Access the full text.
Sign up today, get DeepDyve free for 14 days.
K. Inui, M. Takano, T. Okano, R. Hori (1985)
H+ gradient-dependent transport of aminocephalosporins in rat renal brush border membrane vesicles: role of H+/organic cation antiport system.The Journal of pharmacology and experimental therapeutics, 233 1
F. Sörgel, K. Naber, U. Jaehde, A. Reiter, R. Seelmann, G. Sigl (1989)
Gastrointestinal secretion of ciprofloxacin. Evaluation of the charcoal model for investigations in healthy volunteers.The American journal of medicine, 87 5A
(1995)
Spar ̄oxacin secretion across Caco-2 cells involves a multidrug
S. Dautrey, L. Rabbaa, D. Laouari, B. Lacour, Claude Carbón, R. Farinotti (1999)
Influence of Renal Failure on Intestinal Clearance of Ciprofloxacin in RatsAntimicrobial Agents and Chemotherapy, 43
N. Griffiths, B. Hirst, N. Simmons (1993)
Active secretion of the fluoroquinolone ciprofloxacin by human intestinal epithelial Caco‐2 cell layersBritish Journal of Pharmacology, 108
G. Nagel, C. Volk, T. Friedrich, J. Ulzheimer, E. Bamberg, H. Koepsell (1997)
A Reevaluation of Substrate Specificity of the Rat Cation Transporter rOCT1*The Journal of Biological Chemistry, 272
(1990)
The gastrointestinal secretion of quinolones ± Preliminary evaluation of in vivo animal model
Lei Zhang, C. Brett, K. Giacomini (1998)
Role of organic cation transporters in drug absorption and elimination.Annual review of pharmacology and toxicology, 38
(1998)
Cipro ̄oxacin (CIP) is eliminated by rat intestine via a DIDS-sensitive, PGP-like transporter
M. Cavet, M. West, N. Simmons (1997)
Fluoroquinolone (ciprofloxacin) secretion by human intestinal epithelial (Caco‐2) cellsBritish Journal of Pharmacology, 121
F. Sörgel, M. Kinzig (1993)
Pharmacokinetics of gyrase inhibitors, Part 2: Renal and hepatic elimination pathways and drug interactions.The American journal of medicine, 94 3A
(1983)
Mise au point. Inte reà t clinique de la scintigraphie dans l'exploration du tube digestif
S. Barriere, D. Catlin, P. Orlando, A. Noe, R. Frost (1990)
Alteration in the pharmacokinetic disposition of ciprofloxacin by simultaneous administration of azlocillinAntimicrobial Agents and Chemotherapy, 34
E. Cormet-Boyaka, J. Huneau, A. Mordrelle, P. Boyaka, Claude Carbón, E. Rubinstein, D. Tomé (1998)
Secretion of Sparfloxacin from the Human Intestinal Caco-2 Cell Line Is Altered by P-Glycoprotein InhibitorsAntimicrobial Agents and Chemotherapy, 42
E. Cormet, J. Huneau, M. Bouras, Claude Carbón, E. Rubinstein, D. Tomé (1997)
Evidence for a passive diffusion mechanism for sparfloxacin uptake at the brush-border membrane of the human intestinal cell-line Caco-2.Journal of pharmaceutical sciences, 86 1
CORMET (1995)
Sparfloxacin secretion across Caco-2 cells involves a multidrug resistance-like mechanismDrugs, 29
E. Rubinstein, L. Julien, J. Ramon, S. Dautrey, R. Farinotti, J. Huneau, Claude Carbón (1994)
The intestinal elimination of ciprofloxacin in the rat.The Journal of infectious diseases, 169 1
F. Sörgel, M. Kinzig (1993)
Pharmacokinetics of gyrase inhibitors, Part 1: Basic chemistry and gastrointestinal disposition.The American journal of medicine, 94 3A
N. Griffiths, B. Hirst, N. Simmons (1994)
Active intestinal secretion of the fluoroquinolone antibacterials ciprofloxacin, norfloxacin and pefloxacin; a common secretory pathway?The Journal of pharmacology and experimental therapeutics, 269 2
R. Jian (1983)
[Clinical value of scintigraphy in the study of the digestive tract].Gastroenterologie clinique et biologique, 7 8-9
F. Sharom (1997)
The P-Glycoprotein Efflux Pump: How Does it Transport Drugs?The Journal of Membrane Biology, 160
D. Ross, C. Riley (1994)
Dissociation and complexation of the fluoroquinolone antimicrobials--an update.Journal of pharmaceutical and biomedical analysis, 12 10
L. Rabbaa, S. Dautrey, N Colas-Linhart, Claude Carbón, R. Farinotti (1996)
Intestinal elimination of ofloxacin enantiomers in the rat: evidence of a carrier-mediated processAntimicrobial Agents and Chemotherapy, 40
Y. Emi, D. Tsunashima, K. Ogawara, K. Higaki, T. Kimura (1998)
Role of P-glycoprotein as a secretory mechanism in quinidine absorption from rat small intestine.Journal of pharmaceutical sciences, 87 3
L. Jetté, Gérard Murphy, Jean-Marie Leclerc, R. Béliveau (1995)
Interaction of drugs with P-glycoprotein in brain capillaries.Biochemical pharmacology, 50 10
M. Cavet, M. West, N. Simmons (1997)
Fluoroquinolone ( cipro ̄ oxacin ) secretion by human intestinal epithelial ( Caco-2 ) cells
R. Rohwedder, R. Rohwedder, T. Bergan, T. Bergan, S. Thorsteinsson, S. Thorsteinsson, H. Scholl, H. Scholl (1990)
Transintestinal elimination of ciprofloxacin.Chemotherapy, 36 2
J. Mason (1990)
Pharmacology of cyclosporine (sandimmune). VII. Pathophysiology and toxicology of cyclosporine in humans and animals.Pharmacological reviews, 41 3
C. Bair, M. Tang, Jin‐ding Huang (1992)
Concentration‐dependent Exsorption of Quinidine in the Rat IntestineJournal of Pharmacy and Pharmacology, 44
Two in vivo models, in the rat, were used to investigate, in the presence of different substrates, the overall and net intestinal elimination of ciprofloxacin: an open‐intestinal perfusion model and an intestinal loop model respectively. In the presence of quinidine, verapamil and cyclosporin (substrates of the P‐glycoprotein (P‐gp)), plasma AUCs of ciprofloxacin were 1.5–2 fold increased, while biliary clearance (1.5–2 fold), intestinal overall and net clearances (2–4 fold and 1.5–8 fold respectively) decreased. The weak effect obtained with cyclosporin as compared to verapamil and especially quinidine, suggests, for ciprofloxacin, the existence of transport systems distinct from the P‐gp, as the OCT1 transporter which could be inhibited by quinidine. With cephalexin and azlocillin, two β‐lactam antibiotics, plasma AUCs of ciprofloxacin increased and biliary and intestinal overall clearances decreased in a similar fashion (1.3–2 fold), suggesting the involvement of organic anion and/or cation transporters. In the presence of structural analogues, the effect was dependent on the compound administered: Sparfloxacin had no effect on intestinal clearance of ciprofloxacin. In contrast, with pefloxacin, overall intestinal clearance of ciprofloxacin was decreased and net intestinal clearance increased. The specificity of ciprofloxacin intestinal transport appears to be different from P‐gp as outlined by the lack of competition with sparfloxacin, a P‐gp substrate. Ciprofloxacin intestinal elimination seems to be mediated by organic anion and/or cation transporters and a mechanism sensitive to quinidine and verapamil.
British Journal of Pharmacology – Wiley
Published: Jan 1, 1999
Keywords: ; ; ; ;
Read and print from thousands of top scholarly journals.
Already have an account? Log in
Bookmark this article. You can see your Bookmarks on your DeepDyve Library.
To save an article, log in first, or sign up for a DeepDyve account if you don’t already have one.
Copy and paste the desired citation format or use the link below to download a file formatted for EndNote
Access the full text.
Sign up today, get DeepDyve free for 14 days.
All DeepDyve websites use cookies to improve your online experience. They were placed on your computer when you launched this website. You can change your cookie settings through your browser.