Mechanism of Action
Nitroxoline exerts a bacteriostatic effect through two main mechanisms. First, it selectively inhibits bacterial DNA synthesis. Second, the drug acts as a chelator: it forms stable complexes with metal ions that serve as cofactors for microbial enzymes, thereby blocking their function and disrupting pathogen metabolism.
Pharmacological Effects
The drug is active against a wide range of pathogens:
- Gram-positive: Staphylococcus spp., Streptococcus spp. (including enterococci and pneumococci), Corynebacterium diphtheriae.
- Gram-negative: Escherichia coli, Proteus spp., Klebsiella spp., Salmonella spp., Shigella spp., Enterobacter spp.
- Other: Mycobacterium tuberculosis, Trichomonas vaginalis, and Candida species.
Indications
The primary clinical application is urinary tract infections, such as cystitis, urethritis, and pyelonephritis. The drug is also prescribed for the prevention of infectious complications following urogenital surgeries.
Adverse Effects
Therapy may cause dyspeptic symptoms (nausea, digestive disturbances), allergic reactions, and neurological disorders (ataxia, paresthesias). A notable feature is the saffron-yellow discoloration of urine, which patients must be informed about to prevent anxiety.
Administration and Dosage
The drug is rapidly and completely absorbed from the gastrointestinal tract. It is excreted by the kidneys unchanged, which ensures therapeutic concentrations specifically in the urine. Dosing regimen: orally, 0.1 g 3–4 times daily. The maximum daily dose (MDD) is 0.8 g.