Ciprofloxacin ADME

Stable Identifier
Homo sapiens
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Ciprofloxacin (Cipro) is a widely used broad spectrum bacterial antibiotic. Due to its association with disabling and potentially persistent adverse reactions and current high levels of resistance its use is now recommended in patients who have no alternative treatment option for respiratory and urinary tract infections, skin and soft tissue infections, bone and joint infections, infectious diarrhea, typhoid fever and gonorrhea with susceptible strains. Adverse reactions include tendinitis, tendon rupture, peripheral neuropathy, and CNS effects. The usual dosages are 250 mg and 500 mg (FDA, 2016; Bayer Inc, 2020).

Cipro is highly soluble in aqeuous media below pH 5 and above pH 10. About 60 to 80 percent are taken up by the body. The main absorption site of ciprofloxacin is the upper GI tract, up to the jejunum (Harder et al, 1990; summarized in Olivera et al, 2011). In the context of the Biopharmaceutics Classification System (BCS) Cipro is "not highly soluble", and "not highly permeable". It is classified as BCS class 2, 3, and 4, and uptake and efflux transporters have a big effect on its absorption and excretion. BCS class 4 drugs are primarily excreted unchanged via the biliary or renal routes (Wu and Benet, 2005).

Very high concentrations of Cipro with respect to plasma concentrations are seen in kidney and gall bladder; high concentrations are also found in liver, prostatic tissue, and lung. The main excretion routes for unchanged Cipro are renal (about 65% of plasma amount) and intestinal (about 10%) (Rohwedder et al, 1990; Viell et al, 1992; reviewed by Sörgel, 1989). The intestinal figure includes excretion through epithelial GI cells, and through hepatic cells and the bile duct. The rest of plasma Cipro (10 to 20%) is metabolised, with the major species recovered from urine being oxociprofloxacin and, in faeces, sulfociprofloxacin. Both account for about five per cent each of total excretion (reviewed by Campoli-Richards et al, 1988).
Literature References
PubMed ID Title Journal Year
20602455 Biowaiver monographs for immediate release solid oral dosage forms: ciprofloxacin hydrochloride

Midha, KK, Stavchansky, S, Manzo, RH, Junginger, HE, Dressman, JB, Barends, DM, Olivera, ME, Shah, VP

J Pharm Sci 2011
1293050 Transintestinal elimination of ciprofloxacin in humans--concomitant assessment of its metabolites in serum, ileum and colon

Vestweber, KH, Schaaf, S, Krause, B, Viell, B, Scholl, H

Infection 1992
15771225 Predicting drug disposition via application of BCS: transport/absorption/ elimination interplay and development of a biopharmaceutics drug disposition classification system

Wu, CY, Benet, LZ

Pharm Res 2005
  Cipro: Highlights of Prescribing Information

Food and Drug Administration, FDA

2369809 Transintestinal elimination of ciprofloxacin

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

Diagn Microbiol Infect Dis 1990
2549606 Metabolism of gyrase inhibitors

Sörgel, F

Rev Infect Dis 1989
3292209 Ciprofloxacin. A review of its antibacterial activity, pharmacokinetic properties and therapeutic use

Ward, A, Campoli-Richards, DM, Monk, JP, Todd, PA, Benfield, P, Price, A

Drugs 1988
2390430 Ciprofloxacin absorption in different regions of the human gastrointestinal tract. Investigations with the hf-capsule

Fuhr, U, Beermann, D, Staib, AH, Harder, S

Br J Clin Pharmacol 1990
  CIPRO English Product Monograph

Bayer Inc., BAYER

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