Journal of Antimicrobial Chemotherapy, Vol 40, 35-43, Copyright © 1997 by The British Society for Antimicrobial Chemotherapy
C Efthymiopoulos
Grepafloxacin is a fluoroquinolone antibiotic which is rapidly absorbed in
healthy volunteers following oral dosing. It reaches peak plasma levels
around 2 h after administration, then declines bi-exponentially, with an
extended half-life of around 12 h. Grepafloxacin is eliminated primarily
through metabolism and is excreted mainly in the faeces. Renal clearance
accounts for only 10-15% of the administered dose. Grepafloxacin plasma
concentrations increase disproportionately with increasing doses, but this
is unlikely to be of clinical significance over the range of therapeutic
doses. The rate and extent of absorption are not affected by food or
elevated intragastric pH. The pharmacokinetics of grepafloxacin are
affected by gender, with these differences relating to variations in body
weight. No effect of age on the pharmacokinetics of grepafloxacin was
found. Renal impairment does not affect grepafloxacin pharmacokinetics,
whereas peak plasma concentrations, areas under plasma concentration-time
curves and renal excretion are increased in patients with hepatic
impairment. Grepafloxacin can be co-administered with warfarin and
theophylline, though reduction of the theophylline dose is necessary.
Following oral administration, higher grepafloxacin concentrations are
achieved in lung and genital tissues than in serum, indicating its
potential in the treatment of respiratory and sexually transmitted
diseases. In addition, it exceeds therapeutically effective levels in bile
and gall- bladder tissues, and accumulates in polymorphonuclear leucocytes
such that it may be useful against intracellular pathogens.
ORIGINAL ARTICLES
Pharmacokinetics of grepafloxacin
Glaxo Wellcome Research & Development, Clinical Pharmacology Division, Greenford, UK. ce12833@ggr.co.uk
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