MAOIs Flashcards
MOA: binds irreversibly to MAO-A (in DA & NE neurons of brain, gut, placenta & liver) & MAO-B (serotonergic & hisaminergic neurons of brain, liver & platelets) blocking function
Use: treatment of depression not responsive to other antidepressants
Metab: undergoes significant first-pass effect; inhibit MAO in the gut
Interaction: tyramine, meperidine
Adverse: serotonergic syndrome when in combo with serotonergic agents (SSRIs, SNRIs, TCAs)
phenelzine
Nardil
MOA: binds irreversibly to MAO-A (in DA & NE neurons of brain, gut, placenta & liver) & MAO-B, blocking function
Use: treatment of depression not responsive to other antidepressants
Metab: undergoes significant first-pass effect; inhibit MAO in the gut
Interaction: tyramine
Adverse: serotonergic syndrome when in combo with serotonergic agents (SSRIs, SNRIs, TCAs)
Isocarboxacid
Marplan
MOA: binds irreversibly to MAO-A (in DA & NE neurons of brain, gut, placenta & liver) & MAO-B blocking function; resembles amphetamine in structure
Use: treatment of depression not responsive to other antidepressants
Metab: undergoes significant first-pass effect; inhibit MAO in the gut
Interaction: tyramine, meperidine
Adverse: serotonergic syndrome when in combo with serotonergic agents (SSRIs, SNRIs, TCAs)
tranylcypromine
Parnate
MOA: at high doses it is nonselectively binding to MAO-A and MAO-B blocking function; metabolite resembles amphetamine
Use: treatment of depression not responsive to other antidepressants; Parkinson’s disease (low dose)
Metab: undergoes significant first-pass effect; inhibit MAO in the gut
Interaction: tyramine, meperidine
Adverse: serotonergic syndrome when in combo with serotonergic agents (SSRIs, SNRIs, TCAs)
selegeline
Eldepryl
enzyme with primary substrate of NE, epi and serotonin
found in DA & NE neurons of brain, liver, gut and placenta
MAO-A
enzyme with primary substrate of tyramine, phenylethylamine, and benzylamine
found in serotonergic and histaminergic neurons of brain, liver and platelets
MAO-B
