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Ciprofloxacin


ACCESSION NB: DB00537 (APRD00424, EXPT00999)


TYPE: small molecule


GROUP: approved


DESCRIPTION:
A broad-spectrum antimicrobial carboxyfluoroquinoline. [PubChem]

VOLUME OF DISTRIBUTION: Not Available

CATEGORIES:
Anti-Infective Agents Anti-Infectives Quinolones Nucleic Acid Synthesis Inhibitors

ABSORPTION: Rapidly and well absorbed from the gastrointestinal tract after oral administration. The absolute bioavailability is approximately 70% with no substantial loss by first pass metabolism.

INDICATION:
For the treatment of the following infections caused by susceptible organisms: urinary tract infections, acute uncomplicated cystitis, chronic bacterial prostatitis, lower respiratory tract infections, acute sinusitis, skin and skin structure infections, bone and joint infections, complicated intra-abdominal infections (used in combination with metronidazole), infectious diarrhea, typhoid fever (enteric fever), uncomplicated cervical and urethral gonorrhea, and inhalational anthrax (post-exposure).

PHARMACODYNAMICS:
Ciprofloxacin is a broad-spectrum antiinfective agent of the fluoroquinolone class. Ciprofloxacin has in vitro activity against a wide range of gram-negative and gram-positive microorganisms. The mechanism of action of quinolones, including ciprofloxacin, is different from that of other antimicrobial agents such as beta-lactams, macrolides, tetracyclines, or aminoglycosides; therefore, organisms resistant to these drugs may be susceptible to ciprofloxacin. There is no known cross-resistance between ciprofloxacin and other classes of antimicrobials. Notably the drug has 100 times higher affinity for bacterial DNA gyrase than for mammalian.

MECHANISM OF ACTION:
The bactericidal action of ciprofloxacin results from inhibition of the enzymes topoisomerase II (DNA gyrase) and topoisomerase IV, which are required for bacterial DNA replication, transcription, repair, strand supercoiling repair, and recombination.

PROTEIN BINDING:
20 to 40%

METABOLISM:
Hepatic. Four metabolites have been identified in human urine which together account for approximately 15% of an oral dose. The metabolites have antimicrobial activity, but are less active than unchanged ciprofloxacin.

TOXICITY:
The major adverse effect seen with use of is gastrointestinal irritation, common with many antibiotics.

AFECTED ORGANISMS:
Enteric bacteria and other eubacteria