Composition, form of production and packaging
The tablets covered with a film membrane white with a yellowish tinge are oblong, biconcave, with a separation groove and engraved "M" on the left side and "XI" on the right side of the groove on both sides of the tablet.
1 tab.
ofloxacin 200 mg
[PRING] lactose, starch, giprolose (hydroxypropylcellulose), carmellose (carboxymethyl cellulose), magnesium stearate, hypromellose (hydroxypropylmethylcellulose), macrogol (polyethylene glycol) 8000, titanium dioxide (E171), talc.
10 pieces. - packings of cellular contour (1) - packs cardboard.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2011.
PHARMACHOLOGIC EFFECT
Antimicrobial drug from the group of fluoroquinolones of broad spectrum of action. It is bactericidal. The mechanism of the action of ofloxacin is associated with the blockade of the DNA-gyrase enzyme in bacterial cells.
Highly active against most Gram-negative and some Gram-positive microorganisms : Aeromonas hydrophila, Branhamella catarrhalis, Brucella spp., Clostridium perfringens, Esherichia coli, Salmonella spp., Enterobacter spp., Serratia spp., Citrobacter spp., Yersinia spp., Providencia spp., Haemophilus influenzae and parainfluenzae, Haemophilus ducreyi, Plesiomonas, Legionella, Shigella spp., Proteus spp., Including Proteus mirabilis, Proteus vulgaris (indole + and indole-), Moraxella morganii, Klebsiella spp., Including Klebsiella pneumoniae, Helicobacter pylori, Mycoplasma spp ., Vibrio spp., Gardnerella vaginalis. Neisseria gonorrhoeae, Neisseria meningitidis, Chlamydia trachomatis, Staphylococcus aureus methi-S, Staphylococcus coagulase negative. Mildly sensitive to ofloxacin, Acinetobacter spp., Ureaplasma urealyticum, Bacteroides fragilis, Mycobacterium tuberculosis, Mycobacterium leprae, Chlamidia psittaci, anaerobic gram-positive cocci, Enterococcus faecalis, Streptococcus pneumoniae, Pseudomonas spp, Streptococcus spp. (especially beta-hemolytic).
To ofloxacin, Acinetobacter braumanmii, Clostridium difficile, Enterococci, Listeria monocytogenes, Staphylococci methi-R, Nocardia spp. Are insensitive.
Ofloxacin is inactive with respect to Treponema pallidum.
PHARMACOKINETICS
Once ingested, ofloxacin is rapidly and almost completely absorbed from the digestive tract. Biodostupity is almost 100%. C max ofloxacin in blood plasma after taking a single dose of 200 mg is 2.5-3 Ојg / ml and is achieved after 1 hour. Binding to plasma proteins is 25%. Metabolized about 5% ofloxacin. T 1/2 - 6-7 h. V dapproximately 120 l. Up to 90% ofloxacin is excreted by the kidneys in unchanged form, about 4% with bile.
INDICATIONS
Treatment of infectious-inflammatory diseases caused by microorganisms sensitive to ofloxacin:
- respiratory tract infections (except for cases of pneumococcal infection);
- infections of the ear, throat, nose (except for cases of acute tonsillitis);
- infection of the abdominal cavity and bile ducts;
- infections of the kidneys, urinary tract, prostate, urethra (including gonococcal nature);
- infections of the pelvic organs;
- infections of bones and joints;
- skin and soft tissue infections;
- prevention of infections in patients with impaired immune status (including neutropenia).
DOSING MODE
Inside.
The dose of ofloxacin and the duration of treatment depend on the severity and type of infection, the general condition of the patient and the function of the kidneys.
The average daily intake for adults is from 200 mg to 600 mg. Duration of treatment is 7-10 days.
A dose of up to 400 mg / day can be given in one session, preferably in the morning. Doses over 400 mg / day should be divided into 2 divided doses with an equal time interval. Tablets should be taken whole, washed down with water before and during meals. It is necessary to avoid simultaneous reception together with antacids.
In severe infections or in the treatment of patients with overweight, the daily dose can be increased to 800 mg.
In uncomplicated infections of the lower urinary tract, the drug is prescribed at a dose of 200 mg / day for 3-5 days.
With gonorrhea prescribed 400 mg once.
In patients with impaired renal function, the dose should be reduced depending on the creatinine clearance:
Creatinine clearance Single dose Interval between doses
50-20 ml / min 100-200 mg 24 hours
less than 20 ml / min or hemodialysis 100 mg 24 hours
hemodialysis less than 20 ml / min or hemodialysis 200 mg 48 hours
In patients with hepatic insufficiency it is not recommended to exceed the maximum daily dose of 400 mg.
Initiated iv treatment withloxacin can be continued with the tablet form of the drug at the same dose (with improvement of the patient's condition).
SIDE EFFECT
The information below is based on clinical trials and on a broad post-marketing experience with the drug.
Individual cases:
• Anaphylactic / anaphylactoid reactions, skin and mucosal reactions
Uncommon: Rare:
Symptoms such as: itching, rashes, burning in the eyes, dry cough, rhinitis.
Anaphylactic / anaphylactoid reactions such as urticaria, angioedema, choking / bronchospasm; hyperemia, sweating, papular rash.
Anaphylactic / anaphylactoid shock, multiforme exudative erythema, toxic epidermal necrolysis, photosensitivity, persistent drug rash, vascular purpura, bullous hemorrhagic dermatitis, pinpoint hemorrhages, vasculitis, which in exceptional cases can lead to skin necrosis.
Separate Stevens-Johnson Syndrome, severe suffocation, allergic
cases: pneumonitis, allergic nephritis.
• From the gastrointestinal tract
Infrequently Abdominal pain, diarrhea, nausea, vomiting, decreased appetite,
meeting:
Rare: Anorexia, flatulence, enterocolitis, which can in individual
cases of being hemorrhagic. Very rare: Pseudomembranous colitis.
• Neurological
Excitation, dizziness, headache, sleep disturbance / insomnia.
Psychotic reactions (eg, hallucinations), anxiety, confusion, intense or "nightmarish" dreams, depression, drowsiness, peripheral sensitivity disorders, such as paresthesia, taste and smell disturbance, color dysfunction, diplopia. Hearing impairment, such as tinnitus or hearing loss, epileptic seizures, extrapyramidal disorders or other disorders of muscle coordination, hypoesthesia, tremor, convulsions.
Psychotic reactions accompanied by dangerous behavior for the patient, including suicidal tendencies, increased intracranial pressure.
Cardiovascular
Reduction of blood pressure, tachycardia.
Locomotorium
Rare: Tendonitis.
Very rarely: Arthralgia, myalgia.
Tendon tendon rupture (i.e. Achilles tendon); as with the use of other fluoroquinolones, this side effect can be observed within 48 hours after the initiation of treatment and may be bilateral.
Individual rhabdomyolysis (acute necrosis of skeletal muscles) and / or myopathy.
Cases: Muscular weakness, which may be particularly important
value in patients with severe pseudo-paralytic myasthenia gravis.
• From the side of the liver
Cholestatic jaundice.
Hepatitis, which can be severe.
Rare: Increased hepatic enzymes (ACT, ALT, LDH, GTT and / or
alkaline phosphatase) and / or bilirubin.
From the urinary system
Hypercreatinemia, increased urea concentration. Acute kidney failure. Interstitial nephritis.
Anemia, hemolytic anemia, leukopenia, eosinophilia, thrombocytopenia.
Agranulocytosis, pancytopenia, oppression of bone marrow hematopoiesis.
Development of secondary infection caused by drug-resistant microorganisms and fungi.
Acute attacks of porphyria in patients with porphyria, vaginitis, intestinal dysbiosis, hypoglycemia in patients with diabetes treated with hypoglycemic drugs.
CONTRAINDICATIONS
- epilepsy;
- lesions of the central nervous system with a lower convulsive threshold (after craniocerebral trauma, stroke, inflammatory processes in the central nervous system (CNS);
- lesions of tendons during the previous treatment with quinolones;
- age up to 18 years;
- pregnancy and lactation;
- hypersensitivity to ofloxacin, other quinolones or components of the drug.
With caution : in patients with atherosclerosis of the cerebral vessels, blood circulation disorder (in the anamnesis), chronic renal failure, organic CNS lesions, with prolongation of the QT interval.
PREGNANCY AND LACTATION
Contraindicated in pregnancy and lactation.
APPLICATION FOR FUNCTIONS OF THE LIVER
In patients with impaired renal function, the dose should be reduced depending on the creatinine clearance:
Creatinine clearance Single dose Interval between doses
50-20 ml / min 100-200 mg 24 hours
less than 20 ml / min or hemodialysis 100 mg 24 hours
hemodialysis less than 20 ml / min or hemodialysis 200 mg 48 hours
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
In patients with hepatic insufficiency it is not recommended to exceed the maximum daily dose of 400 mg.
APPLICATION FOR CHILDREN
Contraindicated in children under 18 years.
SPECIAL INSTRUCTIONS
Renal insufficiency
Due to the fact that ofloxacin is excreted mainly through the kidneys, patients with renal insufficiency need a dose adjustment of ofloxacin.
Prevent photosensitivity
During the treatment with ofloxacin, due to the risk of photosensitization, exposure to bright sunlight and ultraviolet rays should be avoided.
Secondary infection
As with other antibiotics, taking ofloxacin, especially prolonged, can cause a secondary infection associated with the growth of resistant to the drug microorganisms.A reassessment of the patient's condition is necessary. If a secondary infection occurs during therapy, appropriate measures must be taken.
Pseudomembranous colitis
The appearance of diarrhea, especially in severe form, persistent and / or with an admixture of blood, during or after treatment with ofloxacin may be a manifestation of pseudomembranous colitis. If the pseudomembranous colitis is suspected, the treatment with ofloxacin should be discontinued immediately, and appropriate specific antibiotic therapy (eg, vyakomitsin inside, teicoplanin inside or metronidazole) should be given promptly. In this clinical situation, drugs that suppress the intestinal peristalsis are contraindicated.
Patients who are prone to epileptic seizures
Like other quinolones, ofloxacin should be given with extreme caution to patients predisposed to developing epileptic seizures (patients with a history of central nervous system history who take fenbufen and similar non-steroidal anti-inflammatory drugs or drugs that lower the seizure threshold, such as theophylline).
Tendonitis
Tendinitis, which occurs very rarely, can sometimes lead to the rupture of tendons, mainly the Achilles tendon, especially in elderly patients. In case of signs of tendinitis (inflammation of the tendon), it is recommended to immediately stop the treatment, immobilize the Achilles tendon and provide orthopedic consultation.
QT interval extension
Some caution is needed when taking fluoroquinolones, including ofloxacin, in patients with known risk factors for prolonging the QT interval, such as:
- elderly age;
- uncorrectable imbalance of electrolytes (eg, hypokalemia, hypomagnesemia);
- congenital extension of the QT interval;
- diseases of the cardiovascular system (heart failure, myocardial infarction, bradycardia)
- simultaneous reception of drugs that extend the interval of QT (IA and III classes of antiarrhythmic drugs, tricyclic antidepressants, macrolides).
Myasthenia gravis
Ofloxacin can lead to a worsening of myasthenia flow.
Porphyria
Perhaps more frequent attacks of porphyria. During the treatment with ofloxacin, false-positive results are possible when determining opiates and porphyrins in urine.
Other
Ofloxacin prevents the release of Mycobacterium tuberculosis, leading to false-negative results in the bacteriological diagnosis of tuberculosis.
Also during the treatment is not recommended to use ethanol.
When using the drug, women are not recommended to use hygiene tampons due to the increased risk of thrush development.
Ofloxacin is not a drug of choice for pneumonia caused by pneumococci.
Not indicated in the treatment of acute tonsillitis.
Impact on the ability to drive vehicles and manage mechanisms
Some adverse reactions, for example: dizziness, drowsiness, and visual impairments can reduce the reaction and the ability to concentrate, and therefore increase the risk in situations in which the availability of these abilities is particularly important (for example, when driving or using other mechanisms).
OVERDOSE
The most important symptoms of an overdose are symptoms from the side of the central nervous system: dizziness, confusion, inhibition, disorientation, drowsiness, and also reactions from the gastrointestinal tract: vomiting.
In case of an overdose, it is recommended to perform gastric lavage (refers to tablets) and symptomatic therapy. There is no specific antidote.
DRUG INTERACTION
Antacids containing aluminum hydroxide (including sucralfate) and magnesium, aluminum phosphate, zinc, iron reduce the absorption of ofloxacin. When taking antacids and ofloxacin between their intake should be observed approximately two-hour interval.
With the simultaneous use of vitamin K antagonists, control over the blood coagulation system is necessary.
Ofloxacin may slightly increase the serum concentrations of glibenclamide when used concomitantly.
In the case of using high doses of ofloxacin and other drugs released by renal tubular secretion, such as probenicide, cimetidine, furosemide or methotrexate, it is possible to increase the concentration of ofloxacin in the serum.
In clinical studies no pharmacokinetic interaction of ofloxacin with theophylline has been revealed. However, a noticeable lowering of the threshold of convulsive activity could be observed with the appointment of quinolones in combination with theophylline, fenbufen or other nonsteroidal anti-inflammatory drugs, as well as other drugs that lower the threshold of convulsive activity.
When administered together with non-steroidal anti-inflammatory drugs, nitroimidazole derivatives and methylxanthines, the risk of neurotoxic effects increases.
At simultaneous appointment with glucocorticosteroids, the risk of rupture of tendons increases, especially in the elderly.
When co-prescribing with QT prolonging drugs (IA and III classes of antiarrhythmic drugs, tricyclic antidepressants, macrolides), the risk of prolonging the QT interval increases.
When administered with drugs that alkalinize urine (inhibitors of carbonic anhydrase, citrates, sodium bicarbonate), the risk of crystalluria and nephrotoxic effects increases.
TERMS OF RELEASE FROM PHARMACY
The drug is released by prescription.
