Ofloxacin, 2 mg/ml 100 ml

Ofloxacin is bactericidal, antibacterial.

Acts on the bacterial enzyme DNA-hyraza, which provides superspiralization and thus the stability of bacterial DNA (destabilization of DNA chains leads to their death). It has a wide spectrum of action, has a bactericidal effect

Pharmacodynamics

Active against beta-lactamase-producing microorganisms and fast-growing atypical mycobacteria. Sensitive: Staphylococcus aureus, Staphylococcus epidermidis, Neisseria gonorrhoeae, Neisseria meningitidis, Escherichia coli, Citrobacter, Klebsiella spp, (including Klebsiella pneumoniae), Enterobacter spp. (including Enterobacter cloacae), Hafnia, 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, Plesiomonas aeruginosa, Vibrio cholerae, Vibrio parahaemolyticus, Haemophilus influenzae, Chlamydia spp, Serratia spp., Providencia spp., Haemophilus ducreyi, Bordetella parapertussis, Bordetella pertussis, Moraxella catarrhalis, Propionibacterium acnes, Staphylococcus spp.

Different sensitivities to the drug are: Enterococcus faecalis, Streptococcus pneumoniae, Streptococcus pyogenes, Streptococcus viridans, Serratia marcescens, Pseudomonas aeruginosa, Acinetobacter, Mycoplasma hominis, Mycoplasma pneumoniae, Mycobacterium tuberculosis, Mycobacterium fortuitum, Ureaplasma urealyticum, Clostridium perfringens, Corynebacterium spp., Helicobacter pylori, Listeria monocytogenes, Gardnerella vaginalis.

In most cases Nocardia asteroides, anaerobic bacteria (e.g. Bacteroides spp., Peptococcus spp., Peptostreptococcus spp., Eubacterium spp., Fusobacterium spp., Clostridium difficile) are not sensitive. It does not work on Treponema pallidum.

Pharmacokinetics

After oral administration it is quickly and completely absorbed. Bioavailability is more than 96%, plasma protein binding is 25%. Tmax is 1-2 h, Cmax after doses of 100, 300, 600 mg is 1, 3.4 and 6.9 mg/l. After a single dose of 200 or 400 mg, it is 2.5 mcg/ml and 5 mcg/ml, respectively.

The apparent volume of distribution is 100 l. It penetrates into tissues, organs and media of the body: cells (leukocytes, alveolar macrophages), skin, soft tissues, bones, abdominal and pelvic organs, respiratory system, urine, saliva, bile, prostate secretion, passes well through the BBB, placental barrier, secreted with the mother’s milk. It penetrates into the cerebrospinal fluid with inflamed and uninflamed cerebral membranes (14-60%).

It is metabolized in the liver (about 5%) with the formation of N-oxide ofloxacin and dimethylofloxacin. T1/2 is independent of the dose and is 4.5-7 hours. Excreted by the kidneys 75-90% (unchanged), about 4% – in the bile. Extra renal clearance is less than 20%.

After a single dose of 200 mg, it is detectable in the urine within 20-24 hours. With renal/hepatic insufficiency, excretion may be delayed. It does not cumulate.

Indications

Active ingredient

How to take, the dosage

Intravenously, dropwise as an infusion over 30-60 minutes in a single dose of 200 mg. If the patient’s condition improves, the patient is transferred to oral administration of the drug in the same daily dose.

Intravenously.

Urinary tract infections – 100 mg 1-2 times daily, renal and genital infections – 100 to 200 mg 2 times daily; respiratory tract infections, ENT organs, skin and soft tissue infections, bones and joints, abdominal cavity, bacterial enteritis, septic infections – 200 mg 2 times daily. If necessary, the dose is increased to 400 mg 2 times a day.

For prophylaxis of infections in patients with severe immune impairment, the dose is 400-600 mg daily. If necessary, 200 mg in 5% dextrose solution by intravenous drip. Duration of infusion – 30 minutes Only freshly prepared solutions should be used.

Interaction

Compatible with the following infusion solutions: isotonic sodium chloride solution, Ringer’s solution, 5% fructose solution, 5% dextrose (glucose) solution.

Do not mix with heparin (risk of precipitation).

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

Decreases clearance of theophylline by 25% (theophylline dose should be reduced with concomitant use).

Cimetidine, furosemide, methotrexate and drugs that block tubular secretion increase plasma concentration of ofloxacin.

Increases the plasma concentration of glibenclamide.

Concomitant administration with vitamin K antagonists requires monitoring of the clotting system.

The risk of neurotoxic effects increases when prescribed with NSAIDs, nitroimidazole derivatives and methylxanthine.

The risk of tendon rupture increases when concomitantly prescribed with glucocorticoids, especially in the elderly.

The risk of crystalluria and nephrotic effects increases when prescribed with drugs that alkalize the urine (carboanhydrase inhibitors, sodium bicarbonate).

Special Instructions

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

At the time of treatment it is necessary to refrain from driving vehicles and engaging in potentially dangerous activities that require increased concentration and quick psychomotor reactions. Alcohol must not be consumed.

Tampax tampons should not be used during treatment with the drug due to increased risk of thrush.

Treatment may cause worsening of myasthenia gravis, and increased incidence of porphyria in susceptible patients.

Possible false-negative results in bacteriological diagnosis of tuberculosis (prevents isolation of Mycobacterium tuberculosis).

Contraindications

Hypersensitivity, glucose-6-phosphate dehydrogenase deicitis, epilepsy (including anamnesis), decreased seizure threshold (including after craniocerebral injury, stroke or inflammatory processes in the central nervous system); age under 18 years (until the skeleton growth), pregnancy, lactation.
With caution – cerebral atherosclerosis, cerebral circulatory disorders (in anamnesis), chronic renal insufficiency, organic lesions of the central nervous system.

Side effects

Gastrointestinal system disorders: gastralgia, anorexia, nausea, vomiting, diarrhea, flatulence, abdominal pain, increased liver transaminases activity, hyperbilirubinemia, cholestatic jaundice, pseudomembranous enterocolitis.

Nervous system and sensory organs: Headache, dizziness, uncertainty of movements, tremor, convulsions, numbness and paresthesias of the extremities, intense dreams, “nightmares” dreams, psychotic reactions, anxiety, state of agitation, phobias, depression, confusion, hallucinations, increased intracranial pressure; color perception disorders, diplopia, disorders of taste, smell, hearing and balance. When using the ointment – a burning sensation and discomfort in the eyes, hyperemia, itching and dryness of the conjunctiva, photophobia, lacrimation.

Musculoskeletal system: tendinitis, myalgia, arthralgia, tenosynovitis, tendon rupture.

Cardiovascular and blood (hematopoiesis, hemostasis): tachycardia, BP decrease (when infused; if BP drops rapidly, the infusion is stopped), vasculitis, collapse; leukopenia, agranulocytosis, anemia, thrombocytopenia, pancytopenia, hemolytic and aplastic anemia.

Allergic reactions: skin rash, itching, urticaria, allergic pneumonitis, allergic nephritis, eosinophilia, fever, Quincke’s edema, bronchospasm, Stevens-Johnson and Lyell syndrome, photosensitization, erythema multiforme, rarely – anaphylactic shock.

Skin disorders: petechial hemorrhages (petechiae), bullous hemorrhagic dermatitis, papular rash with crust, indicating vascular lesions (vasculitis).

Urinary system disorders: acute interstitial nephritis, impaired renal function, hypercreatininemia, increased urea.

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

Overdose

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

Treatment: gastric lavage, symptomatic therapy.

Similarities