Summary
Dose tolerance and pharmacokinetic studies of pseudoephedrine sustained action capsules were performed in thirty-three adult male subjects who received either 120 mg or 150 mg capsules every twelve hours for seven consecutive days in a double-blind parallel design study. Although only one subject in the 150 mg group was discontinued prematurely from this study, a large number of side effects typical of CNS stimulation were seen. A placebo effect might account for a portion of these complaints, however symtoms evaluated as being due to drug were significantly more severe and persistent in the 150 mg group. Pulse rates showed a persistent and significant increase while systolic and diastolic blood pressure fell from the baseline values in both groups. A pharmacokinetic analysis of the pseudoephedrine plasma concentration-time data provided estimates of half-life and the volume of distribution/availability ratio. The values obtained were in good agreement with values reported by others. Half-life was not influenced by urine pH probably as a result of the narrow range of urine pHs observed in the subjects. Calculations of relative bioavailability suggest that the 120 mg capsule formulation has a 30% greater bioavailability compared to the 150 mg capsule.
This is a preview of subscription content, log in via an institution to check access.
Similar content being viewed by others
References
Bye, C., Hill, H. M., Hughes, D. T. D., Peck, A. W.: A comparison of plasma levels of L (+) pseudoephedrine following different formulations and their relation to cardiovascular and subjective effects in man. Europ. J. clin. Pharmacol.8, 47–53 (1975)
Cummins, L. M., Fourier, M. J.: GLC determination of pseudoephedrine and related ephedrines in serum as the heptafluorobutyryl derivatives. Anal. Lett2, 403–409 (1969)
Metzler, C. M.: Nonlin: A computer program for parameter estimation in nonlinear situations, Upjohn Co., Kalamazoo, Michigan. Technical report no. 7292/69/7292/005, November 25, 1969
Colburn, W. A., Shen, D., Gibaldi, M.: Pharmacokinetic analysis of drug concentration data obtained during repetitive drug administration. J. Pharmacokin. Biopharm.4, 469–486 (1976)
Wagner, J. G., Northam, J. D., Alway, C. D., Carpenter, O. S.: Blood levels of drug at the equilibrium state after multiple dosing. Nature207, 1301–1302 (1965)
Gibaldi, M., Perrier, D.: Pharmacokinetics, p. 150. New York: Marcel Dekker 1975
Bye, C., Dewsbury, D., Peck, A. W.: Effects on the human central nervous system of two isomers of ephedrine and triprolidine and their interaction. Brit. J. Clin. Pharmacol.1, 71–78 (1974)
Aviado, D. M., Wnuck, A. L., DeBeer, E. J.: Cardiovascular effects of sympathomimetic bronchodilators: epinephrine, ephedrine, pseudoephedrine, isoproterenol, methoxyphenamine and isoprophenamine. J. Pharmacol. Exp. Ther.122, 406–417 (1958)
Patil, P. N., Tye, A., Lapidus, J. B.: A pharmacological study of the ephedrine isomers. J. Pharmacol. Exp. Ther.148, 158–168 (1965)
Koelle, G. B.: Neurohumoral transmission and the autonomic nervous system. In: The Pharmacological basis of therapeutics. (L. S. Goodman and A. Gilman) (eds.), pp. 404–444. New York: Macmillan 1975
Innes, I. R., Nickerson, M.: Norepinephrine, epinephrine and the sympathomimetic amines. In: The pharmacological basis of therapeutics. L. S. Goodman and A. Gilman (eds.) pp. 477–513. New York: Macmillan 1975
Kuntzman, R. G., Tsai, I., Brand, L., Mark, L. C.: The influence of urinary pH on the plasma half-life of pseudoephedrine in man and dog and a sensitive assay for its determination in human plasma. Clin. Pharmacol. Ther.12, 62–67 (1970)
Benson, M. K.: Maximal basal respiratory flow rate: its use in assessing the effect of pseudoephedrine in vasomotor rhinitis. Europ. J. clin. Pharmacol.3, 182–184 (1971)
Empey, D. W., Bye, C., Hodder, M., Hughes, D. T. D.: A double-blind crossover trial of pseudoephedrine and triprolidine alone and in combination, for the treatment of allergic rhinitis. Annals Allergy34, 41–46 (1975)
Lipschutz, A.: Oral decongestion therapy in allergic respiratory diseases of children. Annals Allergy18, 998–1003 (1960)
Miller, G. F.: Influence of an oral decongestant on eustachian tube function in children. J. Allergy45, 187–193 (1970)
Siegel, S.: Nonparametric statistics for the behavioral sciences, p. 96–104 New York: McGraw-Hill 1956
Author information
Authors and Affiliations
Rights and permissions
About this article
Cite this article
Dickerson, J., Perrier, D., Mayersohn, M. et al. Dose tolerance and pharmacokinetic studies of L (+) pseudoephedrine capsules in man. Eur J Clin Pharmacol 14, 253–259 (1978). https://doi.org/10.1007/BF00560458
Received:
Revised:
Accepted:
Issue date:
DOI: https://doi.org/10.1007/BF00560458