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

Active substance: ofloxacin - 200 mg. Excipients: microcrystalline cellulose, potato starch, polyvidone (kollidon 25), calcium stearate, talc, aerosil, hydroxypropyl cellulose, titanium dioxide, tween-80.

Description:

Tablets are round, biconvex, covered with a coat of white color. 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 enzyme DNA hydrase, which ensures super-shrinkage 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, 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, Plesiomonas 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.

Different sensitivity to the drug has: Enterococcus faecalis, Streptococcus pyogenes, pneumoniae and viridans, Serratio marcescens, Pseudomonas aeruginosa, Acinetobacter, Mycoplasma hominis and 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 over 96%, the connection with plasma proteins is 25%, TCmat oral intake - 1-2 hours, Cmax after taking 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. 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.

Indications:

Respiratory tract infections (bronchitis, pneumonia), LOP-organov (sinusitis, pharyngitis, otitis, laryngitis), skin, soft tissue, bone, joints, infectious and inflammatory diseases of the abdominal cavity and biliary tract (except bacterial enteritis), kidney (pyelonephritis)urinary tract (cystitis, urethritis), pelvic organs (endometritis, salpingitis, oophoritis, cervicitis, parametritis, prostatitis), genital organs (colpitis, orchitis, epididymitis), gonorrhea, chlamydia; meningitis; prevention of infections in patients with impaired immune status (including neutropenia).

Contraindications:

Hypersensitivity, deficiency of glucose-6-phosphate dehydrogenase, epilepsy (including in the anamnesis), reduction of convulsive threshold (including after cerebrospinal trauma, stroke or inflammatory processes in the central nervous system); age to 18 years (until the growth of the skeleton is completed), pregnancy, lactation.

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

Pregnancy and lactation:Contraindicated.

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, the course of treatment - 7-10 days, the frequency 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: creatinine clearance 50-20 ml / min - single dose - 50% of the average, 2 times a day or a full single dose administered once a day. When creatinine clearance is less than 20 ml / min, a single dose of 200 mg, then - 100 mg per day every other day.

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: gastralgia, anorexia, nausea, vomiting, diarrhea, flatulence, abdominal pain, increased activity of "liver" transaminases, hyperbilirubinemia, cholestatic jaundice, pseudomembranous enterocolitis.

From the nervous system: headache, dizziness, motion uncertainty, tremor,convulsions, numbness and paresthesia of the extremities, 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, tenosynovitis, rupture of the tendon.

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, collapse.

Allergic reactions: skin rash, itching, hives, allergic pneumonitis, allergic nephritis, eosinophilia, fever, Quincke's edema, bronchospasm, Stevens-Johnson and Lyell syndrome, photosensitivity, erythema multiforme, rarely anaphylactic shock.

From the skin: pinpoint hemorrhages (petechiae), dermatitis bullous hemorrhagic, papular rash with 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 content.

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

Overdose:

Symptoms: dizziness, confusion, inhibition, disorientation, drowsiness, vomiting. Treatment: gastric lavage, symptomatic therapy.

Interaction:

Food products, antacids containing A13 +, Ca2 +, Mg2 + 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.

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 developing neurotoxic effects 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 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, be 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 tendinitis, it is necessary to immediately stop treatment, to make an immobilization of the Achilles tendon and consult an orthopedist.

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, one should not use ethanol.

When using the drug, women are not recommended to use tampons like "Tampax", 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).

Children are only used in case of a life threat, taking into account the prospective benefit and the potential risk of side effects, when it is impossible to use other, less toxic drugs. The average daily dose in this case is 7.5 mg / kg, the maximum - 15 mg / kg.

Form release / dosage:

The tablets covered with a cover, on 200 mg.

Packaging:For 10 tablets in a planar cell package. For 10 or 20 tablets in polymer cans or polystyrene cans. Each bank, 1 or 2 contour mesh packs, along with instructions for medical use, are placed in a cardboard box.

Storage conditions:

List B. In a dry, dark place, out of the reach of children, at a temperature of no higher than 25 ° C.

Shelf life:

2 years. Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:P N003417 / 01

Date of registration:18.06.2009

Expiration Date:Unlimited

The owner of the registration certificate:VALENTA PHARM, PAO VALENTA PHARM, PAO Russia

Manufacturer: & nbsp

VALENTA PHARMACEUTICS, JSC Russia

Information update date: & nbsp16.06.2017

Illustrated instructions

Instructions

Ofloxacin (Ofloxacin)