Antidepressants - Linger Flashcards
citalopram
SSRI
escitalopram
SSRI
fluoxetine
SSRI
fluvoxamine
SSRI
paroxetine
SSRI
sertraline
SSRI
duloxetine
SNRI
venlafaxine
SNRI
amitriptyline
TCA
desipramine
TCA
imipramine
TCA
nortriptyline
TCA
trazodone
5-HT2 antagonist
bupropion
tetracyclinc/unicyclic
mertazapine
tetracyclic/unicyclic
selegiline
MAOI
antidepressants
affect serotonin, NE, or both
reserpine
decreases biogenic amines
blocks vesicular uptake of monoamines
neurotrophic factor
BDNF
-growth factor -neurogenesis
involved mood and depression disorders
fluoxetine
long t-1/2
selegiline
transdermal and sublingual forms
-decrease food interactions
SSRI MOA
inhibit serotonin transporter - SERT
increased serotonin at synaptic cleft
80% blocked - therapeutic dosage
possible chronic adapatation to SSRIs
downregulation of postsynaptic 5-HT2 receptor density
SNRI MOA
inhibit SERT and NET
higher affinity of SERT than NET
TCA MOA
inhibit SERT and NET
different TCAs - different affinities for SERT and NET
TCA
also have high affinity - adrenergic, cholinergic, histmaine receptors
-more side effects
trazodone
5-HT2 antagonist
nefazodone
5-HT2 antagonist
counterintuitive why they work
suicide patients
more 5-HT2 receptors - overdensity
may be involved in path of depression
bupropion MOA
selective inhibitor of DAT - dopamine transporter
stimulate presynaptic release of NE and DA
no effect on serotonin
MAOI MOA
mitochondrial enzyme - MAO - metabolize monoamines to inactive metabolites
MAO-A - NE and 5-HT
cause accumulation of NE, 5-HT, DA in vesicles of nerve endings
tyramineselegiline MOA
metabolized by MAO-A and MAO-B
with MAOI - can get accumulation - not goodselective irreversible MAO-B inhibitor (low dose
and nonselective MAO-A/B inhibitor - high dose (refractory depression)
1-2 months
until max benefit of antidepressants
adequate response achieved - recommend minimum 6-12 months of tx
85% patients with major depressive disorder
have at least one recurrence in lifetime
> 2 MDD episodes in 5 years, or >3 episodes lifetime
long-term maintenance anti-depressant therapy
tx of anxiety disorders
many SSRI and SNRIs approved
antidepressants vs. benzos for anxiety
antidepressants - slower acting, but no risk of dependence
OCD tx
respond to serotonergic agents
fluoxetine, fluvoxamine, paroxetine, clomipramine
premenstrual dysphoric disorder tx
SSRIs - fluoxetine and sertraline
smoking cessation tx
bupropion
reduce urge to smoke
eating disorder tx
antidepressants
-tx of bulimia, not nervosa
insomnia tx
amitriptyline and trazodone
depression related insomia
HA tx
SSRIs less effective than TCA in chronic tension HAs
tx pruritis
TCA - antihistamine
finding right antidepressant for patient
empiric - trial and error
first line tx MDD and anxiety
SSRI
less cardiotoxic with OD
fewer antimuscarinic properties
pt cannot tolerate sexual dysfunction
bupropion
bupropion and mirtazapine
common combined with other antidepressants - augment therapeutic response
TCA and MAOI
lethal in OD
patient under age 25
increased suicidality with all antidepressants
but untreated depression - even more risk of suicide
adverse SSRIs
minor sedation and antimuscarinic
GI - N/V, upset stomach, constipation
diminished sexual function - loss libido, delayed organism
HA, insomnia, hypersomnia, weight gain
discontinuation syndrome
of SSRIs
dizzy and paresthesia
withdraw agents with short half lives - paroxetine and sertraline
short half life SSRI
paroxetine and sertraline
withdraw - discontinuation syndrome
CI of SSRI
active manic episode
paroxetine CI in pregnant
CI in pregnant
SSRI paroxetine
SNRI ADRs
insomnia, anxiety, agitation
elevated BP and HR
increased risk of bleeding
venlafaxine
antiplatelet aggregation effect
more cardiac toxicity in OD as well
TCA ADRs
anticholinergic - drowsy, dry mouth, constipation, urinary retention, blurry vision, confusion
orthostatic hypotension (a-adrenergic block)
weight gain - H1 histamine antagonist
cardiotoxicity, arrhythmia, convulsion, hepatic dysfxn, hyponatremia
sexual dysfunction
imipramine and amitriptyline
significant antimuscarinic and cardiac side effects
CI for TCA
arrhythmia, recent MI, liver disease, glaucoma, mania
5-HT2 antagonist ADRs
sedation and GI issues
sexual dysfxn - uncommon
orthostatic hypotension
black box warning for hepatotoxicity
nefazodone 5-HT2 antagonist
agitation, anorexia, insomnia
wuth bupropion
no sexual side effects
mirtazapine and bupropion
tyramine food
avoid if taking MAOIs
overdose
TCA - most toxic - arrhythmia, altered mental status, seizure
also - MAOIs - potentially lethal - autonomic instability, hyperadrenergic symptoms, psychotic symptoms, confusion, delirium, fever, seizures
st johns wort
herbal tx of depression
inducer of CYP450
serotonin syndrome
interaction of MAOI with SSRI, SNRI, TCA, and some analgesics
overstiumation of 5-HT receptors
delirium, agitation, coma, HTN, tachy, hyperthermia, diaphoreses, myoclonus, hyperreflexia, tremor
serotonin syndrome
pt switched from SSRI to MAOI
therapy discontinued for at least 2 weeks - prior to initiation of new therapy - risk of serotonin syndrome
tx of serotonin syndrome
withdrawal offending drug - sedate -benzos
intubate, ventilate
5-HT2 block - with cyproheptadine or chlorpromazine
tyramine foods
chocolate, meat, pickled, aged, cheeses, alcoholi
metabolized by MAO
if take MAOI - reduce metabolism - get catecholamine release - rise in HR and BP
attention, motivation, pleasure, reward
dopamine
alertness, energy
NE
obsession/compulsion
serotonin
bupropion
DA selective - low potency
more effective antidepressant therapy
combined with psychotherapy
inhibit neuronal 5-HT reuptake - little effect on DA and NE
SSRIs
bad interaction with alcohol
SSRI
cardiotoxicity
venlafaxine
tx smoking cessation
bupropion
ADR with therapeutic TCA
antimuscarinic effect
arrhythmia and seizure - if OD
three Cs of TCA overdose
coma, cardiotoxicity, convulsions
tx enuresis
TCAs
tx premature ejaculation
SSRIs
tx bulimia nervosa
fluoxetine - and other SSRIs