Tocainida

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

An antiarrhythmic agent which exerts a potential- and frequency-dependent block of sodium channels.

Tocainida is a primary amine analog of lidocaine with antiarrhythmic properties useful in the treatment of ventricular arrhythmias. Tocainida, like lidocaine, produces dose dependent decreases in sodium and potassium conductance, thereby decreasing the excitability of myocardial cells. In experimental animal models, the dose-related depression of sodium current is more pronounced in ischemic tissue than in normal tissue. Tocainida is a Class I antiarrhythmic compound with electrophysiologic properties in man similar to those of lidocaine, but dissimilar from quinidine, procainamide, and disopyramide.

Trade Name Tocainida
Availability Discontinued
Generic Tocainide
Tocainide Other Names Tocainida, Tocainide, Tocainidum
Related Drugs propranolol, amiodarone, lidocaine, verapamil, sotalol, magnesium sulfate, Inderal, dofetilide, acebutolol, Epsom Salt
Type
Formula C11H16N2O
Weight Average: 192.2575
Monoisotopic: 192.126263144
Protein binding

Approximately 10 percent bound to plasma protein.

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

Uses

Tocainida is an orally active class 1b antiarrhythmic agent that interferes with cardiac sodium channels and typically used to treat ventricular arrhythmias.

For the treatment of documented ventricular arrhythmias, such as sustained ventricular tachycardia, that, in the judgment of the physician, are life-threatening.

How Tocainida works

Tocainida acts on sodium channels on the neuronal cell membrane, limiting the spread of seizure activity and reducing seizure propagation. Tocainida binds preferentially to the inactive state of the sodium channels.The antiarrhythmic actions are mediated through effects on sodium channels in Purkinje fibers.

Toxicity

The oral LD50 of tocainide was calculated to be about 800 mg/kg in mice, 1000 mg/kg in rats, and 230 mg/kg in guinea pigs; deaths were usually preceded by convulsions.

Elimination Route

Following oral administration, the bioavailability approaches 100 percent, and is unaffected by food.

Half Life

The average plasma half-life in patients is approximately 15 hours. May be prolonged up to 35 hours in patients with severe renal function impairment (creatinine clearance less than 30 mL per min per 1.73 square meters of body surface area.

Innovators Monograph

You find simplified version here Tocainida

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http://classyfire.wishartlab.com/tax_nodes/C0004150
https://www.ebi.ac.uk/chebi/searchId.do?chebiId=CHEBI:9611
http://www.hmdb.ca/metabolites/HMDB0015189
http://www.genome.jp/dbget-bin/www_bget?drug:D06172
http://www.genome.jp/dbget-bin/www_bget?cpd:C07142
https://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=38945
https://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46505385
https://www.chemspider.com/Chemical-Structure.35632.html
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=50092595
https://mor.nlm.nih.gov/RxNav/search?searchBy=RXCUI&searchTerm=42359
https://www.ebi.ac.uk/chebi/searchId.do?chebiId=9611
https://www.ebi.ac.uk/chembldb/index.php/compound/inspect/CHEMBL1762
http://bidd.nus.edu.sg/group/cjttd/ZFTTDDRUG.asp?ID=DAP000517
http://www.pharmgkb.org/drug/PA451706
http://www.rxlist.com/cgi/generic3/tocainide.htm
https://www.drugs.com/mtm/tocainide.html
http://www.pdrhealth.com/drug_info/rxdrugprofiles/drugs/ton1451.shtml
https://en.wikipedia.org/wiki/Tocainide
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