Ofloxacin Zentiva - instructions for use, dose, side effects, contraindications

lactose monohydrate - 190,400 mg; corn starch - 95,200 mg; povidone 25-24,000 mg; crospovidone - 40,000 mg; poloxamer - 0.400 mg; magnesium stearate - 16,000 mg; talcum - 8,000 mg;

film sheath

hypromellose 2910/5 - 18,840 mg; macrogol 6000 - 1,060 mg; titanium dioxide - 4,700 mg; talcum - 1,400 mg.

Description:

White or almost white biconvex oblong tablets, covered with a film membrane, with a risk on both sides and engraving "400" on one side.

Pharmacotherapeutic group:antimicrobial agent-fluoroquinolone

ATX: & nbsp

S.01.A.E.01 Ofloxacin

J.01.M.A.01 Ofloxacin

Pharmacodynamics:

A broad-spectrum antimicrobial agent from the group of fluoroquinolones, acts on the bacterial DNA-gyrase enzyme, providing super-convoliation and, thus, the stability of bacterial DNA (the destabilization of DNA chains leads to their death). Has a bactericidal effect.

Active against microorganisms producing beta-lactamases and fast-growing atypical mycobacteria. Sensitive: Aeromonas hydrophila, Branhamella catarrhalis, Brucella spp., Clostridium perfringens, Esherichia coli, Salmonella spp., Enterobacter spp., Serratia spp., Citrobacter spp., Yersinia spp., Providencia, spp.,

Haemophilus influenzae and parainfluenzae, Haemophilus ducreyi., Plesiomonas, Legionella, Shigella spp., Proteus spp., Proteus mirabilis, Proteus vulgaris (indole-positive and indole-negative), Moraxella morganii, Klebsiella spp., Klebsiella pneumoniae, Helicobacter pylori, Mycoplasma spp., Vibrio spp., Gardnerella vaginalis, Neisseria gonorrhoeae, Neisseria meningitidis, Chlamydia trachomatis, Staphylococcus aureus methi-S, Staphylococcus coagulase negative.

Different sensitivity to the drug possess: Acinetobacter spp., Ureaplasma

urealyticum, Bacteroides fragilis; Mycobacterium tuberculosis, Mycobacterium leprae,

Chlamidia psittaci, Anaerobic Gram positive cocci, Enterococcus faecalis, Streptococcus pneumoniae, Pseudomonas spp, Streptococcus spp.,

In most cases, they are insensitive: Acinetobacter braumanmii, Clostridium difficile, Enterococci, Listeria monocytogenes, Staphylococci methi-R, Nocardia spp. He acts on Treponema pallidum.

Pharmacokinetics:

Absorption after oral administration is rapid and complete (95%). Bioavailability - over 96%, association with plasma proteins - 25 %, time to reach the maximum concentration (TCmOh)at oral intake - 1-2 hours, the maximum concentration (Сmах) after a single reception at a dose of 200 mg and 400 mg, it is 2.5 μg / ml and 5 μg / ml, respectively. Food can slow absorption, but does not have a significant effect on bioavailability. Apparent volume of distribution - 100 liters. Distribution: cells (leukocytes, alveolar macrophages), skin, soft tissues, bones, abdominal organs and small pelvis, respiratory system, urine, saliva, bile, the secret of the prostate gland, penetrates well through the blood-brain barrier, the placental barrier, is secreted with the mother's milk. Penetrates into cerebrospinal fluid with inflamed and non-inflamed meninges (14-60%).

Metabolized in the liver (about 5 %) with education Noxide ofloxacin and desmethylofloxacin. The half-life is 4.5 to 7 hours (regardless of the dose). It is excreted by the kidneys - 75 - 90% (unchanged), about 4% - with bile. The extrarenal clearance is less than 20%.

After a single application in a dose of 200 mg in urine is detected within 20 to 24 hours. In renal / hepatic insufficiency, excretion can be slowed down. Do not cumulate. With hemodialysis, 10-30% of the drug is removed.

Indications:

Treatment of infectious-inflammatory diseases caused by microorganisms sensitive to ofloxacin:

- respiratory tract infections (except for pneumococcal

infection);

- infections of the ear, throat, nose (except for cases of acute tonsillitis);

- infection of the abdominal cavity and biliary tract;

- infection of the kidneys, urinary tract, prostate, urethra (incl. gonococcal nature);

- infections of the pelvic organs;

- infections of bones and joints;

- infections of the skin and soft tissues;

- prevention of infections in patients with impaired immune status (including neutropenia).

Contraindications:- Hypersensitivity to ofloxacin, the components of the drug and other fluoroquinolones;

- epilepsy (including in the anamnesis);

- lesions of the central nervous system with a lower convulsive threshold (including after craniocerebral trauma, stroke or inflammatory processes in the central nervous system);

- the defeat of tendons in the previously conducted treatment with fluoroquinolones;

- renal failure (creatinine clearance less than 20 ml / min) and patients,

- who are on hemodialysis and peritoneal dialysis (for this drug forms);

- hereditary diseases, such as lactose intolerance, lactase deficiency or glucose-galactose malabsorption (due to the presence of lactose in the composition);

- age to 18 years (until the growth of the skeleton is completed);

- Pregnancy;

- the period of breastfeeding.

Carefully:

in patients with atherosclerosis of cerebral vessels, cerebral circulation disorders (in the anamnesis), lengthening of the interval QT, diseases of the cardiovascular system (heart failure, myocardial infarction, bradycardia), organic diseases of the central nervous system with predisposition to convulsive reactions, psychoses and other psychiatric disorders in the anamnesis, myasthenia gravis, liver failure, hepatic porphyria, chronic renal failure, glucose- 6-phosphate dehydrogenase, diabetes mellitus, impaired electrolyte blood composition (eg, hypokalemia, hypomagnesemia); old age, simultaneous use of drugs that extend the interval QT (antiarrhythmic drugs IA and III classes, tricyclic and tetracyclic antidepressants, neuroleptics, macrolides, antifungal agents,derivatives of imidazole, some antihistamines, incl. astemizole, terfenadine, ebastine), drugs for general anesthesia from the barbiturate group, drugs that reduce blood pressure.

Pregnancy and lactation:

The use of ofloxacin during pregnancy and during breastfeeding is contraindicated.

Dosing and Administration:

Inside. Doses are selected individually depending on the localization and severity of the infection, as well as the sensitivity of microorganisms, the general condition of the patient and the function of the liver and kidneys. Tablets are taken whole, washed down with a small amount of water for 0.5-1 hour before meals.

Adults - 400-800 mg per day, the course, treatment - 7-10 days, the frequency of application - 2 times a day. With gonorrhea - 400 mg once.

In patients with impaired renal function

- with a creatinine clearance of 50 ml / min, the dose of the drug is not required to be reduced;

- with a creatinine clearance of 50-20 ml / min, the dose of the drug should be taken once

every 24 hours. -

In patients with impaired hepatic function:

it is not recommended to exceed the maximum daily dose of 400 mg.

The duration of the course of treatment is determined by the sensitivity of the pathogen and the clinical picture; treatment should continue for at least 3 more days after the disappearance

symptoms of the disease and complete normalization of temperature.

In the treatment of salmonellosis treatment course - 7-8 days, in the treatment of uncomplicated and complicated infections of the lower urinary tract treatment course - 7 and 10 days respectively, with prostatitis treatment course - up to 6 weeks, with infections of the pelvic organs treatment course - 10-14 days , with, respiratory and skin infections treatment course -10 days.

Side effects:

The following frequency of side effects was used: very widespread (10%), widespread (1 %- 10%), infrequently occurring (0.1 % - 1%), rare (0.01 % - 0.1%), very rare (less than 0.01%), isolated cases.

From the nervous system

infrequently encountered - excitement, dizziness, headache, sleep disturbance / insomnia;

rare - psychotic reactions (for example, hallucinations), anxiety,

confusion, intense or "nightmarish" dreams, depression, drowsiness, violations of peripheral sensitivity, such as paresthesia, impaired taste and smell, violation of color perception, diplopia. very rare - Hearing impairment, such as tinnitus or hearing loss,epileptic seizures, extrapyramidal disorders or other disorders of muscle coordination, hypoesthesia, tremor, convulsions, sensory or sensory-motor peripheral neuropathy;

isolated cases - psychotic reactions accompanied by a behavior dangerous to the patient, including suicidal tendencies, increased intracranial pressure.

From the cardiovascular system:

rare - lowering blood pressure, tachycardia;

very rare - interval lengthening QT, ventricular arrhythmia, incl. ventricular tachysystolic arrhythmia of the "pirouette" type.

From the digestive system

infrequently encountered - decreased appetite, nausea, vomiting, diarrhea, abdominal pain; rare - anorexia, flatulence, enterocolitis, which can in some cases be hemorrhagic;

very rare - pseudomembranous colitis.

From the liver and biliary tract

rare - Increase in activity of "liver" enzymes, such as alanine aminotransferase (ALT), aspartate aminotransferase (ACT), lactate dehydrogenase (LDH), gamma-glutamyltransferase (GGT) and / or alkaline phosphatase and / or bilirubin concentrations in the blood;

very rare - cholestatic jaundice;

isolated cases - hepatitis.

From the urinary system:

rare - Hypercreatinemia, increased urea concentration in the blood; very rare - acute renal insufficiency; isolated cases - interstitial nephritis.

From the side of the musculoskeletal system: rare - tendonitis;

very rare - arthralgia, myalgia, tendon rupture (i.e. Achilles tendon); individual cases - rhabdomyolysis and / or myopathy; muscle weakness, which may be particularly important in patients with severe pseudo-paralytic myasthenia gravis.

From the hematopoiesis:

very rare - anemia (including hemolytic), leukopenia, eosinophilia, thrombocytopenia;

isolated cases - agranulocytosis, pancytopenia, oppression of bone marrow hematopoiesis.

Allergic reactions:

infrequent - itching, skin rash, burning sensation in the eyes, dry cough, rhinitis; rare- Anaphylactic / anaphylactoid reactions, such as urticaria, angio-neurotic edema, asphyxia / bronchospasm; hyperemia, sweating, papular rash;

very rare - Anaphylactic / anaphylactoid shock, multiforme exudative erythema, toxic epidermal necrolysis, photosensitivity, persistent

drug rash, vascular purpura, pinpoint hemorrhages, vasculitis, which in exceptional cases can lead to skin necrosis;

individual cases - Stevens-Johnson syndrome, severe suffocation, allergic pneumonitis, allergic nephritis.

Other:

infrequently - development of secondary infection caused by microorganisms and fungi that are resistant to perforating;

individual cases - acute attacks of porphyria in patients with porphyria, vaginitis, intestinal dysbiosis, hypoglycemia in diabetic patients receiving treatment with hypoglycemic drugs.

Overdose:

Symptoms: dizziness, confusion, inhibition, disorientation, drowsiness, vomiting.

Treatment: gastric lavage, symptomatic therapy. When hemodialysis is removed 10 - 30% of the drug.

Interaction:

Food products, antacids, containing Al³⁺, Ca²⁺, Mg²⁺ or iron salts, reduce the absorption of ofloxacin, forming insoluble complexes (the time interval between administration of these drugs should be at least 2 hours).

Reduces the clearance of theophylline by 25 % (with simultaneous use should reduce the dose of theophylline). Cimetidine, furosemide, methotrexate and drugs that block tubular secretion increase the concentration of ofloxacin in plasma.

Increases the concentration of glibenclamide in plasma.

When taken concomitantly with indirect anticoagulants (coumarin derivatives, including warfarin) it is necessary to control the blood coagulation system.

When administered with non-steroidal anti-inflammatory drugs, derivatives of nitroimidazole and methylxanthines, the risk of developing neurotoxic effects, including convulsions, increases.

At simultaneous appointment with glucocorticosteroids, the risk of rupture of tendons increases, especially in the elderly.

When administered with drugs that alkalinize urine (inhibitors of carbonic anhydrase, citrates, sodium bicarbonate), the risk of crystalluria and nephrotoxic effects increases.

Increases serum concentration of cyclosporine.

With a simultaneous appointment with hypoglycemic agents, both hypo- and hyperglycemia are possible, and in this connection it is necessary to monitor the concentration of glucose in the blood plasma.

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

Special instructions:

Renal / hepatic impairment

In patients with impaired liver or kidney function, it is necessary to monitor the concentration of ofloxacin in plasma. In severe renal and hepatic insufficiency, the risk of toxic effects increases (dose adjustment is required).

Prevent photosensitivity It is not recommended to be exposed to sunlight, ultraviolet rays (mercury quartz lamps, solarium).

Interval lengthening QT.

In patients who took fluoroquinolones, in very rare cases, an increase in the duration of the QT interval was observed. Caution should be exercised when using ofloxacin in patients with risk factors for prolonging the QT interval, such as advanced age, uncorrectable disorders of electrolyte blood composition (eg hypokalemia or hypomagnesemia), congenital QT interval prolongation syndrome,diseases of the cardiovascular system (heart failure, myocardial infarction, bradycardia), simultaneous use of drugs that extend

interval QT (antiarrhythmic drugs IA and III classes, tricyclic antidepressants, macrolides).

Peripheral Neuropathy

In patients who received fluoroquinolones, including ofloxacin, reported the development of sensory and sensory-motor neuropathy, which can have a rapid onset. If patients develop neuropathy symptoms, ofloxacin should be discontinued, thereby minimizing the possible risk of developing irreversible conditions.

Patients who are predisposed to develop seizures

Like other quinolones, ofloxacin should be used with caution in patients predisposed to developing seizures (patients with lesions of the central nervous system (CNS) in history, patients taking fenbufen or other non-steroidal anti-inflammatory drugs, or drugs that reduce the threshold of convulsive readiness of the brain, for example, theophylline).

Patients with disorders of the central nervous system

Elderly patients with CNS disorders (eg, with epilepsy,sharply expressed atherosclerosis of cerebral vessels) should take fluoroquinolones only under the close supervision of a physician.

In case of side effects from the CNS and / or allergic reactions, the drug should be discontinued.

Myasthenia gravis

On the background of treatment, myasthenia flow may worsen in predisposed

patients.

Porphyria

Against the background of treatment, there may be an increase in porphyria attacks in predisposed patients. During the treatment with ofloxacin, false-positive results may occur in the determination of opiates and porphyrins in the urine

Pseudomembranous colitis

With pseudomembranous colitis, confirmed colonoscopically and / or histologically, the drug should be discontinued immediately. Oral administration of vancomycin and metronidazole is indicated.

Tendonitis

Rarely developing tendonitis can lead to rupture of tendons (mainly

Achilles tendon), especially in elderly patients. In case of signs of tendinitis, it is necessary to immediately stop treatment, to make an immobilization of the Achilles tendon and consult an orthopedist.

Other

To prevent the hyperconcentration of urine and subsequent crystalluria, during

adequate hydration is recommended.

Can lead to false-negative results in the bacteriological diagnosis of tuberculosis (prevents the isolation Mycobacterium tuberculosis).

During the period of treatment can not be consumed ethanol.

When using the drug, women are not recommended to use hygiene tampons due to the increased risk of thrush development.

Ofloxacin is not a drug of choice for pneumonia caused by pneumococci. Not indicated in the treatment of acute tonsillitis.

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

Some adverse reactions such as dizziness, drowsiness and visual impairment can reduce the psychomotor reaction and the ability to concentrate, so during the treatment with the drug OFLOXACINE ZENTIVA Film coated tablets, care must be taken when driving vehicles and occupations by other potentially dangerous activities requiring increased concentration of attention and speed of psychomotor reactions.

Form release / dosage:

Film coated tablets 400 mg.

Packaging:For 10 tablets in a blister of PVC / A1.Each blister along with instructions for use is placed in a cardboard box.

Storage conditions:

At a temperature of 10 ° C to 25 ° C, in a dry place.

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:LS-000824

Date of registration:20.06.2011

The owner of the registration certificate:Zentiva c.s.Zentiva c.s. Czech Republic

Manufacturer: & nbsp

ZENTIVA, k.s. Czech Republic

Representation: & nbspZENTIVA PHARMA, LLCZENTIVA PHARMA, LLC

Information update date: & nbsp20.01.2014

Illustrated instructions

Instructions

Ofloxacin Zentiva (Ofloxacin Zentiva)