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

The bactericidal effect of ofloxacin is associated with inhibition of DNA gyrase and topoisomerase IV, which leads to a disruption in the replication of bacterial DNA and the death of microbial cells. Ofloxacin has a wide spectrum of antimicrobial action, including microorganisms resistant to other antibiotics, including strains that produce beta-lactamases.

It is active against gram-positive microorganisms: Staphylococcus aureus (methicillin-sensitive strains), Staphylococcus epidermidis; most gram-negative aerobic microorganisms: Aeromonas spp., Campylobacter jejuni, Citrobacter (diversus) koseri, Chlamydia trachomatis, Chlamydophila psittaci, Chlamydophila pneumoniae, Enterobacter aerogenes, Enterobacter cloacae, Escherichia coli, producing and not producing beta-lactamase strains Haemophilus influenzae, Haemophilus parainfluenzae, Hafnia spp., Klebsiella pneumoniae, Klebsiella oxytoca, Legionella spp., producing and not producing beta-lactamase strains Neisseria gonorrhoeae, Neisseria meningitidis, Proteus mirabilis, Proteus vulgaris, Plesiomonas spp., Salmonella spp., Shigella spp., Vibrio cholerae, Vi brio parahaemolyticus, Yersinia enterocolitica.

Different sensitivity to the drug has: Acinetobacter spp., Citrobacter freundii, Gardnerella vaginalis., Pseudomonas aeruginosa, Streptococcus pneumoniae (penicillin-sensitive and penicillin resistant strains), Streptococcus pyogenes, Streptococcus viridans, Streptococcus bovis, Streptococcus agalactae, Serratia marcescens, Mycobacterium fortuitum, Mycobacterium tuberculosis, Mycoplasma hominis, Mycoplasma pneumoniae.

Are resistant to ofloxacin: Nocardia asteroids, most anaerobes, including Peptostreptococcus spp., Eubacterium spp., Fusobacterium spp., Clostridium difficile; Treponema pallidum, Ureaplasma urealyticum.

Pharmacokinetics:

At the end of a 30-minute intravenous (iv) infusion of 200 mg ofloxacin, the serum antibiotic concentrations are 5.2 mg / L, 4 hours after the infusion, -1.1 mg / L, after 12 hours - 0.3 mg / L . Quickly penetrates and is well distributed in many organs, tissues and fluids of the body, penetrates into cells. Therapeutically significant concentrations, exceeding the concentration in the blood serum,are observed in the interstitial tissue, saliva, sputum, lung tissue, myocardium, bones, mucosa and intestinal wall, peritoneal fluid, pancreatic juice and pancreatic tissue, prostate, semen, organs of the female reproductive system, skin and subcutaneous tissue; penetrates into leukocytes and alveolar macrophages. The volume of distribution is 120 liters. It penetrates well through the blood-brain barrier, reaching therapeutic concentrations; in high concentrations passes through the hematoplacental barrier, excreted in breast milk. About 25% of the administered dose binds to blood plasma proteins. The half-life period (T1 / 2) is 4.7-7 hours, and does not depend on the administered dose. With multiple administrations, the cumulative effect is not expressed, serum concentrations increase slightly. After administration in a dose of 200 mg, the total clearance is 258 ml / min. Ofloxacin is allocated mainly kidneys in an unchanged form - 80-90% of the administered dose, creating high concentrations of antibiotic in the urine. In small quantities is excreted through the intestine. Biotransformation in the liver undergoes about 5% of the administered dose; major metabolites - ofloxacin Noxide and N-dimethylofloxacin, which are secreted through the kidneys.In patients with renal failure, the half-life of ofloxacin increases; total and renal clearance decrease in proportion to the decrease in creatinine clearance. At the time of hemodialysis, 10-30% of the drug is removed.

Indications:

- Infections of the lower respiratory tract (acute and chronic bronchitis, pneumonia, including those caused by intracellular or atypical pathogens, with the exception of pneumococcal infections *);

- acute, chronic and recurrent infections of the ENT organs (except for cases of acute tonsillitis) *;

- infections of the skin and soft tissues;

- infection of bones (osteitis, osteomyelitis) and joints;

- infections of the abdominal cavity, including bile duct infection;

- intestinal infections, incl. Escherichiosis, salmonellosis, shigellosis, cholera, yersiniosis;

- Infectious-inflammatory diseases of the pelvic organs (pelvioperitonitis, salpingitis, oophoritis, tubo-ovarian abscesses, endometritis);

- complicated and uncomplicated infectious and inflammatory diseases of the kidney and urinary tract, prostate and urethra, including gonococcal etiology;

- sepsis;

- prevention of bacterial infections in patients with impaired immune status, including neutropenia.

* Since strains Streptococcus spp. moderately sensitive to ofloxacin, the drug should not be prescribed as a first choice for the treatment of pneumonia caused by pneumococci, as well as acute tonsillitis (β-hemolytic streptococcus).

Contraindications:

Hypersensitivity to fluoroquinolones; children under 18 years of age, pregnancy, lactation; patients with deficiency of glucose-6-phosphate dehydrogenase; patients with epilepsy (including in the anamnesis), lowering convulsive threshold (including after TBI, stroke or inflammatory processes in the central nervous system); if there are indications of a lesion of the tendons against the background of the previous administration of fluoroquinolones.

Carefully:

Severe atherosclerosis of cerebral vessels, cerebral circulation disorders, incl. in the anamnesis, other organic lesions of the central nervous system, chronic renal failure, lengthening of the interval QT.

Pregnancy and lactation:Contraindicated.

Dosing and Administration:

Ofloxabol® is administered iv by drip; the duration of administration of 200 mg of Ofloxabol® is 30 minutes. Doses are selected individually, depending on the location and severity of the infection,as well as the sensitivity of microorganisms and the general condition of the patient. In patients with normal renal function, the medicated single dose of Ofloxabol® is 200 mg, which is administered twice a day at intervals of 12 hours. When the patient's condition is improved, they are transferred to oral intake of the drug at the same daily dose.

For the treatment of severe infections, including in patients with impaired immune status, a single dose can be increased to 400 mg, which is injected / drip 2 times a day.

In patients with impaired renal function, the first, loading, dose is the same as in patients with normal renal function and depends on the localization and severity of the infection. Further doses and dosage regimens are set taking into account the value of creatinine clearance (see table).

Creatinine clearance, ml \ min	>80	80-50	50-20	<20
Dosing regimen	200-400 mg every 12 hours	200-400 mg every 12 hours	200 mg every 24 hours	100 mg every 24 hours
With hemodialysis and peritoneal dialysis: 100 mg every 24 hours

Solution Ofloxabol® It is impossible to mix and dissolve in it other medicines.

For infusion of Ofloxabol® it is preferable to use a separate system for intravenous infusions.

If there is an unused solution of Ofloxabol in the vial®, it should be disposed of and not used for other patients.

Ofloxabol ® infusion solution 2 mg / ml is compatible with 0.9 % solution of sodium chloride, 5% solution of dextrose.

Side effects:

The therapy with Ofloxabol® is usually well tolerated; side reactions under specified dosages and modes of administration are rare, and in most cases are stopped independently without requiring discontinuation of therapy; severe side effects are described as single episodes.

From the digestive system: nausea, vomiting, diarrhea, flatulence, abdominal pain, increased activity of "liver" transaminases, hyperbilirubinemia, cholestatic jaundice, loss of appetite, pseudomembranous enterocolitis.

From the nervous system and sense organs: headache, dizziness, lack of movement, tremors, convulsions, paresthesia and numbness of extremities, "nightmare" dreams, psychotic reactions, anxiety, a state of excitation, phobia, depression, confusion, hallucinations, increased intracranial pressure; violation of color perception, diplopia, violation of taste, smell, hearing and balance.

From the side of the musculoskeletal system: tendonitis, myalgia, arthralgia, tendon rupture.

From the side of the cardiovascular system: arterial hypotension, collapse (with a sharp decrease in blood pressure, the introduction is discontinued), tachycardia, arrhythmia (risk factor - hypokalemia, diseases and taking medications that promote the lengthening of the interval Q-T).

Allergic reactions: skin rash, itching, hives, allergic pneumonitis, allergic nephritis, eosinophilia, fever, angioedema, bronchospasm; multiforme exudative erythema (including Stevens-Johnson syndrome) and toxic epidermal necrolysis (Lyell's syndrome), photosensitivity, vasculitis, bullous hemorrhagic dermatitis, anaphylactic shock.

From the blood system and hematopoiesis: leukopenia, agranulocytosis, anemia, thrombocytopenia, pancytopenia, hemolytic and aplastic anemia.

From the urinary system: acute interstitial nephritis, impaired renal function, hypercreatininaemia, increased urea concentration.

Local Reactions: pain, hyperemia in the place of intravenous administration, thrombophlebitis.

Other: dysbacteriosis of the intestine, superinfection, hyper- or hypoglycemia (in patients with diabetes mellitus against the background of taking antidiabetic drugs), exacerbation of porphyria, vaginitis.

Overdose:

Symptoms: dizziness, confusion, inhibition, disorientation, convulsions, drowsiness, vomiting, symptoms of irritation of the mucous membranes.

Treatment: forced diuresis, symptomatic therapy; for relief of neurological disorders (convulsive syndrome) use diazepam.

Interaction:

Simultaneous reception of Ofloxabol® and barbiturates can lead to a sharp drop in blood pressure. Therefore, with the simultaneous use of barbiturates, for example as an anesthetic, and Ofloxabol®, cardiovascular function should be monitored.

Reduces the clearance of theophylline by 25% (with simultaneous use should reduce the dose of theophylline).

Theophylline, fenbufen, other non-steroidal anti-inflammatory drugs: their simultaneous administration with Ofloxabol® can reduce the threshold of convulsive activity.

Ofloxabol® practically does not affect the concentration of theophylline in blood serum.

Probenecid, cimetidine, furosemide, methotrexate reduce the tubular secretion of Ofloxabol®, which, when taken concomitantly, leads to an increase in the concentration of antibiotic in the serum, increasing the likelihood of unwanted drug reactions.

Vitamin K antagonists: simultaneous administration with Ofloxabol® leads to an increase in the activity of coumarin derivatives, which requires monitoring of the parameters of the blood coagulation system.

Glibenclamide: with simultaneous reception with Ofloxabol®, there may be a slight increase in the level of hypoglycemic drugs and, as a consequence, hypoglycemia, which requires monitoring of blood glucose levels.

With simultaneous administration with glucocorticosteroids, the risk of rupture of tendons increases, especially in elderly patients.

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

The solution of Ofloxabol® should not be mixed with heparin due to the risk of precipitation in solution.

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

Special instructions:

Ofloxabol ® is not a drug of choice for diseases of the upper and lower respiratory tract caused by pneumococci.

As with other fluoroquinolones, due to possible photosensitization, it is recommended to avoid prolonged exposure to direct sunlight or ultraviolet radiation.

Rarely developing tendonitis can lead to rupture of tendons (mainly Achilles tendon), especially in elderly patients. In case of signs of tendonitis, it is necessary immediately to stop treatment, to immobilize the Achilles tendon and consult an orthopedist.

In the presence of severe liver disease requires an individual selection of the dose depending on the degree of impaired liver function.

If you experience severe or prolonged diarrhea during or after treatment with Ofloxabol®, the development of pseudomembranous colitis should be ruled out (immediate withdrawal of the drug and oral administration of vancomycin and metronidazole is required).

Ofloxabol® inhibits growth Mycobacterium tuberculosis, which can lead to false-negative results of bacteriological tests in patients tuberculosis.

Against the backdrop of treatment, myasthenia flow may worsen, and porphyria attacks may be more frequent in predisposed patients.

When determining the porphyrin in urine, a false positive result can be determined.

For the treatment of mixed aerobic-anaerobic infections (peritonitis, endometritis, etc.), it is recommended to combine Ofloxabol® with one of the anti-anaerobic antibiotics that have anti-anaerobic activity.

Form release / dosage:

Solution for infusions 2 mg / ml.

Packaging:

For 100 ml of the drug in bottles of glass with a capacity of 100 ml.

1 A bottle or bottle with instructions for use is placed in a pack of cardboard.

Storage conditions:

In the dark place at a temperature not higher 25 FROM. Keep out of the reach of children. Do not freeze.

Shelf life:

2 of the year.

Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:LSR-005198/09

Date of registration:29.06.2009 / 10.12.2014

Expiration Date:Unlimited

The owner of the registration certificate:PREBAND PFC, LLCPREBAND PFC, LLC Russia

Manufacturer: & nbsp

PREBAND PFC LLC Russia

Information update date: & nbsp16.06.2017

Illustrated instructions

Instructions

Ofloxabol® (Ofloxabol)