Migraine Medchem Flashcards
what are the basic structural features of triptans?
- indole ring system
- short side chain (2-3 Cs) at C-3 to a tertiary or secondary amine
- a polar group
what is the name of the inactive metabolite of sumatriptan?
indole acetic acid metabolite
why does naratriptan not have MAO-A metabolism? (only structural difference to sumatriptan)
has a ring side-chain to block MAO-A metabolism
what are the 2 metabolites of zolmitriptan?
indole acetic acid metabolite
N-desmethylzolmitriptan
what are the 2 metabolites of rizatriptan?
acetic acid derivative
N-desmethyrizatriptan
what is difference between zolmitriptan and sumatriptan?
what does this mean as far as side effects?
position 5 has a ring formation
greater potential for CNS SEs
what is difference between rizatriptan and sumatriptan?
what does this mean as far as side effects?
position 5 has a ring formation
greater potential for CNS SEs
how does frovatriptan primarily look different than sumatriptan?
does it undergo MAO-A metabolism?
does it have increased CNS effects?
has 3 rings all connected to each other
no
no
how is eletriptan structurally different to sumatriptan?
does it undergo MAO-A metabolism?
does it have increased CNS effects?
has 4 rings
no
yes
what is unique-looking about lasmiditan to distinguish it?
a phenyl ring with 3 fluorenes
all “pant” drugs are contraindicated with?
strong 3A4 inhibitors
which triptans have MAO-A metabolism? (ZARS)
zolmitriptan
almotriptan
rizatriptan
sumatriptan
which triptans have 1A2 metabolism?
Zolmitriptan
which triptans have 3A4 metabolism?
eletriptan
