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

film sheath: [hypromellose 9,000 mg, giprolose (hydroxypropyl cellulose) 3,490 mg, talc 3,470 mg, titanium dioxide 1,956 mg, iron oxide yellow (iron oxide) 0.084 mg] or [dry film coating mixture containing hypromellose (50%) , giprolose (hydroxypropylcellulose) (19.4%), talc (19.26%), titanium dioxide (10.87%), iron oxide yellow (iron oxide) (0.47%)] - 18,000 mg.

Description:Round biconvex tablets, covered with a film coating of yellow color. On the cross section, the core is light yellow in color.

Pharmacotherapeutic group:Antimicrobial agent - fluoroquinolone.

ATX: & nbsp

S.01.A.E.02 Norfloxacin

Pharmacodynamics:

Antibacterial 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 wide range of antibacterial action.

Active in vitro and in vivo in relation to the following microorganisms: 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 pneumonia, Neisseria gonorrhoeae, Proteus mirabilis, Proteus vulgaris, Pseudomonas aeruginosa, Serratia marcescens, Salmonella spp., Shigella spp. Active in vitro in relation to the following microorganisms: 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:

Norfloxacin rapidly, but not completely (30-40%) is absorbed after administration. Food slows the absorption of the drug. The maximum concentration in blood plasma is achieved after 1-2 hours and is from 0.8 to 2.4 μg / ml, depending on the dose.

The low binding 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 cavity and small pelvis, bile breast milk). Penetrates through blood-brain and placental barriers.

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

It is metabolized to an insignificant degree in the liver.

The elimination half-life is 3-4 hours. It is excreted by the kidneys through glomerular filtration and tubular secretion. Within 24 hours after receiving 32% of the dose is excreted by the kidneys unchanged, 5-8% - in the form of metabolites, about 30% of the dose is allocated with bile.

Indications:

Infectious-inflammatory diseases caused by pathogens sensitive to norfloxacin:

- urinary tract infections, including chronic relapsing (except for acute and chronic complicated pyelonephritis);

- chronic bacterial prostatitis;

- gonorrhea uncomplicated;

- bacterial gastroenteritis (salmonellosis, shigellosis);

- prevention of sepsis in patients with neutropenia;

- prevention of travelers' diarrhea.

Contraindications:

- increased sensitivity to norfloxacin, components of the drug and other drugs of the quinolone group;

- tendonitis, tendovaginitis, tendon ruptures associated with the intake of fluoroquinolones, including in the anamnesis;

- myasthenia gravis;

- deficiency of glucose-6-phosphate dehydrogenase;

- pregnancy and the period of breastfeeding;

- age to 18 years.

Carefully:

- atherosclerosis of cerebral vessels;

- age over 60 years;

- simultaneous reception glucocorticosteroid drugs, drugs, lengthening interval QT (antiarrhythmic drugs IA and III classes, tricyclic and tetracyclic antidepressants, neuroleptics, macrolides, antifungals, imidazole derivatives, some antihistamines, astemizole, terfenadine, ebastine);

- condition after kidney, heart, lung transplantation;

- disturbance of cerebral circulation (in anamnesis);

- organic diseases of the central nervous system;

- mental abnormalities in the anamnesis;

- epilepsy, epileptic syndrome;

- renal / hepatic impairment;

- hepatic porphyria;

- diabetes;

- congenital lengthening syndrome QT;

- heart disease (heart failure, myocardial infarction, bradycardia); electrolyte imbalance (eg, hypokalemia, hypomagnesemia);

- among women;

- simultaneous reception of barbiturates and medicines for general anesthesia;

- simultaneous administration of drugs that lower blood pressure.

Pregnancy and lactation:

The safety of use during pregnancy and during breastfeeding has not been studied. The drug is contraindicated in pregnancy. If it is necessary to prescribe the drug during breastfeeding, breastfeeding should be stopped.

Dosing and Administration:

Inside, on an empty stomach (not less than 1 hour before or 2 hours after eating), squeezed with enough liquid.

With infections of the urinary tract: 400 mg twice a day for 7-10 days, in case of a complicated infection, 10-21 days.

In acute uncomplicated cystitis: 400 mg twice a day for 3-7 days.

With a chronic recurrent urinary tract infection: 400 mg twice a day for up to 12 weeks, with the possibility of reducing the dose to 400 mg per day in 4 weeks from the start of therapy with sufficient antibacterial efficacy.

With chronic bacterial prostatitis: 400 mg twice a day for 4 weeks.

With bacterial gastroenteritis (shigellosis, salmonellosis): 400 mg twice a day for up to 5 days.

To prevent travelers' diarrhea: on 400 mg a day for 1 day before departure, during all time of travel (no more than 21 the day).

For the prevention of sepsis in neutropenia: 400 mg twice a day for up to 8 weeks.

With uncomplicated gonorrhea: once 800 mg.

Patients with impaired renal function with a clearance of creatinine of more than 30 ml / min, correction of the dosing regimen is not required.

When the creatinine clearance is less than 30 ml / min (or the serum creatinine level is more than 5 mg / 100 ml) and patients on hemodialysis are given a full one-time dose (400 mg) once a day.

Side effects:

From the digestive system: loss of appetite, dyspepsia, nausea, vomiting, abdominal pain, anorexia, diarrhea, constipation, pain in the rectum or anus, flatulence, dryness of the oral mucosa, heartburn, bitter taste in the mouth, ulceration of the oral mucosa, itching of the anus,pseudomembranous colitis (with prolonged use), hepatitis, jaundice, including cholestatic, pancreatitis, stomatitis, hepatic insufficiency (including fatal outcome).

From the urinary system: renal colic, glomerulonephritis, dysuria, polyuria, urethral bleeding, interstitial nephritis, renal failure.

From the nervous system: headache, dizziness, ataxia, fainting sleeplessness, hallucinations, peripheral neuropathy, tingling sensation, hypoesthesia, mental disorders (including confusion), drowsiness, anxiety, depression, sleep disorders, convulsions, myoclonia, tremor, Hyenna syndrome -Barre, fatigue, anxiety, irritability, a sense of fear, paresthesia.

From the cardiovascular system: myocardial infarction, tachycardia, arrhythmias, ventricular arrhythmia, including "pirouette" type, lowering of arterial pressure, vasculitis, lengthening of the interval QT.

From the musculoskeletal system: arthralgia, tendinitis, tendon ruptures (usually in the case of a combination with contributing factors), bursitis, swelling of the hands and feet, exacerbation of myasthenia, muscle spasm.

On the part of the hematopoiesis system: eosinophilia, leukopenia, neutropenia, thrombocytopenia, agranulocytosis, hemolytic anemia.

Allergic reactions: anaphylactoid reactions, rash, itching, urticaria, swelling, angioedema, dyspnea, vasculitis, arthritis, arthalgia, myalgia, toxic epidermal necrolysis, leukocytoclastic vasculitis, drug rash with eosinophilia and systemic symptoms (DRESS-syndrome).

From the skin: malignant exudative erythema (Stevens-Johnson syndrome), erythema multiforme, exfoliative dermatitis, photosensitivity.

Laboratory indicators: increased activity of "liver" transaminases,

alkaline phosphatase, lactate dehydrogenase, creatine kinase; proteinuria; decrease in hematocrit and hemoglobin; increased urea concentration in the blood, hypercreatinemia, glucosuria, crystalluria, albuminuria.

From the sense organs: blurred vision, loss / loss of hearing, tinnitus, diplopia, dysgeusia.

Other: pain in the back, chest pain, dysmenorrhea, fever, candidiasis, including the vagina, hyperhidrosis, asthenia, edema, erythema, chills.

Other side effects of quinolones: albuminuria, candiduria, Cylinderia, dysphagia, hyperglycemia, hypercholesterolemia, hyperkalemia, hypertriglyceridemia, hematuria, liver necrosis, hypoglycemia, nystagmus, postural hypotension, prolongation of prothrombin time.

Overdose:

Symptoms: In case of an overdose, the following symptoms may occur: nausea, vomiting, diarrhea; in severe cases - dizziness, drowsiness, "cold" sweat, cramps, puffy face without changing the basic hemodynamic indications.

Treatment: gastric lavage, adequate hydration therapy with forced diuresis and symptomatic therapy. It requires a survey 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%, and the development of corresponding undesirable side effects can occur.

Simultaneous use of norfloxacin and drugs that cause lengthening of the interval QT (eg, cisapride, tricyclic and tetracyclic antidepressants, antiarrhythmics IA and III classes, antipsychotics,macrolides, antifungal drugs, imidazole derivatives, some antihistamines, including anti- astemizole, thoserfenadine, ebastine and others), should under careful medical supervision.

Norfloxacin reduces the effect of nitrofurans.

Norfloxacin can enhance the therapeutic effects of cyclosporine and warfarin. In some cases, with the use of norfloxacin with cyclosporine, there was an increase in the serum creatinine concentration, therefore, such patients need control of this index.

The simultaneous use of norfloxacin and antacid agents containing aluminum or magnesium hydroxide, as well as preparations containing iron, zinc (including multivitamins), sucralfate, didanosine (tablets and oral solution for children), reduces the absorption of norfloxacin (the interval between their intake should be less than 2 hours).

Simultaneous use with drugs that reduce the threshold of convulsive readiness (incl.with non-steroidal anti-inflammatory drugs), can lead to the development of seizures.

Norfloxacin in vitro inhibits CYP1A2, which can lead to an increase in the concentration of its substrates in the blood (for example, caffeine, clozapine, ropinirole, Tacrine, theophylline, tizanidine).

The simultaneous use of norfloxacin with glucocorticosteroids may increase the risk of tendonitis and cases of rupture of tendons. Norfloxacin can enhance the therapeutic effect of hypoglycemic drugs (sulfonylurea derivatives). With simultaneous admission with glibenclamide, the development of severe hypoglycemia is possible.

Probenecid can reduce the excretion of norfloxacin.

Simultaneous reception 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 indices electrocardiograms.

Special instructions:

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

To avoid the formation of crystals, norfloxacin in the kidney should not exceed the recommended doses.

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 direct sunlight should be avoided.

Norfloxacin, like other fluoroquinolones, can cause tendonitis and tendon ruptures, especially if there are the following risk factors: age over 60 years, glucocorticosteroids, kidney, heart or lung transplantation, increased physical activity, chronic renal failure, tendon lesions in the anamnesis including rheumatoid arthritis). These phenomena can occur and a few months after completion of the drug. At the first signs of tendonitis or rupture of the tendon, you should stop taking norfloxacin and consult a doctor.

During therapy with norfloxacin it is recommended to avoid excessive physical exertion.

Norfloxacin can reduce the threshold of convulsive readiness and cause seizures. In case of seizures, the drug is discontinued.

Fluoroquinolones can also stimulate the central nervous system, causing tremors, toxic psychoses, anxiety, confusion and hallucinations, increased intracranial pressure.

Norfloxacin is not effective in syphilis.

The use of norfloxacin can lead to the development of pseudomembranous colitis caused by Clostridium difficile. In this case, it is necessary to cancel the drug and prescribe the appropriate treatment (use of vancomycin inwards or metronidazole). Contraindicated use of drugs that inhibit intestinal peristalsis.

In patients who use fluoroquinolones, including norfloxacin, cases of sensory and sensorimotor axonal polyneuropathy affecting small and (or) large axons are recorded, leading to paresthesia, hypostasis, dysesthesia and weakness. Symptoms may appear soon after the onset of use and be irreversible. If the patient develops symptoms of neuropathy, including pain, burning, tingling,numbness and / or weakness or other sensitivity disorders, including tactile, pain, temperature, vibration sensitivity and a sense of position, norfloxacin must be immediately canceled. 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.

In some cases, after the first use of the drug may develop hypersensitivity and allergic 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 abolished and the necessary medical measures (including anti-shock).

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.Consideration should be given to the potential for the development of side effects such as dizziness, drowsiness, and visual impairment. When these undesirable phenomena appear, one should refrain from performing these activities.

Form release / dosage:

Tablets, film-coated, 400 mg.

Packaging:

5, 10 or 20 tablets in a contour cell box made of a polyvinylchloride film and aluminum foil.

10 or 20 tablets in a can of high-density polyethylene.

2 or 4 contourcell packs of 5 tablets, 1 or 2 contour packs of 10 tablets, 1 circuit pack of 20 tablets, or one bank, along with instructions for medical use in a pack of cardboard.

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 after expiry date.

Terms of leave from pharmacies:On prescription

Registration number:LP-002563

Date of registration:05.08.2014

The owner of the registration certificate:VERTEKS, AO VERTEKS, AO Russia

Manufacturer: & nbsp

VERTEKS, AO Russia

Information update date: & nbsp09.08.2015

Illustrated instructions

Instructions

Norfloxacin (Norfloxacin)