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Effects of renal dysfunction on the pharmacokinetics of loracarbef
Author(s) -
Therasse Donald G,
Farlow Diane S,
Davidson Robert L,
Quadracci Leonard J,
Hatcher Barbara L,
Cerimele Benito J,
Desante Karl A
Publication year - 1993
Publication title -
clinical pharmacology and therapeutics
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.941
H-Index - 188
eISSN - 1532-6535
pISSN - 0009-9236
DOI - 10.1038/clpt.1993.152
Subject(s) - pharmacokinetics , hemodialysis , medicine , clearance , dosing , renal function , dialysis , urology , urine , creatinine , pharmacology
Loracarbef, the first carbacephem antibiotic to undergo clinical development, is excreted primarily unchanged in the urine (>90%). Data analyzed from subjects with various degrees of renal dysfunction who were given single oral doses of loracarbef indicated a linear relationship between creatinine clearance (CL CR ) and plasma clearance [CL p (L/hr) = 0.106 CL CR (ml/min/1.73 m 2 )]. The mean area under the plasma concentration‐time curve in normal subjects and in patients with severe renal insufficiency (no dialysis/receiving dialysis) was 32 μg · hr/ml and 1085 μg · hr/ml/103 μg · hr/ml, respectively. Therefore, for individuals with moderate renal insufficiency (CL CR , 10 to 49 ml/min/1.73 m 2 ), the dose should be halved or the dosing interval doubled; patients with severe renal insufficiency who are not receiving dialysis should be treated with the normal dose given once every 3 to 5 days. Loracarbef is readily cleared from plasma by hemodialysis; dosing should be repeated after a hemodialysis treatment. Clinical Pharmacology and Therapeutics (1993) 54, 311–316; doi: 10.1038/clpt.1993.152