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PHARM 3 > Antidepressants > Flashcards

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
Q

escitalopram

A

SSRI

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26
Q

fluoxetine

A

SSRI

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27
Q

fluvoxamine

A

SSRI

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28
Q

paroxetine

A

SSRI

29
Q

sertraline

A

SSRI

30
Q

SSRI MOA

A

specific inhibition of serotonin reuptake

- little activity at alpha, M, and H1 receptors

31
Q

DOC depression

A

SSRI

32
Q

SSRI AE

A

inc serotinergic activity =

GI upset
weight gain (paroxetine)
decreased sexual function/interest
33
Q

SSRI interactions

A

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
Q

SSRI OD

A

seizures

low likely for fatalities

35
Q

venlafaxine

A

SNRI

36
Q

duloxetine

A

SNRI

37
Q

SNRI OA

A

block serotonin and NE reuptake

lack H1, M, and a1 blockade**

38
Q

venlafaxine

A

potent inhibitor of 5HT uptake

higher doses inhibit NE uptake

also weakly inhibits DA reuptake

39
Q

duloxetine

A

inhbits serotonin and NE reuptake at all doses

40
Q

bupropion

A

NDRI

  • inhibits NE and DA uptake - increases their release

no sexual dysfunction b/c lacks 5HT component

41
Q

buproprion OD

A

seizures

42
Q

nefazodone

A

5HT2 antagonist/reuptake inhibitor SARIs

**severe hepatotoxicity - no longer prescribed

43
Q

trazodone

A

5HT2 antagonist/reuptake inhibitors SARIs - also inhibits alpha 1 and H1

-extremely sedating and good hypnotic (MAIN USE = hypnotic)

44
Q

SARIs function

A

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
Q

mirtazapine

A

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
Q

anti-depressant discontinuation syndrome

A

associated with SSRI discontinuation (most commonly prescribed)

  • anxiety, dizzy, HA, lethargy, flu sxs
  • electric shock sensations
  • insomnia
  • n/v/d
47
Q

which drugs are most likely to cause discontinuation syndrome

A

paroxetine
venlafaxine

most common with short half life drugs

(least likely with fluoxetine b/c long half life)

48
Q

which TCAs have greater effects on serotonin

A

amitriptyline
clomipramine
imipramine

also greater orthostatic hypotension and antimuscarinic effects

49
Q

which TCAs have stronger NET effects - (greater adrenergic)

A

2ndary amines: desipramine, nortriptyline

less sedation, anti- muscarinic effects, orthostatic hypotension

50
Q

which antidepressant is most commonly used as a hypnotic

A

trazodone

51
Q

DOC for depression

A

SSRI

52
Q

depression adjuncts

A

atypical antipsychotic

53
Q

anxiety disorder DOC

A

SSRI

buproprion is less effective than others

54
Q

chronic pain use

A

TCAs and SNRIs (drugs blcoking NE and 5HT reuptake)

SSRIs are not effective

55
Q

bulimia tx

A

antidepressants - but not helpful for anorexia

56
Q

premenstrual dysphoric disorder

A

SSRIs

57
Q

smoking cessation tx

A

bupropion

58
Q

bipolar contraindication with anti-depressants

A

may precipitate mania - must screen pts for biopolar disorder

59
Q

DOC bipolar disorder

A

lithium

60
Q

lithium MOA

A

“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
Q

lithium AE

A 
tremor
sedation
ataxia
seizure
wt gain
hypothyroidism
leukocytosis
alopecia
nephrogenic diabetes insipidus
62
Q

tx lithium tremor

A

propanolol or atenolol

63
Q

tx nephrogenic DI assoc with lithium

A

discontinue lithium if possible

–> amiloride otherwise
also thiazides and NSAIDs

64
Q

lithium intoxication sxs

A 
vomiting
diarrhea
coarse tremor
ataxia
coma
65
Q

lithium in pregnancy

A

congenital cardiac anomalies

category D

66
Q

what tests to do in someone taking lithium

A

serum lithium concentrations
thyroid function
renal function

67
Q

lithium interactions

A 
dec renal clearance by:
thiazides
NSAIDs
ACE-I
ARBs
68
Q

lithium alternatives

A

carbamazepine (check CBCs)

valproate (LFT and CBC monitored)

PHARM 3 (21 decks)

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