two active metabolites?

A

Cyp3A4
m-chlorophenylpiprazine and alpha-hydroxynefazodone

52
Q

both nefazodone and alpha-hydroxynefazodone are inhibitors of what route of metabolism?

A

cyp3A4

53
Q

what drug class is vilazodone?

A

serotonin modulator and stimulator

54
Q

what metabolism does vilazodone undergo?

A

Cyp3A4 N-dealkhylation

55
Q

what drug class is vortioxetine?

A

serotonin modulator and stimulator

56
Q

what route of metabolism does vortioxetine undergo?

A

Cyp2D6

57
Q

what drug class is venlafaxine?

A

SNRI

58
Q

what metabolite is formed when venlafaxine undergoes Cyp3A4 metabolism? active or inactive?

A

N-desmethylvenlafaxine
inactive

59
Q

what metabolite is formed when venlafaxine undergoes Cyp2D6 O-demethylation metabolism? active or inactive?

A

desvenlafaxine
active

60
Q

what is the major route of metabolism of desvenlafaxine?
minor route?
which is active/inactive?

A

glucuronidation
3A4 N-demethylation
neither are active

61
Q

what drug class is duloxetine?

A

SNRI

62
Q

duloxetine is metabolized by Cyp1A2 and 2D6, what is the specific target of their metabolism? what else metabolizes duloxetine? active or inactive?

A

napthalene ring hydroxylation
glucuronidation
inactive

63
Q

duloxetine is an inhibitor of what route of metabolism?

A

2D6

64
Q

what drug class is levomilnacipran?

A

SNRI

65
Q

which SNRI is used as the single 1S,2R enantiomer?

A

levomilnacipran

66
Q

what is the metabolic route of levomilnacipran?
active or inactive?

A

3A4-mediated N-deethylation
inactive

67
Q

bupropion undergoes hydroxylation via which enzyme? what is the metabolite formed? active or inactive?

A

Cyp2B6
hydroxybupropion
active

68
Q

bupropion undergoes reduction into what metabolite? active or inactive?

A

threo and erythro hydroxybupropion
active

69
Q

bupropion and hydroxybupropion are inhibitors of what enzyme?

A

2D6

70
Q

what distinguishes mirtazapine from TCAs despite having very similar structuring?

A

the basic nitrogen is closer to the tricyclic ring system than in TCAs

71
Q

what dosage form does esketamine come in?

A

nasal spray

72
Q

what are the main routes of metabolism of esketamine?

A

2B6 and 3A4 N-demethylation

73
Q

drug class of esketamine?

A

NMDA receptor antagonist

74
Q

drug class of phencyclidine?

A

NMDA receptor antagonist

IDT Fall (29 decks)

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