anti-depressants Flashcards
TCAs are nonselective ___ reuptake inhibitors
NE, 5-HT
which antidepressant has NO P450 interactions
venlafaxine
class: Selegiline
o Isocarboxazid
o Tranylcypromine
o Phenelzine (off the market)
* LINEZOLID (abx)
non-selective MAOIs
MAOI washout period
2 weeks for most (before starting another antidepressant class). fluoxetine is 6 wks
AEs:
o Orthostatic hypotension, dizziness
o HA
o Insomnia
o Weight gain (phenelzine)
o Sexual side effects (lower w/ selegiline)
MAOIs
MOA: inhibit NE and 5-HT reuptake into presynaptic nerve terminals, block NE/5-HT transporter sites
o Increase monoamine levels rapidly
o Also antihistamine, anti-alpha adrenergic, anticholinergic, anti-cardiac Na/K channel effects
TCAs
which has more SEs: secondary or tertiary amines
tertiary
class: Nortriptyline, Desipramine
secondary amine TCAs
AEs:
o H1 receptor blockade = drowsiness, sedation, impaired mental function, weight gain
o A1 receptor blockade = orthostatic hypotension, reflex tachycardia
o Anticholinergic AEs
o Glaucoma
o Elevated NE = tachycardia, seizures, hyperthermia
o Na/K: QT prolongation, TdP, seizures
o Most likely to see overdose with this class
§ Especially tertiary amines
o BBW: suicidality
TCAs
TCA DIs
MAOIs = cardiotoxicity
§ Anticholinergics = enhanced anticholinergic side effects
§ CNS Depressants = enhanced sedation
TCAs as monotherapy for depression?
no
MOA: selectively blocks 5-HT reuptake by inhibiting transporter on pre-synaptic neurons
o Increases amount of active and available serotonin in synaptic cleft
o No therapeutic action at NE reuptake transporter or other receptor sites
o Increases monoamine levels fairly rapidly
SSRIs
AEs:
o Common: drowsiness, HA, nausea, sexual dysfunction, insomnia, dizziness, agitation, weight
gain (paroxetine worst)
o Serious:
§ Serotonin syndrome, suicidality, glaucoma, seizures
§ QT prolongation, TdP (citalopram/escitalopram)
SSRIs
worst SSRI for weight gain
paroxetine
least problematic SSRI for weight gain
fluoxetine
SSRI cautions
Other medications that elevate serotonin: Most other antidepressants, St. John’s Wort, sumatriptan
o Avoid abrupt withdrawal
o Pts <25 y/o, elderly (need to monitor Na), pregnant
avoid alcohol
poss increased risk for bleeding
can cause manic episode in bipolar
SSRI w/ the most CYP2D6 activity
fluoxetine
serotonin syndrome antidote
cyproheptadine
cymbalta CI
hepatic and renal dysfunction
cymbalta caution
Moderate CYP2D6 inhibitor - this can diminish response to opioids
AEs:
o Common: NAUSEA, HA, sexual dysfunction, insomnia, dizziness, agitation, weight loss
§ Can HR and BP
o GI intolerance w/ duloxetine
o Serotonin syndrome, suicidality, glaucoma, seizures
moderately common: decreased libido, ED, delayed ejaculation, anorgasmia
rare: bleeding, hyponatremia, bone resorption
some anticholinergic effects w/ Effexor
SNRIs
SNRIs cautions
CIs/Cautions
o Other meds elevating 5HT/NE
o Avoid abrupt withdrawal
o CV dz or seizure hx
o Patients <25 y/o, elderly, pregnant
MOA: Weak DA and NE reuptake inhibitor, greater effect on dopamine, weak antagonism of nicotinic receptors
bupropion
AEs:
§ Restlessness, tremors, insomnia, lowers seizure threshold, , dry mouth (in 21%), increased anxiety, nausea, agitation, dyspepsia
bupropion
bupropion CIs
CIs:
§ Seizure hx, bulimia, recent MAOI use, abrupt alcohol or BZ discontinuation
MOA: Antagonizes 5-HT2, 5-HT3 receptors, high affinity for H1 receptors causing sedation
mirtazapine
AEs:
§ Sedation
§ Weight gain (increased appetite), xerostomia
mirtazapine
MOA: 5-HT antagonist, weak inhibition of SERT, a2/H2 antagonists
trazodone
AEs:
§ SOMNOLENCE, HA, xerostomia, dizziness
§ Orthostatic hypotension
§ Syncope
§ Sexual dysfunction
§ Priapism
§ Suicidality
§ Serotonin syndrome, QT prolongation, TdP
trazodone
trazodone CI
§ Cardiovascular dz history
§ <25, elderly, pregnant
class: Nefazodone, Vilazodone, Vortioxetine
atypical antidepressants
