Mexirate

Mexirate Uses, Dosage, Side Effects, Food Interaction and all others data.

Antiarrhythmic agent pharmacologically similar to lidocaine. It may have some anticonvulsant properties.

Mexirate is a local anesthetic, antiarrhythmic agent (Class Ib), structurally similar to lidocaine, but orally active. Mexirate has fast onset and offset kinetics, meaning that they have little or no effect at slower heart rates, and more effects at faster heart rates. It shortens the action potential duration, reduces refractoriness, and decreases Vmax in partially depolarized cells with fast response action potentials. Mexirate either does not change the action potential duration, or decreases the action potential duration.

Trade Name Mexirate
Availability Prescription only
Generic Mexiletine
Mexiletine Other Names Mexiletina, Mexilétine, Mexiletine, Mexiletinum
Related Drugs propranolol, atenolol, amiodarone, lidocaine, verapamil, flecainide, Tenormin, Inderal, dofetilide
Type
Formula C11H17NO
Weight Average: 179.2588
Monoisotopic: 179.131014171
Protein binding

50-60%

Groups Approved, Investigational
Therapeutic Class
Manufacturer
Available Country Japan
Last Updated: September 19, 2023 at 7:00 am
Mexirate
Mexirate

Uses

Mexirate is a class 1B antiarrhythmic agent used in the treatment of documented ventricular arrhythmias that warrant treatment.

For the treatment of ventricular tachycardia and symptomatic premature ventricular beats, and prevention of ventricular fibrillation.

Mexirate is also used to associated treatment for these conditions: Severe Ventricular tachycardia, Severe ventricular arrhythmias

How Mexirate works

Mexirate, like lidocaine, inhibits the inward sodium current required for the initiation and conduction of impulses, thus reducing the rate of rise of the action potential, Phase 0. It achieves this reduced sodium current by inhibiting sodium channels. Mexirate decreases the effective refractory period (ERP) in Purkinje fibers in the heart. The decrease in ERP is of lesser magnitude than the decrease in action potential duration (APD), which results in an increase in the ERP/APD ratio. It does not significantly affect resting membrane potential or sinus node automaticity, left ventricular function, systolic arterial blood pressure, atrioventricular (AV) conduction velocity, or QRS or QT intervals

Toxicity

Symptoms of overdose include nausea, hypotension, sinus bradycardia, paresthesia, seizures, bundle branch block, AV heart block, asystole, ventricular tachyarrythmia, including ventricular fibrillation, cardiovascular collapse, and coma.

Food Interaction

  • Take with food. Food reduces irritation.

Volume of Distribution

  • 5 to 7 L/lg

Elimination Route

Well absorbed (bioavailability 90%) from the gastrointenstinal tract.

Half Life

10-12 hours

Elimination Route

Approximately 10% is excreted unchanged by the kidney. The urinary excretion of N-methylmexiletine in man is less than 0.5%.

Innovators Monograph

You find simplified version here Mexirate

http://classyfire.wishartlab.com/tax_nodes/C0000000
http://classyfire.wishartlab.com/tax_nodes/C0002448
http://classyfire.wishartlab.com/tax_nodes/C0002341
http://classyfire.wishartlab.com/tax_nodes/C0002341
http://classyfire.wishartlab.com/tax_nodes/C0004209
http://classyfire.wishartlab.com/tax_nodes/C0004742
http://classyfire.wishartlab.com/tax_nodes/C0000128
http://classyfire.wishartlab.com/tax_nodes/C0004557
http://classyfire.wishartlab.com/tax_nodes/C0000469
http://classyfire.wishartlab.com/tax_nodes/C0004150
https://www.ebi.ac.uk/chebi/searchId.do?chebiId=CHEBI:6916
http://www.hmdb.ca/metabolites/HMDB0014523
http://www.genome.jp/dbget-bin/www_bget?cpd:C07220
https://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=4178
https://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46505491
https://www.chemspider.com/Chemical-Structure.4034.html
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=50117271
https://mor.nlm.nih.gov/RxNav/search?searchBy=RXCUI&searchTerm=6926
https://www.ebi.ac.uk/chebi/searchId.do?chebiId=6916
https://www.ebi.ac.uk/chembldb/index.php/compound/inspect/CHEMBL558
http://bidd.nus.edu.sg/group/cjttd/ZFTTDDRUG.asp?ID=DAP000505
http://www.pharmgkb.org/drug/PA450488
http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2629
http://www.rxlist.com/cgi/generic3/mexiletine.htm
https://www.drugs.com/cdi/mexiletine.html
http://www.pdrhealth.com/drug_info/rxdrugprofiles/drugs/mex1261.shtml
https://en.wikipedia.org/wiki/Mexiletine
*** Taking medicines without doctor's advice can cause long-term problems.
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