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Steady State Pharmacokinetics and Dose‐Proportionality of Phenylpropanolamine in Healthy Subjects
Author(s) -
Scherzinger S. S.,
Dowse R.,
Kanfer I.
Publication year - 1990
Publication title -
the journal of clinical pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.92
H-Index - 116
eISSN - 1552-4604
pISSN - 0091-2700
DOI - 10.1002/j.1552-4604.1990.tb03608.x
Subject(s) - phenylpropanolamine , pharmacokinetics , medicine , pharmacology , anesthesia
The pharmacokinetics of phenylpropanolamine (PPA) were studied in five healthy male volunteers after single oral doses of 25, 50 and 100 mg of the drug as well as at steady state after seven, 4‐hourly doses of PPA. The peak serum concentrations and AUC ∞ values increased linearly with an increase in dose, whereas the time to reach peak serum concentrations did not vary significantly between doses. The half‐life remained relatively constant with an increase in dose (t 1/2 = 3.8 to 4.3 hours), as did renal clearance (Cl R = 0.41 to 0.44 1/kg/h). The percentage of unchanged PPA excreted in the urine over a 14 hour period was 64%, 63% and 73% for the 25, 50 and 100 mg doses, respectively. The pharmacokinetics of PPA were found to be linear in the dosage range 25 to 100 mg. Steady state serum concentrations were significantly higher than single dose concentrations, with the mean peak serum concentration increasing from 113 ng/ml after a single dose to 183 ng/ml at steady state. The time at which these were attained decreased from 1.47 hours after a single dose to 0.73 hours at steady state. Both clearance and volume of distribution were significantly different after a single dose compared to steady state ( P <0.05), whereas no significant differences were found between the other parameters .