Genomes and Genes
Summary: Antiarrhythmic agent pharmacologically similar to LIDOCAINE. It may have some anticonvulsant properties.
Publications206 found, 100 shown here
- Mexiletine for symptoms and signs of myotonia in nondystrophic myotonia: a randomized controlled trialJeffrey M Statland
Department of Neurology, University of Rochester Medical Center, Rochester, New York, USA
JAMA 308:1357-65. 2012..Patients experience delayed muscle relaxation causing functionally limiting stiffness and pain. Mexiletine-induced sodium channel blockade reduced myotonia in small studies; however, as is common in rare diseases, ..
- Partial expression defect for the SCN5A missense mutation G1406R depends on splice variant background Q1077 and rescue by mexiletineBi Hua Tan
Dept of Medicine, Univ of Wisconsin, 600 Highland Ave H6 349, Madison, WI 53792, USA
Am J Physiol Heart Circ Physiol 291:H1822-8. 2006..channels in both backgrounds were transfected into HEK-293 cells and incubated for up to 72 h with and without mexiletine. At 8 h, neither current nor cell surface expression was observed for the mutant in either background, but both ..
- The effect of mexiletine on the level of lipid peroxidation and apoptosis of endothelium following experimental subarachnoid hemorrhageOrhan Sen
Department of Neurosurgery, Baskent University, Ankara, Turkey
Neurol Res 28:859-63. 2006..b>Mexiletine blocks sodium and calcium channels and activates ATP-sensitive K(+) channels...
- Morphine versus mexiletine for treatment of postamputation pain: a randomized, placebo-controlled, crossover trialChristopher L Wu
Division of Pain Medicine, Department of Anesthesiology and Critical Care Medicine, The Johns Hopkins Medical Institutions, Baltimore, Maryland, USA
Anesthesiology 109:289-96. 2008..Stump and phantom pains are debilitating sequelae of amputations that are often resistant to treatment. The efficacy of pharmacologic therapies, including opioids and sodium channel blockers, for postamputation pain is uncertain...
- Mexiletine is an effective antimyotonia treatment in myotonic dystrophy type 1E L Logigian
Department of Neurology, University of Rochester, Rochester, NY, USA
Neurology 74:1441-8. 2010To determine if mexiletine is safe and effective in reducing myotonia in myotonic dystrophy type 1 (DM1).
- Gating of myotonic Na channel mutants defines the response to mexiletine and a potent derivativeJ F Desaphy
Unit of Pharmacology, Faculty of Pharmacy, University of Bari, Italy
Neurology 57:1849-57. 2001..and periodic paralysis caused by sodium channel mutations show variable responses to the anti-myotonic drug mexiletine. OBJECTIVE: To investigate whether variability among sodium channel mutants results from differences in drug ..
- Mexiletine and lidocaine suppress the excitability of dorsal horn neuronsAndrea Olschewski
Department of Anesthesiology, Intensive Care Medicine, Pain Therapy, University Clinic Giessen and Marburg GmbH, Giessen, Germany
Anesth Analg 109:258-64. 2009..Thus, we investigated the effects of the Na+ channel blockers mexiletine and lidocaine on sensory spinal dorsal horn neurons.
- Effect of mexiletine on vincristine-induced painful neuropathy in miceJunzo Kamei
Department of Pathophysiology and Therapeutics, School of Pharmacy and Pharmaceutical Sciences, Hoshi University, 4 41, Ebara 2 Chome, Shinagawa ku, Tokyo 142 8501, Japan
Eur J Pharmacol 536:123-7. 2006In the present study, we examined the effect of mexiletine on vincristine-induced thermal hyperalgesia in mice. Mice were intraperitoneally treated with vincristine at a dose of 0...
- The preventive effect of mexiletine on cerebral ischemic injury following experimental middle cerebral artery occlusionCem Yilmaz
Baskent University, Neurosurgery Department, Ankara, Turkey
Turk Neurosurg 19:367-73. 2009Previous studies demonstrated that mexiletine has some important features in the prevention of ischemic brain injury such as sodium and calcium canal blockage and free radical occurrence...
- Mexiletine-responsive erythromelalgia due to a new Na(v)1.7 mutation showing use-dependent current fall-offJin Sung Choi
Department of Neurology, Yale University School of Medicine, New Haven, CT 06510, USA
Exp Neurol 216:383-9. 2009..to pharmacotherapy, although occasional reports document patients as showing partial relief with lidocaine or mexiletine. A 7-year-old girl, with a two-year history of symmetric burning pain and erythema in her hands and feet, was ..
- The cellular electrophysiologic effect of a new amiodarone like antiarrhythmic drug GYKI 16638 in undiseased human ventricular muscle: comparison with sotalol and mexiletineM Opincariu
Department of Pharmacology and Pharmacotherapy, Albert Szent Gyorgyi Medical and Pharmaceutical Center, University of Szeged, Szeged, Hungary
Curr Med Chem 9:41-6. 2002..effect of GYKI 16638, a new antiarrhythmic compound was studied and compared with that of sotalol and mexiletine in undiseased human right ventricular muscle preparation by applying the conventional microelectrode technique...
- Role of K+ channels in augmented relaxations to sodium nitroprusside induced by mexiletine in rat aortasH Kinoshita
Department of Anesthesia, Japanese Red Cross Society, Wakayama Medical Center, Japan
Anesthesiology 92:813-20. 2000A class Ib antiarrhythmic drug, mexiletine, augments relaxations produced by adenosine triphosphate (ATP) sensitive K+ channel openers in isolated rat aortas, suggesting that it produces changes in the vasodilation mediated by ATP-..
- Non-dystrophic myotonia: prospective study of objective and patient reported outcomesJaya R Trivedi
Department of Neurology and Neurotherapeutics, UT Southwestern Medical Centre, Dallas, TX 75390, USA
Brain 136:2189-200. 2013....
- Fragment-based discovery of mexiletine derivatives as orally bioavailable inhibitors of urokinase-type plasminogen activatorMartyn Frederickson
Astex Therapeutics Ltd, 436 Cambridge Science Park, Milton Road, Cambridge, CB4 0QA, United Kingdom
J Med Chem 51:183-6. 2008..The (R)-enantiomer of the orally active drug mexiletine 5 (a fragment hit from X-ray crystallographic screening) was the chemical starting point...
- Neuroprotective effect of mexiletine in the central nervous system of diabetic ratsOzkan Ates
Inonu University, School of Medicine, Department of Neurosurgery, Malatya, Turkey
Mol Cell Biochem 286:125-31. 2006..In the present study we investigated the possible neuroprotective effect of mexiletine against streptozotocin-induced hyperglycaemia in the rat brain and spinal cord...
- Intravenous lidocaine and mexiletine in the management of trigeminal autonomic cephalalgiasMichael J Marmura
Department of Neurology, Thomas Jefferson University, Philadelphia, PA 19107, USA
Curr Pain Headache Rep 14:145-50. 2010Lidocaine and mexiletine are class 1B antiarrhythmic drugs that act on sodium channels...
- Refractory erythromelalgia of the ears: response to mexiletineAlejandra C Vivas
Department of Dermatology and Cutaneous Surgery, University of Miami Miller School of Medicine, Miami, FL, USA
Am J Otolaryngol 32:168-70. 2011..of the ears in a patient who has been refractory to multiple therapies and in whom relief of symptoms was achieved with the use of mexiletine. A review of clinical presentation, pathophysiology, and therapeutic options are presented.
- Mexiletine in the symptomatic treatment of diabetic peripheral neuropathyJ M Wright
School of Medicine, University of Missouri, Kansas City 64108, USA
Ann Pharmacother 31:29-34. 1997To evaluate the efficacy and safety of mexiletine in the symptomatic treatment of diabetic peripheral neuropathy (DPN).
- Enantioselective drug-protein interaction between mexiletine and plasma proteinLushan Yu
Department of Pharmaceutical Analysis and Drug Metabolism, College of Pharmaceutical Sciences, Zhejiang University, Hangzhou, China
J Pharm Pharmacol 64:792-801. 2012This study examined the interaction of mexiletine enantiomers with human plasma, human serum albumin (HSA), and human α1-acid glycoprotein (hAGP), and characterized the binding modes of mexiletine enantiomers with hAGP in the molecular ..
- Stereoselective binding of mexiletine and ketoprofen enantiomers with human serum albumin domainsDa Shi
Department of Drug Metabolism and Pharmaceutical Analysis, College of Pharmaceutical Sciences, Zhejiang University, Hangzhou, China
Acta Pharmacol Sin 33:710-6. 2012To investigate the stereoselective binding of mexiletine or ketoprofen enantiomers with different recombinant domains of human serum albumin (HSA).
- Mexiletine. A review of its therapeutic use in painful diabetic neuropathyB Jarvis
Adis International Limited, Auckland, New Zealand
Drugs 56:691-707. 1998b>Mexiletine is an orally active local anaesthetic agent which is structurally related to lidocaine (lignocaine) and has been used for alleviating neuropathic pain of various origins...
- A trafficking defective, Brugada syndrome-causing SCN5A mutation rescued by drugsCarmen R Valdivia
Department of Medicine and Physiology, University of Wisconsin, Madison, WI, USA
Cardiovasc Res 62:53-62. 2004..Mutations in SCN5A cause arrhythmia syndromes including Brugada syndrome (BrS) and congenital long QT syndrome subtype 3 (LQT3). Here, we report a trafficking defective BrS-causing SCN5A mutation that was drug-rescued...
- New potent mexiletine and tocainide analogues evaluated in vivo and in vitro as antimyotonic agents on the myotonic ADR mouseAnnamaria De Luca
Unit of Pharmacology, Department of Pharmacobiology, Faculty of Pharmacy, University of Bari, Via Orabona 4, Campus, 70125 Bari, Italy
Neuromuscul Disord 14:405-16. 2004The antimyotonic activity of chiral derivatives of mexiletine and tocainide, selected as potent use-dependent blockers of skeletal muscle sodium channels, was evaluated in vivo acutely in myotonic ADR mice...
- The use-dependent sodium channel blocker mexiletine is neuroprotective against global ischemic injuryK E Hewitt
Loeb Health Research Institute, Division of Neuroscience, Ottawa Hospita -Civic Campus, University of Ottawa, 725 Parkdale Avenue, Ont, K1Y 4K9, Ottawa, Canada
Brain Res 898:281-7. 2001..This study investigates mexiletine, a use-dependent sodium channel blocker known to provide significant ischemic neuroprotection to white matter, ..
- Evaluation of the pharmacological activity of the major mexiletine metabolites on skeletal muscle sodium currentsM De Bellis
Unit of Pharmacology, Department of Pharmacobiology, University of Bari, Bari, Italy
Br J Pharmacol 149:300-10. 2006b>Mexiletine (Mex), an orally effective antiarrhythmic agent used to treat ventricular arrhythmias, has also been found to be effective for myotonia and neuropathic pain...
- Trafficking defects and gating abnormalities of a novel SCN5A mutation question gene-specific therapy in long QT syndrome type 3Yanfei Ruan
Cardiovascular Genetics Program, Leon H Charney Division of Cardiology, New York University School of Medicine, New York, NY, USA
Circ Res 106:1374-83. 2010..Sodium channel blockers are used as gene-specific treatments in long-QT syndrome type 3, which is caused by mutations in the sodium channel gene (SCN5A). Response to treatment is influenced by biophysical properties of mutations...
- Mexiletine reverses oxaliplatin-induced neuropathic pain in ratsNobuaki Egashira
Department of Pharmacy, Kyushu University Hospital, Japan
J Pharmacol Sci 112:473-6. 2010..b>Mexiletine, an orally available Na(+)-channel blocker, has widely been used in patients with chronic painful diabetic ..
- Experience with oral mexiletine in primary erythromelalgia in childrenJaveed Iqbal
Department of Pediatrics and Neonatology, Sher I Kashmir Institute of Medical Sciences, Srinagar, Jammu and Kashmir 190019, India
Ann Saudi Med 29:316-8. 2009..Both patients stopped taking part in school and social activities. We tried oral mexiletine, a class Ib antiarrythmic agent, in view of its reported role in various chronic painful conditions...
- The effect of intravenous lidocaine, tocainide, and mexiletine on spontaneously active fibers originating in rat sciatic neuromasC Chabal
Department of Anesthesiology, University of Washington School of Medicine, Seattle
Pain 38:333-8. 1989The effects of intravenously administered subanesthetic concentrations of lidocaine, tocainide, and mexiletine on spontaneously active fibers (SAFs) originating in 7-day-old rat sciatic neuromas were studied...
- The analgesic effect of gabapentin and mexiletine after breast surgery for cancerArgyro Fassoulaki
Department of Anesthesiology, Aretaieion Hospital, Medical School, University of Athens, Greece
Anesth Analg 95:985-91, table of contents. 2002We investigated the analgesic efficacy of mexiletine and gabapentin on acute and chronic pain associated with cancer breast surgery in 75 patients...
- Mexiletine block of disease-associated mutations in S6 segments of the human skeletal muscle Na(+) channelM P Takahashi
Department of Neurology, Massachusetts General Hospital, Boston, MA 02114, USA
J Physiol 537:701-14. 2001..We examined state-dependent mexiletine block for mutations involving the putative binding site in S6 segments (V445M, S804F, V1293I, V1589M and M1592V)...
- Validated HPTLC methods for quantification of mexiletine hydrochloride in a pharmaceutical formulationRafal Pietraś
Medical University of Lublin, Department of Medicinal Chemistry, Jaczewskiego 4, 20 090 Lublin, Poland
J AOAC Int 93:820-4. 2010Two simple, accurate, and precise HPTLC methods have been established for the determination of mexiletine hydrochloride, an antiarrhythmic agent, in Mexicord capsules...
- Muscle cramp in Machado-Joseph disease: altered motor axonal excitability properties and mexiletine treatmentKazuaki Kanai
Department of Neurology, Chiba University School of Medicine, Chiba, Japan
Brain 126:965-73. 2003..threshold electrotonus, refractoriness and supernormality] using threshold tracking and the effects of mexiletine hydrochloride on those cramps...
- Analgesic activity of a novel use-dependent sodium channel blocker, crobenetine, in mono-arthritic ratsJ M Laird
Department of Physiology, University of Alcala, Alcala de Henares, E 28871 Madrid, Spain
Br J Pharmacol 134:1742-8. 2001..The clinically effective sodium channel blocker, mexiletine, was compared with crobenetine (BIII 890 CL), a new, highly use-dependent sodium channel blocker. 2...
- Gating properties of SCN5A mutations and the response to mexiletine in long-QT syndrome type 3 patientsYanfei Ruan
Molecular Cardiology, Fondazione Salvatore Maugeri, Via Maugeri 10 10A, 27100 Pavia, Italy
Circulation 116:1137-44. 2007b>Mexiletine (Mex) has been proposed as a gene-specific therapy for patients with long-QT syndrome type 3 (LQT3) caused by mutations in the cardiac sodium channel gene (SCN5A)...
- Drug-induced hypersensitivity syndrome due to mexiletine associated with human herpes virus 6 and cytomegalovirus reactivationAtsushi Sekiguchi
Department of Dermatology, Asahikawa Medical College, Asahikawa 078 8510, Japan
J Dermatol 32:278-81. 2005A 66-year-old man developed a fever of 38 degrees C and generalized pruritic rash about one month after mexiletine hydrochloride administration for ventricular tachycardia...
- Primary erythromelalgia in a child responding to intravenous lidocaine and oral mexiletine treatmentAruna Nathan
Department of Anesthesiology and Critical Care Medicine, Children s Hospital of Philadelphia, Philadelphia, PA 19104, USA
Pediatrics 115:e504-7. 2005..However, intravenous lidocaine infusion, with subsequent transition to oral mexiletine therapy, proved very effective in reducing the frequency and severity of the pain episodes...
- Preferred mexiletine block of human sodium channels with IVS4 mutations and its pH-dependenceBahram Mohammadi
Department of Neurology, Medical School Hannover, Hannover, Germany
Pharmacogenet Genomics 15:235-44. 2005The effects of extracellular pH (6.2, 7.4 and 8.2) and 0.1 mM mexiletine, a channel blocker of the lidocaine type, are studied on two mutations of the fourth voltage sensor of the Nav1.4 sodium channel, R1448H/C...
- Suppression of atrial fibrillation with mexiletine pharmacotherapy in a young woman with type 1 long QT syndromeMalek El Yaman
Department of Pediatrics Division of Pediatric Cardiology, Mayo Clinic, Rochester, MN 55905, USA
Heart Rhythm 5:472-4. 2008
- Mexiletine-induced severe skin eruption, fever, eosinophilia, atypical lymphocytosis, and liver dysfunctionK Higa
Department of Anesthesiology, School of Medicine, Fukuoka University, Japan
Pain 73:97-9. 1997..skin eruption, fever, eosinophilia, atypical lymphocytosis, and liver dysfunction 30 days after ingestion of mexiletine, a sodium channel blocker, prescribed to treat postherpetic neuralgia...
- A novel SCN5A arrhythmia mutation, M1766L, with expression defect rescued by mexiletineCarmen R Valdivia
Departments of Medicine and Physiology, University of Wisconsin, Madison, WI, USA
Cardiovasc Res 55:279-89. 2002..Mutations in the cardiac sodium channel gene, SCN5A, cause congenital long QT syndrome (LQT3), Brugada syndrome, idiopathic ventricular fibrillation, and conduction disease by distinct cellular and clinical electrophysiological phenotypes...
- Stereoselective effects of mexiletine enantiomers on sodium currents and excitability characteristics of adult skeletal muscle fibersA De Luca
Unità di Farmacologia, Dipartimento Farmacobiologico, Bari, Italy
Naunyn Schmiedebergs Arch Pharmacol 352:653-61. 1995The effects of the enantiomers of mexiletine were tested on sodium currents of frog skeletal muscle fibers recorded by means of the three vaseline gap voltage clamp method and compared with the effects produced by tocainide enantiomers...
- Translation of flecainide- and mexiletine-induced cardiac sodium channel inhibition and ventricular conduction slowing from nonclinical models to clinicalB M Heath
Department of Safety Pharmacology, GlaxoSmithKline, Park Road, Ware, SG12 0DP, UK
J Pharmacol Toxicol Methods 63:258-68. 2011..sodium channel block, and translation of the effect from in vitro to in vivo models using sodium channel inhibitors flecainide and mexiletine; flecainide, but not mexiletine is commonly associated with QRS complex prolongation in humans.
- Effect of sodium channel blocker (mexiletine) on pathological ectopic firing pattern in a rat chronic constriction nerve injury modelSatoru Nakamura
Department of Orthopedic Surgery, Asahikawa Medical College, 2 1 1 1 Midorigaoka Higashi, Asahikawa, 078 8510, Japan
J Orthop Sci 10:315-20. 2005We studied the efficacy of mexiletine as a sodium channel blocker for neuropathic pain by investigating the effect of mexiletine on the pathological ectopic firing pattern in a chronic constriction nerve injury (CCI) model...
- Deracemization of mexiletine biocatalyzed by omega-transaminasesDominik Koszelewski
Department of Chemistry, Organic and Bioorganic Chemistry, Research Centre Applied Biocatalysis, University of Graz, Heinrichstrasse 28, A 8010 Graz, Austria
Org Lett 11:4810-2. 2009S)- as well as (R)-mexiletine [1-(2,6-dimethylphenoxy)-2-propanamine], a chiral orally effective antiarrhythmic agent, was prepared by deracemization starting from the commercially available racemic amine using omega-transaminases in up ..
- Hydroxylated analogs of mexiletine as tools for structural-requirements investigation of the sodium channel blocking activityAlessia Catalano
Department of Medicinal Chemistry, University of Bari, Bari, Italy
Arch Pharm (Weinheim) 343:325-32. 2010..1 and 4-(2-aminopropoxy)-3-(hydroxymethyl)-5-methylphenol 2, two dihydroxylated analogs of mexiletine - a well known class IB anti-arrhythmic drug - were synthesized and used as pharmacological tools to investigate ..
- Inhibition of skeletal muscle sodium currents by mexiletine analogues: specific hydrophobic interactions rather than lipophilia per se account for drug therapeutic profileAnnamaria De Luca
Sezione di Farmacologia, Dipartimento Farmacobiologico, Facolta di Farmacia, Universita di Bari, Campus, Via Orabona 4, 70125 Bari, Italy
Naunyn Schmiedebergs Arch Pharmacol 367:318-27. 2003In striated fibers, the activity of mexiletine (Mex)-like sodium channel blockers is strongly modulated by the part of the molecule nearby the asymmetric carbon atom...
- Effect of pacing and mexiletine on dispersion of repolarisation and arrhythmias in DeltaKPQ SCN5A (long QT3) miceLarissa Fabritz
Department of Cardiology and Angiology, University Hospital Munster, Munster, Germany
Cardiovasc Res 57:1085-93. 2003It has been suggested that both pacing and treatment with mexiletine may reduce torsade de pointes (TdP) arrhythmias in patients with long QT syndrome 3 (LQT3), but it is not fully understood how these interventions could prevent TdP...
- Effect of oral mexiletine on capsaicin-induced allodynia and hyperalgesia: a double-blind, placebo-controlled, crossover studyK Ando
Department of Anesthesiology, University of California, San Diego, La Jolla 92093-0924, USA
Reg Anesth Pain Med 25:468-74. 2000BACKGROUND AND OBJECTIVES: Mexiletine is a sodium channel blocker that has been used for the treatment of a variety of neuropathic pain syndromes...
- A case of fulminant Type 1 diabetes associated with mexiletine hypersensitivity syndromeY Seino
Diabet Med 21:1156-7. 2004
- Digoxin and mexiletine sensitivity in a Collie with the MDR1 mutationRosemary A Henik
Department of Medical Sciences, School of Veterinary Medicine, University of Wisconsin, Madison, USA
J Vet Intern Med 20:415-7. 2006
- A case of primary erythromelalgia improved by mexiletineH S Jang
Br J Dermatol 151:708-10. 2004
- Mexiletine block of wild-type and inactivation-deficient human skeletal muscle hNav1.4 Na+ channelsGing Kuo Wang
Department of Anaesthesia, Harvard Medical School and Brigham and Women s Hospital, Boston, MA, USA
J Physiol 554:621-33. 2004b>Mexiletine is a class 1b antiarrhythmic drug used for ventricular arrhythmias but is also found to be effective for paramyotonia congenita, potassium-aggravated myotonia, long QT-3 syndrome, and neuropathic pain...
- Optically active mexiletine analogues as stereoselective blockers of voltage-gated Na(+) channelsCarlo Franchini
Dipartimento Farmaco Chimico and Farmaco Biologico, Università degli Studi di Bari Via E Orabona 4, 70125 Bari, Italy
J Med Chem 46:5238-48. 2003Optically active mexiletine analogues were synthesized and evaluated in vitro as use-dependent blockers of skeletal muscle sodium channels...
- Positive symptoms in multiple sclerosis: their treatment with sodium channel blockers, lidocaine and mexiletineM Sakurai
Department of Neurology, Graduate School of Medicine, University of Tokyo, Japan
J Neurol Sci 162:162-8. 1999..Similar effects were obtained with orally-administered mexiletine (300-400 mg/day), a derivative of lidocaine, but to a lesser extent...
- Inhibition of frog skeletal muscle sodium channels by newly synthesized chiral derivatives of mexiletine and tocainideA De Luca
Dipartimento Farmacobiologico, Facolta di Farmacia, Bari, Italy
Naunyn Schmiedebergs Arch Pharmacol 356:777-87. 1997..muscle sodium channels as potential antimyotonic agents, the actions of newly synthesized chiral analogs of mexiletine and tocainide were tested in vitro on sodium currents of single fibers of frog semitendinosus muscle by vaseline-..
- A novel spinal action of mexiletine in spinal somatosensory transmission of nerve injured ratsV Chapman
Department of Pharmacology, University College London, UK
Pain 77:289-96. 1998b>Mexiletine is widely used for the treatment of neuropathic pain although its site(s) of action remain unclear...
- Design and assessment of a potent sodium channel blocking derivative of mexiletine for minimizing experimental neuropathic pain in several rat modelsRobert M Weston
Howard Florey Institute, University of Melbourne, Parkville, VIC 3010, Australia
Neurochem Res 34:1816-23. 2009..We have developed an analogue of mexiletine which is approximately 80 times more potent than mexiletine in competing with the radioligand, 3H-..
- 2D- and 3D-QSAR of tocainide and mexiletine analogues acting as Na(v)1.4 channel blockersAntonio Carrieri
Dipartimento Farmaco Chimico, Universita degli Studi di Bari, Via Orabona 4, 70125 Bari, Italy
Eur J Med Chem 44:1477-85. 2009Enantiomeric forms of Tocainide, Mexiletine, and structurally related local anaesthetic compounds, were analyzed with respect to their potency in blocking Na(v)1.4 channel...
- Systemic lidocaine or mexiletine for neuropathic painMark H Ebell
Am Fam Physician 74:79. 2006
- Acute exanthematous pustular drug eruption induced by mexiletineK Sasaki
Department of Dermatology, Tokyo Medical and Dental University, School of Medicine, 1 5 45 Yushima, Bunkyo ku, Tokyo 113 8519, Japan
Eur J Dermatol 11:469-71. 2001..infiltrated erythemas on the trunk, extremities, and face with marked facial edema, one month after taking mexiletine hydrochloride for his arrhythmia...
- Regional block and mexiletine: the effect on pain after cancer breast surgeryA Fassoulaki
Department of Anesthesiology, St Savas Hospital, Athens, Greece
Reg Anesth Pain Med 26:223-8. 2001..The present study investigates the effect of regional block, oral mexiletine, and the combination of both, on acute and chronic pain associated with cancer breast surgery.
- Mexiletine for refractory chronic daily headache: a report of nine casesMichael J Marmura
Department of Neurology, Thomas Jefferson University, Philadelphia, PA 19107, USA
Headache 48:1506-10. 2008To describe the use of mexiletine in the treatment of chronic daily headache in a refractory headache population.
- Drug-induced hypersensitivity syndrome due to mexiletine hydrochloride associated with reactivation of human herpesvirus 7Akiko Yagami
Department of Dermatology, Fujita Health University, School of Medicine, Toyoake, Aichi, Japan
Dermatology 213:341-4. 2006..He was diagnosed with DIHS due to mexiletine hydrochloride based on laboratory data, results of a patch test and the clinical course of his complaint, and ..
- Mexiletine protects myocardium during acute ischemia by opening sarcolemmal K-ATP channel: studies in closed-chest acute ischemia model in rabbitsShinichi Niwano
Department of Internal Medicine, Kitasato University School of Medicine, Sagamihara, Japan
J Cardiovasc Pharmacol 44:639-44. 2004Although we have previously shown that mexiletine might protect myocardium during acute ischemia, the precise mechanism was unclear...
- A multifunctional aromatic residue in the external pore vestibule of Na+ channels contributes to the local anesthetic receptorSuk Ying Tsang
The Johns Hopkins University, 720 Rutland Avenue, Ross 1165, Baltimore MD 21205, USA
Mol Pharmacol 67:424-34. 2005..g., 300 microM mexiletine induced a use-dependent block with 65.0 +/- 2.9% remaining current and -11.0 +/- 0...
- Mexiletine therapy for chronic pain: survival analysis identifies factors predicting clinical successIan R Carroll
Stanford Pain Management Center, Stanford University Medical Center, Palo Alto, CA 94304 1573, USA
J Pain Symptom Manage 35:321-6. 2008b>Mexiletine, a sodium channel blocker, treats neuropathic pain but its clinical value has been questioned due to its significant side effects and limited efficacy...
- The effects of Na movement on surgical myocardial protection: the role of the Na+-H+ exchange system and Na-channel in the development of ischemia and reperfusion injuryKe Xiang Liu
Department of Cardiovascular Surgery, The Second Clinical Hospital, Jilin University, Changchun, China
Ann Thorac Cardiovasc Surg 13:301-7. 2007We investigated whether the Na+-H+ exchange inhibitor, HOE642 (Hoe), and/or the Na channel blocker, mexiletine (Mex), enhance a cardioprotective effect on St...
- Rate-dependent QRS prolongation during exercise testing associated with hyperkalemiaHirokazu Shiraishi
Kyoto Perfectual University of Medicine, Kyoto, Japan
J Electrocardiol 37:241-5. 2004..The increase of QRS duration was possibly due to the combination of hyperkalemia and the effect of mexiletine. The rate dependent blocking effect on sodium channel of mexiletine might be intensified under hyperkalemia.
- Differential contribution of sodium channel subtypes to action potential generation in unmyelinated human C-type nerve fibersPhilip M Lang
Department of Anesthesiology, University of Munich, Munich, Germany
Anesthesiology 107:495-501. 2007..The aim of the current study was to characterize subtypes of Na(v) that contribute to action potential generation in peripheral unmyelinated human C-type nerve fibers...
- Unexpected mexiletine responses of a mutant cardiac Na+ channel implicate the selectivity filter as a structural determinant of antiarrhythmic drug accessKoji Sasaki
Department of Cardiovascular Medicine, Hokkaido University Graduate School of Medicine, Sapporo, Japan
Mol Pharmacol 66:330-6. 2004..next to the putative selectivity filter residue of domain 4, and evaluated the pharmacological properties to mexiletine using whole-cell, patch-clamp recordings...
- Characterization of mexiletine as an antagonist of beta-adrenoceptor in Chinese hamster ovary cells expressing cloned human beta-adrenoceptorsKenji Sakamoto
Department of Molecular Pharmacology, Kitasato University School of Pharmaceutical Sciences, 9 1 Shirokane 5 chome, Minato ku, Tokyo 108 8641, Japan
Biochem Pharmacol 67:815-22. 2004We characterized the beta-adrenoceptor-blocking property of mexiletine, a class Ib antiarrhythmic drug, on Chinese hamster ovary (CHO) cells stably expressing cloned human beta1-, beta2-, and beta3-adrenoceptors...
- The effects of mexiletine on excitability properties of human median motor axonsSatoshi Kuwabara
Department of Neurology, Chiba University School of Medicine, 1 8 1 Inohana, Chuo Ku, Chiba 260 8670, Japan
Clin Neurophysiol 116:284-9. 2005To investigate the effects of mexiletine, an analog of lidocaine, on excitability of human axons in vivo.
- [The filter region of the myocardial Na channel, together with ion selectivity, controls pharmacodynamics of anti-arrhythmia agents--an analysis using the channel altered by idiopathic ventricular fibrillation]Koji Sasaki
Hokkaido Igaku Zasshi 79:747-54. 2004
- Acetazolamide acts directly on the human skeletal muscle chloride channelHiroto Eguchi
First Department of Internal Medicine, Nagasaki University Graduate School of Biomedical Sciences, 1 12 4 Sakamoto, Nagasaki 852 8523, Japan
Muscle Nerve 34:292-7. 2006....
- Successful parental use of an automated external defibrillator for an infant with long-QT syndromeAbhay Divekar
Section of Pediatric Cardiology, Department of Pediatrics, Health Sciences Center, University of Manitoba, FE 241, 685 William Ave, Winnipeg, Manitoba, Canada R3E 0Z2
Pediatrics 118:e526-9. 2006..In this case report we describe the first successful parental use of an automated external defibrillator prescribed for primary prophylaxis against sudden cardiac death in an infant with long-QT syndrome...
- Class Ic antiarrhythmics block human skeletal muscle Na channel during myotonia-like stimulationFutoshi Aoike
Department of Neurology, Osaka University Graduate School of Medicine D 4, 2 2 Yamadaoka, Suita, Osaka 565 0871, Japan
Eur J Pharmacol 532:24-31. 2006..In contrast to mexiletine, flecainide did not markedly block sodium current during prolonged depolarization, suggesting an open-channel ..
- A common cardiac sodium channel variant associated with sudden infant death in African Americans, SCN5A S1103YLeigh D Plant
Department of Pediatrics and Institute for Molecular Pediatric Sciences, Pritzker School of Medicine, Biological Sciences Division, University of Chicago, Chicago, Illinois 60637, USA
J Clin Invest 116:430-5. 2006..Only Y1103 channels gained abnormal function, demonstrating late reopenings suppressible by the drug mexiletine. The variant appeared to confer susceptibility to acidosis-induced arrhythmia, a gene-environment interaction...
- Paced electrogram fractionation analysis of arrhythmogenic tendency in DeltaKPQ Scn5a miceCatherine E Head
Physiological Laboratory, University of Cambridge, Downing Street, Cambridge, UK
J Cardiovasc Electrophysiol 16:1329-40. 2005....
- The cutaneous analgesic effect of class I antiarrhythmic drugsJann Inn Tzeng
Department of Medical Research, Chi Mei Medical Center, Tainan, Taiwan
Anesth Analg 104:955-8. 2007..Because all Class I antiarrhythmic drugs are Na+ channel blockers, theoretically, they may have local anesthetic effects. In this study, we sought to define the cutaneous local anesthetic actions of three Class I antiarrhythmic drugs...
- Comparison of the effects of four Na+ channel analgesics on TTX-resistant Na+ currents in rat sensory neurons and recombinant Nav1.2 channelsThomas Weiser
Department CNS Research, Boehringer Ingelheim Pharma GmbH and Co KG, D 88397 Biberach, Germany
Neurosci Lett 395:179-84. 2006..2 alpha subunits. The compounds were lidocaine, mexiletine, benzocaine, and ambroxol, which are clinically used to treat pain after local or systemic administration...
- The effect of intravenously administered mexiletine on tinnitus - a pilot studyErik Berninger
Department of Audiology, Karolinska Institutet, Karolinska University Hospital, Stockholm, Sweden
Int J Audiol 45:689-96. 2006The effect of intravenously administered mexiletine on subjective tinnitus and hearing was studied in six patients, who initially responded positively to lidocaine...
- Molecular basis for exaggerated sensitivity to mexiletine in the cardiac isoform of the fast Na channelHiroyuki Kawagoe
Department of Physiology, School of Medicine, Hiroshima University, Kasumi 1 2 3, Minami Ku, 734 8551, Hiroshima, Japan
FEBS Lett 513:235-41. 2002..To examine if this is also true for mexiletine, we have systematically measured mexiletine sensitivity of the Na channel isoforms, rH1, (mu)1, and rBII, which ..
- Analysis of human Nav1.8 expressed in SH-SY5Y neuroblastoma cellsLodewijk V Dekker
Ionix Pharmaceuticals Ltd, 418 Cambridge Science Park, Cambridge CB4 0PA UK
Eur J Pharmacol 528:52-8. 2005..8 were inhibited by the sodium channel blockers BIII 890 CL, NW-1029, and mexiletine. Inhibition of Nav1.8 by these compounds may underlie their known analgesic effects in animal models.
- A common SCN5A variant alters the responsiveness of human sodium channels to class I antiarrhythmic agentsMossaab Shuraih
Electrophysiology Research Laboratory, Texas Heart Institute St Luke s Episcopal Hospital, Houston, Texas 77030, USA
J Cardiovasc Electrophysiol 18:434-40. 2007..However, little is known about the impact of those polymorphisms on the pharmocological response of hNav1.5 to various antiarrhythmic agents...
- Inhibitory effects of lidocaine and mexiletine on vasorelaxation mediated by adenosine triphosphate-sensitive K+ channels and the role of kinases in the porcine coronary arteryYoshiki Kimoto
Department of Anesthesiology, Wakayama Medical University, Wakayama, Japan
Anesthesiology 102:581-7. 2005..The current study examined whether lidocaine and mexiletine in the porcine coronary artery modify the vasorelaxation mediated by adenosine triphosphate-sensitive K channels ..
- Inactivation-deficient human skeletal muscle Na+ channels (hNav1.4-L443C/A444W) in stably transfected HEK-293 cellsS Y Wang
Department of Biology, State University of New York at Albany, Albany, NY, USA
Receptors Channels 10:131-8. 2004..Persistent late Na+currents were far more sensitive to block by class 1 anti-arrhythmic flecainide, mexiletine, propafenone, and amiodarone at 10 microM than peak Na+currents...
- [Clinical applications and the effect of mexiletine on refractory epilepsies]H Enoki
Department of Child Neurology, Okayama University Medical School
No To Hattatsu 32:29-34. 2000Twenty-four patients with refractory epilepsy were treated with mexiletine as an additional antiepileptic drug. As the initial responses, seizures were decreased by 50% or more in 7 (46...
- The sodium channel blocker RS100642 reverses down-regulation of the sodium channel alpha-subunit Na(v) 1.1 expression caused by transient ischemic brain injury in ratsC Yao
Division of Neurosciences, Walter Reed Army Institute of Research, 503 Robert Grant Ave Rm 2W14, Silver Spring, MD 20910 7500, USA
Neurotox Res 5:245-53. 2003..with the NaCh blocker and experimental neuroprotective agent RS100642 as compared to the prototype NaCh blocker mexiletine. The expression of Na(v) 1.1, Na(v) 1.2, Na(v) 1.3, Na(v) 1.7, Na(v) 1...
- Ventricular tachyarrhythmias in a canine model of LQT3: arrhythmogenic effects of sympathetic activity and therapeutic effects of mexiletineMasaomi Chinushi
School of Health Science, Niigata University School of Medicine, Japan
Circ J 67:263-8. 2003..The VSP was performed 8 times before and 5 times after administration of mexiletine in each experiment...
- Mexiletine differentially modulates vasorelaxation mediated by adenosine triphosphate-sensitive K+ channels in aortas from normotensive and hypertensive ratsYoshiki Kimoto
Department of Anesthesiology, Wakayama Medical College, Japan
Anesth Analg 96:673-9, table of contents. 2003..We designed the present study to examine whether mexiletine modulates vasorelaxation via these channels in hypertensive rat aortas...
- A molecular basis for the therapy of the long QT syndromeS G Priori
Dipartimento di Cardiologia, Facolta di Medicina e Chirurgla, , Policlinico San Matteo IRCCS, Italy
Arch Mal Coeur Vaiss 89:1185-7. 1996..Results showed that 1) mexiletine shortened significantly the QT interval among LQT3 patients but not among LQT2 patients and 2) LQT3 patients ..
- Storms of ventricular tachyarrhythmias associated with primary hyperparathyroidism in a patient with dilated cardiomyopathyChristof Kolb
Int J Cardiol 87:115-6. 2003
- [Differential diagnosis of idiopathic ventricular fibrillation]A Buob
Medizinische Universitätsklinik und Poliklinik, Innere Medizin III, Universitatskliniken des Saarlandes, Homburg Saar, Germany
Dtsch Med Wochenschr 127:2517-23. 2002
- Effects of disopyramide and mexiletine on the terminal repolarization process of the in situ heart assessed using the halothane-anesthetized in vivo canine modelHiroshi Yoshida
Department of Pharmacology, Yamanashi Medical University, Nakakoma gun, Japan
Circ J 66:857-62. 2002..Disopyramide (0.3 and 3.0 mg/kg per 10 min, n = 6) or mexiletine (0.3 and 3...
- Activation-recovery interval as a parameter to assess the intracardiac ventricular repolarization in patients with congenital long QT syndromeMasaomi Chinushi
School of Health Science, Niigata, Japan
Am J Cardiol 90:432-5. 2002
- Pharmacological rescue of mutant ion channelsConnie R Bezzina
Cardiovasc Res 55:229-32. 2002
- Possible mechanism for pharmacokinetic interaction between lidocaine and mexiletineYorinobu Maeda
Department of Pharmacy, Chugoku Rousai Hospital, 1 5 1 Hiro Tagaya, Kure City, Hiroshima 737 0193, Japan
Clin Pharmacol Ther 71:389-97. 2002Our objective was to elucidate the mechanism of pharmacokinetic interaction between lidocaine and mexiletine, because an unexpected increase in plasma lidocaine concentration accompanied by severe side effects was observed when mexiletine ..
- DDPH inhibited L-type calcium current and sodium current in single ventricular myocyte of guinea pigX D Hu
Department of Pharmacology, Tongji Medical College of Huazhong University of Science and Technology, Wuhan 430030, China
Acta Pharmacol Sin 22:415-9. 2001..L-type calcium current (ICa) and sodium current (INa), and to compare its inhibitory potency with verapamil and mexiletine. METHODS: Whole-cell patch clamp technique was used to record ICa and INa in a single ventricular myocytes of ..
- Sodium channel blocking actions of the kappa-opioid receptor agonist U50,488 contribute to its visceral antinociceptive effectsX Su
Department of Pharmacology, College of Medicine, The University of Iowa, Bowen Science Building, Iowa City, IA 52242, USA
J Neurophysiol 87:1271-9. 2002..The mean inhibitory doses of these drugs were not different (range: 6.6-10.8 mg/kg). Sodium channel blockers mexiletine and carbamazepine mimicked the effect of U50,488...
- Alteration of ischemic reperfusion injury in the rat neocortex by a potent antioxidant mexiletineC Z Chang
Department of Neurosurgery, Kaohsiung Medical University Hospital, No 100, Shih Chuan 1st Road, Kaohsiung, Taiwan, Repiblic of China
Acta Neurochir (Wien) 144:189-93; discussion 193. 2002The mechanisms by which mexiletine exerts its effects in increasing myocardial circulation, and smooth muscle perfusion and alleviating diabetic neuropathic pain have been widely discussed...
- Phase II Therapeutic Trial of Mexiletine Richard J Barohn; Fiscal Year: 2010..Most cases of NDM are related to mutations in voltage-dependent sodium or chloride channels. Mexiletine is a class 1B antiarrhythmic medication that has high affinity for muscle sodium channels...
- Local anesthetic receptor in peripheral Na+ channelsGING K WANG; Fiscal Year: 2013..amitriptyline and duloxetine, antiarrhymthic flecainide, antianginal ranolazine, and anticonvulsant mexiletine, all preferentially block persistent late Na+ currents via the LA receptor...
- Phase 2 Study of Mexiletine for the Treatment of Myotonic Dystrophy Richard T Moxley; Fiscal Year: 2013..Two recent, short-term, FDA funded, 7 week double-blind, placebo-controlled, crossover trials of mexiletine (150 mg TID vs. placebo TID;200mg TID vs. placebo TID) have been performed in our Neuromuscular Disease Center...
- MASS SPECTROMETER SYSTEM AND ACCESSORIESALAN NIES; Fiscal Year: 1990..This proposal is to develop GC/MS methodology for the analysis of mexiletine enantiomers in serum in order to determine the stereochemical aspects of disposition when mexiletine (a racemic ..
- RANDOMIZED AMIODARONE THERAPY FOR SURVIVORS OF VFLeon Greene; Fiscal Year: 1991..whether treatment with amiodarone and conventional antiarrhythmic agents (quinidine, procainamide, disopyramide, mexiletine, flecainide or tocainide) yields equivalent survival, equal suppression of ambient ventricular arrhythmias, ..
- PAIN MANAGEMENT IN PERSONS WITH DISABILITIESBarbara de Lateur; Fiscal Year: 2000..will use a double-blind, placebo-controlled, cross-over study to assess the efficacy of long acting opioids and mexiletine to ameliorate pain and improve function in persons with phantom limb pain...
- THERAPUTIC TRIAL IN PATIENTS WITH LQTS 3 GENE MUTATIONArthur Moss; Fiscal Year: 2002..aims of this study of LQT3 patients are to determine: 1) if a low dose of the oral sodium-channel blocking drug mexiletine significantly shortens QTc by greater than or equal to 40 msec; and 2) if chronic administration of mexiletine ..
- STEROSPECIFIC ANALYSIS OF NEW ANTIARRHYTHMIC AGENTSJoseph Gal; Fiscal Year: 1990..The search for new and better antiarrhythmic drugs has produced several promising agents, including mexiletine, flecainide and propafenone...
- NEUROLOGIC AIDS RESEARCH CONSORTIUMDavid Clifford; Fiscal Year: 2001..performance as a measure of disease progression, (3) A double-blind controlled study of amitriptyline and mexiletine in the treatment of HIV associated painful peripheral neuropathy, (4) A controlled clinical trial testing the ..
- REGULATION OF LATE INWARD CURRENT IN HUMAN HEART FAILUREJonathan Makielski; Fiscal Year: 2003....
- THERAPEUTIC NA+ CHANNEL BLOCKERS: RECEPTOR & DRUG DESIGNGING WANG; Fiscal Year: 2007..screening demonstrated that drugs taken orally for neuropathic pain, such as amitriptyline, flecainide, and mexiletine, also block open Na+ channels effectively at their therapeutic plasma concentrations...
- MOLECULAR BASIS OF LIGAND/SODIUM CHANNEL INTERACTIONSGING WANG; Fiscal Year: 2002....
- Cellular Mechanisms of Hyperalgesia and Opioid ToleranceJianren Mao; Fiscal Year: 2005....
- CHARGED DIHYDROPYRIDINES--PROBES OF HEART CA++ CHANNELSRobert Kass; Fiscal Year: 2001....
- PHARMACOLOGY OF CARDIAC SODIUM CHANNEL MODIFIERSMichael Sheets; Fiscal Year: 2008..The results of these studies should improve our overall understanding of the molecular mechanisms of anti-arrhythmic drugs modification of cardiac Na channels. [unreadable] [unreadable]..
- OPIOID-INDUCED PAIN SENSITIVITY: CLINICAL DIAGNOSIS AND MANAGEMENTJianren Mao; Fiscal Year: 2010....
- Glutamate Uptake & the Pathogenesis of Neuropathic PainJianren Mao; Fiscal Year: 2007..abstract_text> ..
- Neuropathic Pain Modulation by CannabinoidsJianren Mao; Fiscal Year: 2006..A better understanding of cannabinoid actions in neuropathic pain states could open a new avenue to developing novel pharmacological tools for the improved management of often intractable and debilitating neuropathic pain syndromes. ..