Rizatriptan

Mechanism of action:
Rizatriptan is a triptan derivative. During a migraine attack, intracranial blood vessels become abnormally dilated. Rizatriptan activates 5-HT1B receptors, which are Gi/o protein-coupled receptors, on intracranial vascular smooth muscle, promoting vasoconstriction and reducing the throbbing pain caused by vasodilation. Rizatriptan also activates 5-HT1D receptors, which are Gi/o protein-coupled receptors, on trigeminal nerve terminals and inhibits the release of inflammatory neuropeptides from these terminals.
Reference(s):
1. Wellington K et al. (2002). Rizatriptan: an update of its use in the management of migraine. Drugs.
2. Tfelt-Hansen P et al. (2000). Triptans in migraine: a comparative review of pharmacology, pharmacokinetics and efficacy. Drugs.
3. Lainez MJ et al. (2006). Rizatriptan in the treatment of migraine. Neuropsychiatr Dis Treat.
