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Nitroxoline

Nitroxolinum

For medical students2 min readUpdated 2026-10-10

Nitroxoline is a synthetic antibacterial agent derived from 8-hydroxyquinoline. The drug exhibits prominent bacteriostatic activity and is primarily used to treat infectious and inflammatory diseases of the urinary tract.

Pharmacological class8-hydroxyquinoline derivatives
Spectrum of activityBroad: Gram-positive and Gram-negative bacteria, fungi, protozoa
PharmacokineticsExcreted by the kidneys unchanged, achieving high concentrations in urine
Formulation0.05 g tablets

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:

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.

Mnemonic

5-NOK: 5 (nitro) — O (oxyquinoline/hydroxyquinoline) — K (Klebsiella/coliforms/kidney UTIs). Yellow urine — the 'golden' standard of excretion.

Frequently asked questions

What neurological side effects can nitroxoline cause?

Ataxia and paresthesias may occur during nitroxoline treatment.

Why is nitroxoline effective for cystitis?

The drug is excreted by the kidneys unchanged, creating high concentrations of the active substance directly in the urine and targeting urinary tract pathogens.

Should the patient be warned about urine discoloration?

Yes, this is a specific side effect of the drug (saffron-yellow discoloration) that is not a sign of pathology but can startle the patient.

What is the maximum daily dose of nitroxoline?

The maximum daily dose is 0.8 g.

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