Antidepressants Flashcards

1
Q

monoamine hypothesis

A

reserpine used for HTN found to cause depression - depleted DA, 5HT, NE

iproniazid/isoniazid - lift depression - inhibit MAO

“depression d/t lowered monoamine NT in synapses - achieve tx via restoring monoamine levels”

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2
Q

isocarboxazid

A

MAOI

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3
Q

phenelzine

A

MAOI

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4
Q

traylcypromine

A

MAOI

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5
Q

selegiline

A

MAOI

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6
Q

MAOI MOA

A

mitochondrial enzyme MAO is inhibited = inactivates excess NE, DA, and 5HT that may leak out – they escape degradation

MAO-A: metabolizes NE and 5HT

MAO-B: metabolizes DA and tyramine

antidepressant effect correlates with MAO-A inhibition

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7
Q

hydrazine derivative MAOI

A

phenelzine

isocarboxazid

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8
Q

non-hydrazine derivative MAOI

A

tranylcypromine

selegiline

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9
Q

which MAOIs bind irreversibly and nonselectively to MAO-A and MAO-B

A

phenelzine
isocarboxazid
tranylcypromine

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10
Q

which MAOI only binds MAO-B

A

selegiline

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11
Q

which MAOI is approved for early tx parkinsons

A

selegiline

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12
Q

MAOI use

A

rarely used b/c of AE

used when other tx’s are ineffective

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13
Q

MAOI AE

A

drowsiness
orthostatic hypotension
weight gain
muscle pain

  • serotonin syndrome: hyperthermia, muscle rigidity, myoclonus
    • MAOI + serotinergic drug
  • cheese reaction
    • tyramine causes release of catecholamines = tachycardia, HTN, arrhythmias, seizures

(also seen with sympathomimetic drugs - pseudoephedrine and phenylpropanoloamine)

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14
Q

which MAOI is less likely to cause tyramine induced HTN crisis

A

selegiline transdermal patch

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15
Q

tx of cheese reaction

A

phentolamine

prazosin

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16
Q

amitriptyline

A

TCA

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17
Q

clomipramine

A

tCA

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18
Q

desipramine

A

TCA

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19
Q

imipramine

A

TCA

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20
Q

nortriptyline

A

TCA

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21
Q

TCA MOA

A

block SERT and NET = increased MA in cleft

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22
Q

TCA AE

A

blockade of alpha (orthostatic hypotension, reflex tachy)

  • muscarinic (blurred vision, xerostomia, urinary retention) - histamine (sedation, weight gain)
  • cardiac fast sodium channels (arrhythmias)
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23
Q

TCA OD tx

A

sodium bicarbonate - reverse conduction block

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24
Q

citalopram

A

SSRI

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25
escitalopram
SSRI
26
fluoxetine
SSRI
27
fluvoxamine
SSRI
28
paroxetine
SSRI
29
sertraline
SSRI
30
SSRI MOA
specific inhibition of serotonin reuptake | - little activity at alpha, M, and H1 receptors
31
DOC depression
SSRI
32
SSRI AE
inc serotinergic activity = ``` GI upset weight gain (paroxetine) decreased sexual function/interest ```
33
SSRI interactions
fluoxetine + paroxetine (inhibit CYP2D6) Fluvoxamine (inhibit CYP1A2, CYP2C19, CYP3A4) citalopram, escitalopram, sertraline (low potential for interactions) (if question tells you person taking multiple medications for HTN, DM, gout etc - give low potential drug)
34
SSRI OD
seizures low likely for fatalities
35
venlafaxine
SNRI
36
duloxetine
SNRI
37
SNRI OA
block serotonin and NE reuptake lack H1, M, and a1 blockade**
38
venlafaxine
potent inhibitor of 5HT uptake higher doses inhibit NE uptake also weakly inhibits DA reuptake
39
duloxetine
inhbits serotonin and NE reuptake at all doses
40
bupropion
NDRI - inhibits NE and DA uptake - increases their release no sexual dysfunction b/c lacks 5HT component
41
buproprion OD
seizures
42
nefazodone
5HT2 antagonist/reuptake inhibitor SARIs **severe hepatotoxicity - no longer prescribed
43
trazodone
5HT2 antagonist/reuptake inhibitors SARIs - also inhibits alpha 1 and H1 -extremely sedating and good hypnotic (MAIN USE = hypnotic)
44
SARIs function
stimulation of 5H2 causes anxiety - so blocking prevents that and may cause sexual dysfunction combo of 5HT reuptake and 5HT2 antagonist weak SERT and NET antagonists, strong antagonist at 5HT2
45
mirtazapine
NASSA = antagonist of central presynaptic alpha 2 receptors - inc release of NE and 5HT antagonist at 5HT1 and 5HT3 H1 antagonist - *sedation and weight gain
46
anti-depressant discontinuation syndrome
associated with SSRI discontinuation (most commonly prescribed) - anxiety, dizzy, HA, lethargy, flu sxs - electric shock sensations - insomnia - n/v/d
47
which drugs are most likely to cause discontinuation syndrome
paroxetine venlafaxine most common with short half life drugs (least likely with fluoxetine b/c long half life)
48
which TCAs have greater effects on serotonin
amitriptyline clomipramine imipramine also greater orthostatic hypotension and antimuscarinic effects
49
which TCAs have stronger NET effects - (greater adrenergic)
2ndary amines: desipramine, nortriptyline less sedation, anti- muscarinic effects, orthostatic hypotension
50
which antidepressant is most commonly used as a hypnotic
trazodone
51
DOC for depression
SSRI
52
depression adjuncts
atypical antipsychotic
53
anxiety disorder DOC
SSRI | buproprion is less effective than others
54
chronic pain use
TCAs and SNRIs (drugs blcoking NE and 5HT reuptake) SSRIs are not effective
55
bulimia tx
antidepressants - but not helpful for anorexia
56
premenstrual dysphoric disorder
SSRIs
57
smoking cessation tx
bupropion
58
bipolar contraindication with anti-depressants
may precipitate mania - must screen pts for biopolar disorder
59
DOC bipolar disorder
lithium
60
lithium MOA
"inositol depletion theory" G protein linked receptors to Gq -- PLC = cleaves PIP2 = DAG + IP3 IP3 -> IP2 -> IP1 -> inositol lithium blocks inositol polyphosphatase and monophosphatase = blocking regeneration of inositol - whole cascade stopped inhibition of central adrenergic, muscarinic, serotonergic transmission NON-COMPETITIVE = only active receptors on neurons are affected
61
lithium AE
``` tremor sedation ataxia seizure wt gain hypothyroidism leukocytosis alopecia nephrogenic diabetes insipidus ```
62
tx lithium tremor
propanolol or atenolol
63
tx nephrogenic DI assoc with lithium
discontinue lithium if possible | --> amiloride otherwise also thiazides and NSAIDs
64
lithium intoxication sxs
``` vomiting diarrhea coarse tremor ataxia coma ```
65
lithium in pregnancy
congenital cardiac anomalies category D
66
what tests to do in someone taking lithium
serum lithium concentrations thyroid function renal function
67
lithium interactions
``` dec renal clearance by: thiazides NSAIDs ACE-I ARBs ```
68
lithium alternatives
carbamazepine (check CBCs) | valproate (LFT and CBC monitored)