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Chemotherapy. 1990;36(2):77-84.
Transintestinal elimination of ciprofloxacin.

Rohwedder R, Bergan T, Thorsteinsson SB, Scholl H.

Pharma Research Center, Bayer AG, Wuppertal, FRG.

This study elucidates the routes of elimination of ciprofloxacin and its metabolites in two groups of 5 subjects each, one of healthy volunteers, the other of patients with severe renal failure having a creatinine clearance of 12 ml/min (range 8-16 ml/min). Each subject received one dose of 200 mg ciprofloxacin infused intravenously over 30 min. In an effort to recover the total dose administered, all urine and faeces were collected for the 7 days following dosing. Blood was collected at set intervals after dosing. Serum, urine, and faeces were assayed by high-pressure liquid chromatography for ciprofloxacin and metabolites. The ciprofloxacin serum half-life in healthy volunteers was 3.9 +/- 0.4 h and in patients with marked renal failure 11.2 +/- 2.5 h. The total amount of ciprofloxacin recovered in urine fell by a multiple of 3.4 from 65.3 +/- 10.7% in healthy subjects to 19.0 +/- 15.9% in patients with renal failure, and the metabolites from 12.2 +/- 2.3% in the former group to 5.8 +/- 5.1% in the latter. In contrast, the amount of ciprofloxacin eliminated in faeces increased, by a similar factor, from 11.4 +/- 2.6% in healthy subjects to 37.2 +/- 12.5% in patients with renal failure. The amount of metabolites in faeces increased analogously from 7.3 +/- 1.6 to 26.2 +/- 6.5%. Since ciprofloxacin was administered intravenously and biliary elimination of the drug and its metabolites is negligible, we propose that elimination by faeces is due primarily to transintestinal elimination. This study demonstrates that transintestinal elimination of ciprofloxacin serves as an extrarenal safety factor compensating for reduced elimination by the renal route.

online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=2311444&dopt=Abstract




Antimicrob Agents Chemother. 1990 Mar;34(3):496-7.
Influence of N substitution on antimycobacterial activity of ciprofloxacin.

Haemers A, Leysen DC, Bollaert W, Zhang MQ, Pattyn SR.

Department of Pharmaceutical Sciences, University of Antwerp, Belgium.

Ciprofloxacin analogs with various substitutions on the piperazine nitrogen were tested against several mycobacteria. In contrast to what has been found with other gram-positive and gram-negative bacteria, alkyl analogs such as N-isopropylciprofloxacin were shown to be significantly more active than ciprofloxacin. MICs of 0.125 microgram/ml against Mycobacterium tuberculosis were found.

online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=2334166&dopt=Abstract




Diagn Microbiol Infect Dis. 1990 Mar-Apr;13(2):127-33.
Transintestinal elimination of ciprofloxacin.

Rohwedder RW, Bergan T, Thorsteinsson SB, Scholl H.

Pharma Research Center, Bayer AG, Wuppertal, FRG.

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 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.(ABSTRACT TRUNCATED AT 250 WORDS)

online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=2369809&dopt=Abstract












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