Sumatriptan

BACKGROUND: Serotonin receptors 5-HT1B and 5-HT1D in the cerebral arteries are activated by the 5-hydroxytryptophan agonists (triptans) to relieve the discomfort associated with migraines. Even though triptans are often used to treat acute migraines, there is some debate over their effectiveness. OBJECTIVES: Our systematic review aimed to evaluate the effectiveness of triptans acute treatment of migraine in young individuals. METHODS: Utilizing the databases of Google Scholar, Cochrane Library, and PubMed, a literature search was conducted, and all papers published till July 2022 were included...

A 56-year-old man presented to the clinic with episodic headaches for several years which had been worsening over a few months prior to the presentation. He described headache as sharp, stabbing pain around the left eye associated with nausea, vomiting, photophobia, and phonophobia lasting for hours associated with flushing on the left side of the face. The picture of his face during these episodes showed flushing of the left side of the face, ptosis of the right eyelid, and miosis (panel A). Flushing in his face would resolve with the abortion of the headache...

As a primary headache disorder, cluster headache (CH) is a severe unilateral headache that recurs at certain times of the year, such as during season changes. It is characterized by autonomic symptoms, such as ipsilateral lacrimal and nasal discharge, as well as an inability to stay still during headache attacks. We report a rare case of CH in a 67-year-old male who presented with a severe right-sided headache lasting 30 minutes to one hour and occurring only during sleep. The headache resolved within five minutes after the subcutaneous injection of sumatriptan and was not accompanied by any autonomic symptoms or clear agitation...

Headaches are one of the most frequent reasons people visit the neurology department. In 2019, headache issues ranked as the 14th most common cause of disability-adjusted life years globally. According to the International Headache Society, migraine is a particular type of headache that is unilateral, frequently throbbing, associated with vertigo, and sensitive to light, sound, and head movement. A migraine has four stages: premonitory, aura, headache, and postdrome. Migraine is the type of discomfort that most frequently complicates the pregnancy...

INTRODUCTION: Patients are seeking greater involvement in their healthcare. It therefore may be beneficial to provide guidance on initial oral sumatriptan dose selection for the treatment of acute migraine in nontraditional settings, such as telehealth and other remote forms of medical care. We sought to determine whether clinical or demographic factors are predictive of oral sumatriptan dose preference. METHODS: This was a post hoc analysis of two clinical studies designed to determine preference for 25, 50, or 100 mg oral sumatriptan...

Abdominal migraine (AM) is a common childhood disease that rarely presents in adulthood. While multiple diagnostic guidelines have been established, AM can generally be described as unprovoked episodes of acute central abdominal pain with migrainous features and periods of relief. AM is believed to be caused by a disturbance in the gut-brain axis. We are presenting a case of a 47-year-old Caucasian female with a six-month history of abdominal pain and vomiting. The episodes occurred one to two times per week, for 12-18 hours...

INTRODUCTION: Membrane transporters are now widely recognized for their role in the absorption, distribution, clearance and elimination of drugs. The organic cation transporters (OCTs, SLC22A) are expressed in the intestine, liver and kidneys and are of importance in determining systemic pharmacokinetics and tissue-specific exposure of drugs and metabolites. AREAS COVERED: An overview of the role of OCTs in drug disposition is presented. Genetic variation in OCTs and the effects on pharmacokinetics and drug response were discussed...

BACKGROUND: Headache is a common presenting condition for patients seen in the pediatric emergency department (ED). Intranasal (IN) sumatriptan is a well-tolerated and safe abortive treatment for migraine headache, but it is infrequently administered in pediatric EDs. In this study we characterize an ED migraine pathway that uses IN sumatriptan as a first-line treatment. METHODS: We performed retrospective chart analysis from a single center, reviewing a cohort of patients treated on an ED migraine pathway between October 2016 and February 2020...

BACKGROUND: Mesenteric ischemia has remained without effective pharmacological management for many years. Sumatriptan, an abortive medication for migraine and cluster headaches, has potent anti-inflammatory properties and ameliorated organ ischemia in previous animal studies. Similarly, inhibition of the kynurenine pathway ameliorated renal and myocardial ischemia/reperfusion (I/R) in many preclinical studies. Herein, we assessed the effect of sumatriptan on experimental mesenteric I/R and investigated whether kynurenine pathway inhibition is a mechanism underlying its action...

BACKGROUND: As episodes of acute migraine for migraineurs, a self-treatment that promptly relieves headaches and eliminates the associated symptoms would be optimal. Based on the consideration, a rapidly dissolving double-layer microneedles derived from natural acacia was developed. METHODS: Under the optimized reaction conditions that was screened out through orthogonal designing test, acacia (GA) was conducted on the ionic crosslinking, a prescribed amount of cross-linking composites was applied to fabricate the double-layer microneedles loaded with sumatriptan at the tip...

Previous clinical and basic studies have shown that migraine is associated with cognitive impairment, anxiety, and depression. It severely affects the quality of life. In this study, C57BL/6 mice were randomly divided into four groups: IS group, IS+M group, and IS+S group with repeated application of dural inflammatory soup (IS) stimulation to establish a migraine model, followed by PBS, memantine, and sumatriptan interventions, respectively; the blank control group underwent the same treatment procedure but with PBS instead of IS and intervention drugs...

Ritlecitinib, an inhibitor of Janus kinase (JAK)3 and hepatocellular carcinoma family kinases, is in development as potential treatment for several inflammatory diseases. In vitro studies presented ritlecitinib as an inhibitor of hepatic organic cation transporter (OCT)1, renal transporters OCT2 and multidrug and toxin extrusion (MATE) proteins 1/2K using multiple substrates, and ritlecitinib's major inactive metabolite M2, as an inhibitor of OCT1. A clinical interaction study with an OCT1 drug probe (sumatriptan) and relevant probe biomarkers for OCT/MATE was conducted to assess the effect of ritlecitinib on these transporters in healthy adult participants...

Objective Little is known about the prevalence and characteristics of chronic cluster headache (CCH) in Japan. We therefore characterized the clinical profile of CCH in Japan by surveying patients with CCH who were registered at a Japanese regional headache center. We also reviewed the existing literature for the prevalence and clinical characteristics of CCH reported in various populations. Methods In this single-center retrospective study, we assessed consecutive patients with cluster headache (CH) who visited a regional tertiary headache center between February 2011 and July 2020...

BACKGROUND: The response to cluster headache treatments has a high interindividual variation. To date, treatment response has only been assessed by candidate gene approach and no investigations into metabolic pathways have been performed. To investigate the association between polygenetic risk of cluster headache and treatment response to first line cluster headache treatments as well as known functional variants of CYP3A4 and the response to verapamil. Further, to replicate previous single nucleotide polymorphisms found to be associated with treatment response in cluster headache and/or migraine...

Background: For many years triptans have been the cornerstone of acute migraine treatment. Nevertheless, treatment with triptans may not always be initiated due to contraindications (seen in approximately one fifth of patients) or inadequate response (seen in approximately one third of patients). New acute therapies, including 5-hydroxytryptamine (5-HT)1F receptor agonists, also known as ditans (lasmiditan) and small molecule antagonists of the calcitonin gene-related peptide receptor, also known as gepants (rimegepant and ubrogepant), may be an effective alternative...

Multidrug and toxin extrusion protein (MATE/SLC47A) secretes metabolites and xenobiotics into the urine in the proximal tubules of the kidney. Uptake assays have been commonly used for evaluating MATE-mediated transport of new chemical entities in drug development. The purpose of this study was to examine the relationship between in vitro uptake activities by MATEs and the impact of MATE-mediated transport in in vivo renal secretion. In vitro uptake in mouse Mate1- (mMate1) expressing HEK293 cells and several in vivo parameters from mMate1 knockout and wild type mice were compared using nine cationic compounds (almotriptan, naratriptan, talinolol, sumatriptan, alogliptin, sitagliptin, rivaroxaban, saxagliptin, and vildagliptin)...

Scientific literature describes that sumatriptan is metabolized by oxidative deamination of its dimethylaminoethyl residue by monoamine oxidase A (MAO A) and not by cytochrome P450 (CYP)-mediated demethylation, as is usual for such structural elements. Using recombinant human enzymes and HPLC-MS analysis, we found that CYP enzymes may also be involved in the metabolism of sumatriptan. The CYP1A2, CYP2C19, and CYP2D6 isoforms converted this drug into N-desmethyl sumatriptan, which was further demethylated to N,N-didesmethyl sumatriptan by CYP1A2 and CYP2D6...

UNLABELLED: Several tribal medicinal systems assert anti-migraine and common headache-remedying properties in all parts of Priva cordifolia (L.f.) Druce. Therefore, there are no clear scientific references to the validated traditional use of this plant. The present study provides a scientific basis for the ethnobotanical utility of P. cordifolia whose whole-plant extracts were evaluated against target proteins (PACAP 38 and PAC1-R) that cause migraine. Understanding the polarity-based distribution and oxidative stress scavenging ability was reported higher in ethyl acetate extracts due to the moderate distribution of secondary metabolites...

Although migraine is one of the most common chronic diseases and is the subject of numerous studies, there is still a considerable proportion of patients who are not satisfied with their acute treatment. Left without any real new therapeutic option to offer patients since sumatriptan was introduced on the Belgian market 30 years ago, neurologists have recently seen a change in the therapeutic landscape with the advent of new specific acute treatments for migraine: gepants and ditans. Being the only ones currently available in Belgium, gepants (including the newly marketed rimegepant) bring added value to traditional treatments such as non-steroidal anti-inflammatory drugs and triptans...

Posttraumatic headache (PTH) attributed to traumatic brain injury (TBI) is a secondary headache developed within 7 days after head injury, and in a substantial number of patients PTH becomes chronic and lasts for more than 3 months. Current medications are almost entirely relied on the treatment of primary headache such as migraine, due to its migraine-like phenotype and the limited understanding on the PTH pathogenic mechanisms. To this end, increasing preclinical studies have been conducted in the last decade...