Antidepressants Flashcards
Antidepressants increase which transmitters in the synapse?
Serotonin
Norepinephrine
Dopamine
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
Identify the class for the drugs listed below:
Vilazodone (Viibryd)
Vortioxetine (Trintellix)
Trazadone
Nefazodone
SSRS and Serotonin receptor modulator
SSRI MOA?
Blocks/delays the removal of serotonin re-uptake pump AKA (serotonin transporter/SERT)
SSRI metabolized via what system?
CYP450 (mainly in the liver)
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
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
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
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
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
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
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
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
Sexual dysfunction can also be triggered by which receptor?
A. 5-HT3
B. 5-HT4
C. 5-HT2
5-HT2
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
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
Which SSRI should be avoided in patients with QTc risk?
A. Sertraline
B. Citalopram
C. Paroxetine
Citalopram
(Inhibits K channels Ikr/hERG) - dangerous
Which SSRI drug has the longest acting half life, allowing less withdraw symptoms?
Fluoxetine
Sertraline
Which SSRI drug has the shortest acting half life, allowing more withdraw symptoms?
Fluvoxamine
Metabolic Pathways:
Fluoxetine
Norfluoxetine via 2D6*
*active metabolite
Metabolic Pathways:
paroxetine
M2 via 2D6
Metabolic Pathways:
Sertraline
*Desmethlsertraline via 3A4
(depends a lot on 3A4)
Metabolic Pathways:
Fluvoxamine
1A2
2C19
Metabolic Pathways:
Citalopram
*Desmethylcitalopram via
2D6
2C19
3A4
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
- NMDA glutamate receptor antagonism (glutamate blocker)
- NE, 5-HT & DA reuptake inhibitor
- 5-HT1b agonist
- 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%)
