Norbactin tablets 400mg, No. 10

Treatment of infectious and inflammatory diseases caused by sensitive microorganisms, including:

• urinary tract infections;

• genital infections;

• uncomplicated gonorrhea;

• gastrointestinal infections;

• prevention of sepsis in patients with neutropenia;

• diarrhea of ??travelers.

Inside, on an empty stomach (at least 1 hour before or 2 hours after meals), drinking plenty of fluids.

In acute uncomplicated cystitis appoint 200-400 mg 2 times / day for 3-5 days.

In acute urinary tract infections - 400 mg 2 times / day for 7-10 days.

For recurrent or chronic recurrent urinary tract infections - 400 mg 2 times / day for 4 weeks and 400 mg / day for up to 12 weeks in case of relapse.

For genital infections - 400-600 mg 2 times / day for 7 days.

In acute uncomplicated gonococcal infection - 800 mg once.

For the prevention of sepsis in patients with neutropenia - 400 mg 3 times / day for 8 weeks.

In case of gastrointestinal tract infections - 400 mg 2 times / day for 3-5 days.

For the prevention of bacterial diarrhea in epidemically unfavorable areas - 400 mg 1 time / day.

In patients with impaired renal function with a Cl creatinine of more than 20 ml / min, correction of the dosage regimen is not required. When Cl creatinine is below 20 ml / min (or serum creatinine level is more than 5 mg / 100 ml) and patients on hemodialysis are prescribed 1/2 therapeutic dose 2 times a day or a full dose 1 time per day.

Each film-coated tablet contains:

Active ingredient: norfloxacin - 400 mg.

Excipients: microcrystalline cellulose 147.78 mg, croscarmellose sodium 25.00 mg, sodium lauryl sulfate 6.35 mg, corn starch 25.00 mg, colloidal silicon dioxide 8.00 mg, magnesium stearate 7.40 mg, purified talc 7, 35 mg.

Film shell: hypromellose 7.78 mg, macrogol - 400 1.82 mg, purified talc 2.07 mg, titanium dioxide 3.34 mg, purified water. *

* - lost in the production process.

• Hypersensitivity to norfloxacin or other drugs from the fluoroquinolone group;

• deficiency of glucose-6-phosphate dehydrogenase;

• cerebral atherosclerosis;

• violation of cerebral circulation;

• epilepsy, convulsive syndrome;

• renal / hepatic impairment;

• pregnancy;

• lactation period;

• children and adolescents (up to 18 years old).

Pharmacodynamics

Antimicrobial agent from the fluoroquinolone group. It has a bactericidal effect by inhibiting the bacterial enzyme DNA gyrase, which provides supercoiling and, thus, the stability of bacterial DNA. Destabilization of the DNA chain leads to the death of bacteria. Possesses a wide spectrum of antibacterial action. 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, Neisserria gonorrhoeae, Proteus mirabilis, Proteus vulgaris, Pseudomonas aeruginosa, Serratia marcescens.

Sensitive in vitro: gram-negative aerobes - Citrobacter diversus, Edwardsiella tarda, Enterobacter agglomerans, Haemophilus ducreyi, Klebsiella oxytoca, Morganella morganii, Providencia alcalifacients, Providencia stuartii, Pseudomonseudomonascens, Pseudomonseudomonascens, Pseudomonseudomonascens other, Ureaplasma urealyticum.

Inactive against obligate anaerobes.

Pharmokinetics

Absorption when taken orally - 20-40%, food reduces. The average maximum concentration (C max) when taking 200 mg, 400 mg, and 800 mg is 0.8 mg / ml, 1.5 mg / ml, 2.4 mg / ml, respectively. The time to reach the maximum concentration (T cm) in plasma is 1 hour. The effective half-life from plasma (T1 / 2) is 3-4 hours. The connection with plasma proteins is 10-15%. In the elderly, excretion is slowed down (due to age-related decrease in renal function), after oral administration of 400 mg, the average concentration in urine (AUC) is 6.97-12.63 mg h / ml and Cmax-1.25-2.79 ?g / ml (in young 6.4 mgh / ml and 1.5 ?g / ml, respectively), T1 / 2-4 hours. In chronic renal failure (CRF) (creatinine clearance less than 30 ml / min / 1.73 sq. m) T1 / 2 is extended to 6.5 hours It is well distributed in the body (renal parenchyma, ovaries, seminiferous tubule fluid, prostate gland, uterus, abdominal and pelvic organs, bile, breast milk). Penetrates the blood-brain barrier (BBB) ??and the placenta. It is slightly metabolized in the liver. It is excreted by the kidneys (renal clearance - 275 ml / min.), By glomerular filtration and tubular secretion. Within 24 hours from the moment of admission

26-32% of the dose is excreted by the kidneys unchanged, 5-8% - in the form of metabolites. Subsequently, 1% of the dose taken is excreted by the kidneys. About 30% of the dose taken is excreted in the bile. In the elderly, 22% of norfloxacin is excreted by the kidneys (renal clearance - 154 ml / min.)

2-3 hours after taking 400 mg orally, the concentration in the urine exceeds 200 ?g / ml, within 12 hours it is maintained above 30 ?g / ml. At pH 7.5, the solubility of norfloxacin decreases.

Overdose

Symptoms: dizziness, nausea, vomiting, drowsiness, cold sweat, puffy face without changes in basic hemodynamic parameters.

Treatment: gastric lavage, adequate hydration therapy with forced diuresis. Examination and observation in a hospital for several days is required. There is no specific antidote.

Side effects

From the digestive system: loss of appetite, bitterness in the mouth, nausea, vomiting, abdominal pain, pain in the rectum or anus, constipation, dyspepsia, flatulence, dryness of the oral mucosa, loose stools, ulceration of the oral mucosa, itching of the anus, spasms of smooth muscles of the gastrointestinal tract, diarrhea, heartburn, pseudomembranous colitis (with prolonged use), stomatitis, dysphagia.

From the endocrine system: pancreatitis, hypoglycemia.

From the liver and biliary tract: hepatitis, jaundice (including cholestatic jaundice), increased activity of 'hepatic' transaminases, liver failure (including fatal), liver necrosis.

On the part of the kidneys and urinary tract: renal failure, crystalluria, glomerulonephritis, dysuria, polyuria, albuminuria, urethral bleeding, hypercreatininemia, interstitial nephritis, candiduria, cylindruria, hematuria, renal colic, proteinuria.

On the part of the blood and lymphatic system: leukopenia, eosinophilia, decreased hematocrit and hemoglobin, neutropenia, thrombocytopenia, prolongation of prothrombin time (PT), hemolytic anemia associated with a deficiency of glucose-6-phosphate dehydrogenase, agranulocytosis.

Allergic reactions: anaphylaxis, angioedema, dyspnea, interstitial nephritis, arthralgia, vasculitis, shortness of breath, myalgia.

From the immune system: arthritis.

Musculoskeletal and connective tissue disorders: tendinitis, tendon ruptures, myalgia, exacerbation of myasthenia gravis, bursitis, swelling of the hands and feet.

From the nervous system: headache, dizziness, fainting, insomnia, hallucinations, depression, anxiety / nervousness, confusion, irritability, euphoria, nystagmus, disorientation, ringing in the ears, polyneuropathy, Guillain-Barre syndrome, paresthesia, psychotic reactions, convulsions , convulsions, tremors, myoclonus, peripheral neuropathy, ataxia, hypesthesia, tingling in the fingers, drowsiness, sleep disturbance.

From the side of the cardiovascular system: tachycardia, arrhythmias, postural hypotension, decreased blood pressure, myocardial infarction, palpitations, prolongation of the QT interval, ventricular arrhythmia, tachycardia of the 'pirouette' type.

Skin and subcutaneous tissue disorders: pruritus, urticaria, malignant exudative erythema (Stevens-Johnson syndrome), photosensitivity, exfoliative dermatitis, polymorphic erythema, rash, toxic epidermal necrolysis.

From the senses: dysgeusia, visual disturbances, blurred vision, hearing loss, tinnitus, diplopia, increased separation of lacrimal fluid (epiphora).

On the part of laboratory parameters: hyperglycemia, hypercholesterolemia, hyperkalemia, hypertriglyceridemia, an increase in the concentration of urea in the blood, an increase in the activity of creatinine phosphokinase.

Other: vaginal candidiasis, hyperhidrosis, asthenia, back pain, fever, chills, chest pain, dysmenorrhea, edema.

If any of the side effects indicated in the instructions are aggravated, or you notice any other side effects that are not indicated in the instructions, inform your doctor.

Special conditions

If it is necessary to prescribe norfloxacin during lactation, the question of stopping breastfeeding should be resolved.

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

During therapy with norfloxacin, an increase in the prothrombin index is possible.

When carrying out surgical interventions, the state of the blood coagulation system should be monitored.

Direct sunlight should be avoided during treatment with norfloxacin.

Norfloxacin, like other fluoroquinolones, can cause tendonitis and tendon rupture. Risk factors: age over 60 years, taking glucocorticosteroids (GCS), kidney, heart or lung transplantation, increased physical activity, chronic renal failure (CRF), a history of tendon damage (including rheumatoid arthritis). These phenomena can occur several months after the end of the drug intake.

If you experience pain in the tendons or at the first sign of tendovaginitis, it is recommended to cancel the drug and consult a doctor.

Norfloxacin can lower the seizure threshold and cause seizures; fluoroquinolones can also stimulate the central nervous system, causing tremors, toxic psychosis, anxiety, confusion and hallucinations, and increased intracranial pressure.

Norfloxacin can lead to the development of pseudomembranous colitis caused by Clostridium difficile. In this case, it is necessary to discontinue the drug and prescribe appropriate treatment (oral vancomycin or metronidazole).

The drug is not effective for syphilis.

Norfloxacin can cause peripheral neuropathy (paresthesia, hypoesthesia, dysesthesia, muscle weakness). At the first signs of neuropathy (pain, tingling, numbness or weakness in the limbs, impaired other types of sensitivity), the drug should be canceled in order to avoid irreversible changes.

In order to avoid the formation of crystals of norfloxacin in the kidneys, do not exceed the recommended doses, it is necessary to drink the tablets with a sufficient amount of liquid.

Influence on the ability to drive vehicles, mechanisms:

Due to the possible occurrence of dizziness, patients taking norfloxacin should be careful when driving a car and engaging in other potentially hazardous activities that require increased attention and speed of psychomotor reactions.

Drug interactions

The simultaneous intake of antacids containing aluminum or magnesium hydroxide, as well as preparations containing iron, zinc, sucralfate, as well as multivitamins, reduces the absorption of norfloxacin (the interval between their appointment should be at least 4 hours).

Reduces the clearance of theophylline by 25%, therefore, with simultaneous use, the dose of theophylline should be reduced.

Norfloxacin reduces hepatic metabolism by inhibiting the isoenzyme CY1A2, which can lead to an increase in the concentration of its substrates in the blood (including caffeine, clozapine, ropinirole, tacrine, theophylline, tizanidine).

Didanosine should not be administered concomitantly with any fluoroquinolone, since concurrent use of didanosine may reduce the absorption of fluoroquinolones.

Parallel use of probenecid reduces the renal tubular secretion of fluoroquinolones, leading to a decrease in urinary excretion of fluoroquinolones, prolongs

elimination half-life and increases the risk of toxicity.

Concomitant use of norfloxacin with drugs that have the potential to lower blood pressure (BP) can cause a sharp decrease. In this regard, in such cases, as well as with the simultaneous administration of barbiturate-containing anesthetics, the heart rate, blood pressure, and electrocardiogram (ECG) indicators should be monitored.

Fluoroquinolones in combination with fenbufen can lead to convulsions, therefore quinolones and fenbufen should be avoided together.

Combining warfarin with norfloxacin increases the anticoagulant effect of warfarin, increasing the likelihood of bleeding.

Simultaneous use with drugs that lower the seizure threshold can lead to the development of epileptiform seizures.

Increases the concentration of indirect anticoagulants, cyclosporine (mutually) in the blood serum.

Reduces the effect of nitrofurans.