Rizatriptan (Maxalt), a new entity of triptan for migraine: pharmacology and therapeutic relevance.

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  • 新規トリプタン，安息香酸リザトリプタン（マクサルト）の片頭痛治療への導入
  • 新薬紹介総説 新規トリプタン,安息香酸リザトリプタン(マクサルト)の片頭痛治療への導入
  • シンヤク ショウカイ ソウセツ シンキ トリプタン アンソクコウサン リザトリプタン マクサルト ノ ヘンズツウ チリョウ エ ノ ドウニュウ
  • Rizatriptan (Maxalt®), a new entity of triptan for migraine: pharmacology and therapeutic relevance

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Rizatriptan is a highly potent, selective serotonin 5-HT1B/1D-receptor agonist. Current theories on the mechanism of migraine suggest the central role of vasodilation of intracranial, extracerebral blood vessels and activation of perivascular trigeminal sensory nerves. There abundantly exist 5-HT1B receptors in meningeal blood vessels and 5-HT1D receptors in the trigeminal ganglia. The therapeutic activity of rizatriptan in migraine can most likely be attributed to agonist effects at 5-HT1B/1D receptors on these target sites. Two types of the 10 mg formulation, a tablet (Maxalt® tablet) and an orally disintegrating tablet (Maxalt®RPD tablet), are available. The latter may have a clinical relevance for patients who administer it without liquid. Pharmacokinetic study demonstrated the approximate Tmax of 1.0 or 1.1 h in tablets and 1.3 h in RPD tablets, resulting in early onset for headache relief and also pain free. Bioavailability was estimated to be about 45%. The efficacy and good tolerability and underlying profiles of pharmacokinetics of rizatriptan are almost similar between Japanese and other races, and a reduction in headache response up to 2 h can be attained in a large majority of patients. Several reports have described the favorable clinical profile of rizatriptan in comparison to other triptans. Rizatriptan is thus effective and provides migraine sufferers with an appropriate quality of life.<br>

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