Abstract
The pharmacokinetics of R(-) and S(+)- tocainide were studied in twelve patients requiring intravenous tocainide. In all patients, a progressive increase in the S(+):R(-) ratio was observed during the infusion. Mean +/- s.d. ratios increased from 1.03 +/- 0.05 at 2 min to 1.76 +/- 0.35 at 48.5 h. Data from eight patients were fitted to a two-compartment model and there was a significant difference (Wilcoxon matched-pairs test P less than 0.01) in the clearance estimates for the two enantiomers. The median values were: S(+)-tocainide = 6.25 l h-1 and R(-)-tocainide = 9.31 l h-1. There was no differences in V1 or Vss.
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- Antonsson A. M., Gyllenhaal O., Kylberg-Hanssen K., Johansson L., Vessman J. Monitoring of S- and R-tocainide in human plasma after heptafluorobutyrylation, separation on Chirasil-Val and electron-capture detection. J Chromatogr. 1984 Jun 8;308:181–187. doi: 10.1016/s0021-9673(01)87544-0. [DOI] [PubMed] [Google Scholar]
- Ariëns E. J. Stereochemistry, a basis for sophisticated nonsense in pharmacokinetics and clinical pharmacology. Eur J Clin Pharmacol. 1984;26(6):663–668. doi: 10.1007/BF00541922. [DOI] [PubMed] [Google Scholar]
- Breckenridge A., Orme M., Wesseling H., Lewis R. J., Gibbons R. Pharmacokinetics and pharmacodynamics of the enantiomers of warfarin in man. Clin Pharmacol Ther. 1974 Apr;15(4):424–430. doi: 10.1002/cpt1974154424. [DOI] [PubMed] [Google Scholar]
- Byrnes E. W., McMaster P. D., Smith E. R., Blair M. R., Boyes R. N., Duce B. R., Feldman H. S., Kronberg G. H., Takman B. H., Tenthorey P. A. New antiarrhythmic agents. 1. Primary alpha-amino anilides. J Med Chem. 1979 Oct;22(10):1171–1176. doi: 10.1021/jm00196a005. [DOI] [PubMed] [Google Scholar]
- Elvin A. T., Keenaghan J. B., Byrnes E. W., Tenthorey P. A., McMaster P. D., Takman B. H., Lalka D., Manion C. V., Baer D. T., Wolshin E. M. Tocainide conjugation in humans: novel biotransformation pathway for a primary amine. J Pharm Sci. 1980 Jan;69(1):47–49. doi: 10.1002/jps.2600690113. [DOI] [PubMed] [Google Scholar]
- Gal J., French T. A., Zysset T., Haroldsen P. E. Disposition of (R,S)-tocainide. Some stereoselective aspects. Drug Metab Dispos. 1982 Jul-Aug;10(4):399–404. [PubMed] [Google Scholar]
- Holmes B., Brogden R. N., Heel R. C., Speight T. M., Avery G. S. Tocainide. A review of its pharmacological properties and therapeutic efficacy. Drugs. 1983 Aug;26(2):93–123. doi: 10.2165/00003495-198326020-00001. [DOI] [PubMed] [Google Scholar]
- Lalka D., Meyer M. B., Duce B. R., Elvin A. T. Kinetics of the oral antiarrhythmic lidocaine congener, tocainide. Clin Pharmacol Ther. 1976 Jun;19(6):757–766. doi: 10.1002/cpt1976196757. [DOI] [PubMed] [Google Scholar]
- Morganroth J., Panidis I. P., Harley S., Johnson J., Smith E., MacVaugh H. Efficacy and safety of intravenous tocainide compared with intravenous lidocaine for acute ventricular arrhythmias immediately after cardiac surgery. Am J Cardiol. 1984 Dec 1;54(10):1253–1258. doi: 10.1016/s0002-9149(84)80075-2. [DOI] [PubMed] [Google Scholar]
- Sedman A. J., Bloedow D. C., Gal J. Serum binding of tocainide and its enantiomers in human subjects. Res Commun Chem Pathol Pharmacol. 1982 Oct;38(1):165–168. [PubMed] [Google Scholar]
- Sedman A. J., Gal J., Mastropaolo W., Johnson P., Maloney J. D., Moyer T. P. Serum tocainide enantiomer concentrations in human subjects. Br J Clin Pharmacol. 1984 Jan;17(1):113–115. doi: 10.1111/j.1365-2125.1984.tb05012.x. [DOI] [PMC free article] [PubMed] [Google Scholar]