Norfloxacin (When ATH S01AX12)

When ATH:
S01AX12

Characteristics norfloxacin

Fluoroquinolone antibacterial agent II generation. Synthetic pyridone analog of nalidixic acid; is a fluorine atom in position 6 (It enhances the effect on gram-negative microorganisms) and piperazine group at position 7 (It provides activity against Pseudomonas). Norfloxacin is a metabolite pefloksatsina, which is different from the absence of a methyl group at the piperazine nucleus.

White or pale yellow crystalline powder. Octanol-water partition coefficient is 0,46. Easily soluble in glacial acetic acid, very slightly in ethanol, methanol and water. Solubility in 25 °C (mg / ml): in the water- 0,28; methanol is 0,98; ethanol — 1,9; acetone is 5,1; chloroform — 5,5; diethyl ether- 0,01; benzene is 0,15; ethyl acetate- 0,94; oktilovom alcohol- 5,1; glacial acetic acid is 340. Water solubility is pH dependent: increases sharply at pH<5 и pH>10. Hygroscopic, air forms a hemihydrate. Molecular weight - 319,34.

The pharmacological action of norfloxacin

Broad-spectrum antibacterial, bactericide.

The use of norfloxacin

Infection, caused by pathogens sensitive to norfloxacin:

inside - Acute and chronic urinary tract infection (incl. pyelonephritis, cystitis, uretrit), genital infections (incl. prostatitis, cervicitis, endometritis), neoslojnennaya gonorrhea, GI (incl. salmonellosis, dysenteries); prevention of infections in patients with granulocytopenia;

locally - Otitis externa, and acute exacerbation of chronic otitis media; eye infection, incl. conjunctivitis, keratit, keratokonъyunktyvyt, kornealynaya ulcer, .Aloe, blefarokonъyunktyvyt.

Contraindications norfloxacin

Hypersensitivity (incl. history), tendonitis or tendon rupture, associated with the intake of other drugs or norfloxacin quinolone; deficiency of glucose-6-fosfatdegidrogenazы, childhood and adolescence up 18 years, for the drops, until 12 years (safety and efficacy of norfloxacin in children and adolescents are not defined; it should be understood, that norfloxacin cause arthropathy in immature animals).

Restrictions on the use of norfloxacin

Cerebral atherosclerosis, cerebrovascular accident, epilepsy and convulsions, myastenia gravis, renal / hepatic insufficiency.

Application of norfloxacin in pregnancy and breastfeeding

When pregnancy is possible, if the effect of therapy for the mother outweighs the potential risk to the fetus (adequate and well-controlled studies safety of norfloxacin in pregnant women is not carried out, incl. for topical application in the form of drops).

Unknown, Do norfloxacin penetrates into the milk of nursing women. Upon receiving the nursing mothers in low doses norfloxacin (200 mg) Inside, it was not detected in breast milk. However, it should be taken into account, that other quinolone derivatives systemic action into breast milk and there is a potential risk of serious adverse reactions in children, breastfed. Nursing women should either stop breast-feeding, or receiving norfloxacin (Considering the importance of the drug to the mother), incl. for local action in the form of drops.

Side effects of norfloxacin

Systemic effects

From the digestive tract: decreased appetite, nausea, vomiting, bitter taste in the mouth (incl. After instillation into the eye), abdominal pain, diarrhea, increase in liver transaminases, Alkaline phosphatase, LDH; psevdomembranoznыy colitis (prolonged use).

With the genitourinary system: kristallurija, glomerulonephritis, dizurija, polyuria, albuminuria, giperkreatininemiя, Urethral bleeding.

From the nervous system and sensory organs: headache, dizziness, insomnia, hallucinations, fainting.

Cardio-vascular system and blood (hematopoiesis, hemostasis): tachycardia, irregular heartbeat, decrease in blood pressure, vasculitis, leukopenia, eozinofilija, decrease in hematocrit.

On the part of the musculoskeletal system: Tendinitis, tendon rupture, arthralgia.

Allergic reactions: itching, hives, swelling, Syndrome Stevens - Johnson.

Other: candidiasis.

When instillation into the eye: blurred vision, burning and pain in the eye, conjunctival hyperemia, xemoz, photophobia, allergic reactions.

Interaction of norfloxacin

Pharmacokinetic-simultaneous antatsidov, containing aluminum hydroxide or magnesium hydroxide, PM, containing iron, zinc and sucralfate slows absorption of norfloxacin (the time interval between their appointment should be at least 2-4 hours). Cnizhaet clearance of theophylline on 25% (while the application should decrease the dose of theophylline), increases serum concentration of anticoagulants, cyclosporine (mutually). Pharmacodynamic-co-administration with medicines, have the potential to reduce blood pressure, it can cause a sharp decrease; in such cases, and the simultaneous introduction of barbiturates and other drugs for general anesthesia, heart rate should be monitored, Blood pressure and ECG. The simultaneous use of medicines, lowering the seizure threshold, It can lead to the development of epileptiform seizures. Reduces the nitrofurans.

Overdose norfloxacin

Symptoms (3 d for 45 m): dizziness, nausea, vomiting, drowsiness, the appearance of a cold sweat (without major changes in hemodynamic indices), convulsions.

Treatment: gastric lavage, Adequate hydration therapy forced diuresis, appointment of symptomatic drugs. The specific antidote is absent.

Dosage and administration of norfloxacin

Inside, by 400 mg 2 once a day. Course duration depends on indication for use, severity of infection and the activity of the pathogen: in normal infections urinary tract within 7-10 days, neoslojnennom cystitis is 3-7 days, chronic recurrent urinary tract infection — to 12 Sun, in acute bacterial gastroenteritis is 5 days. In acute uncomplicated gonococcal infection — once 800 mg.

Patients with impaired renal function in Cl creatinine less than 30 ml / min and patients, hemodialysis, appointed 1/2 therapeutic dose 2 times a day or full dose 1 once a day.

Locally - 1-2 drops in the affected eye or ear 4 once a day. Depending on the degree of infection dose on the first day, maybe 1-2 drops every 2 no.

Precautions priprimenenii norfloxacin

Пролонгация интервала QT / torsades de pointes. There are rare reports of the development torsades de pointes during the post-marketing studies in patients, receiving quinolones, including norfloxacin. These rare cases are associated with the following factors: Age more 60 years, female, previous heart disease and / or the use of combination therapy. Norfloxacin should not be used in patients with known prolongation of the QT interval, when uncorrectable hypokalemia, and patients, receiving class IA antiarrhythmics (quinidine, prokaynamyd) or Class III (Amiodarone, sotalol).

Convulsions. It was reported on the development of seizures in patients, treated with norfloxacin. Patients, take other drugs of this class, It reported on the development of seizures, accompanied by increased intracranial pressure, and toxic psychosis. Quinolones may also cause central nervous system stimulation, leads to tremor, anxiety, light headedness, confusion, and hallucinations. When these reactions against the backdrop of norfloxacin should immediately remove the drug and conduct appropriate therapy.

The impact on the functioning of norfloxacin and the electrical activity of the brain has not been studied. Therefore, caution should be exercised in patients with diagnosed or suspected CNS diseases (incl. cerebral arteriosclerosis, epilepsy and other factors, predisposing to seizures) (cm. "Restrictions on the use").

Giperchuvstvitelynosty / anaphylaxis. Reported cases of serious hypersensitivity reactions (anaphylactoid and anaphylactic), when receiving the first dose of the quinolone. In some cases, these reactions are accompanied by cardiac collapse, loss of consciousness, swoon, swelling of the face or throat, dyspnoea, krapivnicej, zudom; Only a few patients had a history of hypersensitivity reactions. In the case of allergic reactions to the drug norfloxacin should be abolished. With the development of severe acute hypersensitivity reactions require immediate administration of epinephrine and carrying out related activities (oxygen, in / in a liquid, antihistamine drugs, corticosteroids and others.). Patients with hypersensitivity to norfloxacin systemic effects or other quinolones may be sensitive to norfloxacin and topical (in the form of drops).

Psevdomembranoznыy colitis. It is important to take into account the possibility of pseudomembranous colitis, If the intake of antibiotics in patients appear diarrhea. Treatment antibacterial agents leads to modification of the normal colonic flora, and can lead to increased growth of clostridia. Studies show, toxin seems to be built, produced Clostridium difficile, It is the primary cause of "antibiotic-associated colitis". If the diagnosis "pseudomembranous colitis" should start appropriate therapy.

Peripheral neuropathy. It was reported about rare cases of sensory or sensorimotor axonal polyneuropathy, motor, leading to paresthesia, gipestezii, dysesthesia and weakness in patients, taking quinolones, incl. norfloxacin. When the patient has symptoms of neuropathy, including pain, burning, pricking, numbness and / or weakness, fever and others., should stop taking norfloxacin.

Cases of tendon rupture shoulder, hands, Achilles tendon, require surgical treatment or leads to a prolonged disruption of limb function, patients, receiving quinolones, including norfloxacin. In postmarketing studies indicated an increased risk of tendon rupture in the background simultaneously receiving corticosteroids, especially in elderly patients. When the pain in joints and muscles, signs of inflammation or rupture of a tendon norfloxacin should be lifted immediately; the patient should be at rest and avoid stress to the complete exclusion of the diagnosis "tendinitis" or "tendon rupture". Tendon rupture is possible both during treatment quinolones (incl. norfloxacin), and after completion of treatment.

It will be appreciated, that norfloxacin is not indicated for the treatment of syphilis. Antimicrobial drugs, used in high doses over a short period of time for the treatment of gonorrhea, may mask or delay the symptoms of syphilis developing. All patients with gonorrhea is necessary to conduct a serological test for syphilis at the time of diagnosis, and again (through 3 Months) after the appointment of norfloxacin.

During the double-blind cross-over study with volunteers in order to compare the single dose norfloxacin and when receiving placebo 800 or 1600 mg norfloxacin (1-2 Recommended daily dose) some volunteers were found in the urine of needle-like crystals of substance, especially in alkaline urine. Although not expected to develop crystalluria under recommended dosing regimen (by 400 mg 2 once a day), during therapy requires norfloksacinom precautions patients should receive sufficient amounts of fluid to maintain the diuresis of at least 1.2-1.5 l/day in adults, and do not exceed the recommended dose.

When applying eye drops need to wear sunglasses. During treatment should avoid insolation. Patients, taking some quinolones, with excessive exposure to direct sunlight observed phototoxicity reactions. In the case of photosensitivity reactions norfloxacin therapy should be discontinued.

Khinolony, including norfloxacin, can exacerbate symptoms myastenia gravis and lead to life-threatening weakness of the respiratory muscles. Caution should be exercised when using quinolones, incl. NOR, patients myastenia gravis.

As with other antibacterials, norfloxacin with prolonged use can lead to increased growth of non-susceptible organisms, incl. mushrooms. In the case of superinfection is necessary to take appropriate action.

Unlikely, that the use of norfloxacin in the absence of confirmed or suspected bacterial infection or a prophylactic benefit to the patient, it increases the risk of developing drug resistance.

During the surgery requires monitoring of the blood coagulation system (During therapy may increase the prothrombin index).

During treatment norfloxacin must be careful when driving and occupation of potentially hazardous activities, require high concentration and speed of psychomotor reactions.

Interaction of norfloxacin