The pharmacokinetics and antihistaminic effects of brompheniramine.
We studied the pharmacokinetics and antihistaminic effect of brompheniramine in seven normal adults. The mean peak serum brompheniramine concentration of 11.6 +/- 3.0 ng/ml occurred at a mean time of 3.1 +/- 1.1 hr. The mean serum half-life value was 24.9 +/- 9.3 hr, the mean clearance rate was 6.0 +/- 2.3 ml/min/kg, and the mean volume of distribution was 11.7 +/- 3.1 L/kg. The mean wheal size was significantly suppressed (p less than or equal to 0.1) at 3, 6, and 9 hr after the brompheniramine dose when mean concentrations ranged from 10.2 +/- 2.9 to 7.0 +/- 2.2 ng/ml. Significant suppression (p less than or equal to 0.05) of mean flare size was found from 3 to 48 hr after the brompheniramine dose, when mean concentrations ranged from 10.2 +/- 2.9 to 2.5 +/- 0.6 nl/ml. The mean pruritus score was significantly suppressed at 9 and 12 hr (p less than or equal to 0.1) and at 24 hr (p less than or equal to 0.05). Brompheniramine had a long half-life and large volume of distribution in normal adults. It also had a prolonged antihistaminic effect in the skin as evidenced by suppression of the wheal and flare response to histamine and by suppression of pruritus.
D000293:Adolescent; D000328:Adult; D001977:Brompheniramine / Q000008:administration & dosage / Q000009:adverse effects / Q000097:blood*; D002851:Chromatography, High Pressure Liquid; D005260:Female; D006207:Half-Life; D006634:Histamine H1 Antagonists / Q000008:administration & dosage / Q000494:pharmacology*; D006801:Humans; D007428:Intradermal Tests; D007700:Kinetics; D008297:Male; D011537:Pruritus / Q000139:chemically induced; D011725:Pyridines / Q000097:blood*
D006634:Histamine H1 Antagonists; D011725:Pyridines; D001977:Brompheniramine