Abstract
The pharmacokinetics of propranolol in blood was studied in healthy volunteers, following intravenous administration of 0.1 mg/kg and increasing oral doses of 10,20, and 40 mg, using a specific and sensitive gas Chromatographie method. The systemic availability of orally administered propranolol varied from 9% to 38% between subjects, but it was constant within each subject. A linear relationship was found between the area under the blood concentration-time curve and the oral dose. At variance with literature data, we could not observe a threshold dose.
This is a preview of subscription content, log in via an institution to check access.
Similar content being viewed by others
References
E. di Salle, K. M. Baker, F. R. Bareggi, W. D. Watkins, C. A. Chidsey, A. Frigerio, and P. L. Morselli. A sensitive gas Chromatographic method for the determination of propranolol in human plasma.J. Chromatog. 84:347–353 (1973).
P. L. Morselli, A. Morganti, G. Bianchetti, E. di Salle, G. Leonetti, C. A. Chidsey, and A. Zanchetti. Plasma levels and pharmacokinetic studies of propranolol during chronic treatment in hypertensive patients.Eur. J. Clin. Invest. 4:347, abst. 118 (1974).
G. Leonetti, G. Mayer, A. Morganti, L. Terzoli, A. Zanchetti, G. Bianchetti, E. di Salle, P. L. Morselli, and C. A. Chidsey. Hypotensive and renin-suppressing activities of propranolol in hypertensive patients.Clin. Sci. Mol. Med. 48:491–499 (1975).
C. A. Chidsey, P. L. Morselli, G. Bianchetti, A. Morganti, G. Leonetti, and A. Zanchetti. Studies of the absorption and removal of propranolol in hypertensive patients during therapy.Circulation 52:313–318 (1975).
D. G. Shand and R. E. Rangno. The disposition of propranolol. I. Elimination during oral absorption in man.Pharmacology 7:159–168 (1972).
C. M. Metzler. NONLIN, Technical Report No. 7292/69/7293/005, Upjohn Co., Kalamazoo, Mich., 1969.
J. C. K. Loo and S. Riegelman. Assessment of pharmacokinetic constants from postinfusion blood curves obtained after infusion.J. Pharm. Sci. 59:53–55 (1970).
J. M. Ottaway. Normalization in the fitting of data by iterative methods-application to tracer kinetics and enzyme kinetics.Biochem. J. 134:729–736 (1973).
S. Riegelman, J. Loo, and M. Rowland. Concept of volume of a volume of distribution and possible errors in the evaluation of these parameters.J. Pharm. Sci. 57:128–133 (1968).
J. G. Wagner,Fundamentals of Clinical Pharmacokinetics, Drug Intelligence Publications, Hamilton, Ill., 1975, pp. 82–90.
H. G. Boxenbaum, S. Riegelman, and R. M. Elashoff. Statistical estimation in pharmacokinetics.J. Pharmacokin. Biopharm. 2:123–148 (1974).
G. H. Evans and D. G. Shand. Disposition of propranolol. VI. Independent variation in steady-state circulating drug concentrations and half-life as result of plasma drug binding in man.Clin. Pharmacol. Ther. 14:494–500 (1973).
A. S. Nies and D. G. Shand. Clinical pharmacology of propranolol.Circulation 52:6–15 (1975).
C. A. Chidsey, A. Zanchetti, P. L. Morselli, and G. Leonetti. Pharmacokinetic and pharmacodynamic studies of propranolol in hypertension. In P. Milliez and M. Safar (eds.),Recent Advances in Hypertension, Laboratories Boehringer, Ingelheim, West Germany, 1975, pp. 319–326.
G. H. Evans, A. S. Nies, and D. G. Shand. The disposition of propranolol. III. Decreased half-life and volume of distribution as a result of plasma binding in man, monkey, dog and rat.J Pharmacol. Exp. Ther. 186:114–121 (1973).
D. T. Lowenthal, W. A. Briggs, T. P. Gibson, H. Nelson, and W. J. Cirksena. Pharmacokinetics of oral propranolol in chronic renal disease.Clin. Pharmacol. Ther. 16:761–769 (1974).
G. Bianchetti, G. Graziani, D. Brancaccio, A. Morganti, G. Leonetti, M. Manfrin, R. Sega, R. Gomeni, C. Ponticelli, and P. L. Morselli. Pharmacokinetics and effects of propranolol in terminal uraemic patients and in patients undergoing regular dialysis treatment.Clin. Pharmacokin. 1:373–384 (1976).
J. W. Paterson, M. E. Conolly, C. T. Dollery, A. Hayes, and R. G. Cooper. The pharmacodynamics and metabolism of propranolol in man.Pharmacol. Clin. 2:127–133 (1970).
C. F. George, M. L'E. Orme, P. Buranapong, D. Macerlean, A. M. Breckenridge, and C. T. Dollery. Contribution of the liver to overall elimination of propranolol.J. Pharmacokin. Biopharm. 4:17–27(1976).
Author information
Authors and Affiliations
Rights and permissions
About this article
Cite this article
Gomeni, R., Bianchetti, G., Sega, R. et al. Pharmacokinetics of propranolol in normal healthy volunteers. Journal of Pharmacokinetics and Biopharmaceutics 5, 183–192 (1977). https://doi.org/10.1007/BF01065394
Received:
Revised:
Published:
Issue Date:
DOI: https://doi.org/10.1007/BF01065394