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Pharmacokinetics of chlormethiazole in humans

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Summary

The pharmacokinetics of chlormethiazole have been studied in six healthy volunteers following an intravenous infusion of the drug. The log. plasma concentration-time curve of chlormethiazole after cessation of the infusion was found to be curvilinear and was fitted therefore, by a bi-exponential equation computed by non-linear least squares regression analysis. Half-lives for the inital α-phase (0.54±0.05 h) and the terminal β-phase (4.05 ±0.60 h) were calculated together with other pharmacokinetic parameters of the two compartment open model. An explanation for the discrepancy between the presently reported plasma half-lives and those appearing in the literature has been presented. The pharmacokinetic treatment of the plasma concentration-time data obtained following intravenous infusion also enabled the prediction that the maximal systemic availability of an orally administered dose of chlormethiazole would be of the order of 15%.

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Moore, R.G., Triggs, E.J., Shanks, C.A. et al. Pharmacokinetics of chlormethiazole in humans. Eur J Clin Pharmacol 8, 353–357 (1975). https://doi.org/10.1007/BF00562662

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  • DOI: https://doi.org/10.1007/BF00562662

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