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

Ofloxacin is a bactericidal antimicrobial drug of a wide spectrum actions from the group of fluoroquinolones. The main mechanism of action of quinolones is specific inhibition of bacterial DNA-gyrase. DNA-gyrase is necessary for replication, transcription, repair and recombination of bacterial DNA. Its inhibition leads to unwinding and destabilization bacterial DNA and, as a result, to the death of a microbial cell.

Ofloxacin is highly active (minimum inhibitory concentration <0.5 mg / l) for the following microorganisms: Aeromonas hydrophila, Moraxella catarrhalis, Brucella spp, Chlamydia trachomatis, Citrobacter freundii, Clostridium perfringens, Enterobacter aerogenes, Enterobacter cloacae, Escherichia coli, Haemophilus ducreyi, Haemophilus influenzae, Haemophilus parainjluenzae, Helicobacter coli, Helicobacter jejuni, Klebsiella oxytoca, Legionella pneumophila, Morganella morganii, Mycoplasma hominis, Neisseria gonorrhoeae, Neisseria meningitidis, Plesiomonas spp., Proteus mirabilis, Proteus vulgaris, Salmonella enterica, Serratia marcescens, Shigella spp., Staphylococcus spp. (coagulase-negative), including Staphylococcus aureus (methicillin-sensitive), Yersinia enterolytica.

Moderately sensitive to ofloxacin Acinetobacter calcoaceticus, Anaerobic Gram V positive cocci (anaerobic Gram-positive cocci), Bacteroides fragilis, Chlamydia psittaci, Gardnerella vaginalis, Mycobacterium tuberculosis, Mycobacterium leprae, Pseudomonas aeruginosa, Streptococcus pneumoniae, Streptococcus spp. Resistant microorganisms

(minimal suppressive concentration> 1 mg / l): Acinetobacter baumannii,

Clostridium difficile, Enterococcus spp., Listeria monocytogenes. Staphylococcus aureus (methicillin-resistant), Nocardia asteroides.

He acts on Treponema pallidum.

Pharmacokinetics:

The maximum serum concentration with a 30-minute intravenous infusion of the drug is achieved at the end of the infusion.

Concentrations of ofloxacin in serum after a 30-minute intravenous infusion of the drug OFLOXACINE ZENTIVA.

Dose	Serum concentration of ofloxacin after infusion	Serum concentration of ofloxacin 4 hours after infusion	Serum concentration of ofloxacin 12 hours after infusion
100 mg	2.9 mg / L	0.5 mg / l	0,2 mg / l
200 mg	5.2 mg / l	1.1 mg / l	0.3 mg / l

In the course of the use of ofloxacin, the serum concentration does not increase significantly (the accumulation factor when administered twice a day is 1,5).

Ofloksatsin well penetrates into many body fluids and tissues, including saliva, bronchial secretions, bile, tear and spinal fluid, pus, into the lungs, the prostate, the skin, through the blood-brain barrier, the placental barrier, is secreted with the mother's milk.

Ofloxacin is subject to partial (5%) metabolism in the liver. Binding to plasma proteins is 20 - 25%. The half-life of ofloxacin is 6-7 hours. Up to 80% of the injected drug is excreted by the kidneys unchanged, a small part of the active substance is excreted through the gastrointestinal tract.

In patients with impaired renal function (creatinine clearance 50 ml / min or less), the half-life of ofloxacin increases.

In elderly patients, the half-life increases, but the maximum serum concentration does not change.

Indications:

Infectious-inflammatory diseases caused by microorganisms sensitive to ofloxacin:

- respiratory infections, with the exception of cases of established pneumococcal infection or suspected of it (some pneumococcal strains are only partially sensitive to ofloxacin, therefore it should not be used as the first-choice drug for community-acquired pneumonia caused by pneumococcus);

- infection of the ear, throat, nose (AOPorgan organs), except for cases of acute tonsillitis caused by βhemolytic streptococcus (some strains βhemolytic streptococcus are only partially sensitive to ofloxacin, so it should not be used as a first-choice drug for acute tonsillitis caused by βhemolytic streptococcus);

- infection of the abdominal cavity and biliary tract;

- infection of the kidneys, urinary tract, prostate; gonococcal

urethritis;

- infection of bones and joints;

- infections of the skin and soft tissues;

- female genital organs;

- septicemia;

- prevention of infections caused by floxacin-sensitive microorganisms in patients with a predisposition to the development of infections (eg, neutropenia).

Contraindications:

- Hypersensitivity to ofloxacin, other quinolones or excipients of the drug;

- Epilepsy (including in the anamnesis);

- Defeat of tendons with previous treatment with fluoroquinolones;

- Age to 18 years (until the skeleton has been completed);

- Pregnancy;

- Breastfeeding period.

Carefully:

in patients with atherosclerosis of cerebral vessels, cerebral circulatory disorders in history, organic lesions of the central nervous system, chronic renal failure, hepatic insufficiency, myasthenia gravis, hepatic porphyria, deficiency of glucose-6-phosphate dehydrogenase, diabetes mellitus, impaired electrolyte blood composition (eg, hypokalemia, hypomagnesemia ), the syndrome of congenital lengthening interval QT, diseases of the cardiovascular system (heart failure, myocardial infarction, bradycardia), psychoses and other psychiatric disorders in the anamnesis; decrease in the threshold of convulsive activity (after craniocerebral trauma, stroke, inflammatory processes in the central nervous system), elderly age, simultaneous use of drugs that extend the interval QT (antiarrhythmic IA and III classes, tricyclic and tetracyclic antidepressants, neuroleptics, macrolides, antifungal, imidazole derivatives, some antihistamines, including antihistamines. astemizole, terfenadine, ebastine), preparations for non-induction general anesthesia from the barbiturate group, drugs that lower blood pressure.

Pregnancy and lactation:

Use of ofloxacin during pregnancy and during breastfeeding it is contraindicated.

Dosing and Administration:

The dosage regimen depends on the type and severity of the infection and the function of the kidneys.

Dosing regimen in adults with normal kidney function (creatinine clearance more than 50 ml / min)

In the treatment of infections caused by microorganisms that are sensitive to ofloxacin, the recommended dose is 200 mg twice a day or 400 mg once a day. Usually the daily dose is 400 mg. In case of treatment of severe infections or in patients with overweight, the daily dose can be increased to 600 mg.

Dosage regimen for renal dysfunction

Creatinine clearance

Single dose (mg) *

Multiplicity of the introduction

50-20 ml / min

100-200

1 time per day (every 24 hours)

<20 ml / min ** or hemodialysis and peritoneal dialysis

100 or 200

1 time per day (every 24 hours)

1 every 2 days (every 48 hours)

* In accordance with the testimony.

** It is recommended to monitor

serum concentrations of ofloxacin in patients with severe renal dysfunction or in patients on dialysis.

Dosage regimen for violations of liver function

In case of severe impairment of liver function (eg, with cirrhosis of the liver with ascites), it is not recommended to exceed the dose of ofloxacin 400 mg / day.

Dosage regimen in elderly patients

The age of the patient, as such, does not require dose adjustment of ofloxacin. However, when the drug is used in elderly patients, special attention should be paid to the function of the patient's kidneys, since in the event of a decrease, a corresponding correction of the dosing regimen may be required (see above).

Dosage regimen for infectious-inflammatory diseases Urinary tract infection - 100 mg

1 - 2 times a day; infection of the kidneys and genitals - from 100 mg twice a day to 200 mg twice a day; respiratory tract infections, as well as ENT organs, skin and soft tissue infections, infections of bones and joints, abdominal infections, bacterial enteritis, septic infections - 200 mg

2 times a day.If necessary, increase the dose to 400 mg twice a day.

For the prevention of infections in patients with a marked decrease in immunity - 400-600 mg / day.

Administration of the drug

The ofloxacin solution is intended only for slow infusion administration. Intravenous infusion is performed once or twice a day. The duration of the infusion should be at least 30 minutes for each dose of ofloxacin 200 mg. This is especially important if ofloxacin is administered concomitantly with other drugs that can reduce blood pressure or means for non-general general anesthesia from the barbiturate group. The daily dose to 400 mg ofloxacin can be administered once a day. In this case, it is preferable to administer the drug in the morning.

A daily dose of more than 400 mg should be divided into two parts and administered at 12-hour intervals.

Compatibility with ofloxacin with

infusion solutions (see "Interaction with Other Drugs, Laboratory and Diagnostic Tests").

Administration of the drug OFLOXACINE ZENTIVA After opening the vial should be done immediately. Duration of treatment The duration of treatment depends on the severity of the disease. Like any treatment with antimicrobial drugs, ofloxacin should be continued for at least 48-72 hours after the normalization of body temperature or if there is evidence of eradication of the bacterial agent.

A few days after the improvement of the patient's condition, the onloxacin started in the form of intravenous infusions can be continued by taking the drug inside at the same doses.

Side effects:

The following side effects are given according to the following gradations of their frequency: very frequent (> 1/10), frequent (> 1/100, <1/10); infrequent (> 1/1000, <1/100); rare (> 1/10000, <1/1000); very rare (<1/10000) (including individual messages), unknown frequency (according to available data, set the frequency

occurrence is not possible).

Violations from the heart and blood vessels Frequent: phlebitis.

Infrequent: arterial hypotension.

During the infusion of ofloxacin, a decrease in arterial pressure is possible, accompanied by the development of sinus tachycardia, which in very rare cases is strongly pronounced up to the development of collapse.In the case of a significant reduction in blood pressure should immediately stop the infusion of the drug. Rare: sinus tachycardia, "tides" of blood to the skin of the face.

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

Violations of the blood and lymphatic system

Very rare: Anemia, hemolytic anemia, leukopenia, thrombocytopenia.

Individual cases: agranulocytosis, pancytopenia, oppression of the medullar

hematopoiesis.

Disorders from the nervous system Infrequent: dizziness, headache.

Rare: drowsiness, paresthesia, dysgeusia (a disorder of perception of taste), parosmia (a disorder of perception of a smell).

Very rare: peripheral sensory neuropathy, peripheral sensory-motor neuropathy, seizures, epileptic seizures, extrapyramidal disorders, including tremor, and other disorders of muscle coordination.

Unknown frequency: increased intracranial pressure.

Disturbances on the part of the organ of sight

Infrequent: irritation of the mucous membrane of the eye.

Rare: visual impairment.

Hearing impairments and labyrinthine infringements Infrequent: Vertigo.

Very rare: hearing impairment (ringing in the ears), hearing loss.

Disturbances from the respiratory system, chest and mediastinal organs Infrequent: dry cough, nasopharyngitis, rhinitis.

Rare: shortness of breath, bronchospasm.

Very rare (isolated cases): allergic pneumonitis, pronounced dyspnea. Disorders from the gastrointestinal tract

Infrequent: abdominal pain, diarrhea, nausea, vomiting.

Rare: Enterocolitis (in some cases, hemorrhagic).

Unknown frequency: constipation, flatulence.

Very rare: pseudomembranous colitis.

Disturbances from the liver and bile ducts

Rare: an increase in the activity of "hepatic" enzymes, such as alanine amine transferase (ALT), aspartate aminotransferase (ACAT), lactate dehydrogenase (LDH), gamma-glutamyltransferase (GGT) and / or alkaline phosphatase (ACF), and / or bilirubin concentrations in the blood.

Very rare: cholestatic jaundice; individual cases: hepatitis, which can be severe.

Disorders from the kidneys and urinary tract Rare: increased serum creatinine concentration.

Very rare: acute renal failure.

Individual cases: acute interstitial nephritis.

Unknown frequency: increased urea concentration in the blood.

Disturbances from the skin and subcutaneous tissues

Infrequent: itching, rash.

Rare: urticaria, hyperhidrosis, pustular rash.

Very rare: multiforme exudative erythema, toxic epidermal necrolysis, photosensitivity reactions, drug rash, purpura, vasculitis, which in exceptional cases can lead to skin necrosis.

Individual cases: Stevens-Johnson syndrome.

Unknown frequency: spot hemorrhages (petechiae), bullous haemorrhagic dermatitis.

Disturbances from the musculoskeletal and connective tissue.

Rare: tendonitis.

Very rare: arthralgia; myalgia; tendon rupture (Achilles tendon) (as with the use of other fluoroquinolones, this side effect can develop within 48 hours after the initiation of treatment and can be bilateral), isolated cases: rhabdomyolysis and / or myopathy, muscle weakness, which is especially important for patients with pseudo-paralytic myasthenia .

Disorders from the metabolism and nutrition

Rare: anorexia.

Very rare (isolated cases): hypoglycemia, in patients with diabetes mellitus,

receiving treatment with hypoglycemic agents; Attacks of porphyria in patients with porphyria.

Infectious and parasitic diseases

Infrequent: fungal infections, resistance of pathogenic microorganisms.

Unknown frequency: intestinal dysbacteriosis, vaginitis, vaginal discharge.

Common disorders and disorders together

Frequent: pain and redness at the site of infusion, phlebitis.

Immune system disorders

Rare: anaphylactic reactions, anaphylactoid reactions, angioedema. Very rare: anaphylactic shock, anaphylactoid shock.

Individual cases: allergic pneumonitis.

Unknown frequency: allergic nephritis, eosinophilia.

Disorders of the psyche

Infrequent: agitation, sleep disorders, insomnia.

Rare: psychotic reactions (for example, hallucinations), anxiety, anxiety, nervousness, confusion, nightmares, depression.

Individual cases: psychotic reactions and depression with self-harm, in rare cases, up to suicidal thoughts or attempts.

Overdose:

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

Treatment: symptomatic therapy. The specific antidote is unknown. Excretion of the drug can be accelerated in the course of forced diuresis. About 15-25% of the drug is excreted by hemodialysis.

Interaction:

Compatible with the following infusion solutions: isotonic sodium solution

chloride, Ringer's solution, 5% fructose solution, 5 % solution of dextrose.

Do not mix with heparin (risk of precipitation).

Reduces the clearance of theophylline by 25% (with simultaneous use should reduce the dose of theophylline).Drugs that block tubular secretion, such as probenecid, cimetidine, furosemide, methotrexate increase the concentration of ofloxacin in plasma.

- Increases the concentration of glibenclamide in blood plasma.

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

When used with non-steroidal anti-inflammatory drugs, derivatives of nitroimidazole and methylxanthines,lowering the threshold of convulsive activity of the brain, the risk of developing neurotoxic effects, including convulsions, increases.

When used simultaneously with glucocorticosteroids, the risk of rupture of tendons increases, especially in the elderly.

With the use of drugs, urine alkalizing (carbonic anhydrase inhibitors, citrates, sodium bicarbonate), increases the risk of crystalluria and nephrotoxic effects.

Increases serum concentration of cyclosporine.

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

When applied simultaneously with ofloxacin preparations able to reduce blood pressure and / or medicaments for neingalyatsionnyh general anesthesia barbiturate group possible from a sudden and significant decrease in blood pressure, so it requires especially careful monitoring the functional condition of the cardiovascular system.

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,

ebastin), the occurrence of paroxysms of ventricular tachycardia such as "pirouette".

Special instructions:

It is not a drug of choice for pneumonia caused by pneumococci.

Not indicated in the treatment of acute tonsillitis.

It is not recommended to use more than 2 months, exposed to sunlight, ultraviolet rays (mercury-quartz lamps, solarium).

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

Elderly patients with CNS disorders (for example, with epilepsy, severe atherosclerosis of the cerebral vessels) should take fluoroquinolones only under close supervision of the doctor.

In the event of side effects from the central nervous system and / or allergic reactions, drug withdrawal is necessary.

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.

In patients taking fluoroquinolones, in very rare cases there was an increase in the duration of the interval QT. Caution should be exercised when taking fluoroquinolones, including ofloxacin, in a patientwith risk factors for lengthening the interval QT, such as: old age, uncorrectable imbalance of electrolytes (eg, hypokalemia or hypomagnesemia), congenital lengthening interval syndrome QT, diseases of the cardiovascular system (heart failure, myocardial infarction, bradycardia), simultaneous use of drugs that extend the interval QT (antiarrhythmic drugs IA and III classes, tricyclic antidepressants, macrolides).

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

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

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

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).

To prevent the hyperconcentration of urine and subsequent crystalluria, during the treatment it is recommended to conduct adequate hydration.

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.

During the treatment you can not drink alcohol.

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

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

Effect on the ability to drive transp. cf. and fur:During the period of drug treatment OFLOXACINE ZENTIVA, solution for infusions, care must be taken when driving vehicles and engaging in other potentially dangerous activities that require increased concentration and speed of psychomotor reactions.

Form release / dosage:

Solution for infusions 2 mg / ml.

Packaging:For 100 ml of the drug in a vial of colorless glass (hydrolytic class I or II), sealed with a rubber stopper and an aluminum cap under running-in with a lid type "flip off". Each vial with the instruction for use is placed in a cardboard box pack.

Storage conditions:

In a dry, dark place at a temperature of 10 to 25 ° C. Keep out of the reach of children.

Shelf life:

3 of the year.

Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:П N015708 / 02

Date of registration:25.07.2011

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

Manufacturer: & nbsp

FREZENIUS JV, CJSC Russia

Representation: & nbspZENTIVA PHARMA, LLCZENTIVA PHARMA, LLC

Information update date: & nbsp21.01.2014

Illustrated instructions

Instructions

Ofloxacin Zentiva (Ofloxacin Zentiva)