Cipro is imported by organic cation transporters

Stable Identifier
R-HSA-9793628
Type
Reaction [uncertain]
Species
Homo sapiens
Compartment
extracellular region, cytosol
ReviewStatus
5/5
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Cipro is imported by organic cation transporters
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Cipro(1+) ion is taken up in the upper GI tract (Harder et al, 1990; reviewed by Olivera et al, 2010). Due to its charge and its size it is unlikely that translocation of Cipro(1+) into cells happens via diffusion through the membrane or through ion channels. Candidates for transport proteins include the organic cation transporters SLC47A1, SLC47A2, SLC22A1, SLC22A2, and SLC22A3 although they are not abundantly expressed in stomach. Interaction of fluoroquinolones with each of these proteins and inhibition has been shown, with different models emerging for transport in enterocytes, hepatocytes, and renal proximal tubule cells. However, as the measured interactions were too weak to have clinical relevance, more studies are needed to get the complete picture (Mulgaonkar et al, 2013).

In the cytosol Cipro(1+) releases a proton, turning into the Cipro zwitterion, the preferred species at physiologic pH.
Literature References
PubMed ID Title Journal Year
20602455 Biowaiver monographs for immediate release solid oral dosage forms: ciprofloxacin hydrochloride

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

J Pharm Sci 2011
23545524 Human organic cation transporters 1 (SLC22A1), 2 (SLC22A2), and 3 (SLC22A3) as disposition pathways for fluoroquinolone antimicrobials

Mulgaonkar, A, Venitz, J, Gründemann, D, Sweet, DH

Antimicrob Agents Chemother 2013
2390430 Ciprofloxacin absorption in different regions of the human gastrointestinal tract. Investigations with the hf-capsule

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

Br J Clin Pharmacol 1990
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Authored
Stephan, R  (2022-06-21)
Reviewed
Thorn, CF  (2022-11-09)
Created
Stephan, R  (2022-06-22)
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