Nitroxoline
Sandoz
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Clinical Pharmacology
Pharmacodynamics
Antimicrobial, 8-hydroxyquinoline derivative. It has a wide spectrum of action. Selectively inhibits the synthesis of bacterial DNA, forms complexes with metal-containing microbial cell enzymes.
Active in relation to:
Gram positive bacteria: Staphylococcus spp. (including Staphylococcus aureus); Streptococcus spp., Including: Beta-hemolytic streptococci; Streptococcus pneumoniae; Enterococcus faecalis; Corynebacterium spp; Bacillus subtilis.
Gram-negative bacteria: Escherichia coli; Proteus spp; Klebsiella spp; Salmonella spp; Shigella spp; Enterobacter spp; Haemophilus influenzae; Neisseria gonorrhoeae.
Other microorganisms: Ureaplasma urealyticum; Mycoplasma hominis; Mycobacterium tuberculosis; Trichomonas vaginalis.
Some types of mushrooms: candida, dermatophytes, mold fungi, some causative agents of deep mycoses.
Pharmacokinetics
Suction
Nitroxoline is well absorbed from the gastrointestinal tract (90%). WITHmax in plasma is reached in 1.5-2 hours after ingestion.
Metabolism and excretion
Metabolized in the liver. Excreted mainly by the kidneys unchanged and partially with bile. There is a high concentration of conjugated and unconjugated drug in the urine.
Indications
Treatment of acute, chronic and recurrent urinary tract infections caused by microorganisms sensitive to nitroxoline:
- pyelonephritis;
- cystitis;
- urethritis;
- epididymitis;
- an infected prostate adenoma or carcinoma.
Prevention of infectious complications in the postoperative period:
- in surgical interventions on the kidneys and urinary tract;
- with diagnostic and therapeutic procedures: catheterization, cystoscopy.
Prevention of recurrent urinary tract infections.
Composition
1 coated tablet contains:
Active substance: nitroxoline - 50 mg.
Excipients: calcium phosphate, lactose monohydrate, corn starch, colloidal silicon dioxide, Povidone K25, purified talc, crospovidone, magnesium stearate.
Shell composition: acacia gum, carmellose sodium, povidone K25, sucrose, colloidal silicon dioxide, purified talcum, corn starch, calcium carbonate, titanium dioxide, sunset dye yellow E110, yellow quinoline E104.
Nitroxoline is marketed under different brands and generic names, and comes in different dosage forms:
| Brand name | Manufacturer | Country | Dosage form |
|---|---|---|---|
| 5-noc | Sandoz | Switzerland | pills |
| Nitroxoline | Anzhero-Sudzhensky HFZ | Russia | pills |
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Dosage and Administration
For adults and adolescents: the standard dose is 400 mg / day, divided into 4 doses (2 pills, 4 times / day). The maximum dose is 800 mg / day.
Children older than 5 years: the average dose is 200-400 mg / day, divided into 4 doses.
Children 3-5 years old: the average dose is 200 mg / day, divided into 4 doses.
The course of treatment is 2-4 weeks, if necessary, the therapy is continued with intermittent courses (2 weeks during the month). pills should be taken before meals.
Application for violations of the liver
Patients with liver failure are recommended to use half the standard daily dose of the drug - 200 mg / (1 tablet 4 times / day).
Application for violations of renal function
Patients with moderate renal insufficiency (QC more than 20 ml / min) are recommended to use half of the standard daily dose of the drug - 200 mg / (1 tablet 4 times / day).
Adverse reactions
From the digestive system: nausea, vomiting (can be prevented by taking the drug during a meal), increased activity of hepatic transaminases.
From the side of the central nervous system and peripheral nervous system: ataxia, headache, paresthesia, polyneuropathy.
Since the cardiovascular system: tachycardia.
Allergic reactions: skin rash.
Other: thrombocytopenia, increased serum uric acid levels.
Contraindications
- Cataract;
- severe renal failure (CC less than 20 ml / min);
- severe liver failure;
- children up to 3 years;
- pregnancy;
- lactation period (breastfeeding);
- hypersensitivity to nitroxoline or other components of the drug;
- hypersensitivity to quinolines.
Drug interactions
Not described.
Pregnancy and Lactation
Contraindicated in pregnancy and lactation (breastfeeding).
Special instructions
It should not be prescribed simultaneously with drugs containing hydroxyquinolines or their derivatives.
When used in patients with impaired renal function due to the possible accumulation of the drug, medical supervision is necessary.
You should not assign treatment for more than 4 weeks without additional examination of the liver and kidneys.
During treatment with nitroxoline, urine is stained an intense yellow-red color.
Impact on the ability to drive vehicles and other mechanisms that require high concentration of attention
There is no data on the effect on the ability to drive a car or machinery.
Overdosage
There is no data on overdose or clinical signs of nitroxolin poisoning.
- Brand name: 5-noc
- Active ingredient: Nitroxoline
- Dosage form: pills, coated.
- Manufacturer: Sandoz
- Country of Origin: Switzerland
Studies and clinical trials of Nitroxoline (Click to expand)
- Novel Mechanism of Cathepsin B Inhibition by Antibiotic Nitroxoline and Related Compounds
- Electrochemistry of the antibacterial and antifungal drug nitroxoline and its determination in bulk form, pharmaceutical formulation and human blood
- Powder diffraction study of the hydrogen bonds in nitroxoline and its hydrochloride
- Neuromyopathy in the mouse produced by the antimicrobial agent nitroxoline
- Quantitative high-perormance liquid chromatographic analysis of nitroxoline and structurally related compounds
- Effects of subinhibitory concentrations of nitroxoline on the surface properties ofEscherichia coli
- High-performance liquid chromatographic analysis of nitroxoline in plasma and urine
- Use of galvanostatic coulometry for determining nitroxoline
- ChemInform Abstract: A Microwave-Assisted Nucleophilic Substitution Reaction on a Quinoline System: The Synthesis of Amino Analogues of Nitroxoline.
- Production control of nitroxoline by spectrophotometric method
- Analysis of pharmacopoeia nitroxoline
- A microwave-assisted nucleophilic substitution reaction on a quinoline system: the synthesis of amino analogues of nitroxoline
- In vitro activity of nitroxoline against clinical isolates of Candida species : Die Aktivitat von Nitroxolin in vitro auf klinische Candida-Isolate
- Nitroxoline (8-hydroxy-5-nitroquinoline) is more a potent anti-cancer agent than clioquinol (5-chloro-7-iodo-8-quinoline)
- Development of New Cathepsin B Inhibitors: Combining Bioisosteric Replacements and Structure-Based Design To Explore the Structure–Activity Relationships of Nitroxoline Derivatives
- In vitro activity of the chelating agents nitroxoline and oxine against Mycobacterium bovis BCG
- Antibacterial and Antifungal Activities of Nitroxoline Mannich Bases
- Nitroxoline for treatment of uncomplicated UTI: IPD meta-analysis of four controlled clinical studies
- Nitroxoline/Sulfamethizole Eliminates UTI
- Investigation of nitroxoline-human serum albumin interactions by spectroscopic methods
- Nitroxoline induces apoptosis and slows glioma growth in vivo
- Roles of divalent cations and pH in mechanism of action of nitroxoline against Escherichia coli strains
- In Vitro Activity of Nitroxoline against Escherichia coli Urine Isolates from Outpatient Departments in Germany
- Effect of Nitroxoline on Angiogenesis and Growth of Human Bladder Cancer
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