Anti-depressants Flashcards
What are the 5 R’s of antidepressant efficacy?
- Response– 50% or better reduction in symptoms from baseline
- Remission– symptom free
- Recovery– 2-6 months of remission (no symptoms)
- Relapse–return of symptoms after remission but before recovery
- Recurrence–return of symptoms after recovery
What are the symptoms of withdrawal from antidepressants?
F- flu like symptoms I- insomnia N- nausea I- imbalance S- sensory disturbances H- hyperarousal
Which antidepressant can also be used for nicotine withdrawal?
bupropion
Which antidepressant can be used for enuresis
imipramine
Which antidepressant can be used for diabetic peripheral neuropathy, fibromyalgia, and chronic msk pain?
duloxetine
Which antidepressant can be used for stress incontinence?
duloxetine
Which SSRI is only used for OCD?
fluvoxamine
MOA SSRI
selectively inhibit the pre-synaptic reuptake of serotonin, via the SERT channel
SSRIs
Citalopram
escitalopram
fluoxetine
paroxetine
vortioxetine–also partial agonist at 5-HT1b & full agonist at 5-HT1a, full antagonist at 5-HT1d3,7
sertaline
vilazodone–also partial agonist at 5-HT1a
SE of SSRIs
sedation or insomnia/agitation/nervousness
sexual dysfunction
weight gain
acute withdrawal reactions
Rare SE of SSRIs, dose dependent
QT prolongation
hyponatremia
serotonin syndrome
suicidality
Symptoms of serotonin syndrome
sweating, hyperreflexia, akathisia/myoclonus, shivering/termors
What are the distinguishing features of serotonin syndrome vs neuroleptic malignant syndrome?
neuroleptic malignant syndrome is caused by dopaminergic agents (antipsychotics)
will have hyporeflexia vs hyper & clonus
will have normal pupils vs dilated
will have normal or decreased bowel sounds vs increased activity
Which SSRI has the most risk of drug-drug interaction
fluoxetine
Which SSRIs has the least risk of drug-drug interaction
vortioxetine & escitalopram
MOA of SNRIs
selectively inhibit the pre-synaptic reuptake of serotonin (SERT) & norepinephrine (NET)
what do tertiary amines TCAs inhibit
TCAs are part of SNRIs
inhibit both NE/5HT relatively equally
What do secondary amines TCAs inhibit
NE>5-HT
list the tertiary amine TCAs
amitriptyline
clomipramine
doxepin
imipramine
list the secondary amine TCAs
amoxapine
desipramine
nortriptyline
list the other SNRIs
desvenlafaxine
duloxetine
venlafaxine
levomilnacipran
What 3 other receptors do TCAs have an effect on
histamine (H1)
muscarinic
a1 adrenergic
What are the 3 key TCA side effects
- cardiovascular (alpha)–tachy, ortho hypotension, dysrhythmias
- anticholinergic (muscarinic)–dry mouth, urinary retention/constipation, blurred vision
- CNS (histamine)–sedation/fatigue, dizziness/seizures
3 Cs of toxic ingestion of TCAs
Coma
Cardiotoxicity (conduction abnormalities)
Convulsions
SE of non-TCA SNRIs
like SSRIs but with less risk of sexual dysfunction
MOA of action of SARAs
2 agents block SERT but also block post-synaptic a1 receptors on noradrenergic neurons & post-synaptic 5-HT2 receptors
–trazadone & nefazodone
1 agent blocks pre-synaptic a2 receptors on noradrenergic & serotonergic neurons & blocks post-synaptic 5-HT2/3 receptors
–miratazapine
SE of SARAs
sedation (most with trazadone/mirtazapine) ortho hypotension (most with trazadone) weight gain (most with mirtazapine)
MOA of NDRIs
selectively inhibits pre-synaptic reuptake of norepinephrine (NET) and dopamine (DAT)
Which SNRI also blocks dopamine
amoxapine
what is the only NDRI called
bupropion
which 2 drugs mess with dopamine
bupropion (NDRI) and amoxapine (SNRI)
SE of NDRIs
agitation/insomnia
seizures (dose dependent, or those at risk)!!
MOA of MAOIs
inhibition of MAO (a and b subtypes) increase levels of monoamines in neuronal vesicles & increase amounts of NE, 5-HT, and DA released
–all are nonselective except selegiline (B selective)
List the MAOIs
isocarboxazidp
phenelzine
selegiline
tranylcypromine
SE of MAOIs
orthostatic hypotension
sexual dysfunction
weight gain
insomnia/agitation/nervousness
Drug interactions of MAOIs
any 5-HT/NE affecting drugs–SSRIs/TCAs/SNRIs, amphetamines, anti-hypertensives
—2 wk washout period (whatever that means)
risk of serotonin syndrome
risk of hypertensive crisis
Risk of hypertensive crisis in MAOIs increased with
increased tyramine in GI tract may induce significant catecholamine release
–least risk with selegiline
tyramine containing foods: aged cheeses soy beans fermented & pickled meats, fish processed, pickled or cured meats tap beer, red wine over-ripe fruits soy/fish/shrimp sauces
s/s of hypertensive crisis
severe headache nausea/vomiting sweating/severe anxiety nosebleeds tachycardia CP changes in vision SOB confusion
MOA & administration of esketamine
NMDA-receptor (glutamate) antagonist
- -indicated for treatment resistant depression in conjunction with ongoing antidepressant therapy
- -nasal admin
- -pt observed for 2 hours post dose
MOA & administration of brexanolone
GABAa receptor positive allosteric modulator
- -indicated for post-partum depression
- -60 hr IV administration
List the anti-seizure agents used as mood stabilizers
carbamazepine
lamotrigine
divalproex/valproic acid
MOA of lithium
neurotransmitter modulation– inhibits dopamine neurotransmission
interferes with both stimulatory & inhibitory G-proteins by keeping them in inactive state
–downregulates NMDA receptor
–increases GABA levels in CSF
–inhibits PKC, MARCKS, GSK-3
SE of lithium
polyuria–looks like nephrogenic diabetes insipidus
–lithium handled by kidneys similar to Na/K, competes with Na for kidney reabsorption
also, tremor, mental confusion/dizziness/sedations. thyroid goiter, leukocytosis, seizures, serotonin syn
Drug interactions of Lithium
diuretics (esp. thiazides)
ACEIs
NSAIDs
Indications for lithium
- -acute & maintenance tx of mania/bipolar I disorder
- -augmentation in unipolar depression
- -Off label: reduced risk of suicide in mood disorders
What is valproic acid/divalproex used for
acute bipolar I (with & w/o psychotic features)
What is lamotrigine used for
maintenance of bipolar I & II
What is Carbamazepine used for
acute & mainenance tx of acute mania & mixed episodes of bipolar I
–CYP450 inducer!
