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Cetirizine Pharmacokinetics and Pharmacodynamics in Primary Biliary Cirrhosis
Author(s) -
Simons F. Estelle R.,
Watson Wade T. A.,
Minuk Gerald Y.,
Simons Keith J.
Publication year - 1993
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.1552-4604.1993.tb01928.x
Subject(s) - primary biliary cirrhosis , pharmacokinetics , pharmacodynamics , medicine , cetirizine , pharmacology
The new H 1 ‐receptor antagonist, cetirizine, is eliminated primarily unchanged by renal excretion and is thus potentially useful for relief of pruritus in patients with hepatic dysfunction, in whom many H 1 ‐receptor antagonists are contraindicated. The authors studied the elimination of cetirizine in six patients with primary biliary cirrhosis. In contrast to data obtained in healthy adults with normal hepatic function reported in the medical literature, they found that the mean serum elimination half‐life value of cetirizine, 13.8 ± 1.8 hours, was longer, and the mean clearance rate, 0.44 ± 0.10 mL/min/kg, was lower (P < .05). The mean peak serum cetirizine concentration, 498 ± 118 ng/mL, was higher, the mean area under the curve, 6438 ± 1621 ng/mL/hr, was larger, and the mean fraction of the dose excreted as unchanged cetirizine in the urine, .32 ± .14, was lower (P < .05). The duration of action of cetirizine was prolonged, as evidenced by significant suppression of the histamine‐induced wheal and flare for 48 and 72 hours, respectively, after a single dose. Cetirizine elimination was impaired in patients with hepatic dysfunction.