Anti-Migraine Flashcards
Dihydroergotamine brand name and class
Migranal - Injectable
D.H.E. 45 - Nasal Spray
Ergot alkaloid
Dihydroergotamine MOA
Partial agonist at Serotonin receptors
- SE’s due to activity at other receptors
- Dopamine receptors
- a,b-adrenergic receptors
Basic Triptan SAR features
- Indole Ring system
- Side chain on carbon #3 is 2 to 3 c’s long with a tertiary, or sometimes secondary amine at the terminal end.
- A “polar” group at position 5 capable of hydrogen bonding.
Sumatriptan brand name ( * )
Imitrex - The only First Generation Triptan ( * )
Naratriptan brand name
Amerge
Zolmitriptan brand name
Zomig
Rizatriptan brand name
Maxalt
Frovatriptan brand name
Frova
Frovatriptan brand name
Frova
Eletriptan brand name
Relpax
First vs. Second generation Triptan MOA
5-HT( 1B, 1D ) agonism - Sumatriptan
5-HT( 1B, 1D, 1F) agonism - Second Generation
Role of 5-HT1 agonism in anti-migraine mechanism
- 5-HT(1B) = Located on the endothelium of the cranial vasculature, leads to constriction.
- 5-HT(1D) = Located on the pre-synaptic terminal of the trigeminal nerve as a heteroreceptor; leads to decreased release of CGRP (mostly)
- 5-HT(1F) = Similar to 1D?
Which of the triptans have active metabolites?
Zolmitriptan: 1A2 N-desmethyl product
- Major metabolite
Rizatriptan: (?) N-desmethyl product.
- Minor metabolite
Eletriptan: 3A4 N-desmethyl product
- Major metabolite
Dihydroergotamine structure
Sumatriptan structure
Almotriptan structure
Think “almost”
Naratriptan structure
Zolmitriptan structure
Rizatriptan structure
Frovatriptan structure
Eletriptan structure
