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PPP Winter FINAL > Antidepressants > Flashcards

Antidepressants Flashcards

1
Q

Describe the monoamine deficiency hypothesis

A

Current antidepressants either block reuptake or inhibit enzyme that breaks down NTs

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2
Q

Describe the dysregulation hypothesis

A

Failure of homeostatic regulation of NT systems

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3
Q

Describe the hypothalamic-pituitary stress model

A

Chronic stress and increased cortisol may cause disruption in neuronal function

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4
Q

What drugs act on

5HT transporter

A

Selective serotonin reuptake inhibitors (SSRI)

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5
Q

What drugs act on

5HT, NE transporter

A

Serotonin norepinephrine reuptake inhibitors (SNRI)

Tricyclics antidepressants (TCAs)

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6
Q

What drugs act on

5HT, NE, DA transporter

A

Monoamine oxidase inhibitor (MAOI)

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7
Q

What drugs act on

NE, DA transporter

A

Bupropion

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8
Q

What drugs act on miscellaneous sites of action?

A

Nefazodone

Trazodone

Mirtazapine

Vilazodone

Vortioxetine

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9
Q

What are activities of

5HT1A partial agonist

A

Anxiolytic

Antidepressants

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10
Q

What are activities of

5HT2A antagonist

A

Anxiolytic

Sleep restoring

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11
Q

What are activities of

5HT2C antagonist

A

Anxiolytic

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12
Q

What are activities of

Serotonin transporter inhibition

A

Antidepressant

Anxiolytic

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13
Q

What is the MOA of SSRIs?

What one other action does (only) paroxetine have?

A

Block pre-synaptic reuptake of serotonin

Paroxetine: blocks post-synaptic muscarinic receptor

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14
Q

What agents are examples of SSRIs?

A

Fluoxetine
Sertraline
Paroxetine

Fluvoxamine
Citalopram
Escitalopram

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15
Q

What are examples of SNRIs?

A

Venlafaxine

Duloxetine

Desvenlafaxine

Levomilnacipran

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16
Q

What is the MOA of SNRIs?

A

Block pre-synaptic 5HT and NE reuptake

*no blockade of alpha1, muscarinic, or histamine receptors

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17
Q

Differentiate venlafaxine dose-related effects

A

<150 = mostly 5HT action

> 150 = dual 5HT and NE

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18
Q

Which SNRI has higher binding affinity to NE and 5HT reuptake transporters and increases these neurotransmitters at initial doses?

A

Duloxetine

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19
Q

What is the MOA of TCAs?

A

Block pre-synaptic reuptake of serotonin and NE

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20
Q

Differentiate between tertiary and secondary amines

A

Tertiary = more AEs

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21
Q

List examples of TCAs

A

Tertiary =
+Amitriptyline
+Imipramine
+Clomipramine

Secondary =

  • Nortriptyline
  • Desipramine
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22
Q

List examples of MAOIs

A

Phenelzine

Tranylcypromine

Selegiline

23
Q

What are the MOA of MOAIs?

A

Bind to MAO irreversibly and destroy its function

24
Q

Differentiate between monoamine oxidase A and B

A

MOA A =
Metabolizes NE, 5HT (involved in depression)

MOA B =
Metabolizes dopamine
(Involved in Parkinson’s disease)

25
Q

What do nefazodone and trazodone do?

A 
Block 
\+presynaptic 5HT reuptake
\+postsynpatic 5HT2 receptor
\+postsynpatic alpha1 receptor
\+postynaptic histamine receptor
26
Q

What does bupropion do?

A

Blocks reuptake of NE and DA

27
Q

What does mirtazapine do?

A

Blocks alpha2 autoreceptor
(Causes inc. NE, 5HT)

Blocks postsynaptic 5HT2A
Stimulates 5HT1A 
Blocks post 5HT2C
Blocks 5HT3
Blocks H1
28
Q

What does vortioxetine do?

A

Indicated for major depression

29
Q

What AEs are caused by

ACh blockade

A

Anorexia

Blurry vision

Constipation/confusion

Dry mouth

Sedation, stasis of urine

30
Q

What AEs are caused by

H1 blockade

A

Sedation

Dizziness

Confusion

Weight gain

31
Q

What AEs are caused by

Alpha1 blockade

A

Orthostatic hypotension

Reflex tachycardia

Dizziness

Sexual dysfunction

Inc. urinary outflow

32
Q

Which class of antidepressants are worst for anticholinergic effects?

A

TCAs

Followed by MAOIs

33
Q

What class of antidepressants are worst for antihistamine effects?

A

TCAs

Followed by mirtazapine

34
Q

Which class of antidepressants are worst for alpha1 blockade effects?

A

TCAs
Trazodone
Nefazodone

35
Q

What antidepressant AEs is the receptor involved in

5HT

A

GI (N/V/D)

Platelet dysfunction

36
Q

What antidepressant AEs is the receptor involved in

5HT2A stimulation

A

CNS (disturbed sleep)

Sexual dysfunction

37
Q

What antidepressant AEs is the receptor involved in

5HT2C blockade

A

Weight gain

38
Q

What antidepressant AEs is the receptor involved in

5HT3 blockade

A

No nausea

No GI upset

39
Q

What antidepressant AEs is the receptor involved in

NE, DA reuptake blockade

A

Inc. BP/HR

Inc. energy/anxiety/jitteriness

40
Q

What class of antidepressants are the worst for GI effects?

A

MAOIs

Followed by TCAs

41
Q

Why are SSRIs associated with increase in bleeding episodes?

A

Serotonin potentiates platelet activation

42
Q

Which antidepressants have the highest risk for seizures?

A

TCAs

Bupropion

43
Q

What are miscellaneous AEs associated with antidepressants?

A 
Osteoporosis
QT prolongation (citalopram)

Conduction abnormalities
(TCAs highest risk)
Inc. BP/HR - NE/DA drugs

Withdrawal syndrome
Sweating
SIADH, hyponatremia
Weight gain
Hepatitis
44
Q

Compare different antidepressant classes regarding their potential to cause a “hypertensive crisis”

A

TCAs

SNRIs

Bupropion

45
Q

Which drugs have the worse withdrawals?

Short acting agents

A

Paroxetine

Venlafaxine

Fluvoxamine

46
Q

Which side effect are you most likely to see first with SSRI?

A

Insomnia

47
Q

Compare and contrast serotonin syndrome vs. neuroleptic malignant syndrome

A

Serotonin
+drug = pro-serotonergic
+<12 hrs to develop
+hyperactive bowel sounds

Neuroleptic
+drug = dopamine antagonist
+1-3 days to develop
+rigidity present in muscles

48
Q

Describe DDIs with MAOIs

A

Do not use w/in 5 weeks of D/C fluoxetine

Do not use w/in 2 weeks of DC other SSRI, TCA, MAOI

Wait 2 weeks after D/C MAOIs to switch to another antidepressants

49
Q

If you had a patient complaining of significant nausea,

Which receptor activity would you need in your antidepressant?

A

5HT3 antagonist

50
Q

Which drug should be avoided in a patient with significant cardiac history and abnormal EKG findings?

A

Citalopram

Imipramine

Amitriptyline

51
Q

A patient who has previously responded to clomipramine for an anxiety condition is requiring a change in medication

Which drug has similar MOA?

A

Venlafaxine

52
Q

A 38 YO male with a long h/o alcohol abuse is diagnosed with depression

Which agent would be least desirable to initiate?

A

Duloxetine

53
Q

What is the MOA of duloxetine?

A

5HT and NE reuptake inhibitor

54
Q

Which antidepressant is least preferred in an elderly patient with glaucoma?

A

Amitriptyline (TCA)

PPP Winter FINAL (8 decks)

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