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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
What do nefazodone and trazodone do?
``` Block +presynaptic 5HT reuptake +postsynpatic 5HT2 receptor +postsynpatic alpha1 receptor +postynaptic histamine receptor ```
26
What does bupropion do?
Blocks reuptake of NE and DA
27
What does mirtazapine do?
Blocks alpha2 autoreceptor (Causes inc. NE, 5HT) ``` Blocks postsynaptic 5HT2A Stimulates 5HT1A Blocks post 5HT2C Blocks 5HT3 Blocks H1 ```
28
What does vortioxetine do?
Indicated for major depression
29
What AEs are caused by ACh blockade
Anorexia Blurry vision Constipation/confusion Dry mouth Sedation, stasis of urine
30
What AEs are caused by H1 blockade
Sedation Dizziness Confusion Weight gain
31
What AEs are caused by Alpha1 blockade
Orthostatic hypotension Reflex tachycardia Dizziness Sexual dysfunction Inc. urinary outflow
32
Which class of antidepressants are worst for anticholinergic effects?
TCAs | Followed by MAOIs
33
What class of antidepressants are worst for antihistamine effects?
TCAs | Followed by mirtazapine
34
Which class of antidepressants are worst for alpha1 blockade effects?
TCAs Trazodone Nefazodone
35
What antidepressant AEs is the receptor involved in 5HT
GI (N/V/D) Platelet dysfunction
36
What antidepressant AEs is the receptor involved in 5HT2A stimulation
CNS (disturbed sleep) Sexual dysfunction
37
What antidepressant AEs is the receptor involved in 5HT2C blockade
Weight gain
38
What antidepressant AEs is the receptor involved in 5HT3 blockade
No nausea No GI upset
39
What antidepressant AEs is the receptor involved in NE, DA reuptake blockade
Inc. BP/HR Inc. energy/anxiety/jitteriness
40
What class of antidepressants are the worst for GI effects?
MAOIs | Followed by TCAs
41
Why are SSRIs associated with increase in bleeding episodes?
Serotonin potentiates platelet activation
42
Which antidepressants have the highest risk for seizures?
TCAs Bupropion
43
What are miscellaneous AEs associated with antidepressants?
``` Osteoporosis QT prolongation (citalopram) ``` Conduction abnormalities (TCAs highest risk) Inc. BP/HR - NE/DA drugs ``` Withdrawal syndrome Sweating SIADH, hyponatremia Weight gain Hepatitis ```
44
Compare different antidepressant classes regarding their potential to cause a "hypertensive crisis"
TCAs SNRIs Bupropion
45
Which drugs have the worse withdrawals? | Short acting agents
Paroxetine Venlafaxine Fluvoxamine
46
Which side effect are you most likely to see first with SSRI?
Insomnia
47
Compare and contrast serotonin syndrome vs. neuroleptic malignant syndrome
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
Describe DDIs with MAOIs
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
If you had a patient complaining of significant nausea, Which receptor activity would you need in your antidepressant?
5HT3 antagonist
50
Which drug should be avoided in a patient with significant cardiac history and abnormal EKG findings?
Citalopram Imipramine Amitriptyline
51
A patient who has previously responded to clomipramine for an anxiety condition is requiring a change in medication Which drug has similar MOA?
Venlafaxine
52
A 38 YO male with a long h/o alcohol abuse is diagnosed with depression Which agent would be least desirable to initiate?
Duloxetine
53
What is the MOA of duloxetine?
5HT and NE reuptake inhibitor
54
Which antidepressant is least preferred in an elderly patient with glaucoma?
Amitriptyline (TCA)

PPP Winter FINAL (8 decks)

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