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

Excipients: cellulose microcrystalline, croscarmellose sodium (impellose), povidone (polyvinylpyrrolidone low molecular medical), magnesium stearate, silicon dioxide colloid (aerosil), hypromellose (hydroxypropylmethylcellulose), titanium dioxide, macrogol (polyethylene glycol 4000), talc.

Description:The tablets covered with a film membrane of white or almost white color, round, biconcave. On the cross-section, two layers are visible, the inner layer of white with a yellowish hue of color.

Pharmacotherapeutic group: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, providing super-spiralization, 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 that produce 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 indol-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 pyogenes, Streptococcus pneumoniae, Streptococcus viridans, Serrratia marfromescens, Pseudomonas aeruginosa, Acinetobafromter spp., Mycoplasma hominis, Mycoplasma pneumoniae, Mycobacterium tuberculosis, Mycobacterium fortuitum, Ureaplasma urealyticum, Clostridium perfringens, Corynebacterium spp., Helicobacter pilori, 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 over 96%. Connection with blood plasma proteins - 25%.The time to reach the maximum concentration for oral administration is 1 to 2 hours. The maximum concentration depends on the dose: after a single dose of 200 mg or 400 mg or 600 mg, it is 2.5 μg / ml, 5 μg / ml, 6.9 μg / ml, respectively. Food can slow absorption, but does not have a significant effect on bioavailability.

Ofloxacin has a large volume of distribution (100 liters), so almost all the amount of the injected drug can freely penetrate into the cells, creating high concentrations in the organs, tissues and body fluids: cells (leukocytes, alveolar macrophages), skin, soft tissues, bones, abdominal organs cavity and small pelvis, respiratory system, urine, saliva, bile, the secret of the prostate gland; well penetrates the blood-brain barrier, the placental barrier, is secreted with the mother's milk. Penetrates into cerebrospinal 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 to 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 microorganisms sensitive to ofloxacin: respiratory tract infections (bronchitis, pneumonia), LOP(sinusitis, pharyngitis, otitis media, laryngitis), skin, soft tissues, bones, joints, abdominal cavity and bile ducts, kidneys (pyelonephritis), urinary tract (cystitis, urethritis), pelvic organs (endometritis, salpingitis, oophoritis , cervicitis, parametritis, prostatitis), genital organs (colpitis, orchitis, epididymitis), gonorrhea, chlamydia; prevention of infections in patients with impaired immune status (including with neutropenia).

Contraindications:

- Increased sensitivity or intolerance of ofloxacin and other derivatives of fluoroquinolone, quinolone;

- deficiency of glucose-6-phosphate dehydrogenase;

- the defeat of the tendons during the previous treatment with quinolones;

- epilepsy (including in the anamnesis);

- decreased convulsive threshold (incl.after traumatic brain injury, stroke or inflammatory processes of the central nervous system);

- age to 18 years (until the skeleton has been completed);

- pregnancy;

- lactation period;

- creatinine clearance less than 20 ml / min.

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 on an electrocardiogram (including in the anamnesis).

Pregnancy and lactation:Contraindicated.

Dosing and Administration:

Inside, not liquid, with a little water before or after eating. 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 course of treatment - 7-10 days, the frequency of application - 2 times a day. In severe infections or in the treatment of patients with overweight, the daily dose can be increased to 800 mg. 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 a creatinine clearance of 50-20 ml / min), the daily dose should not exceed 200 mg with a frequency of 1-2 times per day.The maximum daily dose for liver failure is 400 mg / day.

The duration of the course of treatment is determined by the sensitivity of the pathogen and the clinical picture. Treatment should continue for another 2-3 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: gastralegia, anorexia, nausea, vomiting, diarrhea, flatulence, abdominal pain, increased activity of "hepatic" transaminases, hyperbilirubinemia, cholestatic jaundice, pseudomembranous enterocolitis.

From the nervous system: headaches, dizziness, motion uncertainty, tremors, convulsions, numbness and paresthesia 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, lengthening the interval QT.

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), dermatitis bullous hemorrhagic, papular rash with a cortex, indicating the defeat of blood vessels (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, hypercreatininemia, increased urea levels.

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

Overdose:

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

Treatment: gastric lavage, symptomatic therapy. With hemodialysis, 10-30% of the drug is removed.

Interaction:

Food products, antacids, containing Al³⁺, Ca²⁺,Mg²⁺ or iron salts, reduce the absorption of ofloxacin, forming insoluble complexes (the time interval between the appointment of these drugs should be at least 2 hours).

Reduces ground clearance 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 the blood plasma.

Increases concentration glibenclamide in the plasma.

With simultaneous reception with antagonists of vitamin K it is necessary to control the blood coagulation system.

When appointed with nonsteroidal anti-inflammatory drugs, derivatives of nitroimidazole and methylxanthines the risk of neurotoxic effects increases.

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

When administered with drugs alkalinizing urine (inhibitors of carbonic anhydrase, citrates, sodium bicarbonate), the risk of crystalluria and nephrotoxic effects increases.

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

Special instructions:

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

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 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 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).

It is not recommended to use more than 2 months, during the treatment to be exposed to sunlight, irradiation with ultraviolet rays (mercury quartz lamps, solarium).

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).

Effect on the ability to drive transp. cf. and fur:During the treatment period, it is necessary to refrain from activities that require an increased concentration of attention and speed of psychomotor reactions (driving, working with potentially dangerous mechanisms), alcohol intake.

Form release / dosage:

Tablets, film-coated, 200 mg.

Packaging:For 10 tablets in a planar cell package.1 circuit cell pack together with the instruction for use is placed in a pack of cardboard.

Storage conditions:

List B. In a dry, the dark place at a temperature of no higher than 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:P N001953 / 01

Date of registration:23.01.2009

Expiration Date:Unlimited

The owner of the registration certificate:MAKIZ-PHARMA, LLC MAKIZ-PHARMA, LLC Russia

Manufacturer: & nbsp

MAKIZ-PHARMA, LLC Russia

Representation: & nbspMAKIZ-PHARMA, LLCMAKIZ-PHARMA, LLCRussia

Information update date: & nbsp18.06.2017

Illustrated instructions

Instructions

Ofloxacin STADA (Ofloxacin STADA)