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Pharmacological Characterization of 5-Hydroxytryptamine Receptors in the Gastrointestinal Tract
Published in T.S. Gaginella, J.J. Galligan, SEROTONIN and GASTROINTESTINAL FUNCTION, 2020
Jeremy D. Gale, Keith T. Bunce
The only well-defined agonist at the 5-HT1D receptor is sumatriptan, where it is approximately 10 times less potent than 5-HT.9 Sumatriptan has approximately 10-fold selectivity for the 5-HT1D over the rat 5-HT1B receptor and demonstrates approximately 10- to 50-fold selectivity for 5-HT1D receptors over 5-HT1A receptors.53 This situation may be further complicated by recent reports that sumatriptan shows some binding affinity for the newest members of the 5-HT receptor family, which have been identified through molecular biological techniques.54,55 Whether this translates to functional activity has still to be demonstrated. When used in vivo it should be noted that sumatriptan only poorly penetrates the blood-brain barrier.
Chronic Headache Pain
Published in Andrea Kohn Maikovich-Fong, Handbook of Psychosocial Interventions for Chronic Pain, 2019
RuthAnn R. Lester, Eleanor S. Brammer, Allison Gray
Abortive treatment varies based upon headache type. Medications specific for acute treatment of migraine include triptans and ergots, with triptans generally considered first-line treatment (Becker, 2017). Triptans are 5-HT1b and 5-HT1d receptor agonists thought to work by causing vasoconstriction of the cerebral blood vessels and by decreasing the release of neuropeptides in the first and second order neurons of the trigeminal complex (Burnstein, Collins, & Jakubowski, 2004). Triptans theoretically can cause constriction of the coronary arteries as well, and for this reason should be avoided in patients with a history of stroke, coronary artery disease, or peripheral vascular disease. They also should be avoided generally with patients with hemiplegic or basilar migraines. Triptans also carry a risk of causing medication overuse headache when used too often, so their use must be regulated to two to three times per week at most.
Headache
Published in Peter R Wilson, Paul J Watson, Jennifer A Haythornthwaite, Troels S Jensen, Clinical Pain Management, 2008
Peer Tfelt-Hansen, Rigmor Jensen
The mechanisms of action of triptans in migraine are mainly constriction of dilated cranial extracerebral blood vessels,75 reduction of neuropeptide release and plasma protein extravasation across dural vessels,34 and inhibition impulse transmission centrally within the trigeminovascular system.76 However, the possible contribution of the neuronal effect of triptans, mediated via 5-HT1D receptor, has been put in doubt because PNU142633, a selective 5-HT1D receptor agonist, has not proved effective in the acute treatment of migraine.77
The current state of acute treatment for migraine in adults in the United States
Published in Postgraduate Medicine, 2020
Wade Cooper, Erin Gautier Doty, Helen Hochstetler, Ann Hake, Vincent Martin
Triptans (potent 5-HT1B/1D receptor agonists) are considered first-line treatment for moderate-to-severe migraine attacks [1]. Triptans specifically target the 5-HT1B and 5-HT1D receptor subtypes (some triptans also have an affinity for the 5-HT1F receptor subtype) [30]. Triptans were specifically developed for the acute treatment of migraine based on their ability to induce vasoconstriction through their agonism of the 5-HT1B receptor, at a time when migraine was believed to be a vascular disorder. Because of their vasoconstrictive properties, triptans are contraindicated in patients with cerebrovascular and cardiovascular disease.
Current understanding of the etiology of cyclic vomiting syndrome and therapeutic strategies in its management
Published in Expert Review of Clinical Pharmacology, 2022
Rosita Frazier, Thangam Venkatesan
Triptans work by selectively binding to serotonin receptors 5-hydroxytryptamine 1B (5-HT1B) which are located in the smooth muscle cells of blood vessels, leading to vasoconstriction of the cranial arteries and 5-hydroxytryptamine 1D (5-HT1D). When triptans bind to the neurogenic and central 5-HT1D receptors, they limit the transmission of pain signals to the brain and prevent the production of vasoactive neuropeptides by suppressing the activation of trigeminal nerves [78]. How triptans work in CVS is not known. However, many anti-migraine medications are as effective in CVS and could be due to a shared pathophysiology [79].
Are 5-HT1 receptor agonists effective anti-migraine drugs?
Published in Expert Opinion on Pharmacotherapy, 2021
Masaru Tanaka, Nóra Török, László Vécsei
Sumatriptan is the first clinically available drug introduced in 1991 among triptans (Figure 1). Sumatriptan is a 5-HT1B/D agonist, but its efficacy is considered based on its action on the 5-HT1D receptors, which leads to vasoconstriction of the basilar artery and the blood vessels of the dura mater, increasing blood flow velocity in the middle cerebral artery and the internal carotid artery, and reducing carotid arterial flow. Sumatriptan blocks the plasma leakage caused by vasoactive compounds including CGRP, substance P, and neurokinin A from the trigeminovascular neurons. However, the affinity to 5-HT1B precipitates vasoconstriction of the cerebral artery, which may limit the efficacy as an antimigraine agent and is responsible for uncomfortable side effects including a mild allergic reaction, such as flush (Table 1 and Table 2). Due to its peripheral vasoconstrictive action, furthermore, sumatriptan is contraindicated to patients who suffered from cardiovascular diseases, cerebrovascular diseases, and uncontrollable hypertension. Other triptans approved for clinical use are naratriptan, zolmitriptan, rizatriptan, almotriptan, frovatriptan, and eletriptan, which are indicated according to the age of migraineurs, the duration of migraine, or menstruation-induced migraine. The triptans are considered to act as antimigraine drugs by stimulating the presynaptic 5-HT1D receptor to inhibit the dural vasodilation and neurogenic inflammation, inhibiting the trigeminal nuclei cell excitability through 5-HT1B/D activation in the brainstem, and stimulating the vascular 5-HT1B receptors triggering meningeal, dural cerebral, and pial vasoconstriction. They are indicated for the acute phase of migraine attack and almotriptan is the only oral triptan approved for the treatment of migraine between 12 and 17 years old in the United States of America [4]. Main side effects of triptans are chest pressure or heaviness, flushing, weakness, drowsiness, dizziness, malaise, a feeling of warmth, and paresthesia.