Week 1 Flashcards
MAOIs
(phenelzine, tranylcypromine, isocarboxazid)
irreversible inhibition of oxdiase
increases 5HT, NE, and DA in synaptic cleft–downregulation
SE: hypertensive crisis with high tyramine diet, delayed effectiveness, serotonin syndrome, sexual dysfunction
*helpful in treatment-resistant depression and anxiety
TCAs
(amitriptyline, amoxapine, clomipramine, desipramine, doxepin, imipramine, maprotiline, nortriptyline, protriptyline)
blocks reuptake of 5HT and NE
*very effective antidepressants
SE: antihistaminergic actions (sedation, weight gain), anticholinergic actions (dry everything), a-1 adrenergic blockage, weak blockade of voltage-sensitive Na channels in heart and brain (prolongation of Q-T interval on EKG)
SSRIs
(fluoxetine, sertraline, paroxetine, fluvoxamine, citalopram, escitalopram, vilazodone)
*drugs of choice for most anxiety disorders
inhibition of 5HT transporter–overtime = downregulation (accounts for therapeutic action and tolerance to side effects because of the flood of serotonergic pathways)
SE: sexual dysfunction, sedation, insomnia, delayed effectiveness, discontinuation syndrome, agitation, myoclonus, akathasia, serotonin syndrome
fluoxetine
SSRI
(Prozac)
antagonist action on 5HT2C receptor = slight increase in disinhibition of NE and DA release
makes this drug an activating SSRI (increased risk of suicide in suicidal patients!)
good for anhedonia, hypersomnia, psychomotor retardation, apathy, fatigue, and poor concentration
*10 day half-life
weekly capsule
sertraline
SSRI
(Zoloft)
weakly inhibits DA transport which slightly increases DA
improves hypersomnia, low energy, and mood reactivity
often paired with bupropion to maximize increase in DA
sigma-1 receptor binding makes it advantageous in psychotic depression
paroxetine
SSRI
(Paxil)
preferred in anxiety patients due to calming, sedating properties (anti-cholinergic effects)
SE: discontinuation withdrawal syndrome, heart effects in fetus if taken during pregnancy!
fluvoxamine
SSRI
(Luvox)
used for treatment of anxiety and OCD
potent at sigma-1 site–may be reason for calming properites and usefulness in psychotic depression
citalopram/escitalopram
SSRI
(Celexa/Lexapro)
citalopram is a racemic mixture of R and S enantiomers–escitalopram contains only the R enantiomer
escitalopram– more effective at lower doses and is the purest SSRI and best tolerated SSRI
–> acts only on serotonin transporters
SE: GI upset for first 3-5 days
vilazodone
SSRI
(Viibryd)
partial agonist at 5HT1A receptor
first line for depression and anxiety
SE: nausea, vomiting, diarrhea, insomnia
**very low weight gain and sexual side effects
SNRIs
increases both 5HT and NE in synergistic way (weak DA increase in prefrontal cortex)
activating drugs
SE: sexual dysfunction
venlafaxine
SNRI
(Effexor)
potency: 5HT > NE
may cause intense discontinuation withdrawal symptoms, HTN
***take this medication on time!
also useful for anxiety, fibromyalgia/chronic pain at higher doses
desvenlafaxine
SNRI
(Pristiq)
5HT>NE activity
may be useful in postmenopausal women with depression; also useful in chronic pain/fibromyalgia
duloxetine
SNRI
(Cymbalta)
both 5HT and NE activity at lower doses
useful in chronic pain/fibromyalgia at higher doses
milnacipran
SNRI
(Savella)
approved for fibromyalgia only in the US
NE>5HT activity
–> higher NE activity may account for improvement in cognition seen in chronic pain patients
levomilnacipran ER
SNRI
(Fetzima)
L enantiomer of milnacipran
NE>5HT activity
SE: GI upset, sweating, insomnia, increased HR and BP
shows significant improvement on Sheehan Disability Scale
