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

Description:Oval, biconvex tablets, white, with a risk on both sides. On one side of the tablet on one side of the risk of engraving "200", on the other - "A".

Pharmacotherapeutic group:Antimicrobial agent-fluoroquinolone

ATX: & nbsp

S.01.A.E.01 Ofloxacin

J.01.M.A.01 Ofloxacin

Pharmacodynamics:

The broad-spectrum antimicrobial agent from the group of fluoroquinolones acts on the bacterial DNA-gyrase enzyme, which provides super-convolution and thus the stability of bacterial DNA (the 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 freundii, Citrobacter koseri, Klebsiella spp. (including Klebsiella pneumonia), Enterobacter spp., Hafnia, Proteus spp. (including Proteus mirabilis, Proteus vulgaris - indole-positive and indole-negative), Salmonella spp., Shigella spp. (including Shigella sonnei), Yersinia enterocolitica, Campilobacter jejuni, Aeromonas hydrophila, Vibrio cholerae, Vibrio parahaemolyticus, Haemophilus influenzae, Chlamydia spp., Legionella spp., Serratia spp., Providencia spp., Haemophilus ducreyi, Bordetella parapertussis, Bordetella pertussis, Moraxella catarrhalis, Propionibacterium acnes, Brucella spp.

Different sensitivity to the drug has: Enterococcus faecalis, Streptococcus pneumoniae (penicillin-sensitive), Streptococcus pyogenes, Serratia marcescens, Pseudomonas aeruginosa, Acinetobacter, Mycoplasma hominis, Mycoplasma pneumoniae, Mycobacterium tuberculosis, and Mycobacterium fortuim, 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., Eubacterium 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 (TCmah) with oral intake - 1-2 hours, the maximum concentration (Cma) after the dose of 100 mg, 300 mg 600 mg is 1.3.4 and 6.9 mg / L and depends on the dose: after a single dose of 200 mg and 400 mg, it is 2.5 μg / ml 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 gland, penetrates well through the blood-brain barrier, the placental barrier, is secreted with the mother's milk. Penetrates into spinal fluid with inflamed and non-inflamed meninges (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. Out-of-site clearance - less than 20 %.

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

Indications:

Respiratory tract infections (bronchitis, pneumonia), LOP-organ (sinusitis, pharyngitis, otitis media, laryngitis), skin, soft tissues, bones, joints, infectious inflammatory diseases caused by microorganisms sensitive to ofloxacin, abdominal cavity and bile ducts, kidneys (pyelonephritis), urinary tract (cystitis, urethritis), (endometritis, salpingitis, oophoritis, cervicitis, parametritis, prostatitis), genital organs (colpitis, orchitis, epididymitis), gonorrhea, chlamydia, prevention of infections in patients with impaired immune status (including neutropenia).

Contraindications:

Hypersensitivity to ofloxacin, other fluoroquinolones, components of the drug; patients with rare hereditary diseases, such as lactose intolerance, lactase deficiency or glucose-galactose malabsorption (due to the presence of lactose), deficiency of glucose-6-phosphate dehydrogenase, tendon damage in previous treatment with fluoroquinolones; epilepsy (including in the anamnesis),reduction of convulsive threshold (including after traumatic brain injury, stroke or inflammatory processes in the central nervous system); age to 18 years (until the growth of the skeleton is completed), pregnancy, the period of breastfeeding.

Carefully:

Atherosclerosis of cerebral vessels, cerebral circulatory disorders (in the anamnesis), chronic renal failure, hepatic insufficiency, organic diseases of the central nervous system, predisposition to convulsive reactions, myasthenia gravis, hepatic porphyria, diabetes mellitus, congenital lengthening syndrome Q-T, heart disease (heart failure, myocardial infarction, bradycardia), psychoses and other mental disorders in the anamnesis; simultaneous reception of AC, extending the interval Q-T (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, LC, lowering blood pressure.

Pregnancy and lactation:

The drug is contraindicated in pregnancy and during breastfeeding.

Dosing and Administration:

Inside.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 - 200-800 mg per day, treatment course - 7-10 days, multiplicity of application - 2 times a day. A dose of up to 400 mg per day can be given in one session, preferably in the morning. With gonorrhea - 400 mg once.

In patients with impaired renal function (with creatinine clearance 50-20 ml / min), the recommended single dose is applied once a day. When creatinine clearance is less than 20 ml / min 1/2 the recommended single dose is applied once a day.

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 hemodialysis and peritoneal dialysis - 100 mg every 24 hours. The maximum daily dose for liver failure is 400 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 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: Dryness of the oral mucosa, dry cough, rhinitis, pharyngitis, pseudomembranous colitis, enterocolitis (including hemorrhagic), constipation, gastralgia, anorexia, nausea, vomiting, diarrhea, flatulence, abdominal pain, increased activity "liver" transaminases , hyperbilirubinemia, cholestatic jaundice, hepatitis.

From the nervous system: Headache, dizziness, ataxia, tremors, convulsions, numbness and paresthesias of extremities, intense dreams, "nightmarish" dream, psychotic reactions, anxiety, state of arousal, phobias, depression, confusion, hallucinations, drowsiness or insomnia, seizures, extrapyramidal disorder, psychotic reactions and suicidal, or sensornomotornaya sensory peripheral neuropathy, increased intracranial pressure.

From the side of the musculoskeletal system: Tendinitis, myalgia, arthralgia, tenosynovitis, tendon rupture, pain in the extremities, rhabdomyolysis, muscle weakness.

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 of arterial pressure, vasculitis, lengthening interval QT, ventricular arrhythmia, incl. arrhythmia ventricular tachysystolic type "pirouette".

Allergic reactions: Skin rash, itching, itching of the external genitalia in females, rash, hypersensitivity pneumonitis, allergic nephritis, eosinophilia, fever, angioedema, bronchoconstriction, Stevens-Johnson syndrome and toxic epidermal necrolysis, photosensitivity, erythema multiforme, anaphylactic shock.

From the skin: Petechial hemorrhages (petechiae), hemorrhagic bullous dermatitis, maculopapular rash with a crust, showing vascular involvement (vasculitis), acute attack of porphyria (in patients with porphyria).

On the part of the organs of hematopoiesis: Leukopenia, agranulocytosis, anemia (including hemolytic, aplastic), thrombocytopenia, pancytopenia, hemolytic and aplastic anemia, "tides" of blood to the skin.

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

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

Overdose:

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

Treatment: gastric lavage, symptomatic therapy. When hemodialysis is removed from 10 to 30% of the drug.

Interaction:

Food products, antacids containing 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).

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

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

Increases the concentration of glibenclamide in plasma.

Increases serum concentration of cyclosporine.

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.

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.

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 bicarbonate), the risk of crystalluria and nephrotoxic effects increases.

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, ultraviolet 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. In case of symptoms of peripheral neuropathy, the drug should be stopped. Rarely developing tendonitis can lead to rupture of tendons (mainly Achilles tendon), especially in elderly patients. In case of signs of tendinitis, it is necessary to immediately stop treatment, to make an immobilization of the Achilles tendon and consult an orthopedist.

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 (dose adjustment is required).

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

During the period of treatment can not be consumed ethanol.

Effect on the ability to drive transp. cf. and fur:During the period of treatment it is necessary to refrain from driving motor vehicles and practicing potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions.

Form release / dosage:

Tablets, film-coated, 200 mg.

Packaging:10 tablets per blister (PVC / aluminum foil). One blister, along with instructions for use, is placed in a cardboard pack.

Storage conditions:

In a dry place at a temperature of 15 to 25 ° C.

Keep out of the reach of children.

Shelf life:

3 of the year. Do not use after the expiry date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:LS-002400

Date of registration:29.12.2011

Expiration Date:Unlimited

The owner of the registration certificate:Mekofar Chemical-Pharmaceutical Joint Stock CompanyMekofar Chemical-Pharmaceutical Joint Stock Company Vietnam

Manufacturer: & nbsp

MEKOPHAR CHEMICAL-PHARMACEUTICAL, Joint Stock Company Vietnam

Representation: & nbspDominanta-Service CJSCDominanta-Service CJSC

Information update date: & nbsp16.06.2017

Illustrated instructions

Instructions

Ofloxacin DS (Ofloxacin DC)