Composition, form of production and packaging
The solution for infusions is transparent, greenish-yellow in color.
1 ml
ofloxacin hydrochloride 2.2 mg,
which corresponds to the content of ofloxacin 2 mg
[PRING] sodium chloride, hydrochloric acid 1n (to adjust the pH), water d / u.
100 ml - vials of colorless glass (1) - packs cardboard.
INSTRUCTION FOR THE SPECIALIST.
The product description was approved by the manufacturer for the 2009 print edition.
PHARMACHOLOGIC EFFECT
Ofloxacin belongs to the broad spectrum antimicrobial agents from the group of fluoroquinolones. The main mechanism of action is the inhibition of the enzyme DNA-gyrase of a bacterial cell, which leads to destabilization of DNA molecule chains and cell death.
The drug is usually sensitive : Aeromonas hydrophila; (Branhamella) catarrhalis; Brucella spp .; Chlamydia trachomatis; Citrobacter spp .; Clostridium perfringens;Enterobacter spp .; Escherichia coli; Haemophilus ducreyi; Haemophilus influenzae and parainfluenzae; Helicobacter coli; Helicobacter jejuni; Klebsiella oxytoca;Legionella spp .; Moraxella morganii; Mycoplasma hominis; Neisseria gonorrhoeae, Neisseria meningitidis; Plesiomonas; Proteus indole +; Proteus mirabilis, Proteus vulgaris; Salmonella spp .; Serratia spp .; Schigella spp .; Staphylococcus aureus methi-S; Staphylococuss coagulase negative; Yersinia enterolytica.
The drug is moderately sensitive: Acinetobacter spp., Anaerobic Gram positive cocci; Bacteroides fragilis; Chlamydia psittaci; Garnerella vaginalis; Mycobacterium tuberculosis, Mycobacterium leprae; Pseudomonas aeruginosa; Streptococcus pneumoniae; Streptococcus spp.
The drug is resistant to: Acinetobacter baumanii; Clostridium difficile; Enterococcus spp .; Listeria monocytogenes, Staphylococci methi-R; Nocardia.
PHARMACOKINETICS
The bioavailability of Tarivid is almost 100%. C max drug in the blood plasma after iv injection of 200 mg (0.5 h) is 5 mg / ml and is achieved after 0.5 h.
With the out-of-office assignment of ofloxacin, serum concentration does not change significantly (the multiplication factor is approximately 1.5). Plasma protein binding is 25%.
Metabolized in the liver about 5% of the drug with the formation of two major metabolites: N-oxide ofloxacin and dimethylofloxacin.
T 1/2 - 5 hours. Up to 90% of the drug is excreted by the kidneys unchanged.
In patients with renal insufficiency in proportion to the decrease in creatinine clearance, the half-life increases, the total and renal clearance decreases.
INDICATIONS
Tarium is intended for treatment of bacterial infections 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 (gonococcal nature);
- infections in gynecology;
- infections of bones and joints;
- skin and soft tissue infections;
- septicemia (injection form only);
- prevention of infections in patients with a decreased immune status (eg, neutropenia).
* Since some strains of microorganisms are moderately sensitive to ofloxacin, the drug should not be prescribed as the first choice for the treatment of pneumonia caused by pneumococci, as well as acute tonsillitis (? -gemolytic streptococcus).
DOSING MODE
Applied to / in. The dose, purpose and duration of therapy depend on the severity of the infectious disease, the sensitivity of the pathogens, the patient's condition and kidney function.
Dosage in adults with normal renal function
The usual dose for patients with infections caused by microorganisms sensitive to the preparation is 200 mg (w / w) 2 times / day with an interval of 12 hours (daily dose - 400 mg). At a daily dose exceeding 400 mg, it should be divided into two equal parts and taken 2 times / day at the same time intervals. Doses not exceeding 400 mg may be given 1 time / day, preferably in the mornings.
The daily dose can be increased to 600 mg in case of treatment of severe infections or in patients with excessive body weight.
Dosage in adults with impaired renal function
Ofloxacin is excreted mainly by the kidneys. The dose should be reduced in patients with impaired renal function.
Creatinine clearance (CC) Single dose Number of doses / 24 h Interval between administration
50-20 ml / min 200 1 24 h
<20 ml / min ** or hemodialysis or peritoneal dialysis 100 or 200 1 1 24 h 48 h
In cases where it is not possible to determine QC, it can be calculated from the serum creatinine level using the Cockcroft formula for adults:
For men:
CK (ml / min) = body weight (kg)? (140 age) / 72? Creatinine (mg%) or
CK (ml / min) = body weight (kg)? (140 age) /0.814? Creatinine (mmol / l)
For women:
CK (ml / min) = 0.85 - an indicator for men
Dosage in patients with hepatic impairment
It is recommended not to exceed the maximum daily dose of ofloxacin - 400 mg.
Dosage in elderly patients
The age of the patient does not require a special dose adjustment of ofloxacin.
The solution of ofloxacin is intended only for slow IV injection; the drug is administered 1 or 2 times a day. Time infusion should be at least 30 minutes for every 200 mg ofloxacin. This should be especially taken into account when using ofloxacin together with antihypertensive agents and anesthetic agents from the barbiturate group. The started treatment of ofloxacin in the form of intravenous infusions in a few days can be continued in the form of oral administration in the same dosage, if the patient's condition allows.
The duration of treatment depends on the severity of the disease. As with antibiotic therapy, the use of ofloxacin should continue for at least 48-72 hours after the normalization of body temperature or if there is evidence of eradication of the bacterial agent.
It is recommended to monitor the concentrations of ofloxacin in the serum in patients with severe renal failure and in patients on hemodialysis.
SIDE EFFECT
The information below is based on clinical research data and on a wide post-marketing experience of the drug.
The following rating of incidence of side effects was used: very widespread: 10%, widespread: 1% -10%, infrequent: 0.1% - 1%, rare: 0.01% -0.1%, very rare: less than 0.01% .
Anaphylactic / anaphylactoid reactions, reactions from the skin and mucous membranes: infrequent - itching, rashes, burning in the eyes, dry cough, rhinitis; rare - hives, angioedema, asthma / bronchoslasm; hyperemia, sweating, pustular rash; very rare - anaphylactic / anaphylactoid shock, erythema multiforme, toxic epidermal necrolysis, photosensitivity, persistent drug rash, vascular purpura, vasculitis, which in exceptional cases can lead to skin necrosis; isolated cases - Stevens-Johnson syndrome, severe suffocation.
From the gastrointestinal tract: infrequent - abdominal pain, diarrhea, nausea, vomiting, decreased appetite; rare - anorexia, flatulence, enterocolitis, which can in some cases be hemorrhagic; very rare - pseudomembranous colitis.
From the side of the central nervous system: infrequent - excitement, dizziness, headache, sleep disturbance / insomnia; rare - psychotic reactions (eg, hallucinations), anxiety, confusion, nightmarish dreams, depression, drowsiness, peripheral sensitivity disorders such as paresthesia, taste and smell disturbances, visual impairment;very rare - hearing impairments, such as tinnitus or hearing loss, epileptic seizures, extrapyramidal disorders or other disorders of muscle coordination, hypoesthesia, tremor, convulsions; isolated cases - psychotic reactions accompanied by a behavior dangerous to the patient, including suicidal tendencies, increased intracranial pressure.
From the cardiovascular system: rare - hypotension, tachycardia. During intravenous drip ofloxacin, tachycardia and a decrease in blood pressure can occur. Thus, a reduction in blood pressure in very rare cases can be pronounced. In the case of a marked reduction in blood pressure, an IV injection should be stopped immediately.
From the musculoskeletal system: rare - tendonitis; very rare - arthralgia, myalgia, 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 cases - rhabdomyolysis (acute necrosis of skeletal muscles) and / or myopathy, muscle weakness, which can be especially important in patients with severe pseudo-paralytic myasthenia gravis.
On the part of the liver: rare - increased hepatic enzymes (ACT, ALT, LDH, GGT and / or AP) and / or bilirubin; very rare - cholestatic jaundice; isolated cases - hepatitis, which can be severe.
From the kidneys: rare - increased serum creatinine levels, increased urea concentration; very rare - acute renal failure; isolated cases - interstitial nephritis.
From the peripheral blood: very rare - anemia, hemolytic anemia, leukopenia, eosinophilia, thrombocytopenia; agranulocytosis, individual cases - pancytopenia, oppression of bone marrow hematopoiesis.
Other: common - pain and redness at the site of intravenous administration and phlebitis; infrequently occurring - the development of secondary infection caused by drug-resistant microorganisms and fungi; isolated cases - allergic pulmonitis, acute attacks of porphyria in patients with porphyria, hypoglycemia in patients with diabetes treated with hypoglycemic drugs.
CONTRAINDICATIONS
- violations in the tendons, as a result of the intake of fluoroquinolones;
- epilepsy;
- children and adolescents under the age of 18 (due to incomplete growth of the skeleton);
- Pregnancy;
- the period of breastfeeding;
- hypersensitivity to ofloxacin, other quinolones or components of the drug.
With caution should be taken in patients with a decrease in the convulsive threshold (after traumatic brain injury, stroke or inflammation in the central nervous system).
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
It is recommended not to exceed the maximum daily dose of ofloxacin - 400 mg.
APPLICATION FOR CHILDREN
Contraindications: children and adolescents under the age of 18 (due to the incomplete growth of the skeleton).
APPLICATION IN ELDERLY PATIENTS
In elderly patients, no special dose adjustment of ofloxacin is required.
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 it is suspected that pseudomembranous colitis develops, ofloxacin should be stopped immediately, and appropriate specific antibiotic therapy (for example, vancomycin inwards, teicoplanin 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.
Driving or other 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 overdose are symptoms from the side of the central nervous system: dizziness, confusion, inhibition, as well as 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 can reduce the absorption of ofloxacin tablets. 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 drugs with co-administration of quinolones and other drugs released by renal tubular secretion, such as probenicide, cimetidine, furosemide or methotrexate, their serum concentrations may be increased due to mutual excision disorders.
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.
Ofloxacin moderately sensitive Mycobacterium tuberculosis, which can lead to false-negative results in the bacteriological diagnosis of tuberculosis.
During the treatment with ofloxacin, false-positive results may appear in the determination of opiates and porphyrins in the urine.
When administered together with non-steroidal anti-inflammatory drugs, nitroimidazole derivatives 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.
Compatibility Guidelines
Heparin should not be mixed with ofloxacin because of the risk of precipitation. Possible use of the following infusion solutions: 0.9% sodium chloride solution, Ringer's solution, 5% glucose solution.
TERMS OF RELEASE FROM PHARMACY
The drug is released by prescription.
TERMS AND CONDITIONS OF STORAGE
Store in a dark place inaccessible to children at a temperature not exceeding 25 В° C. Do not freeze! Shelf life - 3 years.
