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Pharmacokinetic Profile
Mohammed A. Al-Omar
Department of Pharmaceutical Chemistry
College of Pharmacy, King Saud University
P.O. Box 2457, Riyadh-11451
Kingdom of Saudi Arabia
CONTENTS
3. METABOLISM
At least four active metabolites have been identified, namely desethylene-
ciprofloxacin, sulfo-ciprofloxacin, oxo-ciprofloxacin, and N-acetyl-
ciprofloxacin. Oxo-ciprofloxacin appears to be the major urinary
metabolite, and sulfo-ciprofloxacin the primary fecal metabolite [4, 11].
212 M.A. AL-OMAR
4. EXCRETION
Ciprofloxacin is eliminated by renal and non-renal mechanisms. The
drug is partially metabolized in the liver by modification of the
piperazinyl group to atleast four metabolites. These metabolites, which
have been identified as desethylene-ciprofloxacin, sulfo-ciprofloxacin,
oxo-ciprofloxacin, and N-acetyl-ciprofloxacin, have microbiological
activities that are less than that of the parent drug, but may be similar
to or greater than that of some other quinolones [4, 8, 9].
CH3
HN C N
H o
N N N
H
F COOH F COOH
O O
Desethylene-ciprofloxacin N-Accetyl-ciprofloxacin
HN
N N
F COOH
O
Ciprofloxacin
HO3S N HN
N N N N
O
F COOH F COOH
O O
Sulfo-ciprofloxacin Oxo-ciprofloxacin
5. REFERENCES
1. C.J. Gilles, R.A. Magonigle, W.T.R. Grinshaw, A.C. Tanner,
J.E. Risk, M.J. Lynch and J.R. Rice, J. Vet. Pharmacol. Therapy,
14, 400 (1991).
214 M.A. AL-OMAR