Description
Release form
film-coated tablets
Packing
10 pcs.
Pharmacological action of
The bactericidal effect of ofloxacin is associated with the inhibition of bacterial DNA gyrase, which leads to the destabilization of bacterial DNA and the death of bacterial cells.
The prevalence of acquired resistance of certain bacterial species to ofloxacin may vary in different geographical regions and at different times, therefore it is very important to have information on the structure of local resistance, especially in the treatment of severe infections. If the structure of local resistance is such that the feasibility of using a particular drug is in doubt, you should seek the advice of microbiologists.
Ofloxacin has a wide spectrum of antimicrobial activity, including microorganisms that are resistant to other antibiotics, including strains that produce beta-lactamases.
sensitive microorganisms: Aerobic Gram-positive microorganisms -Staphylococcus aureus (metitsillinchuvstvitelnye), Staphylococcus epidermidis (metitsillinchuvstvitelnye), Staphylococcus saprophyticus, Streptococcus pneumoniae (penitsillinchuvstvitelnye), Streptococcus pyogenes aerobic Gram-negative organisms – Acinetobacter calcoaceticus, Bordetella pertussis, Citrobacter freundii, Enterobacter aerogenes, Enterobacter cloacae, Escherichia coli, Haemophilus ducreyi, Haemophilus influenzae, Klebsiella oxytoca, Klebsiella pneumoniae, Moraxella catarrhalis, Morganella morganii, Neisseria gonorrhoeae, Proteus vulgaris, Providencia rettgeri, Providencia stuartii, Pseudomonas aeruginosa (quickly develops resistance), Serratia marcescens anaerobic microorganisms – Clostridium perfringens, other microorganisms – Chlamydia pneumoniae, Chlamydia trachomatis, Gardnerella vaginalis, Legionella pneumophila, Mycoplasmaummalamisapismalaminapismalaminapismalaminapismalamisapislomamalamis
In most cases, insensitive: Nocardia asteroids anaerobic microorganisms – Bacteroides spp., Clostridium difficile, Eubacterium spp., Fusobacterium spp., Peptococcus spp., Peptostreptococcus spp., Enterococcus sppcus., most. does not affect Treponema pallidum.
The mechanism of bacterial resistance to ofloxacin is associated with one or more mutations of the target enzymes, which are mainly resistant to other fluoroquinolones.
Pharmacokinetics
Absorption after oral administration is fast and complete (about 95%). Bioavailability is 96%. About 25% of the administered dose binds to plasma proteins. The maximum concentration (Cmax) = 2.6 μg / ml is achieved 1 hour after ingestion of 200 mg of the drug. The apparent volume of distribution is 100 liters. It penetrates quickly and is well distributed in many organs, tissues and body fluids, penetrates into the cells. Therapeutically significant concentrations in excess of plasma concentrations are observed in the interstitial tissue, saliva, sputum, lung tissue, myocardium, bones, mucous membrane and wall of the intestine, peritoneal fluid, pancreatic juice and pancreatic tissue, prostate tissue, seminal fluid, organs female reproductive system, skin and subcutaneous tissue penetrates into white blood cells and alveolar macrophages. It penetrates well through the blood-brain barrier, reaching therapeutic concentrations, in high concentrations it penetrates the blood-brain barrier, excreted in breast milk. 14-60% penetrates into the cerebrospinal fluid. Biotransformation in the liver undergoes about 5% of the administered dose. The main metabolites of ofloxacin are: N-oxide and N-dimethylofloxacin. The half-life (F / 4) is 5.7-7 hours and does not depend on the dose administered. With multiple injections, the cumulative effect is not pronounced, plasma concentrations increase slightly. Ofloxacin is excreted mainly by the kidneys unchanged (80-90% of the administered dose), about 4% – with bile. Extrarenal clearance – 20%. After administration at a dose of 200 mg, the total clearance is 258 ml / min. In small quantities, it is excreted through the intestines. In patients with T1 / 2 renal insufficiency, ofloxacin increases overall and renal clearance decreases proportionally. With hemodialysis, 10-30% ofloxacin is removed. With liver failure, excretion may be slowed
Indications
Infectious and inflammatory diseases caused by microorganisms sensitive to ofloxacin, including:
lower respiratory tract (exacerbation of chronic bronchitis, pneumonia)
of the kidneys and urinary tract, including pyelonephritis, urethritis
of the genitals and pelvic organs, including cervicitis, prostatitis
of the skin and soft tissues.
Contraindications
Hypersensitivity to ofloxacin, other quinolones, or other components of the drug under 18 years of age pregnancy breast-feeding deficiency of glucose-6-phosphate dehydrogenase epilepsy, including a history of a decrease in the seizure threshold after cranial stroke, including cranial threshold cerebral trauma, acute cerebrovascular accident, inflammatory diseases of the central nervous system of the tendon lesion amid previous administration of fluoroquinolones lacto intolerance PS, lactase deficiency, glucose-galactose malabsorption, peripheral neuropathy.
Precautions
Organic Brain Disease, including cerebral arteriosclerosis, cerebrovascular accident (history) predisposition to convulsive reactions myasthenia gravis impaired renal function (creatinine clearance (CC) less than 50 ml / min) severe liver dysfunction liver porphyria diabetes mellitus heart disease, including chronic heart failure, myocardial infarction, bradycardia, paroxysmal ventricular tachycardia such as pirouette, congenital lengthening of the QT interval, concomitant use of drugs, lengthening constituents interval QT, including antiarrhythmics IA and Class III, tricyclic and tetracyclic antidepressants, neuroleptics, macrolides, antifungals, imidazole derivatives, some antihistamines (astemizole, terfenadine, ebastin) the simultaneous administration of drugs for non-inhalation general anesthesia from the group of barbiturates, antihypertensive drugs, psychoses and other mental disorders, including a history of electrolyte imbalance (for example, with hypokalemia, with hypomagnesemia) elderly age.
Special instructions
Ofloxacin should not be prescribed as the first choice for treating community-acquired pneumonia caused by Streptococcus pneumoniae and Mycoplasma spp., and acute tonsillitis caused by Streptococcus pyogenes.
Superinfection is possible due to the growth of ofloxacin-insensitive microorganisms, especially Enterococcus spp. and Candida spp. In this case, it is necessary to conduct tests for sensitivity to antibiotics and adjust the treatment regimen. If severe and prolonged diarrhea occurs during or after treatment with ofloxacin, it is necessary to exclude the possibility of developing pseudomembranous colitis, confirmation of which requires discontinuation of the drug.
Ofloxacin inhibits the growth of Mycobacterium tuberculosis, which may lead to false negative results of bacteriological tests in patients with tuberculosis.
Although ofloxacin rarely causes photosensitivity, it is recommended to avoid prolonged exposure to direct sunlight or artificial ultraviolet radiation (UVI) (tanning beds, UVI treatment) during treatment with this drug. To prevent excessive salt in the urine and subsequent crystalluria during treatment, it is recommended to carry out adequate hydration.
Rarely occurring tendonitis can lead to rupture of tendons (mainly Achilles tendon). The risk of tendon rupture increases when taking fluoroquinolones while taking GCS. Tendonitis often develops in elderly patients. In case of signs of tendonitis, it is necessary to immediately stop treatment, immobilize the Achilles tendon and consult an orthopedist.
When using ofloxacin, women should not use sanitary tampons due to the increased risk of developing thrush.
In patients predisposed to the development of paroxysmal ventricular tachycardia such as pirouette or taking drugs that extend the QT interval, and also to detect ventricular conduction disturbances before treatment with ofloxacin, it is necessary to conduct an electrocardiogram (ECG) study and regularly monitor ECG parameters during treatment.
With a treatment duration of more than 2 weeks, it is necessary to monitor the parameters of the blood formula and the biochemical parameters of the blood.
Ethanol should not be consumed during treatment.
When used simultaneously with indirect anticoagulants, it is necessary to control the coagulation system of the blood.
With simultaneous use with hypoglycemic drugs, both hypo- and hyperglycemia are possible, in connection with which it is necessary to control the concentration of glucose in the blood plasma.
In patients with impaired renal function (CC less than 50 ml / min), severe impairment of liver function requires dose adjustment of ofloxacin (see section Dosage and Administration).
In case of liver disease, it is necessary to determine indicators of the functional state of the liver before treatment with ofloxacin, as well as monitor these indicators during treatment.
In patients with impaired liver or kidney function, plasma monitoring of ofloxacin concentration is necessary. In severe renal and hepatic insufficiency, the risk of toxic effects increases (reducing dose adjustment is required).
During treatment with ofloxacin, the course of myasthenia gravis and frequent attacks of porphyria may worsen.
In patients receiving fluoroquinolones, including ofloxacin, the development of sensory and sensory-motor neuropathy, which can have a quick onset, has been reported. When symptoms of neuropathy appear, treatment with ofloxacin should be discontinued, which helps minimize the possible risk of developing irreversible conditions.
Ofloxacin-Teva should be used with caution in patients with a history of seizures (patients with a central nervous system (CNS) history, including cerebrovascular accident, patients taking NSAIDs, and other drugs that lower the seizure threshold of the brain, such as theophylline) (see Interaction with Other Medicines section).
In case of adverse reactions from the central nervous system and allergic reactions, a change of the drug is necessary.
Influence on the results of laboratory tests: with treatment with ofloxacin, false-positive results are possible in the determination of opiates and porphyrins in urine.
Influence on the ability to drive a car and control mechanisms
During treatment with ofloxacin, care should be taken when driving vehicles and controlling mechanisms due to the possibility of developing side effects from the nervous system (dizziness, drowsiness) that affect the ability to concentrate and speed psychomotor reactions .
Composition
1 tablet contains: active substance ofloxacin 200.0 mg
excipients: lactose monohydrate 105.6 mg, pregelatinized starch 54.0 mg, hypromellose 20.0 mg, croscarmellose sodium 16.0 mg, silicon dioxide colloidal 0.4 mg, magnesium stearate 4.0 mg, Opadry II white shell 33G28707 (hypromellose-6cP 6.00 mg, titanium dioxide E171 3.60 mg, lactose monohydrate 3.30 mg, macrogol-3000 1.20 mg, triacetin 0.90 mg).
Dosage and Administration
Inside. The dose of ofloxacin should be selected depending on the type and severity of the infection, as well as the general condition of the patient and liver and kidney function. Tablets are taken whole, washed down with water, before or during meals.
200-800 mg per day in 2 divided doses at regular intervals. A dose of up to 400 mg per day can be taken in one dose, preferably in the morning.
Patients with impaired renal function (CC less than 50 ml / min) require correction of the dosage regimen depending on the value of CC.
KK Plasma creatinine concentration (mg / dl), / td> Dose and frequency of administration of
20-50 ml / min 1.5-5.0 100-200 mg every 24 hours
Less than 20 ml / min or hemodialysis and peritoneal dialysis At least 5.0 100 mg every 24 hours or 200 mg every 48 hours
After hemodialysis or peritoneal dialysis, additional doses are not required.
Creatinine clearance can be calculated using the formulas below.
For men: [body weight (kg) x (140 – age (full years))] / [72 x plasma creatinine concentration (mg / dl)]
For women: 0.85 x CC of men
In patients with severe impaired liver function, ofloxacin excretion may be reduced. In such cases, the daily dose of ofloxacin should not exceed 400 mg.
In elderly patients, dose adjustment is not required.
Duration of treatment is determined by the sensitivity of the pathogen, the severity of the infectious disease and the response to therapy. Treatment should be continued for at least 3 days after full normalization of body temperature or after confirmation of the eradication of the bacterial agent. Typically, the duration of treatment is 7-10 days, with the exception of the treatment of gonorrhea, and should not exceed 2 months.
Side effects
The frequency of adverse reactions is classified according to the recommendations of the World Health Organization: very often – at least 10% often – at least 1%, but less than 10% infrequently – at least 0.1%, but less than 1% rarely – not less than 0.01%, but less than 0.1% very rarely – less than 0.01%, including individual messages.
From the digestive system: often – nausea, vomiting, diarrhea, abdominal pain infrequently – decreased appetite, constipation, flatulence rarely – increased activity of hepatic transaminases, hyperbilirubinemia, cholestatic jaundice, colitis (including hemorrhagic), dry oral mucosa is very rare – hepatitis, pseudomembranous colitis.
From the nervous system: infrequently – headache, dizziness, insomnia, anxiety, nervousness rarely – nightmares, intense dreams, psychotic reactions, anxiety, a state of agitation, phobias, depression, confusion, hallucinations, suicidal attempts, drowsiness, tremor, cramps, numbness and paresthesia of the extremities, insecurity of movements, increased intracranial pressure is very rare – extrapyramidal disorders, sensory or sensory-motor neuropathy, peripheral neuropathy.
From the sensory organs: infrequently – conjunctivitis is rare – impaired color perception, diplopia, taste disturbances, smell, balance is very rare – tinnitus, hearing impairment, including deafness in exceptional cases.
From the musculoskeletal system: very rarely – tendonitis, myalgia, muscle weakness in patients with myasthenia gravis, arthralgia, tendosynovitis, tendon rupture, muscle and joint symptoms of rhabdomyolysis, limb pain.
From the cardiovascular system: infrequently – palpitations rarely – heart failure, hypotension very rarely – ventricular arrhythmias, including paroxysmal ventricular tachycardia such as pirouette, prolongation of the QT interval, hypertension.
From the respiratory system: infrequently – dry cough, rhinopharyngitis rarely – shortness of breath, bronchospasm unknown frequency – allergic pneumonitis.
From the skin and subcutaneous tissues: very rarely – petechiae, bullous hemorrhagic dermatitis, papular rash with a crust, evidence of vascular damage (vasculitis).
From the blood system and hemopoietic organs: very rarely – leukopenia, including agranulocytosis, anemia (including hemolytic and aplastic), thrombocytopenia, pancytopenia, exacerbation of porphyria.
From the urinary system: very rarely – acute interstitial nephritis, impaired renal function, hypercreatininemia, increased urea concentration, dysuria, urinary retention, acute renal failure.
Allergic reactions: infrequently – skin rash, pruritus, urticaria, very rarely – erythema multiforme exudative (including Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell’s syndrome), photosensitivity, allergic pneumonitis, allergic nephritis, eosinofeci, ichorothyroidism, bronchospasm hypotension, hypertension, anaphylactic shock, itching of the external genital organs in women.
Other: very rare – intestinal dysbiosis, superinfection, chest pain, hyper- or hypoglycemia (in patients with diabetes mellitus with antidiabetic drugs), nosebleeds, thirst, weight loss, vaginitis, vaginal discharge, fatigue, asthenia general weakness.
Drug Interactions
With the simultaneous use of ofloxacin with sucralfate, antacid preparations and other preparations containing metal ions (aluminum, magnesium, zinc or iron), the absorption of ofloxacin decreases. Ofloxacin should be taken 2 hours before or 2 hours after taking these drugs.
It is possible to increase the effectiveness of indirectly acting anticoagulant drugs (coumarin derivatives), including warfarin, while taking it with ofloxacin. It is necessary to control the coagulation system of the blood.
With simultaneous use with non-steroidal anti-inflammatory drugs (NSAIDs), including fenbufen, as well as derivatives of nitroimidazole and methylxanthines, the risk of developing neurotoxic effects, including a decrease in the threshold for convulsive activity, is increased.
With the simultaneous use of ofloxacin and theophylline, theophylline clearance decreases by 25% and T1 / 2 of theophylline increases.
With simultaneous use with hypoglycemic drugs, both hypo- and hyperglycemia may develop. When used with glibenclamide, it increases the concentration of glibenclamide in the blood plasma and causes a state of hypoglycemia, in connection with which it is necessary to control the concentration of glucose in the blood plasma.
With simultaneous use with cyclosporine, an increase in T1 / 2 and Cmax of cyclosporine in blood plasma is noted.
Probenecid, cimetidine, furosemide, methotrexate with simultaneous use of ofloxacin reduce tubular secretion of ofloxacin, which leads to an increase in the concentration of ofloxacin in blood plasma.
With simultaneous use with drugs that extend the QT interval, including antiarrhythmic drugs of classes IA and III, tricyclic and tetracyclic antidepressants, antipsychotics, macrolides, antifungal drugs, imidazole derivatives, some antihistamines (astemizole, terfenadine, ebastin) prolongation of the QT interval is possible.
With simultaneous use with non-inhalational general anesthesia drugs from the barbiturate group, antihypertensive drugs, a sharp and significant decrease in blood pressure is possible, therefore, monitoring of the cardiovascular system is required in this case.
Concomitant use with glucocorticosteroids (GCS) increases the risk of tendon rupture, especially in elderly patients.
When used with drugs that alkalinize urine (carbonic anhydrase inhibitors, citrates, sodium bicarbonate), the risk of crystalluria and nephrotoxic effects increases.
Ofloxacin is not compatible with ethanol.
Overdose
Symptoms: dizziness, confusion, lethargy, disorientation, convulsions, drowsiness, vomiting, mucous membrane irritation symptoms.
Treatment: gastric lavage, forced diuresis, symptomatic therapy for stopping neurological disorders (convulsive syndrome) use diazepam.
Storage conditions
Do not store above 25 ° C in a dark place.
Keep out of the reach and sight of children.
The Expiration of
is 3 years.
lekarstvennaja form
tablets
Indications Indications
from prostatitis, cystitis, from otitis media, From skin infections, From urinary tract infections, From sinusitis, From osteomyelitis, From lung inflammation, Bronchitis, From bile duct infections, From female genital infections, From urethritis, From sinusitis
Teva Pharmaceutical Enterprises Co., Ltd.,
