Instructions for Norfloxacin
Norfloxacin Pharmacological properties:
Norfloxacin (1-ethyl-6-fluoro-1,4-dihydro-4-oxo-7- (1-piperazinyl) -3-quinolinecarboxylic acid) is an antibacterial agent of the fluoroquinolone group. Acts bactericidal, suppressing DNA gyrase, disrupts the process of DNA supercoiling. Active against most gram-negative bacteria - Escherichia coli, Salmonella spp., Shigella spp., Proteus spp., Morganella morganii, Klebsiella spp . (including Klebsiella pneumoniae ), Enterobacter spp., Serratia spp., Citrobacter spp., Yersinia spp., Providencia spp., Haemophilus influenzae, Pseudomonas spp . (including Pseudomonas aeruginosa ), Neisseria gonorrhoeae, Neisseria meningitidis, Brucella spp., Vibrio spp... Active against gram-positive microorganisms ( Staphylococcus spp., Staphylococcus pneumoniae, Staphylococcus epidermidis, Staphylococcus aureus), methicillin-resistant, Enterococcus faecalis . Norfloxacin is active against β-lactamase-producing bacteria. Anaerobic bacteria are insensitive to norfloxacin, Enterococcus spp. Is insensitive .
Food intake reduces the rate of absorption, when taken orally, about 30-40% is absorbed norfloxacin. Plasma protein binding is 14%. The maximum concentration in the blood is reached within 1-3 hours after taking the drug, depending on the prescribed dose. Norfloxacin accumulates in peripheral tissues; It penetrates well into the tissues of the gallbladder, bile ducts, liver, kidneys, prostate gland, female genital organs. High concentrations of the drug are also detected in the mucous membrane of the bronchi, bronchial secretions and in the pleural fluid. Penetrates the placenta. Does not penetrate the BBB. The half-life is 3-6 hours. Norfloxacin undergoes biotransformation in the liver with the formation of metabolites, which are excreted in the urine in unconjugated form; some of the metabolites have microbiological activity (less pronounced than that of norfloxacin). Metabolites are not detected in blood serum and are detected in bile, feces and urine (approximately in the same proportion). Urinary excretion of norfloxacin metabolites is less than 10% of the dose taken. About 30% is excreted in the urine unchanged.
Indications Norfloxacin:
Infectious and inflammatory diseases caused by microorganisms sensitive to Norfloxacin:
infections of the ear
throat
nose
respiratory tract
gastrointestinal tract (salmonellosis, shigellosis, dysentery, cholera, typhoid fever)
abdominal organs (including the small pelvis)
acute and chronic infections of the genitourinary tract (pyelonephritis
cystitis
urethritis
prostatitis
cervicitis
endometritis)
infections of the skin and soft tissues
bones and connective tissue
gynecological infections
uncomplicated gonorrhea
prevention of infections in patients with granulocytopenia
Application Norfloxacin:
The dosage regimen is determined individually. Norfloxacin is administered orally 1 hour before meals or 2 hours after meals with a glass of water. For urinary tract infections - 400 mg 2 times a day for 7-10 days;
with uncomplicated cystitis - 3-7 days;
with chronic recurrent urinary tract infection - up to 12 weeks, if the effect is achieved during the first 4 weeks, then the dose is reduced to 400 mg / day. In acute bacterial gastroenterocolitis - 5 days; with acute gonococcal urethritis, pharyngitis, proctitis, cervicitis - 800 mg once;
with typhoid fever - 400 mg 3 times a day for 14 days.
For the prevention of recurrence of urinary tract infections - 200 mg / day for 4-6 weeks. In patients with impaired renal function with creatinine clearance of more than 20 ml / min, no dosage adjustment is required.1 / 2 r erapevticheskoy dose 2 times a day, or one full dose once a day. In order to prevent infections in patients with granulocytopenia, the drug is prescribed at a dose of 400 mg every 8 hours. The duration of treatment is set individually. The average daily dose for adults and children over 15 years of age is 800 mg / day. The maximum daily dose is 1600 mg.
Contraindications:
Hypersensitivity to quinolones
age up to 15 years
pregnancy and lactation
liver failure
glucose-6-phosphate dehydrogenase deficiency
cerebral atherosclerosis
cerebrovascular accident
epilepsy
epileptiform syndrome of various etiologies
Norfloxacin Side effects:
Norfloxacin is generally well tolerated. The overall incidence of side effects is approximately 5%. With prolonged use or prescribing the drug in the maximum daily dose, gastrointestinal disorders (bitter taste in the mouth, nausea, diarrhea, anorexia, pseudomembranous enterocolitis), increased activity of hepatic transaminases, disorders of the cardiovascular system (tachycardia, arrhythmia, decreased blood pressure, fainting), disorders of the central nervous system (headache, dizziness, insomnia or drowsiness), disorders of the urinary system (crystalluria, glomerulonephritis, dysuria, polyuria, albuminuria, urethral bleeding, hypercreatinemia), disorders of the musculoskeletal system (myalgia , arthralgia, tendinitis), from the hematopoietic organs (leukopenia, eosinophilia, decreased hematocrit,
special instructions:
Adequate diuresis should be maintained during treatment. When treating with Norfloxacin, an increase in the prothrombin index is possible (during surgery, the state of the blood coagulation system should be monitored). Patients taking the drug should avoid sun exposure and ultraviolet radiation. It is necessary to refrain from driving and work requiring concentration of attention and speed of psychomotor reactions.
Interactions:
The simultaneous use of antacids containing calcium, aluminum or magnesium, preparations containing iron or zinc, as well as sucralfate , can lead to a significant decrease in the absorption of Norfloxacin. The interval between the use of these drugs and Norfloxacin should be at least 2 hours. Simultaneous use of theophylline or cyclosporinecan lead to an increase in their concentration in the blood, therefore, while taking them simultaneously, the dose of these drugs should be reduced and their level in the blood plasma should be monitored. With the simultaneous use of indirect anticoagulants (warfarin or its derivatives), an increase in their action may be noted, in this regard, regular monitoring of the level of prothrombin is necessary. With the simultaneous use of probenecid, the excretion of Norfloxacin in the urine decreases. Concomitant use of nitrofurantoinmay be accompanied by a decrease in the antimicrobial effect of Norfloxacin. Simultaneous administration of Norfloxacin with drugs that have the potential to lower blood pressure can cause a sharp decrease in blood pressure. In this regard, in such cases, as well as with the simultaneous administration of barbiturates, anesthetics, heart rate, blood pressure, and ECG indicators should be monitored. Simultaneous use with drugs that lower the seizure threshold can lead to the development of epileptiform seizures. Synergism has been noted between Norfloxacin and antifungal agents (eg amphotericin B, ketoconazole , miconazole , flucytosine and nystatin).
Overdose:
Symptoms
Dizziness, nausea, vomiting, drowsiness, cold sweat, swelling of the face, convulsions.
Treatment:
Induction of vomiting or gastric lavage, adequate hydration therapy with forced diuresis, symptomatic therapy. There is no specific antidote.
