The bioavailability and kinetics of dihydroquinidine in patients with heart disease

M. Regazzi Bonora, J. A. Salerno, R. Rondanelli, D. Cristiani, M. Chimienti

Research output: Contribution to journalArticlepeer-review

Abstract

The absolute bioavailability of dihydroquinidine chloride (normal tablet and sustained-release capsule) was studied in 12 hospitalized patients with heart disease. A 300-mg dose of dihydroquinidine gluconate was administered to each patient by short intravenous infusion. After a single dose of two tablets of dihydroquinidine chloride (300 mg), the average peak concentration was 0.74 ± 0.43 mg/l (± SD); following administration two capsules of the sustained-release form (500 mg dihydroquinidine chloride) the average peak concentration was 0.55 ± 0.25 mg/l. T[max] was approximately 5 h with the dihydroquinidine tablet and 7 h with the dihydroquinidine capsule. The mean absolute biovailability was 89 ± 9% for the conventional tablet and 52 ± 15% for the sustained-release capsule. After intravenous infusion of dihydroquinidine (2.63 ± 0.29 mg/kg), the disposition of the drug is described by a two-compartment open model. The volume of distribution (V[d]) was 4.67 l/kg. Distribution (t[1/2α] = 18.63 ± 15.2 h) and the apparent elimination half-life (t[1/2β] = 10.8 ± 4.7 h) were longer than the corresponding values reported by Ueda et al. [1976]. These discrepancies are presumably due to the different sampling period that was extended to 24 h in our study, consequently evidencing a slower rate of elimination from 12 to 24 h. Mean total body clearance (Cl) was 0.28 ± 0.057 l/h/kg. Urine sample collection for 48 h showed 21% of the dose was excreted unchanged. The renal clearance (Cl[r]) was 0.062 ± 0.018 l/h/kg.

Original languageEnglish
Pages (from-to)212-218
Number of pages7
JournalInternational Journal of Clinical Pharmacology Therapy and Toxicology
Volume20
Issue number5
Publication statusPublished - 1982

ASJC Scopus subject areas

  • Toxicology
  • Pharmacology (medical)

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