Ofloxacin

General characteristics. Structure:

Active ingredient: 1 ml ofloxacin of 2 mg;

Excipients: sodium chloride, water for and.

Description: solution for infusions transparent, chartreuse color.

Pharmacological properties:

Antimicrobic drug of a wide range of bactericidal action from group of ftorkhinolon. Affects the DNK-girazu enzyme providing superspiralling and, thus, stability of DNA of bacteria (destabilization of chains of DNA leads to death of microorganisms).

It is active concerning the microorganisms producing β-lactamelements and fast-growing atypical mycobacteria., including Staphylococcus aureus, Staphylococcus epidermidis, Neisseria gonorrhoeae, Neisseria meningitidis, Escherichia coli, Citrobacter spp., Klebsiella spp. (vlyuchy Klebsiella pneumoniae), Enterobacter spp., Hafnia spp., Proteus spp. (including Proteus mirabilis, Proteus vulgaris – an indole - positive and an 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 pertussis, Moraxella catarrhalis, Propionibacterium acnes, Staphylococcus spp., Brucella spp.

Various sensitivity to drug Enterococcus faecalis, Streptococcus pyogenes, Streptococcus pneumoniae and viridans, Serratia marcescenes, Pseudomonas aeruginosa, Acinetobacter, Mycoplasma hominis and pneumoniae, Mycobacterium tuberculosis, and also Mycobacterium fortuitum, Ureaplasma urealyticum, Clostridium perfringens, Corynebacterium spp have., Helicobacter pylori, Listeria monocytogenes, Gardnerella vaginalis.

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

It is inactive concerning Treponema pallidum.

 

Pharmacokinetics. Distribution

After one-time infusion of 200 mg of an ofloksatsin within 60 min. Cmax makes 2.7 mkg/ml, in 12 h after introduction concentration of an ofloksatsin makes 0.3 mkg/ml.

Equilibrium concentration are reached after 4 infusions. At in introduction of an ofloksatsin in a dose of 200 mg each 12 h within 7 days average maximum and minimum equilibrium concentration make 2.9 and 0.5 mkg/ml respectively. Ofloxacin widely gets into many fabrics and fluid mediums of an organism, including into saliva, a bronchial secret, bile, the lacrimal and cerebrospinal fluid, pus, into lungs, a prostate gland and skin.

Linkng with proteins of a blood plasma makes 20-25%.

Metabolism and removal

Ofloxacin partially (5%) biotransformirutsya in a liver. T1/2 is 6-7 h. To 80% of a dose a small part – with a stake is removed by kidneys in not changed look.

At a hemodialysis 10-30% of drug are removed. At patients with renal failures (KK of 50 ml/min. and less) T1/2 of an ofloksatsin increases.

Indications to use:

— respiratory infections (bronchitis, pneumonia);

— infections of ENT organs (sinusitis, pharyngitis, average otitis, laryngitis);

— infections of skin and soft tissues;

— infections of bones and joints;

— infectious and inflammatory diseases of an abdominal cavity (including infections of a GIT and biliary tract);

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

— infections of bodies of a small pelvis (endometritis, salpingitis, oophoritis, cervicitis, parametritis, prostatitis) and generative organs (colpitis, orchitis, epididymite);

— gonorrhea;

— clamidiosis;

— septicaemia;

— meningitis;

— prevention of infections at patients with disturbance of the immune status (including at a neutropenia).

Route of administration and doses:

The drug is administered in/in kapelno. Doses select 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.

Therapy there begin with in/in drop (within 30-60 min.) introductions drug in a dose of 200 mg. At improvement of a condition of the patient transfer to oral administration of drug in the same daily dose.

At infections of urinary tract drug appoint on 100 mg 1-2, at infections of kidneys and generative organs – from 100 to 200 mg 2; at respiratory infections, and also ENT organs, infections of skin and soft tissues, bones and joints, infections of an abdominal cavity, septic infections – on 200 mg 2 If necessary the dose is increased to 400 mg 2

For prevention of infections at patients with the expressed decrease in immunity – on 400-600 mg /

At patients with renal failures (at KK from 50 to 20 ml/min.) the single dose has to make 50% from average recommended at frequency rate of appointment 2 It is possible to enter a full single dose of 1 times / At KK less than 20 ml/min. a single initial dose makes 200 mg, then the drug is administered on 100 mg / every other day.

At peritoneal dialysis and a hemodialysis the drug is administered on 100 mg by each 24 h.

At a liver failure the maximum daily dose makes 400 mg.

Features of use:

Ofloxacin is not choice drug at the pneumonia caused by pneumococci is not shown at treatment of acute tonsillitis.

It is not recommended to apply more than 2 months. Against the background of use of drug it is impossible to be affected by sunshine, to UF-radiation.

At emergence of side effects from TsNS, allergic reactions, pseudomembranous colitis drug withdrawal is necessary.

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.

At drug use women are not recommended to use tampons like tampax in connection with the increased risk of development of candidiasis.

Against the background of treatment deterioration in a current of a myasthenia, increase of attacks of a porphyria at predisposed patients is possible.

Emergence of false-negative results at bacteriological diagnosis of tuberculosis is possible (interferes with Mycobacterium tuberculosis allocation).

At an abnormal liver function or kidneys control of concentration of an ofloksatsin in a blood plasma is necessary. At a heavy renal and liver failure the risk of development of toxic effects increases (the reducing dose adjustment is required).

Against the background of use of drug it is impossible to use ethanol.

Use in pediatrics

At children drug is used only at life-threatening infections, taking into account estimated clinical performance and potential risk of development of side effects when it is impossible to use less toxic drugs. An average daily dose in this case – 7.5 mg/kg of body weight, maximum – 15 mg/kg.

Influence on ability to driving of motor transport and to control of mechanisms

At use of drug it is necessary to abstain from occupations potentially dangerous types of activity requiring special attention and high speed of psychomotor reactions.

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 TsNS and peripheral 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, disturbance of color perception, diplopia, disturbance of taste, sense of smell and balance.

From a musculoskeletal system: the tendinitis, mialgiya, arthralgias, tendosinovit, a rupture of a sinew.

From cardiovascular system: tachycardia, decrease in the ABP (at sharp decrease in the ABP introduction is stopped), a vasculitis, a collapse.

From system 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.

Dermatological reactions: dot hemorrhages, dermatitis violent hemorrhagic, papular rash testimonial of defeat of vessels (vasculitis).

Allergic reactions: skin rash, skin itch, small tortoiseshell, allergic pneumonitis, allergic nephrite, eosinophilia, fever, Quincke's edema, bronchospasm, Stephens-Johnson's syndrome and Lyell's disease, photosensitization, multiformny exudative erythema, acute anaphylaxis.

Others: dysbacteriosis, superinfection, a hypoglycemia (at patients with a diabetes mellitus), a vaginitis.

Local reactions: pain, reddening in an injection site, thrombophlebitis.

Interaction with other medicines:

At simultaneous use ofloxacin reduces clearance of theophylline by 25% (at simultaneous use it is necessary to lower a theophylline dose).

At simultaneous use Cimetidinum, furosemide, a methotrexate and drugs blocking canalicular secretion increase concentration of an ofloksatsin in plasma.

Ofloxacin increases concentration of Glibenclamidum in plasma.

At a concomitant use with indirect anticoagulants antagonists of vitamin K it is necessary to exercise control of a condition of coagulant system of blood.

At combined use with NPVS, derivatives of a nitroimidazole and methylxanthines the risk of development of neurotoxic effects increases.

At co-administration with GKS 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.

Pharmaceutical interaction

Solution of an ofloksatsin is compatible to the following infusion solutions: isotonic solution of sodium of chloride, Ringer's solution, 5% solution of fructose, 5% solution of a dextrose (glucose).

Contraindications:

— deficit glyukozo-6-fosfatdegidrogenazy;

— epilepsy (including in the anamnesis);

— reduction of the threshold of convulsive readiness (including after a craniocereberal injury, a stroke or inflammatory processes in TsNS);

— age up to 18 years (before completion of growth of bones of a skeleton);

— pregnancy;

— lactation;

— hypersensitivity to drug.

 

Use of the drug OFLOXACIN for infusions at pregnancy and feeding by a breast
Drug is contraindicated to use at pregnancy and in the period of a lactation.

 

Use at abnormal liver functions
At a liver failure the maximum daily dose makes 400 mg.

 

Use at renal failures
At patients with renal failures (at KK from 50 to 20 ml/min.) the single dose has to make 50% from average recommended at frequency rate of appointment 2 It is possible to enter a full single dose of 1 times / At KK less than 20 ml/min. a single initial dose makes 200 mg, then the drug is administered on 100 mg / every other day.

At peritoneal dialysis and a hemodialysis the drug is administered on 100 mg by each 24 h.

 

Use for children
Drug is contraindicated to children and teenagers up to 18 years since growth of a skeleton is not complete.

At children drug is used only at life-threatening infections, taking into account estimated clinical performance and potential risk of development of side effects when it is impossible to use less toxic drugs. An average daily dose in this case – 7.5 mg/kg of body weight, maximum – 15 mg/kg.

Overdose:

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

Treatment: gastric lavage, symptomatic therapy.

Storage conditions:

List B. Drug should be stored in protected from light, the place, unavailable to children, at a temperature from 15 to 25 °C; not to freeze. A period of validity - 2 years.

Issue conditions:

According to the recipe

Packaging:

100 ml - bottles of colourless glass (1) - a pack cardboard.
100 ml - bottles of dark glass (1) - a pack cardboard.