Vascular effects of 5-HT-receptor agonists in patients with migraine headaches

Abstract

Selective 5-HT1B/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.

Effects of 5-HT1B/1D Receptor Agonist Rizatriptan on Cerebral Blood Flow and Blood Volume in Normal Circulation

“…This is presumably due to the flow-induced vasodilatation in the smaller arteries known to be not affected by triptans (de Hoon et al, 2000). A small but significant decrease of CBF in earlier phase after treatment might have caused the vasodilatory response in cerebral circulation.…”

“…The therapeutic vasoconstrictor effect of triptans presumably acts by counterbalancing the vasodilation of major vessels that might be responsible to induce headache. However, the flowinduced vasodilation in peripheral circulation is not affected by these drugs (Feniuk et al, 1989;Williamson et al, 1997;de Hoon et al, 2000). Although patients with migraine did not show changes in CBF after treatment with sumatriptan (Friberg et al, 1991), triptans may induce small changes in CBF and blood volume as a result of vasoconstriction in the major cerebral arteries, followed by reduction in arterial perfusion pressure.…”

“…Triptans have been used for migraine treatment, and several investigations reported that their vasoconstrictor effect counteracted vasodilatory changes in migraine headache (Friberg et al, 1991;Caekebeke et al, 1992). Both animal experiments and isolated human arteries, as well as clinical studies, reported their direct vasoconstrictor effect on various vessels (Feniuk et al, 1989;Parsons et al, 1989;Longmore et al, 1998), and the drug-induced vasoconstriction lasted for 1.5 h after drug administration in patients (de Hoon et al, 2000). In the latter study, the change in diameter of the CCA at 1.5 h from drug administration was significant but relatively small, and the resistance of the CCA was not different compared with placebo treatment.…”

A Review of the Pharmacokinetics, Pharmacodynamics and Efficacy of Zolmitriptan in the Acute Abortive Treatment of Migraine

“…In addition, 5-HT 1B receptor activation of the vascular smooth muscle results in intracranial, coronary and peripheral vasoconstriction of vessels. 9,13 The 5-HT 1D receptor sites are found on nerve terminals predominantly in the extrapyramidal pathways but also in the hippocampus, dorsal nucleus raphe and the cerebral cortex. 12 Similar to the 5-HT 1B receptors, 5-HT 1D receptors mediate inhibition of the release of 5-HT.…”

“…Centrally, triptans inhibit excitability of cells in the trigeminal nucleus caudalis via 5-HT 1D agonism. 13,17 Specifi cally, zolmitriptan has also been shown to decrease the neuropeptides, calcitonin generelated peptide (CGRP) and vasoactive intestinal polypeptide (VIP) following stimulation of the trigeminal ganglion in both animal and human models. 15,19 This mechanism is consistent with an inhibition of pre-junctional receptors on perivascular afferent fi bers of the trigeminal nerve.…”