Antidepressants Flashcards
what are the MAOI inhibitors
MAO Take Pride In Shanghai
Tranylcypromine (non hydrazine)
Phenelzine (hydrazine)
Isocarboxazid (hydrazine)
Selegiline (non hydrazine)
mechanism of MAO inhibitors (name them)
tranylcypromine, phenelzine, isocarboxazid, selegiline
- prevent the breakdown of serotonin, dopamine, norepinephrine
- PIT bind irreversibly and nonselectively to MAO-A and MAO-B
- Selegiline binds to MAO-B
use of MAOI
- depression unresponsive to other antidepressants
- Selegiline for early Parkinson’s
AE of MAOI
tranylcypromine, phenelzine, isocarboxazid, selegiline
drowsiness, insomnia, orthostatic hypotension, weight gain, muscle pain, sexual dysfunction
contraindication of MAOI (name them)
tranylcypromine, phenelzine, isocarbaxozid, selegiline
- serotonin agents: SSRI, SNRIs, or TCAs –> serotonin syndrome due to excess stimulation –> hyperthermia, muscle rigidity, myoclonus, rapid changes in mental status and vitals (so they must be stopped 2 weeks before administering MAOIs)
- tyramine containing food such as aged wine and cheese: they are broken down by MAO –> large release of catecholamines –> hypertension, tachycardia, arrhythmias, headache, stiff neck
- sympathomimetic drugs: pseudoephedrine and phenylpropanolamine (both in cold meds)
what is used to control or manage tyramine induce hypertension
Phentolamine
Prazosin
what happens if overdose on MAOI
tranylcypromine, phenelzine, isocarboxazid, selegeline
autonomic instability, hyperadrenergic symptoms, psychotic symptoms, confusion, delirium, fever
what happens with discontinuation of MAOI
discontinuation syndrome (seen with all antidepressants) –> worsening of depressive symptoms, confusion, disorientation, psychosis, anxiety
what are the TCAs
DANI and CAM
Desipramine
Amitriptyline
Nortriptyline
Imipramine
Clomipramine
Amoxapine
Maprotiline
mechanism of action of TCAs (name them)
desipramine, amitripyline, nortriptyline, imipramine, clomipramine, amoxapine, maprotiline
blocks reuptake of serotonin and NE by competitively binding their carrier protein –> increased monoamine in the cleft
block alpha adrenergic, muscarinic, histamine, and cardiac fast Na channels
AE of TCAs (name them)
desipramine, amitriptyline, nortriptyline, imipramine, clomipramine, amoxapaine, maprotiline
- block muscarinic receptors –> blurred vision, xerostomia, urinary retention, constipation, narrow angle glaucoma
- increase catecholamine receptors –> increased cardiac stimulation
- inhibit cardiac fast Na channel –> arrhythmias
- block alpha 1 receptor: orthostatic hypotension with rebound tachycardia
- H1 blocker: sedation and weight gain
- sexual effects
what metabolizes TCAs and how does it affect the population
CYP2D6 so those (esp whites) with polymorphism are associated with slow metabolism of TCAs
what occurs with overdose of TCAs
lethal arrhythmias –> v-tach and v-fib
what reverses the cardiac block caused by overdose of TCAs
sodium bicarbonate
what are the SSRIs
SEP of FFC
Sertraline Escitalopram Paroxetine Fluoxetine Fluvoxamine Citalopram
mechanism of SSRIs (name them)
Sertraline, Escitalopram, Paroxetine, Fluoxetine, Fluvoxamine, Citalopram
- inhibit the reuptake of serotonin
- unlike TCAs, they have little blocking activity at muscaranic, histamine H1, and alpha adrenergic receptors
SSRIs are first line treatment for what conditions
Depression and Premature Ejaculation
SSRIs because of few sider effects
SEP of FFC Sertraline Escitalopram (S enantiomer of Citalopram) Paroxetine Fluoxetine Fluvoxamine Citalopram
what else are SSRIs used for
OCD, panic disorder, generalized anxiety disorder, PTSD, Social anxiety disorder, premenstrual dysphoric disorder, bulimia nervosa
AE of SSRIs (name them)
sertraline, escitalopram, paroxetine, fluoxetine, fluvoxamine, citralopram
Increased serotonergic activity in the gut
Diminished sexual interest and function
Weight gain
drug interaction of SSRIs
- Fluoxetine and Paroxetine are inhibitors of CYP2D6 needed for metabolism of TCAs
- Fluvoxamine is inhibitor of CYP1A2, CYP2C19, and CYP3A4
- Serotonin Syndrome
what occurs with overdose of SSRIs
seizures
what are the SNRIs
Venlafaxine
Duloxetine
mechanism of SNRIs (name them)
Venlafaxine and Duloxetine
inhibit the reuptake of serotonin and NE but differ from TCAs in that they do not block the muscarinic, H1, and alpha adrenergic 1 receptors
which of the SNRIs behaves like an SSRI and why
Venlafaxine at low doses only inhibits uptake of serotonin but at high doses also inhibits uptake of NE
adverse of SNRIs
dry mouth, constipation, decreased appetite, fatigue, somnolence, sweating, asthenia, dizziness, sexual dysfunction
name and mechanism of NDRI
Bupropion
norepinephrine and dopamine reuptake inhibitor
use of NDRI
bupropion
decrease the craving and attenuating the withdrawal symptoms of nicotine in tobacco users
overdose and contraindication of bupropion
seizures
name and mechanism of SARIs
5HT2 (serotonin) antagonist and 5-HT reuptake inhibitor
Nefazodone
Trazodone
use of SARIs
nefazodone and trazodone
- since 5-HT2 is inhibited –> no agitation, anxiety, or sexual dysfunction
- actions of 5-HT with blockade of 5-HT2 –> antidepressive, antianxiety, antipsychotic
AE of nefazodone
hepatotoxicity
AE of trazodone
block alpha 1 and H1 –> extreme sedation and hypnotic hence why it is used as an off label hypnotic
example and mechanism of NASSAs
noradrenergic and specific serotonergic antidepressant –> alpha 2, 5-HT2, and 5-HT3 antagonist
also H1 antagonist
Mirtazapine
AE of NASSA
Mirtazapine
sedation
weight gain
first choice for depression in adults and children not taking any drug that can antagonize it
Fluoxetine
first choice for depression in adults taking medication that can antagonize fluoxetine
Citaprolam or Sertraline
since SSRI are first choice for depression, what are TCAs used for
neuropathic and other pain conditions
antidepressants that is approved for pain associated with diabetic neuropathy and fibromyalgia
SNRI Duloxetine
antidepressant approved for treatment of bulimia
Fluoxetine
antidepressant approved for premenstrual dysphoric disorder
Fluoxetine and Sertraline
