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Chemical Compound Review

Risatriptan     N,N-dimethyl-2-[5-(1,2,4- triazol-1...

Synonyms: rizatriptan, rizatriptanum, rizatriptan;, CHEMBL905, Maxalt MLT, ...
 
 
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Disease relevance of Risatriptan

 

High impact information on Risatriptan

 

Chemical compound and disease context of Risatriptan

 

Biological context of Risatriptan

  • Chest pain was reported by 1 to 3% of rizatriptan recipients and by 3 to 6% of patients receiving sumatriptan (25, 50 or 100 mg); clinically significant effects on ECG parameters, heart rate or blood pressure were not observed with rizatriptan [13].
  • Neurogenic dural vasodilation was also blocked by the 5-HT(1B/1D) agonist rizatriptan (100 microg kg(-1)) with estimated plasma levels commensurate with concentrations required for anti-migraine efficacy in patients [14].
  • For the commonly prescribed antimigraine drug rizatriptan, inhalation of these particles results in nearly instantaneous systemic drug action [15].
  • Merck & Co., Inc. evaluates outcomes of the use of rizatriptan during pregnancy through a Pregnancy Registry in the United States (US) and spontaneous reports for pregnancies reported from sources outside the US [4].
  • In naratriptan-, rizatriptan-, and sumatriptan-treated animals, jugular venous oxygen saturation decreased dose dependently (geometric mean ED50 values of 3.1, 17.9, and 16.0 microg/kg, respectively) concomitantly with increases in carotid vascular resistance [16].
 

Anatomical context of Risatriptan

 

Associations of Risatriptan with other chemical compounds

 

Gene context of Risatriptan

 

Analytical, diagnostic and therapeutic context of Risatriptan

References

  1. Within-patient consistency of response of rizatriptan for treating migraine. Dahlöf, C.G., Lipton, R.B., McCarroll, K.A., Kramer, M.S., Lines, C.R., Ferrari, M.D. Neurology (2000) [Pubmed]
  2. Rizatriptan: an update of its use in the management of migraine. Wellington, K., Plosker, G.L. Drugs (2002) [Pubmed]
  3. Meta-analysis of rizatriptan efficacy in randomized controlled clinical trials. Ferrari, M.D., Loder, E., McCarroll, K.A., Lines, C.R. Cephalalgia : an international journal of headache. (2001) [Pubmed]
  4. Exposure to rizatriptan during pregnancy: post-marketing experience up to 30 June 2004. Fiore, M., Shields, K.E., Santanello, N., Goldberg, M.R. Cephalalgia : an international journal of headache. (2005) [Pubmed]
  5. Effects of 5-HT1B/1D receptor agonist rizatriptan on cerebral blood flow and blood volume in normal circulation. Okazawa, H., Tsuchida, T., Pagani, M., Mori, T., Kobayashi, M., Tanaka, F., Yonekura, Y. J. Cereb. Blood Flow Metab. (2006) [Pubmed]
  6. Comparison of rizatriptan and other triptans on stringent measures of efficacy. Adelman, J.U., Lipton, R.B., Ferrari, M.D., Diener, H.C., McCarroll, K.A., Vandormael, K., Lines, C.R. Neurology (2001) [Pubmed]
  7. Rizatriptan versus usual care in long-term treatment of migraine. Silberstein, S.D. Neurology (2000) [Pubmed]
  8. A placebo-controlled crossover study of rizatriptan in the treatment of multiple migraine attacks. Rizatriptan Multiple Attack Study Group. Kramer, M.S., Matzura-Wolfe, D., Polis, A., Getson, A., Amaraneni, P.G., Solbach, M.P., McHugh, W., Feighner, J., Silberstein, S., Reines, S.A. Neurology (1998) [Pubmed]
  9. Oral therapy for migraine: comparisons between rizatriptan and sumatriptan. A review of four randomized, double-blind clinical trials. Tfelt-Hansen, P., Ryan, R.E. Neurology (2000) [Pubmed]
  10. Anti-migraine action of triptans is preceded by transient aggravation of headache caused by activation of meningeal nociceptors. Burstein, R., Jakubowski, M., Levy, D. Pain (2005) [Pubmed]
  11. Preference for rizatriptan 10-mg wafer vs. eletriptan 40-mg tablet for acute treatment of migraine. Láinez, M.J., Evers, S., Kinge, E., Allais, G., Allen, C., Rao, N.A., Massaad, R., Lis, K. Cephalalgia : an international journal of headache. (2006) [Pubmed]
  12. Rizatriptan vs. rizatriptan plus trimebutine for the acute treatment of migraine: a double-blind, randomized, cross-over, placebo-controlled study. Krymchantowski, A.V., Filho, P.F., Bigal, M.E. Cephalalgia : an international journal of headache. (2006) [Pubmed]
  13. Rizatriptan: a review of its efficacy in the management of migraine. Dooley, M., Faulds, D. Drugs (1999) [Pubmed]
  14. The anti-migraine 5-HT(1B/1D) agonist rizatriptan inhibits neurogenic dural vasodilation in anaesthetized guinea-pigs. Williamson, D.J., Hill, R.G., Shepheard, S.L., Hargreaves, R.J. Br. J. Pharmacol. (2001) [Pubmed]
  15. Fast onset medications through thermally generated aerosols. Rabinowitz, J.D., Wensley, M., Lloyd, P., Myers, D., Shen, W., Lu, A., Hodges, C., Hale, R., Mufson, D., Zaffaroni, A. J. Pharmacol. Exp. Ther. (2004) [Pubmed]
  16. Investigation of the effects of naratriptan, rizatriptan, and sumatriptan on jugular venous oxygen saturation in anesthetized pigs: implications for their mechanism of acute antimigraine action. Létienne, R., Verscheure, Y., John, G.W. J. Pharmacol. Exp. Ther. (2003) [Pubmed]
  17. Autoradiography of serotonin 5-HT1A receptor-activated G proteins in guinea pig brain sections by agonist-stimulated [35S]GTPgammaS binding. Dupuis, D.S., Palmier, C., Colpaert, F.C., Pauwels, P.J. J. Neurochem. (1998) [Pubmed]
  18. Comparison of the vasoconstrictor effects of rizatriptan and sumatriptan in human isolated cranial arteries: immunohistological demonstration of the involvement of 5-HT1B-receptors. Longmore, J., Razzaque, Z., Shaw, D., Davenport, A.P., Maguire, J., Pickard, J.D., Schofield, W.N., Hill, R.G. British journal of clinical pharmacology. (1998) [Pubmed]
  19. 5-HT1D receptor agonists and human coronary artery reactivity in vitro: crossover comparisons of 5-HT and sumatriptan with rizatriptan and L-741,519. Longmore, J., Boulanger, C.M., Desta, B., Hill, R.G., Schofield, W.N., Taylor, A.A. British journal of clinical pharmacology. (1996) [Pubmed]
  20. Clinical-biochemical correlates of migraine attacks in rizatriptan responders and non-responders. Sarchielli, P., Pini, L.A., Zanchin, G., Alberti, A., Maggioni, F., Rossi, C., Floridi, A., Calabresi, P. Cephalalgia : an international journal of headache. (2006) [Pubmed]
  21. Cost-effectiveness of almotriptan and rizatriptan in the treatment of acute migraine. Williams, P., Reeder, C.E. Clinical therapeutics. (2003) [Pubmed]
  22. Triptan-induced contractile (5-HT1B receptor) responses in human cerebral and coronary arteries: relationship to clinical effect. Edvinsson, L., Uddman, E., Wackenfors, A., Davenport, A., Longmore, J., Malmsjö, M. Clin. Sci. (2005) [Pubmed]
  23. Influence of beta-adrenoceptor antagonists on the pharmacokinetics of rizatriptan, a 5-HT1B/1D agonist: differential effects of propranolol, nadolol and metoprolol. Goldberg, M.R., Sciberras, D., De Smet, M., Lowry, R., Tomasko, L., Lee, Y., Olah, T.V., Zhao, J., Vyas, K.P., Halpin, R., Kari, P.H., James, I. British journal of clinical pharmacology. (2001) [Pubmed]
  24. An in vitro interethnic comparison of monoamine oxidase activities between Japanese and Caucasian livers using rizatriptan, a serotonin receptor 1B/1D agonist, as a model drug. Iwasa, T., Sano, H., Sugiura, A., Uchiyama, N., Hara, K., Okochi, H., Nakagawa, K., Yasumori, T., Ishizaki, T. British journal of clinical pharmacology. (2003) [Pubmed]
  25. Safety and rational use of the triptans. Tepper, S.J. Med. Clin. North Am. (2001) [Pubmed]
  26. Rizatriptan, a novel 5-HT1B/1D agonist for migraine: single- and multiple-dose tolerability and pharmacokinetics in healthy subjects. Goldberg, M.R., Lee, Y., Vyas, K.P., Slaughter, D.E., Panebianco, D., Ermlich, S.J., Shadle, C.R., Brucker, M.J., McLoughlin, D.A., Olah, T.V. Journal of clinical pharmacology. (2000) [Pubmed]
  27. A comparison of visual analog scale and categorical ratings of headache pain in a randomized controlled clinical trial with migraine patients. Lines, C.R., Vandormael, K., Malbecq, W. Pain (2001) [Pubmed]
  28. Disposition and pharmacokinetics of the antimigraine drug, rizatriptan, in humans. Vyas, K.P., Halpin, R.A., Geer, L.A., Ellis, J.D., Liu, L., Cheng, H., Chavez-Eng, C., Matuszewski, B.K., Varga, S.L., Guiblin, A.R., Rogers, J.D. Drug Metab. Dispos. (2000) [Pubmed]
 
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