Antidepressants Flashcards by Kirsten Ho

Antidepressants increase which transmitters in the synapse?

Serotonin
Norepinephrine
Dopamine

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

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

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

SSRS and Serotonin receptor modulator

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SSRI MOA?

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

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SSRI metabolized via what system?

CYP450 (mainly in the liver)

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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

5-HT4 receptor

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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

Most: Sertraline
Least: Fluvoxamine

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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

5-HT3

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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

Most: Fluvoxamine
Least: Fluoxetine

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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

5-HT1

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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

Most: Sertraline
Least: Escitalopram

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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

5-HT2

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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

Most: Fluvoxamine
Least: Escitalopram

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Sexual dysfunction can also be triggered by which receptor?

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

5-HT2

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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

Most: Paroxetine
Least: Citalopram

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

A. Sertraline
B. Citalopram
C. Paroxetine

Paroxetine

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Which SSRI should be avoided in patients with QTc risk?

A. Sertraline
B. Citalopram
C. Paroxetine

Citalopram
(Inhibits K channels Ikr/hERG) - dangerous

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

Fluoxetine
Sertraline

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

Fluvoxamine

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Metabolic Pathways:
Fluoxetine

Norfluoxetine via 2D6*
*active metabolite

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Metabolic Pathways:
paroxetine

M2 via 2D6

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Metabolic Pathways:
Sertraline

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

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Metabolic Pathways:
Fluvoxamine

1A2
2C19

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Metabolic Pathways:
Citalopram

*Desmethylcitalopram via
2D6
2C19
3A4

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Metabolic Pathways: Escitalopram

*S-desmethylcitalopram via 2D6 2C19 3A4

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

Fluoxetine Paroxetine

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

Desiparamine ! Metabolized by CYP450 2D6

PharmacologyClass: Vilazodone (Viibryd)

Serotonin 1a partial agonist

Identify the class: Vortioxetine (Trintellix)

Serotonin 1a agonist Serotonin 7 antagonists

Pharmacology/ Drug class: Trazadone

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

Should trazodone be used for depression?

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

Drug interaction: Trazadone

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

Adverse Effects: Trazadone

Sedation Dizziness H/A

Pharmacology/drug class: Nefazodone

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

Drug interaction: Nefazodone

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

Pharmacology/Drug class: Mirtazapine

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

Drug interaction: Mirtazipine

Don't use with clonidine! Serotonin syndrome/HTN

Kinetic: Mirtazipine

Uses multiple CYP450 pathways for metabolism Not an inducer or inhibitor

Adverse Effects: Mirtazipine

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

Identify the class for: Venlafaxine (Effexor) Duloxetine (Cymbalta) Desvenlafaxine ( Pristiq) Levomilnacipran (Fetzima)

SNRI

Pharmacology: Venlafaxine

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

Drug interaction: Venlafaxine

Serotonin syndrome HTN crisis

Kinetic: Venlafaxine

Metabolized by CYP 450 2D6

Adverse Effects: Venlafaxine

Nausea H/A Insomnia

What patient population would you mainly prescribe a SNRI for?

Major Depression ADHD

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

Desvenlafaxine (Pristiq)

Is Venlafaxine and Desvenlafaxine kinetics the same?

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

Pharmacology: Duloxetine

SNRI More potent in serotonin than NE

Drug interaction: Duloxetine

Serotonin syndrome HTN crisis

Pharmacology: Levomilnacipran

SNRI More potent in NE than serotonin

When patient population would you prescribe levomilnacipran to?

Patients with little depression and neuro epi pain.

Drug interaction: Levomilnacipran

Serotonin syndrome HTN crisis

Adverse effects: Levomilnacipran

Nausea Constipation H/A Tachycardia Sex dysfunction Urinary hesitation

What SNRI requires monitoring vitals when prescribed?

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

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

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

Drug interaction: Bupropion

- Alpha 1 blockers (terazosin) - dopamine blockers

Adverse effects: Buproprion

Agitation insomnia Irritability Xerostomia Nausea Tachycardia

Main important adverse effects for Bupropion?

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

What is the recommended dosing for Bupropion IR?

150mg TID

Recommended dosing for bupropion SR?

200mg BID

Recommended dosing for bupropion XL?

450mg QD

Pharmacology: Dextromethorphan/Buprobion

-Mu opiate receptor agonists - Glutamate receptor antagonists Inhibits CYP450 2D6 from bupropbrion increasing CNS levels of dextromethorphan

Adverse effects: Dextromethorphan/Buprobion

Dizziness Xerostomia Nausea Tachycardia

Main important adverse effects forDextromethorphan/Buprobion?

Seizures Abusive drug

Identify class/Pharmacology: Imipramine Amitriptyline Desipramine Nortriptyline Clomipramine

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

Pharmacology: TCAs

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

Impramine (parent Rx) metabolites into what?

Desipramine

Amitriptyline (parent Rx) metabolites into what?

Nortriptyline

Which drug has more 5ht effect then NE? Nortriptyline Amitryipline Despramine Impramine

Parent drugs (Impramine and Amitriptlyine)

Which drug has more NE effect then 5HT? Nortriptyline Amitryipline Despramine Impramine

Metabolites (Despiramine & Nortriptyline)

Adverse effects: TCAs

Constipation blurred vision xerostomia sedation H/A Sex dysfunction

More serious adverse effects: TCAs

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

Drug interactions: TCAs

Serotonin syndrome Alpha 1 blockers HTN crisis

Kinetics: TCAs

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

Drug class: Selegiline Transdermal (safest)

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

High doses of Selegiline patch can cause what?

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

MOA: Esektamine

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

What is Esektamine mainly used for?

As an add not therapy to antidepressants

Name the only FDA approved drug for post partum depression

Brexanolone

MOA: Brexanolone

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

How is Brexanolon given?

via a 60 hr infusion

Adverse effects: Brexanolon

Excessive sedation Loss of consciousness

What receptors causes serotonin syndrome?

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

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

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

What class would you use for reducing acute migraines?

Triptan class! (used as a rescue drug only) sumatriptan naratriptan zolmitriptan Eletriptan Frovatriptan Razatriptan

When is the best time to use a triptan medication?

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

MOA: Triptan class

Agonists at 5-HT 1B and 1D subtypes

Drug interactions: Triptan class

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

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

Switch to Lasmiditan. (plan b)

Pharmacology: Lasmiditan

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

Pharmacology: Urogepant & Rimegepant

-CGRP releases during a migraine and promotes vasodilation and pain signaling - AMY1 recetor antagonists

What are the difference between Urogepant & Rimegepant?

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

Antidepressants Flashcards

(92 cards)