Antidepressants / Bipolar drugs Flashcards
MOA/Neurochemical Effects: Block reuptake of NE and/or 5HT
Desipramine = NE-selective
Imipramine = NE and 5HT
Higher concentration of NT at their receptors
Tricyclic Antidepressants
Desipramine (Norpramin)
Imipramine (Tofranil)
Clinical Effects: Elevation in mood (2-3 wks delayed)
Causes antimuscarinic effects, sleepiness, lightheadedness in those who don’t have depression
Tricyclic Antidepressants
Desipramine (Norpramin)
Imipramine (Tofranil)
AE/Toxicity: Weight gain, drowsiness, dry mouth, blurred vision, constipation, drowsiness, lightheadedness, orthostatic hypotension, arrhythmias, cardiac arrest, seizures
Tricyclic Antidepressants
Desipramine (Norpramin)
Imipramine (Tofranil)
TI is low»_space; lethality in overdose
Metabolized by CYP2D6 (E is inhibited by fluoxetine)
Tricyclic Antidepressants
Desipramine (Norpramin)
Imipramine (Tofranil)
MOA/Neurochemical Effects: Irreversibly blocks MAO-A (NE and 5HT) and MAO-B (DA)
Increased NT in vesicles/released/action at R
Monoamine Oxidase Inhibitors
Phenelzine (Nardil)
AE/Toxicity: Serotonin Syndrome (overactivation of 5HT2A hyperthermia), potentiates sympathomimetic amines (tyramine hypertensive crisis)
Monoamine Oxidase Inhibitors
Phenelzine (Nardil)
Low TI
Do not start until 14 days following discontinuation of SSRIs
Monoamine Oxidase Inhibitors
Phenelzine (Nardil)
MOA/Neurochemical Effects: Blocks reuptake of 5HT from synapse (5HT2A R) can trigger actions postsynaptically or bind to autoreceptors & inhibit more 5HT release
Selective Serotonin Reuptake Inhibitors
Fluoxetine (Prozac),
Sertraline (Zoloft), Escitalopram (Lexapro)
AE/Toxicity: Nausea, diarrhea, weight loss, sexual dysfunction, anxiety, nervousness, insomnia (NOT sedating like TCAs)
Black box warning suicide
Selective Serotonin Reuptake Inhibitors
Fluoxetine (Prozac),
Sertraline (Zoloft), Escitalopram (Lexapro)
Should NOT be used alone in bipolar can flip switch to manic
Selective Serotonin Reuptake Inhibitors
Fluoxetine (Prozac),
Sertraline (Zoloft), Escitalopram (Lexapro)
MOA/Neurochemical Effects: SNRI – blocks 5HT + NE reuptake
Efficacy improves with increasing dose (increase dose: only 5HTalso NEalso DA)
Venlafaxine (Effexor)
Clinical Effects: Effect on mood driven by same mechanism as TCAs but does NOT affect NE/HA/ACh R (less AE)
Venlafaxine (Effexor)
AE/Toxicity: Contraindicated in patients on MAOIs
Venlafaxine (Effexor)
Atypical (dual/mixed action)
May be mediated by 3 different monoamines (depends on dose)
Venlafaxine (Effexor)
Blocks presynaptic α2 receptor on NE neurons (autoR) and 5HT neurons (heteroR) increases NE and 5HT levels
Mirtazapine (Remeron)