Depression Flashcards
What the 5 most popular SSRIs
Citalopram (celesta) Escitalopram (lexapro) Fluoxetine (Prozac) Sertraline (Zoloft) Paroxetine (Paxil)
Which is the worse SSRI?
Paroxetine
What is the mechanism of SSRIs? How much activity inhibited at clinical doses? Why isn’t effect immediate?
Allosteric 5-HT inhibition.
80% inhibited
Clinical effect probably from overtime desensitization and down regulation of 5HT R’s
SSRIs have little affinity for ___, ____, or ____ receptors. Except for _____
histamine, α, or muscarinic
paroxetine (hits hist and muscarinic)
Fluoxetine is FDA approved for _____
bulimia
_______ is an SSRI that is safe to use in patients with CV disease
sertraline
SAD-HART trial
How long do Adverse effects from SSRIs last
1-2 weeks
What are some adverse effects from SSRIs
Nausea, GI upset, diarrhea (increase 5ht stimulation everywhere)
Headaches, insomnia
Sexual dysfunction
Paroxetine inhibits ________ which leads to even more sexual dysfunction than other SSRIs might cause
nitric oxide synthase
An AE of SSRIs that’s a concern for geriatric patients is ____________ due to __________
syndrome of inappropriate antidiuretic hormone secretion/hyponatremia
stimulation of arginine vasopressin from posterior pituitary
Paroxetine specifically has adverse effects of
increased weight gain, sexual dysfunction, sedation, anticholinergic adverse effects
Citalopram has the specific adverse effect _______.
What is the max dose that can be used in adults vs geriatrics?
What drug drug interaction does someone NEED to look for?
QTc prolongation 40mg adults, 20mg geriatrics CYP2C19 inhibitors (omeprazole PPI-> max 20mg)
Are SSRIs fatal in overdose?
no
What can happen if someone suddenly discontinues their SSRI?
dreams, paresthesias, flu like symptoms,
paroxetine specific-> cholinergic rebound
Which SSRI has a lower risk of withdrawal symptoms and why?
fluoxetine bc long half life and active metabolite
Which SSRIs are potent inhibitors of CYP2D6?
fluoxetine and paroxetine
What’s the deal with NSAIDs and SSRIs?
SSRIs prevent 5ht from being taken up into platelets and released for aggregation-> increase GI bleed risk
Some groups of things that might cause serotonin syndrome?
MAOIs, linezolid, triptans, tramadol
What are 4 commonly used SNRIs?
Venlafaxine (Effexor)
Duloxetine (Cymbalta)
Desvenlafaxine (Pristiq) (metabolite of venlafaxine)
levomilnacipran (fetzima)
What is the MOA for SNRIs?
inhibit 5ht and NE reuptake transporters
What is special about the MOA of Venlafaxine? (what dose do you need)
weak inhibitor of NE reuptake due to low affinity
Need dose greater than 150mg for SNRI. otherwise its just an SSRI
What is special about duloxetine MOA?
inhibits 5ht and NE at low doses
Do SNRIs have affinity for histamine, α, or muscarinic receptors?
not really
SNRIs are useful in depression with _____ because ______
lethargy
increase in NE
SNRIs can also be used in _______
anxiety, peripheral neuropathy, fibromyalgia
What are NE related AEs from SNRIs?
increased BP, HR, sweating
caution in patients with CV disease
What is the MOA of bupropion?
Inhibition of NE and DA. no effect at 5HT, muscarinic, α, or histamine
Bupropion can be used with another antidepressant for __________ and _______
anhedonia, low mood
decreased sexual dysfunction compared to other antidepressants
________ is the antidepressant of choice for depression with lethargy, lack of energy, sexual dysfunction and low mood
Bupropion
also helpful in smoking cessation, ADHD, and weight loss
Bupropion is not good when depression is comorbid with ____, _____, or _____
anxiety, irritability, insomnia
Bupropion _______ at really high doses. Where should you exhibit caution?
lower seizure threshold. Eds, epilepsy, alcoholism, CNS tumor
What are some adverse effects of bupropion?
nausea, agitation, tremor, insomnia, decreased appetite
What is the mechanism of action for MIrtazapine (remeron)
Antagonist at presynaptic auto and hetero α 2 and 5ht receptors -> increase release NE and 5HT
NOT an reuptake inhibitor
What is Mirtazapine an antagonist at?
5ht2a, 5ht2c, 5ht3
Histamine 1 (good for insomnia)
no activity at α 1 or muscarinic
Miratazapine will have an _____ in sexual dysfunction vs other antidepressants, useful in depression with __________
decrease
insomnia, weight loss, anxiety, N/V, failure to thrive
Do not use Mirtazapine in depression with __________
sedation, hypersonic, weight gain
What is the mechanism of tricyclic antidepressants?
Inhibit 5ht and NE reuptake transporters
high affinity for histamine, α 1, or muscarinic
When would you whip out the tricyclic antidepressants?
later stage. its as effective but less tolerated becasue more AEs and DDIs
Are tricyclic antidepressants lethal in overdose? if so, how?
Yes
Inhibit Na channels->longer ventricular depolarization->QRS widen->arrhythmia
Treat with sodium bicarb (displaces TCA)
What are TCA specific AEs and what population should they be avoided using in
anticholinergic (dry mouth, blurry vision, urinary retention, constipation)
avoid in geriatric patients
What is the dietary restriction for MAO-Is?
don’t eat tyramine rich foods -> increase in peripheral NE -> hypertensive crisis.
Are MAO I’s fatal in OD?
yes
What is esketamine used for?
treatment resistant depression, rapid antisuicidal properties
What is brexanolone used for?
treatment for post partum depression
