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Flupirtine

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https://www.readbyqxmd.com/read/29771716/flupirtine-is-an-effective-analgesic-is-the-associated-rare-liver-injury-a-limiting-factor-to-its-use
#1
Kim Lawson
No abstract text is available yet for this article.
May 15, 2018: Anesthesia and Analgesia
https://www.readbyqxmd.com/read/29744325/inhibition-of-spontaneous-contractility-of-isolated-caprine-ureter-by-flupirtine
#2
Girish S Naik, Rohit Kodagali, Manoj G Tyagi, Kalpana Ernest, Margaret Shanthi, Sumith K Mathew, Jacob Peedicayil
Context: Kv7 potassium channels are expressed in several types of smooth muscles and could mediate physiological responses in the tissues expressed. Flupirtine is an analgesic that acts by opening Kv7 potassium channels. It has been shown to inhibit the contractility of several types of isolated smooth muscle. Aims: This study investigated the ability of flupirtine to inhibit the spontaneous contractility of isolated distal caprine (goat) ureter. Settings and Design: Spontaneous contractility of the isolated goat ureter was recorded using a physiograph...
April 2018: International Journal of Applied and Basic Medical Research
https://www.readbyqxmd.com/read/29617563/protein-surface-structural-recognition-in-inactive-areas-a-new-immobilization-strategy-for-acetylcholinesterase
#3
Jianxiong Diao, Xiaolu Yu, Lin Ma, Yuanqing Li, Ying Sun
This work reported a new method of design for the immobilization of acetylcholinesterase (AChE) based on its molecular structure to improve its sensitivity and stability. The immobilization binding site on the surface of AChE was determined using MOLCAD's multi-channel functionality. Then, 11 molecules ((+)-catechin, (-)-epicatechin, (-)-gallocatechin, hesperetin, naringenin, quercetin, taxifolin, (-)-epicatechin gallate, flupirtine, atropine, and hyoscyamine) were selected from the ZINC database (about 50 000 molecules) as candidate affinity ligands for AChE...
May 16, 2018: Bioconjugate Chemistry
https://www.readbyqxmd.com/read/29596091/flupirtine-an-effective-analgesic-but-hepatotoxicity-should-limit-its-use
#4
Livia Puljak
No abstract text is available yet for this article.
March 27, 2018: Anesthesia and Analgesia
https://www.readbyqxmd.com/read/29560967/randomized-controlled-trial-about-pain-medication-flupirtine-ignores-recent-pharmacovigilance-warnings
#5
COMMENT
Livia Puljak
No abstract text is available yet for this article.
2018: Journal of Pain Research
https://www.readbyqxmd.com/read/29523613/flupirtine-drug-induced-liver-injury-in-a-patient-developing-acute-liver-failure
#6
David Noiva Perdigoto, Pedro Amaro, Manuela Ferreira, Luis Tomé
A patient is admitted with complaints of recent onset nausea, discomfort, jaundice and blood tests that reveal severe hepatitis. At the time, she had been taking medication with Hypericum perforatum (St John's wort) for 6 months, and 6 weeks before this event, she took flupirtine maleate. A few days after being admitted, she developed encephalopathy progressing to acute liver failure (ALF) requiring unsuccessful liver transplantation. The patient was ultimately diagnosed with drug-induced liver injury (DILI)...
March 9, 2018: BMJ Case Reports
https://www.readbyqxmd.com/read/29474372/zinc-pyrithione-activates-k-channels-and-hyperpolarizes-the-membrane-of-rat-pulmonary-artery-smooth-muscle-cells
#7
Basma G Eid, Alison M Gurney
The membrane potential helps determine pulmonary artery smooth muscle cell (PASMC) contraction. The Kv7 channel activators, retigabine and flupirtine, are thought to dilate pulmonary arteries by hyperpolarising PASMC. Zinc pyrithione activates Kv7 channels by a mechanism distinct from retigabine and with different Kv7 subunit selectivity. This study aimed to determine if zinc pyrithione selectively activates Kv7 channels in rat PASMC to evoke pulmonary artery dilation. Zinc pyrithione relaxed pulmonary arteries with half-maximal effect at 4...
2018: PloS One
https://www.readbyqxmd.com/read/29381516/flupirtine-a-less-explored-neglected-nonopioid-analgesic
#8
Abhijit S Nair
No abstract text is available yet for this article.
April 2018: Anesthesia and Analgesia
https://www.readbyqxmd.com/read/29296617/flupirtine-and-diazepam-combination-terminates-established-status-epilepticus-results-in-three-rodent-models
#9
Terry Zhang, Marko S Todorovic, John Williamson, Jaideep Kapur
Objective: Status epilepticus (SE) is a neurological emergency requiring rapid termination of seizures. New treatment choices are needed for benzodiazepine-refractory SE or established SE (ESE). Previous studies have demonstrated that the potassium-channel opener flupirtine terminates seizures in neonatal animals. However, its effectiveness in adult ESE has not been tested. We tested whether flupirtine alone or in combination with the benzodiazepine diazepam would terminate ESE in three animal models...
December 2017: Annals of Clinical and Translational Neurology
https://www.readbyqxmd.com/read/29284847/evaluation-of-preoperative-flupirtine-in-ambulatory-functional-endoscopic-sinus-surgery-a-prospective-double-blind-randomized-controlled-trial
#10
Anjan Das, Hirak Biswas, Anindya Mukherjee, Sandip Roy Basunia, Subinay Chhaule, Tapobrata Mitra, Partha Sarathi Halder, Subrata Kumar Mandal
Background: Functional endoscopic sinus surgery (FESS) is the mainstay therapeutic management for nasal pathologies. We evaluated flupirtine, a centrally acting analgesic, for producing perfect perioperative conditions in FESS for adults in a day-care setting. Materials and Methods: Sixty-two patients (25-40 years) scheduled for FESS under general anesthesia were randomly divided into Group F ( n = 31) receiving preoperative flupirtine (100 mg) and Group C ( n = 31) receiving identical-looking placebo capsule per oral 60 min before induction of anesthesia...
October 2017: Anesthesia, Essays and Researches
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
#11
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
#12
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 × 4.6 mm i.d.), using as mobile phase water/acetonitrile/methanol (72:18:10 v/v/v) mixed with 0...
May 2018: 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
#13
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
#14
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
#15
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)...
January 5, 2018: 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
#16
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...
February 2018: 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
#17
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
#18
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
#19
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
#20
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
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