Tocainide
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| Clinical data | |
|---|---|
| Trade names | Tonocard |
| AHFS/Drugs.com | Micromedex Detailed Consumer Information |
| MedlinePlus | a601248 |
| ATC code | |
| Pharmacokinetic data | |
| Bioavailability | 0.9-1 (oral) |
| Protein binding | 10-20% |
| Metabolism | glucuronidation (primary) |
| Elimination half-life | 9-14 R, 13-20 S |
| Excretion | 30-50% urine (unchanged) |
| Identifiers | |
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Tocainide (Tonocard) is a class Ib antiarrhythmic agent. It is no longer sold in the United States.
Synthesis
Pharmacokinetics
Tocainide is a
first pass metabolism. It occurs as two enantiomers. The R isomer is three times more potent than the S isomer.[5] Tocainide's oral bioavailability is almost 100%.[6] Plasma half-life generally lasts for 11.5-15.5 hours (13.5 ± 2 hours[7]). In the blood, tocainide is 10-20% protein bound.[8][6] The volume of distribution is 2.8-3.2 L/kg.[8] 31-45% is excreted unchanged in the urine.[8] The more active R-isomer is cleared faster in anephric patients (without kidneys) or those with severe kidney dysfunction. The main metabolite is tocainide carbamoyl ester glucuronlde.[9]
Drug interactions
plasma clearance of theophylline.[11]
References
- ^ DE 2235745, Boyes RN, Byrnes EW, "Antiarrhythmisch Wirksame Verbindung, Verfahren zu Deren Herstellung und Deren Verwendung", issued 1972, assigned to Astra Pharmaceutical Products Inc.
- ^ GB 1461602, "Primary Amino Acylanilides Methods of Making the Same and Use as Antiarrhythmic Drugs", issued 1974, assigned to Astra Pharmaceutical Products Inc.
- ^ DE 2400540, Boyes RN, Duce BR, Smith EM, Byrnes EW, "Primaeraminoacylanilide, Verfahren zu Deren Herstellung und Sie Enthaltende Arzneimittel", issued 1974, assigned to Astra Pharmaceutical Products Inc.
- PMID 513064.
- S2CID 24456292.
- ^ PMID 3927807.
- PMID 791536.
- ^ a b c "Kidney Disease Program (KDP)". University of Louisville. Archived from the original on 2023-12-12. Retrieved 2023-12-12.
- ^ a b Kwok DW (1987). Studies on the metabolism of tocainide in humans (Thesis). University of British Columbia.
- PMID 2495879.
- PMID 8485025.
Further reading
- Burton ME (2006). Applied Pharmacokinetics & Pharmacodynamics: Principles of Therapeutic Drug Monitoring. Lippincott Williams & Wilkins. OCLC 59148565.