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Comparison of the pharmacokinetics of intravenous dl-propranolol in borderline and permanent hypertension

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Summary

In borderline and permanent hypertensives after rapid i.v. injection of dl-propranolol 0.2 mg/kg plasma levels were measured and were fitted to a two-compartment open-model. In borderline patients, characterized by a high basal cardiac output (CO), plasma levels were always lower than in permanent hypertensives. The biological half-life was reduced and the central volume of distribution, volume of distribution at pseudo-equilibrium and total clearance (TC) were markedly increased. In the overall population, there was a significant positive correlation between CO and TC. Rapid achievement of a predetermined plateau in each group constituted experimental proof of the validity of the two-compartment open-model for kinetic analysis of propranolol i.v. If kinetic parameters from permanent hypertensives were applied to borderline hypertensives a lower plateau was obtained. Thus, in so far as β-blockade is related to plasma level of propranolol, an increased intravenous dose may be required in patients with high CO.

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Weiss, Y.A., Safar, M.E., Chevillard, C. et al. Comparison of the pharmacokinetics of intravenous dl-propranolol in borderline and permanent hypertension. Eur J Clin Pharmacol 10, 387–393 (1976). https://doi.org/10.1007/BF00563074

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  • DOI: https://doi.org/10.1007/BF00563074

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