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Marta Vila-Pueyo
Migraine is a common neurological disease characterised by the presence of attacks of unilateral, severe head pain accompanied by other symptoms. Although it has been classified as the sixth most disabling disorder, the available therapeutic options to treat this condition have not progressed accordingly. The advance in the development of 5-HT1 receptor agonists for migraine, including 5-HT1B/D and 5-HT1F receptor agonists, has meant a major step forward towards the progression of a better treatment for migraine...
April 2018: Neurotherapeutics: the Journal of the American Society for Experimental NeuroTherapeutics
José Ángel García-Pedraza, Oswaldo Hernández-Abreu, Mónica García, Asunción Morán, Carlos M Villalón
Serotonin (5-hydroxytryptamine; 5-HT) inhibits the rat cardioaccelerator sympathetic outflow by 5-HT1B/1D/5 receptors. Because chronic blockade of sympatho-excitatory 5-HT2 receptors is beneficial in several cardiovascular pathologies, this study investigated whether sarpogrelate (a 5-HT2 receptor antagonist) alters the pharmacological profile of the above sympatho-inhibition. Rats were pretreated for 2 weeks with sarpogrelate in drinking water (30 mg/kg per day; sarpogrelate-treated group) or equivalent volumes of drinking water (control group)...
April 2018: Canadian Journal of Physiology and Pharmacology
José-Ángel García-Pedraza, Mónica García-Domingo, Miriam Gómez-Roso, Alicia Rodríguez-Barbero, María-Luisa Martín, Asunción Morán
5-hydroxytryptamine (5-HT) modulates noradrenergic activity in different cardiovascular territories, but its effect on the mesenteric vasopressor outflow has not yet been clarified. This study investigated the in vivo serotonergic influence, characterizing 5-HT receptors implicated, in sympathetic innervation of mesenteric vasculature. Wistar rats were anaesthetised and prepared for the in situ autoperfused rat mesentery, monitoring systemic blood pressure (SBP), heart rate (HR) and mesenteric perfusion pressure (MPP)...
August 3, 2017: Clinical and Experimental Pharmacology & Physiology
Bianca Raffaelli, Heike Israel, Lars Neeb, Uwe Reuter
Migraine is among the most disabling disorders worldwide, with a significant therapeutic need. Triptans are drugs of choice in the acute attack treatment, but they are contraindicated in patients with vascular conditions due to their potential vasoconstrictive properties. Further limitations include side effects, inconsistency in therapeutic action and possible non-response. Lasmiditan, a highly selective 5-HT1F receptor agonist, is a novel acute anti-migraine substance devoid of vasoconstriction. Areas covered: This article reviews the clinical efficacy and safety of oral and intravenous lasmiditan as a possible acute migraine treatment...
September 2017: Expert Opinion on Pharmacotherapy
Anna Steinberg, Simona D Frederiksen, Frank W Blixt, Karin Warfvinge, Lars Edvinsson
BACKGROUND: Migraine and Cluster Headache (CH) are two primary headaches with severe disease burden. The disease expression and the mechanisms involved are poorly known. In some attacks of migraine and in most attacks of CH, there is a release of vasoactive intestinal peptide (VIP) originating from parasympathetic cranial ganglia such as the sphenopalatine ganglion (SPG). Patients suffering from these diseases are often deprived of effective drugs. The aim of the study was to examine the localization of the botulinum toxin receptor element synaptic vesicle glycoprotein 2A (SV-2A) and the vesicular docking protein synaptosomal-associated protein 25 (SNAP25) in human and rat SPG...
December 2016: Journal of Headache and Pain
Paolo Palatini, Elisabetta Benetti, Lucio Mos, Guido Garavelli, Adriano Mazzer, Susanna Cozzio, Claudio Fania, Edoardo Casiglia
Whether and how coffee use influences glucose metabolism is still a matter for debate. We investigated whether baseline coffee consumption is longitudinally associated with risk of impaired fasting glucose in a cohort of 18-to-45 year old subjects screened for stage 1 hypertension and whether CYP1A2 polymorphism modulates this association. A total of 1,180 nondiabetic patients attending 17 hospital centers were included. Seventy-four percent of our subjects drank coffee. Among the coffee drinkers, 87% drank 1-3 cups/day (moderate drinkers), and 13% drank over 3 cups/day (heavy drinkers)...
March 2015: European Journal of Epidemiology
Maria Adele Giamberardino, Paolo Martelletti
INTRODUCTION: Migraine is a highly prevalent and disabling neurological condition whose personal, social and economic impact is substantial. Abortive and preventative treatments of this condition are still unsatisfactory, with poor control of the acute symptoms of the single attacks in many cases and a frequent progression towards chronicity. AREAS COVERED: The major drug classes recently developed and/or in current development for migraine treatment are discussed...
March 2015: Expert Opinion on Emerging Drugs
Jan Hoffmann, Peter J Goadsby
Migraine is a common and highly disabling neurological disorder. Despite the complexity of its pathophysiology, substantial advances have been achieved over the past 20 years in its understanding, as well as the development of pharmacological treatment options. The development of serotonin 5-HT(1B/1D) receptor agonists ("triptans") substantially improved the acute treatment of migraine attacks. However, many migraineurs do not respond satisfactorily to triptans and cardiovascular co-morbidities limit their use in a significant number of patients...
January 2014: CNS Drugs
Martha B Ramírez Rosas, Sieneke Labruijere, Carlos M Villalón, Antoinette Maassen Vandenbrink
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...
August 2013: Expert Opinion on Pharmacotherapy
S D Silberstein
Migraine is a primary brain disorder resulting from altered modulation of normal sensory stimuli and trigeminal nerve dysfunction. The second edition of the International Classification of Headache Disorders (ICHD-2) defines seven subtypes of migraine. Migraine treatment can be acute or preventive. New targeted therapies include 5-HT(1F) receptor agonists, calcitonin gene-related peptide (CGRP) antagonists, nitric oxide synthetase inhibitors, and ion channel antagonists. A recent development is the creation of antibodies to CGRP and its receptor for migraine prevention...
January 2013: Clinical Pharmacology and Therapeutics
Alan M Rapoport
There are many categories and individual types of headache and most have a variety of treatment protocols, while a few are best treated by just one medication. This paper will concentrate on acute care medications for migraine and discuss some new and future acute care treatments. There is not much to discuss about prevention, except that onabotulinumtoxinA has been approved for prevention of chronic migraine. Cluster headache will also be discussed, as there are some future treatments for acute care and prevention being studied at present...
May 2012: Neurological Sciences
Markus Färkkilä, Hans-Christoph Diener, Gilles Géraud, Miguel Láinez, Jean Schoenen, Nadja Harner, Alison Pilgrim, Uwe Reuter
BACKGROUND: Lasmiditan (COL-144) is a novel, centrally acting, highly selective 5-HT(1F) receptor agonist without vasoconstrictor activity that seemed effective when given as an intravenous infusion in a proof-of-concept migraine study. We aimed to assess the efficacy and safety of oral lasmiditan for the acute treatment of migraine. METHODS: In this multicentre, double-blind, parallel-group, dose-ranging study in 43 headache centres in five European countries, patients with migraine with and without aura and who were not using prophylaxis were randomly assigned (1:1:1:1:1) to treat one moderate or severe attack at home with 50 mg, 100 mg, 200 mg, or 400 mg lasmiditan, or placebo...
May 2012: Lancet Neurology
Carl Dahlöf, Antoinette Maassen Van Den Brink
The 5-hydroxytryptamine (5-HT) receptor family mediates the effects of several drugs highly effective in migraine primarily by activating 5-HT(1B) , 5-HT(1D) , and 5-HT(1F) receptors. Ergotamine, dihydroergotamine, and methysergide, as well as the "triptan" sumatriptan, are all agonists for these receptors. The receptor profile and degree of selectivity of these four drugs differ, which is reflected by their side effects that limit their use in the acute and prophylactic treatment of migraine. The acute antimigraine efficacy of these remedies is very much dependent on the formulation used where, in general, parenteral formulations are more effective in reliving the symptoms of a migraine attack...
April 2012: Headache
Peer C Tfelt-Hansen, Jes Olesen
Lasmiditan is a novel selective 5-HT(1F) receptor agonist. It is both scientifically and clinically relevant to review whether a 5-HT(1F) receptor agonist is effective in the acute treatment of migraine. Two RCTs in the phase II development of lasmiditan was reviewed. In the intravenous placebo-controlled RCT, lasmiditan doses of 2.5-45 mg were used, and there was a linear association between headache relief (HR) rates and dose levels (P < 0.02). For lasmiditan 20 mg, HR was 64 % and for placebo it was 45 % (NS)...
June 2012: Journal of Headache and Pain
Richard Peatfield
What Happens to the Old Headache Medicines? Rapoport AM, MD. Old headache medicines never die; they either fade away or come back in disguise. The disguise is often a new route of administration, which may work better, faster, more completely, with fewer adverse events, and/or have certain other advantages. The clinical aspects of 3 of the oldest headache medicines (ergotamine tartrate, dihydroergotamine, and methysergide) will be discussed here. Sumatriptan will then be discussed as the prototype of the newest category of acute care therapy (triptans) for migraine...
April 2012: Headache
Dipak V Amrutkar, Kenneth B Ploug, Anders Hay-Schmidt, Frank Porreca, Jes Olesen, Inger Jansen-Olesen
Triptans, a family of 5-hydroxytryptamine (5-HT) 1B, 1D, and 1F receptor agonists, are used in the acute treatment of migraine attacks. The site of action and subtypes of the 5-HT(1) receptor that mediate the antimigraine effect have still to be identified. This study investigated the mRNA expression of these receptors and the role of 5-HT(1) receptor subtypes in controlling the release of calcitonin gene-related peptide (CGRP) in rat dura mater, trigeminal ganglion (TG), and trigeminal nucleus caudalis (TNC)...
April 2012: Pain
M T Klein, M Teitler
BACKGROUND AND PURPOSE: The 5-ht(1E) receptor is highly expressed in the human brain and its structure is conserved in humans, suggesting an important physiological role for 5-ht(1E) receptors. However, neither the function nor the distribution of this receptor has been characterized in the mammalian brain. EXPERIMENTAL APPROACH: Rats and mice lack the 5-ht(1E) receptor gene; thus, we used guinea pig brain tissue and immunofluorescent staining techniques to provide the first specific localization of 5-ht(1E) receptors in the mammalian brain...
June 2012: British Journal of Pharmacology
Hyo-Jin Jeong, Vanessa A Mitchell, Christopher W Vaughan
BACKGROUND AND PURPOSE: 5-HT receptor agonists have variable nociceptive effects within the spinal cord. While there is some evidence for 5-HT(1A) spinally-mediated analgesia, the role of other 5-HT(1) receptor subtypes remains unclear. In the present study, we examined the spinal actions of a range of 5-HT(1) agonists, including sumatriptan, on acute pain, plus their effect on afferent-evoked synaptic transmission onto superficial dorsal horn neurons. EXPERIMENTAL APPROACH: For in vivo experiments, 5-HT agonists were injected via chronically implanted spinal catheters to examine their effects in acute mechanical and thermal pain assays using a paw pressure analgesymeter and a Hargreave's device...
March 2012: British Journal of Pharmacology
Katherine C Murray, Marilee J Stephens, Michelle Rank, Jessica D'Amico, Monica A Gorassini, David J Bennett
Sensory afferent transmission and associated spinal reflexes are normally inhibited by serotonin (5-HT) derived from the brain stem. Spinal cord injury (SCI) that eliminates this 5-HT innervation leads to a disinhibition of sensory transmission and a consequent emergence of unusually long polysynaptic excitatory postsynaptic potentials (EPSPs) in motoneurons. These EPSPs play a critical role in triggering long polysynaptic reflexes (LPRs) that initiate muscles spasms. In the present study we examined which 5-HT receptors modulate the EPSPs and whether these receptors adapt to a loss of 5-HT after chronic spinal transection in rats...
August 2011: Journal of Neurophysiology
A Rapoport
There are numerous headache therapies available for our patients, more for migraine than for any of the other primary headache disorders. Only four medications have been approved for migraine prevention in the last few decades in the US and onabotulinumtoxinA was recently approved in the UK and the US for chronic migraine. We have been more fortunate in the acute care arena where in the US we have had seven triptans and one nonsteroidal anti-inflammatory medication approved by the FDA and currently available...
May 2011: Neurological Sciences
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