Ciprofloxacin

Ciprofloxacin. It is a broad-spectrum fluoroquinolone antibiotic used to treat a variety of bacterial infections. Developed by Bayer AG, it is effective against both Gram-positive and Gram-negative bacteria, including Pseudomonas aeruginosa. Its use is typically reserved for serious infections or when other antibiotics have failed due to concerns about side effects.

Medical uses

It is indicated for the treatment of complicated urinary tract infections, chronic bronchitis, certain types of infectious diarrhea, and skin and skin structure infections. It is a key drug for treating anthrax exposure and infections caused by Neisseria meningitidis. In ophthalmology, topical formulations like Ciloxan are used for bacterial keratitis. It is often employed in hospital-acquired infections, particularly those involving multidrug-resistant organisms in settings like the intensive care unit. However, due to antibiotic resistance concerns, guidelines from the World Health Organization and the U.S. Food and Drug Administration recommend limiting its use.

Adverse effects

Common side effects include nausea, diarrhea, and rash. Serious adverse effects include tendinitis and tendon rupture, particularly of the Achilles tendon, which led to a prominent black box warning from the U.S. Food and Drug Administration. Other significant risks are peripheral neuropathy, central nervous system effects like seizures, and exacerbation of myasthenia gravis. It carries a risk of Clostridioides difficile infection and can cause photosensitivity. These risks have prompted regulatory actions by agencies like the European Medicines Agency.

Pharmacology

It exerts its bactericidal effect by inhibiting bacterial DNA gyrase and topoisomerase IV, enzymes critical for DNA replication and transcription. This mechanism is distinct from that of beta-lactam antibiotics like penicillin. It demonstrates concentration-dependent killing and has a significant post-antibiotic effect. Its absorption can be impaired by divalent cations such as those found in antacids. It is metabolized partially by the cytochrome P450 system, specifically CYP1A2, and is excreted primarily by the kidney.

History

It was first patented in 1983 by researchers at Bayer AG in Wuppertal, Germany, following work on the predecessor nalidixic acid. It received approval from the U.S. Food and Drug Administration in 1987. Its use expanded dramatically during the 2001 anthrax attacks in the United States, where it was employed as a primary prophylactic agent. Subsequent safety reviews, particularly regarding tendon damage, led to significant label changes and restrictions initiated by the FDA in 2008 and again in 2016.

Society and culture

It is on the World Health Organization's List of Essential Medicines. Generic versions are widely manufactured by companies like Teva Pharmaceutical Industries and Mylan. Its use in agriculture, particularly in poultry, has been controversial due to its contribution to fluoroquinolone resistance, leading to bans in countries like the United States under the FDA. It has been the subject of numerous product liability lawsuits. The drug gained notoriety in popular culture through its mention in the John Grisham novel The Street Lawyer and its central role in the anthrax attacks.

Category:World Health Organization essential medicines Category:Quinolone antibiotics Category:Bayer brands