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The pharmacokinetics and organ distribution of ajmaline and quinidine in the mouse

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Summary

After i.v. infusion into mice (lasting 10 s) the time courses of ajmaline and quinidine concentrations in blood, heart, lung, liver, and brain were studied. The drugs were assayed by a spectrofluorophotometric procedure. Blood concentration data obtained were fitted graphically and calculations were performed in accordance with an open two compartment model.

Blood kinetic data were very similar for both alkaloids. A rapid distribution phase with a t 0.5α of 3.0 min for ajmaline and 2.5 min for quinidine was followed by a disposition phase with a t0.5β of 16 min for ajmaline and 20 min for quinidine. High tissue accumulation of both alkaloids was found in lung, liver, and heart and this is also reflected by the volume of distribution V dβ, which was 136 ml for ajmaline and 116 ml for quinidine (body weight of the mice=31 g). With equilibrium dialysis a 62% binding of ajmaline and a 77% binding of quinidine to mouse blood constituents was found. Both drugs were highly metabolized since only 5% of a given dose was excreted unchanged in the urine.

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  1. Abteilung für Pharmakologie der Medizinischen Hochschule Lübeck, Ratzeburger Allee 160, D-2400, Lübeck, Germany

    H. Iven

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Iven, H. The pharmacokinetics and organ distribution of ajmaline and quinidine in the mouse. Naunyn-Schmiedeberg's Arch. Pharmacol. 298, 43–50 (1977). https://doi.org/10.1007/BF00510985

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  • DOI: https://doi.org/10.1007/BF00510985

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