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)
MOA/Neurochemical Effects: Injectable anesthetic, NMDA antagonist (glutamate)
Ketamine
Clinical Effects: Single dose improves depression sx in 2 hrs, effects last for 1 wk
Ketamine
AE/Toxicity: Nightmares and hallucinations
Ketamine
AZD6765 = NMDA channel blocker with low rates of psycho AE
Ketamine
Tricyclic Antidepressants
Desipramine (Norpramin)
Imipramine (Tofranil)
Monoamine Oxidase Inhibitors
Phenelzine (Nardil)
Selective Serotonin Reuptake Inhibitors
Fluoxetine (Prozac),
Sertraline (Zoloft), Escitalopram (Lexapro)
MOA/Neurochemical Effects: Effects postsynaptic neuron – alters gene expression implicated in long-term neuroplastic events long-term mood stabilization
Lithium Carbonate
Lithobid, Eskalith
Clinical Effects: Effective in 60-80% of those with bipolar, therapeutic effect seen in 5-21 days
Prevents mood swings –increases euthymia range
Lithium Carbonate
Lithobid, Eskalith
AE/Toxicity: Therapeutic: fatigue, weakness, slurred speech, ataxia, tremor, excessive thirst/urination
Toxic: LOC, coma, muscular rigidity, hyperreflexia, tremor, muscle fasciculations (TI LOW)
Lithium Carbonate
Lithobid, Eskalith
Tolerance to AE after 4 wks (except for tremor and urination/thirst)
Renal clearance reduced 25% by diuretics
Lithium Carbonate
Lithobid, Eskalith
MOA/Neurochemical Effects: Anticonvulsant
Valproic Acid
Depakene
Clinical Effects: Efficacy similar to Li+, superior to Li+ for rapid-cycling bipolar
Valproic Acid
Depakene
Appropriate 1st line therapy for some (can combine with Li+)
Valproic Acid
Depakene
Anticonvulsant
Carbamazepine
Tegretol
Prophylaxis of bipolar disorder
Carbamazepine
Tegretol
Fluoxetine (Prozac),
Sertraline (Zoloft), Escitalopram (Lexapro)
Selective Serotonin Reuptake Inhibitors
Phenelzine (Nardil)
Monoamine Oxidase Inhibitors
Desipramine (Norpramin)
Imipramine (Tofranil)
Tricyclic Antidepressants