Rizatriptan is an orally active serotonin 5-HT1 receptor agonist that potently and selectively binds to 5-HT1B/1D subtypes.
Earlier clinical trials demonstrated that rizatriptan 5 or 10mg is more effective than placebo at providing pain relief and a pain-free state, relieving associated symptoms of migraine, normalising functional ability and improving patient quality of life, and showed that rizatriptan provides faster freedom from pain and reduces nausea to a greater extent than oral sumatriptan.
More recently, rizatriptan 10mg was shown to be more effective than zolmitriptan 2.5mg or naratriptan 2.5mg at producing a pain-free state 2 hours postdose. Furthermore, compared with naratriptan, significantly more patients who received rizatriptan were pain free or had pain relief from 1 hour onwards. The number of patients with normal functional ability at 2 hours was significantly higher after rizatriptan than after naratriptan or zolmitriptan. Rizatriptan was also generally more effective than zolmitriptan or naratriptan at relieving migraine-associated symptoms.
Rizatriptan is generally well tolerated, and adverse events are usually mild and transient. The most common adverse events associated with rizatriptan in recent randomised trials were asthenia/fatigue, dizziness, somnolence and nausea. There was a trend towards a lower incidence of adverse events with rizatriptan compared with zolmitriptan (31.2 vs 38.8%). However, rizatriptan was associated with a significantly higher incidence of adverse events than naratriptan (39 vs 29%). The incidence of chest pain was similar after the administration of rizatriptan, zolmitriptan or naratriptan (2–4%).
In conclusion, rizatriptan is an effective drug for the acute treatment of moderate or severe migraine. Oral rizatriptan 5 and 10mg have shown greater efficacy than placebo in providing pain relief, an absence of pain, relief from associated symptoms, normal functional ability and an improvement in patient quality of 1 This Spotlight is derived from abstract and summary text of an Adis Drug Evaluation originally published in full in Drugs 2002; 62 (5): 817–840. life. Earlier results showed that rizatriptan provides faster freedom from pain and reduces nausea to a greater extent than oral sumatriptan. More recent studies have shown that rizatriptan 10mg provides faster pain relief and a higher percentage of patients with an absence of pain and normal functional ability at 2 hours than naratriptan 2.5mg or zolmitriptan 2.5mg. The efficacy of rizatriptan is retained when used in the long term, and the drug is generally well tolerated. Although well designed studies comparing rizatriptan with almotriptan, eletriptan and frovatriptan would further define the position of rizatriptan, current data suggest that rizatriptan should be considered as a first-line treatment option in the management of migraine.
KeywordsMigraine Sumatriptan Zolmitriptan Rizatriptan Almotriptan
The full text article in Drugs 2002; 62 (5): 817-840 was reviewed by: W.J. Becker, Division of Neurology, Foothills Medical Centre, Calgary, Alberta, Canada; G. Bussone, Third Neurological Division and Headache Centre, National Neurological Institute “C. Besta”, Milan, Italy; N.R. Cutler, California Clinical Trials Medical Group, Beverly Hills, Los Angeles, California, USA; C. Dahlöf, The Gothenburg Migraine Clinic, Sociala Huset, Gothenburg, Sweden; H.C. Diener, Department of Neurology, Klinik und Poliklinik fur Neurologie, Universitat Essen, Essen, Germany; L. Edvinsson, Department of Internal Medicine, University Hospital of Lund, Lund, Sweden; S. Evers, Department of Neurology, University of Munster, Munster, Germany; F. Facchinetti, Istituto di Clinica Osterica e Ginecologica, Universita Degli Stuid di Modena, Modena, Italy; K. Ghose, Department of Pharmacology, Faculty of Medicine, University of Otago, Dunedin, New Zealand; J. Sramek, California Clinical Trials Medical Group, Beverly Hills, Los Angeles, California, USA.
- 7.Noveck RJ, Bialy GP, Bradstreet TE, et al. Effects of rizatriptan on blood pressure in hypertensive patients. Clin Pharmacol Ther 1998 Feb; 63: 184Google Scholar
- 11.Merck and Co., Inc. Maxalt® and Maxalt-MLT® prescribing information: West Point, USA, 1998 [online]. Available from URL: http://www.merck.com [Accessed 2002 Mar 7]
- 24.Lines C, Visser WH, Vandormael K, et al. Rizatriptan 5 mg versus sumatriptan 50 mg in the acute treatment of migraine. Headache 1997 May; 37(5): 319–20Google Scholar
- 25.Pascual J, Vega P, Diener HC, et al. Comparison of rizatriptan 10 mg vs. zolmitriptan 2.5 mg in the acute treatment of migraine: the Rizatriptan-Zolmitriptan Study Group. Cephalalgia 2000; 20(5): 455–61Google Scholar
- 26.Bomhof M, Paz J, Legg N, et al. Comparison of rizatriptan 10 mg vs. naratriptan 2.5 mg in migraine: the Rizatriptan-Naratriptan Study Group. Eur Neurol 1999; 42(3): 173–9Google Scholar
- 30.Cady R, Crawford G, Ahrens S, et al. Long-term efficacy and tolerability of rizatriptan wafers in migraine: the Rizatriptan-RPD Study Group. Med Gen Med 2001 Jun 1; 3(3): 1Google Scholar
- 32.Belsey J. Reconciling effectiveness and tolerability in oral triptan therapy: a quantitative approach to decision making in migraine management. J Clin Res 2001; 4: 105–25Google Scholar