Tocainide detailed information

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Tocainide detailed information
Gene therapy
Clinical data
ATC code
Physiological data
Legal status
Pharmacokinetic data
Bioavailability0.9-1 (oral)
Protein binding10-20%
Metabolismglucuronidation (primary)
Elimination half-life9-14 R, 13-20 S
Excretion30-50% urine (unchanged)
Identifiers
CAS Number
PubChem Template:Abbreviation
DrugBank
Chemical and physical data
FormulaC11H16N2O
Molar mass192.258 g/mol

Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]


Overview

Tocainide (Tonocard®) is a class Ib antiarrhythmic agent. It is no longer sold in the United States.

Quick look at the Pharmacokinetics

Tocaine is a lidocaine analog, that does not have significant 1st pass metabolism. It is found in two enantiomers. The R isomer is 4x as potent as the S. Oral bioavaliability is 0.9-1.0. In the blood tocainide is 10-20% protein bound. The Volume of distribution is 2.5-3.5 L/kg. 30-50% is excreted unchanged in the urine. The more active R-isomer is cleared faster in anephric patients or those with severe renal dysfunction. The main metabolite is the glucuronidated tocainide carbamic acid. The glucuronosyl transferase is apparently induced by rifampin. Weak inhibition of Cyp1A2 leads to a mild theophylline interaction. (Not verbatim)

Burton ME. Applied Pharmacokinetics & Pharmacodynamics: Principles of Therapeutic Drug Monitoring. 4th ed. Philadelphia: Lippincott Williams & Wilkins; 2006.


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