Antidepressants Flashcards
MAO inhibitors
phenelzine
tranylcypromine
selegiline
TCAs
amitriptyline
imipramine
SSRIs
fluoxetine paroxetine sertraline citalopram escitalopram
SNRIs
venlafaxine
duloxetine
serotonin modulators
trazodone
vilazodone
vortioxetine
antidepressants
all work to inc levels of DA, NE, 5HT
all are Na+ channel blockers –> prolonged QRS
all have black box warning of sucidal thinking/behavior
MAO inhibitors
MOA?
Side effects?
inhibition of monoamine oxidase blocks degradation pathway for biogenic amines (DA, NE, 5-HT), thus inhibition increases levels these NTs
side effects: hypertensive crisis if administer w/ sympathomimetics (decongestants) or foods high in tyramine
avoid use w/ other antidepressants
rarely used today
Selegiline
MAO-B selective (DA)
tx: Parkinson’s, smaller doses for depression
black box warning that applies to all antidepressants?
suicidal thinking and behavior
unique to younger patients (adolescents)
MAO-A inhibitors selectively block ___ breakdown
MAO-A inhibitors selectively block NE breakdown
TCAs
MOA?
Side effects?
Primarily blocks re-uptake of NE (and some 5-HT)
side effects:
- some binding to muscarinic ACh receptors (dry mouth/urinary retention/constipation/blurred vision)
- weight gain
- orthostasis
- ECG changes, sexual dysfunction, hematologic abnormalities
anti-histamines also block _______ receptors
anti-histamines also block muscarinic receptors
Dissociation constant (Kd)
measure of post-synaptic receptor affinity
lower Kd –> more tightly bound drug to its receptor
the more seretogenic the drug, more likely side effect of _______________
the more seretogenic the drug, more likely side effect of SEXUAL DYSFUNCTION
TCA overdose tx
- do NOT induce vomiting (–> neuro/hemodynamic deterioration, aspiration)
- use activated charcoal/gastric lavage to bind free drug
If QRS widening…
- alkalinize serum w/ NaHCO3 to dec metabolic acidosis
- may need intubation w/ hyperventilation
SSRIs
MOA?
Side effects?
selectively block pre-synaptic re-uptake of serotonin
side effects:
- NAUSEA
- HA
- sexual dysfunction
- sleep disturbances
- anxiety/restlessness/tremor
other concerns:
- suicide risk
- mania/hypomania
- QT prolongation
- hyponatremia
- serotonin syndrome
- antiplatelet effects
SSRIs metabolism
all undergo extensive HEPATIC metabolism
Serotonin syndrome
vague constellation of sx
autonomic: diaphoresis, shivering, tachycardia, hyperthermia
CNS: agitation, hallucinations, seizure, coma
GI: nausea, vomiting, diarrhea
neuromuscular: weakness, hyperreflexia, myoclonus, incoordination
SNRIs
increase 5-HT and NE by blocking-reupake
bupropion (Wullbutrin)
MOA?
Side effects?
primary blocks re-uptake of DA and some NE
side effects: nausea, tremors, agitation, insomnia
bupropion should be avoided if ______, ______, or _______.
bupropion should be avoided if PSYCHOTIC, AGITATED, or SEIZURES.
bupropion can also used for ______________
smoking cessation
Zyban
mirtazapine (Remeron)
MOA?
Side effects?
Indications?
blocks activity at alpha-2 pre-synaptic receptors –> increases 5HT and NE levels (adding antagonism at other receptors)
side effects: SEDATION, WEIGHT GAIN, orthostasis, dry mouth, agranulocytosis
indications: difficulty sleeping, poor appetite, sexual dysfunction
Consideration during initiation of antidepressants
small doses gradually titrated upwards
Consideration during discontinuation of antidepressants
slowly to prevent withdrawal
HA, nausea, dizziness, insomnia, nervousness
antidepressants to consider using if difficulty sleeping or poor appetite
mirtazapine
paroxetine
antidepressants to consider using if sexual dysfunction
bupropion (lacks ability to elevate serotonin)
mirtazapine
antidepressants to AVOID if h/o cardiovascular disease
TCAs
SNRIs
MAOIs
antidepressants to AVOID if risk for OD
TCAs
antidepressants to AVOID if h/o seizures
buproprion
esketamine
NEW
NMDA receptor agonist
nasal spray for tx-resistant depression
in-office only
CNS, GI, CV side effects
brexanolone
NEW
allopregnanolone analogue (steroid hormone inc during pregnancy)
IV infusion for post-partum depression, 60hr tx
mainly CNS side effects (GABA agonist)
