Norfloxacin - instructions for use, dose, side effects, contraindications

The drug has antimicrobial activity, inhibiting the work of such enzymes of a bacterial cell as a topoisomerase II (DNA gyrase) and / or topoisomerase IV. By suppressing DNA-gyrase, it breaks the process of DNA supercoiling, which disrupts the processes of transcription, repair and duplication of bacterial DNA, which eventually leads to the death of bacteria.

The preparation is bactericidal for a wide range of microorganisms: Enterococcus faecalis, Staphylococcus aureus, Staphylococcus epidermidis, Staphylococcus saprophyticus, Streptococcus agalactiae, Citrobacter freundii, Enterobacter aerogenes, Enterobacter cloacae, Escherichia coli, Klebsiella pneumoniae, Neisseria gonorrhoeae, Proteus mirabilis, Proteus vulgaris, Pseudomonas aeruginosa, Serratia marcescens, Salmonella spp., Shigella spp., Yersinia enterocolitica, Haemophilus influenza, Staphylococcus aureus, Staphylococcus epidermidis, Staphylococcus warneri, Streptococcus pneumoniae, Acinetobacter calcoaceticus, Aeromonas hydrophila, Haemophilus influenzae, Proteus mirabilis, Pseudomonas aeruginosa, Serratia marcescens, Bacillus cereus, Citrobacter diversus, Edwardsiella tarda, Enterobacter agglomerans, Hafnia alvei, Haemophilus aegyptius, Haemophilus ducreyi, Klebsiella oxytoca, Klebsiella rhinoscleromatis, Morganella morganii, Providencia alcalifaciens, Providencia rettgeri, Providencia stuartii, Pseudomonas fluorescens, Pseudomonas stutzeri, Salmonella typhi, Vibrio cholerae, Vibrio parahaemolyticus, Yersinia enterocolitica, Ureaplasma urealyticum.

In most cases, it is inactive with respect to obligate anaerobes, does not show activity against Treponema pallidum.

Pharmacokinetics:

When taking with food absorbs 30-40% of the drug. Pseeking to slow absorption. The maximum concentration in the blood is reached for about 1 hour. The drug penetrates the blood-brain barrier and placenta, the connection with plasma proteins is 10-15%, metabolized in the liver (20%) and kidneys to less active metabolites. The half-life is 3-4 hours. Excreted by the kidneys and the gastrointestinal tract.

Indications:

Infectious-inflammatory diseases caused by microorganisms sensitive to the preparation.

Orally: diseases of the prostate, urinary tract, prevention of recurrence of urolithiasis, gastrointestinal tract diseases, travelers' diarrhea, bacterial infections in patients with granulocytopenia.

Locally: keratitis, conjunctivitis, keratoconjunctivitis, blepharitis, corneal ulcers, prevention of eye infections, after removal of the foreign body,surgical intervention, chemical eye trauma; chronic otitis media, complications in surgical interventions on the hearing organ, external otitis, acute inflammation of the meibomian glands and dacryocystitis.

ICD-10

I.A00-A09.A02 Other salmonella infections

I.A00-A09.A03.0 Shigellosis caused by Shigella dysenteriae

I.A00-A09.A09 Diarrhea and gastroenteritis of allegedly infectious origin

I.A50-A64.A54 Gonococcal infection

VII.H00-H06.H01.0 Blepharitis

VII.H00-H06.H04.3 Acute and unspecified inflammation of lacrimal ducts

VII.H00-H06.H04.4 Chronic inflammation of lacrimal ducts

VII.H10-H13.H10 Conjunctivitis

VII.H10-H13.H10.2 Other acute conjunctivitis

VII.H10-H13.H10.5 Blepharoconjunctivitis

VII.H15-H22.H16 Keratite

VII.H15-H22.H16.0 Corneal ulcer

VII.H15-H22.H16.2 Keratoconjunctivitis

VIII.H60-H62.H60 External otitis media

VIII.H65-H75.H66 Purulent and unspecified otitis media

VIII.H65-H75.H66.4 Purulent otitis media, unspecified

VIII.H65-H75.H68 Inflammation and occlusion of the auditory [Eustachian] tube

XI.K80-K87.K81.0 Acute cholecystitis

XI.K80-K87.K81.1 Chronic cholecystitis

XI.K80-K87.K83.0 Cholangitis

XIV.N10-N16.N10 Acute tubulointerstitial nephritis

XIV.N10-N16.N11 Chronic tubulointerstitial nephritis

XIV.N10-N16.N12 Tubulointerstitial nephritis, not specified as acute or chronic

XIV.N30-N39.N30 Cystitis

XIV.N30-N39.N34 Urethritis and urethral syndrome

XIV.N40-N51.N41 Inflammatory diseases of the prostate

XIV.N40-N51.N41.9 Inflammatory disease of prostate, unspecified

XIV.N40-N51.N45 Orchitis and epididymitis

XIV.N70-N77.N71 Inflammatory diseases of the uterus, except the cervix

XIV.N70-N77.N72 Inflammatory disease of the cervix

XXI.Z20-Z29.Z29.2 Another type of preventive chemotherapy

Contraindications:

Pregnancy.

Lactation.

Age under 18 years, for drops - up to 12 years (safety and effectiveness of norfloxacin in children and adolescents are not defined, it should be borne in mind that norfloxacin causes arthropathy in immature animals).

Hypersensitivity.

Deficiency of glucose-6-phosphate dehydrogenase.

Tendonitis or rupture of tendons associated with taking norfloxacin or other Drugs from the group of quinolones.

Hereditary lactose intolerance, lactase deficiency or glucose-galactose malabsorption.

Carefully:

Epilepsy and convulsive syndromes of another etiology.

Predisposition to convulsive reactions.

Psychoses and other mental disorders in the anamnesis.

Renal / hepatic insufficiency.

Atherosclerosis of cerebral vessels, cerebral circulation disorder (in the anamnesis).

Organic diseases of the central nervous system.

Myastenia gravis.

Hepatic porphyria.

Diabetes.

Syndrome of congenital extension of the QT interval.

Diseases of the heart (heart failure, myocardial infarction, bradycardia).

Electrolyte imbalance (eg, hypokalemia, hypomagnesemia).

Elderly age

In women, simultaneous administration of drugs that extend the QT interval (antiarrhythmic agents of IA and III classes, tricyclic and tetracyclic antidepressants, neuroleptics, macrolides, antifungals, imidazole derivatives, some antihistamines, including astemizole, terfenadine, ebastine), means for general anesthesia from the barbiturate group; medicines that reduce blood pressure.

Pregnancy and lactation:

Category FDA - C. When pregnancy is possible, if the expected effect of therapy in the mother exceeds the potential risk for the fetus (adequate and strictly controlled safety studies of the use of norfloxacin in pregnant women have not been conducted, including for topical administration in the form of drops).

There is a potential risk of serious adverse reactions in children who are breastfeeding. Breastfeeding women should either stop breastfeeding,or taking norfloxacin (given the importance of the medicine for the mother), including for local action in the form of drops.

Dosing and Administration:

Inside fasting (not less than 1 hour before or 2 hours after eating) and drink plenty of liquid.

Orally 400-800 mg 1-2 times a day. The duration of treatment is determined individually. The duration of the course depends on the indications for use, the severity of the infection process and the activity of the pathogen: for uncomplicated urinary tract infections - for 7-10 days, for uncomplicated cystitis - 3-7 days, for chronic recurrent urinary tract infections - up to 12 weeks, with acute bacterial gastroenteritis - 5 days. In acute uncomplicated gonococcal infection - once 800 mg.

Patients with impaired renal function ground clearance creatinine less than 30 ml / min and patients on hemodialysis are prescribed 1/2 therapeutic dose 2 times a day or a full dose 1 time per day.

Locally applied in ophthalmology and ENT-practice as directed by a doctor.

Locally - 1-2 drops in the affected eye or ear 4 times a day. Depending on the degree of infection, the dose on the first day can be 1-2 drops every 2 hours.

Side effects:

From the nervous system: dizziness, headache, sleep disorder, anxiety, fatigue, tingling in the fingers, drowsiness, depression, insomnia.

On the part of the digestive system: anorexia, heartburn, nausea, abdominal pain, diarrhea, bitter taste in the mouth (including after instillation in the eye), increased activity of hepatic transaminases, alkaline phosphatase, lactate dehydrogenase; pseudomembranous colitis (with prolonged use), pain in the rectum or anus, constipation, flatulence, dryness of the oral mucosa, ulceration of the oral mucosa, itching of the anus.

From the hematopoiesis: leukopenia, thrombocytopenia, eosinophilia, neutropenia.

From the musculoskeletal system: tendonitis, rupture of tendons, arthralgia, bursitis, puffiness of hands and feet.

From the senses: blurred vision.

From the cardiovascular system: tachycardia, heart rhythm disturbance, decrease HELL, vasculitis, myocardial infarction.

Allergic reactions: itching, angioedema, rash.

From the side of the urinary system: interstitial nephritis, renal colic.

Other: candidiasis, albuminuria, crystalluria, cylindruria, dysphagia, hyperglycemia, hypercholesterolemia, hyperkalemia, hypertriglyceridemia, hematuria, liver necrosis, hypoglycemia, nystagmus, postural hypotension, prolongation of prothrombin time.

When instillation in the eye: visual impairment, burning and pain in the eye, congestion hyperemia, chemosis, photophobia, allergic reactions.

Overdose:

Symptoms (3 g for 45 minutes): dizziness, nausea, vomiting, drowsiness, the appearance of cold sweat (without changes in the basic hemodynamic indicators), convulsive syndrome, puffy face.

Treatment: gastric lavage, adequate hydration therapy with forced diuresis, the appointment of symptomatic drugs. There is no specific antidote.

Interaction:

Simultaneous reception of the drug with drugs that lower blood pressure, can lead to a sharp and significant decrease in blood pressure.

Combination Algebra + magnesium hydroxide slows the absorption of norfloxacin (the interval between the intake should be at least 2 hours).

Didanosine may slow absorption and reduce the level of norfloxacin in tissues; notshould be taken at the same time - an interval of at least 2 hours is necessary.

The drug reduces the effectiveness of nitrofurans.

With the joint use of caffeine, caffeine in the combination drotaverin + caffeine + naproxen + paracetamol + pheniramine maleate and norfloxacin, it is possible to reduce the metabolism of caffeine in the liver (slowing its elimination and increasing the concentration in the blood). With the simultaneous use of caffeine (in combination drotaverin + caffeine + naproxen + paracetamol + pheniramine maleate) and norfloxacin - a decrease in the metabolism of caffeine in the liver (slowing its elimination and increase in blood concentration).

Iron gluconate, iron sulfate, iron fumarate slow down absorption and reduce the level of norfloxacin in tissues; should not be taken together or within 3 hours after. A drug norfloxacin forms complexons with metal ions.

The drug enhances the anticoagulant properties of warfarin.

The drug increases the concentration of cyclosporine in the blood when taken together. In some cases, with the use of norfloxacin with cyclosporine, an increase in the serum creatinine concentration was observed, therefore, in such patients monitoring of this index is necessary.

The drug reduces the clearance of theophylline by 25%.

Rifampicin accelerates biotransformation, reduces the concentration of norfloxacin in tissues.

Simultaneous use of norfloxacin and sucralfate reduces the absorption of norfloxacin (the interval between their intake should be at least 2-4 hours).

The simultaneous use of tizanidine with norfloxacin is not recommended (isoenzyme inhibitor CYP1A2).

Special instructions:

When performing surgical interventions, monitoring of the state of the blood coagulation system is required (during the period of therapy, an increase in the prothrombin index is possible).

Impact on the ability to drive vehicles and manage mechanisms

During treatment with norfloxacin, caution should be exercised when driving a car and practicing potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions.

Instructions

Norfloxacin (Norfloxacinum)