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

Active substance:
Norfloxacin	- 200 mg	400 mg
Excipients:
silicon dioxide colloid (aerosil)	- 3.6 mg	- 7.2 mg
magnesium stearate	- 3.6 mg	- 7.2 mg
microcrystalline cellulose	- 120.4 mg	240.8 mg
croscarmellose sodium	- 10.8 mg	- 21.6 mg
Crospovidone	- 21.6 mg	- 43.2 mg
Excipients for the shell
hypromellose (hydroxypropylmethylcellulose)	- 6.57 mg	13.14 mg
macrogol 6000 (polyethylene glycol 6000)	- 2.2 mg	- 4.4 mg
titanium dioxide	- 2.2 mg	- 4.4 mg
quinoline yellow dye	- 0.03 mg	- 0.06 mg
*Average weight of coated tablet*	- 0.371 g	- 0.742 g

Description:The tablets covered with a film membrane of yellow color, biconvex, oblong with rounded ends, with a risk on one side.On the cross-section, two layers are visible, the inner layer is white or pale yellow.

Pharmacotherapeutic group:Antimicrobial agent - fluoroquinolone.

ATX: & nbsp

S.01.A.E.02 Norfloxacin

Pharmacodynamics:

Antimicrobial agent from the group of fluoroquinolones. It has a bactericidal effect, inhibiting the DNA-gyrase, which ensures supercoiling and stability of bacterial DNA, leads to destabilization of the DNA chain and the death of bacteria.

To norfloxacin 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 pneumonia, Neisseria gonorrhoeae, Proteus mirabilis, Proteus vulgaris, Pseudomonas aeruginosa, Serratia marcescens.

To norfloxacin 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.

The drug is inactive with respect to obligate anaerobes.

Pharmacokinetics:

Absorption when ingested is fast (30-40%), food reduces absorption. The maximum concentration of norfloxacin in the blood plasma (FROMmOh) when 200 mg, 400 mg and 800 mg are administered, 0.8 μg / ml, 1.5 μg / ml and 2.4 μg / ml, respectively. Time to reach the maximum concentration in the blood plasma (TCmax) -1h. Effective half-life (T1 / 2) - 3-4 hours.The equilibrium concentration of the drug in the blood plasma (Css) is achieved within 2 days.

In the elderly excretion is slowed (due to age-related decline in kidney function): after ingestion of 400 mg of norfloxacin, the area under the pharmacokinetic curve "concentration-time" (AUC) is 6.97-12.63 mg * h / ml and C_mOh - 1,25-2,79 mcg / ml (in young people - 6.4 mg * h / ml and 1.5 mcg / ml, respectively), T1 / 2 - 4 hours.

The connection with plasma proteins is 10-15%.

In chronic renal failure (CRF) (creatinine clearance (CK) less than 30 ml / min / 1.73 sq.m) T1/2 extends to 6.5 hours.

Norfloxacin is metabolized in the liver. Kidney clearance - 275 ml / min. Within 24 hours, 26-32% is excreted by the kidneys in the form of unchanged substance, 5-8% in the form of a weakly active metabolite. In the subsequent kidneys, less than 1% of the dose taken is excreted. About 30% is excreted by the intestine. In the elderly, 22 % norfloxacin(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:

Infections caused by microorganisms sensitive to norfloxacin: urinary tract infections (except acute and chronic complicated pyelonephritis), prostatitis, uncomplicated gonorrhea.

Contraindications:

Hypersensitivity to the components of the drug and other fluoroquinolones; tendonitis, tendon rupture caused by fluoroquinolones (including in the anamnesis); pregnancy, lactation, children under 18 years of age, deficiency of glucose-6-phosphate dehydrogenase.

Carefully:

With caution apply the drug in the following diseases:

Epilepsy, convulsive syndrome, renal / hepatic insufficiency, myasthenia gravis gravis, atherosclerosis of cerebral vessels, cerebral circulatory disorders (in anamnesis), organic diseases of the central nervous system, hepatic porphyria, diabetes mellitus, congenital lengthening interval syndrome Q-T, heart disease (heart failure, myocardial infarction, bradycardia), electrolyte imbalance (eg, hypokalemia, hypomagnesemia), elderly age, mental disorders in the anamnesis; simultaneous reception of drugs, extending the interval Q-T (antiarrhythmic IA and III classes, tricyclic and tetracyclic antidepressants, neuroleptics, macrolides, antifungal, imidazole derivatives, some antagistamine, including / astemizole, terfenadine, ebastine).

Pregnancy and lactation:The drug is contraindicated for use by pregnant women and women during lactation. When used during lactation, breastfeeding should be discarded.

Dosing and Administration:

Inside.

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 gonococcal urethritis, pharyngitis, proctitis, cervicitis - once 800 mg.

To prevent recurrence of urinary tract infections - 200 mg / day.

In patients with impaired renal function with QC greater than 20 ml / min, correction of the dosing regimen is not required. When QC is below 20 ml / min (or serum creatinine concentration is more than 5 mg / 100 ml) and patients on hemodialysis, 1/2 therapeutic dose is administered twice a day or a full dose once a day.

Side effects:

From the central nervous system (CNS): dizziness, headache, 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,dyspepsia, flatulence, vomiting, dryness of the oral mucosa, heartburn, loose stool, bitter taste in the mouth, ulceration of the oral mucosa, itching of the anus.

From the hematopoiesis: leukopenia, thrombocytopenia, eosinophilia, neutropenia.

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

From the sense organs: blurred vision.

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

From the cardiovascular system (SSS): myocardial infarction, palpitation.

From the urinary system: renal colic.

Laboratory indicators: increased activity of aspartate aminotransferase, alanine aminotransferase, alkaline phosphatase, lactate dehydrogenase, proteinuria, decreasehematocrit and hemoglobin, increased urea concentration in the blood, hypercreatininaemia, glucosuria.

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

Postmarketing experience.

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

Allergic reactions: anaphylactoid reactions, angioedema, dyspnea, vasculitis, arthritis, arthralgia, myalgia.

From the skin: toxic epidermal necrolysis, Stevens-Johnson syndrome, erythema multiforme, exfoliative dermatitis, photosensitivity.

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

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

From the urinary system: interstitial nephritis, kidney failure.

From the musculoskeletal system: tendonitis, tendon rupture, myasthenia gravis exacerbation gravis, increased activity of creatine kinase.

From the hematopoiesis: agranulocytosis, hemolytic anemia.

From the sense organs: reducedno hearing, noises in the ears, diplopia, dysgeusia.

Other side effects of quinolones: albuminuria, candiduria, crystalluria, cylindruria, dysphagia, hyperglycemia, hypercholesterolemia, hyperkalemia, hypertriglyceridemia, hematuria, hepatic necrosis, hypoglycemia, nystagmus, postural hypotension, prothrombin time elongation, vaginal candidiasis.

If any of the side effects listed in the manual are aggravated, or if you notice any other side effects not listed in the instructions, tell your doctor.

Overdose:

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

Treatment: gastric lavage, adequate hydration therapy with forced diuresis. It requires a survey and observation in the hospital for several days!

There is no specific antidote.

Interaction:

Reduces the clearance of theophylline by 25%, so with simultaneous use should reduce the dose of theophylline. Increases the concentration of indirect anticoagulants, cyclosporine in the blood serum.

Reduces the effectiveness of nitrofurans.

Simultaneous reception of antacids containing aluminum or magnesium hydroxide, as well as medicines containing salts of iron, zinc, sucralfate, reduces absorption norfloxacin (the interval between their appointment should be at least 4 h).

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 isoenzyme CYP1A2, which can lead to an increase in the concentration of its substrates in the blood (including caffeine, clozapine, ropinirole, tacrine, theophylline, tizanidine).

With simultaneous admission with glibenclamide, the development of severe hypoglycemia is possible.

Probenecid can reduce the excretion of norfloxacin.

Antacids, sucralfate, multivitamins, containing zinc, didanosine should be taken 2 hours before or 2 hours after taking norfloxacin (may reduce its absorption).

With simultaneous application with drugs that extend the interval Q-T (antiarrhythmic drugs IA and III classes, tricyclic and tetracyclic antidepressants, neuroleptics, macrolides, antifungal, imidazole derivatives, some antihistamines, including. astemizole, terfenadine, ebastine), lengthening is possible the latter.

Special instructions:

During the treatment period, patients should receive a sufficient amount of liquidtroli diuresis).

During the period of therapy, an increase in the prothrombin index is possible (with the surgerythe coagulation system should be monitored).

During treatment, exposure to direct sunlight should be avoided.

Norfloxacin, like other fluoroquinolones, can cause tendinitis and a rupture tendongt; Risk factors: age over 60 years, glucocorticosteroids, kidney, heart or lung transplantation, increased physical activity, CRF, tendon lesions in history (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.

Norfloxacin can reduce the threshold of convulsive alertness and cause seizures; fluoroquinolones can also stimulate the CNS, causing tremors, toxic psychoses, anxiety, confusion and hallucinations; increased intracranial pressure.

Norfloxacin can lead to the development of pseudomembranous colitis, caused by Clostridium difficile. In this case, it is necessary to cancel the drug and designate(use of vancomycin in or metronidazole).

Not effective with syphilis.

Norfloxacin can cause peripheral neuropathy (paresthesia, hypesthesia, dysystasias, muscle weakness). At the first signs of neuropathy (pain, tingling, numbness or weakness in the limbs, violation of other sensitivities) in fromAn irreversible change in the drug should be avoided.

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

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

Care must be taken when driving vehicles and occupations with other potentially hazardous activities that require an increased concentration of attention and speed of psychomotor reactions.

Form release / dosage:The film-coated tablets are 200 mg and 400 mg.

Packaging:

By 10,15,20,30 tablets in a contour mesh box made of polyvinylchloride film and aluminum foil printed lacquered.

1, 2 contour squares with instructions for use in a pack of cardboard.

Storage conditions:

In a dry, protected from light place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

2 years.

Do not use after the expiry date printed on the package

Terms of leave from pharmacies:On prescription

Registration number:P N003833 / 01

Date of registration:25.07.2011

The owner of the registration certificate:OBOLENSKOE PHARMACEUTICAL ENTERPRISE, CJSC OBOLENSKOE PHARMACEUTICAL ENTERPRISE, CJSC Russia

Manufacturer: & nbsp

OBOLENSKOE PHARMACEUTICAL ENTERPRISE, CJSC Russia

Information update date: & nbsp10.08.2015

Illustrated instructions

Instructions

Norfloxacin (Norfloxacin)