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Vascular effects of 5‐HT 1B/1D ‐receptor agonists in patients with migraine headaches
Author(s) -
Hoon Jan N. J. M.,
Willigers Jean M.,
Troost Jaap,
StruijkerBoudier Harry A. J.,
Bortel Luc M. A. B.
Publication year - 2000
Publication title -
clinical pharmacology and therapeutics
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.941
H-Index - 188
eISSN - 1532-6535
pISSN - 0009-9236
DOI - 10.1067/mcp.2000.110502
Subject(s) - zolmitriptan , medicine , sumatriptan , triptans , rizatriptan , anesthesia , placebo , vasodilation , migraine , brachial artery , cardiology , blood pressure , agonist , receptor , alternative medicine , pathology
Objectives Second‐generation triptans are believed to have fewer cardiovascular effects than sumatriptan. This was investigated in vivo by comparing the vascular effects of equipotent therapeutic dosages of selective 5‐HT 1B/1D ‐receptor agonists. Methods Sixteen patients with migraine headaches completed a double‐blind, placebo‐controlled, four‐way crossover study. With ultrasonography and applanation tonometry used 1.5 hours after the oral intake of sumatriptan (50 mg), rizatriptan (10 mg), zolmitriptan (2.5 mg), or placebo arterial vessel wall properties, blood flow and pressure waveforms were measured in common carotid, brachial, and temporal arteries. At the brachial artery, flow‐induced vasodilation (an endothelium‐dependent process) was evaluated, and blood pressures were recorded. Results Mean arterial pressure, 91 ± 2 mm Hg after placebo, increased (P < .05) by 4% to 6% after administration of each triptan. Each active treatment decreased (P < .001) both brachial and carotid artery diameter. Isobaric compliance of the brachial artery, 0.077 ± 0.010 mm 2 /kPa after placebo, decreased (P < .01) by 11% ± 8%, 11% ± 11%, and 23% ± 7% after administration of sumatriptan, rizatriptan, and zolmitriptan, respectively. Isobaric compliance of the carotid artery was 1.31 ± 0.10 mm 2 /kPa after placebo (no change). Zolmitriptan was the only triptan that decreased temporal artery diameter significantly (by 12% ± 3%, P < .001). The resistance of the temporal artery vascular bed increased after administration of sumatriptan (by 26% ± 11%, P < .05) and zolmitriptan (by 40% ± 9%, P = .001). Flow‐induced vasodilation was unaffected. Conclusions Selective 5‐HT 1B/1D ‐receptor agonists induce vasoconstriction and decrease compliance of conduit arteries. These effects are more pronounced at muscular (temporal, brachial) compared with elastic (carotid) arteries. Resistance is only increased at the temporal artery vascular bed, suggesting cranioselectivity for resistance vessels. Endothelial function is not differently affected by any of the triptans tested. (Clin Pharmacol Ther 2000;68:418‐26.) Clinical Pharmacology & Therapeutics (2000) 68 , 418–426; doi: 10.1067/mcp.2000.110502