OXIFAN [Ofloxacin] 200 mg IV solution

OXIFAN

instructions for medical use of the medicinal product

Tradename

Oxifan, Оксифан

International non-proprietary name

Ofloxacin, Офлоксацин

Composition

Each vial (100 ml solution) contains:

active ingredient: ofloxacin C P   200 mg

excipients: sodium chloride, lactic acid, water for injection

Dosage form

Solution for infusion.

Pharmacotherapeutic group

The antimicrobial agent is a fluoroquinolone .

Pharmacological properties

Oksifan is an antimicrobial agent with a wide spectrum of antibacterial activity against gram-positive and gram-negative bacteria from the group of fluoroquinolones. The active substance is ofloxacin.

Pharmacodynamics

The mechanism of action of ofloxacin is due to the suppression of bacterial DNA replication by blocking DNA topoisomerase IV and DNA topoisomerase II (gyrase). It has a bactericidal effect.

Active against microorganisms producing β-lactamase, and fast-growing atypical mycobacteria., Incl. Staphylococcus aureus, Staphylococcus epidermidis, Neisseria gonorrhoeae, Neisseria meningitidis, Escherichia coli, Citrobacter spp., Klebsiella spp. (including Klebsiella pneumoniae), Enterobacter spp., Hafnia spp., Proteus spp. (including Proteus mirabilis, Proteus vulgaris - indole positive and indole negative), Salmonella spp., Shigella spp. (including Shigella sonnei), Yersinia enterocolitica, Campylobacter jejuni, Aeromonas hydrophila, Pseudomonas aeruginosa, Vibrio cholerae, Vibrio parahaemolyticus, Haemophilus influenzae, Chlamydia spp., Legionella spp., Serratia spp., Providencia spp., Haemophilus ducreyi, Bordetella parapertussis, Bordetella parapertussis pertussis, Moraxella catarrhalis, Propionibacterium acnes, Staphylococcus spp., Brucella spp.

Enterococcus faecalis, Streptococcus pyogenes, Streptococcus pneumoniae and viridans, Serratia marcescenes, Pseudomonas aeruginosa, Acinetobacter, Mycoplasma hominis and pneumoniae, Mycobacterium tuberculosis, as well as Mycobacterium fortuitum, Ureplasma urealyticum, Clostridium perfringens, Corynebacter. Listeria monocytogenes, Gardnerella vaginalis.

In most cases, insensitive: Nocardia asteroides, anaerobic bacteria (Bacteroides spp., Peptococcus spp., Peptostreptococcus spp., Eubacterium spp., Fusobacterium spp., Clostridium difficile).

Not active against Treponema pallidum.

Pharmacokinetics

After a single infusion of 200 mg of ofloxacin over 60 minutes, C _max is 2.7 μg / ml, 12 hours after administration, the concentration of ofloxacin is 0.3 μg / ml.

Steady-state concentrations are reached after 4 infusions. With the on / in the introduction of ofloxacin at a dose of 200 mg every 12 hours for 7 days, the average maximum and minimum equilibrium concentrations are 2.9 and 0.5 μg / ml, respectively. Ofloxacin widely penetrates into many tissues and body fluids, incl. into saliva, bronchial secretions, bile, lacrimal and cerebrospinal fluid, pus, into the lungs, prostate gland and skin.

Plasma protein binding is 20-25%.

Ofloxacin is partially (5%) biotransformed in the liver. T _{1 / 2} - 6-7 hours. Up to 80% of the dose is excreted by the kidneys unchanged, a small part - with feces.

With hemodialysis, 10-30% of the drug is removed. In patients with impaired renal function (CC 50 ml / min or less), T _1/2 of ofloxacin increases.

Indications for use

·   respiratory tract infections (bronchitis, pneumonia);

·   infections of ENT organs (sinusitis, pharyngitis, otitis media, laryngitis);

·   skin and soft tissue infections;

·   bone and joint infections;

·   infectious and inflammatory diseases of the abdominal cavity (including infections of the gastrointestinal tract and biliary tract);

·   infections of the kidneys (pyelonephritis) and urinary tract (cystitis, urethritis);

·   infections of the pelvic organs (endometritis, salpingitis, oophoritis, cervicitis, parametritis, prostatitis) and genital organs (colpitis, orchitis, epididymitis);

·   gonorrhea;

·   chlamydia;

·   septicemia;

·   meningitis;

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

Contraindications

·   hypersensitivity to the drug;

·   epilepsy (including history);

·   lowering the threshold for convulsive readiness (including after a traumatic brain injury, stroke, or inflammatory processes in the central nervous system);

·   age up to 18 years (until the growth of the bones of the skeleton is completed);

·   pregnancy;

·   breastfeeding period .

Dosage and administration

The drug is administered intravenously. Doses are selected individually depending on the location 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.

Therapy begins with intravenous drip (within 30-60 minutes) administration of the drug at a dose of 200 mg. When the patient's condition improves, they are transferred to oral administration of the drug in the same daily dose.

For urinary tract infections , the drug is prescribed 100 mg 1-2 times / day; with infections of the kidneys and genital organs - from 100 to 200 mg 2 times / day; with infections of the respiratory tract, as well as ENT organs, infections of the skin and soft tissues, bones and joints, infections of the abdominal cavity, septic infections - 200 mg 2 times / day. If necessary, the dose is increased to 400 mg 2 times / day.

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

In patients with impaired renal function (with CC from 50 to 20 ml / min), a single dose should be 50% of the average recommended with a multiplicity of appointments 2 times / day. You can enter a full single dose 1 time / day. With CC less than 20 ml / min , a single initial dose is 200 mg, then the drug is administered at 100 mg / day every other day.

With peritoneal dialysis and hemodialysis , the drug is administered at 100 mg every 24 hours.

In hepatic insufficiency , the maximum daily dose is 400 mg.

Special instructions and precautions

Oksifan is not the drug of choice for pneumonia caused by pneumococci, is not indicated for the treatment of acute tonsillitis.

Not recommended for more than 2 months. Against the background of the use of the drug should not be exposed to sunlight, UV radiation.

If side effects from the central nervous system, allergic reactions, pseudomembranous colitis occur, the drug should be discontinued.

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

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

Alcohol should be avoided during treatment with the drug.

Influence on the ability to drive vehicles and mechanisms

Use with caution in patients whose activities are associated with the need for a high concentration of attention and speed of psychomotor reactions.

Use during pregnancy and during breastfeeding

Use during pregnancy and during breastfeeding is contraindicated.

Interaction with other drugs

With simultaneous use ofloxacin reduces the clearance of theophylline by 25% (with simultaneous use, the dose of theophylline should be reduced).

With the simultaneous use of cimetidine, furosemide, methotrexate and drugs that block tubular secretion, increase the concentration of ofloxacin in plasma.

Ofloxacin increases the plasma concentration of glibenclamide.

When taken simultaneously with indirect anticoagulants-vitamin K antagonists, it is necessary to monitor the state of the blood coagulation system.

When used together with NSAIDs, nitroimidazole derivatives and methylxanthines, the risk of developing neurotoxic effects increases.

With simultaneous appointment with GCS, the risk of tendon rupture increases, especially in the elderly.

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

Pharmaceutical interaction

Ofloxacin solution is compatible with the following infusion solutions: isotonic sodium chloride solution, Ringer's solution, 5% fructose solution, 5% dextrose (glucose) solution.

Side effect

From the digestive system: gastralgia, anorexia, nausea, vomiting, diarrhea, flatulence, abdominal pain, increased activity of hepatic transaminases, hyperbilirubinemia, cholestatic jaundice, pseudomembranous enterocolitis.

From the side of the central nervous system and peripheral nervous system: headache, dizziness, uncertainty of movements, tremor, convulsions, numbness and paresthesia of the extremities, intense dreams, nightmares, psychotic reactions, anxiety, psychomotor agitation, phobias, depression, confusion, hallucinations, increased intracranial pressure, impaired color perception, diplopia, impaired taste, smell and balance.

From the musculoskeletal system: tendinitis, myalgia, arthralgia, tendosynovitis, tendon rupture.

From the side of the cardiovascular system: tachycardia, decrease in blood pressure (with a sharp decrease in blood pressure, the administration is stopped), vasculitis, collapse.

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

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

Dermatological reactions: pinpoint hemorrhages, bullous hemorrhagic dermatitis, papular rash indicating vascular damage (vasculitis).

Allergic reactions: skin rash, pruritus, urticaria, allergic pneumonitis, allergic nephritis, eosinophilia, fever, angioedema, bronchospasm, Stevens-Johnson syndrome and Lyell's syndrome, photosensitivity, erythema multiforme exudative, anaphylactic shock.

Others: dysbacteriosis, superinfection, hypoglycemia (in diabetic patients), vaginitis.

Local reactions: pain, redness at the injection site, thrombophlebitis.

Overdose

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

Treatment: gastric lavage, symptomatic therapy.

Storage conditions

Store in a dry and dark place, at a temperature not exceeding 30 ⁰ С.

Keep out of the reach of children.

Best before date

3 years. Do not use after the expiry date stated on the packaging.

Holiday conditions

Released by prescription.

Release form

1 bottle of 100 ml with instructions for use in a cardboard box.