Mexiletine drug data and news

Mexiletine drug data, resources, and news articles (when available). Onconews.org provides news on cancer research. This section, which includes profiles on medicines that may or not be cancer-related is in beta form. If things run smoothly we will be releasing a new format late in the summer of 2006.

Generic name Mexiletine
Brand Names/Synonyms CHEMBANK1425; Mexiletina [Inn-Spanish]; Mexiletine; Mexiletine Hcl; Mexiletinum [Inn-Latin]; Mexilitene; Mexilitine; Mexitil
Indication For the treatment of documented ventricular arrhythmias, such as sustained, life threatening ventricular tachycardia
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Description Not Available
Pharmacology Mexiletine, a hydantoin anticonvulsant, is used alone or with phenobarbital or other anticonvulsants to manage tonic-clonic seizures, psychomotor seizures, neuropathic pain syndromes including diabetic neuropathy, digitalis-induced cardiac arrhythmias, and cardiac arrhythmias associated with QT-interval prolongation.
Mechanism Of Action Mexiletine acts on sodium channels on the neuronal cell membrane, limiting the spread of seizure activity and reducing seizure propagation. The antiarrhythmic actions are mediated through effects on sodium channels in Purkinje fibers.
Mexiletine News
(When available)

Common genetic variation increases SIDS risk in African Americans  Feb 12, 2006
Fortunately, a drug called mexiletine, used to treat patients with arrhythmias, blocks late re-openings of sodium channels at low levels that do not interfere ... - News-Medical.net,

A genetic clue to high SIDS rate in black infants  Feb 2, 2006
Goldstein's team also found that treating cells that carried two copies of the new mutation with the drug mexiletine, used in adults with heart arrhythmias ... - Seattle Post Intelligencer

Researchers Link Mutant Gene to Crib Deaths in Blacks  Feb 2, 2006
...rapid, erratic heartbeats — under stress, but studies have shown that the heart rate can be controlled with a drug called mexiletine, which closes sodium ... - Los Angeles Times,

Common Gene Variant Linked to African American SIDS  Feb 2, 2006
Although the effects of the Y1103 variant can be suppressed by the anti-arrhythmic drug Mexitil (mexiletine), the current study needs to be replicated, and ... - CNN

Gene variation increases SIDS risk in African Americans  Feb 5, 2006
Fortunately, a drug called mexiletine, used to treat patients with arrhythmias, blocks late re-openings of sodium channels at low levels that do not interfere ... - Biology News Net (press release),

A genetic clue to high SIDS rate in black infants  Feb 2, 2006
Goldstein's team also found that treating cells that carried two copies of the new mutation with the drug mexiletine, used in adults with heart arrhythmias ... - Seattle Post Intelligencer

Researchers Link Mutant Gene to Crib Deaths in Blacks  Feb 2, 2006
...rapid, erratic heartbeats — under stress, but studies have shown that the heart rate can be controlled with a drug called mexiletine, which closes sodium ... - Los Angeles Times,

Common Gene Variant Linked to African American SIDS  Feb 2, 2006
Although the effects of the Y1103 variant can be suppressed by the anti-arrhythmic drug Mexitil (mexiletine), the current study needs to be replicated, and ... - CNN

Eyesight, toxin connection  12 Dec 2005
...current research studies are ongoing through the National Institutes of Health in Washington, DC These studies include the use of mexiletine for the treatment ... - San Bernardino Sun,

Data Reported From First Head-To-Head Study Evaluating Lidoderm(R) ...  Nov 16, 2005
...with severe hepatic disease, pregnant or nursing mothers, or those receiving Class 1 antiarrhythmic drugs (such as tocainide and mexiletine) because of the ... - PR Newswire (press release),

Local anesthetics are effective for neuropathic pain  Oct 26, 2005
The authors reviewed 30 studies on the effectiveness of Lidocaine and similar drugs Mexiletine, Tocainide and Flecainide in treating pain. ... - Xagena.it,

Local Anesthetics Are Effective For Neuropathic Pain  Oct 26, 2005
The authors reviewed 30 studies on the effectiveness of lidocaine and similar drugs mexiletine, tocainide and flecainide in treating pain. ... - Science Daily (press release)

Results Reported in Open-Label Pilot Study of Lidoderm(R) in ...  Oct 27, 2005
...with severe hepatic disease, pregnant or nursing mothers, or those receiving Class 1 antiarrhythmic drugs (such as tocainide and mexiletine) because of the ... - PR Newswire (press release),

Neuropathic Pain Market to Reach $3.5 Billion by 2014, Despite ...  Jul 11, 2005
Pfizer) and ziconotide (Elan Pharmaceuticals); sodium channel antagonists topiramate (J&J / Ortho-McNeil Pharmaceutical), mexiletine (Boehringer Ingelheim ... - Yahoo News (press release) <**results**>

Neuropathic Pain Market to Reach $3.5 Billion by 2014, Despite ...  11 Jul 2005
Pfizer) and ziconotide (Elan Pharmaceuticals); sodium channel antagonists topiramate (J&J / Ortho-McNeil Pharmaceutical), mexiletine (Boehringer Ingelheim ... - Yahoo News (press release)

FDA Sends Endo Pharmaceuticals Warning Letter Over Lidoderm Direct ...  Jun 29, 2005
Antiarrhythmic Drugs: LIDODERM should be used with caution in patients receiving Class I antiarrhythmic drugs (such as tocainide and mexiletine) since the ... - PharmaLive.com (press release),

Dosage Forms CAPSULE
Drug_Category Antiarrhythmic Agents; ATC:C01BB02
Absorption Well absorbed (90%) from the gastrointenstinal tract
Interactions Interactions for Mexiletine:

Since MEXITIL is a substrate for the metabolic pathways involving CYP2D6 and CYP1A2 enzymes, inhibition or induction of either of these enzymes would be expected to alter mexiletine plasma concentrations. In a formal, single-dose interaction study (n = 6 males) the clearance of mexiletine was decreased by 38% following the coadministration of fluvoxamine, an inhibitor of CYP1A2. In another formal study (n = 8 extensive and n = 7 poor metabolizers of CYP2D6), coadministration of propafenone did not alter the kinetics of mexiletine in the poor CYP2D6 metabolizer group. However, the metabolic clearance of mexiletine in the extensive metabolizer phenotype decreased by about 70% making the poor and extensive metabolizer groups indistinguishable. In this crossover steady state study, the pharmacokinetics of propafenone were unaffected in either phenotype by the coadministration of mexiletine. Addition of mexiletine to propafenone did not lead to further electrocardiographic parameters changes of QRS, QTc, RR, and PR intervals than propafenone alone. When concomitant administration of either of these two drugs with mexiletine is initiated, the dose of mexiletine should be slowly titrated to desired effect.

In a large compassionate use program Mexitil® has been used concurrently with commonly employed antianginal, antihypertensive, and anticoagulant drugs without observed interactions. A variety of antiarrhythmics such as quinidine or propranolol were also added, sometimes with improved control of ventricular ectopy. When phenytoin or other hepatic enzyme inducers such as rifampin and phenobarbital have been taken concurrently with Mexitil®, lowered Mexitil® plasma levels have been reported. Monitoring of Mexitil® plasma levels is recommended during such concurrent use to avoid ineffective therapy.

In a formal study, benzodiazepines were shown not to affect Mexitil® plasma concentrations. ECG intervals (PR, QRS, and QT) were not affected by concurrent Mexitil® and digoxin, diuretics, or propranolol.

Concurrent administration of cimetidine and Mexitil® has been reported to increase, decrease, or leave unchanged Mexitil® plasma levels; therefore patients should be followed carefully during concurrent therapy.

Mexitil® does not alter serum digoxin levels but magnesium-aluminum hydroxide, when used to treat gastrointestinal symptoms due to Mexitil®, has been reported to lower serum digoxin levels.

Concurrent use of Mexitil® and theophylline may lead to increased plasma theophylline levels. One controlled study in eight normal subjects showed a 72% mean increase (range 35-136%) in plasma theophylline levels. This increase was observed at the first test point which was the second day after starting Mexitil®. Theophylline plasma levels returned to pre-Mexitil® values within 48 hours after discontinuing Mexitil®. If Mexitil and theophylline are to be used concurrently, theophylline blood levels should be monitored, particularly when the Mexitil® dose is changed. An appropriate adjustment in theophylline dose should be considered.

Additionally, in one controlled study in five normal subjects and seven patients, the clearance of caffeine was decreased 50% following the administration of Mexitil®.

Toxicity Side effects may include blurred vision, chest pain, constipation, depression, diarrhea, dizziness, nausea and nervousness
Organisms Affected Humans and other mammals
Chemical IUPAC Name 1-(2,6-dimethylphenoxy)propan-2-amine
Chemical Formula C11H17NO
Molecular Weight 179.259 g/mol
Smiles String CC1=C(C(=CC=C1)C)OCC(C)N
Melting Point 203-205 °C
Water Solubility 8.3 mg/mL
State Solid
LogP/Hphobicity 2.039
Isoelectric Point Not Available
Biotransformation Primarily hepatic (85%) via CYP2D6 and CYP1A2
Half Life 10-12 hours
Protein Binding [%] 50-60%
RxList Link RXlist
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Drug Reference http://www.drugs.com/cons/Mexiletine.html
http://www.rxlist.com/cgi/generic3/mexiletine.htm
http://www.pdrhealth.com/drug_info/rxdrugprofiles/drugs/mex1261.shtml
Drug Type Approved Drug
Accession No APRD00242
CAS Registry Number 31828-71-4
KEGG Compound ID C07220
PubChem ID SID:9429
PharmGKB ID PA450488
SwissProt ID Not Available
GenBank ID Not Available
Drug ID Number [DIN] 2230359

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