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Chemical Compound Review

Almogran     N,N-dimethyl-2-[5- (pyrrolidin-1...

Synonyms: Almotriptan, Axert, Almotriptan;, CHEMBL1505, SureCN1957, ...
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Disease relevance of Almotriptan

  • Dose finding, placebo-controlled study of oral almotriptan in the acute treatment of migraine [1].
  • CONCLUSIONS: Almotriptan has effects on blood pressure in subjects with controlled hypertension that are consistent with those of other members of the pharmalogic class [2].
  • Treatment-emergent adverse events occurred in 15.2% of the subjects in the almotriptan-treated group and in 19.4% in the sumatriptan-treated group (P =.06); treatment-related adverse events occurred in 9.1% and 15.5% of the subjects, respectively (P =.001), including chest pain, which occurred in 0.3% and 2.2%, respectively (P =.004) [3].
  • Other symptoms of migraine, including nausea, photophobia and phonophobia, are also alleviated by almotriptan [4].
  • Results.-The incidence of nausea, photophobia, and phonophobia at 2 hours after dosing with study medication was significantly reduced (all P <.05) with almotriptan 6.25 mg or 12.5 mg compared with placebo [5].

High impact information on Almotriptan


Chemical compound and disease context of Almotriptan

  • For the relief of single attacks of migraine, oral almotriptan 12.5mg had similar efficacy to oral sumatriptan 50mg [4].
  • Although these data suggest that rizatriptan may be a more effective treatment for migraine than almotriptan, further randomized studies are required to confirm this conclusion [8].
  • This study was designed to assess the pharmacokinetics of almotriptan, a 5HT1B/1D agonist used to treat migraine attacks, when administered in the presence and absence of fluoxetine [9].
  • Methods: This multicentre, double-blind trial randomized adult migraineurs to almotriptan 12.5 mg (n = 532) or zolmitriptan 2.5 mg (n = 530) for the treatment of a single migraine attack [10].
  • We studied the possible cardiovascular effects of single oral doses of 12.5, 25, and 50 mg of almotriptan, a new triptan for treatment of migraine, in a randomized, double-blind, four-way crossover, placebo-controlled study in 24 healthy volunteers aged 18 to 35 years [11].

Biological context of Almotriptan


Anatomical context of Almotriptan


Associations of Almotriptan with other chemical compounds


Gene context of Almotriptan


Analytical, diagnostic and therapeutic context of Almotriptan

  • METHODS: Twenty patients with hypertension controlled by medication received the following treatments in a randomized, double-blind, crossover design: one placebo tablet, one 12.5-mg almotriptan tablet, and one 25-mg almotriptan tablet [2].
  • Almotriptan plasma concentrations were determined by liquid chromatography-tandem mass spectrometry; urine samples were analyzed by ultraviolet HPLC [6].
  • Pain-free status at 2 h postdose is achieved by approximately 39% of patients receiving almotriptan in clinical trials [12].
  • A meta-analysis of pooled individual patient data from four randomized, placebo-controlled, double-blind trials comparing several doses of almotriptan (n = 1,908) with placebo (n = 386) was used to investigate the efficacy, speed of onset and tolerability of almotriptan in the acute treatment of migraine [23].
  • Plasma and urinary almotriptan concentrations were measured by high-performance liquid chromatography [24].


  1. Dose finding, placebo-controlled study of oral almotriptan in the acute treatment of migraine. Dahlöf, C., Tfelt-Hansen, P., Massiou, H., Fazekas, A. Neurology (2001) [Pubmed]
  2. Cardiovascular effect of almotriptan in treated hypertensive patients. Fleishaker, J.C., McEnroe, J.D., Azie, N.E., Francom, S.F., Carel, B.J. Clin. Pharmacol. Ther. (2002) [Pubmed]
  3. Oral almotriptan vs. oral sumatriptan in the abortive treatment of migraine: a double-blind, randomized, parallel-group, optimum-dose comparison. Spierings, E.L., Gomez-Mancilla, B., Grosz, D.E., Rowland, C.R., Whaley, F.S., Jirgens, K.J. Arch. Neurol. (2001) [Pubmed]
  4. Almotriptan: a review of its use in migraine. Keam, S.J., Goa, K.L., Figgitt, D.P. Drugs (2002) [Pubmed]
  5. Almotriptan reduces the incidence of migraine-associated symptoms: a pooled analysis. Cady, R. Headache. (2002) [Pubmed]
  6. Pharmacokinetic interaction between verapamil and almotriptan in healthy volunteers. Fleishaker, J.C., Sisson, T.A., Carel, B.J., Azie, N.E. Clin. Pharmacol. Ther. (2000) [Pubmed]
  7. Clinical pharmacokinetics of almotriptan, a serotonin 5-HT(1B/1D) receptor agonist for the treatment of migraine. McEnroe, J.D., Fleishaker, J.C. Clinical pharmacokinetics. (2005) [Pubmed]
  8. Almotriptan versus rizatriptan in patients with migraine in Spain. Leira, R., Dualde, E., del Barrio, H., Machuca, M., López-Gil, A. Headache. (2003) [Pubmed]
  9. Evaluation of the potential pharmacokinetic interaction between almotriptan and fluoxetine in healthy volunteers. Fleishaker, J.C., Ryan, K.K., Carel, B.J., Azie, N.E. Journal of clinical pharmacology. (2001) [Pubmed]
  10. Almotriptan and zolmitriptan in the acute treatment of migraine. Goadsby, P.J., Massiou, H., Pascual, J., Diener, H.C., Dahl??f, C.G., Mateos, V., Dowson, A.J., Raets, I., Cunha, L., F??rkkil??, M., Manzoni, G.C. Acta Neurol. Scand. (2007) [Pubmed]
  11. Hemodynamic and electrocardiographic effects of almotriptan in healthy volunteers. Boyce, M., Dunn, K., Warrington, S. J. Cardiovasc. Pharmacol. (2001) [Pubmed]
  12. Clinical profile and practice experience of almotriptan. Gendolla, A. Cephalalgia : an international journal of headache. (2004) [Pubmed]
  13. Interaction between ketoconazole and almotriptan in healthy volunteers. Fleishaker, J.C., Herman, B.D., Carel, B.J., Azie, N.E. Journal of clinical pharmacology. (2003) [Pubmed]
  14. Cardiovascular safety profile of almotriptan, a new indolic derivative for the treatment of migraine. Gras, J., Cardelús, I., Llenas, J., Palacios, J.M. Eur. J. Pharmacol. (2000) [Pubmed]
  15. Absolute bioavailability, pharmacokinetics, and urinary excretion of the novel antimigraine agent almotriptan in healthy male volunteers. Jansat, J.M., Costa, J., Salvà, P., Fernandez, F.J., Martinez-Tobed, A. Journal of clinical pharmacology. (2002) [Pubmed]
  16. Vascular effects of the new anti-migraine agent almotriptan on human cranial and peripheral arteries. Bou, J., Gras, J., Cortijo, J., Morcillo, E.J., Llenas, J., Palacios, J.M. Cephalalgia : an international journal of headache. (2001) [Pubmed]
  17. Functional profile of almotriptan in animal models predictive of antimigraine activity. Gras, J., Bou, J., Llenas, J., Fernández, A.G., Palacios, J.M. Eur. J. Pharmacol. (2000) [Pubmed]
  18. Lack of pharmacokinetic interaction between the antimigraine compound, almotriptan, and propranolol in healthy volunteers. Fleishaker, J.C., Sisson, T.A., Carel, B.J., Azie, N.E. Cephalalgia : an international journal of headache. (2001) [Pubmed]
  19. Effect of MAO-A inhibition on the pharmacokinetics of almotriptan, an antimigraine agent in humans. Fleishaker, J.C., Ryan, K.K., Jansat, J.M., Carel, B.J., Bell, D.J., Burke, M.T., Azie, N.E. British journal of clinical pharmacology. (2001) [Pubmed]
  20. Identification of the human liver enzymes involved in the metabolism of the antimigraine agent almotriptan. Salva, M., Jansat, J.M., Martinez-Tobed, A., Palacios, J.M. Drug Metab. Dispos. (2003) [Pubmed]
  21. Pharmacokinetics and safety of oral almotriptan in healthy male volunteers. McEwen, J., Salva, M., Jansat, J.M., Cabarrocas, X. Biopharmaceutics & drug disposition. (2004) [Pubmed]
  22. Safety profile of almotriptan, a new antimigraine agent. Effects on central nervous system, renal function and respiratory dynamics. Gras, J., Llupià, J., Llenas, J., Palacios, J.M. Arzneimittel-Forschung. (2001) [Pubmed]
  23. Efficacy, speed of action and tolerability of almotriptan in the acute treatment of migraine: pooled individual patient data from four randomized, double-blind, placebo-controlled clinical trials. Dahlöf, C.G., Pascual, J., Dodick, D.W., Dowson, A.J. Cephalalgia : an international journal of headache. (2006) [Pubmed]
  24. A comparison of the pharmacokinetics and tolerability of the anti-migraine compound almotriptan in healthy adolescents and adults. Baldwin, J.R., Fleishaker, J.C., Azie, N.E., Carel, B.J. Cephalalgia : an international journal of headache. (2004) [Pubmed]
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