Transintestinal elimination of ciprofloxacin in humans — Concomitant assessment of its metabolites in serum, ileum and colon

Viell, B.; Krause, Bettina; Schaaf, Simon; Vestweber, K. H.; Scholl, H

doi:10.1007/bf01710676

Cited by 4 publications

(2 citation statements)

References 9 publications

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“…This bidirectional transport with net flux from the basal to the apical side of mucosal cells has been confirmed in vitro in studies of human intestinal epithelial cell cultures [21]. Animal experiments demonstrate that the jejunum and ileum are the main sites of transintestinal secretion [22,23], but human colonic tissue may also secrete considerable amounts of ciprofloxacin [24]. Absorption is negligibly low in the large intestine [25].…”

Section: Discussionmentioning

confidence: 75%

Elimination of Fecal Enterobacteriaceae by Intravenous Ciprofloxacin Is not Inhibited by Concomitant Sucralfate - a Microbiological and Pharmacokinetic Study in Patients

Krueger¹,

Ruckdeschel

Unertl³

1999

Infection

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Intravenously administered ciprofloxacin is partially secreted into the intestinal lumen and thereby eliminates fecal Enterobacteriaceae. Sucralfate inhibits the antimicrobial activity of ciprofloxacin by chelate binding. In a prospective study, we investigated the impact of intravenous ciprofloxacin on the intestinal microflora during oral administration of sucralfate. A total of 45 stool specimens were analyzed in 20 hospitalized patients who were treated with 200 mg of ciprofloxacin i.v. bid. Ten patients concomitantly received 1 g sucralfate p.o. tid (group A). After more than 3 days of i.v. ciprofloxacin, the mean fecal ciprofloxacin concentration was 185.3 +/- 158.7 micrograms/g in patients of group A and 108.7 +/- 76.9 micrograms/g in patients without concurrent sucralfate (group B). There was no significant difference in mean fecal ciprofloxacin levels between both groups (Wilcoxon's test). Enterobacteriaceae were below the threshold of detection (10(2) cfu/g) in all patients of group B after 3 days of treatment whereas small numbers were found in only 2 samples of patients of group A (10(4) cfu/g). Intravenous ciprofloxacin eliminates or largely reduces intestinal Enterobacteriaceae irrespective of concurrent administration of sucralfate.

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Section: Discussionmentioning

confidence: 75%

Elimination of Fecal Enterobacteriaceae by Intravenous Ciprofloxacin Is not Inhibited by Concomitant Sucralfate - a Microbiological and Pharmacokinetic Study in Patients

Krueger¹,

Ruckdeschel

Unertl³

1999

Infection

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“…This is only partly due to incomplete absorption, since approximately 15% of a dose is found in feces after intravenous application (25). Whereas the amount of biliary excretion is very low, transintestinal secretion is a pharmacokinetic property of ciprofloxacin (6,31,37). This way of elimination can amount to up to 50% of the total body clearance in cases of renal insufficiency (25).…”

Section: Discussionmentioning

confidence: 99%

Influence of intravenously administered ciprofloxacin on aerobic intestinal microflora and fecal drug levels when administered simultaneously with sucralfate

Krueger

Ruckdeschel

Unertl

1997

Antimicrob Agents Chemother

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Ciprofloxacin, when given intravenously (i.v.), is secreted in significant amounts via the mucosa into the intestinal lumen. Sucralfate inhibits the antimicrobial activity of ciprofloxacin. The effect of combined therapy on the intestinal flora was investigated in 16 healthy volunteers. They were randomly assigned to two groups. Group A received 2 g of sucralfate orally three times a day for 7 days and 400 mg of ciprofloxacin i.v. twice a day (b.i.d.) starting 3 days after the sucralfate administration began. Group B was given only 400 mg of ciprofloxacin i.v. b.i.d. for 4 days. A total of 9 stool samples were collected from each subject beginning the week before ciprofloxacin was administered and on days -1, 1, 2, 3, 4, 7, 9, and 10 or 11 after commencement of the infusion period. The aerobic fecal flora was determined by standard microbiological methods. Measurements of fecal ciprofloxacin levels were based on high-performance liquid chromatography. Counts of bacteria of the family Enterobacteriaceae decreased in all subjects and were below 10(2) CFU/g in eight of eight subjects (group A) and six of eight subjects (group B) on day 4, but they returned to normal in all but one subject (group A) 10 days after the last infusion. The decreases in levels of bacteria of the family Enterobacteriaceae were not significantly different in groups A and B (Kaplan-Meier test). Staphylococci and nonfermenters responded variably, enterococci and lactobacilli remained unchanged, and candida levels increased transiently in four subjects (two in each group). Maximum fecal drug levels ranged from 251 to 811 microg/g. No significant difference could be found between the two groups. The i.v. application of ciprofloxacin eliminates intestinal bacteria of the family Enterobacteriaceae in a rapid and selective manner. This effect is not affected by simultaneous oral application of sucralfate.

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Consequences of Renal Failure on Non-Renal Clearance of Drugs

et al. 2014

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Kidney disease not only alters the renal elimination but also the non-renal disposition of drugs that are metabolized by the liver. Indeed, modifications in the expression and activity of intestinal and hepatic drug metabolism enzymes and uptake and efflux transporters have been reported. Accumulated uremic toxins, inflammatory cytokines, and parathyroid hormones may modulate these proteins either directly or by inhibiting gene expression. This can lead to important unintended variations in exposure and response when drugs are administered without dose adjustment for reduced renal function. This review summarizes our current understanding of non-renal clearance in circumstances of chronic and acute renal failure with experimental but also clinical studies. It also evaluates the clinical impact on drug disposition. Predicting the extent of the drug disposition modification is difficult first because of the complex interplay between metabolic enzymes and transport proteins but also because of the differential effects in the different organs (liver, intestines). Recommendations of the US FDA are presented as they may be potentially helpful tools to predict these modifications when no specific pharmacokinetic studies are available.

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Transintestinal elimination of ciprofloxacin in humans — Concomitant assessment of its metabolites in serum, ileum and colon

Cited by 4 publications

References 9 publications

Elimination of Fecal Enterobacteriaceae by Intravenous Ciprofloxacin Is not Inhibited by Concomitant Sucralfate - a Microbiological and Pharmacokinetic Study in Patients

Elimination of Fecal Enterobacteriaceae by Intravenous Ciprofloxacin Is not Inhibited by Concomitant Sucralfate - a Microbiological and Pharmacokinetic Study in Patients

Influence of intravenously administered ciprofloxacin on aerobic intestinal microflora and fecal drug levels when administered simultaneously with sucralfate

Consequences of Renal Failure on Non-Renal Clearance of Drugs

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