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Flupirtine

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https://www.readbyqxmd.com/read/29238169/bioequivalence-study-of-two-formulations-of-flupirtine-maleate-capsules-in-healthy-male-chinese-volunteers-under-fasting-and-fed-conditions
#1
Yanfang Liu, Hua Huo, Zhibo Zhao, Wenli Hu, Yujia Sun, Yunbiao Tang
Aim: This study developed a high-performance liquid chromatography-tandem mass spectrometry method to simultaneously determine the concentrations of flupirtine and its major active metabolite D-13223 in human plasma in order to assess the bioequivalence (BE) of two flupirtine maleate capsules among healthy male Chinese volunteers under fasting and fed conditions. Materials and methods: There were two single-center, randomized, single-dose, open-label, laboratory-blinded, two-period, cross-over studies which included 24 healthy male Chinese volunteers under fasting and fed conditions, respectively...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/29235121/a-simple-and-rapid-hplc-uv-method-for-the-determination-of-retigabine-in-human-plasma
#2
Valentina Franco, Katia Baruffi, Giuliana Gatti, Roberto Marchiselli, Cinzia Fattore, Maria Paola Canevini, Francesca Crema, Emilio Perucca
A simple and rapid high-performance liquid chromatographic method with ultraviolet detection was developed for the quantitative determination of retigabine, known also as ezogabine, in human plasma. The assay uses a simple solid phase extraction for sample preparation and direct injection of the extract into the chromatograph. Flupirtine is used as an internal standard. Chromatographic separation is achieved on a C18 Chromolith column (Chromolith Performance, 100 x 4.6 mm ID), using as mobile phase water/acetonitrile/methanol (72:18:10 vol/vol/vol) mixed with 0...
December 12, 2017: Biomedical Chromatography: BMC
https://www.readbyqxmd.com/read/29110485/discovery-of-aromatic-carbamates-that-confer-neuroprotective-activity-by-enhancing-autophagy-and-inducing-the-anti-apoptotic-protein-b-cell-lymphoma-2-bcl-2
#3
Nihar Kinarivala, Ronak Patel, Rose-Mary Boustany, Abraham J Al-Ahmad, Paul C Trippier
Neurodegenerative diseases share certain pathophysiological hallmarks that represent common targets for drug discovery. In particular, dysfunction of proteostasis and the resultant apoptotic death of neurons, represent common pathways for pharmacological intervention. A library of aromatic carbamate derivatives based on the clinically available drug flupirtine was synthesized to determine a structure-activity relationship for neuroprotective activity. Several derivatives were identified that possess greater protective effect in human induced pluripotent stem cell-derived neurons, protecting up to 80% of neurons against etoposide-induced apoptosis at concentrations as low as 100 nM...
November 7, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29081669/a-comparative-study-of-efficacy-and-safety-of-flupirtine-versus-piroxicam-in-postoperative-pain-in-patients-undergoing-lower-limb-surgery
#4
Sowmya Chinnaiyan, Narayana Sarala, Heddur Shanthappa Arun
BACKGROUND: Effective control of pain postoperatively is essential in providing enhanced patient care and a cost-effective hospital stay. Though many treatment modalities exist for postoperative pain management in orthopedic surgeries they are often accompanied by adverse effects. This study was carried out to assess the efficacy of flupirtine and piroxicam in postoperative pain reduction using visual analog scale (VAS) score. MATERIALS AND METHODS: An open-label, parallel group, comparative study was conducted on patients undergoing lower limb orthopedic surgery, randomized into two groups of 38 patients each...
2017: Journal of Pain Research
https://www.readbyqxmd.com/read/29050967/role-of-k-channels-in-regulating-spontaneous-activity-in-the-muscularis-mucosae-of-guinea-pig-bladder
#5
Ken Lee, Ayu Isogai, Minori Antoh, Shunichi Kajioka, Masatoshi Eto, Hikaru Hashitani
To explore the roles of various K(+) channels in regulating the spontaneous activity of bladder muscularis mucosae (MM) that is considered to play an important role in maintaining mucosal function. Effects of K(+) channel modulators on electrical and contractile activity in the guinea-pig bladder MM were examined using intracellular microelectrode and isometric tension recording. The MM predominately generated bursting spontaneous action potentials (SAPs) and phasic contractions (SPCs) that were blocked by nifedipine (1µM)...
October 16, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28782153/n-acetylcysteine-and-prednisolone-treatment-improved-serum-biochemistries-in-suspected-flupirtine-cases-of-severe-idiosyncratic-liver-injury
#6
Jürgen Borlak, Florian van Bömmel, Thomas Berg
BACKGROUND & AIMS: The analgesic flupirtine has been linked to cases of severe idiosyncratic drug-induced liver injury (sFILI). We therefore examined whether N-acetylcysteine (NAC) and glucocorticoid therapy is effective in the management of sFILI. METHODS: In a retrospective cohort study efficacy of NAC-infusion and oral prednisolone treatments on liver-function-tests (LFTs) and clinical outcome of 21 sFILI cases was evaluated by comparing it to an external cohort of 30 sFILI cases not receiving the antidote...
August 7, 2017: Liver International: Official Journal of the International Association for the Study of the Liver
https://www.readbyqxmd.com/read/28587899/anticonvulsant-effect-of-flupirtine-in-an-animal-model-of-neonatal-hypoxic-ischemic-encephalopathy
#7
Dayalan Sampath, Robert Valdez, Andrew M White, Yogendra H Raol
Research studies suggest that neonatal seizures, which are most commonly associated with hypoxic-ischemic injury, may contribute to brain injury and adverse neurologic outcome. Unfortunately, neonatal seizures are often resistant to treatment with current anticonvulsants. In the present study, we evaluated the efficacy of flupirtine, administered at clinically relevant time-points, for the treatment of neonatal seizures in an animal model of hypoxic-ischemic injury that closely replicates features of the human syndrome...
September 1, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28510996/tramadol-with-or-without-paracetamol-acetaminophen-for-cancer-pain
#8
REVIEW
Philip J Wiffen, Sheena Derry, R Andrew Moore
BACKGROUND: Tramadol is an opioid analgesic licensed for use in moderate to severe pain. It is considered as a low risk for abuse, so control regulations are not as stringent as for 'strong' opioids such as morphine. It has a potential role as a step 2 option of the World Health Organization (WHO) analgesic ladder. OBJECTIVES: To assess the benefits and adverse effects of tramadol with or without paracetamol (acetaminophen) for cancer-related pain. SEARCH METHODS: We searched the following databases using a wide range of search terms: the Cochrane Central Register of Controlled Trials (CENTRAL), MEDLINE, Embase, and LILACS...
May 16, 2017: Cochrane Database of Systematic Reviews
https://www.readbyqxmd.com/read/28442953/role-of-flupirtine-in-reducing-preoperative-anxiety-of-patients-undergoing-craniotomy-procedure
#9
Ghanshyam Yadav, Gaurav Jain, Malkhan Singh
BACKGROUND: Kv7 neuronal channels are recognized as a potential drug target for anxiolytic effects. We hypothesize that flupirtine as a potassium channel opener would effectively reduce the preoperative anxiety of patients undergoing craniotomy procedure. METHODS: In prospective-double-blinded fashion, 124 counseled patients were randomized to receive 5 sequential doses of capsule flupirtine 100 mg (F Group) or physically similar starch capsules (C Group), at 12 h intervals during preoperative hospitalization...
April 2017: Saudi Journal of Anaesthesia
https://www.readbyqxmd.com/read/28125509/kcnq2-3-channel-agonist-flupirtine-reduces-cocaine-place-preference-in-rats
#10
James Mooney, Scott M Rawls
The efficacy of KCNQ2/3 channel agonists against drug reward has not been defined despite their ability to reduce locomotor-stimulant and dopamine-activating effects of psychostimulants. We tested the hypothesis that flupirtine (FLU) (2.5, 10, 20 mg/kg), a KCNQ2/3 agonist, reduces cocaine (15 mg/kg) conditioned place preference. FLU (20 mg/kg), injected concurrently with cocaine during conditioning, reduced the development of cocaine conditioned place preference. FLU (20 mg/kg) also reduced cocaine locomotor activation without affecting baseline activity...
August 2017: Behavioural Pharmacology
https://www.readbyqxmd.com/read/27836910/insights-from-therapeutic-studies-for-prp-prion-disease
#11
Kenta Teruya, Katsumi Doh-Ura
Although an effective therapy for prion disease has not yet been established, many advances have been made toward understanding its pathogenesis, which has facilitated research into therapeutics for the disease. Several compounds, including flupirtine, quinacrine, pentosan polysulfate, and doxycycline, have recently been used on a trial basis for patients with prion disease. Concomitantly, several lead antiprion compounds, including compound B (compB), IND series, and anle138b, have been discovered. However, clinical trials are still far from yielding significantly beneficial results, and the findings of lead compound studies in animals have highlighted new challenges...
November 11, 2016: Cold Spring Harbor Perspectives in Medicine
https://www.readbyqxmd.com/read/27833227/creutzfeldt-jakob-disease-phenotype-and-course-our-experience-from-a-tertiary-center
#12
Sadanandavalli Retnaswami Chandra, Thomas Gregor Issac, Mariamma Philip, Veeranna Gadad
INTRODUCTION: Prion diseases are protein conformation disorders and neither caused by viroid or virus but is a transmissible particle labeled a prion by Pruisner. Normal prion protein becomes infectious by a different folding, but the triggers are not known. Based on the characteristic brain pathology, they are grouped under spongiform encephalopathy affecting both man and animals. Estimated prevalence is one per million. Creutzfeldt-Jakob disease (CJD) registry from National Institute and Neurosciences (NIMHANS), Bengaluru, reported 69 cases in 30 years...
September 2016: Indian Journal of Psychological Medicine
https://www.readbyqxmd.com/read/27761601/kv7-channels-in-the-human-detrusor-channel-modulator-effects-and-gene-and-protein-expression
#13
Riccardo Bientinesi, Cesare Mancuso, Maria Martire, Pier Francesco Bassi, Emilio Sacco, Diego Currò
Voltage-gated type 7 K(+) (KV7 or KCNQ) channels regulate the contractility of various smooth muscles. With this study, we aimed to assess the role of KV7 channels in the regulation of human detrusor contractility, as well as the gene and protein expression of KV7 channels in this tissue. For these purposes, the isolated organ technique, RT-qPCR, and Western blot were used, respectively. XE-991, a selective KV7 channel blocker, concentration-dependently contracted the human detrusor; mean EC50 and Emax of XE-991-induced concentration-response curve were 14...
February 2017: Naunyn-Schmiedeberg's Archives of Pharmacology
https://www.readbyqxmd.com/read/27721001/altered-contractile-responses-of-arteries-from-spontaneously-hypertensive-rat-the-role-of-endogenous-mediators-and-membrane-depolarization
#14
Michal Bencze, Michal Behuliak, Anna Vavřínová, Josef Zicha
AIMS: The goal of our study was to reveal the important mechanism(s) responsible for the enhanced contractility of isolated arteries from animals suffering genetic hypertension. MAIN METHODS: Contractile force of endothelium-denuded arteries, modulated by various interventions, was measured by wire myography. KEY FINDINGS: Spontaneously hypertensive rat (SHR) and Wistar-Kyoto rat (WKY) arteries were stimulated by norepinephrine, increased extracellular K(+) or tyramine...
December 1, 2016: Life Sciences
https://www.readbyqxmd.com/read/27455901/effects-of-k-channel-openers-on-spontaneous-action-potentials-in-detrusor-smooth-muscle-of-the-guinea-pig-urinary-bladder
#15
Hiroaki Takagi, Hikaru Hashitani
The modulation of spontaneous excitability in detrusor smooth muscle (DSM) upon the pharmacological activation of different populations of K(+) channels was investigated. Effects of distinct K(+) channel openers on spontaneous action potentials in DSM of the guinea-pig bladder were examined using intracellular microelectrode techniques. NS1619 (10μM), a large conductance Ca(2+)-activated K(+) (BK) channel opener, transiently increased action potential frequency and then prevented their generation without hyperpolarizing the membrane in a manner sensitive to iberiotoxin (IbTX, 100nM)...
October 15, 2016: European Journal of Pharmacology
https://www.readbyqxmd.com/read/26999128/the-role-of-kv7-3-in-regulating-osteoblast-maturation-and-mineralization
#16
Ji Eun Yang, Min Seok Song, Yiming Shen, Pan Dong Ryu, So Yeong Lee
KCNQ (KV7) channels are voltage-gated potassium (KV) channels, and the function of KV7 channels in muscles, neurons, and sensory cells is well established. We confirmed that overall blockade of KV channels with tetraethylammonium augmented the mineralization of bone-marrow-derived human mesenchymal stem cells during osteogenic differentiation, and we determined that KV7.3 was expressed in MG-63 and Saos-2 cells at the mRNA and protein levels. In addition, functional KV7 currents were detected in MG-63 cells...
March 18, 2016: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/26959717/hla-drb1-16-01-dqb1-05-02-is-a-novel-genetic-risk-factor-for-flupirtine-induced-liver-injury
#17
Paola Nicoletti, Anneke N Werk, Ashley Sawle, Yufeng Shen, Thomas J Urban, Sally A Coulthard, Einar S Bjornsson, Ingolf Cascorbi, Aris Floratos, Thomas Stammschulte, Ursula Gundert-Remy, Matthew R Nelson, Guruprasad P Aithal, Ann K Daly
OBJECTIVE: Flupirtine is a nonopioid analgesic with regulatory approval in a number of European countries. Because of the risk of serious liver injury, its use is now limited to short-term pain management. We aimed to identify genetic risk factors for flupirtine-related drug-induced liver injury (DILI) as these are unknown. MATERIALS AND METHODS: Six flupirtine-related DILI patients from Germany were included in a genome-wide association study (GWAS) involving a further 614 European cases of DILI because of other drugs and 10,588 population controls...
May 2016: Pharmacogenetics and Genomics
https://www.readbyqxmd.com/read/26955312/effect-of-preoperative-flupirtine-on-postoperative-morphine-sparing-in-patients-undergoing-total-abdominal-hysterectomy
#18
D Thapa, V Ahuja, C Dass, S Gombar, A Huria
BACKGROUND: Flupirtine is a unique non-opioid, centrally acting analgesic with muscle relaxant properties. So far no study has evaluated, use of preoperative flupirtine on postoperative morphine sparing effect in patients undergoing total abdominal hysterectomy (TAH). MATERIALS AND METHODS: We performed a prospective, controlled, and randomized study in 50 female patients of American Society of Anesthesiologists physical status I-II, aged between 30 and 60 years scheduled for TAH under general anesthesia (GA)...
January 2016: Saudi Journal of Anaesthesia
https://www.readbyqxmd.com/read/26869923/a-humanized-clinically-calibrated-quantitative-systems-pharmacology-model-for-hypokinetic-motor-symptoms-in-parkinson-s-disease
#19
Patrick Roberts, Athan Spiros, Hugo Geerts
The current treatment of Parkinson's disease with dopamine-centric approaches such as L-DOPA and dopamine agonists, although very successful, is in need of alternative treatment strategies, both in terms of disease modification and symptom management. Various non-dopaminergic treatment approaches did not result in a clear clinical benefit, despite showing a clear effect in preclinical animal models. In addition, polypharmacy is common, sometimes leading to unintended effects on non-motor cognitive and psychiatric symptoms...
2016: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/26869667/inhibition-of-kv7-channels-protects-the-rat-heart-against-myocardial-ischemia-and-reperfusion-injury
#20
Elise R Hedegaard, Jacob Johnsen, Jonas A Povlsen, Nichlas R Jespersen, Jeffrey A Shanmuganathan, Mia R Laursen, Steen B Kristiansen, Ulf Simonsen, Hans Erik Bøtker
The voltage-gated KV7 (KCNQ) potassium channels are activated by ischemia and involved in hypoxic vasodilatation. We investigated the effect of KV7 channel modulation on cardiac ischemia and reperfusion injury and its interaction with cardioprotection by ischemic preconditioning (IPC). Reverse-transcription polymerase chain reaction revealed expression of KV7.1, KV7.4, and KV7.5 in the left anterior descending rat coronary artery and all KV7 subtypes (KV7.1-KV7.5) in the left and right ventricles of the heart...
April 2016: Journal of Pharmacology and Experimental Therapeutics
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