INSTRUCTIONS FOR USE
NIRLIV
Trade name: NIRLIV
International nonproprietary name: Levofloxacin
Dosage form: Solution for infusion
Ingredients:
Levofloxacin hemihydrate
equivalent to levofloxacin…………………………….500 mg
Water for injection US F.…………………………………QS
Description: Transparent greenish-yellow solution
Pharmacological properties
Pharmacodynamics
Levofloxacin is a synthetic broad-spectrum antibacterial drug from the group of fluoroquinolones, containing levofloxacin, a levorotatory isomer of ofloxacin, as an active substance.
Levofloxacin blocks DNA gyrase (topoisomerase II) and topoisomerase IV, disrupts supercoiling and cross-linking of DNA breaks, inhibits DNA synthesis, and causes profound morphological changes in the cytoplasm, cell wall and membranes of bacteria.
Levofloxacin is active against most strains of microorganisms in vitro and in vivo.
Sensitive microorganisms (MIC ≤2 mg/ml):
Aerobic gram-positive microorganisms: Corynebacterium diphtheriae, Enterococcus faecalis, Enterococcus spp, Listeria monocytogenes, Staphylococcus coagulase-negative methicillin-sensitive/-moderately sensitive, Staphylococcus aureus methicillin-sensitive, Staphylococcus epidermidis methicillin-sensitive, Staphylococcus spp (CNS), ococci group C and G, Streptococcus agalactiae, Streptococcus pneumoniae penicillin-sensitive/-moderately sensitive/-resistant, Streptococcus pyogenes, Viridans streptococci penicillin-sensitive/-resistant.
Aerobic gram-negative microorganisms: Acinetobacter baumannii, Acinetobacter spp, Citrobacter freundii, Eikenella corrodens, Enterobacter aerogenes, Enterobacter agglomerans, Enterobacter cloacae, Enterobacter spp, Escherichia coli, Gardnerella vaginalis, Haemophilus ducreyi, Haemophilus influenzae ampicillin-sensitive/-resistant Haemophilus, parainfluenzae, Helicobacter pylori, Klebsiella oxytoca, Klebsiella pneumoniae, Klebsiella spp, Moraxela catarrhalis β+/β-, Morganella morganii, Neisseria gonorrhoeae (including those producing penicillinase), Neisseria meningitidis, Pasteurella conis, Pasteurella dagmatis, Pasteurella multocida, Pasteurella spp, Proteus mirabilis, Proteus vulgaris, Providencia rettgeri, Providencia stuartii, Providencia spp, Pseudomonas aeruginosa, Pseudomonas spp, Salmonella spp, Serratia marcescens, Serratia spp.
Anaerobic microorganisms: Bacteroides fragilis, Bifidobacterium spp, Clostridium perfringens, Fusobacterium spp, Peptostreptococcus, Propionibacterium spp, Veilonella spp.
Other microorganisms: Bartonella spp, Chlamydia pneumoniae, Chlamydia psittaci, Chlamydia trachomatis, Legionella pneumophila, Legionella spp, Mycobacterium spp, Mycobacterium leprae, Micobacterium tuberculosis, Mycoplasma hominis, Mycoplasma pneumoniae, Ricketsia spp, Ureaplasma urealyticum.
Moderately sensitive (MIC ≥4 mg/l):
Aerobic gram-positive microorganisms: Corynebacterium urealiticum, Corynebacterium xerosis, Enterococcus faecium, Staphylococcus epidermidis methicillin-resistant, Staphylococcus haemolyticus methicillin-resistant.
Aerobic gram-negative microorganisms: Burkholderia cepacia, Campilobacter jejuni/coli.
Anaerobic microorganisms: Bacteroides thetaiotaomicron, Bacteroides vulgatus, Bacteroides ovaius, Prevotella spp, Porphyromonas spp.
Resistant (MIC ≥8 mg/l):
Aerobic gram-positive microorganisms: Corynebacterium jeikeium, Staphylococcus aureus methicillin-resistant, Staphylococcus coagulase-negative methicillin-resistant.
Aerobic gram-negative microorganisms: Alcaligenes xylosoxidans.
Other microorganisms: Mycobacterium avium.
Pharmacokinetics .
Absorption
When administered orally and intravenously, maximum plasma concentrations are achieved within an hour. Bioavailability is 100%.
Distribution
30-40% of levofloxacin binds to blood proteins.
When levofloxacin is administered at a dose of 500 mg twice a day, a slight accumulation of the drug is observed.
The maximum concentration of levofloxacin after administration of 500 mg is achieved:
Metabolism
The drug is metabolized to form desmethyllevofloxacin and levofloxacin-N-oxide.
Of these, 5% is excreted in the urine.
Elimination
Levofloxacin is eliminated from the blood relatively slowly (t= 6-8 hours)
85% of the administered dose of the drug is excreted in the urine.
When the drug is administered orally or intravenously, there is no significant difference in its removal from the body.
Indications for use
Infectious and inflammatory diseases caused by microorganisms sensitive to Nirliv:
Contraindications
The drug should be used with caution in the elderly due to the high likelihood of a concomitant decrease in renal function, with deficiency of glucose-6-phosphate dehydrogenase.
Directions for use and doses
Nirliva infusion solution is administered once or twice a day. Doses and duration of treatment are determined by the nature and severity of the infection, as well as the sensitivity of the suspected pathogen. The next administration of the drug should be done after 48-72 hours.
Dosage and duration of treatment:
If bacteremia is suspected – 500 mg 1 time per day – orally or intravenously for 7-14 days
Acute sinusitis: 500 mg orally for 10-14 days.
Exacerbation of chronic bronchitis: 500 mg orally for 7 days.
Chronic prostatitis: 500 mg orally for 28 days.
Mixed urinary tract infection: 250 mg orally for 3 days.
Bacterial infections of skin and soft tissues: 750 mg – 10-14 days.
Nirliv is excreted primarily through the kidneys, therefore, when treating patients with impaired renal function, it is necessary to reduce the dose of the drug: Creatinine clearance 50-80 ml/min 20-49 ml/min 10-19 ml/min
— 500 mg 250 mg 500 mg 250 mg
every 24 hours every 24 hours
Calculation of clearance: weight (kg) x (140-age)
In men = 72x serum creatinine (mg/ml)
For women = 0.85x the digital value of men
If liver function is impaired, no change in dosage regimen is required, since Nirliv is metabolized in the liver to a small extent.
Nirliva infusion solution is administered intravenously slowly. The duration of infusion of 100 ml of Nirliva solution (1 bottle) should be at least 60 minutes. (See “Special Instructions”). Depending on the patient’s condition, after a few days of treatment, you can switch from intravenous drip administration to taking the same dose of the drug in a form intended for oral administration.
Nirliv solution for infusion is compatible with the following infusion solutions: 0.9% sodium chloride solution, 5% dextrose solution, 2.5% Ringer’s solution with dextrose, combined solutions for parenteral nutrition (amino acids, carbohydrates, electrolytes).
Nirliv solution 500 mg/100 ml cannot be mixed with heparin or solutions with an alkaline reaction (for example, sodium bicarbonate solution).
The duration of treatment should be no more than 14 days. As with the use of other antibiotics, it is recommended to continue treatment with the drug for at least 48–78 hours after the body temperature has normalized or after the pathogen has been effectively destroyed.
Side effects
Frequency of occurrence of side effects
often: in 1–10 patients out of 100
sometimes: less than 1 patient out of 100
rare: less than 1 patient in 1,000
very rare: less than 1 patient in 10,000
in some cases: less than 1 patient out of more than 10,000
Skin reactions and general hypersensitivity reactions
Sometimes: itching and redness of the skin.
Rare: general hypersensitivity reactions (anaphylactic and anaphylactoid reactions) with symptoms such as urticaria, bronchospasm and laryngospasm.
In very rare cases: swelling of the skin and mucous membranes (for example, in the face and throat), sudden drop in blood pressure and shock; increased sensitivity to solar and ultraviolet radiation (see “Special instructions”); allergic pneumonitis; vasculitis
In some cases: severe skin rashes with blistering, such as Stevens-Johnson syndrome, toxic epidermal necrolysis (Lyell’s syndrome) and exudative erythema multiforme. General hypersensitivity reactions may sometimes be preceded by milder skin reactions. The above reactions can develop after the first dose, a few minutes or hours after administration of the drug.
Effect on the gastrointestinal tract and metabolism
Common: nausea, diarrhea.
Sometimes: loss of appetite, vomiting, abdominal pain, digestive disorders.
Rarely: diarrhea (including blood), which in very rare cases can be a sign of intestinal inflammation and even pseudomembranous colitis (see section “Special instructions”).
Very rare: a drop in blood glucose levels (hypoglycemia), which is of particular importance for patients with diabetes, with symptoms: increased appetite, nervousness, perspiration, trembling.
Experience with other quinolones suggests that they can cause exacerbation of porphyria (a very rare metabolic disease) in patients already suffering from this disease. A similar effect cannot be excluded when using the drug Nirliv.
Effect on the nervous system
Sometimes: headache, dizziness and/or stupor, drowsiness, sleep disturbances.
Rare: depression, anxiety, psychotic reactions (eg with hallucinations), discomfort (eg paresthesia in the hands), trembling, restlessness, convulsions and confusion.
Very rare: visual and hearing impairment, impaired taste and smell, decreased tactile sensitivity.
Effect on the cardiovascular system
Rarely: increased heart rate, decreased blood pressure.
Very rare: (shock-like) vascular collapse.
In some cases: prolongation of the QT interval.
Effect on muscles, tendons and bones
Rarely: tendon lesions (including tendinitis), joint and muscle pain.
Very rare: tendon rupture (for example, Achilles tendon) may develop on both sides within 48 hours after the start of treatment (see also section “Special instructions”); muscle weakness, which is of particular importance for patients suffering from asthenic bulbar palsy.
In some cases: muscle damage (rhabdomyolysis).
Effect on the liver and kidneys
Common: increased activity of liver enzymes (eg, alanine aminotransferase and aspartate aminotransferase).
Rarely: increased levels of bilirubin and creatinine in the blood serum (a sign of decreased liver or kidney function).
Very rare: hepatic reactions (eg hepatitis); deterioration of kidney function up to acute renal failure, for example, due to allergic reactions (interstitial nephritis).
Effect on blood
Sometimes: an increase in the number of eosinophils, a decrease in the number of leukocytes.
Rarely: neutropenia; thrombocytopenia, which may be accompanied by increased bleeding.
Very rare: agranulocytosis and the development of severe infections (persistent or recurrent fever, sore throat and persistent deterioration in health).
In some cases: hemolytic anemia; pancytopenia.
Other side effects
Common: pain, redness at the injection site and phlebitis.
Sometimes: general weakness (asthenia).
Very rare: fever.
Any antibiotic therapy can cause changes in the microflora (bacteria and fungi) that is normally present in humans. For this reason, a secondary infection or superinfection may develop, which may require additional treatment.
Overdose
Symptoms: manifest mainly from the central nervous system (confusion, dizziness, disturbances of consciousness and seizures similar to epileptic seizures). In addition, gastrointestinal disorders (for example, nausea) and erosive lesions of the mucous membranes of the gastrointestinal tract and prolongation of the QT interval may occur.
Treatment: symptomatic. Levofloxacin is not eliminated by dialysis (hemodialysis, peritoneal dialysis and continuous peritoneal dialysis). There is no specific antidote.
special instructions
Nirliv should not be used to treat children and adolescents due to the risk of damage to articular cartilage.
When treating elderly patients, it should be taken into account that they often have impaired renal function (see section “Method of administration and dosage”).
In severe pneumonia, Nirliv may not provide an optimal therapeutic effect. Hospital-acquired infections caused by certain pathogens (P. aeruginosa) may require combination treatment.
The recommended duration of administration should be strictly adhered to, which should be at least 60 minutes (100 ml of infusion solution). Experience with levofloxacin shows that increased heart rate and a transient drop in blood pressure may occur during infusion. In rare cases, a pronounced drop in blood pressure can cause vascular collapse. If a significant drop in blood pressure is observed during the infusion of levofloxacin (the L-isomer of ofloxacin), the infusion is stopped immediately.
During treatment with Nirliv, it is possible to develop an attack of seizures in patients with previous brain damage caused, for example, by a stroke or severe injury. Convulsive activity may also increase with the simultaneous use of fenbufen, similar non-steroidal anti-inflammatory drugs or theophylline (see “Interactions”).
Despite the fact that photosensitivity is observed very rarely with the use of levofloxacin, in order to avoid it, patients are not recommended to be exposed to sunlight and artificial ultraviolet irradiation.
If pseudomembranous colitis is suspected, Nirliv should be discontinued immediately and appropriate treatment should be initiated. In such cases, drugs that inhibit intestinal motility should not be used.
Rarely observed with the use of the drug, tendonitis (primarily inflammation of the Achilles tendon) can lead to tendon rupture. Elderly patients are more prone to tendinitis. Treatment with corticosteroids increases the risk of tendon rupture. If tendonitis is suspected, treatment with Nirliv should be stopped immediately and appropriate treatment of the affected tendon should be initiated, for example by resting it (see “Contraindications” and “Side Effects”).
Patients with glucose-6-phosphate dehydrogenase deficiency may respond to fluoroquinolones by destroying red blood cells (hemolysis). In this regard, treatment of such patients with Nirliv should be carried out with great caution.
Side effects of Nirliv, such as dizziness or stupor, drowsiness and visual disturbances (see “Side Effects”), may impair the ability to react quickly and concentrate, which poses a certain risk in situations where these abilities are of particular importance ( for example, when driving a car, when servicing machines and mechanisms, when performing work in an unstable position).
Best before date
2 years.
Storage conditions : In a dry place, protected from light at a temperature not exceeding 30 0 C. Do not freeze
Release form
100 ml, in glass bottles.
Conditions for dispensing from pharmacies
Dispensed with a doctor’s prescription
Manufacturer: Aculife , India
