Summary
The plasma level and urinary excretion rate of guanethidine have been measured in 30 patients during oral maintenance therapy, and in 5 patients following discontinuation of therapy. A significant correlation was found between the daily average urinary excretion and the maintenance dose, although wide interindividual variation was noted among patients maintained on the same dose. A statistically significant correlation was also observed between the area under the plasma level curve during the dose interval and the oral maintenance dose. After discontinuation of chronic therapy, the half-life of 1.5 days of the initial phase of elimination was essentially in agreement with the half-life of almost 2 days determined in acute studies. In addition, a second phase of elimination with a half-life of 4 to 8 days was observed.
Similar content being viewed by others
References
Bisson, G. M., Muscholl, E.: Die Beziehungen zwischen der Guanethidin-Konzentration im Rattenherzen und dem Noradrenalingehalt. Naunyn-Schmiedebergs Arch. Pharmakol. exptl. Pathol.244, 185 (1962)
Chang, C. C., Costa, E., Brodie, B. B.: Reserpin-induced release of drugs from sympathetic nerve endings. Life Sci.3, 839 (1964)
Hengstmann, J. H., Weyand, U., Dengler, H. J.: The pysiological disposition of etilefrine in man. Europ. J. clin. Pharmacol.9, 179 (1975)
Hengstmann, J. H., Hengstmann, R., Brecht, Th.: Pharmacokinetics of the antihypertensive drug guabenzodioxan in man. 7th Int. Congr. Pharmacol. Abstr. No 2798
Hengstmann, J. H., Falkner, F. C., Watson, J. T., Oates, J.: Quantitative determination of guanethidine and other guanidocontaining drugs in biological fluids by gas chromatography with flame ionization detection and multiple ion detection. Anal Chem.46, 34 (1974)
Leishman, A. W. D., Matthews, H. L., Smith, A. J.: Guanethidine — hypotensive drug with prolonged action. Lancet1959/II, 1044
McMartin, C., Rondel, R. K., Winter, J., Allan, B. R., Humberstone, P., Leishman, A. W. D., Sandler, G., Thirkettle, J. L.: The fate of guanethidine in two hypertensive patients. Clin. Pharmacol. Ther.11, 423 (1970)
McMartin, C., Simpson, P.: The absorption and metabolism of guanethidine in hypertensive patients requiring different doses of the drug. Clin. Pharmacol. Ther.12 73 (1971)
Rahn, K. H.: Plasmaspiegel und renale Ausscheidung von Guanethidin bei Hypertonikern. Arzneim. Forsch. (Drug Res.)21, 1487 (1971)
Rahn, K. H.: The influence of renal function on plasma levels, urinary excretion, metabolism, and antihypertensive effect of guanethidine (Ismelin) in man. Clin. Nephrology1, 14 (1973)
Rahn, K. H., Goldberg, L. I.: Comparison of antihypertensive efficacy, intestinal absorption, and excretion of guanethidine in hypertensive patients. Clin. Pharmacol. Ther.10, 858 (1969)
Author information
Authors and Affiliations
Additional information
Supported by Deutsche Forschungsgemeinschaft (He 791/4)
Rights and permissions
About this article
Cite this article
Hengstmann, J.H., Falkner, F.C. Disposition of guanethidine during chronic oral therapy. Eur J Clin Pharmacol 15, 121–125 (1979). https://doi.org/10.1007/BF00609875
Received:
Accepted:
Issue Date:
DOI: https://doi.org/10.1007/BF00609875