Pharmacokinetics of hydroxy-3(S)-dihydroquinidine in healthy volunteers after intravenous and oral administration
- Resource Type
- Original Paper
- Authors
- Jaillon, P.; Poirier, J. M.; Lecocq, B.; Jarreau, C.; Pays, M.; Richard, M. O.; Cheymol, G.
- Source
- European Journal of Drug Metabolism and Pharmacokinetics. July 1986 11(3):233-238
- Subject
- Pharmacokinetics
hydroxy-3(S)-dihydroquinidine
healthy volunteers
- Language
- English
- ISSN
- 0378-7966
2107-0180
Summary:The pharmacokinetics of hydroxy-3(S)-dihydroquinidine (HDHQ) were studied in 6 healthy volunteers following a 15 min intravenous infusion of a 300 or 400 mg dose, a 300 mg oral dose in solution and a 300 mg tablet administration on three separate occasions (random order) with at least one week intervals. Using a specific HPLC assay for HDHQ, the post-infusion and post-absorption plasma HDHQ concentrations declined bi-exponentially. Both oral forms of HDHQ were absorbed rapidly (tmax 1 h – 1.2 h) with an absolute bioavailability of the oral solution (F = 0.54 to 0.93) which was not significantly different from that of the tablet (F = 0.66 to 0.90). HDHQ was rapidly and extensively distributed to the tissues with a high steady-state volume of distribution (6.82 ± 1.85 l.kg-1). Mean elimination half-life was 6.7 ± 1.4 h after IV infusion, 8.4 ± 1.7 h after the oral solution and 11.3 ± 4.4 h after the tablet administration. HDHQ was partially eliminated from the body in the unchanged non-conjugated form by the urine and renal clearance represented approximately 50% of the total body clearance.These results show that HDHQ is rapidly and almost completely absorbed and has potential for a twice daily administration regimen for the treatment of cardiac arrhythmias.