Nitroxoline

General characteristics. Structure:

Active agents: 50 mg of nitroxoline. 

Excipients: lactose (sugar milk), potato starch, silicon dioxide colloid (aerosil), talc, calcium stearate, polysorbate – 80 (the twin - 80) – enough before receiving  a tablet weighing 100 mg (without cover); sugar (sucrose), magnesium a hydroxycarbonate, povidone (polyvinylpirrolidone low-molecular medical), silicon dioxide colloid (aerosil), talc, titanium dioxide, tropeolin Oh, an azoruby (acid red 2C for the pharmaceutical purposes), beeswax –  before receiving a tablet with a cover weighing 200 mg.

Description. Tablets, coated light orange or orange color, round, biconvex. On a break three layers are visible: internal – from yellow till grayish-yellow color, is allowed slightly greenish shade; average - white color and outside – from light orange till orange color.

Pharmacological properties:

Antimicrobic broad-spectrum agent. Nitroxoline selectively inhibits synthesis of bacterial DNA and has effect as on gram-positive microorganisms: Staphylococcus spp. (including S.aureus), Streptococcus spp. (including beta and hemolitic streptococci, Streptococcus pneumoniae, Enterococcus faecalis), Corynebacterium diphtheriae Bacillus subtilis; and on gram-negative microorganisms: N. gonorrhoeae, E. сoli, Proteus spp., Klebsiella spp., Salmonella spp., Shigella spp., Enterobacter spp. Nitroxoline is active also concerning Mycobacterium tuberculosis, Trichomonas vaginalis, some species of mushrooms (Candida spp., dermatophytes, mold, some causative agents of deep mycoses). 

Pharmacokinetics. Absorption – high. It is removed by kidneys in an invariable look, at the same time high concentration in urine is noted (100 mkg/ml and more).

Indications to use:

Infectious and inflammatory diseases of preferential urinogenital ways (including pyelonephritis, cystitis, urethritis, epididymite; the infected adenoma or a carcinoma of a prostate, etc.), caused by microorganisms, sensitive to nitroxoline.

Prevention of infectious complications at diagnostic and medical manipulations (catheterization, a tsistoskopiya) in the postoperative period at surgical interventions on kidneys and urinogenital ways.

Route of administration and doses:

Drug is accepted inside.

For adults the daily dose makes 400-800 mg.

Frequency rate of reception 3-4 times a day with an interval of 6-8 h. Course of treatment 2-3 weeks.

At persistent infections of urinary tract it is possible to appoint drug repeatedly for 2 weeks with the 2nd week break.

The average daily dose for children is more senior than 5 years – 0,2-0,4 g (on 0,05-0,1 g 4 times a day), 5 years – 0,2 g a day are younger.

For prevention of infections at kidney and urinary tract operations appoint 0,1 g to reception 4 times a day within 2-3 weeks.

To children appoint in a daily dose 10-30 mg/kg in 3-4 receptions. 

Features of use:

During treatment urine is painted in saffron-yellow color.

Side effects:

Nausea, vomiting, appetite loss are sometimes possible, it is very rare – skin allergic reactions. In rare instances – tachycardia, an ataxy, a headache, paresthesias, polyneuropathy, abnormal liver functions. At prolonged use the case of development of neuritis of an optic nerve is described.

Interaction with other medicines:

It is not described.

Contraindications:

The renal failures which are followed oligo-or an anury; serious illness of a liver; deficit glyukozo-6-fosfatdegidrogenazy; children's age up to three years (taking into account a firm indivisible dosage form), a cataract, neuritis, a polyneuritis, pregnancy (the III trimester), the lactation period. Hypersensitivity to drugs of a quinolinic row.

Overdose:

Cases are not described.

Storage conditions:

In the dry, protected from light place, at a temperature not above 25 °C. List B. To store in the place, unavailable to children. Period of validity 4 years. After validity period not to use drug.

Issue conditions:

According to the recipe

Packaging:

Tablets, coated, 50 mg.

On 10 tablets in a blister strip packaging from a film of the polyvinyl chloride  and printing aluminum foil varnished.

On 50  tablets in bank of orange glass, or a bottle from polyethylene, or to bank from polymeric materials.

5 blister strip packagings or to bank of orange glass with the application instruction place  in a pack from a cardboard.

100 bottles from polyethylene or cans from polymeric materials with application instructions place in a box from a cardboard (for hospitals).