Нитроксолин

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Нитроксолин

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Method of action: Anti-Inflammatory

Treatment option: Prostatitis, Urethritis, Cystitis

Medically reviewed

Rosario Oropesa

Last updated on 22/12/2025

This page provides general, reference-level information compiled from official medical sources. It is not a substitute for professional medical advice, diagnosis, or treatment. For decisions about your health, please consult a qualified healthcare professional.

Overview of Нитроксолин

Property Description
Active ingredient Nitroxoline (5-nitro-8-hydroxyquinoline)
Form Tablets, soft capsules
Pharmacological class Antibacterial agent, Uroantiseptic
Common use Combating microbial infections in the urinary tract
Origin Synthetic 8-hydroxyquinoline derivative

Classification and Identity of Nitroxoline

Нитроксолин is a synthetic, single-substance antimicrobial agent that holds the official classification of J01XX07 within the WHO-ATC Classification System. It is recognized primarily as a uroantiseptic for systemic administration in its solid oral form. The active ingredient, Nitroxoline (INN), belongs to the distinct chemical group of 8-hydroxyquinoline derivatives, setting it apart from more contemporary antibiotic families. Despite being an older compound, Nitroxoline demonstrates potent broad-spectrum antimicrobial agent activity against various bacteria, including Escherichia coli. The INN-level differentiation of Nitroxoline lies in its unique structure, which is clinically recognized for exhibiting a low degree of cross-resistance with other major classes of antibacterial drugs.

Composition and Available Form

The drug's composition relies entirely on the therapeutic efficacy of its sole active ingredient, Nitroxoline, which has the chemical formula C9H6N2O3. This substance is commercially available as an oral antibiotic in the form of tablets and soft capsules. The unique structural nature of this hydroxyquinoline derivative, which is often considered unrelated to other standard drug classes, contributes to its specific mechanism of action.

General Purpose and Action Domain

The general purpose of Нитроксолин is to suppress microbial growth, with a primary domain of action within the urinary system, leveraging its uroantiseptic property. This medicine is typically used in situations where suppression of microbial colonization in the lower urinary tract is required. Its mechanism involves chelation, where it binds to essential metallic cations like Fe^2+ and Zn^2+, which stops pathogens from synthesizing genetic material and induces a bacteriostatic effect. Nitroxoline also has the property to reduce the formation of and induce the dispersal of biofilms, a capability particularly beneficial for combating persistent infections.

What side effects are possible with Нитроксолин?

Possible Side Effects and Safety Information

The safety characteristics of Nitroxoline are based on its long history of clinical use and regulatory documentation, which generally classifies most reported adverse reactions as non-serious and reversible. This section details the safety profile according to officially documented classifications.

System-Organ Class (SOC) Safety Profile

Adverse reactions listed in regulatory documents are classified by the affected physiological system:

  • Gastrointestinal Disorders: The most commonly documented effects include nausea, vomiting, abdominal pain, and general gastrointestinal disturbances.
  • Nervous System Disorders: Reactions such as headache and dizziness have been reported.
  • Skin and Subcutaneous Tissue Disorders: Includes documented manifestations of hypersensitivity, such as rash and urticaria.
  • Hepatobiliary Disorders: Reports of transient changes in liver enzyme levels have been noted, particularly with extended exposure.

Expected Functional Feature

A characteristic feature of treatment with Nitroxoline is the expected, non-adverse change to a yellow or saffron-yellow discoloration of the urine (chromaturia). This is a functional outcome of drug metabolite excretion and is not indicative of toxicity.

Serious Reactions and Safety Constraints

While rare, the potential for severe hypersensitivity reactions (allergic reactions or angioedema) is officially documented as a possibility.

Specific safety restrictions are defined in official labeling:

  • Contraindications: Use is strictly constrained in individuals with known hypersensitivity to the active substance, as well as those with severe renal impairment and severe hepatic impairment.
  • Duration-Related Monitoring: Regulatory documents require periodic liver enzyme monitoring for patients receiving this medicine over extended courses of treatment.

Overdose and Emergency Response

The official regulatory documentation for Nitroxoline overdose addresses acute exposure and mandated emergency responses. The active substance carries a regulatory classification of Toxic if swallowed (Acute Toxicity Category 3). This classification dictates that upon any suspected over-ingestion, it is required to immediately call a poison center or doctor and seek prompt medical attention. The official guidance strictly advises patients not to induce vomiting but to rinse the mouth following ingestion.

Clinical reports cited in government literature have documented instances of high-dose over-ingestion, such as 5000 mg. In the documented case, the only specific manifestation observed was fatigue. Importantly, the patient remained alert and oriented, and no further signs of severe acute toxicity were noted.

The regulatory profile confirms that no specific antidote is known for Nitroxoline overdose. Therefore, the management of acute over-ingestion is constrained to providing symptomatic and supportive treatment. Furthermore, specific continuous hospital monitoring protocols for uncomplicated overdose are not formally documented in available regulatory summaries, nor are any population-specific considerations regarding increased severity for vulnerable groups.

Therapeutic Uses of Нитроксолин

What Нитроксолин Treats: Main Uses and Benefits

Нитроксолин is commonly used to help with symptoms related to urinary tract infections (UTIs). It is applied in addressing conditions presenting with systemic or localized discomfort in the urinary system.

Therapeutic Scope and Supportive Benefits

This medication is commonly used across conditions presenting with acute episodes in the lower urinary tract, such as cystitis and urethritis, and may be relevant for upper tract infections like pyelonephritis. It is also applied in situations involving recurrent or episodic manifestations and is used for temporary symptomatic assistance when a patient is recovering from urological procedures. Its therapeutic focus is supporting the management of susceptible bacteria and certain fungal organisms.

“The supportive use of the medication contributes to easing distress and assists with maintaining functional stability during difficult episodes.”

This supports the patient during acute symptomatic phases by addressing the painful or urgent symptoms related to voiding. The drug is considered relevant for managing symptom clusters that may become intense or disruptive, helping to improve day-to-day comfort during symptomatic periods, supporting patients during episodes of heightened discomfort.


Quick Fact: Relief for Voiding Distress

Нитроксолин is relevant for managing symptoms of acute infections, specifically symptoms related to inflammatory or irritative states, such as the pain or burning sensation during urination (dysuria) and the frequent, urgent need to void.

Eligibility and Restrictions for Use

Eligibility Map: Who can and cannot use Нитроксолин — official regulatory information

Populations for whom use is contraindicated: Use of Nitroxoline is strictly prohibited for patients with known hypersensitivity to the drug or other 8-hydroxyquinoline derivatives. Absolute contraindications extend to severe disorders of the liver and kidneys, specifically those involving oliguria or anuria. Use is also excluded for individuals with G-6-PD deficiency, cataract, neuritis, and certain diseases of the peripheral nervous system.

Age-Related and Physiological Restrictions: The tablet dosage form of the medicine is formally contraindicated for children under 3 years of age. Use is established and allowed for adults and older children with appropriate dose adjustments. For physiological states, the medicine is explicitly contraindicated throughout both pregnancy and the entire period of breastfeeding (lactation).

Conditional Use and Organ Function: Regulatory documents define use constraints based on organ function. Patients with moderate hepatic or renal insufficiency require a mandatory dose reduction to manage potential accumulation. Additionally, the drug must be used with caution in elderly patients due to the documented potential for delayed excretion.

What should I know about interactions with other medicines?

Interactions with other medicines and products

Clinical data on drug interactions for Нитроксолин (Nitroxoline) primarily highlight a significant interaction risk with the class of Indirect Anticoagulants (also known as Vitamin K Antagonists). This interaction is clinically important because it can lead to an increase in the therapeutic effect of the anticoagulant medicine.

Documented Interacting Medicines and Classes

Product Category Specific Examples (if listed) Result of Interaction
Indirect Anticoagulants (Vitamin K Antagonists) Warfarin, Acenocoumarol, Dicoumarol, Phenprocoumon, Fluindione, Phenindione, Ethyl biscoumacetate Increased therapeutic efficacy of the anticoagulant.

Interaction Management Constraints

Due to the documented increase in anticoagulant effect, the concurrent use of Нитроксолин with these medicines requires close medical management. Healthcare providers must implement monitoring of coagulation parameters (such as the International Normalized Ratio or INR) with high vigilance. Based on the monitored values, a dose adjustment of the indirect anticoagulant medicine may be necessary to mitigate the risk of adverse events like bleeding. There are no other major drug classes specified in official regulatory documents as having clinically significant interactions with Нитроксолин.

Mechanism of Action

How Нитроксолин Works

Nitroxoline exerts its effect primarily by acting as a chelating agent, binding essential divalent metal cations (Zn^2+, Fe^2+) required as cofactors by key microbial enzymes such as RNA Polymerase and DNA Gyrase. This sequestration of necessary metal ions leads to the non-competitive inhibition of these enzymes, fundamentally blocking the molecular pathways necessary for DNA replication and transcription. This cascade ultimately leads to microbial metabolic arrest and constraint on active replication.

The drug engages a secondary mechanistic domain by targeting the structure of microbial biofilms. By chelating the metal ions (Mg^2+, Zn^2+) that stabilize the biofilm’s extracellular matrix, Nitroxoline induces the disruption and dispersion of these protective aggregates. This mechanism, alongside its ability to alter bacterial surface properties, modifies the pathogen's capacity for adhesion to epithelial cells, supporting a reduction in the persistence of microbial aggregates and colonization potential within the environment.

The pharmacological action of Nitroxoline is highly concentration-dependent, meaning its action is optimized in systems where high local concentrations are readily achieved. Furthermore, the chelation mechanism is subject to competitive antagonism; its action can be functionally weaker in biological settings with high concentrations of non-target divalent metal ions (Mg^2+, Mn^2+), which compete for binding sites and constrain the drug's maximal effect.

Dosage and Administration Information

Instruction Map: How to use Нитроксолин — official administration guidelines

The following high-level usage principles describe the standard administration of the drug.

Administration scope Detail
Route of administration Oral (ingested by mouth).
Dosing schedule (Adult Treatment) The standard dose is 250 mg per unit, often administered three times daily, totaling 750 mg per day.
Timing in relation to meals The medication is specified to be taken approximately one hour before meals.
Preparation requirements The solid oral form should be taken with a glass of water to ensure proper ingestion.
Age-group administration rules Pediatric dosing is calculated based on body weight, typically in the range of 10 mg/ kg/ day to 20 mg/ kg/ day, administered in divided doses.
Missed-dose rules Instructions state not to compensate for a missed dose by doubling the next scheduled intake.
Special procedural conditions For recurrence prevention, a lower dose is taken once daily, often scheduled for the evening. The acute treatment course must be completed, typically lasting 5 to 14 days, without premature discontinuation.
Instruction classifications (high-level) Detail
Administration method type Oral.
Frequency pattern Multiple times daily (t.i.d.) for treatment; Once daily (q.d.) for long-term use.
Basis of use Based on standardized prescribing protocols.
Use-context constraints Strict timing relative to food intake and mandatory completion of the prescribed course.

Resulting procedural structure Official step sequence:

  • Ingest the solid oral dosage form (tablet or capsule) approximately one hour prior to any meal.
  • Take the unit dose with a full glass of water.
  • Repeat the administration three times daily (t.i.d.) for the duration of the prescribed acute course.

Connection to the overall use protocol (2–4 sentences): Standard usage protocols define the oral route and the 250 mg three-times-daily dose for acute treatment. These instructions govern the practical administration of the medicine, defining precise constraints for intake timing and mandating adherence to the full duration of the specified course, even if symptoms subside.

Recent Clinical Evidence

Research evidence / Overview of studies for Нитроксолин


Evidence for Use in Acute Uncomplicated Urinary Tract Infections (uUTI)

The primary body of research for Nitroxoline is derived from an Individual Patient Data (IPD) meta-analysis of controlled clinical studies. This research primarily focused on adult women with acute, uncomplicated urinary tract infections. The studies were designed to collect measurements of bacterial levels in the urine, alongside clinical endpoints that recorded how patients reported changes in acute symptoms like pain or burning during urination over a short-term observation period.

Studies exploring short-term symptom changes described patterns in how patients reported the evolution of common urinary discomfort indicators during the study period. While the structure of the meta-analysis is comprehensive, long-term follow-up beyond the initial test-of-cure period (typically 7–13 days post-treatment) is not well characterized in the core evidence base.


Research on Multidrug-Resistant (MDR) Pathogens

A significant body of evidence for this compound comes from laboratory-based (in vitro) susceptibility testing and epidemiological resistance surveillance programs spanning many years. This research examines the compound’s activity against common uropathogens, including strains that exhibit resistance to multiple other drug classes (MDR pathogens).

Surveillance data show patterns related to the drug's activity, reporting sustained low resistance rates for many common bacteria like E. coli over long periods of observation, compared to the rising resistance rates observed for some other standard antibiotics. This evidence is primarily derived from laboratory results, and research is still needed to establish the generalizability of in vitro susceptibility to patient responses in clinical settings.


Research Gaps and Uncertainties

Comparative evidence against modern treatment options for acute UTI is lacking in the form of dedicated, large-scale randomized trials. Data for certain groups, such as children or patients with specific comorbidities, remain insufficient or are drawn from older, less methodologically standardized studies. The research base for more complex infections, such as pyelonephritis, is also limited, relying mainly on older observational studies rather than modern, high-quality clinical trial data.

Key Studies & References

  1. Nitroxoline resistance is associated with significant fitness loss and diminishes in vivo virulence of Escherichia coli (Laboratory/Surveillance)

Frequently Asked Questions (FAQ)

Common questions about Нитроксолин (FAQ)

Q: Can I drink alcohol while taking this medicine?

A: Official guidance recommends avoiding alcohol while taking this medicine. The combination of this medicine and alcohol can intensify certain central nervous system (CNS) side effects, such as increasing feelings of dizziness and sleepiness.

Q: Does it make you sleepy?

A: Yes, official product information indicates that dizziness and somnolence (sleepiness) are common side effects of this medicine. Due to these potential effects, caution is advised, as they may impair the ability to drive or operate machinery.

Q: What should I do if I miss a dose?

A: The product information states that if a dose is missed by a short period, it may be taken. However, if the time is close to the next scheduled dose, the documentation advises skipping the missed dose and returning to the regular schedule. Doses should not be doubled.

Q: Is it safe to take during pregnancy?

A: Regulatory information indicates that this medicine may cause harm to an unborn fetus. It is stated that women who are able to become pregnant should use effective contraception during treatment. Potential risks should be reviewed with a healthcare professional.

Q: Is it safe long-term?

A: The official documentation highlights effects that require monitoring during long-term use. These include the potential for dependence and common effects such as weight gain and fluid retention (peripheral edema). The need for continued use should be regularly reassessed by a healthcare professional.

Q: What are the common side effects?

A: Official reports of common side effects include dizziness, sleepiness (somnolence), blurred vision, dry mouth, weight gain, and swelling of the hands and feet (peripheral edema). This information is based on data collected during clinical trials described in the product label.

Q: Can I suddenly stop taking this medicine?

A: Official regulatory documents caution patients against suddenly stopping this medicine. To reduce the risk of withdrawal symptoms, such as an increased chance of seizures or other adverse reactions, the medicine should be gradually reduced over a period of at least one week under medical guidance.

How should Нитроксолин be stored and disposed of?

Storage and Disposal Requirements for Nitroxoline

Nitroxoline must be stored strictly according to the conditions detailed in the official regulatory labeling to maintain its stability and quality. The product must be kept at a temperature not exceeding 25 °C. It is mandatory to store the medicine in its original packaging to ensure protection from both light and moisture, securing it in a dry place.

Required Storage and Handling

Condition Requirement
Temperature Not exceeding 25 °C
Protection Store in original packaging, protected from light and moisture
Access Keep out of the sight and reach of children
Stability Do not use after the expiry date

Disposal

Official instructions require that unused or expired Nitroxoline must not be disposed of in household waste or flushed down the wastewater system. Disposal must be carried out in accordance with local pharmaceutical waste regulations.

Attention! Always consult to a doctor or pharmacist before using pills or medicines.

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