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Pharm Exam 3 > 33: Antidepressants > Flashcards

33: Antidepressants Flashcards

1
Q

symptoms of major depression

A
  • depressed mood

- anhedonia (loss of pleasure) and loss of interest in life

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2
Q

gold standard treatment for major depression

A

electroconvulsive therapy

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3
Q

2 common reasons why chemical antidepressants may not work for people?

A
  • delay of therapeutic response (weeks or months of regular dosing to achieve benefit)
  • side effects can limit usage, especially in elderly
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4
Q

What are the two hypotheses of depression?

A
  1. Monoamine/Biogenic Amine hypothesis (abnormalities in 5HT, NE, and DA neurotransmission
  2. Neurotrophic Hypothesis (changes in nerve growth factors BDNF play a role in cell survival and synaptic plasticity)

these two hypotheses are likely not mutually exclusive

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5
Q

BDNF –>

A

TRK-B receptors –> increased neuronal survival and growth

antidepressants increase BDNF in the brain: neurotrophic hypothesis

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6
Q

side effects = GI disturbances, anxiety, sexual dysfunction

A

5HT reuptake blockade

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7
Q

side effects = tremors, tachycardia

A

NE reuptake blockade

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8
Q

side effects = psychomotor activation, antiparkinsonian effects, psychosis, increased attention and concentration

A

DA uptake blockade

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9
Q

side effects = sedation, drowsiness, weight gain, hypotension

A

H1 receptor blockade

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10
Q

side effects = blurred vision, dry mouth, sinus tachycardia, constipation, urinary retention, memory dysfunction

A

Muscarinic Ach receptor blockade

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11
Q

side effects = postural hypotension, reflex tachycardia, dizziness

A

a1 receptor blockade (adrenergic)

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12
Q

MOA MAOIs

A

increase synaptic availability of NE and 5HT blocking their catabolism via inhibition of MAO enzymes

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13
Q

MAO-A vs. MAO-B

A

MAO-A : targets tyramine, NE, 5HT and DA

MAO-B : targets mainly DA

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14
Q

irreversible MAO-A and MAO-B inhibitors

A

phenelzine

tranylcypromine

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15
Q

MOA selegiline

A

MAO-B inhibitor at low dose, non-selective MAOi at higher dose

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16
Q

low dose use selegline

A

parkinson’s disease

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17
Q

antidepressant use selegline

A

high dose (patch to prevent first pass effect and tyramine effect)

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18
Q

tyramine and MAOIs —>

A

hypertensive crisis

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19
Q

tyramine and MAOIs —>

A

hypertensive crisis

amine from tyrosine triggers release of catecholamines in the synapse leading to overwhleming vasoconstriction and a hypertensive crisis

watch out for cheese and chianti wines especially

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20
Q

current major clinical use for TCAs

A

chronic pain conditions

used for major deprssion if SSRIs are not effective

21
Q

MOA TCAs

A

block reuptake of both 5HT and NE by inhibition of SERT and NET respectively

dirty drugs - also work as agonists at cholinergic, histaminergic and a-adrenergic receptors

22
Q

which TCA is used to treat enuresis (bedwetting)?

A

imipraimine

23
Q

which TCA is more effective at treating neuropathic pain?

A

desipramine

has stronger NE than 5HT properties

24
Q

which TCA is known for sedative effects?

A

amitriptyline

25
Q

why are TCAs known as “hip breakers” in elderly patients?

A

antagonist action at alpha1 receptors –> orthostatic hypotension

also have dry mouth, constipation, blurred vision, urinary retention and confusion side effects due to antagonist actions at muscarinic receptors

26
Q

most serious side effect of TCAs

A

lethal cardiac arrhythmias

due to Na/Ca channel blocking properties

27
Q

3 C overdose of TCAs

A

convulsion
coma
cardiac arrhythmia

28
Q

MOA SSRIs

A

selectively inhibit SERT and block the reuptake of 5HT into the presynaptic terminal –> increases synaptic 5HT

29
Q

short term side effects SSRIs =

long term =

A

short term = nausea, GI upset, diarrhea (1st week)

long term = sexual dysfunction

30
Q

observe: lethargy, restlessness, mental confusion, flushing, diaphoresis, tremor

A

Serotonin Syndrome

-rare side effect of SSRIs due to long half-life that occurs usually when drug combos or switching meds

31
Q

which SSRIs pose the greatest risk for discontinuation syndrome?

A

paroxetine and sertraline

sudden discontinuation of short half-life SSRIs may cause advers side effects such as dizziness, paresthesias, and anxiety 1-7 days after stopping because of sensitization

switch to SSRI with longer half-life and then discontinue if pt is susceptible to this effect

32
Q

MOA SNRI

A

selective serotonin-norepinephrine reuptake inhibitors

both inhibit serotonin SERT and norepinephrine NET transporters

unlike TCAs do not have much affinity for other receptors –> better side effect profile

33
Q

clinical use venlafaxine

A

SNRI used for severe depression

34
Q

clinical use duloxetine

A

SNRI with increasing use for chronic pain over TCAs

35
Q

Trazodone is a…

A

5HT2 antagonist that also blocks H1 receptor –> sedative effects without tolerance or dependence

36
Q

negative side effect of trazodone

A

priapism

due to peripheral a1 blocking effect

37
Q

smoking cessation drug

A

bupropion

38
Q

MOA bupropion

A

blocks NE and DA reuptake and increases presynaptic release of catecholamines

39
Q

MOA mirtazapine

A

blocks presynpative a2 receptors and increase synaptic release of 5HT and NE
- blocks 5HT2 and 5HT2 (antiemetic)
blocks H1 receptor –> sedation, weight gain, few sexual side effects

40
Q

major side effect SNRIs

A

discontinuation syndrome

41
Q

what anti-depressants can you combine?

A

MAOIs, TCAs, and SSRIs should NOT be combined - fatal side effects!

42
Q

which drugs are potent inhibitors of CYP2D6?

A

paroxetine
fluoxetine
fluvoxamine

43
Q

drug of choice for bipolar disorder

A

lithium

mood-stabilizing. depressive phase requires use of anti-depressants

44
Q

anticonvulsants used in bipolar disorder treatment

A

valproic acid and carbamazepine

45
Q

treatment of acute mania

A

valproic acid and carbamazepine

46
Q

MOA lithium

A

prevents recycling of inositol phosphate (mood dampening) and inhibits release of NE (prevent mania)

47
Q

4 side effects of lithium

A
  • tremor
  • hypothyroidism
  • nephrogenic diabetes insipidus
  • skin rxn
48
Q

what drugs interact with lithium?

A

thiazide and loop diuretics –> diminish Li clearance and can cause toxicity

Pharm Exam 3 (11 decks)

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