Transintestinal elimination of ciprofloxacin

doi:10.1016/0732-8893(90)90095-D

Diagnostic Microbiology and Infectious Disease

Volume 13, Issue 2, March–April 1990, Pages 127-133

https://doi.org/10.1016/0732-8893(90)90095-D Get rights and content

Abstract

This study identified the routes of elimination of ciprofloxacin in two groups of five subjects each: one of healthy volunteers; the other of patients with severe renal failure having a mean creatinine clearance of 12 ml/min (range, 8–16 ml/min). Each subject received one dose of 200 mg ciprofloxacin infused intravenously (IV) over 30 min. In an effort to recover the total drug administered, all urine and feces were collected for 7 days following dosing. Blood samples were drawn at set intervals. Serum, urine, and feces were assayed for ciprofloxacin and metabolites by high-pressure liquid chromatography. The ciprofloxacin elimination half-life was 3.9 ± 0.4 hr in the healthy volunteers and 11.2 ± 2.5 hr in the patients with severe renal failure. The total 7-day recovery of ciprofloxacin and its metabolites in urine and feces ranged from 74.0% to 114.7% of the dose (mean, 96.3 ± 14.1%) in normal subjects and from 48.5% to 109.1% (mean, 88.1 ± 20.9%) in patients. The dose of ciprofloxacin recovered in urine was 65.3 ± 10.7% in healthy subjects and 19.0 ± 15.9% in impaired patients (reduction factor, 3.4). In contrast, the dose recovered in feces was 11.4 ± 2.6% in the group of normal subjects and 37.2 ± 12.5% in the group of patients with impaired renal function in a 3.3-fold increase. The total of metabolites recovered in urine and feces, which can be considered as a reflection of ciprofloxacin biotransformation, was 19.6 ± 3.7% in the group of normal subjects and 32.0 ± 7.6% in the patients (a 1.6-fold increase). Becase ciprofloxacin was administered IV and biliary elimination of the drug is negligible, transfer of ciprofloxacin into feces must be due primarily to a direct transintestinal elimination. The extrarenal route of elimination represents an important route and becomes a major route of elimination of ciprofloxacin in reduced renal function to the extent that it serves as a safety valve of excretion compensating for reduced renal elimination. This study also demonstrates that transintestinal elimination of ciprofloxacin is an important alternative route in patients with renal impairment, thereby avoiding accumulation of the drug in the plasma and tissues in these patients.

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Ciprofloxacin symposium: Major advances in inteavenous and oral quinolone therapyTransintestinal elimination of ciprofloxacin

Abstract

J Chromatogr

Biliary excretion of orally administered ciprofloxacin

Chemotherapia

Multiple-dose ciprofloxacin kinetics in normal subjects

Clin Pharmacol Ther

Metabolism of ciprofloxacin in man

Quinolones

Antimicrob Agents Chemother

Pharmacokinetik von ciprofloxacin

Fortschr Antimikrob Antineoplast Chemother

Pharmacokinetics of ciprofloxacin: intravenous and increasing oral doses

Am J Med

The pharmacokinetics of ciprofloxacin in patients with impaired renal function

J Antimicrob Chemother

Renal ausscheidung von ciprofloxacin und einigen metaboliten nach einmaliger oraler und intravenoeser applikation von 50 mg

Fortschr Antimikrob Antineoplast Chemother

Pharmacokinetics of ciprofloxacin in healthy volunteers after oral and intravenous administration

Eur J Clin Microbiol

Comparison of high pressure liquid chromatography and microbiological assay for the determination of biliary elimination of ciprofloxacin in humans

Antimicrob Agents Chemother

Penetration of ciprofloxacin into human intestinal mucosa (abstr F8)

An overview of the pharmacology of intravenously administered ciprofloxacin

Am J Med

Pharmacokinetics of intravenously administered ciprofloxacin in patients with various degrees of renal function

Antimicrob Agents Chemother

Ciprofloxacin pharmacokinetics in patients with normal and impaired renal function

Antimicrob Agents Chemother

Isolation and structural elucidation of urinary metabolites of ciprofloxacin

Arzneim Forsch

Ciprofloxacin symposium: Major advances in inteavenous and oral quinolone therapy
Transintestinal elimination of ciprofloxacin