Ofloxacin

General characteristics. Structure:

Active ingredient: 200 mg or 400 mg of an ofloksatsin in 1 tablet.

The antimicrobic drug having antibacterial and bactericidal effect.

Pharmacological properties:

Pharmacodynamics. Inhibits DNK-girazu (topoisomerase II and IV), breaks process of superspiralling and a stitching of ruptures of DNA, cell fission oppresses, causes structural changes of cytoplasm and death of microorganisms.

Has a broad spectrum of activity. Influences preferential gram-negative and some gram-positive microorganisms. It is effective concerning the microorganisms steady against the majority of antibiotics and sulfanamide drugs. Cross resistance of bacteria to an ofloksatsin, etc. to ftorkhinolona is possible. The action spectrum includes: E. coli, Salmonella spp., Enterobacter spp., Serratia spp., Citrobacter spp., Yersinia spp., Haemophilus influenzae, Haemophilus ducreyi, Proteus mirabilis, Proteus vulgaris, Pseudomonas spp., including Pseudomonas aeruginosa, Acinetobacter spp., Aeromonas hydrophilia, Bordetella parapertussis, Bordetella pertussis, Klebsiella spp., including Klebsiella pneumoniae, Moraxella (Branhamella) catarrhalis, Morganella morganii, Providencia spp., Neisseria gonorrhoeae, Neisseria meningitidis, Shigella sonnei, Helicobacter pylori, Mycoplasma spp., Ureaplasma urealyticum, Vibrio spp., Gardnerella vaginalis, Chlamydia spp., Legionella pneumophila, Staphylococcus spp., Streptococcus spp., Enterococcus faecalis, Listeria monocytogenes, Propionibacterium acnes, Clostridium perfringens, Mycobacterium tuberculosis (including multiresistant strains).

Pharmacokinetics. At intake absolute bioavailability — 96% is completely soaked up from a GIT (about 95%). After reception of an ofloksatsin in a dosage form of the usual tablets Cmax in plasma it is reached in 1–2 h, after reception of tablets of the prolonged action — during 6–8 h. Linkng with proteins of plasma — 32%. The seeming volume of distribution of 100 l. T1/2  at reception of usual tablets is 4,5–7 h. Gets into cells (leukocytes, alveolar macrophages) most bodies and fabrics, creates high concentration in urine, bile, saliva, a phlegm, a prostate secret, kidneys, a liver, a gall bladder, skin, lungs, passes through GEB and a placental barrier. In a liver (about 5%) turns into N-oxide of an ofloksatsin and деметилофлоксацин. It is removed preferential by kidneys in not changed look (80–90%); a small part is allocated with bile, excrements, breast milk (the extrarenal clearance makes less than 20%). After single use in 200 mg in urine it is found during 20–24 h. At diseases of a liver and/or kidneys excretion can be slowed down. Repeated appointment does not lead to cumulation.

Indications to use:

The infectious and inflammatory diseases caused by sensitive microorganisms including respiratory infections (pneumonia, an exacerbation of bronchitis), ENT organs (sinusitis, pharyngitis, average otitis, laryngitis, tracheitis), skin and soft tissues, bones and joints, an abdominal cavity, bodies of a small pelvis, kidneys and urinary tract (pyelonephritis, cystitis, an urethritis), generative organs (including gonorrhea, prostatitis), chlamydial infections, a septicaemia, tuberculosis (as a part of complex therapy), prevention of infections at patients with an immunodeficiency.

In ophthalmology: bacterial helcomas, conjunctivitis, a blepharitis, a meibomitis, a dacryocystitis, a keratitis, chlamydial infections of eyes, prevention of infectious complications in the postoperative period after surgical interventions concerning removal of a foreign body and an injury of an eye.

Expert Laure: acute and chronic bacterial outside and average otitis, otitis with perforation of a tympanic membrane or a tympanopuncture; prevention of infectious complications at surgical interventions.

Route of administration and doses:

Inside, in/in, locally (subkonjyunktivalno, in outside acoustical pass). The mode of dosing is set individually, depending on localization and weight of a course of an infection, sensitivity of microorganisms, the general condition of the patient, function of a liver and kidneys, the applied dosage form.

The adult, a daily dose — 200–800 mg, frequency rate of use — 1–2 times a day; at gonorrhea — 400 mg once. Against the background of liver diseases the daily dose should not exceed 400 mg, at a renal failure — depends on clearance of creatinine: at Cl of creatinine of 20-50 ml/min. the first dose — 200 mg, then 100 mg each 24 h, less than 20 ml/min. — 200 mg, further 100 mg each 48 h.

Features of use:

Use at pregnancy and feeding by a breast. Use at pregnancy is possible (including in the form of dosage forms for topical administration) if the expected effect of therapy exceeds potential risk for a fruit (adequate and strictly controlled researches of safety of use for pregnant women were not conducted).

Teratogenic effects. Ofloxacin had no teratogenic effect at introduction by a pregnant animal in the period of an organogenesis: to rats in doses over 810 mg/kg/days, cht of 11 times exceed MRDCh at intake and by 9000 times — at use in the form of eye drops; to rabbits in doses over 160 mg/kg/days that exceeds МРДЧв 4 and 1800 times respectively. The doses equivalent 50 and 10 MRDCh at oral administration were fetotoksichny — decrease in mass of bodies of fruits and increase in fetalis mortality at rats and rabbits was observed.

Category of action on a fruit on FDA — C. At a single dose of 200 mg of an ofloksatsin the feeding women of its concentration in breast milk are similar to those in plasma. As potentially ofloxacin can cause serious side reactions in the babies who are on breastfeeding, the feeding women need to stop either breastfeeding, or reception of an ofloksatsin (considering the importance of medicine for mother).

After disappearance of clinical signs treatment is continued by 2–3 days. With care appoint to patients with atherosclerosis of vessels of a brain. Constant observation at the combined use with insulin, caffeine, theophylline, cyclosporine, NPVS, peroral anticoagulants (including with warfarin) and the drugs which are metabolized with the participation of P450 cytochrome is necessary.

At children it is applied only at threat of life (because of risk of development of side effects). At bystry in introduction decrease in the ABP is possible.

It is not necessary to inject subkonjyunktivalno or to enter into an anterior chamber of an eye. When using ophthalmologic forms carrying eye lenses is not recommended. Perhaps combined use of eye drops and an oculentum, at the same time ointment is used by the last.

During treatment it is not necessary to be exposed solar or UF to radiation. It is recommended to abstain from the activity demanding speed of psychomotor reactions (driving of transport, work with potentially dangerous mechanisms) and alcohol intake.

Side effects:

From bodies of a GIT: dyspepsia, nausea, vomiting, diarrhea, anorexia, an abdominal pain, dryness in a mouth, tranzitorny increase in level of bilirubin and liver enzymes in a blood plasma, hepatitis, jaundice, dysbacteriosis, pseudomembranous colitis.

From a nervous system and sense bodys: dizziness, headache, insomniya, concern, reduction in the rate of reactions, excitement, increase in intracranial pressure, tremor, spasms, nightmares, hallucinations, psychosis, paresthesia, phobias, lack of coordination of movements, taste, sense of smell, sight, diplopia, disorders of color perception, loss of consciousness.

From cardiovascular system and blood (a hemopoiesis, a hemostasis): a cardiovascular collapse, hemolitic and aplastic anemia, thrombocytopenia, including a Werlhof's disease, a leukopenia, a neutropenia, an agranulocytosis, a pancytopenia.

From urinogenital system: acute intersticial nephrite, disturbance of secretory function of kidneys with increase in level of urea and creatinine, a vaginitis.

Allergic reactions: skin rash, itch, Quincke's disease, including laryngeal, pharyngeal, persons, phonatory bands, bronchospasm, small tortoiseshell, mnogoformny exudative erythema, Stephens-Johnson's syndrome, toxic epidermal necrolysis, acute anaphylaxis.

Others: a hypoglycemia (at patients with a diabetes mellitus), a vasculitis, a tendinitis, a mialgiya, an arthralgia, superinfection, a photosensitization.

When using in ophthalmology: a burning sensation and discomfort in eyes, reddening, an itch and dryness of a conjunctiva, a photophobia, dacryagogue; seldom — dizziness, nausea.

After an instillation in acoustical pass: an itch in the field of acoustical pass, feeling of bitter smack in a mouth; seldom — system reactions (eczema, dizziness, noise and ear pain, dryness of a mucous membrane of an oral cavity).

Interaction with other medicines:

The antacids containing Al3 + Ca2 + Mg2+, iron salts, salt laxatives, сукральфат zinc reduce absorption and reduce activity (the interval between receptions has to be not less than 2 h).

At the accompanying reception of NPVS and hinolon (including an ofloksatsina) the risk of stimulation of TsNS and development of convulsive attacks can amplify.

At a concomitant use of an ofloksatsin with theophylline T1/2 can be prolonged  and raise Css of theophylline owing to what the risk of toxicity of theophylline increases.

Furosemide and methotrexate slow down removal and can increase toxicity.

Increases concentration of Glibenclamidum. It is not necessary to mix in solution with heparin (risk of precipitation).

Contraindications:

Hypersensitivity (including to other ftorkhinolona, hinolona), epilepsy (including in the anamnesis), dysfunction of TsNS with reduction of the threshold of convulsive readiness (including after ChMT, a stroke, inflammatory processes in TsNS), damage of sinews at earlier carried out treatment of a ftorkhinolonama, age up to 18 years (growth of a skeleton is not completed yet). For local forms: chronic not bacterial conjunctivitis or otitis.

Overdose:

Symptoms: drowsiness, nausea, vomiting, dizziness, disorientation, block, confusion of consciousness.

Treatment: gastric lavage, maintenance of the vital functions.

Storage conditions:

To store at a temperature of 15-25 °C, in dry, protected from light and the place, unavailable to children. Period of validity 3 years. Not to use after the expiry date specified on packaging.

Issue conditions:

According to the recipe

Packaging:

Tablets of 200 mg and 400 mg, on 10 tablets in each blister, on one, two or three blisters together with the application instruction in cardboard packaging.