Toxicity and application of Norfloxacin

Description

Norfloxacin is an organic compound with the chemical formula C16H18FN3O3. It is an antibiotic that belongs to the class of fluoroquinolone antibiotics. It is usually sold under the brand name Noroxin among others. Current agents were developed following fluoridation of the quinolone molecule and the first to receive approval by the US Food and Drug Administration (FDA) was norfloxacin (1-ethyl-6-fluoro-1,4-dihydro-4-oxo-7-(1-piperazinyl)-3-quinoline carboxylic acid) in 1984 and it was patented by Kyorin granted Merck & Company[1].

Biological activity

The first-generation quinolones have their greatest potency against Gram-negative bacteria, but newly developed molecules have exhibited increased potency against Gram-positive bacteria, and existing agents are available with additional activity against anaerobic microorganisms[2]. Norfloxacin is a broad-spectrum antimicrobial fluoroquinolone. It is commonly used in the clinical treatment of bacterial-infected cornea for its wide antibiotic spectrum against both Gram-positive and Gram-negative microbes by affecting bacterial DNA gyrase.

Uses

It is used to treat urinary tract infections, gynecological infections, inflammation of the prostate gland, gonorrhea, and bladder infection. Norfloxacin is used for the prevention of spontaneous bacterial peritonitis in cirrhotic patients who have a low ascites fluid protein level, impaired renal function, severe liver disease, have had a prior episode of spontaneous bacterial peritonitis, or esophageal variceal bleeding.

Cytotoxic effects

As a frequently used ocular antibiotic, its eye drops were approved for use in children older than one year of age. But might have cytotoxic effects on human corneal endothelial cells (HCECs), subsequently damaging the cornea and finally impairing human vision. Studies have found that the cytotoxicity of norfloxacin in HCECs is induced by mitochondrion-dependent apoptosis and is probably mediated by death receptor[3].

References

[1] Chierentin L, et al. Review of Properties and Analytical Methods for the Determination of Norfloxacin. Critical Reviews in Analytical Chemistry, 2016; 46. 

[2] Liu D, et al. A thermo-responsive polyurethane organogel for norfloxacin delivery. Polymer Chemistry, 2018; 9: 228-235. 

[3] Fan T, et al.Apoptotic effects of norfloxacin on corneal endothelial cells. Naunyn-Schmiedeberg's Archives of Pharmacology, 2019; 393: 77–88.