Tocainide
Template:Short description Template:Cs1 config Template:Drugbox Tocainide (Tonocard) is a class Ib antiarrhythmic agent. It is no longer sold in the United States.
Synthesis
Pharmacokinetics
Tocainide is a lidocaine derivative, that undergoes very less 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
Rifampicin increases conversion of tocainide into its main metabolite, tocainide carbamoyl ester glucuronlde,[9] by inducing the glucuronosyl transferase enzyme that catalyzes glucuronidation of tocainide to produce that metabolite. Rifampicin also increases elimination rate and decreases oral clearance of tocainide.[10] Tocainide decreases plasma clearance of theophylline.[11]
References
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- ↑ <templatestyles src="Citation/styles.css"/>Template:Citation/make link, Boyes RN, Byrnes EW, "Antiarrhythmisch Wirksame Verbindung, Verfahren zu Deren Herstellung und Deren Verwendung", issued Script error: No such module "auto date formatter"., assigned to Astra Pharmaceutical Products Inc.Script error: No such module "Check for unknown parameters".
- ↑ <templatestyles src="Citation/styles.css"/>Template:Citation/make link, "Primary Amino Acylanilides Methods of Making the Same and Use as Antiarrhythmic Drugs", issued Script error: No such module "auto date formatter"., assigned to Astra Pharmaceutical Products Inc.Script error: No such module "Check for unknown parameters".
- ↑ <templatestyles src="Citation/styles.css"/>Template:Citation/make link, Boyes RN, Duce BR, Smith EM, Byrnes EW, "Primaeraminoacylanilide, Verfahren zu Deren Herstellung und Sie Enthaltende Arzneimittel", issued Script error: No such module "auto date formatter"., assigned to Astra Pharmaceutical Products Inc.Script error: No such module "Check for unknown parameters".
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Further reading
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External links
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