| Description | Naramig was launched in Germany, Sweden and the UK for use in migraine.
It is chemically available via a number of related synthetic routes all having about
three steps starting from 5-bromoindole. It is a new serotonin 5-HT1B/1D receptor
antagonist with modest affinity for 5-HT1a, and very weak affinity for 5-HT3 receptors. It
has little or no affinity for a wide range of non-serotonin receptors including a- and padrenoceptors,
dopamine, neurokinin NK1, and opiate receptors. It mediates
vasoconstriction in cerebral vasculature (extra cerebral intracranial vessels), reduces
neurogenic inflammation, and inhibits responses mediated by the trigeminal nerves. It
has a 6- and 3-fold greater affinity for 5-HT1B, and 5-HT1D, receptors, respectively, than
sumatriptan which translates to a 2-3 fold increase in potency. The reoccurance of
headache was less compared to sumatriptan, zolmitriptan and rizatriptan. Naramig
had no clinical effects on blood pressure or heart rate, had a long duration of action
with very good tolerability, and has high oral bioavailability. |
