and Answers
What neurotransmitters do TCAs inhibit reuptake of into the presynaptic neuron?
✓ ~~~ Norepinephrine and serotonin.
If discovered today, what class of antidepressants might TCAs have been referred to
as?
✓ ~~~ SNRIs (Serotonin-Norepinephrine Reuptake Inhibitors).
What distinguishes TCAs from SNRIs despite their similar mechanism of action?
✓ ~~~ TCAs have different adverse effects relative to SNRIs.
Name the tertiary amine that serves as the prototype drug for TCAs.
✓ ~~~ Imipramine
Which TCAs are classified as secondary amines?
✓ ~~~ Desipramine and nortriptyline.
What are the N-demethylated metabolites of imipramine and amitriptyline,
respectively?
✓ ~~~ Desipramine (of imipramine) and nortriptyline (of amitriptyline).
Name two related "tetracyclic" antidepressant agents that are commonly included in
the general class of TCAs.
, ✓ ~~~ Maprotiline and amoxapine.
What neurotransmitter reuptake do TCAs and amoxapine inhibit?
✓ ~~~ Norepinephrine and serotonin.
Besides TCAs, which specific agents are relatively selective inhibitors of
norepinephrine reuptake?
✓ ~~~ Maprotiline and desipramine.
Apart from inhibiting neurotransmitter reuptake, what other receptors do TCAs
block?
✓ ~~~ Serotonergic, α-adrenergic, histaminic, and muscarinic receptors.
What is likely responsible for many of the adverse effects of TCAs?
✓ ~~~ Actions at serotonergic, α-adrenergic, histaminic, and muscarinic receptors.
Besides serotonin receptors, what other receptors does amoxapine block?
✓ ~~~ Amoxapine also blocks 5-HT2 and dopamine D2 receptors.
What are the actions of TCA's?
✓ ~~~ TCAs improve mood, in 50% to 70% of individuals with major depression.
How long does it take for TCA's to start working?
✓ ~~~ 2 weeks or longer
Why is tapering doses recommended in TCA's?