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

Excipients (core): cellulose microcrystalline - 139.0 mg, potato starch - 60.0 mg, povidone (polyvinylpyrrolidone) - 32.0 mg, croscarmellose sodium 13.0 mg, magnesium stearate 6.0 mg.

Auxiliary substances (shell): hypromellose - 8.50 mg, macrogol - 4000 - 2.20 mg, titanium dioxide - 4.30 mg.

Description:

Round biconvex tablets, covered with a coat of white or almost white. On the break of the tablet, two layers are visible: a white or white core with a yellowish tint of color and a film membrane.

Pharmacotherapeutic group:Antimicrobial agent-fluoroquinolone

ATX: & nbsp

S.01.A.E.01 Ofloxacin

J.01.M.A.01 Ofloxacin

Pharmacodynamics:

The bactericidal effect of ofloxacin is associated with the inhibition of DNA gyrase, which leads to a disruption in the replication of bacterial DNA and the death of microbial cells.

Ofloxacin has a broad spectrum of antimicrobial action, including microorganisms resistant to other antibiotics, including strains that produce beta-lactamases.

Active (IPC ≤ 0.5 mg / l) for Gram-positive microorganisms: Staphylococcus aureus (methicillin-sensitive strains), Staphylococcus spp. (coagulase-negative); Gram-negative aerobic microorganisms: Aeromonas hydrophila, Citrobacter freundii, Enterobacter aerogenes, Enterobacter cloacae, Escherichia coli, producing and not producing beta-lactamase strains Haemophilus influenzae, Haemophilus parainfluenzae, Haemophilus ducreyi, Klebsiella oxytoca, Morganella morganii, Moraxella catarrhalis, producing and not producing beta-lactamase strains Neisseria gonorrhoeae, Neisseria meningitidis, Proteus mirabilis, Proteus vulgaris, Plesiomonas spp., Salmonella enterica, Shigella spp., Serratia marcescens, Yersinia enterocolitica; other microorganisms: Chlamydia trachomatis, Chlamydia pneumoniae, Mycoplasma hominis, Legionella pneumophila, Mycoplasma pneumoniae, Ureaplasma urealyticum.

Different sensitivity to the drug has: Acinetobacter spp., Gardnerella vaginalis, Pseudomonas aeruginosa Staphylococcus epidermidis, Staphylococcus haemolyticus, Staphylococcus hominis, Streptococcus pneumoniae (penicillin-sensitive and penicillin-resistant), Streptococcus pyogenes, Streptococcus spp. groups viridians, Streptococcus bovis, Streptococcus agalactae, Klebsiella pneumoniae, Mycobacterium leprae, Mycobacterium tuberculosis.

Are resistant to ofloxacin: Staphylococcus aureus (methicillin-resistant strains), Nocardia asteroides, Enterococcus spp., Treponema pallidum, Listeria monocytogenes, most anaerobes, including Peptostreptococcus spp., Eubacterium spp., Fusobacterium spp., Clostridium difficile.

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 is 1-2 hours, the maximum concentration of ofloxacin after a single dose of 200 mg and 400 mg is 2.5 μg / ml and 5 μg / ml, respectively.Eating can slow suction, but does not have a significant effect on bioavailability.

Quickly penetrates and is well distributed in many organs, tissues and fluids of the body, penetrates into cells. Therapeutically significant concentrations exceeding serum levels are observed in interstitial tissue, saliva, sputum, lung tissue, myocardium, bones, mucosa and intestinal wall, peritoneal fluid, pancreatic juice and pancreatic tissue, prostate gland, semen, pelvic organs , skin and subcutaneous tissue; penetrates into leukocytes and alveolar macrophages. Apparent volume of distribution 100 liters. It penetrates well through the blood-brain barrier, reaching therapeutic concentrations; in high concentrations passes through the hematoplacental barrier, excreted in breast milk. The connection with plasma proteins is approximately 25%.

The half-life is 4.5-7 hours. Less than 5% ofloxacin undergoes biotransformation in the liver. In the urine there are two main metabolites: dimethylfloxacin and N-oxide ofloxacin.

Excretion by the kidneys (80-90% of the dose) in unchanged form.

In small quantities is excreted through the intestine. In the bile ofloxacin is found in a glucuronated form. After a single dose of 200 mg in urine is detected within 20-24 hours. With renal / hepatic failure, excretion can be slowed down. Do not cumulate. When hemodialysis is removed 10-30% ofloxacin.

In elderly patients, the elimination half-life increases; total and renal clearance decrease in proportion to the decrease in creatinine clearance.

Indications:

Infectious-inflammatory diseases caused by microorganisms sensitive to ofloxacin:

- lower respiratory tract (bronchitis, pneumonia);

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

- skin and soft tissues;

- bones (osteitis, osteomyelitis) and joints;

- infections of the abdominal cavity and biliary tract;

- kidney and lower urinary tract;

- genital organs and pelvic organs (pelvioperitonitis, endometritis, salpingitis, oophoritis, tubo-ovarian abscesses, prostatitis);

- gonorrhea;

- prevention of infections in patients with impaired immune status

(including neutropenia).

Contraindications:

Hypersensitivity to ofloxacin, the components of the drug and other fluoroquinolones; epilepsy (including in the anamnesis), reduction of convulsive threshold (including after a craniocerebral injury, stroke or inflammatory processes in the central nervous system); chronic renal failure (with creatinine clearance less than 50 ml / min), children under 18 years of age, pregnancy, lactation period, tendon damage with previous treatment with fluoroquinolones.

Carefully:

Atherosclerosis of cerebral vessels, cerebral circulatory disorders (in the anamnesis), hepatic insufficiency, organic diseases of the central nervous system, predisposition to convulsive reactions, myasthenia gravis, hepatic porphyria, glucose-6-phosphate dehydrogenase deficiency, diabetes mellitus, congenital lengthening 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 Q-T (antiarrhythmic IA and III classes, tricyclic and tetracyclic antidepressants, neuroleptics, macrolides, antifungal, imidazole derivatives, some antihistamines, including astemizole, terfenadine, ebastine), for general anesthesia from the barbiturate group, drugs that lower blood pressure; electrolyte imbalance (eg, hypokalemia, hypomagnesemia); elderly age.

Pregnancy and lactation:

Ofloxacin is contraindicated for use in pregnancy.

As ofloxacin excreted into breast milk, then due to the risk to the child, breast-feeding women, women should not use the drug. In case of urgent need for the drug, breastfeeding at this time should be discontinued.

Dosing and Administration:

Inside. Tablets are taken whole, washed down with water, before or during meals. Doses are selected individually depending on the location and severity of the infection, as well as the sensitivity of microorganisms and the general condition of the patient and the function of the liver and kidneys.

In patients with normal renal function the drug is prescribed in a dose of 400-800 mg / day, the frequency of reception is 2 times a day.A dose of 400 mg per day is prescribed in one session, preferably in the morning.

With gonorrhea - 400 mg once.

In patients with impaired renal function (when creatinine clearance is less than 50 ml / min), 400 mg dose is not recommended. If necessary, use another dosage form in the form of 200 mg tablets.

When liver failure is not recommended to exceed the dose of ofloxacin 400 mg / day.

The duration of treatment depends on the localization and severity of the disease; treatment should continue for at least 48-72 hours after the disappearance of the symptoms of the disease and normalization of body temperature. In the treatment of uncomplicated and complicated infections of the lower urinary tract treatment course of 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.

Side effects:

From the digestive system: gastralgia, dryness of the oral mucosa, abdominal pain, diarrhea, nausea, vomiting, enterocolitis (in some cases, hemorrhagic), constipation, flatulence, pseudomembranous colitis.

From the nervous system: dizziness, headache, paresthesia,peripheral sensory neuropathy, peripheral sensory-motor neuropathy, seizures, extrapyramidal symptoms, including tremor, and other disorders of muscle coordination, increased intracranial pressure.

From the side of the musculoskeletal system: tendonitis, myalgia, arthralgia, tendon rupture (Achilles tendon), rhabdomyolysis and / or myopathy, muscle weakness, which is especially important for patients with pseudo-paralytic myasthenia gravis.

From the sense organs: irritation of the mucous membrane of the eye, vertigo, visual impairment, hearing impairment (ringing in the ears), hearing loss, dysgeusia (a perception disorder of taste), parosmia (odor perception disorder).

From the side of the cardiovascular system: decrease or increase in blood pressure, sinus tachycardia, "tides" of blood to the skin of the face.

Allergic reactions: skin rash, itching, angioedema, urticaria, pustular rash, multiforme erythema exudative (including Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell's syndrome), drug rash, photosensitivity, which in exceptional cases can lead to cutaneous necrosis,anaphylactic shock, allergic pneumonitis, bullous haemorrhagic dermatitis, allergic nephritis, eosinophilia.

Disturbances from the respiratory system and chest organs: dry cough, nasopharyngitis, shortness of breath, bronchospasm.

Disorders of the psyche: agitation, sleep disorders, insomnia, intense dreams, psychotic reactions (eg, hallucinations), anxiety, anxiety, nervousness, confusion, nocturnal nightmares, depression, psychotic reactions and depression with self-harm, in rare cases, up to suicidal thoughts or attempts.

From the skin: point hemorrhages (petechiae), vasculitis.

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

From the urinary system: increased serum creatinine concentration, acute renal failure, acute interstitial nephritis, increased urea concentration in the blood.

From the liver and biliary tract: increased activity of "hepatic" transaminases, alkaline phosphatase, increased bilirubin concentration, cholestatic jaundice, hepatitis.

Other: asthenia, superinfection, candidiasis, anorexia, hyperhidrosis, hypoglycemia (in patients with diabetes mellitus), porphyria attacks in patients with porphyria, intestinal dysbacteriosis, vaginitis, vaginal discharge.

Overdose:

Symptoms: dizziness, confusion, inhibition, disorientation, convulsions, drowsiness, vomiting, symptoms of irritation of the mucous membranes.

Treatment: gastric lavage, forced diuresis, symptomatic therapy.

Interaction:

Food products, antacids containing salts of aluminum, calcium, magnesium; iron preparations reduce the absorption of ofloxacin, forming insoluble complexes (the time interval between the intake of these drugs and ofloxacin should be at least 2 h).

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

Simultaneous reception of theophylline, fenbufen and other non-steroidal anti-inflammatory drugs with ofloxacin can increase convulsive activity.

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

Indirect anticoagulants: simultaneous administration with ofloxacin leads to an increase in the activity of coumarin derivatives, which requires monitoring of the parameters of the blood coagulation system.

Increases the concentration of glibenclamide, which requires monitoring the concentration of blood glucose.

When used simultaneously with glucocorticosteroids, the risk of rupture of tendons increases, especially in elderly patients.

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

Increases serum concentration of cyclosporine.

Possible lengthening interval Q-T with simultaneous use with drugs, lengthening interval Q-T (see section "C caution ").

Special instructions:

Ofloxacin is not a drug of choice for diseases of the upper and lower respiratory tract caused by pneumococci. Not indicated in the treatment of acute tonsillitis.

As with other fluoroquinolones, due to possible photosensitization,It is recommended to avoid prolonged exposure to direct sunlight or ultraviolet radiation.

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.

If a severe and prolonged diarrhea occurs during or after treatment, the diagnosis of pseudomembranous colitis should be ruled out, which requires immediate discontinuation of the drug and the appropriate treatment (oral administration of vancomycin and metronidazole). The use of drugs that inhibit intestinal peristalsis is contraindicated.

Ofloxacin inhibits growth Mycobacterium tuberculosis, which can lead to false-negative results of bacteriological tests in patients with tuberculosis.

Against the backdrop of treatment may worsen the flow of myasthenia, the increased frequency of porphyria in predisposed patients.

If there are side effects from the nervous system, allergic reactions need to cancel the drug.

In patients with diabetes, especially with the simultaneous use of hypoglycemic drugs, it is necessary to monitor the concentration of glucose in the blood.

In patients with impaired liver or kidney function, it is necessary to control the concentration of ofloxacin in the blood. In patients with renal insufficiency, dose adjustment of ofloxacin is necessary.

When determining opiates and porphyrins in urine, a false positive result can be obtained.When using the drug, women are not recommended to use hygiene tampons due to the increased risk of thrush development. For the treatment of mixed aerobic-anaerobic infections (endometritis, etc.) should be combined ofloxacin with one of the antibiotics that have antianaerobic activity.

Effect on the ability to drive transp. cf. and fur:

During the period of treatment, it is necessary to refrain from driving vehicles and practicing other potentially hazardous activities that require an increased concentration of attention and speed of psychomotor reactions.

Form release / dosage:

Film-coated tablets 400 mg.

Packaging:

For 5, 10 tablets in a contour mesh box made of polyvinylchloride film and aluminum foil printed lacquered.

By 10, 20, 30, 40, 50 or 100 tablets in cans of polymeric for medicines.

One jar or 1, 2, 3, 4, 5 or 10 contour mesh packages together with the instruction for use are placed in a cardboard package (bundle).

Storage conditions:

In the dark place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

3 years. Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:LP-002204

Date of registration:27.08.2013

Expiration Date:27.08.2018

The owner of the registration certificate:OZONE, LLC OZONE, LLC Russia

Manufacturer: & nbsp

OZONE, LLC Russia

Information update date: & nbsp18.06.2017

Illustrated instructions

Instructions

Ofloxacin (Ofloxacin)