Serotonin Agonists Flashcards
5-HT receptors:
1B does what?
mediate vasoconstriction
5-HT receptors:
1D does what?
inhibit neurotransmitter release
5-HT receptors:
1F does what?
inhibit release of nociceptive signaling molecules
what is the structural difference between Ergotamine and Dihydroerotamine?
DHE does not have a double bond in a ring
Ergots are selective for which subsets of serotonin receptors
2A; 1B; 1D; 1F
Poor or Great Absorption of Ergots?
Poor
aka available as IM, nasal spray, SL tablet
Ergots are partial ________ receptor agonists
alpha1
which ergot is less prone to cause severe peripheral vasoconstriction with frequent dosing
DHE
Do Ergots have short or long half lives
long
why do Ergots have a long half life
because they have active metabolites and and tight binding to tissues
what are the side effects of Ergots
GI (diarrhea, N/V)
causes uterine stimulants (aka contraindicated in pregnancy)
Gangrene
Triptans are selective for which subsets of serotonin receptors
1B, 1D, 1F
which triptan has the shortest half life
Sumtriptan and Rizatriptan (with 2 hr)
which triptan has the longest half life
Frovatriptan
what is the notable structural difference in Frovatriptan
it is TRICYCLIC