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https://www.readbyqxmd.com/read/28527055/cluster-headache-present-and-future-therapy
#1
Massimo Leone, Alessandro Giustiniani, Alberto Proietti Cecchini
Cluster headache is characterized by severe, unilateral headache attacks of orbital, supraorbital or temporal pain lasting 15-180 min accompanied by ipsilateral lacrimation, rhinorrhea and other cranial autonomic manifestations. Cluster headache attacks need fast-acting abortive agents because the pain peaks very quickly; sumatriptan injection is the gold standard acute treatment. First-line preventative drugs include verapamil and carbolithium. Other drugs demonstrated effective in open trials include topiramate, valproic acid, gabapentin and others...
May 2017: Neurological Sciences
https://www.readbyqxmd.com/read/28527054/understanding-migraine-as-a-cycling-brain-syndrome-reviewing-the-evidence-from-functional-imaging
#2
Arne May
Due to the clinical picture and also based on early imaging data (Weiller et al. Nat Med 1:658-660, 1995), the brainstem and midbrain structures have been intensely discussed as possible driving or generating structures in migraine. The fact that the brainstem activation persisted after treatment makes it unlikely that this activation was only due to increased activity of the endogenous anti-nociceptive system. It was consequently (and somewhat simplifying) coined the "migraine generator". Since then several studies have focussed on this region when investigating episodic, but also chronic migraine...
May 2017: Neurological Sciences
https://www.readbyqxmd.com/read/28497569/early-onset-of-efficacy-and-consistency-of-response-across-multiple-migraine-attacks-from-the-randomized-compass-study-avp-825-breath-powered-%C3%A2-exhalation-delivery-system-sumatriptan-nasal-powder-vs-oral-sumatriptan
#3
Stephen Silberstein, Paul K Winner, Peter J McAllister, Stewart J Tepper, Rashmi Halker, Ramy A Mahmoud, Joao Siffert
OBJECTIVE: To further characterize the clinical utility of AVP-825 based on additional prespecified outcomes and post hoc analyses of COMPASS, a Phase 3 comparative efficacy trial of AVP-825 vs 100 mg oral sumatriptan (NCT01667679). AVP-825 was approved in January 2016 by the US Food and Drug Administration under the name ONZETRA(®) Xsail(®) (sumatriptan nasal powder) for the acute treatment of migraine with or without aura in adults. BACKGROUND: AVP-825 is a delivery system that uses a patient's own breath to deliver low-dose sumatriptan powder to the upper posterior regions of the nasal cavity beyond the narrow nasal valve, areas lined with vascular mucosa conducive to rapid drug absorption into the systemic circulation...
May 11, 2017: Headache
https://www.readbyqxmd.com/read/28376660/implementation-of-effective-self-sustaining-headache-services-in-the-republic-of-georgia-evaluation-of-their-impact-on-headache-related-disability-and-quality-of-life-of-people-with-headache
#4
Gvantsa Giorgadze, Maka Mania, Maka Kukava, Ana Dzagnidze, Ekaterine Mirvelashvili, Timothy J Steiner, Zaza Katsarava
Background Headache disorders are widespread and disabling. They are common in Georgia, especially headache on ≥15 days/month (HA ≥ 15), but there are no headache services. Objective We established headache services meeting local needs, investigating feasibility, consumer uptake and satisfaction, and cost, with an exit strategy bequeathing effective, self-sustaining services that could be rolled out nationwide. Methods We created headache centres in Tbilisi and Gori offering free expert care for three visits over three months, and affordable medication thereafter...
January 1, 2017: Cephalalgia: An International Journal of Headache
https://www.readbyqxmd.com/read/28376659/kappa-opioid-receptor-antagonists-a-possible-new-class-of-therapeutics-for-migraine-prevention
#5
Jennifer Y Xie, Milena De Felice, Caroline M Kopruszinski, Nathan Eyde, Justin LaVigne, Bethany Remeniuk, Pablo Hernandez, Xu Yue, Naomi Goshima, Michael Ossipov, Tamara King, John M Streicher, Edita Navratilova, David Dodick, Hugh Rosen, Ed Roberts, Frank Porreca
Background Stress is the most commonly reported migraine trigger. Dynorphin, an endogenous opioid peptide acting preferentially at kappa opioid receptors (KORs), is a key mediator of stress responses. The aim of this study was to use an injury-free rat model of functional cephalic pain with features of migraine and medication overuse headache (MOH) to test the possible preventive benefit of KOR blockade on stress-induced cephalic pain. Methods Following sumatriptan priming to model MOH, rats were hyper-responsive to environmental stress, demonstrating delayed cephalic and extracephalic allodynia and increased levels of CGRP in the jugular blood, consistent with commonly observed clinical outcomes during migraine...
January 1, 2017: Cephalalgia: An International Journal of Headache
https://www.readbyqxmd.com/read/28364968/-sphenopalatine-ganglion-block-for-postdural-puncture-headache-in-ambulatory-setting
#6
José Miguel Cardoso, Miguel Sá, Rita Graça, Hugo Reis, Liliana Almeida, Célia Pinheiro, Duarte Machado
BACKGROUND AND OBJECTIVES: Postdural puncture headache (PDPH) is a common complication following subarachnoid blockade and its incidence varies with the size of the needle used and the needle design. Supportive therapy is the usual initial approach. Epidural blood patch (EBP) is the gold-standard when supportive therapy fails but has significant risks associated. Sphenopalatine ganglion block (SPGB) may be a safer alternative. CASE REPORT: We observed a 41 year-old female patient presenting with PDPH after a subarachnoid blockade a week before...
March 30, 2017: Revista Brasileira de Anestesiologia
https://www.readbyqxmd.com/read/28361200/utilization-of-liver-microsomes-to-estimate-hepatic-intrinsic-clearance-of-monoamine-oxidase-substrate-drugs-in-humans
#7
Yusuke Masuo, Shushi Nagamori, Aoi Hasegawa, Kazuki Hayashi, Noriyoshi Isozumi, Noritaka Nakamichi, Yoshikatsu Kanai, Yukio Kato
PURPOSE: Monoamine oxidases (MAOs) are non-CYP enzymes that contribute to systemic elimination of therapeutic agents, and localized on mitochondrial membranes. The aim of the present study was to validate quantitative estimation of metabolic clearance of MAO substrate drugs using human liver microsomes (HLMs). METHODS: Three MAO substrate drugs, sumatriptan, rizatriptan and phenylephrine, as well as four CYP substrates were selected, and their disappearance during incubation with HLMs or mitochondria (HLMt) was measured...
June 2017: Pharmaceutical Research
https://www.readbyqxmd.com/read/28322941/small-dosing-clinical-study-pharmacokinetic-pharmacogenomic-slco2b1-and-abcg2-and-interaction-atorvastatin-and-grapefruit-juice-profiles-of-five-probes-for-oatp2b1-and-bcrp
#8
Yushi Kashihara, Ichiro Ieiri, Takashi Yoshikado, Maeda Kazuya, Masato Fukae, Miyuki Kimura, Takeshi Hirota, Shunji Matsuki, Shin Irie, Noritomo Izumi, Hiroyuki Kusuhara, Yuichi Sugiyama
The aims of this study were (1) to investigate the effects of atorvastatin (10 mg, therapeutic dose) and grapefruit juice (GFJ), inhibitors of OATP2B1, on the pharmacokinetics of substrates for OATP2B1 and BCRP under oral small-dosing conditions (300 μg sulfasalazine, 250 μg rosuvastatin, 300 μg glibenclamide, 1200 μg celiprolol, and 600 μg sumatriptan), and (2) to evaluate the contribution of SLCO2B1*3 and ABCG2 c.421C>A polymorphisms to the pharmacokinetics of the five test drugs in 23 healthy volunteers...
March 17, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28284933/synthesis-of-a-smart-ph-responsive-magnetic-nanocomposite-as-high-loading-carrier-of-pharmaceutical-agents
#9
Razieh Berah, Mohsen Ghorbani, Ali Akbar Moghadamnia
To create facile external controlled drug delivery system, a magnetic porous carrier based on Tin oxide nanoparticles was synthesized by an inexpensive and versatile hydrothermal strategy and used for in-vitro process. Magnetic nanocomposites were qualified by Fourier Transform Infrared (FTIR), Scanning Electron Microscopy (SEM), X-Ray Diffraction (XRD), Vibrational Sample Magnetometer (VSM) and Transmission Electron Microscopy (TEM). Results showed that nanoparticles were synthesized successfully with good dispersion of magnetic nanoparticles in cavity, uniform particle size distribution with average size of 65nm and high magnetization of 33...
June 2017: International Journal of Biological Macromolecules
https://www.readbyqxmd.com/read/28283434/insights-into-the-molecular-mechanism-of-triptan-transport-by-p-glycoprotein
#10
Laura A Wilt, Diana Nguyen, Arthur G Roberts
The P-glycoprotein (Pgp) transporter reduces the penetration of a chemically diverse range of neurotherapeutics at the blood-brain barrier, but the molecular features of drugs and drug-Pgp interactions that drive transport remain to be clarified. In particular, the triptan neurotherapeutics, eletriptan (ETT) and sumatriptan (STT), were identified to have a >10-fold difference in transport rates despite being from the same drug class. Consistent with these transport differences, ETT activated Pgp-mediated ATP hydrolysis ∼2-fold, whereas STT slightly inhibited Pgp-mediated ATP hydrolysis by ∼10%...
March 7, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28251391/a-multicenter-open-label-long-term-safety-and-tolerability-study-of-dfn-02-an-intranasal-spray-of-sumatriptan-10%C3%A2-mg-plus-permeation-enhancer-ddm-for-the-acute-treatment-of-episodic-migraine
#11
MULTICENTER STUDY
Sagar Munjal, Elimor Brand-Schieber, Kent Allenby, Egilius L H Spierings, Roger K Cady, Alan M Rapoport
BACKGROUND: DFN-02 is a novel intranasal spray formulation composed of sumatriptan 10 mg and a permeation-enhancing excipient comprised of 0.2% 1-O-n-Dodecyl-β-D-Maltopyranoside (DDM). This composition of DFN-02 allows sumatriptan to be rapidly absorbed into the systemic circulation and exhibit pharmacokinetics comparable to subcutaneously administered sumatriptan. Rapid rate of absorption is suggested to be important for optimal efficacy. The objective of this study was to evaluate the safety and tolerability of DFN-02 (10 mg) in the acute treatment of episodic migraine with and without aura over a 6-month period based on the incidence of treatment-emergent adverse events and the evaluation of results of clinical laboratory tests, vital signs, physical examination, and electrocardiograms...
December 2017: Journal of Headache and Pain
https://www.readbyqxmd.com/read/28194544/exploring-the-role-of-trpv-and-cgrp-in-adenosine-preconditioning-and-remote-hind-limb-preconditioning-induced-cardioprotection-in-rats
#12
Amritpal Singh, Puneet Kaur Randhawa, Anjana Bali, Nirmal Singh, Amteshwar Singh Jaggi
The cardioprotective effects of remote hind limb preconditioning (RIPC) are well known, but mechanisms by which protection occurs still remain to be explored. Therefore, the present study was designed to investigate the role of TRPV and CGRP in adenosine and remote preconditioning-induced cardioprotection, using sumatriptan, a CGRP release inhibitor and ruthenium red, a TRPV inhibitor, in rats. For remote preconditioning, a pressure cuff was tied around the hind limb of the rat and was inflated with air up to 150 mmHg to produce ischemia in the hind limb and during reperfusion pressure was released...
February 14, 2017: Cardiovascular Drugs and Therapy
https://www.readbyqxmd.com/read/28176899/subcutaneous-sumatriptan-delivery-devices-comparative-ease-of-use-and-preference-among-migraineurs
#13
Anthony D Andre, Elimor Brand-Schieber, Margarita Ramirez, Sagar Munjal, Rajesh Kumar
BACKGROUND: Several sumatriptan subcutaneous autoinjector devices for acute treatment of migraine patients are available, each device differs with respect to design and features. Determining device preference and ease of use is important because patients experiencing a migraine attack are often functionally impaired. OBJECTIVE: The objective of this human factors study was to compare migraine patients' device use performance and preferences for three sumatriptan subcutaneous autoinjectors: a disposable two-step device (Zembrace(®) SymTouch(®)), a disposable three-step device (Sumavel(®) DosePro(®)), and a multistep reloadable device (Imitrex(®) STATdose(®)), using simulated injections...
2017: Patient Preference and Adherence
https://www.readbyqxmd.com/read/28176235/randomized-double-blind-crossover-study-comparing-dfn-11-injection-3%C3%A2-mg-subcutaneous-sumatriptan-with-6%C3%A2-mg-subcutaneous-sumatriptan-for-the-treatment-of-rapidly-escalating-attacks-of-episodic-migraine
#14
RANDOMIZED CONTROLLED TRIAL
Roger K Cady, Sagar Munjal, Ryan J Cady, Heather R Manley, Elimor Brand-Schieber
BACKGROUND: A 6-mg dose of SC sumatriptan is the most efficacious and fast-acting acute treatment for migraine, but a 3-mg dose of SC sumatriptan may improve tolerability while maintaining efficacy. METHODS: This randomized, double-blind, crossover study compared the efficacy and tolerability of 3 mg subcutaneous (SC) sumatriptan (DFN-11) with 6 mg SC sumatriptan in 20 adults with rapidly-escalating migraine attacks. Eligible subjects were randomized (1:1) to treat 1 attack with DFN-11 and matching placebo autoinjector consecutively or 2 DFN-11 autoinjectors consecutively and a second attack similarly but with the alternative dose (3 mg or 6 mg)...
December 2017: Journal of Headache and Pain
https://www.readbyqxmd.com/read/28162729/-478-faster-migraine-pain-and-disability-relief-using-avp-825-compared-to-sumatriptan-tablet-applying-a-novel-method-for-evaluating-migraine-relief-across-multiple-outcomes
#15
K Shulman, L Yedigarova, J McGinley, R Wirth, D Buse, J Siffert, R Lipton
No abstract text is available yet for this article.
April 2016: Journal of Pain: Official Journal of the American Pain Society
https://www.readbyqxmd.com/read/28107913/quantitative-structure-retention-relationship-model-for-the-determination-of-naratriptan-hydrochloride-and-its-impurities-based-on-artificial-neural-networks-coupled-with-genetic-algorithm
#16
Mikołaj Mizera, Anna Krause, Przemysław Zalewski, Robert Skibiński, Judyta Cielecka-Piontek
Mathematical modeling of Quantitative Structure - Property Relationships met great interest in fields of in silico drug design and more recently, pharmaceutical analysis. In our approach we proposed automated method of creation Quantitative Structure-Retention Relationship (QSRR) for analysis of triptans, selective serotonin 5-HT1 receptor agonists used for the treatment of acute headache. The method was created using hybrid machine learning approach, namely Genetic algorithm (GA) coupled with artificial neutral networks (ANN)...
March 1, 2017: Talanta
https://www.readbyqxmd.com/read/28103158/serotonin-receptor-targeted-therapy-for-migraine-treatment-an-overview-of-drugs-in-phase-i-and-ii-clinical-development
#17
REVIEW
Piero Barbanti, C Aurilia, G Egeo, L Fofi, R Palmirotta
Research has focused on serotonin (5-HT) 5-HT1D and 5-HT1F receptors to develop drugs acting through non-vasoconstrictive mechanisms for treating acute migraine and those targeting 5-HT2B and 5-HT7 receptors for preventing migraine. Areas covered: This paper reviews antimigraine drugs targeting 5-HT receptors in one phase I trial (sumatriptan iontophoretic transdermal system, TDS) and five phase II clinical trials (PNU-142633, LY334370, lasmiditan, NOX-188). Expert opinion: Data from our overview on investigational drugs in phase I and II clinical trials using the 5-HT1B/1D receptor agonist (sumatriptan TDS), 5-HT1D receptor agonist (PNU-142633), 5-HT1F receptor agonists (LY334370, lasmiditan) and a combined 5-HT1B/1D receptor agonist with nNOS inhibition (NOX-188) provided encouraging data for sumatriptan TDS and lasmiditan, disappointing results for PNU-142633, and promising findings for NOX-188...
March 2017: Expert Opinion on Investigational Drugs
https://www.readbyqxmd.com/read/28101470/protective-roles-of-n-acetyl-cysteine-and-or-taurine-against-sumatriptan-induced-hepatotoxicity
#18
Javad Khalili Fard, Hossein Hamzeiy, Mohammadreza Sattari, Mohammad Ali Eghbal
Purpose: Triptans are the drug category mostly prescribed for abortive treatment of migraine. Most recent cases of liver toxicity induced by triptans have been described, but the mechanisms of liver toxicity of these medications have not been clear. Methods: In the present study, we obtained LC50 using dose-response curve and investigated cell viability, free radical generation, lipid peroxide production, mitochondrial injury, lysosomal membrane damage and the cellular glutathione level as toxicity markers as well as the beneficial effects of taurine and/or N-acetyl cysteine in the sumatriptan-treated rat parenchymal hepatocytes using accelerated method of cytotoxicity mechanism screening...
December 2016: Advanced Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/28093722/triptan-use-in-australia-1997-2015-a-pharmacoepidemiological-study
#19
B L K D Eyre, M J Eadie, M L van Driel, L Ross-Lee, S A Hollingworth
OBJECTIVE: This study examined the use of triptan derivatives in Australia between 1997 and 2015, based on a national drug reimbursement database, and compared patterns of use with available international data. METHODS: We obtained publically available data on the number of prescriptions for triptans marketed in Australia (sumatriptan, eletriptan, rizatriptan, zolmitriptan, naratriptan). Dispensed use was measured as defined daily dose (DDD per 1000 population per day) for Australia's concessional beneficiaries (low-income earners, people with disabilities, and seniors)...
January 16, 2017: Acta Neurologica Scandinavica
https://www.readbyqxmd.com/read/28091820/depression-of-home-cage-wheel-running-a-reliable-and-clinically-relevant-method-to-assess-migraine-pain-in-rats
#20
Ram Kandasamy, Andrea T Lee, Michael M Morgan
BACKGROUND: The development of new anti-migraine treatments is limited by the difficulty inassessing migraine pain in laboratory animals. Depression of activity is one of the few diagnostic criteria formigraine that can be mimicked in rats. The goal of the present study was to test the hypothesis thatdepression of home cage wheel running is a reliable and clinically relevant method to assess migraine painin rats. METHODS: Adult female rats were implanted with a cannula to inject allyl isothiocyanate (AITC) onto the dura to induce migraine pain, as has been shown before...
December 2017: Journal of Headache and Pain
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