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Chemical Compound Review

Avitriptan     1-[3-[3-[4-(5- methoxypyrimidin-4...

Synonyms: SureCN147315, AG-D-97981, ACMC-20n64q, LS-83176, CTK4C6906, ...
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Disease relevance of Avitriptan

  • Patients (n = 51) who had no clinically significant abnormality at baseline received a high dose (150 mg) of avitriptan orally outside of a migraine attack [1].
  • Only those hypertensive patients receiving medication for hypertension should receive anti-migraine medications, such as avitriptan, which are 5HT1-like receptor agonists [2].

High impact information on Avitriptan


Biological context of Avitriptan


Anatomical context of Avitriptan

  • In this study we sought to compare the effects of CP122,288 and avitriptan on jugular vein CGRP release after stimulation of the superior sagittal sinus (SSS) in the cat [9].
  • Scintigraphic analysis also demonstrated that upon emptying from the stomach, avitriptan was rapidly absorbed from the upper small intestine [7].

Associations of Avitriptan with other chemical compounds

  • Using these two models, we have now investigated the effects of avitriptan (BMS-180048; 3-[3-[4-(5-methoxy-4-pyrimidinyl)-l-piperazinyl[propyl]-N-methyl-l H-indole-5-methane-sulfonamide monofumarate), a new 5-HT 1B/1D receptor agonist [10].
  • Elevation in gastric pH caused by food was not found to be responsible for the food-related decrease in bioavailability of avitriptan since ranitidine pretreatment did not lead to a decrease in bioavailability [8].

Analytical, diagnostic and therapeutic context of Avitriptan

  • Avitriptan was extensively metabolized after oral administration, with the unchanged drug accounting for 32% and 22% of the total radioactivity in plasma in rats and humans, respectively [5].
  • This study demonstrates that the potent inhibitor of PPE, CP122, 288, which has been shown in clinical trials to be ineffective in treating acute migraine attacks, had no effect on CGRP release, whereas the effective anti-migraine drug and relatively impotent inhibitor of PPE, avitriptan, blocked CGRP release [9].
  • In vivo evaluation of the absorption and gastrointestinal transit of avitriptan in fed and fasted subjects using gamma scintigraphy [7].
  • Serial blood samples were collected over 24 h after dosing and analyzed by a validated HPLC method for avitriptan [6].


  1. Safety trial with the 5HT1B/1D agonist avitriptan (BMS-180048) in patients with migraine who have experienced pressure, tightness, and/or pain in the chest, neck, and/or throat following sumatriptan. Dahlöf, C.G., Falk, L., Risenfors, M., Lewis, C.P. Cephalalgia : an international journal of headache. (1998) [Pubmed]
  2. A double-blind, randomized, crossover assessment of blood pressure following administration of avitriptan, sumatriptan, or placebo to patients with mild to moderate hypertension. Jhee, S.S., Salazar, D.E., Ford, N.F., Fulmor, I.E., Sramek, J.J., Cutler, N.R. Cephalalgia : an international journal of headache. (1999) [Pubmed]
  3. A pharmacokinetic interaction study of avitriptan and propranolol. Marathe, P.H., Greene, D.S., Kollia, G.D., Barbhaiya, R.H. Clin. Pharmacol. Ther. (1998) [Pubmed]
  4. Pharmacokinetics and pharmacodynamics of avitriptan during intravenous administration in healthy subjects. Sharma, A., Jusko, W.J., Fulmor, I.E., Norton, J., Uderman, H.D., Salazar, D.E. Journal of clinical pharmacology. (1999) [Pubmed]
  5. Disposition of [14C]avitriptan in rats and humans. Marathe, P.H., Greene, D.S., Barbhaiya, R.H. Drug Metab. Dispos. (1997) [Pubmed]
  6. Assessment of effect of food, gender, and intra-subject variability in the pharmacokinetics of avitriptan. Marathe, P.H., Greene, D.S., Lee, J.S., Barbhaiya, R.H. Biopharmaceutics & drug disposition. (1998) [Pubmed]
  7. In vivo evaluation of the absorption and gastrointestinal transit of avitriptan in fed and fasted subjects using gamma scintigraphy. Marathe, P.H., Sandefer, E.P., Kollia, G.E., Greene, D.S., Barbhaiya, R.H., Lipper, R.A., Page, R.C., Doll, W.J., Ryo, U.Y., Digenis, G.A. Journal of pharmacokinetics and biopharmaceutics. (1998) [Pubmed]
  8. Evaluation of the effect of food on the pharmacokinetics of avitriptan. Marathe, P.H., Greene, D.S., Kollia, G.D., Barbhaiya, R.H. Biopharmaceutics & drug disposition. (1998) [Pubmed]
  9. Blockade of calcitonin gene-related peptide release after superior sagittal sinus stimulation in cat: a comparison of avitriptan and CP122,288. Knight, Y.E., Edvinsson, L., Goadsby, P.J. Neuropeptides (1999) [Pubmed]
  10. Effects of avitriptan, a new 5-HT 1B/1D receptor agonist, in experimental models predictive of antimigraine activity and coronary side-effect potential. Saxena, P.R., De Vries, P., Wang, W., Heiligers, J.P., Maassen vandenBrink, A., Bax, W.A., Yocca, F.D. Naunyn Schmiedebergs Arch. Pharmacol. (1997) [Pubmed]
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