TCAs

Question 1

MOA: inhibition of 5-HT and NE reuptake by inhibition of SERT and NET; has more 5-HT effects initially but its metabolite has more NET inhibition
Use: second-line for MDD
Adverse: dry mouth, constipation from potent antimuscarinic effects; potent antagonist of H1 receptor (hypnotic) as well as alpha adrenoreceptor blockade (orthostatic hypotension in elderly)
-lethal in overdose
Interactions: CYP2D6 inhibitors elevate levels; may have additive effects when combined with antihistamines or antihypertensives

Answer 1

imipramine

Tofranil

Question 2

MOA: active metabolite of imipramine with greater selectivity for NET inhibition
Use: second-line for MDD
Adverse: dry mouth, constipation from potent antimuscarinic effects; potent antagonist of H1 receptor (hypnotic) as well as alpha adrenoreceptor blockade (orthostatic hypotension in elderly)
-lethal in overdose
Interactions: CYP2D6 inhibitors elevate levels; may have additive effects when combined with antihistamines or antihypertensives

Answer 2

desimipramine

Norpramine

Question 3

MOA: inhibition of SERT more than NET with high affinity for muscarinic ACh receptors and alpha-adrenergic receptors, moderate affinity for H1 receptors
Use: second-line tx for MDD
Adverse:dry mouth, constipation from potent antimuscarinic effects; potent antagonist of H1 receptor (hypnotic) as well as alpha adrenoreceptor blockade (orthostatic hypotension in elderly)
-lethal in overdose
Interactions: CYP2D6 inhibitors elevate levels; may have additive effects when combined with antihistamines or antihypertensives

Answer 3

amitriptyline

Elavil

Question 4

MOA: inhibition of NET more than SERT with mild affinity for muscarinic ACh receptors, alpha-adrenergic receptors, HI receptors and 5-HT receptors
Use: second-line tx for MAJOR DEPRESSION
Adverse:dry mouth, constipation from potent antimuscarinic effects; potent antagonist of H1 receptor (hypnotic) as well as alpha adrenoreceptor blockade (orthostatic hypotension in elderly)
-lethal in overdose
Interactions: CYP2D6 inhibitors elevate levels; may have additive effects when combined with antihistamines or antihypertensives

Answer 4

nortriptyline

Pamelor