Ofloxacin-OBL - instructions for use, dose, side effects, contraindications

Excipients: silicon dioxide colloid (aerosil), calcium stearate, microcrystalline cellulose, talcum powder, povidone (Kollidon 30), lactose (milk sugar), croscarmellose sodium (impellose).

Excipients for the shell: hypromellose (hydroxypropylmethylcellulose), macrogol-6000 (polyethylene glycol 6000), titanium dioxide.

Description:

The tablets covered with a cover white or white with a yellowish shade of color, round, biconcave form. On the break the color of the tablets is white.

Pharmacotherapeutic group:The antimicrobial agent fluoroquinolone

ATX: & nbsp

S.01.A.E.01 Ofloxacin

J.01.M.A.01 Ofloxacin

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.

The antimicrobial spectrum includes Gram-positive aerobes: Staphylococcus aureus (methicillin-sensitive), Staphylococcus epidermidis (methicillin-sensitive), Staphylococcus saprophyticus, Streptococcus pneumoniae (penicillin-sensitive), Streptococcus pyogenes.

Gram-negative aerobes: Acinetobacter calcoaceticus, Bordetella pertussis, Citrobacter freundii, Citrobacter koseri, Enterobacter aerobes, Enterobacter cloacae, Escherichia coli, Haemophilus ducreyi, Haemophilus influenzae, Klebsiella oxytoca, Moraxella catarrhalis, Morganella morganii, Klebsiella pneumoniae, Neisseria gonorrhoeae, Proteus mirabilis, Proteus vulgaris, Providencia rettgeri , Providencia stuartii, Pseudomonas aeruginosa (quickly develop resistance), Serratia marcescens.

Anaerobes: Clostridium perfringens.

Other: Chlamydia trachomatis, Chlamydia pneumoniae, Gardnerella vaginalis, Legionella pneumophila, Mycoplasma hominis, Mycoplasma pneumoniae, Ureaplasma urealyticum.

In most cases, they are insensitive: Nocardia asteroides, anaerobic bacteria (incl. Bacteroides spp., Peptococcus spp., Peptostreptococcus spp., Eubacterium spp., Fusobacterium spp., Clostridium difficile), Enterococcus spp., most Streptococcus spp., does not apply to Treponema pallidum.

Pharmacokinetics:

Absorption after oral administration is rapid and complete (95%).

Bioavailability - over 96%, communication with plasma proteins - 25 %, time to reach the maximum concentration (TCmah) with oral intake - 1-2 hours. Maximum concentration (FROMmOh) after taking in a dose of 200, 400 and 600 mg is 2.5, 5 and 6.9 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 gland; well penetrates the hemato-encephalic barrier (GEB), 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 education NOxygen ofloxacin and dimethylfloxacin.

The half-life (T1 / 2) is 4.5-7 hours (regardless of the dose). It is excreted by the kidneys - 75-90 % (unchanged), about 4 % - with bile. Out-of-site clearance - 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. When hemodialysis is removed from 10 to 30% of the drug.

Indications:

Infectious-inflammatory diseases caused by sensitive microorganisms:

- Respiratory tract (bronchitis, pneumonia);

-lore organs (sinusitis, pharyngitis, otitis media, laryngitis, tracheitis);

-skin, soft tissues;

-bones and joints;

-organisms of the abdominal cavity and bile ducts;

-kidneys (pyelonephritis);

- Lower urinary tract (cystitis, urethritis);

- Sex organs and pelvic organs (endometritis, salpingitis, oophoritis, cervicitis, parametritis, bacterial prostatitis, colpitis, orchitis, epididymitis);

-gonorrhea, chlamydia;

-prophylaxis of infections in patients with impaired immune status (including neutropenia).

Contraindications:

Hypersensitivity to ofloxacin and other fluoroquinolones, epilepsy (including in the anamnesis), reduction of the convulsive threshold (including after craniocerebral trauma, stroke or inflammatory processes in the central nervous system), defeat of tendons with previous treatment with fluoroquinolones; lactose intolerance, lactase deficiency, glucose galactose malabsorption; age to 18 years (until the skeleton has been completed), pregnancy, lactation; creatinine clearance less than 20 ml / min.

Carefully:

Cerebral atherosclerosis, cerebrovascular disease (disorder), chronic renal failure, hepatic failure, organic central nervous system disorders, predisposition to convulsive reactions, myasthenia, hepatic porphyria, deficiency of glucose-6-phosphate dehydrogenase, diabetes, congenital long interval syndrome QT, heart disease (heart failure, myocardial infarction, bradycardia), psychoses and other mental disorders in the anamnesis; simultaneous reception of drugs that extend the interval QT (antiarrhythmic IA and III classes, tricyclic and tetracyclic antidepressants, neuroleptics, macrolides, antifungal, imidazole derivatives, some antihistamines, including antihistamines. astemizole, terfenadine, ebastine), for general anesthesia from the barbiturate group, drugs that lower blood pressure; elderly age.

Pregnancy and lactation:Contraindicated.

Dosing and Administration:

Inside. Tablets are taken whole, washed down with water, before or during meals. The duration of treatment is determined by the sensitivity of the pathogen.

The duration of therapy is an average of 7-10 days.

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

Adults - 200-600 mg per day, 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. Doses over 400 mg / day should be divided into 2 divided doses with an equal time interval. In severe infections or in the treatment of patients with overweight, the daily dose can be increased to 800 mg.

In the treatment of uncomplicated and complicated infections of the lower urinary tract treatment course - 7 and 10 days respectively, with prostatitis - up to 6 weeks,with infections of the pelvic organs - 10-14 days, with infections of the respiratory system and skin - 10 days.

With gonorrhea - 400 mg once.

In patients with impaired renal function (with creatinine clearance 50-120 ml / min), a single dose should be 50% of the average dose with a multiplicity of appointment 2 times a day, or a full dose is prescribed once a day. The maximum daily dose for liver failure is 400 mg / day.

Side effects:

From the digestive system: gastralgia, decreased appetite, nausea, vomiting, diarrhea, constipation, flatulence, abdominal pain, increased activity of "liver" transaminases, hyperbilirubinemia, Cholestatic jaundice, pseudomembranous colitis, dryness of the oral mucosa, pharyngitis.

From the nervous system: headache, dizziness, motion uncertainty, tremor, cramps, numbness and paresthesia extremities, intense dreams, "nightmarish" dreams, psychotic reactions, anxiety, arousal, phobias, depression, confusion, hallucinations, increased intracranial pressure, insomnia, nervousness.

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

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

From the side of the cardiovascular system: tachycardia, increase or decrease in blood pressure.

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

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

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

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

Other: intestinal dysbiosis, superinfection, hypoglycemia (in patients with diabetes mellitus), vaginitis, chest pain, fatigue, asthenia, photosensitivity, general weakness, vaginal discharge, epistaxis, thirst, weight loss.

Overdose:

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

Treatment: gastric lavage, symptomatic therapy. Hemodialysis removes 10-30% of the drug.

Interaction:

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

Increases the concentration of glibenclamide in plasma.

Increases serum concentration of cyclosporine.

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

When taken concomitantly with indirect anticoagulants (coumarin derivatives, including warfarin) 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 developing neurotoxic effects, including convulsions, increases.

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

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

With a simultaneous appointment with hypoglycemic agents, both hypo- and hyperglycemia are possible, and in this connection it is necessary to monitor the concentration of glucose in the blood plasma.

When co-administered with drugs that extend QT (IA and III classes of antiarrhythmic drugs, tricyclic antidepressants, macrolides) increases the risk of lengthening the interval QT.

Food products, antacids containing compounds of aluminum, calcium, magnesium or iron salts, reduce the absorption of ofloxacin, forming insoluble complexes (the time interval between administration of these drugs should be at least 2 hours).

Special instructions:

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

It is not recommended to be exposed to sunlight, irradiation with UV rays (mercury-quartz lamps, solarium).

To prevent the hyperconcentration of urine and subsequent crystalluria, during the treatment it is recommended to conduct adequate hydration.

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 (a dose reduction is required).

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

Form release / dosage:

Tablets, film-coated, 200 mg.

Packaging:

For 10 or 20 tablets in a contour mesh box made of polyvinylchloride film and aluminum foil printed lacquered.

For 1 or 2 contour packs with instructions for use are placed in a pack of cardboard.

Storage conditions:List B, B dry, protected from light at a temperature of no higher than 25 ° C. Keep out of the reach of children.

Shelf life: 2 years. Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:P N002493 / 01

Date of registration:21.07.2008

Expiration Date:Unlimited

The owner of the registration certificate:OBOLENSKOE PHARMACEUTICAL ENTERPRISE, CJSC OBOLENSKOE PHARMACEUTICAL ENTERPRISE, CJSC Russia

Manufacturer: & nbsp

OBOLENSKOE PHARMACEUTICAL ENTERPRISE, CJSC Russia

Representation: & nbspOBOLENSKOE PHARMACEUTICAL ENTERPRISE, CJSCOBOLENSKOE PHARMACEUTICAL ENTERPRISE, CJSCRussia

Information update date: & nbsp18.06.2017

Illustrated instructions

Instructions

Ofloxacin-OBL (Ofloxacin-OBL)