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Pham II > Antidepressants > Flashcards

Antidepressants Flashcards

1
Q

Antidepressants increase which transmitters in the synapse?

A

Serotonin
Norepinephrine
Dopamine

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2
Q

Identify the class for the drugs below:
Fluoxetine (prozac)
Paroxetine (Paxil)
Sertraline (Zoloft)
Fluvoxamine (Luvox)
Citalopram (Celexa)
Escitalopram (Lexapro)

A

SSRI
(selective serotonin re-uptake inhibitors)
They allow serotonin to linger in the synapse longer to reduce anxiety/depression

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3
Q

Identify the class for the drugs listed below:
Vilazodone (Viibryd)
Vortioxetine (Trintellix)
Trazadone
Nefazodone

A

SSRS and Serotonin receptor modulator

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4
Q

SSRI MOA?

A

Blocks/delays the removal of serotonin re-uptake pump AKA (serotonin transporter/SERT)

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5
Q

SSRI metabolized via what system?

A

CYP450 (mainly in the liver)

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6
Q

Common Adverse Side Effects d/t too much serotonin:
Patient has taken fluoxetine and is experiencing diarrhea all day. What receptor is causing this effect?
A. 5-HT3
B. 5-HT4
C. 5-HT2

A

5-HT4 receptor

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7
Q

Which of these drugs can cause the most side effect for diarrhea? Which drug causes the least?
A. Fluoxetine/ Fluvoxamine
B. Paroxetine / Fluvoxamine
C. Sertraline / Fluvoxamine

A

Most: Sertraline
Least: Fluvoxamine

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8
Q

Common Adverse Side Effects d/t too much serotonin:
Patient has taken fluoxetine and is experiencing nausea/vomiting all day. What receptor is causing this effect?
A. 5-HT3
B. 5-HT4
C. 5-HT2

A

5-HT3

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9
Q

Which of these drugs can cause the most side effect for nausea/vomitting? Which causes the least?

A. Fluoxetine/ Fluvoxamine
B. Fluvoxamine/Fluoxetine
C. Paroxetine/ Fluoxetine

A

Most: Fluvoxamine
Least: Fluoxetine

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10
Q

Common Adverse Side Effects d/t too much serotonin:

Patient has taken fluoxetine and is experiencing a headache all day. What receptor might be causing this effect?
A. 5-HT2
B. 5-HT4
C. 5-HT1

A

5-HT1

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11
Q

Which of these drugs can cause the most side effect for headaches? Which causes the least?
A. Fluoxetine/ Fluvoxamine
B. Sertraline/Escitalopram
C. Citalopram/Paroxetine

A

Most: Sertraline
Least: Escitalopram

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12
Q

Common Adverse Side Effects d/t too much serotonin:

Patient has been taking sertraline and has been struggling to sleep at night(somnolence). What receptor might be causing this effect?
A. 5-HT3
B. 5-HT4
C. 5-HT2

A

5-HT2

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13
Q

Which of these drugs can cause the most side effect for somnolence? Which causes the least?

A. Fluvoxamine/Escitalopram
B. Fluoxetine / Sertraline
C. Citalopram/Paroxetine

A

Most: Fluvoxamine
Least: Escitalopram

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14
Q

Sexual dysfunction can also be triggered by which receptor?

A. 5-HT3
B. 5-HT4
C. 5-HT2

A

5-HT2

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15
Q

Which of these drugs can cause the most side effect for sexual dysfunction? Which causes the least?

A. Paroxetine/Citalopram
B. Fluoxetine / Sertraline
C. Citalopram/Paroxetine

A

Most: Paroxetine
Least: Citalopram

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16
Q

Which SSRI medications should you avoid when prescribing for a geriatric patient due to acetylcholine reduction (effects memory)?

A. Sertraline
B. Citalopram
C. Paroxetine

A

Paroxetine

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17
Q

Which SSRI should be avoided in patients with QTc risk?

A. Sertraline
B. Citalopram
C. Paroxetine

A

Citalopram
(Inhibits K channels Ikr/hERG) - dangerous

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18
Q

Which SSRI drug has the longest acting half life, allowing less withdraw symptoms?

A

Fluoxetine
Sertraline

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19
Q

Which SSRI drug has the shortest acting half life, allowing more withdraw symptoms?

A

Fluvoxamine

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20
Q

Metabolic Pathways:
Fluoxetine

A

Norfluoxetine via 2D6*
*active metabolite

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21
Q

Metabolic Pathways:
paroxetine

A

M2 via 2D6

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22
Q

Metabolic Pathways:
Sertraline

A

*Desmethlsertraline via 3A4
(depends a lot on 3A4)

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23
Q

Metabolic Pathways:
Fluvoxamine

A

1A2
2C19

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24
Q

Metabolic Pathways:
Citalopram

A

*Desmethylcitalopram via
2D6
2C19
3A4

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25
Q

Metabolic Pathways:
Escitalopram

A

*S-desmethylcitalopram via
2D6
2C19
3A4

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26
Q

Which 2 SSRI are the most potent and can inhibit/clog up 2D6 pathway?

A

Fluoxetine
Paroxetine

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27
Q

Which drug is given to determine how much the 2D6 pathway is blocked?

A

Desiparamine !
Metabolized by CYP450 2D6

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28
Q

PharmacologyClass:
Vilazodone (Viibryd)

A

Serotonin 1a partial agonist

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29
Q

Identify the class:
Vortioxetine (Trintellix)

A

Serotonin 1a agonist
Serotonin 7 antagonists

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30
Q

Pharmacology/ Drug class:
Trazadone

A

Serotonin reuptake inhibitor
5HT-2 receptor blocker
Potent antihistaminic and alpha1 noradrenergic blocker

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31
Q

Should trazodone be used for depression?

A

No.
Mainly for insomnia d/t 5HT-2 receptor

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32
Q

Drug interaction:
Trazadone

A

Don’t use with proserotonergic drugs
(proserontonergic syndrome)
-fainting

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33
Q

Adverse Effects:
Trazadone

A

Sedation
Dizziness
H/A

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34
Q

Pharmacology/drug class:
Nefazodone

A

SNRI (serotonin & NE reuptake inhibitor)
5HT-2 blocker

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35
Q

Drug interaction:
Nefazodone

A

Don’t use with proserotonergic drugs
(proserontonergic syndrome)
- liver toxicity

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36
Q

Pharmacology/Drug class:
Mirtazapine

A
  • Alpha 2 blocker
    Allows 5HT and NE to constantly be released /not shut down transmitter
  • 5HT2a and c & 5HT-3 antagonists
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37
Q

Drug interaction:
Mirtazipine

A

Don’t use with clonidine!
Serotonin syndrome/HTN

38
Q

Kinetic:
Mirtazipine

A

Uses multiple CYP450 pathways for metabolism
Not an inducer or inhibitor

39
Q

Adverse Effects:
Mirtazipine

A

Somnolence
Xerostomia
Increase appetite (5HT-2C receptor) = avoid in obese pts

40
Q

Identify the class for:

Venlafaxine (Effexor)
Duloxetine (Cymbalta)
Desvenlafaxine ( Pristiq)
Levomilnacipran (Fetzima)

A

SNRI

41
Q

Pharmacology:
Venlafaxine

A

Dose dependent for blocking serotonin, NE, and DA reuptake pumps (Dose at 150 mg will increase NE)

42
Q

Drug interaction:
Venlafaxine

A

Serotonin syndrome
HTN crisis

43
Q

Kinetic:
Venlafaxine

A

Metabolized by CYP 450 2D6

44
Q

Adverse Effects:
Venlafaxine

A

Nausea
H/A
Insomnia

45
Q

What patient population would you mainly prescribe a SNRI for?

A

Major Depression
ADHD

46
Q

What is the name of venlafaxine’s metabolite? (the drug that has already gone through the liver)

A

Desvenlafaxine (Pristiq)

47
Q

Is Venlafaxine and Desvenlafaxine kinetics the same?

A

No.
Desvenlafaxine is not a significant inducer/inhibitor of CYP450 or p-glycoprotein transporter

48
Q

Pharmacology:
Duloxetine

A

SNRI
More potent in serotonin than NE

49
Q

Drug interaction:
Duloxetine

A

Serotonin syndrome
HTN crisis

50
Q

Pharmacology:
Levomilnacipran

A

SNRI
More potent in NE than serotonin

51
Q

When patient population would you prescribe levomilnacipran to?

A

Patients with little depression and neuro epi pain.

52
Q

Drug interaction:
Levomilnacipran

A

Serotonin syndrome
HTN crisis

53
Q

Adverse effects:
Levomilnacipran

A

Nausea
Constipation
H/A
Tachycardia
Sex dysfunction
Urinary hesitation

54
Q

What SNRI requires monitoring vitals when prescribed?

A

Levomilnacipran
- can increase HR by 9bpm
Systolic/Diastolic increase by 2-5mmHg

55
Q

Which agent does not contain any serotonin effect? Bupropion (Wellbutrin)

A

Bupropion (Wellbutrin) - only drug w/o serotonin!
DA and NE reuptake inhibitor

56
Q

Drug interaction:
Bupropion

A
  • Alpha 1 blockers (terazosin)
  • dopamine blockers
57
Q

Adverse effects:
Buproprion

A

Agitation
insomnia
Irritability
Xerostomia
Nausea
Tachycardia

58
Q

Main important adverse effects for Bupropion?

A

Seizures d/t over dosing
Smoking Cessation
Helps with sexual dysfunction

59
Q

What is the recommended dosing for Bupropion IR?

A

150mg TID

60
Q

Recommended dosing for bupropion SR?

A

200mg BID

61
Q

Recommended dosing for bupropion XL?

A

450mg QD

62
Q

Pharmacology:
Dextromethorphan/Buprobion

A

-Mu opiate receptor agonists
- Glutamate receptor antagonists

Inhibits CYP450 2D6 from bupropbrion increasing CNS levels of dextromethorphan

63
Q

Adverse effects:
Dextromethorphan/Buprobion

A

Dizziness
Xerostomia
Nausea
Tachycardia

64
Q

Main important adverse effects forDextromethorphan/Buprobion?

A

Seizures
Abusive drug

65
Q

Identify class/Pharmacology:

Imipramine
Amitriptyline
Desipramine
Nortriptyline
Clomipramine

A

Tricyclic antidepressants (TCAs)
(not recommended/bad drugs)

66
Q

Pharmacology:
TCAs

A

Inhibit serotonin and NE reuptake pump
Sodium channel antagonist (arrythmogenic)

67
Q

Impramine (parent Rx) metabolites into what?

A

Desipramine

68
Q

Amitriptyline (parent Rx) metabolites into what?

A

Nortriptyline

69
Q

Which drug has more 5ht effect then NE?

Nortriptyline
Amitryipline
Despramine
Impramine

A

Parent drugs (Impramine and Amitriptlyine)

70
Q

Which drug has more NE effect then 5HT?

Nortriptyline
Amitryipline
Despramine
Impramine

A

Metabolites (Despiramine & Nortriptyline)

71
Q

Adverse effects:
TCAs

A

Constipation
blurred vision
xerostomia
sedation
H/A
Sex dysfunction

72
Q

More serious adverse effects:
TCAs

A
  • Fatal in overdose (within a week worth of meds)
  • cognitive impairment
  • orthostasis (alpha 1 blocked = vasoconstriction)
  • arrhythmia (Na & K blocked)
73
Q

Drug interactions:
TCAs

A

Serotonin syndrome
Alpha 1 blockers
HTN crisis

74
Q

Kinetics:
TCAs

A

CYP 2D6 & 1A2
(mildly inhibits 2d6)

75
Q

Drug class:
Selegiline Transdermal (safest)

A

Monoamine oxidase Inhibitor (MAOI)
-if see serotonin, DA, NE, it will break it down.

76
Q

High doses of Selegiline patch can cause what?

A

9mg-12mg can cause HTN due to increase GI MO inhibition and increase in tyramine absorption

77
Q

MOA:
Esektamine

A
  1. NMDA glutamate receptor antagonism (glutamate blocker)
  2. NE, 5-HT & DA reuptake inhibitor
  3. 5-HT1b agonist
  4. Mild opiate receptor antagonists
78
Q

What is Esektamine mainly used for?

A

As an add not therapy to antidepressants

79
Q

Name the only FDA approved drug for post partum depression

A

Brexanolone

80
Q

MOA:
Brexanolone

A
  • Acts as an alloprenanolone
    (what out body should make automatically, but decreases after childbirth)
  • Positive GABAa effects (makes GABA stick to more GABAa receptors)
81
Q

How is Brexanolon given?

A

via a 60 hr infusion

82
Q

Adverse effects:
Brexanolon

A

Excessive sedation
Loss of consciousness

83
Q

What receptors causes serotonin syndrome?

A

overstimulation of 5-HT1A and 5-HT2A receptors
- Can cause death from anoxia, aspiration, multiple organ failures

84
Q

What drug would you use if pt is experiencing serotonin syndrome?

A

Cyproheptadine .
Blocks all 15 serotonin receptors (SNRI/SSRI)

85
Q

What class would you use for reducing acute migraines?

A

Triptan class! (used as a rescue drug only)

sumatriptan
naratriptan
zolmitriptan
Eletriptan
Frovatriptan
Razatriptan

86
Q

When is the best time to use a triptan medication?

A

When pts experience a H/A before it develops into a migraine.

87
Q

MOA:
Triptan class

A

Agonists at 5-HT 1B and 1D subtypes

88
Q

Drug interactions:
Triptan class

A

Caution in people taking SSRI and has heart disease.
- can cause vasoconstriction

89
Q

What drug do you prescribe if patient is experiencing chest pain with triptan drugs and SSRI medications?

A

Switch to Lasmiditan. (plan b)

90
Q

Pharmacology:
Lasmiditan

A

5-HT1F receptors agonist
(no vasoconstriction, but lower efficacy yet safer)
Reduces p

91
Q

Pharmacology:
Urogepant & Rimegepant

A

-CGRP releases during a migraine and promotes vasodilation and pain signaling

  • AMY1 recetor antagonists
92
Q

What are the difference between Urogepant & Rimegepant?

A

Ubrogepant - metabolized mainly by CYP4503A4
Rimegepant - excrete primary unchanged (77%)

Pham II (6 decks)

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