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Pharmacokinetics of Orally Administered Levocabastine in Patients with Renal Insufficiency
Author(s) -
Zazgornik Jan,
Huang May Lynn,
Peer Achiel,
Woestenborghs Robert,
Heykants Jos,
Stephen Adrian
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.tb03922.x
Subject(s) - pharmacokinetics , medicine , pharmacology , anesthesia
The effects of renal insufficiency and hemodialysis on the pharmacokinetics of orally administered levocabastine were studied in six nondialysis patients and in six patients undergoing regular hemodialysis. Levocabastine .5 mg, supplied as a solution, was administered orally to each patient 1 hour after breakfast Compared with data in healthy volunteers, the oral absorption and disposition of levocabastine were impaired in patients with renal insufficiency. The time to reach peak plasma concentration was increased and the peak plasma concentration was decreased in the patients with renal insufficiency compared with healthy volunteers. Urinary excretion of the unchanged drug, which is the major elimination pathway of levocabastine, was reduced in the patients with renal insufficiency. The decreased urinary excretion most likely contributed to the prolonged half‐life (from 36 hours to 95 hours) and increased area under the plasma concentration‐time curve (+56%) in the patients with renal insufficiency as compared with the healthy volunteers. Although the 6‐hour hemodialysis procedure starting 4 hours after dosing eliminated 10% of the oral dose, the terminal half‐life and the total area under the plasma concentration‐time curve did not differ significantly between the hemodialysis and the nonhemodialysis patients. In conclusion, the current study showed that the initial oral absorption of levocabastine is reduced and that levocabastine elimination is prolonged in patients with renal insufficiency.