Craniovascular selectivity of eletriptan and sumatriptan in human isolated blood vessels

Humphrey, P. P. A.; Fenvik, W.; Salonen, R.; Saxena, P. R.; Broek, R. W. M. van den; MaassenVanDenBrink, Antoinette

doi:10.1212/wnl.57.1.162-a

“…The triptans cause vasoconstriction in human blood vessels both in vitro and in vivo , although they have significantly more selective action in the cranial vasculature compared with the periphery and coronary arteries . Notably, the triptan doses are much higher (up to 1000 or 3‐log units) than the doses required to trigger the same vascular effects in vitro or in vivo , and it is suspected that the higher doses are necessary to reach brain targets .…”

Section: Treatment With Triptans and Ergot Derivativesmentioning

confidence: 99%

“…86 The triptans cause vasoconstriction in human blood vessels both in vitro and in vivo, although they have significantly more selective action in the cranial vasculature compared with the periphery and coronary arteries. [87][88][89][90][91][92][93][94][95][96][97][98] Notably, the triptan doses are much higher (up to 1000 or 3-log units) than the doses required to trigger the same vascular effects in vitro or in vivo, and it is suspected that the higher doses are necessary to reach brain targets. 99 Transcranial Doppler studies have shown an increase in middle cerebral artery cross-sectional lumen with an associated decrease in blood flow velocity on the affected side during unilateral migraine attacks due to vasodilatation, 76,100 with one study estimating a mean diameter increase of 20%.…”

Section: Treatment With Triptans and Ergot Derivativesmentioning

confidence: 99%

Headache, Cerebral Aneurysms, and the Use of Triptans and Ergot Derivatives

Baron

¹

2015

View full text Add to dashboard Cite

Associations between some headaches and aneurysms may exist. Some chronic headaches may respond to surgical aneurysm repair while others may worsen. These associations are undefined by current literature because of variable results, study methods, and limited data. Prospective studies are needed which incorporate pre- and post-procedure headache character and diagnosis, aneurysm characteristics, type of aneurysm repair, associated risk factors for worsening post-procedure headache, and ultimately combining all of these data to better predict headache outcome following surgical aneurysm treatment. Lastly, the caution and avoidance of triptan and ergot derivative use for migraine in the setting of aneurysm is not supported by the current evidence, and much of this concern may be excessive and unwarranted, although more evidence confirming safety is needed.

show abstract

“…It was beyond the scope of our review of sumatriptan tolerability to discuss data from other triptans (1). We would certainly agree that the use of cranio-coronary selectivity ratios derived from EC 50 measurements on incomplete concentration±effect curves on isolated blood vessels (2) may provide data which may be easily misinterpreted (3). Nonetheless, the extent of research conducted on sumatriptan safety and speci®cally the large number of trials on triptan tolerability and vascular effects provide the benchmark for the class.…”

mentioning

confidence: 94%

Tolerability of Sumatriptan: Clinical Trials and Postmarketing Experience

Allen

¹

,

Dayno

²

2001

Cephalalgia

1

0

View full text Add to dashboard Cite

Sir Welch et al.'s careful review of the extensive postmarketing data on sumatriptan (1) shows that this drug is generally well tolerated, with an acceptable bene®t± risk ratio when used in accordance with the prescribing information. As noted by the authors, sumatriptan and other triptans should not be given to patients with, or at high risk for, coronary or cerebrovascular disease.An important safety issue that was not discussed in the article is that data have recently been presented which might be misinterpreted by those not expert in the ®eld as showing that some triptans may have improved cardiovascular safety. These include the use of cranialcoronary contraction ratios from isolated vessel preparations (2), ECG studies in patients at risk of or with frank coronary artery disease that show negative results (3), or citing lower incidence of chest symptoms seen in clinical studies (4). We are concerned that the general medical community might perceive these data as implying a cardiovascular safety bene®t for one triptan over another. We would like to emphasize to your readers that all triptans are contraindicated in patients with coronary artery disease and it would be very unwise at this point to conclude that one triptan is safer than another. Also, given the typical patient population with migraine, focusing on the perception of cardiovascular safety for the triptan class only serves as a distraction from the real work at hand, which includes effective recognition of migraine and appropriate management strategies.

show abstract

Tolerability of Sumatriptan: Clinical Trials and Postmarketing Experience

Welch

¹

,

Feniuk

²

,

Mansbach

³

et al. 2001

View full text Add to dashboard Cite

Sir Welch et al.'s careful review of the extensive postmarketing data on sumatriptan (1) shows that this drug is generally well tolerated, with an acceptable bene®t± risk ratio when used in accordance with the prescribing information. As noted by the authors, sumatriptan and other triptans should not be given to patients with, or at high risk for, coronary or cerebrovascular disease.An important safety issue that was not discussed in the article is that data have recently been presented which might be misinterpreted by those not expert in the ®eld as showing that some triptans may have improved cardiovascular safety. These include the use of cranialcoronary contraction ratios from isolated vessel preparations (2), ECG studies in patients at risk of or with frank coronary artery disease that show negative results (3), or citing lower incidence of chest symptoms seen in clinical studies (4). We are concerned that the general medical community might perceive these data as implying a cardiovascular safety bene®t for one triptan over another. We would like to emphasize to your readers that all triptans are contraindicated in patients with coronary artery disease and it would be very unwise at this point to conclude that one triptan is safer than another. Also, given the typical patient population with migraine, focusing on the perception of cardiovascular safety for the triptan class only serves as a distraction from the real work at hand, which includes effective recognition of migraine and appropriate management strategies.

show abstract

Craniovascular selectivity of eletriptan and sumatriptan in human isolated blood vessels

Cited by 3 publications

References 4 publications

Headache, Cerebral Aneurysms, and the Use of Triptans and Ergot Derivatives

Headache, Cerebral Aneurysms, and the Use of Triptans and Ergot Derivatives

Tolerability of Sumatriptan: Clinical Trials and Postmarketing Experience

Tolerability of Sumatriptan: Clinical Trials and Postmarketing Experience

Contact Info

Product

Resources

About