Zanotsin AUDE

General characteristics. Structure:

Заноцин® ODES of 400 mg
Active agent: ofloxacin of 400 mg
Excipients: кросповидон, Natrii hydrocarbonas, the gipromelloza, water purified sodium alginate, gum xanthane, карбопол, lactoses monohydrate, magnesium stearate, silicon dioxide colloid.
Film cover:
Dye опадрай white 31B58910 (a gipromelloza, lactoses monohydrate, titanium dioxide, a macrogoal), the water purified isopropanol.
Ink for a text:
Opakod S-1-17734 black (shellac of 45% (20% etherified) in SD-45 alcohol, dye ferrous oxide black, N butanol, propylene glycol, methanol, isopropanol, ammonium hydroxide of 28% of brand reagent), isopropanol.

Заноцин® ODES of 800 mg
Active agent: ofloxacin of 800 mg
Auxiliary вещества:кросповидон, Natrii hydrocarbonas, the gipromelloza, water purified sodium alginate, gum xanthane, карбопол, magnesium stearate, silicon dioxide colloid.
Film cover:
Dye опадрай white 31B58910 (a gipromelloza, lactoses monohydrate, titanium dioxide, a macrogoal), the water purified isopropanol.
Ink for a text:
Opakod S-1-17734 black (shellac of 45% (20% etherified) in SD-45 alcohol, dye ferrous oxide black, N butanol, propylene glycol, methanol, isopropanol, ammonium hydroxide of 28% of brand reagent), isopropanol.

Description:
Tablets "Заноцин® ODES of 400 Mg":
Biconvex tablets of an oval form, film coated, from white till almost white color, with the printed black food ink on one party of ZNT OD with the arrow crossing OD text, and smooth on another.
Tablets "Заноцин® OD of 800 Mg":
Biconvex tablets of an oval form, film coated, from white till almost white color, with the printed black food ink on one party of ZNT OD with the arrow crossing OD text, and smooth on another.

Pharmacological properties:

Pharmacodynamics. Antibacterial action of an ofloksatsin is carried out as a result of suppression of effect of enzyme of topoisomerase II (DNK-giraza) in bacterial cells. Topoisomerases are responsible for introduction of negative rings of nucleotides to DNA. Ftorkhinolona reduce introduction of negative rings to DNA and cause bystry disturbance of DNA replication.
Заноцин® ODES of a tablet are capable to release a long time ofloxacin that does drug use (once a day) more convenient. Single use of the tablets Zanotsin® ODES of 400 mg and Zanotsin® of ODES of 800 mg is equivalent by quantity of the released ofloksatsin to use of usual tablets of an ofloksatsin of 200 mg and 400 mg twice during the day.
Antibacterial range:
Ofloxacin is active concerning the following microorganisms:
Aerobic gram-positive microorganisms:
Staphylococcus aureus (Methicillinum - sensitive strains); Streptococcus pneumoniae (penicillin - sensitive strains); Streptococcus pyogenes.
Aerobic gram-negative microorganisms:
Citrobacter (diversus) koseri; Enterobacter aerogenes; Escherichia coli; Haemophilus influenzae; Klebsiella pneumoniae; Neisseria gonorrhoeae; Proteus mirabilis; Pseudomonas aeruginosa.
Other microorganisms:
Chlamydia trachomatis
 In vitro is defined the minimum overwhelming concentration of an ofloksatsin - 2 mkg/ml or less for the majority (90%) of strains of the following microorganisms:
Aerobic gram-positive microorganisms:
Staphylococcus epidermidis (Methicillinum - sensitive strains); Streptococcus pneumoniae (penicillin - resistant strains); Staphylococcus saprophyticus.
Aerobic gram-negative microorganisms:
Acinetobacter calcoaceticus; Bordetella pertussis; Citrobacter freundii; Enterobacter cloacae; Haemophilus ducreyi; Klebsiella oxytoca; Moraxella catarrhalis; Morganella morganii; Proteus vulgaris; Providencia rettgeri; Providencia stuartii; Serratia marcescen.
Anaerobic microorganisms:
Clostridium perfringens
Other microorganisms:
Chlamydia pneumoniae; Gardnerella vaginalis; Legionella pneumophila; Mycoplasma hominis; Mycoplasma pneumoniae; Ureaplasma urealyticum.
Ofloxacin has no activity concerning Treponema pallidum. Many strains of Streptococcus and Enterococcus, and also anaerobic microorganisms of a rezistentna to an ofloksatsin.

Pharmacokinetics. At use inside ofloxacin is quickly absorbed. Absorption after intake bystry and full (95%). Bioavailability – over 96%. Food can slow down absorption, but has no significant effect on bioavailability. After single use of the tablets Zanotsin® ODES of 400 mg and Zanotsin® of ODES of 800 mg peak concentration in plasma are reached within 6 – 8 hours and make 2.090.46 of mkg/ml and 5.151.07 of mkg/ml respectively, and the speed and extent of absorption are comparable with those at double reception of usual tablets of an ofloksatsin of 200 mg and 400 mg. At use of an ofloksatsin together with food lengthening of time of achievement of the maximum concentration of drug in plasma is observed, indicators of level of the maximum concentration of drug in plasma and the area under a pharmacokinetic curve do not change. The seeming distribution volume – 100 l. Distribution: cells (leukocytes, alveolar macrophages), skin, soft tissues, bones, abdominal organs and a small pelvis, the respiratory system, urine, saliva, bile, a prostate secret, well gets through a blood-brain barrier (GEB), a placental barrier, cosecretes with maternal milk. Gets into the medullispinal liquid (ML) (14-60%). It is metabolized in a liver (about 5%). 25% of an ofloksatsin communicate proteins of plasma. The elimination half-life at reception of tablets makes 6 – 8 hours.
Ofloxacin is removed, generally by kidneys: about 70-90% of drug - in not changed look kidneys and less than 5% in the form of metabolites, including dimethyl - or N-oxide-ofloksatsina.
The clearance of an ofloksatsin is reduced at patients with an impaired renal function (clearance of  creatinine of 50 ml/min.), at such patients correction of the mode of dosing is necessary.
At a hemodialysis 10-30% of drug are removed.

Indications to use:

Заноцин® ODES it is shown at the following infectious and inflammatory diseases caused by sensitive microorganisms:
- Lower parts of respiratory tract, including the pneumonia caused by H. influenzae and Streptococcus pneumoniae and an exacerbation of chronic bronchitis.
- Urinogenital system, including: the acute, uncomplicated or complicated, urethral or cervical forms of gonorrhea; the urethritis and a cervicitis caused by Chlamydia trachomatis; the mixed urethral and cervical infections caused by Chlamydia trachomatis and Neisseria gonorrhoeae; prostatitis.
- Infections of skin and soft tissues.
- Bodies of a small pelvis: endometritis, oophoritis, parametritis.

Route of administration and doses:

Inside entirely after meal, washing down with enough water. Tablets cannot be broken or chewed!
The recommended dosages for adults:
Infections Daily
 dose Frequency rate of use of Zanotsin® of ODES use Duration
 Infections of urinary tract:
- the cystitis caused by E.coli or K.pneumoniae of 400 mg Each 24 hours 3 days
- the cystitis caused by other microorganisms of 400 mg Each 24 hours 7 days
- the complicated infections
 urinary tract of 400 mg
 Each 24 hours 10 days

Infections  of integuments and soft tissues of 800 mg Each 24 hours 10 days
 Pneumonia or  exacerbation of chronic bronchitis of 800 mg Each 24 hours 10 days
 Infections, sexually transmitted:
-  uncomplicated gonorrhea of 400 mg Once 1 day
-   not gonococcal   urethritis  and  cervicitis of 800 mg Each 24 hours 7-10 days
-  the mixed    urethral and  cervical infections caused by Chlamydia trachomatis and Neisseria gonorrhoeae. To 800 mg there are Each 24 hours 7-14 days
 Prostatitis of 400 mg Each 24 hours up to 6 weeks
 Acute inflammatory diseases of bodies of a small pelvis of 800 mg Each 24 hours 10 - 14 days
 The dosing mode at patients with an impaired renal function:
After an initial normal dose, it is necessary to adjust the dosing mode according to the following scheme:

Clearance of creatinine (ml/min.) Maintenance of a dose and frequency of dosing
20-50 At infections of integuments and soft tissues, pneumonia or an exacerbation of chronic bronchitis, and also acute inflammatory diseases of bodies of a small pelvis, a chlamydial infection the dose of Zanotsin® of ODES of 400 mg – 1 tablet is recommended each 24 hours.

If only concentration of creatinine in plasma is known, calculation of clearance of creatinine is made on the following formula:
                                                                                      The weight (kg) x (140 – age)
Men: Clearance of creatinine (ml/min.) =      -----------------------------------------
                                                                               72  x  creatinine in plasma (% mg)
Women: 0.85 x the value calculated for men
 Use for patients with the broken function of a liver:
At patients with the expressed abnormal liver function, and also in case of cirrhosis or ascites, some reduction in the rate of removal of an ofloksatsin can be observed. Therefore it is not necessary to exceed the maximum dose of an ofloksatsin of 400 mg a day.
 Use for elderly patients
 In this group of patients any restrictions on use of ftorkhinolon are not revealed. However, at elderly patients with reduced secretory function of kidneys it is necessary to carry out correction of the mode of a drug dosing (See. "The dosing mode at patients with an impaired renal function").

Features of use:

At some patients receiving ftorkhinolona phototoxicity reactions are observed. It is necessary to avoid long influence of direct sunshine. It is necessary to stop use of drug at emergence of signs of phototoxicity.
At combined use of an ofloksatsin with antidiabetic means careful monitoring of concentration of glucose in a blood plasma is recommended.
Ofloxacin is not choice drug at the pneumonia caused by pneumococci.
It is not shown at treatment of acute tonsillitis.
In case of side effects from TsNS, allergic reactions, drug withdrawal is necessary.
At use of drug development of pseudomembranous colitis which can vary from a lung to life-threatening is possible. Therefore, first of all, it is necessary to exclude a possibility of this disease at patients with the diarrhea which arose against the background of use of antibacterial drugs.
At the pseudomembranous colitis confirmed kolonoskopichesk and/or histologically peroral purpose of Vancomycinum and metronidazole is shown.
Seldom arising tendinitis can lead to a rupture of sinews (preferential an Achilles tendon), especially at elderly patients. In case of signs of a tendinitis, it is necessary to stop immediately treatment, to make an immobilization of an Achilles tendon and to consult at the orthopedist.
At drug use women are not recommended to use tampons like "Tampax", in connection with the increased risk of development of the milkwoman.
Against the background of treatment deterioration in a current of a myasthenia, increase of attacks of a porphyria at predisposed patients is possible.
Can result in false-negative results at bacteriological diagnosis of tuberculosis (interferes with Mycobacterium tuberculosis allocation).
At patients with abnormal liver functions or kidneys control of concentration of an ofloksatsin in plasma is necessary.
At a heavy renal and liver failure the risk of development of toxic effects increases (the reducing dose adjustment is required).
During treatment it is necessary to abstain from driving of motor transport and occupations potentially dangerous types of activity demanding the increased concentration of attention and speed of psychomotor reactions.
It is impossible to use ethanol.
During use of Zanotsina® of ODES false positive results when determining in urine of opiates and porphyrines are possible.
Data on use of an ofloksatsin for children, teenagers (age less than 18 years), pregnant women and nursing mothers are insufficient for forecasting of its safety in the specified groups.

Side effects:

Side effects which frequency of emergence was estimated as follows are included below: often – it is more than 1 case on 100 appointments; not often - less than 1 case on 100 appointments; seldom – less than 1 case on 1000 appointments.
From digestive tract and gepatobiliarny system:
Often: nausea, vomiting, diarrhea, abdominal pain, gastralgia, meteorism. Diarrhea can be a coloenteritis symptom (which in certain cases can be hemorrhagic).
Not often: appetite loss, increase in indicators of "hepatic" transaminases and/or bilirubin.
Seldom: development of holestatitechesky jaundice, hepatitis or the expressed abnormal liver function is possible. A rare form of a coloenteritis which arises at use of antibiotics – pseudomembranous colitis (in most cases the caused Clostridium difficile). If pseudomembranous colitis is only suspected, it is necessary to stop use of an ofloksatsin. It is not necessary to use the drugs reducing an intestines peristaltics.
From the central nervous system (CNS):
Often: headache, dizziness, feeling of fatigue.
Not often: uncertainty of movements, spasms, psychomotor excitement, phobias, increase in intracranial pressure, confusion of consciousness, balance disturbance, "dreadful" dreams, feeling of alarm, a depression, hallucinations and psychotic reactions, sleeplessness, shaky gait and a tremor (as a result of disturbance of muscular coordination), neuropathy, feeling of numbness and paresthesia or hyperesthesia.
From sense bodys:
Not often: vision disorder, disturbance of color perception, diplopia, disturbance of taste and sense of smell (in rare instances temporary loss of function).
Seldom: decrease in hearing (including a hearing loss). If these reactions were observed at patients after the first dose of an ofloksatsin, in such cases it is necessary to stop a therapy course.
From cardiovascular system:
Tachycardia and temporary lowering of arterial pressure.
Not often: a circulator collapse (as a result of a bystry lowering of arterial pressure).
From bodies of a hemopoiesis:
Seldom: anemia, a leukopenia (including an agranulocytosis), thrombocytopenia, a pancytopenia, hemolitic and aplastic anemia.
From an urinary system:
Not often: renal failure.
Seldom: acute intersticial nephrite, or an acute renal failure with the progressing increase in concentration of serumal creatinine. Increase in content of urea.
Allergic reactions:
Often: skin rash, itch.
Not often: photodermatitis, exudative erythema, Stephens-Johnson's syndrome,   Lyell's disease and vasculites.
Seldom: fever, an allergic pneumonitis, allergic nephrite, a bronchospasm, диспноэ, shock, a Quincke's disease, vaskulitopodobny reactions, an eosinophilia, eosinophilic pneumonia are possible.
From a musculoskeletal system:
Seldom: the tendinitis, a mialgiya, an arthralgia, tendosinovit, a tendovaginitis, a rupture of a sinew, pain in muscles and joints (in rare instances can be a sign of a rabdomioliz).
Other side effects:
Seldom: hyper - or a hypoglycemia (at patients with a diabetes mellitus), weakness, an intestinal dysbiosis, superinfection, a vaginitis.
At some patients (with special predisposition) use of an ofloksatsin can provoke the attack of a porphyria.
Laboratory indicators:
Increase in an aktivost of an alkaline phosphatase, aminotransferase aspartate, glutamine of transaminase and lactate of a dehydrogenase.

Interaction with other medicines:

Theophylline:
Reduces clearance of theophylline by 25% (at simultaneous use it is necessary to reduce a theophylline dose).
Antiacid drugs, сукральфат, cations of metals, multivitamins, foodstuff:
Reduce absorption of ftorkhinolon therefore their combined use with ofloksatsiny should be avoided (time interval between purpose of these drugs has to be not less than 2 h).
Non-steroidal anti-inflammatory drugs (NPVP):
Combined use with drugs of the specified group strengthens side effects of ftorkhinolon on the central nervous system.
Cyclosporine:
At combined use of cyclosporine with some ftorkhinolona, increase in concentration of cyclosporine in plasma was noted. Reactions of medicinal interaction of cyclosporine and an ofloksatsin are not studied.
The drugs which are metabolized P450 cytochrome:
The majority of ftorkhinolon suppress activity of P450 cytochrome. At combined use from ftorkhinolona increase in time of semi-removal of drugs which are also metabolized by P450 cytochrome is possible (for example, cyclosporine, theophylline/methylxanthine, warfarin etc.). Inhibition degree among various ftorkhinolon is variable.
Warfarin:
Ftorkhinolona strengthen effects of peroral anticoagulant of warfarin and its derivatives. At combined use of these drugs it is necessary to control indicators of coagulant system of blood carefully.
Cimetidinum:
Cimetidinum changes the speed of removal of some ftorkhinolon, leading to significant increase in the pharmacokinetic area under a curve. Hypoglycemic means:
At the patients receiving at the same time ftorkhinolona and antidiabetic means disturbances of concentration of glucose in a blood plasma, including hypo - and a hyperglycemia are noted.
At a concomitant use with antagonists of vitamin K it is necessary to exercise control of coagulant system of blood.
At co-administration with glucocorticosteroids (GKS) the risk of a rupture of sinews, especially at elderly people increases. At appointment with the drugs alkalizing urine (karboangidraza inhibitors, citrates, sodium bicarbonate), the risk of a crystalluria and nephrotoxic effects increases.

Contraindications:

Hypersensitivity to an ofloksatsin or other drugs of group of ftorkhinolon.
– Deficit glyukozo-6-fosfatdegidrogenazy.
– Epilepsy (including in the anamnesis).
– Decrease in a convulsive threshold (including after a craniocereberal injury, a stroke or inflammatory processes in the central nervous system (CNS)).
– Age up to 18 years (growth of a skeleton is not completed yet).
– Pregnancy.
– Lactation period.
– Clearance of Creatinine (CC) less than 20 ml/min.
With care
– Atherosclerosis of vessels of a brain.
– Disturbances of cerebral circulation (in the anamnesis).
– Chronic renal failure.
– Organic lesions of the central nervous system.

Overdose:

Symptoms: dizziness, confusion of consciousness, block, disorientation, drowsiness, vomiting.
Treatment:
The specific antidote for an ofloksatsin does not exist. At overdose treatment has to be symptomatic and supporting, and has to include the following measures:
- gastric lavage;
- maintenance of adequate hydration of an organism;
- maintenance therapy.
Ofloxacin is not removed at a hemodialysis or peritoneal dialysis.

Storage conditions:

List B. To store in the dry place at a temperature not above 25 °C. To store in the place, unavailable to children. Period of validity: 3 years. Not to use after expiry date.

Issue conditions:

According to the recipe

Packaging:

Tablets, film coated the prolonged action of 400 mg, 800 mg.
On 5 tablets in the blister from aluminum foil and PVC of a film; 1 or 2 blisters with the instruction on a medical use in a cardboard pack.