Norfloxacin

General characteristics. Structure:

Active ingredient: 200 mg of norfloxacin.

Excipients: calcium phosphate double-base, starch corn, lactose, the gelatin, Natrium benzoicum, talc purified of magnesium stearate, colloid anhydride of silicon, sodium glikolit starch, a methylene chloride, OpaDryBlue dye (hydroxypropyl marked cellulose, polyethyleneglycol, talc, titanium dioxide, LakeBrilliantBlue dye), polyethyleneglycol 6000, propylene glycol.

Antibacterial agent.

Pharmacological properties:

Pharmacodynamics. Inhibits bacterial DNK-girazu, the providing superspiralling and stability of DNA, protein synthesis breaks and leads to death of microorganisms.

It is active concerning golden staphylococcus (including staphylococcus, resistant to Methicillinum), epidermal staphylococcus, Neisseria gonorrhoeae, Neisseria meningitidis, colibacillus, Citrobacter spp., клебсиелл, enterobakteriya, Hafnia, protiums (indolpositive and indolnegative strains), salmonellas, shigellas, Yersinia enterocolitica, Campylobacter jejuni, Aeromonas plesiomonas, Vibrio cholerae, Vibrio parahaemolyticus, Haemophilus influenzae, chlamydias, легионелл.

Variable sensitivity to norfloxacin enterococci, streptococci of pyogenes, pneumoniae and viridans, Serratia marcescens, Pseudomonas aeruginosa, Acinetobacter, Mycoplasma hominis pneumoniae, a tuberculosis mycobacterium, and also Mycobacterium fortium have.

Are not sensitive - the majority of strains of Ureaplasmaurealyticum, Nocardiaasteroides, anaerobic bacteria (for example, Bacteroidesspp., peptokokk, peptostreptokokk, Eubacteriumspp., Fusobacteriumspp., Clostridiumdifficile), Treponemapallidum.

Pharmacokinetics. It is well soaked up from digestive tract (an absorption indicator - more than 20-40%), food detains absorption. Therapeutic concentration is reached in plasma in 1 h after intake. Communication with proteins of plasma - 10-15%. Distribution - a parenchyma of kidneys, testicles, liquid of seed tubules, a prostate gland, a uterus, abdominal organs and a small pelvis, bile, maternal milk. Permeability through GEB and a placental barrier high. It is metabolized in small degree in a liver and removed with bile and urine. Excretion is carried out by kidneys for the account of both glomerular filtering, and canalicular secretion. During the day 32% of a dose are excreted with urine, about 30% - with excrements; 5-8% are allocated in the form of metabolites.

Indications to use:

Treatment of the infectious and inflammatory diseases caused by the activators sensitive to drug:
- acute and chronic infectious diseases of urinary tract (cystitis, pyelonephritis, urethritis, prostatitis);
- acute gonorrhea;
- prevention of infections at operative measures and diagnostic procedures in urology;
- shigellosis;
- salmonellosis;
- prevention of sepsis at patients with a neutropenia;
- prevention of infectious diseases of digestive tract and prevention of diarrhea of travelers.

Route of administration and doses:

Inside, in 1 hour prior to or in 2 hours after food, washing down with enough water.

Acute infections of urinary tract - 400 mg two times a day within 7-10 days.

Acute uncomplicated cystitis - 400 mg two times a day within 3 days.

Recurrent or persistent infections of an uric path with aggravations - 400 mg two times a day within 4 weeks, then, if necessary, on 400 mg a day up to 12 weeks.

Acute uncomplicated gonococcal infections - 800 mg once.

Bacterial intestinal infections - 400 mg two times a day within 5 days.

For prevention of a recurrence of infections of urinary tract at frequent aggravations (to 4-5 times a year) drug is appointed on 200 mg of 1 times a day it is long.

Women have data on considerable decrease in frequency of a recurrence of infections of urinary tract with frequent recurrent infections at preventive reception of 200 mg of norfloxacin once after sexual intercourse.

Chemoprophylaxis at urological interventions, operations and at postoperative infections - on 400 mg two times a day before operation, on requirement.

For prevention of sepsis at a neutropenia - on 400 mg 2-3 times a day. Duration of antimicrobic action - about 12 hours.

Prevention of diarrhea of travelers - 400 mg once a day (no more than 21 day). Patients with a renal failure (clearance of creatinine from 10 to 30 ml/min.) - 400 mg once a day.

To patients with a renal failure at glomerular filtering less than 30 ml/min. reduce a dose to 400 mg/days. To the patients who are on a hemodialysis appoint a half of a therapeutic dose.

Features of use:

Restrictions to use: atherosclerosis of vessels of a brain, disturbance of cerebral circulation, epilepsy and convulsive syndrome, renal failure and liver.

Safety of appointment is not established to children of dopubertatny age and the feeding women. Therefore these categories of patients should appoint drug with care.

It is necessary to be careful also at patients with a renal failure. At clearance of creatinine less than 30 ml/min. a dose need to be reduced twice.

Side effects:

From a GIT and a liver: nausea, diarrhea, lack of appetite, bitterness in a mouth, an abdominal pain, dysbacteriosis, candidiasis, pseudomembranous colitis, perhaps tranzitorny increase in activity of hepatic transaminases.

From a nervous system: headache, fatigue, drowsiness.

From system of a hemopoiesis: eosinophilia, leukopenia, decrease in a hematocrit.

From cardiovascular system: tachycardia, disturbances of a cordial rhythm, arterial hypotension, a vasculitis, Stephens's syndrome – Johnson.

From an urinary system: glomerulonephritis, dysuria, polyuria, proteinuria, crystalluria, kreatininemiya, urethral bleedings.

Allergic and immunopathological reactions (skin itch, small tortoiseshell, hypostases) at observance of the mode of dosing are noted extremely seldom.

Interaction with other medicines:

Simultaneous use of norfloxacin and the antiacid means containing a hydroxide of aluminum or magnesium, and also drugs calcigerous, iron and zinc, reduces norfloxacin absorption. In this regard it is necessary to take norfloxacin for 1-2 h to or not less than in 4 h after reception of the specified drugs.

At simultaneous use of norfloxacin and theophylline it is necessary to control concentration of theophylline in a blood plasma and to adjust its dose since undesirable increase in concentration of theophylline in blood and development of the corresponding side effects can be observed.

Norfloxacin can strengthen therapeutic effect of cyclosporine and warfarin. In some cases at use of norfloxacin with cyclosporine increase in concentration of serumal creatinine therefore at such patients control of this indicator is necessary was observed.

Simultaneous introduction with the medicines having potential ability to reduce the ABP can cause heavy hypotonia, with the drugs reducing a convulsive threshold of a brain (for example, theophylline) - epileptiform attacks.

Norfloksatsits reduces effect of nitrofurans.

Contraindications:

- hypersensitivity to hinolona;
- liver failure;
- end-stage of a chronic renal failure;
deficit glyukozo-6-fosfatdegidrogenazy;
- pregnancy (at a fruit development of arthropathies is possible);
- lactation;
- children's and teenage age (up to 15 years).

Overdose:

Symptoms: dizziness, nausea, vomiting, drowsiness, emergence of cold sweat (without changes of the main hemodynamic indicators), a convulsive syndrome.

Treatment: a gastric lavage, adequate hydration therapy with an artificial diuresis, purpose of symptomatic means.

Storage conditions:

List B. To store in the dry, protected from light place, at a temperature not above +25 °C. To store in the place, unavailable to children. Period of validity 3 years.

Issue conditions:

According to the recipe

Packaging:

On 10 or 20 tablets in banks polymeric. 1 bank together with a leaf insert in a pack.

On 10 tablets in a blister strip packaging. 1 or 2 blister strip packagings in a pack.