Antidepressants Flashcards
SSRIs
SNRIs
Atypical
Tricyclic
Escitalopram, fluoxetinem sertraline
Duloxetine, venlafaxine
Bupropion, mirtazapine
Amittriptyline, nortrip
Antidepressants vs mood stabilizers
Antidepressants for MD
Mood for BPD
Monoamine hypothesis
Depression causedb y monoamine deficiency
Diminished serotinin, adrenergic, dopaminerigc NT
SSRIs
SNRIs
Atypical
TCAs
effect on monoamines and onset
Serotonin
Serotonin and NE
Individual effects on serotonin, NE, or dopamine
Serotonin and NE
Onset make take several weeks so MOA could be more complicated
Most to least specific
SSRIs
SNRIs
Atypical
TCAs
Incidence and variety of adverse effects increase as you move to TCAs
Options for resistant depression
MOno
comb
Increase dose Switch to different class or same class
Careful use from two classes
Augmenting drug
Augmenting drugs
Apriprazole is most common
Lithium
Most are known to increase synthesis/release of monoamines
Use of SSRIs in depression
Usually drug of choice due to low incidence of side effects
Long delay for effects to occur (6-8 weeks)
SSRIs MOA
Main receptor is SERT, presynaptic transporter which removes 5HT from synaptic cleft
Additional targets could also enhance on pre and post membrane
BDNF effect
Increase serotonin means increase in BDNF means increase neuronal growth and synapse formation means reorganzation
In hippocampus
What is unique about escitalpram, sertraline and fluoxetine
Escitalopram is most specific
Sertraline is also weak inhibitor of dpoamine reuptake in addition to being an SSRI
FLu blocks NE reuptake and 5HT2C receptors in addition to SSRI
Discontinuation syndrome
GI symptoms, need to taper dose
Fluoxetine is best for this because long lived active mtabolite
SSRIs with CYP450 interactions
Fluoxetine and Sertraline
Serotonin syndrome
Basically all antidepressants except for bupropion and atypicals
Early - NM probs, cog probs, temp control
Late - Tonic-clonic convulsions
Any drugs that increase sertoonin
Adverse effects of SSRIs
Nausea, GI, cramping
Activating/insominia
Anorgasmia
Anti-platelet effect
SSRIs and pregnancy and black box
Paroxetine is only one
Postnatal adaptation syndrome and pulmonary hypertension risk
Pediatric suicidality below 24
Venlafaxine special
NE reuptake inhibition is lower so it behaves more like SSRI at low doses
SNRIs vs SSRIs and adverse effects
More widely used in chronic pain disorders
Sexual adverse effects
Discontinuation symptoms
Nausea/GI cramping all from serotonergic…more with venlafaxine
Hypertension from noradrenergic effect
Bupropion unique, interaction, contraindcation
NE reuptaker inhibitor and Dopamine reuptake inhibitor
NO serotonin effects so no sexual/GI
Enhanced noradrenergic and dopaminergic transmission
CYP2D6
Lowers seizrue threshold so no in epilepshy
MIrtazapine mech
Blocks presynaptic alpha 2 adrenergic inhibitory receptors to increase CNS noradrenergic and seroteonergic activity
H1 histaminergic blocker for sedation and increased appetite
LIttle 5-HT uptake inhibition so decreased SSRI like adverse effects
Sturctures of TCA s
Nortriptyline is active mtabolite of amitriptyline
Antidepressant mechansim of action for antidepressant
serotonin reuptake and NE reuptake blocker s
Secondayr vs teriatry amines
Secondary affect NE more than 5-HT
Teritary more balanced
TCA other uses and overdosage
Neuropathic pain
INitial excitatory phase…subsequant depressant phase…cardiac arrythmias
Suicide prevention needs to be considers
TCA adverse effects
Anti-histaminergic (sedation)
Anti-muscarinic
Anti-adrenergic (orthostatic hypotension)
Cardiac toxocity (Na blcok)
What should you start on?
What should be used for tx resistant or refractory
SSRI, SNRI, bupropion, mirtazpine
TCAs and MAOIs
What to avoid in
HTN
Cardaic
Obesity
Chronic pain
SNRIs, TCAs
TCAs
SSRIs/SNRIs/Buproprion usually preferred…avoid mirtazapine/TCAs
Tx with SNRIs or TCAs