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

Excipients (core): lactose monohydrate (milk sugar) - 85,0 mg, microcrystalline cellulose - 98,0 mg, croscarmellose sodium - 37,0 mg, water - 10,0 mg, povidone-K25 - 24.0 mg, magnesium stearate - 6,0 mg.

Auxiliary substances (shell): hypromellose 11.0 mg, macrogol 4000 to 3.0 mg, titanium dioxide 6.0 mg.

Description:

Round biconvex tablets with a risk on one side, covered with a film shell of white or almost white color, on the fracture are visible two layers - the core from white to light yellow color and a film shell.

Pharmacotherapeutic group:antimicrobial agent - fluoroquinolone

ATX: & nbsp

S.01.A.E.02 Norfloxacin

Pharmacodynamics:

Antimicrobial agent from the group of fluoroquinolones. Has a bactericidal effect. The bacterial DNA enzyme acts on the bacterial enzyme, which ensures super-convoliation and, thus, the stability of bacterial DNA. The destabilization of the DNA chain leads to the death of bacteria. Has a broad spectrum of antibacterial action and is active against most strains of microorganisms, both in conditions in vitro, and in vivo.

Sensitive in vivo: Gram-positive aerobes - Enterococcus faecalis, Staphylococcus aureus, Staphylococcus epidermidis, Staphylococcus saprophyticus, Streptococcus agalactiae; gram-negative aerobes - Citrobacter freundii, Enterobacter aerogenes, Enterobacter cloacae, Escherichia coli, Klebsiella pneumoniae, Neisseria gonorrhoeae, Proteus mirabilis, Proteus vulgaris, Pseudomonas aeruginosa, Serratia marcescens, Salmonella spp., Shigella spp. Sensitive in vitro: gram-negative aerobes - Citrobacter diversus, Edwardsiella tarda, Enterobacter agglomerans, Haemophilus ducreyi, Klebsiella oxytoca, Morganella morganii, Providencia alcalifaciens, Providencia rettgeri, Providencia stuartii, Pseudomonas fluorescens, Pseudomonas stutzeri; other - Ureaplasma urealyticum.

Inactive with obligate anaerobes

Pharmacokinetics:

Absorption of norfloxacin for oral administration - rapid; bioavailability - 30-40%; food slows the absorption of the drug, but does not change the maximum concentration and bioavailability.

The maximum plasma concentrations are achieved in 1-2 hours and range from 0.8 to 2.4 μg / ml depending on the dose (200-800 mg). Low valuebinding of norfloxacin to plasma proteins (10-15%) and high solubility in lipids cause a large volume of drug distribution and good penetration into organs and tissues (renal parenchyma, ovaries, seminal tubular fluid, prostate, uterus, abdominal and pelvic organs, bile, mother's milk). Penetrates through the blood-brain barrier and the placenta. Metabolised in the liver. Kidney clearance - 275 ml / min. Within 24 hours, 26-32% is excreted by the kidneys in unchanged form, 5-8% in the form of a weakly active metabolite. In the subsequent kidneys, less than 1% of the dose taken is excreted. 30% is excreted by the intestine. In elderly patients, 22% of norfloxacin is excreted by the kidneys (renal clearance - 154 ml / min).

After 2-3 hours after taking 400 mg, the urine concentration exceeds 200 μg / ml, for 12 hours it is maintained above 30 μg / ml. At pH 7.5, the solubility of norfloxacin is reduced.

Indications:

Infectious-inflammatory diseases caused by microorganisms sensitive to norfloxacin: urinary tract infections (except acute and chronic complicated pyelonephritis), chronic bacterial prostatitis, uncomplicated gonorrhea, salmonellosis, shigellosis.

Prevention of travelers' diarrhea, prevention of sepsis in patients with neutropenia.

Contraindications:

- hypersensitivity to norfloxacin, the components of the drug and other quinolones;

- deficiency of glucose-6-phosphate dehydrogenase;

- tendonitis, tendon rupture caused by fluoroquinolones (including in the anamnesis);

- hereditary lactose intolerance, lactase deficiency or glucose-galactose malabsorption;

- children and adolescence (up to 18 years);

- pregnancy and lactation.

Carefully:

Cerebral atherosclerosis, cerebral blood flow (history), epilepsy, organic central nervous system disorders, predisposition to convulsive reactions, psychosis and other mental disorders a history of renal / hepatic failure, myasthenia gravis, hepatic porphyria, diabetes mellitus, congenital lengthening interval syndrome QT, heart disease (heart failure, myocardial infarction, bradycardia), electrolyte imbalance (e.g., hypokalemia, hypomagnesemia), advanced age in women, simultaneous medicaments interval prolonging QT (antiarrhythmic agents IA and class III, tricyclic and tetracyclic antidepressants,neuroleptics, macrolides, antifungal, imidazole derivatives, some antihistamines, including. astemizole, terfenadine, ebastine), means for general anesthesia from the barbiturate group; medicines that reduce blood pressure.

Pregnancy and lactation:

Safety of use during pregnancy and lactation is not known. The drug is contraindicated during pregnancy. If it is necessary to prescribe the drug during lactation, breastfeeding should be stopped.

Dosing and Administration:

Inside on an empty stomach (at least 1 hour before or 2 hours after eating) and drink down with a sufficient amount of liquid.

In the absence of special doctor's instructions, the following doses are recommended: 1 tablet (400 mg) 2 times a day. Duration of treatment is from 7 to 14 days, if necessary, spend a longer treatment.

With infections of the urinary tract - 400 mg 2 times a day, for 7-10 days; with uncomplicated cystitis - 3-7 days; with a chronic recurrent urinary tract infection - up to 12 weeks; with acute bacterial gastroenteritis (shigellosis, salmonellosis) - 5 days; with acute gonococcal urethritis, pharyngitis, proctitis, cervicitis - once 800 mg.For the prevention of infections (in patients with neutropenia) - 400 mg 2 times a day; for the prevention of bacterial gastroenteritis - 400 mg / day. To prevent traveler's diarrhea - 400 mg / day for 1 day before departure and during the entire period of the trip (no more than 21 days). To prevent recurrence of urinary tract infections - 200 mg / day. With bacterial prostatitis (acute and chronic) - 400 mg 2 times a day for 28 days.

In patients with impaired renal function with creatinine clearance (CK) of more than 30 ml / min, correction of the dosing regimen is not required. When QC is below 30 ml / min and patients on hemodialysis, 1/2 therapeutic dose is administered 2 times a day or a full dose 1 time per day.

Side effects:

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

From the digestive system: nausea, abdominal pain, anorexia, diarrhea, pain in the rectum or anus, constipation, indigestion, flatulence, vomiting, dryness of the oral mucosa, heartburn, loose stool, bitter taste in the mouth, ulceration of the oral mucosa, itching of the anus.

On the part of the organs of hematopoiesis: leukopenia, thrombocytopenia, eosinophilia, neutropenia.

From the skin: itching, rash, erythema, urticaria.

From the sense organs: blurred vision.

From the side of the musculoskeletal system: Bursitis, swelling of the hands and feet.

From the cardiovascular system: myocardial infarction, palpitation.

From the urinary system: renal colic.

Laboratory indicators: increased activity of "hepatic" transaminases (alanine aminotransferase, aspartate aminotransferase, alkaline phosphatase, lactadehydrogenase), proteinuria, decreased hematocrit and hemoglobin, increased urea concentration in the blood, hypercreatininaemia, glucosuria.

Other: hyperhidrosis, asthenia, back pain, fever, chills, chest pain, dysmenorrhea swelling, allergic reactions, fatigue.

Postmarketing experience.

From the nervous system: convulsions, myoclonia, tremor, peripheral neuropathy, Guillain-Barre syndrome, ataxia, paresthesia, hypesthesia, mental disorders (including confusion), irritability, a sense of fear.

Allergic reactions: anaphylactic / anaphylactoid reactions, angioedema, dyspnea, vasculitis, urticaria.

From the skin: toxic epidermal necrolysis, Stevens-Johnson syndrome, erythema multiforme, exfoliative dermatitis, photosensitivity, leukocytoclastic vasculitis, drug rash with eosinophilia and systemic symptoms (DRESS-syndrome).

From the digestive system: pseudomembranous colitis, hepatitis, cholestatic jaundice, pancreatitis, stomatitis, hepatic insufficiency (including fatal outcome).

From the side of the cardiovascular system: interval lengthening QT, ventricular arrhythmia, incl. tachycardia of the "pirouette" type.

From the urinary system: an increase in urea in the plasma, interstitial nephritis, kidney failure.

From the side of the musculoskeletal system: arthritis, arthralgia, myalgia, tendonitis, tendon rupture, exacerbation of myasthenia gravis gravis, increased activity of creatine phosphokinase, muscle spasms.

From the hematopoiesis: agranulocytosis, hemolytic anemia.

From the sense organs: hearing loss, tinnitus, diplopia, dysgeusia.

Other side effects of quinolones: agranulocytosis, albuminuria, candiduria, crystalluria,Cylindyria, dysphagia, hyperglycemia, hypercholesterolemia, hyperkalemia, hypertriglyceridemia, hematuria, liver necrosis, hypoglycemia, nystagmus, postural hypotension, prolongation of prothrombin time, candidiasis of the vagina.

Overdose:

Symptoms: nausea, vomiting, diarrhea, dizziness, drowsiness, "cold" sweat, cramps, puffy face.

Treatment: gastric lavage, adequate girdatsionnaya therapy with forced diuresis and symptomatic therapy. Required examination and observation in the hospital for several days. There is no specific antidote.

Interaction:

With the simultaneous use of norfloxacin and theophylline, the concentration of theophylline in the blood plasma should be monitored and its dose adjusted, since norfloxacin reduces the clearance of theophylline by 25%.

Reduces the effect of nitrofurans.

Norfloxacin can enhance the therapeutic effect of cyclosporine and indirect anticoagulants, in some cases, with the use of norfloxacin with cyclosporine, there has been an increase in the concentration of creatinine in the blood plasma, so these patients need control of this index, as well as plasma concentrations of cyclosporine.

The simultaneous use of norfloxacin and antacid agents containing aluminum or magnesium hydroxide, as well as preparations containing ions of iron, zinc, sucralfate, leads to a decrease in the absorption of norfloxacin (the interval between their intake should be at least 2 hours).

Simultaneous use with medications (including non-steroidal anti-inflammatory drugs) that reduce the convulsive threshold may lead to the development of seizures.

Simultaneous use with glucocorticosteroids may increase the risk of developing tendonitis or cases of rupture of tendons.

Norfloxacin can enhance the therapeutic effect of hypoglycemic drugs (sulfonylureas), and therefore, it is necessary to monitor the concentration of glucose in the blood plasma.

Simultaneous use of norfloxacin with drugs that have the potential to lower blood pressure can cause a sharp decrease in it. In this regard, in such cases, as well as with simultaneous administration with barbiturates and other drugs for general anesthesia, it is necessary to control the heart rate, blood pressure and ECG parameters.

Norfloxacin in vitro inhibits isoenzyme CYP1A2, which can lead to an increase in the concentration of its substrates in the blood plasma (including caffeine, clozapine, ropinirole, tacrine, theophylline, tizanidine), and therefore, it is necessary to monitor patients taking simultaneously with norfloxacin these drugs.

Probenecid can reduce the excretion of norfloxacin.

With simultaneous use with drugs that extend interval QT, perhaps more pronounced elongation of the latter.

Special instructions:

In some cases, after the first use of the drug may develop hypersensitivity reactions (anaphylactic / anaphylactoid reactions), which should immediately inform the doctor. Very rarely even after the first use of the drug, anaphylactic reactions can progress to a life-threatening anaphylactic shock. In these cases, treatment with norfloxacin should be discontinued and immediately begin the necessary medical measures (including anti-shock).

During treatment with norfloxacin, patients should receive a sufficient amount of fluid (under the control of diuresis).

During the period of therapy, an increase in the prothrombin index is possible (during surgical interventions it is necessary to monitor the state of the blood coagulation system).

During treatment with norfloxacin, exposure to ultraviolet rays should be avoided. direct sunlight.

Norfloxacin, like other fluoroquinolones, can cause tendonitis and tendon rupture. Risk factors: age over 60, glucocorticosteroids, kidney, heart or lung transplantation, increased physical activity, chronic renal failure, history of tendon damage (including rheumatoid arthritis). These phenomena can occur and a few months after completion of the drug. When pain occurs in the tendons or at the first signs of tendovaginitis, it is necessary to cancel the drug and consult a doctor. During therapy with norfloxacin it is recommended to avoid excessive physical exertion. Norfloxacin can reduce the threshold of convulsive alertness and cause seizures; fluoroquinolones can also stimulate the central nervous system, causing tremors, toxic psychoses, anxiety, confusion and hallucinations; increased intracranial pressure. In case of seizures, the drug should be discontinued.

Norfloxacin can lead to the development of pseudomembranous colitis caused by Clostridium difficile. In this case, it is necessary to cancel the drug and appointappropriate treatment (including use, vancomycin inwards or metronidazole). Drugs that inhibit the intestinal peristalsis are contraindicated.

When using norfloxacin, cases of development of cholestatic hepatitis were reported. The patient should be informed that if symptoms of liver dysfunction (anorexia, jaundice, darkening of the urine, pruritus, abdominal pain) appear, you should consult a doctor before continuing with norfloxacin treatment.

Not effective with syphilis.

In patients treated with quinolones, including norfloxacin, cases of sensory or sensorimotor axonal polyneuropathy, affecting small and / or large axons, are described and lead to paresthesia, hypostasis, dysesthesia and weakness. Symptoms may appear soon after the onset of use and be irreversible. Patients undergoing treatment with norfloxacin should be warned of the need to seek immediate medical attention in the event of symptoms of neuropathy, including pain, burning, stinging, numbness, weakness, or other sensitivity disorders, including tactile,pain, temperature, vibration sensitivity and sense of position (see section "Side effect"), Norfloxacin must be immediately canceled.

To avoid the formation of crystals, norfloxacin in the kidney should not exceed the recommended doses; it is necessary to drink tablets with a sufficient amount of liquid.

Effect on the ability to drive transp. cf. and fur:

Care must be taken when driving a car and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Form release / dosage:

Film-coated tablets 400 mg.

Packaging:

For 10, 20 tablets in a contour mesh box made of polyvinylchloride film and aluminum foil printed lacquered.

By 5, 10, 20, 30, 40, 50 or 100 tablets in cans of polymer from polypropylene or cans of polyethylene terephthalate.

One jar or 1, 2, 3, 4, 5 or 10 contour mesh packages together with the instruction for use are placed in a cardboard package (bundle).

Storage conditions:

In the dark place at a temperature of no higher than 25 ° C. Keep out of the reach of children.

Shelf life:

3 years.Do not use the drug after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:LP-002653

Date of registration:09.10.2014

The owner of the registration certificate:ATOLL, LLC ATOLL, LLC Russia

Manufacturer: & nbsp

OZONE, LLC Russia

Information update date: & nbsp09.08.2015

Illustrated instructions

Instructions

Norfloxacin (Norfloxacin)