Norfloxacin
Producer: LLC Pharmlend Republic of Belarus
Code of automatic telephone exchange: J01MA06
Release form: Firm dosage forms. Tablets.
General characteristics. Structure:
Active ingredient: 400 mg of norfloxacin.
Auxiliary a veshchestva:kaltion phosphate double-base, starch corn, lactose, the gelatin, Natrium benzoicum, talc purified of magnesium stearate, colloid anhydride of silicon, sodium glikolit starch, a methylene chloride, OpaDryBlue dye (hydroxypropyl marked cellulose, polyethyleneglycol, talc, titanium dioxide, LakeBrilliantBlue dye), polyethyleneglycol 6000, propylene glycol.
Antibacterial agent.
Pharmacological properties:
Pharmacodynamics. Inhibits bacterial DNK-girazu, the providing superspiralling and stability of DNA, protein synthesis breaks and leads to death of microorganisms.
It is active concerning golden staphylococcus (including staphylococcus, resistant to Methicillinum), epidermal staphylococcus, Neisseria gonorrhoeae, Neisseria meningitidis, colibacillus, Citrobacter spp., клебсиелл, enterobakteriya, Hafnia, protiums (indolpositive and indolnegative strains), salmonellas, shigellas, Yersinia enterocolitica, Campylobacter jejuni, Aeromonas plesiomonas, Vibrio cholerae, Vibrio parahaemolyticus, Haemophilus influenzae, chlamydias, легионелл.
Variable sensitivity to norfloxacin enterococci, streptococci of pyogenes, pneumoniae and viridans, Serratia marcescens, Pseudomonas aeruginosa, Acinetobacter, Mycoplasma hominis pneumoniae, a tuberculosis mycobacterium, and also Mycobacterium fortium have.
Are not sensitive - the majority of strains of Ureaplasmaurealyticum, Nocardiaasteroides, anaerobic bacteria (for example, Bacteroidesspp., peptokokk, peptostreptokokk, Eubacteriumspp., Fusobacteriumspp., Clostridiumdifficile), Treponemapallidum.
Pharmacokinetics. It is well soaked up from digestive tract (an absorption indicator - more than 20-40%), food detains absorption. Therapeutic concentration is reached in plasma in 1 h after intake. Communication with proteins of plasma - 10-15%.
Distribution - a parenchyma of kidneys, testicles, liquid of seed tubules, a prostate gland, a uterus, abdominal organs and a small pelvis, bile, maternal milk. Permeability through GEB and a placental barrier high. It is metabolized in small degree in a liver and removed with bile and urine. Excretion is carried out by kidneys for the account of both glomerular filtering, and canalicular secretion. During the day 32% of a dose are excreted with urine, about 30% - with excrements; 5-8% are allocated in the form of metabolites.
Indications to use:
Treatment of the infectious and inflammatory diseases caused by the activators sensitive to drug:
- acute and chronic infectious diseases of urinary tract (cystitis, pyelonephritis, urethritis, prostatitis);
- acute gonorrhea;
- prevention of infections at operative measures and diagnostic procedures in urology;
- shigellosis;
- salmonellosis;
- prevention of sepsis at patients with a neutropenia;
- prevention of infectious diseases of digestive tract and prevention of diarrhea of travelers.
Route of administration and doses:
Norfloxacin should be accepted in 2 hours prior to or in 4 hours after use of drugs of calcium, polyvitaminic drugs, the calciferous, nutrient solutions applied inside and dairy products.
Dosing for patients with normal function of kidneys. The recommended daily dose of norfloxacin is described in the table:
|
Infections |
Dose on reception |
Reception frequency |
Duration |
Daily dose |
|
Uric ways: |
400 mg |
12 hours |
3 days |
800 mg |
|
Infections |
Dose on reception |
Reception frequency |
Duration |
Daily dose |
|
The complicated infections of uric ways |
400 mg |
12 hours |
10-21 days |
800 mg |
|
Diseases, sexually transmitted |
800 mg |
Once |
1 |
800 mg |
|
Prostatitis. Acute or chronic |
400 mg |
12 hours |
28 days |
800 mg |
Dosing at patients with a renal failure: norfloxacin can be used for treatment of infections of uric ways at patients with a renal failure. Patients with clearance of creatinine have 30 ml/min. / 1,73 m3 or less the recommended dose makes 400 mg once a day at duration of treatment stated above. In this dose concentration in urine of drug exceeds MIK for the majority of the uric infectious activators susceptible to norfloxacin even if the clearance of creatinine at the patient is less than 10 ml/min. / 1,73 of sq.m.
Elderly patients. In the absence of a renal failure (the clearance of creatinine is more than 30 ml/min. / 1,73 of m3) there is no need of dose adjustment. For elderly patients who have a clearance of creatinine of 30 ml/min. / 1,73 m3 or less the recommended dose makes 400 mg with a treatment duration as at a renal failure once a day.
Features of use:
Hypersensitivity/anaphylaxis. It was reported about cases of development of serious reactions of hypersensitivity (anaphylactoid and anaphylactic) at reception of the first dose of hinolon. In certain cases these reactions were followed by a cardiac collapse, a loss of consciousness, a faint, hypostasis of a throat or person, диспноэ, urticaria, an itch. In case of development of allergic reactions to norfloxacin it is necessary to cancel drug.
Pseudomembranous colitis. Treatment by antibacterial agents leads to modification of normal flora of a large intestine and can lead to the increased growth of the clostridiums producing toxin which is the prime cause "an antibiotic - the associated colitis". If against the background of use of norfloxacin for patients there is diarrhea, it is necessary to take a possibility of development of a pseudomembranous coloenteritis into account. At establishment of the diagnosis "pseudomembranous colitis" the doctor has to consider depending on indications a question of the treatment termination by norfloxacin and immediately begin the corresponding treatment. At the same time the medicines suppressing a peristaltics should not be applied.
Peripheral neuropathy. At emergence in the patient of symptoms of neuropathy, including pain, burning, a pricking, catalepsy and/or weakness, temperature increase, etc., it is necessary to stop reception of norfloxacin and to see the attending physician.
Prolongatsiyaintervalaqt/torsades de pointes. The patients receiving hinolona have rare messages on development of prolongation of an interval of Qtvo time of carrying out post-market researches including norfloxacin. Exceptional cases were associated with the following factors: age more than 60 years, a female, the previous heart diseases and/or use of complex therapy. Norfloxacin is not recommended to be used or apply with extra care at patients with prolongation of an interval of Qtili with the known risk factors of lengthening of an interval of QT (including, a hypopotassemia), and also at joint appointment with other medicines with the established risk factor of lengthening of an interval of QT, including from antiaritmika of the I Class A (quinidine, procaineamide) or the III class (Amiodaronum, соталол).
Tendinites, ruptures of sinews. At norfloxacin use, as well as at other hinolon, chances of emergence of tendinites and/or ruptures of sinews (especially an Achilles tendon) what the patients of advanced age, patients receiving treatment using corticosteroids or patients with transplants of kidneys, hearts, lungs are most predisposed to. At emergence of the first symptoms of pain in sinews or inflammations in joints, constraint of joints the patient has to record the disturbing joints in a motionless state and consult with the doctor. If it is impossible to exclude emergence of tendinites or a rupture of a sinew, treatment using norfloxacin has to be stopped. The rupture of sinews is possible as during therapy of a hinolonama (including, norfloxacin), and after completion of treatment.
Norfloxacin is not shown for treatment of syphilis. The antimicrobic medicines used in high doses during a short span for treatment of gonorrhea can mask or detain manifestation of symptoms of the developing syphilis. At all patients with gonorrhea carrying out the serological test for syphilis is necessary during diagnosis, and also repeatedly (in 3 months) after purpose of norfloxacin.
Hinolona can also cause the stimulation of TsNS leading to a tremor, the concern easy for dizziness, confusion of consciousness and hallucinations. At emergence of such reactions against the background of norfloxacin it is necessary to cancel drug immediately.
Norfloxacin, as well as other hinolona, patients who accept цисаприд, erythromycin, antipsychotic means, tricyclic antidepressants need to apply with care.
Hinolona, including norfloxacin, can cause an aggravation of symptoms of a myasthenia and result in life-threatening weakness of respiratory muscles. It is necessary to be careful when using hinolon, including, norfloxacin, at patients with a myasthenia. When developing short wind during treatment by norfloxacin it is necessary to see the attending physician and to undertake the relevant urgent activities.
At norfloxacin use, as well as other drugs of group of hinolon, increase in photosensitivity therefore during treatment it is necessary to avoid long and strong impacts of solar radiation is possible. During this period it is also impossible to use a sunbed. At emergence of signs of a photosensitization treatment should be stopped.
At norfloxacin use, as well as other drugs of group of hinolon, hemolitic reactions at patients with the hidden or expressed deficit glyukozo-6-fosfatdegidrogenazy can take place. When carrying out surgical interventions control of a condition of coagulant system of blood is required (during therapy possibly increase in a prothrombin ratio).
Drug contains lactose therefore it is not appointed to patients with hereditary intolerance of a galactose, deficit of lactose or disturbances of absorption of a glucose/galactose.
Restrictions to use: atherosclerosis of vessels of a brain, disturbance of cerebral circulation, epilepsy and convulsive syndrome, renal failure and liver.
Safety of appointment is not established to children of dopubertatny age and the feeding women. Therefore these categories of patients should appoint drug with care.
It is necessary to be careful also at patients with a renal failure. At clearance of creatinine less than 30 ml/min. a dose need to be reduced twice.
Use during pregnancy or feeding by a breast. Drug is contraindicated for use during pregnancy. Norfloxacin, as well as other hinolona gets into mother's milk therefore in case of need uses norfloxacin in the period of a lactation need to be interrupted feeding with a breast.
Children. Norfloxacin is not recommended for use to children and teenagers aged up to 18 years.
Use for elderly patients. Elderly patients have the increased risk of a rupture of sinews at use of ftorkhinolon. This risk even more increases at the patients receiving the accompanying therapy by corticosteroids.
Ability to influence speed of reaction at control of motor transport or work with other mechanisms. During treatment by norfloxacin it is necessary to abstain from control of motor transport or works with other mechanisms.
Side effects:
From a GIT and a liver: nausea, diarrhea, lack of appetite, bitterness in a mouth, an abdominal pain, dysbacteriosis, candidiasis, pseudomembranous colitis, perhaps tranzitorny increase in activity of hepatic transaminases.
From a nervous system: headache, fatigue, drowsiness.
From system of a hemopoiesis: eosinophilia, leukopenia, decrease in a hematocrit.
From cardiovascular system: tachycardia, disturbances of a cordial rhythm, arterial hypotension, a vasculitis, Stephens's syndrome – Johnson.
From an urinary system: glomerulonephritis, dysuria, polyuria, proteinuria, crystalluria, kreatininemiya, urethral bleedings.
Allergic and immunopathological reactions (skin itch, small tortoiseshell, hypostases) at observance of the mode of dosing are noted extremely seldom.
Interaction with other medicines:
At simultaneous use of norfloxacin with other medicines with the established risk factor of lengthening of an interval of QT, including with antiarrhytmic means of IA and the III class, danger of development of arrhythmias and lengthening of an interval of QT increases. In these cases norfloxacin should be applied with extra care, also as well as at patients with the known risk factors of lengthening of an interval of QT.
Nitrofurantoin. In the conditions of invitropokazan antagonism between norfloxacin and nitrofurantoin therefore it is necessary to avoid their combined use.
Probenetsid. Probenetsid reduces release of norfloxacin in urine, but does not influence its normal concentration in blood serum.
Caffeine. Norfloxacin, as well as other hinolona, slows down caffeine degradation that can lead to reduction of allocation and increase in an elimination half-life of caffeine from a blood plasma. It needs to be considered at the use of coffee, and also at use of medicines, the containing caffeine (anesthetics).
Cyclosporine. At simultaneous use with norfloxacin increase in concentration of cyclosporine in blood serum is possible. Therefore it is necessary to control concentration of cyclosporine in blood serum and, if necessary, respectively to modify dosing.
Warfarin. Norfloxacin, as well as other hinolona, can exponentiate effect of peroral anticoagulant of warfarin or its derivatives (for example, a fenprokumona, an atsenokumarola) therefore at simultaneous use of these medicines it is necessary to control attentively a prothrombin time or other parameters of coagulation.
Hormonal contraceptives. Contraceptive action of oral contraceptives in isolated cases can be called into question at treatment using antibiotics therefore at simultaneous use of norfloxacin and oral contraceptives use of non-hormonal contraceptive methods is in addition recommended.
Fenbufen. It is experimentally proved that simultaneous use of hinolon with fenbufeny can be the cause of epileptic attacks therefore it is necessary to avoid use of hinolon together with fenbufeny.
Clozapine, ропинирол. If begin or stop norfloxacin reception, dose adjustment of clozapine or a ropinirol can be necessary for patients who already accept these drugs.
Tizanidin. The concomitant use of a tizanidin and norfloxacin is not recommended.
Glibenclamidum. The concomitant use of hinolon, including norfloxacin, with Glibenclamidum (sulphonylurea derivatives) can cause a heavy hypoglycemia. Therefore at a concomitant use of these drugs monitoring of level of glucose in blood is recommended.
Didanozin. The drugs containing диданозин should not be accepted together with norfloxacin or within 2 hours after norfloxacin reception as such drugs can interfere with one another to be soaked up that results in low concentration of norfloxacin in blood serum and urine.
Non-steroidal anti-inflammatory drugs (NPVS). The concomitant use of NPVS from hinolona, including norfloxacin, can increase risk of stimulation of the central nervous system and convulsive attacks. Therefore norfloxacin should be taken with caution to the persons accepting NPVS.
Simultaneous use of norfloxacin and the antiacid means containing a hydroxide of aluminum or magnesium, and also drugs calcigerous, iron and zinc, reduces norfloxacin absorption. In this regard it is necessary to take norfloxacin for 1-2 h to or not less than in 4 h after reception of the specified drugs.
At simultaneous use of norfloxacin and theophylline it is necessary to control concentration of theophylline in a blood plasma and to adjust its dose since undesirable increase in concentration of theophylline in blood and development of the corresponding side effects can be observed.
Simultaneous introduction with the medicines having potential ability to reduce the ABP can cause heavy hypotonia, with the drugs reducing a convulsive threshold of a brain (for example, theophylline) - epileptiform attacks.
Norfloxacin reduces effect of nitrofurans.
Contraindications:
- hypersensitivity to hinolona;
- liver failure;
- end-stage of a chronic renal failure;
deficit glyukozo-6-fosfatdegidrogenazy;
- pregnancy (at a fruit development of arthropathies is possible);
- lactation;
- children's and teenage age (up to 15 years).
Overdose:
Symptoms: dizziness, nausea, vomiting, drowsiness, emergence of cold sweat (without changes of the main hemodynamic indicators), a convulsive syndrome.
Treatment: a gastric lavage, adequate hydration therapy with an artificial diuresis, purpose of symptomatic means.
Storage conditions:
List B. To store in the dry, protected from light place, at a temperature not above +25 °C. To store in the place, unavailable to children. Period of validity 3 years.
Issue conditions:
According to the recipe
Packaging:
On 10 or 20 tablets in banks polymeric. 1 bank together with a leaf insert in a pack.
On 10 tablets in a blister strip packaging. 1 or 2 blister strip packagings in a pack.
