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Antimigraine Drugs

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Carlos M. Villalón – One of the best experts on this subject based on the ideXlab platform.

  • activation of 5 hydroxytryptamine1b 1d 1f receptors as a mechanism of action of Antimigraine Drugs
    Expert Opinion on Pharmacotherapy, 2013
    Co-Authors: Martha Ramirez B Rosas, Sieneke Labruijere, Carlos M. Villalón, Antoinette Maassen Vandenbrink

    Abstract:

    Introduction: The introduction of the triptans (5-hydroxytryptamine (5-HT)1B/1D receptor agonists) was a great improvement in the acute treatment of migraine. However, shortcomings of the triptans have prompted research on novel serotonergic targets for the treatment of migraine. Areas covered: In this review the different types of Antimigraine Drugs acting at 5-HT receptors, their discovery and development are discussed. The first specific Antimigraine Drugs were the ergot alkaloids, consisting of ergotamine, dihydroergotamine and methysergide, which are agonists at 5-HT receptors, but can also bind α-adrenoceptors and dopamine receptors. In the 1990s, the triptans became available on the market. They are 5-HT1B/1D receptor agonists, showing fewer side effects due to their receptor specificity. In the last years, compounds that bind specifically to 5-HT1D, 5-HT1F and 5-HT7 receptors have been explored for their Antimigraine potential. Furthermore, the serotonergic system seems to act in tight connection …

  • Activation of 5-hydroxytryptamine1B/1D/1F receptors as a mechanism of action of Antimigraine Drugs.
    Expert Opinion on Pharmacotherapy, 2013
    Co-Authors: Martha B. Ramírez Rosas, Carlos M. Villalón, Sieneke Labruijere, Antoinette Maassen Vandenbrink

    Abstract:

    Introduction: The introduction of the triptans (5-hydroxytryptamine (5-HT)1B/1D receptor agonists) was a great improvement in the acute treatment of migraine. However, shortcomings of the triptans have prompted research on novel serotonergic targets for the treatment of migraine. Areas covered: In this review the different types of Antimigraine Drugs acting at 5-HT receptors, their discovery and development are discussed. The first specific Antimigraine Drugs were the ergot alkaloids, consisting of ergotamine, dihydroergotamine and methysergide, which are agonists at 5-HT receptors, but can also bind α-adrenoceptors and dopamine receptors. In the 1990s, the triptans became available on the market. They are 5-HT1B/1D receptor agonists, showing fewer side effects due to their receptor specificity. In the last years, compounds that bind specifically to 5-HT1D, 5-HT1F and 5-HT7 receptors have been explored for their Antimigraine potential. Furthermore, the serotonergic system seems to act in tight connection …

  • role of 5 ht1b 1d receptors in the reduction of formalin induced nociception and secondary allodynia hyperalgesia produced by Antimigraine Drugs in rats
    Life Sciences, 2013
    Co-Authors: Beatriz Godinezchaparro, Carlos M. Villalón, Francisco J Lopezsantillan, Carlos F Arguelles, Vinicio Granadossoto

    Abstract:

    Abstract Aims The present study analyzed the potential antinociceptive effect of the Antimigraine Drugs sumatriptan, dihydroergotamine or methysergide in rats submitted to the formalin test. Moreover, by using selective antagonists, the role of 5-HT 1B/1D serotonergic receptors was investigated in the antinociception induced by these Antimigraine Drugs. Main methods The formalin test was used to assess the nociceptive activity. Overt pain-like behavior (flinching, 1 h) and evoked nociception (long-lasting secondary mechanical allodynia and hyperalgesia, 6 days) were determined in the same rat. Key findings Ipsilateral, but not contralateral, pre-treatment (in μg/paw) with sumatriptan (10–300), methysergide (1–30) or dihydroergotamine (1–30) significantly prevented flinching behavior (at 1 h) as well as secondary allodynia and hyperalgesia (at day 6) induced by formalin. Interestingly, the antinociceptive (flinching), antiallodynic and antihyperalgesic effects of sumatriptan were completely prevented by peripheral pre-treatment with selective antagonists at the 5-HT 1B (SB 224289; 100) or 5-HT 1D (BRL 15572; 100) receptors. In contrast, the acute antinociceptive effects of methysergide and dihydroergotamine were partially prevented by SB 224289 and BRL 15572. The antiallodynic and antihyperalgesic effects of both Drugs were completely prevented by BRL 15572 and partially prevented by SB 224289. Given alone, SB 224289 or BRL 15572 did not modify per se the long-lasting secondary allodynia and hyperalgesia. Significance The above findings suggest that: (i) the Antimigraine Drugs sumatriptan, methysergide and dihydroergotamine reduce the acute and chronic nociception induced by formalin; and (ii) this antinociceptive effect results from activation of peripheral 5-HT 1B/1D serotonergic receptors.

Antoinette Maassenvandenbrink – One of the best experts on this subject based on the ideXlab platform.

  • the need for new acutely acting Antimigraine Drugs moving safely outside acute medication overuse
    Journal of Headache and Pain, 2019
    Co-Authors: Willem Sebastiaan Van Hoogstraten, Antoinette Maassenvandenbrink

    Abstract:

    The treatment of migraine is impeded by several difficulties, among which insufficient headache relief, side effects, and risk for developing medication overuse headache (MOH). Thus, new acutely acting Antimigraine Drugs are currently being developed, among which the small molecule CGRP receptor antagonists, gepants, and the 5-HT1F receptor agonist lasmiditan. Whether treatment with these Drugs carries the same risk for developing MOH is currently unknown. Pathophysiological studies on MOH in animal models have suggested that decreased 5-hydroxytryptamine (5-HT, serotonin) levels, increased calcitonin-gene related peptide (CGRP) expression and changes in 5-HT receptor expression (lower 5-HT1B/D and higher 5-HT2A expression) may be involved in MOH. The decreased 5-HT may increase cortical spreading depression frequency and induce central sensitization in the cerebral cortex and caudal nucleus of the trigeminal tract. Additionally, low concentrations of 5-HT, a feature often observed in MOH patients, could increase CGRP expression. This provides a possible link between the pathways of 5-HT and CGRP, targets of lasmiditan and gepants, respectively. Since lasmiditan is a 5-HT1F receptor agonist and gepants are CGRP receptor antagonists, they could have different risks for developing MOH because of the different (over) compensation mechanisms following prolonged agonist versus antagonist treatment. The acute treatment of migraine will certainly improve with the advent of two novel classes of Drugs, i.e., the 5-HT1F receptor agonists (lasmiditan) and the small molecule CGRP receptor antagonists (gepants). Data on the effects of 5-HT1F receptor agonism in relation to MOH, as well as the effects of chronic CGRP receptor blockade, are awaited with interest.

  • a human trigeminovascular biomarker for Antimigraine Drugs a randomised double blind placebo controlled crossover trial with sumatriptan
    Cephalalgia, 2017
    Co-Authors: Khalil Ibrahimi, Alexander H. J. Danser, Gisela M Terwindt, Anton H Van Den Meiracker, Antoinette Maassenvandenbrink

    Abstract:

    Current Antimigraine Drugs are believed, besides their direct vasoconstrictive effect, to inhibit calcitonin gene-related peptide (CGRP) release from trigeminal nerve endings during migraine.Object…

  • A human trigeminovascular biomarker for Antimigraine Drugs: A randomised, double-blind, placebo-controlled, crossover trial with sumatriptan.
    Cephalalgia : an international journal of headache, 2016
    Co-Authors: Khalil Ibrahimi, Alexander H. J. Danser, Gisela M Terwindt, Ah Van Den Meiracker, Antoinette Maassenvandenbrink

    Abstract:

    Current Antimigraine Drugs are believed, besides their direct vasoconstrictive effect, to inhibit calcitonin gene-related peptide (CGRP) release from trigeminal nerve endings during migraine. Objective The objective of this report is to establish a biomarker for the CGRP-interfering effect of Antimigraine Drugs. Methods We quantified the effect of sumatriptan on the trigeminal nerve-mediated rise in forehead dermal blood flow (DBF), induced by capsaicin application (0.6 mg/ml) and electrical stimulation (0.2-1.0 mA), in a randomised, double-blind, placebo-controlled, crossover study in healthy male ( n = 11, age ± SD: 29 ± 8 years) and female ( n = 11, 32 ± 7 years) individuals. Results DBF responses to capsaicin were attenuated by sumatriptan (ΔDBF, mean ± SEM: 82 ± 18 AU, p = 0.0002), but not by placebo (ΔDBF: 21 ± 12 AU, p = 0.1026). Conclusion We demonstrated that sumatriptan inhibits increases in DBF, induced by the release of, most likely, CGRP. Thus, our model may be used as a biomarker to establish the trigeminovascular effects of (potential) Antimigraine Drugs, such as CGRP receptor antagonists or antibodies directed against CGRP or its receptor.

Richard Hargreaves – One of the best experts on this subject based on the ideXlab platform.

  • differential effects of the 5ht1b 1d receptor agonist naratriptan on trigeminal versus spinal nociceptive responses
    Cephalalgia, 1998
    Co-Authors: Michael J Cumberbatch, Raymond G. Hill, Richard Hargreaves

    Abstract:

    In vivo electrophysiological assays in anesthetized rats have been used to compare the effects of the 5HT1B/1D receptor agonist, naratriptan, on central trigeminal nociceptive processing from dural and cutaneous inputs with its effects on nociceptive processing in the spinal cord. Naratriptan inhibited responses of single trigeminal neurons, to noxious electrical and mechanical stimulation of the dura and face, dose dependently by a maximum of 67+/-3% and 70+/-18%, respectively, at 3 mg kg(-1) i.v. In contrast, naratriptan did not affect spinal dorsal horn neuronal responses to noxious mechanical stimulation of the hind-paw. These findings suggest that 5HT1B/1D receptors have differential effects on nociceptive processing in the trigeminal versus spinal dorsal horns and provide a potential explanation for the lack of general analgesic effects of brain penetrant 5HT(1B/1D) agonist Antimigraine Drugs.

  • Differential Effects of the 5Ht1B/1D Receptor Agonist Naratriptan on trigeminal Versus Spinal Nociceptive Responses
    Cephalalgia, 1998
    Co-Authors: Michael J Cumberbatch, Raymond G. Hill, Richard Hargreaves

    Abstract:

    In vivo electrophysiological assays in anesthetized rats have been used to compare the effects of the 5HT1B/1D receptor agonist, naratriptan, on central trigeminal nociceptive processing from dural and cutaneous inputs with its effects on nociceptive processing in the spinal cord. Naratriptan inhibited responses of single trigeminal neurons, to noxious electrical and mechanical stimulation of the dura and face, dose dependently by a maximum of 67+/-3% and 70+/-18%, respectively, at 3 mg kg(-1) i.v. In contrast, naratriptan did not affect spinal dorsal horn neuronal responses to noxious mechanical stimulation of the hind-paw. These findings suggest that 5HT1B/1D receptors have differential effects on nociceptive processing in the trigeminal versus spinal dorsal horns and provide a potential explanation for the lack of general analgesic effects of brain penetrant 5HT(1B/1D) agonist Antimigraine Drugs.