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

Excipients: cellulose microcrystalline 52 mg; starch corn 36 mg; sodium carboxymethyl starch (type A) 5 mg; silicon dioxide colloidal anhydrous 2 mg; talc purified 3 mg; magnesium stearate 2 mg; shell: hypromellose 6 cps 5 mg, 1.36 mg of macrogol 6000, brilliant blue lacquer 0.14 mg, 1 mg of titanium dioxide, purified talc 1.5 mg

Each tablet 400 mg, coated, contains:

active substance: norfloxacin 400 mg;

Excipients: cellulose microcrystalline 131 mg; corn starch 27.67 mg; sodium croscarmellose 10 mg; sodium carboxymethyl starch (type A) 10 mg; silicon dioxide colloidal anhydrous 3.33 mg; talc purified 9 mg; magnesium stearate 9 mg;

shell: Fell yellow 03F52448 (hypromellose 6 cps, macrogol 6000, titanium dioxide, talc purified, quinoline yellow WS varnish, sunset yellow FCF varnish) 14 mg.

Description:

Tablets 200 mg: blue round biconvex tablets with a smooth surface on both sides, coated.

Tablets 400 mg: light yellow or yellow round biconvex tablets with a smooth surface on both sides, coated.

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, suppressing the DNA-gyrase (topoisomerases II and IV, responsible for the process of supercoiling the chromosomal DNA around the nuclear RNA, which is necessary for reading the genetic information), violates DNA synthesis, growth and division of bacteria; causes significant morphological changes (including the cell wall and membranes) and the rapid death of the bacterial cell. Has a wide range 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. 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 stutzerr, other - Ureaplasma urealyticum.

Inactive with respect to obligate anaerobes.

The low toxicity for macroorganism cells is explained by the absence of DNA-gyrase in them. Against the background of taking norfloxacin, there is no parallel development of resistance to other antibiotics that do not belong to the group of DNA-gyrase inhibitors, which makes it highly effective against bacteria that are stablefor example, aminoglycosides, penicillins, cephalosporins, tetracyclines and many other antibiotics.

Pharmacokinetics:

When taken orally, it is quickly absorbed from the gastrointestinal tract (GIT), mainly in the 12-finger and jejunum. Eating slows down absorption, but does not change the maximum concentration (C_max) and bioavailability. Bioavailability is 20-40%. Time to reach the maximum concentration (Teshah) with oral intake - 60 min. The connection with plasma proteins is 10-15%. It is well distributed in the tissues of the body.Therapeutic concentrations are achieved in the parenchyma of the kidneys, ovaries, seminal tubular fluid, prostate gland, uterus, abdominal and pelvic organs, bile, maternal milk, eye fluid, bronchial secretion. Penetrates through the blood-brain barrier and the placenta.

Metabolised in the liver (5-8%) with the formation of low-activity metabolites. It is mainly excreted by the kidneys by glomerular filtration and tubular secretion in unchanged form (32%) and in the form of metabolites (5-8%), the rest - through the intestine with bile.

In chronic renal failure - CRF (creatinine clearance above 20 ml / min), the percentage of the drug withdrawn through the kidneys decreases, but cumulation in the body does not occur due to a compensatory increase in the metabolism of the drug and its excretion in the intestine.

Indications:

Bacterial infections caused by microorganisms that are sensitive to the drug:

- urinary tract (pyelonephritis, cystitis, urethritis);

- genital organs (chronic bacterial prostatitis, cervicitis, endometritis);

- intestinal infections (salmonellosis, shigellosis);

- uncomplicated gonorrhea (gonococcal urethritis, cervicitis).

Prevention

- traveler's diarrhea;

- sepsis in patients with neutropenia

Contraindications:Hypersensitivity to norfloxacin, other drugs of the quinolone group and to the components of the preparation; deficiency of glucose-6-phosphate dehydrogenase; tendonitis; rupture of tendons caused by the intake of fluoroquinolones (including, in the anamnesis); pregnancy, lactation (breastfeeding), children and adolescence (up to 18 years).

Carefully:

Epilepsy; convulsive syndrome; renal and / or liver failure; myasthenia gravis gravis; atherosclerosis of cerebral vessels; disturbances of cerebral circulation (in the anamnesis); organic diseases of the central nervous system; hepatic porphyria; diabetes; congenital lengthening syndrome QT; heart disease (heart failure, myocardial infarction, bradycardia); electrolyte imbalance (eg, hypokalemia, hypomagnesemia); elderly age; mental abnormalities in the anamnesis; simultaneous reception of drugs that extend the interval QT (antiarrhythmic Ia and III classes, tricyclic and tetracyclic antidepressants, neuroleptics, macrolides, antifungal, imidazole derivatives, some antihistamines, including, astemizole, terfenadine, ebastine).

Dosing and Administration:

Inside, on an empty stomach (at least 1 hour before or 2 hours after eating) and drink plenty of liquid,

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 infections of the genitals - 400 - 600 mg 2 times a day for 7 days.

In acute gonococcal urethritis, cervicitis - once 800 mg.

With chronic bacterial prostatitis - 400 mg 2 times a day, for 4-6 weeks. When intestinal infections (salmonellosis, shigellosis) - 400 mg 2 times a day, up to 5 days.

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).

For the prevention of sepsis with neutropenia - 400 mg 2 times a day to 8 weeks.

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

Side effects:

Depending on the frequency of occurrence, the following groups of side effects are distinguished: frequent - more than 1%,infrequent - 0,1-1%, rare - 0,01-0,1%, very rare - less than 0,01%.

From the central and peripheral nervous system: infrequently - headache, dizziness, fatigue; rarely - insomnia, drowsiness, anxiety, irritability, tinnitus; in very rare cases - a sense of fear, depression, hallucinations, fainting.

From the side of the cardiovascular system: in very rare cases - tachycardia, arrhythmias, lowering blood pressure (BP), vasculitis.

From the digestive system: infrequently - nausea, vomiting, diarrhea, abdominal pain, lack of appetite, bitterness in the mouth; rarely - pseudomembranous colitis (with prolonged use).

On the part of the hematopoiesis system: infrequently - eosinophilia, leukopenia, very rarely - hemolytic anemia.

From the urinary system: rarely - hematuria, crystalluria (primarily in alkaline urine and low diuresis), dysuria, polyuria, urinary retention, albuminuria; very rarely - glomerulonephritis, urethral bleeding.

Allergic reactions: infrequently - itchy skin, hives, rash; rarely - swelling of the face or larynx, dyspnea; very rarely - malignant exerythemavence-Johnson).

From the musculoskeletal system: rarely - arthralgia, tendinitis, very rarely - tendon ruptures.

From the laboratory indicators: rise activity "hepatic" transaminases and alkaline phosphatase, hypercreatininemia, hyperbilirubinemia, a decrease in hematocrit, an increase in urea in the blood plasma.

Other: very rarely - candidiasis.

Overdose:

Symptoms: dizziness, nausea, vomiting, drowsiness, "cold" sweat, swelling of the face.

Treatment: a specific antidote is unknown, symptomatic therapy is performed. It is necessary to carefully monitor the patient's condition, perform gastric lavage and other emergency measures, ensure sufficient fluid intake. With the help of hemo- or peritoneal dialysis, only a small amount (less than 10%) of the drug can be excreted.

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.

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, an increase in the serum creatinine concentration was observed, therefore, in such patients monitoring of this parameter is necessary.

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

Simultaneous use with drugs that reduce the convulsive threshold can lead to the development of epileptiform seizures.

Simultaneous application of from glucocorticosteroids can contribute increased risk of tendonitis or cases of rupture of tendons.

Norfloxacin can enhance the therapeutic effect of hypoglycemic drugs (sulfonylurea derivatives).

Simultaneous reception of norfloxacin with drugs that have the potential to reduce blood pressure can cause a sharp decrease in it. In such cases, as well as with simultaneous administration with barbiturates and other drugs for general anesthesiait is necessary to control the number of heart beats (heart rate), blood pressure and ECG parameters.

With simultaneous application with drugs that extend the interval QT (antiarrhythmic drugs Ia and III classes, tricyclic and tetracyclic antidepressants, neuroleptics, macrolides, antifungal, imidazole derivatives, some antihistamines, including, astemizole, terfenadine, ebastine) it is possible to lengthen the latter.

Special instructions:

During treatment, 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, exposure to direct sunlight should be avoided.

When there is pain in the tendons or at the first signs of tendonitis, it is necessary to cancel the drug.

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

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

Care must be taken when driving vehicles and engaging in other potentially hazardous activities,requiring increased concentration of attention and speed of psychomotor reactions.

Form release / dosage:

The coated tablets are 200 mg and 400 mg.

Packaging:10 tablets in an aluminum strip, the strip 2 are packed in a cardboard box with instructions for use.

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:3 years. Do not use after the expiry date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:П N011324 / 01

Date of registration:16.04.2012

The owner of the registration certificate:Dr. Reddy's Laboratories Ltd.Dr. Reddy's Laboratories Ltd. India

Manufacturer: & nbsp

DR. REDDY`S LABORATORIES, LTD. India

Representation: & nbspDR REDDY'S LABORATORIS LTD. DR REDDY'S LABORATORIS LTD. India

Information update date: & nbsp09.08.2015

Illustrated instructions

Instructions

Norillet® (Norilet)