Brands, Medical Use, Clinical Data
- Oral suspension
- Tablet (combined release)
- Tablet (extended-release)
Brands / Synonyms
Bacquinor; Baycip; Bernoflox; Ciflox; Cifloxin; Ciloxan; Ciprinol; Cipro; Cipro HC; Cipro I.V.; Cipro XL; Cipro XR; Ciprobay; Ciprocinol; Ciprodar; Ciprodex; Ciprofloxacin Base; Ciprofloxacin dihydrochloride; Ciprofloxacin HCl; Ciprofloxacin hydrochloride; Ciprofloxacin monohydrochloride; Ciprofloxacina; Cipromycin; Ciproquinol; Ciproxan; Ciproxin; Flociprin; Floxin; Floxin Otic; Ocuflox; Ofloxacin; Proquin XR; Septicide; Velomonit
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).
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, and recombination.
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.
The major adverse effect seen with use of is gastrointestinal irritation, common with many antibiotics.
Biotrnasformation / Drug 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.
Proquin XR is contraindicated in persons with a history of hypersensitivity to ciprofloxacin or any member of the
quinolone class of antimicrobial agents, or any of the product components.
Some quinolones, including ciprofloxacin, have also been shown to interfere with the metabolism of caffeine. This
may lead to reduced clearance of caffeine and a prolongation of its serum half-life.
Some quinolones, including ciprofloxacin, have been associated with transient elevations in serum creatinine in
patients receiving cyclosporine concomitantly.
The concomitant administration of ciprofloxacin with the sulfonylurea glyburide has, on rare occasions, resulted
in severe hypoglycemia.
Histamine H2-receptor antagonists
Histamine H2-receptor antagonists appear to have no significant effect on the bioavailability of
Renal tubular transport of methotrexate may be inhibited by concomitant administration of ciprofloxacin,
potentially leading to increased plasma levels of methotrexate. This might increase the risk of methotrexate toxic
reactions. Therefore, patients under methotrexate therapy should be carefully monitored when concomitant
ciprofloxacin therapy is indicated.
Multivalent Cation-Containing Products
Concurrent administration of a quinolone, including ciprofloxacin, with multivalent cation-containing products
such as magnesium or aluminum antacids, sucralfate, VIDEX chewable/buffered tablets or pediatric powder, or products
containing calcium, iron, or zinc may substantially decrease the absorption of ciprofloxacin, resulting in serum and
urine levels considerably lower than desired. Proquin XR should be administered at least 4 hours before or 2 hours
after these products. This time window is different than for other oral formulations of ciprofloxacin, which are
usually administered 2 hours before or 6 hours after antacids.
Non-steroidal anti-inflammatory drugs (but not aspirin)
These drugs in combination with very high doses of quinolones have been shown to provoke convulsions in
The rate and extent of absorption of ciprofloxacin was bioequivalent when Proquin XR was given alone or when
Proquin XR was given 2 hours after omeprazole at the dose that maximally suppresses gastric acid secretion.
Omeprazole should be taken as directed and Proquin XR should be taken with a main meal of the day, preferably the
Altered serum levels of phenytoin (increased and decreased) have been reported in patients receiving concomitant
Probenecid interferes with renal tubular secretion of ciprofloxacin and produces an increase in the level of
ciprofloxacin in serum.
As with some other quinolones, concurrent administration of ciprofloxacin with theophylline may lead to elevated
serum concentrations of theophylline and prolongation of its elimination half-life. This may result in increased risk
of theophylline-related adverse reactions. If concomitant use cannot be avoided, serum levels of theophylline should
be monitored and dosage adjustments made as appropriate.
Quinolones have been reported to enhance the effects of the oral anticoagulant warfarin or its derivatives. When
these products are administered concomitantly, prothrombin time or other suitable coagulation tests should be