Antidepressants Flashcards
What kind of drugs are tranylcypromine and phenelzine / what enzymes do they affect?
Antidepressants; MAOI’s: they inhibit both MAO-A and MAO-B
What are 2 possibly life-threatening side effects of taking tranylcypromine and phenelzine?
Hypertensive crisis (with tyramine-rich foods) and serotonin syndrome (with SSRIs) (this is part of the reason MAOIs are now rarely used)
How do the MAOIs treat depression? Which of the enzymes that they inhibit is responsible for oxidizing serotonin and norepi?
inhibit MAO-A and MAO-B to slow monoamine degradation; MAO-A oxidizes serotonin and norepi
What kind of drugs are desipramine, imipramine, nortriptyline, and amitriptyline, what enzymes do they affect, and how?
Tricyclic antidepressants; inhibit reuptake transporters for 5HT and NE (and also block the muscarinic, a-adrenergic, dopamine, and histamine receptors)
Of the 4 tricyclic antidepressants, which 2 are active metabolites of the other 2 drugs?
Desipramine is the active metabolite of imipramine, nortriptyline is the active metabolite of amitriptyline
What organ is most affected by tricyclic overdoses? Name 2 possible effects.
Heart: cardiac arrhythmias and conduction defects (this is part of the reason tricyclics are no longer commonly used)
Which antidepressant is useful for treating tension headaches and migraines, as well as the usual depression/anxiety/PTSD/etc.?
Amitriptyline
What kind of drugs are fluoxetine and paroxetine, and how do they work molecularly?
SSRI antidepressants, inhibit reuptake of 5HT (and, to a lesser extent, of NE)
What kind of drugs are sertraline, escitalopram, citalopram, and how do they work molecularly?
SSRI antidepressants, inhibit reuptake of 5HT (and, to a lesser extent, of NE)
Which antidepressant drug can also be used to treat premenstrual dysmorphic disorder?
Fluoxetine
What side effects do the SSRIs cause, and how do they compare to the side effects of the tricyclics?
SSRIs can cause nausea and sexual dysfunction, but in general their side effects are less intense than that of the tricyclics (this is part of the reason tricyclics are no longer commonly used)
Which 2 antidepressant drugs can inhibit P450 and can therefore interfere with the metabolism of other drugs?
Fluoxetine and paroxetine
What is the active metabolite of fluoxetine? Does the original drug have a longer or shorter half-life than its active metabolite?
Norfluoxetine; the original drug has a shorter half-life than its active metabolite
What kind of drugs are duloxetine and venlafaxine, and how do they work molecularly?
SNRI antidepressants, inhibit reuptake of 5HT and NE equally
Name the 2 atypical antidepressants. Which one can be used to maintain nicotine abstinence?
Buproprion and mirtazapine; buproprion is used in smoking cessation
How does buproprion treat depression?
By inhibiting dopamine and norepi reuptake
How does mirtazapine treat depression?
By antagonizing the 5HT-2a receptor as well as by inhibiting 5HT reuptake
List all the antidepressants that can cause seizures if overdosed.
All the MAOIs (phenelzine, tranylcypromine), all the tricyclics (desipramine, imipramine, amitriptyline, nortriptyline), and buproprion
Give 2 therapeutic uses for lithium.
Bipolar disorder (mood stabilization) and long-term cluster headaches (prevention)
How does lithium help treat bipolar disorder?
Lithium depletes the neuron of IP3 and DAG second messengers, which seems to depress the α-adrenergic and muscarinic signaling pathways
Elevated levels of lithium can cause damage to what 3 organs?
Heart, kidney, and neurons/brain (nausea and vomiting are early signs of lithium overdose)
What 2 classes of antidepressants can cause serotonin syndrome if taken together?
MAOIs and SSRIs
What mood stabilizing drug can cause side effects of drowsiness, weight gain, tremor, polydipsia, and polyuria?
Lithium
List 7 disorders which can be treated by any of the antidepressants (MAOIs, tricyclics, SSRIs, SNRIs, and atypicals).
Depression, anxiety, PTSD, chronic pain, enuresis (loss of urinary retention control), bulimia, and alcoholism
What anesthetic drug and NMDA antagonist is also an atypical antidepressant?
Ketamine
A bipolar patient on lithium presents to the emergency room with altered mental status, nausea, and vomiting. Give 2 drugs the patient might have taken, which could have precipitated this Li overdose.
Indomethacin (NSAID) or a Na-depleting diuretic
