Ofloksin

General characteristics. Structure:

Each bottle (100 ml) contains:
Active agent: ofloxacin of 200 mg.
Excipients: sodium chloride, Acidum hydrochloricum concentrated dinatrium эдетат a dihydrate, water for injections.

Description
Transparent solution with a light yellowish-greenish shade.

Pharmacological properties:

Pharmacodynamics. Antimicrobic broad-spectrum agent from group of ftorkhinolon, affects bacterial DNK-gidrazu enzyme, the providing superspiralling and, thus, stability of DNA of bacteria (destabilization of chains of DNA leads to their death). Renders bactericidal effect. It is active concerning the microorganisms producing beta lactamelements and fast-growing atypical mycobacteria. Are sensitive: Staphylococcus aureus, Staphylococcus epidermidis, Neisseria gonorrhoeae, Neisseria meningitidis, Escherichia coli, Citrobacter, Klebsiella spp. (including Klebsiella pneumonia), Enterobacter spp., Hafhia, Proteus spp. (including Proteus mirabilis, Proteus vulgaris - an indole - positive and an indole - negative), Salmonella spp., Shigella spp. (including Shigella sonnei), Yersinia enterocolitica, Campilobacter jejuni, Aeromonas hydrophila, Plesiomonas aeruginosa, Vibrio cholerae, Vibrio parahaemolyticus, Haemophilus influenzae, Chlamydia spp., Legionella spp., Serratia spp., Providencia spp., Haemophilus ducreyi, Bordetella parapertussis, Bordetella pertussis, Moraxella catarrhalis, Propionibacterium acnes, Staphylococcus spp., Brucella spp.
Have various sensitivity to drug: Enterococcus faecalis, Streptococcus pyogenes, pneumoniae and viridans, Serratio marcescens, Pseudomonas aeruginosa, Acinetobacter, Mycoplasma hominis and pneumoniae, Mycobacterium tuberculosis, and also Mycobacterium fortuim, Ureaplasma urealyticum, Clostridium perfringens, Corynebacterium spp., Helicobacter pylori, Listeria monocytogenes, Gardnerella vaginalis.
Are in most cases insensitive: Nocardia asteroides, anaerobic bacteria (for example, Bacteroides spp., Peptococcus spp., Peptostreptococcus spp., Eubacterium spp., Fusobacterium spp., Clostridium difficile). He acts on Treponema pallidum.

Pharmacokinetics. After one-time 60-minute intravenous infusions of 200 mg of an ofloksatsin average maximum plasma concentration makes 2,7 mkg/ml; in 12 hours after introduction concentration equals 0,3 mkg/ml. Equilibrium concentration are reached after introduction of four doses.
Average peak and minimum equilibrium concentration are reached after intravenous administration of 200 mg of an ofloksatsin each 12 hours within 7 days and make 2,9 and 0,5 mkg/ml, respectively.
Ofloxacin widely gets into many liquids and body tissues, including into saliva, a bronchial secret, bile, the lacrimal and cerebrospinal fluid, pus, into lungs, a prostate gland, skin. Ofloxacin is exposed partial (5%) to metabolism in a liver.
Linkng with proteins of plasma makes 20-25%. The elimination half-life of an ofloksatsin is equal to 6-7 hours. To 80% of the drug accepted inside it is excreted by kidneys in not changed look, a small part of active agent is removed also with a stake.
At patients with a renal failure (clearance of creatinine of 50 ml and less) the elimination half-life of an ofloksatsin increases.

Indications to use:

Respiratory infections (bronchitis, pneumonia), ENT organs (sinusitis, pharyngitis, average otitis, laryngitis), skin, soft tissues, bones, joints, infectious and inflammatory diseases of an abdominal cavity and biliary tract (except for bacterial enteritis), kidneys (pyelonephritis), urinary tract (cystitis, an urethritis), bodies of a small pelvis (an endometritis, a salpingitis, an oophoritis, a cervicitis, a parametritis, prostatitis), generative organs (a colpitis, an orchitis, an epididymite), gonorrhea, clamidiosis; a septicaemia (only for in/in introductions), meningitis; prevention of infections at patients with disturbance of the immune status (including at a neutropenia).

Route of administration and doses:

Intravenously kapelno. Doses are selected individually depending on localization and weight of a course of an infection, and also sensitivity of microorganisms, the general condition of the patient and function of a liver and kidneys.
Intravenous drop administration begin 200 mg which is entered slowly within 30-60 min. with a single dose. At improvement of a condition of the patient transfer to oral administration of drug in the same daily dose.
Infections of urinary tract - 100 mg 1-2 times a day, infections of kidneys and generative organs - from 100 mg 2 times a day to 200 mg 2 times a day, respiratory infections, and also ENT organs, an infection of skin and soft tissues, an infection of bones and joints, infections of an abdominal cavity, bacterial enteritis, septic infections - 200 mg 2 times a day. If necessary the dose is increased to 400 mg by 2 times a day.
For prevention of infections at patients with the expressed decrease in immunity - on 400-600 mg/days.
If necessary in/in kapelno - 200 mg in 5% glucose solution. Duration of infusion is-30 min. It is necessary to use only freshly cooked solutions.
At patients with renal failures (at the clearance of creatinine (CC) of 50-20 ml/min.) the single dose has to make 50% of an average dose at frequency rate of appointment 2 times a day, or the full single dose is entered 1 time a day. At KK less than 20 ml/min. a single dose - 200 mg, then - on 100 mg a day every other day.
At a hemodialysis and peritoneal dialysis - on 100 mg each 24 h. The maximum daily dose at a liver failure - 400 mg/days.

Features of use:

Is not choice drug at the pneumonia caused by pneumococci. It is not shown at treatment of acute tonsillitis.
It is not recommended to apply more than 2 months, to be affected by sunshine, to uviolizing (mercury-quartz lamps, a sunbed).
In case of side effects from the central nervous system, allergic reactions, pseudomembranous colitis drug withdrawal is necessary. At the pseudomembranous colitis confirmed kolonoskopichesk and/or histologically peroral purpose of Vancomycinum and metronidazole is shown.
Seldom arising tendinitis can lead to a rupture of sinews (preferential an Achilles tendon), especially at elderly patients. In case of signs of a tendinitis, it is necessary to stop immediately treatment, to make an immobilization of an Achilles tendon and to consult at the orthopedist.
During treatment it is necessary to abstain from driving of motor transport and occupations potentially dangerous types of activity demanding the increased concentration of attention and speed of psychomotor reactions it is impossible to use ethanol.
At drug use women are not recommended to use tampons, in connection with the increased risk of development of the milkwoman.
Against the background of treatment deterioration in a current of a myasthenia, increase of attacks of a porphyria at predisposed patients is possible.
Can result in false-negative results at bacteriological diagnosis of tuberculosis (interferes with Mycobacterium tuberculosis allocation).
At patients with abnormal liver functions or kidneys control of concentration of an ofloksatsin in plasma is necessary. At a heavy renal and liver failure the risk of development of toxic effects increases (dose adjustment is required).
At children it is applied only at threat of life, taking into account estimated advantage and potential risk of development of side effects when it is impossible to use other, less toxic drugs. An average daily dose in this case - 7,5 mg/kg, maximum - 15 mg/kg.

Side effects:

From the alimentary system: gastralgia, anorexia, nausea, vomiting, diarrhea, meteorism, abdominal pains, increase in activity of "hepatic" transaminases, hyperbilirubinemia, cholestatic jaundice, pseudomembranous coloenteritis.
From a nervous system: headache, dizziness, uncertainty of movements, tremor, spasms, numbness and paresthesias of extremities, intensive dreams, "dreadful" dreams, psychotic reactions, uneasiness, psychomotor excitement, phobias, depression, confusion of consciousness, hallucination, increase in intracranial pressure.
From a musculoskeletal system: the tendinitis, mialgiya, arthralgias, tendosinovit, a rupture of a sinew.
From sense bodys: disturbance of color perception, diplopia, disturbances of taste, sense of smell, hearing and balance.
From cardiovascular system: tachycardia, a lowering of arterial pressure (at in introduction; at a sharp lowering of arterial pressure introduction is stopped), a vasculitis, a collapse.
Allergic reactions: skin rash, skin itch, small tortoiseshell, allergic pneumonitis, allergic nephrite, eosinophilia, fever, Quincke's edema, bronchospasm, Stephens-Johnson and Layell's syndrome, photosensitization, multiformny exudative erythema, acute anaphylaxis.
From integuments: dot hemorrhages (petechias), dermatitis violent hemorrhagic, papular rash with a crust, testimonial of defeat of vessels (vasculitis).
From bodies of a hemopoiesis: leukopenia, agranulocytosis, anemia, thrombocytopenia, pancytopenia, hemolitic and aplastic anemia.
From an urinary system: acute intersticial nephrite, renal failure, giperkreatininemiya, increase in content of urea.
Others: dysbacteriosis, superinfection, a hypoglycemia (at patients with a diabetes mellitus), a vaginitis.
Local reactions: pain, reddening in an injection site, thrombophlebitis (at in introduction).

Interaction with other medicines:

Let's combine with the following infusion solutions: isotonic solution of sodium of chloride, Ringer's solution, 5% solution of fructose, 5% dextrose solution.
Not to mix with heparin (risk of precipitation).
Reduces clearance of theophylline by 25% (at simultaneous use it is necessary to reduce a theophylline dose).
Cimetidinum, furosemide, methotrexate and drugs blocking canalicular secretion - increase concentration of an ofloksatsin in plasma.
Increases concentration of Glibenclamidum in plasma.
At a concomitant use with antagonists of vitamin K it is necessary to exercise control of coagulant system of blood.
At appointment with the non-steroidal anti-inflammatory drugs derivative of a nitroimidazole and methylxanthines the risk of development of neurotoxic effects increases.
At co-administration with glucocorticosteroids the risk of a rupture of sinews, especially at elderly people increases.
At appointment with the drugs alkalizing urine (karboangidraza inhibitors, citrates, sodium bicarbonate), the risk of a crystalluria and nephrotoxic effects increases.

Contraindications:

Hypersensitivity, deficit glyukozo-6-fosfatdegidrogenazy, epilepsy (including in the anamnesis), decrease in a convulsive threshold (including after a cherepnomozgovy injury, a stroke or inflammatory processes in the central nervous system); age up to 18 years (growth of a skeleton is not completed yet), pregnancy, the lactation period.
With care - atherosclerosis of vessels of a brain, disturbance of cerebral circulation (in the anamnesis), a chronic renal failure, organic lesions of the central nervous system.

Overdose:

Symptoms: dizziness, confusion of consciousness, block, disorientation, drowsiness, vomiting.
Treatment: gastric lavage, symptomatic therapy.

Storage conditions:

List B. In the dry, protected from light place at a temperature of 10 - 25 °C. To store in the place, unavailable to children. Period of validity 3 years. Not to use after expiry date.

Issue conditions:

According to the recipe

Packaging:

Solution for infusions of 2 mg/ml. On 100 ml of drug in the bottle of colourless glass (a hydrolytic class I or P) corked by a rubber bung and an aluminum cap under a running in with a cover like "flip off". Each bottle together with the application instruction is placed in a cardboard pack.