Ofloxacin (Ofloxacin)

Composition Pharmacodynamics Indications Carefully Contraindications Dosing and Administration Side effects Form release / dosage
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Dosage form: & nbspfilm-coated tablets
Composition:

Active substance: ofloxacin - 200 mg, 400 mg.

Auxiliary substances: corn starch, microcrystalline cellulose, talc, povidone (polyvinylpyrrolidone low molecular weight), calcium stearate, silicon dioxide colloid (aerosil).

Shell: hypromellose (hydroxypropylmethylcellulose), talc, titanium dioxide, propylene glycol, macrogol 4000 (polyethylene oxide 4000)

Description:

Round biconvex tablets covered with a film shell of almost white color, on the cross-section a layer of almost white color is visible.

Pharmacotherapeutic group:Antimicrobial agent-fluoroquinolone
Pharmacodynamics:

A broad-spectrum antimicrobial agent from the group of fluoroquinolones, acts on the bacterial DNA-gyrase enzyme, which provides super-convoliation, and so on. stability of bacterial DNA (destabilization of DNA chains leads to their death). Has a bactericidal effect.

It is active against microorganisms producing beta-lactamase and fast-growing atypical mycobacteria. Sensitive: Staphylococcus aureus,

Staphylococcus epidermidis, Neisseria gonorrhoeae, Neisseria meningitidis, Escherichia coli,

Citrobacter spp., Klebsiella spp. (including Klebsiella pneumonia), Enterobacter spp., Hafnia spp., Proteus spp. (including Proteus mirabilis, Proteus vulgaris - indole-positive and indolotric), Salmonella spp., Shigella spp. (including Shigella sonnei), Yersinia enterocolitica, Campylobacter jejuni, Aeromonas hydrophila, Vibrio cholerae, Vibrio parahaemolyticus, Haemophilus influenzae, Chlamydia spp., Legionella spp., Serratia spp., Providencia spp., Haemaboutphilus ducreyi, Bordetella parapertussis, Bordetella pertussis, Moraxella catarrhalis, Propionibacterium acne, Brucella spp.

Different sensitivity to the drug has: Enterocaboutccus faecalis,

Streptococcus pneumoniae, Streptococcus pyogenes, Streptococcus viridans, Serratia marcescens, Pseudomonas aeruginosa, Acinetobacter spp, Mycoplasma hominis, Mycoplasma pneumoniae, Mycobacterium tuberculosis, Mycobacterium fortuitum, Ureaplasma urealyticum, Clostridium perfringens, Corynebacterium spp., Helicobacter pylori, Listeria monocytogenes, Gardnerella vaginalis.

In most cases, they are insensitive: Nocardia asteroides, anaerobic bacteria (for example Bacteroides spp., Peptococcus spp., Peptostreptococcus spp., Eubacter spp., Fusobacterium spp., Clostridium difficile). He acts on Treponema pallidum.

Pharmacokinetics:

Absorption after oral administration is rapid and complete (95%). Bioavailability is more than 96%, the connection with plasma proteins is 25%, the time to reach the maximum concentration by oral intake is 1-2 hours, the maximum

concentration after taking a dose of 600 mg is 6.9 mg / l, respectively, and depends on the dose: after a single dose of 200 and 400 mg, it is 2.5 and 5 μg / ml, respectively. Food can slow absorption, but does not have a significant effect on bioavailability.

Apparent volume of distribution - 100 liters. Distribution: cells (leukocytes, alveolar macrophages), skin, soft tissues, bones, abdominal and pelvic organs, respiratory system, urine, saliva, bile, the secret of the Prostate; well penetrates the blood-brain barrier, the placental barrier, is secreted with the mother's milk. It penetrates into the cerebrospinal fluid (14-60%).

Metabolized in the liver (about 5%) with formation NOxygen ofloxacin and dimethylfloxacin. The half-life is 4.5-7 hours (regardless of the dose). It is excreted by the kidneys - 75-90% (unchanged), about 4% - with bile. The extrarenal clearance is less than 20 %.

After a single application in a dose of 200 mg in urine is detected within 20-24 hours. In renal / hepatic insufficiency, excretion can be slowed down. Do not cumulate. With hemodialysis, 10-30% of the drug is removed.

Indications:

Infectious-inflammatory diseases caused by sensitive microorganisms:

-infection of respiratory Pathways (bronchitis, pneumonia);

-infection of ENT organs (sinusitis, pharyngitis, otitis media, laryngitis, tracheitis); -infection of the skin, soft tissues;

- infection of bones, joints;

Infectious-inflammatory diseases of the abdominal cavity and biliary tract;

-infection of the kidneys (pyelonephritis), urinary tract (cystitis, urethritis);

-infection of the pelvic organs (endometritis, salpingitis, oophoritis, cervicitis, parametritis, prostatitis);

-infection of genital organs (colpitis, orchitis, epididymitis);

-gonorrhea;

- Chlamydia;

Prevention of infections in patients with impaired immune status (incl.with neutropenia).

Contraindications:

Hypersensitivity, deficiency of glucose-6-phosphate dehydrogenase, epilepsy (including in the anamnesis), reduction of convulsive threshold (including after craniocerebral trauma, stroke or inflammatory processes in the central nervous system), age to 18 years ( until the growth of the skeleton is completed), pregnancy, lactation period, tendon damage with prior treatment with quinolones, renal dysfunction: with creatinine clearance less than 50 ml / min, when on hemodialysis.

Carefully:
Atherosclerosis of cerebral vessels, cerebral circulatory disorders (in history), chronic renal failure, organic lesions of the central nervous system, lengthening of the interval QT.

Pregnancy and lactation:Contraindicated.
Dosing and Administration:

Inside. Doses are selected individually depending on the location, the severity of the infection, the sensitivity of microorganisms, as well as the general condition of the patient and the function of the liver and kidneys.

Adults - 200-600 mg / day, the course of treatment - 7-10 days, the frequency of application - 2 times a day. A dose of up to 400 mg / day can be given in one session, preferably in the morning.With gonorrhea - 400 mg once. In severe infections or in the treatment of patients with excessive body weight, the daily dose can be increased to 800 mg.

The maximum daily dose for liver failure is 400 mg / day.

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

Tablets are taken whole, washed down with water before or during meals. The duration of the course of treatment is determined by the sensitivity of the pathogen and the clinical picture; treatment should continue for at least 3 more days after the disappearance of the symptoms of the disease and complete normalization of body temperature. In the treatment of salmonellosis treatment course - 7-8 days, with uncomplicated infections of the lower urinary tract treatment course - 3-5 days.

Side effects:

From the digestive system: gastralgia, decreased appetite, nausea, vomiting, diarrhea, flatulence, abdominal pain, increased activity of "liver" transaminases, hyperbilirubinemia, cholestatic jaundice, pseudomembranous enterocolitis.

From the nervous system: headache, dizziness, lack of confidence in movements, tremors, convulsions, numbness and paresthesias of the limbs, intense dreams,"nightmarish" dreams, psychotic reactions, anxiety, arousal, phobias, depression, confusion, hallucinations, increased intracranial pressure.

From the side of the musculoskeletal system: tendonitis, myalgia, arthralgia, tendosynovitis, tendon rupture.

From the sense organs: violation of color perception, diplopia, violation of taste, smell, hearing and balance.

From the side of the cardiovascular system: tachycardia, lowering blood pressure.

Allergic reactions: skin rash, itching, hives, allergic pneumonitis, allergic nephritis, eosinophilia, fever, angioedema, bronchospasm; multiforme exudative erythema (including Stevens-Johnson syndrome) and toxic epidermal necrolysis (Lyell's syndrome), vasculitis, anaphylactic shock.

From the skin: point hemorrhages (petechiae), bullous hemorrhagic dermatitis, papular rash with a cortex, indicative of vascular lesions (vasculitis).

On the part of the organs of hematopoiesis: leukopenia, agranulocytosis, anemia, thrombocytopenia, pancytopenia, hemolytic and aplastic anemia.

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

Other: dysbacteriosis of the intestine, superinfection, photosensitivity, hypoglycemia (in patients with diabetes mellitus), vaginitis.

Overdose:

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

Treatment: gastric lavage, symptomatic therapy.

Interaction:

Reduces the clearance of theophylline by 25% (with simultaneous use should reduce the dose of theophylline).

Increases the concentration of glibenclamide in plasma.

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

At simultaneous admission with antagonists of vitamin K, it is necessary to control the blood coagulation system.

When administered with non-steroidal anti-inflammatory drugs, derivatives of nitroimidazole and methylxanthines, the risk of neurotoxic effects increases.

At simultaneous appointment with a glucocorticosteroid, the risk of rupture of tendons increases, especially in the elderly.

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

When using the drug should take into account that food products, antacids containing alminium (A13 +), calcium (Ca2 +), magnesium (Mg2 +), or iron salts (Fe), reduce the absorption of ofloxacin, forming insoluble complexes (therefore, the time interval between the appointment of Ofloxacin and these drugs should be at least 2 hours).

Special instructions:
It is not a drug of choice for pneumonia caused by pneumococci. Not indicated in the treatment of acute tonsillitis.

It is not recommended to use more than 2 months, exposed to sunlight, UV-rays (mercury-quartz lamps, solarium).

In the event of side effects from the central nervous system, allergic reactions, pseudomembranous colitis, drug withdrawal is necessary. With pseudomembranous colitis, confirmed colonoscopically and / or histologically, oral administration of vancomycin and metronidazole is indicated.

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

During the period of treatment can not be consumed ethanol.

When using the drug, women are not recommended to use hygiene tampons due to the increased risk of thrush development.

Against the backdrop of treatment, myasthenia flow may worsen, and porphyria attacks may be more frequent in predisposed patients.

Can lead to false-negative results in the bacteriological diagnosis of tuberculosis (prevents the isolation Mycobacterium tuberculosis).

In patients with impaired liver or kidney function, it is necessary to monitor the concentration of ofloxacin in plasma. In severe renal and hepatic insufficiency, the risk of toxic effects increases (reduction dose correction is required).

Effect on the ability to drive transp. cf. and fur:During the treatment period, care must be taken when driving vehicles and engaging in other potentially hazardous activities,requiring increased concentration of attention and speed of psychomotor reactions.
Form release / dosage:

The film-coated tablets are 200 mg and 400 mg.

Packaging: 10 tablets in a planar cell package. 1 circuit cell pack with instructions for use is placed in a pack of cardboard.
Storage conditions:

In a dry, protected from light place at a temperature of no higher than 25 ° C. Keep out of the reach of children.

Shelf life:

5 years. Do not use after expiry date.

Terms of leave from pharmacies:On prescription
Registration number:P N002204 / 01
Date of registration:07.08.2008 / 18.08.2009
Expiration Date:Unlimited
The owner of the registration certificate:SYNTHESIS, JSC Joint-stock Kurgan Society of Medical Preparations and Products SYNTHESIS, JSC Joint-stock Kurgan Society of Medical Preparations and Products Russia
Manufacturer: & nbsp
Representation: & nbspSYNTHESIS JSC Joint-Stock Kurgan Society of Medical Preparations and Products SYNTHESIS JSC Joint-Stock Kurgan Society of Medical Preparations and Products Russia
Information update date: & nbsp17.06.2017
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