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Rizatriptan, sold under the brand name Maxalt among others, is a medication used for the treatment of migraine headaches. [1] [3] It is taken by mouth. [1] [3] It can also be applied on the tongue. [2] It is a serotonin (5-HT) 1B/1D receptor agonist (triptan). [1] [2] Common side effects include chest pain, dizziness, dry mouth, and tingling. [3]
The main structural difference of the triptans is the position of the sulfonamide and the side chain attached to it (see figure 1 and table 1). Rizatriptan and zolmitriptan have instead of a sulfonamide a triazole and 2-oxazolidone respectively. Another exception to the classic structure is seen on eletriptan where the nitrogen-alkyl chain ...
A meta-analysis of 53 clinical trials has shown that all triptans are effective for treating migraine at marketed doses and that naratriptan, although less effective than sumatriptan and rizatriptan was more effective than placebo in reducing migraine symptoms at two hours [3] and efficacy was demonstrated in almost two thirds of subjects after four hours of treatment.
Triptans have a wide variety of pharmacokinetic properties. Bioavailability is between 14% and 70%, biological half-life (T 1/2) is between 2 and 26 hours. Their good ability to cross the blood–brain barrier and the rather long half life of some triptans may result in lower frequencies of migraine recurrence. [22] [38] [39] [40]
The triptan drug class includes 1st generation sumatriptan (which has poor bioavailability), and second generation zolmitriptan. [2] Due to their safety, efficacy and selectivity, triptans are considered first line agents for abortion of migraines. [2] These medications are selective 5-HT 1B/1D receptor agonists with some activity at 5-HT 1F.
Rescue treatment involves acute symptomatic control with medication. [4] Recommendations for rescue therapy of migraine include: (1) migraine-specific agents such as triptans, CGRP antagonists, or ditans for patients with severe headaches or for headaches that respond poorly to analgesics, (2) non-oral (typically nasal or injection) route of administration for patients with vomiting, (3) avoid ...
In addition to being 5-HT 1B agonists, triptans (i.e. sumatriptan, almotriptan, zolmitriptan, naratriptan, eletriptan, frovatriptan and rizatriptan) are also agonists at the 5-HT 1D receptor, which contributes to their antimigraine effect caused by vasoconstriction of blood vessels in the brain. The same is true for ergotamine.
The most common side effects [14] reported by at least 2% of patients in controlled trials of sumatriptan (25-, 50-, and 100-mg tablets) for migraine are atypical sensations (paresthesias and warm/cold sensations) reported by 4% in the placebo group and 5–6% in the sumatriptan groups, pain and other pressure sensations (including chest pain ...