FROVATRIPTAN

General Description

Frovatriptan is a newer triptan introduced into the market in2001. With the incorporation of a 3-alkylamino side chaininto a carbazole ring structure, it is not a substrate forMAO-A or CYP3A4. Thus, unlike the other clinicallyavailable triptans, it possesses a much longer duration ofaction with fewer drug–drug interactions with MAO inhibitorsor with drugs metabolized by the CYP3A4isozymes. It is primarily metabolized by CYP1A2 togive its active metabolite, N-desmethyl-frovatriptan, whichhas about one third of the binding affinity for 5-HT1D/1B receptorsbut with three times longer plasma half-life of theparent drug.
Frovatriptan also has the highest affinity for brain 5-HT1B receptors and the longest elimination half-life amongall triptans. The only disadvantage of this drug is itsslower onset of action because of its greater water solubility.However, it is a drug of choice for patients with longlastingmigraines or if recurrence is a problem.