PMID: 3772736Aug 1, 1986Paper

In vivo interaction of the enantiomers of disopyramide in human subjects

Journal of Pharmacokinetics and Biopharmaceutics
K M GiacominiT F Blaschke

Abstract

Disopyramide, an antiarrhythmic agent, is marketed as a racemic mixture of two enantiomers. The racemic drug has unusual pharmacokinetic properties because of its concentration-dependent binding to plasma proteins in the therapeutic plasma concentration range. This study examined, in healthy subjects, the individual pharmacokinetic properties of both total and unbound d- and 1-disopyramide in plasma after intravenous administration of each enantiomer separately (1.5 mg/kg). Also investigated is the pharmacokinetics of total d- and 1-disopyramide in plasma after intravenous administration of a pseudoracemate. Both d- and 1-disopyramide are found to exhibit concentration-dependent binding to plasma proteins, with d-disopyramide being more avidly bound at lower concentrations. The stereoselective, concentration-dependent binding to plasma proteins resulted in distinct pharmacokinetic properties when the enantiomers were given together as the pseudoracemate. d-Disopyramide had a lower plasma clearance and renal clearance, a longer half-life, and a smaller apparent volume of distribution than 1-disopyramide. However, when the enantiomers were administered separately, there were no differences in the clearance, renal clearance, and v...Continue Reading

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Citations

Jan 1, 1991·European Journal of Clinical Pharmacology·J HasselströmR Dahlqvist
Feb 19, 1993·Pharmacy World & Science : PWS·D T WitteR A De Zeeuw
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Jul 10, 2002·Clinical Pharmacokinetics·Reza MehvarMajid Vakily
May 8, 2004·CNS Spectrums·Andrew J Hutt
Sep 1, 1989·Journal of Pharmaceutical Sciences·F JamaliF M Pasutto

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