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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
what drug class is selegiline?
MAO-B inhibitor
26
what drug formulation does selegiline come in?
transderm patch
27
what drug class is fluoxetine?
SSRI
28
what characteristic do all SSRIs have?
an electron withdrawing group consisting of halogens
29
what route of metabolism does fluoxetine undergo? what is the active metabolite? what's significant about fluoxetine's half-life?
N-demethylation into Norfluoxetine has a very long half-life, 4-16 days
30
which two routes of metabolism do fluoxetine/norfluoxetine inhibit?
Cyp2D6 and 2C19
31
how long does the pt need to wait after stopping MAOI therapy to start fluoxetine therapy?
2 weeks
32
how long does the pt need to wait after stopping fluoxetine therapy to start MAOI therapy?
5 weeks
33
which SSRI is used as a single 1S,4S, enantiomer?
sertraline
34
what drug class is sertraline?
SSRI
35
what is the active metabolite of sertraline?
N-desmethylsertraline
36
what route of metabolism does sertraline inhibit?
Cyp2D6
37
which SSRI is used as the 3S,4R enantiomer?
paroxetine
38
what drug class is paroxetine?
SSRI
39
what route of metabolism does sertraline undergo? what is its inactive metabolite?
Cyp2D6 into catechol metabolite
40
paroxetine is a potent irreversible inhibitor of what route of metabolism?
2D6
41
what drug class is fluvoxamine?
SSRI
42
what is the active metabolite of fluvoxamine?
there is none
43
which 2 routes of metabolism does fluvoxamine inhibit?
Cyp1A2 and 2C19
44
which SSRI has the most selectivity for SERT?
citalopram
45
what drug class is citalopram?
SSRI
46
what is the single active S enantiomer of citalopram?
escitalopram
47
what is the active metabolite of citalopram?
desmethylcitalopram
48
what drug class is trazodone?
serotonin modulator and stimulator
49
what metabolizes trazodone? what is the active metabolite? what is the drug classification of the metabolite?
Cyp3A4 m-chlorophenylpiprazine 5HT2A partial agonist
50
what drug class is nefazodone?
serotonin modulator and stimulator
51
what metabolizes nefazodone? the two active metabolites?
Cyp3A4 m-chlorophenylpiprazine and alpha-hydroxynefazodone
52
both nefazodone and alpha-hydroxynefazodone are inhibitors of what route of metabolism?
cyp3A4
53
what drug class is vilazodone?
serotonin modulator and stimulator
54
what metabolism does vilazodone undergo?
Cyp3A4 N-dealkhylation
55
what drug class is vortioxetine?
serotonin modulator and stimulator
56
what route of metabolism does vortioxetine undergo?
Cyp2D6
57
what drug class is venlafaxine?
SNRI
58
what metabolite is formed when venlafaxine undergoes Cyp3A4 metabolism? active or inactive?
N-desmethylvenlafaxine inactive
59
what metabolite is formed when venlafaxine undergoes Cyp2D6 O-demethylation metabolism? active or inactive?
desvenlafaxine active
60
what is the major route of metabolism of desvenlafaxine? minor route? which is active/inactive?
glucuronidation 3A4 N-demethylation neither are active
61
what drug class is duloxetine?
SNRI
62
duloxetine is metabolized by Cyp1A2 and 2D6, what is the specific target of their metabolism? what else metabolizes duloxetine? active or inactive?
napthalene ring hydroxylation glucuronidation inactive
63
duloxetine is an inhibitor of what route of metabolism?
2D6
64
what drug class is levomilnacipran?
SNRI
65
which SNRI is used as the single 1S,2R enantiomer?
levomilnacipran
66
what is the metabolic route of levomilnacipran? active or inactive?
3A4-mediated N-deethylation inactive
67
bupropion undergoes hydroxylation via which enzyme? what is the metabolite formed? active or inactive?
Cyp2B6 hydroxybupropion active
68
bupropion undergoes reduction into what metabolite? active or inactive?
threo and erythro hydroxybupropion active
69
bupropion and hydroxybupropion are inhibitors of what enzyme?
2D6
70
what distinguishes mirtazapine from TCAs despite having very similar structuring?
the basic nitrogen is closer to the tricyclic ring system than in TCAs
71
what dosage form does esketamine come in?
nasal spray
72
what are the main routes of metabolism of esketamine?
2B6 and 3A4 N-demethylation
73
drug class of esketamine?
NMDA receptor antagonist
74
drug class of phencyclidine?
NMDA receptor antagonist

IDT Fall (29 decks)

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