Levofloxacin 5mg/ml 100ml solution

Action: 

antibacterial

Composition:

Levofloxacin 500mg

Vspomogatelny substances: sodium chloride, water d/in

Clinico-pharmacological group

06.051 (Antituberculosis drug)

06.038 (Antibacterial drug group of fluoroquinolones)

26.023 (Antibacterial drug group of fluoroquinolones for local use in ophthalmology)

Pharmacological action:

Fluoroquinolone, antimicrobial germicide of wide spectrum of action. Does DNK-girazu (topoisomerase II) and topoisomerase IV, violates supercoiling and cross-linking of DNA breaks, inhibits DNA synthesis, causes profound morphological changes in cytoplasm, cell wall and membranes. Effective against Enterococcus faecalis, Staphylococcus aureus, Staphylococcus epidermidis, Streptococcus pneumoniae, Streptococcus pyogenes and Streptococcus agalactiae, Viridans group streptococci, Enterobacter cloacae, Enterobacter aerogenes, Enterobacter agglomerans, Enterobacter sakazakii, Escherichia coli, Haemophilus influеnzае, Haemophilus parainfluenzae, Klebsiella pneumoniae, Klebsiella oxytoca, Legionella pneumoniae, Moraxella catarrhalis, Proteus mirabilis, Pseudomonas aeruginosa, Pseudomonas fluorescens, Chlamydia pneumoniae, Mycoplasma pneumoniae, Acinetobacter anitratus, Acinetobacter baumannii, Acinetobacter calcoaceticus, Bordetella pertussis, Citrobacter diversus, Citrobacter freundii, Morganella morganii, Proteus vulgaris, Providencia rettgeri, Providcncia stuartii, Serratia marcescens, Clostridium perfringens.

Pharmacokinetics

If ingestion is absorbed from the gastrointestinal tract rapidly and almost completely. Food intake has little effect on the speed and completeness of absorption. The bioavailability is 99%. Cmax is reached after 1-2 hours and when taking 250 mg and 500 mg is 2.8 and 5.2 µ g/ml, respectively. The plasma protein binding is 30-40%. Well into the organs and tissues: lungs, mucous membranes, bronchi, sputum, urogenital organs, polymorphonuclear leukocytes, alveolar macrophages. In the liver, a small part is oxidized and/or deacetylated. Renal clearance is 70% of total clearance.

T1/2 6-8 hours Excreted mainly kidneys by clubockova filtering and kanalzeva secreta. Less than 5% of levofloxacin is excreted as metabolites. In an unmodified form with the urine within 24 h displayed a 70% and 48 hours – 87% in feces over 72 h found 4% of an oral dose. After the on/in infusions 500 mg for 60 min Cmax = 6.2 µg/ml. at/in single and repeated administration of apparent Vd after administration of the same dose 89-112 l, Cmax = 6.2 µg/ml, T1/2 – 6.4 h.

Dosage

Inside, before meals or in between meals, not liquid, squeezed enough liquid. In/in slowly. In sinus – inside, 500 mg 1 time/day, exacerbation of chronic bronchitis – on 250-500 mg 1 times/day. When pneumonia – inside, 250-500 mg 1-2 times/day (500-1000 mg/day)/500 mg 1-2 times/day. When infections urinary tract – inside, 250 mg 1 time/day or in/at the same dose. When infections of skin and soft tissues – 250-500 mg orally 1-2 times/day or in/in, 500 mg 2 times/day. After the on/in the introduction in a few days, a transition to the ingestion of the same dose.

In diseases of the kidney dose reduced in accordance with the degree of impairment of the function: if QC=20-50 ml/min – on 125-250 mg 1-2 times/day, with KK=10-19 ml/min – 125 mg 1 time per 12-48 h, with KK<, , 10 -=”” 125=”” 24=”” 48=”” 7-10=”” 14=”” p=””>,

Drug interactions

Levofloxacin increases T1/2 cyclosporine.

Effect of levofloxacin reduces the drugs that suppress intestinal motility, sukralfat, magni – and aluminisodergaszczye antatsidnye tools and iron salts (needed to break between the reception of at least 2 hours).

With simultaneous use of NSAIDs, theophylline increases convulsive, GCS increase the risk of tendon rupture.

Cimetidine and drugs that block tubular secretion, slow down the excretion of levofloxacin.

Levofloxacin solution for I/V injection is compatible with 0.9% solution of sodium chloride, 5% dextrose, 2.5% ringer solution with dextrose, combined solutions for parenteral nutrition (amino acids, carbohydrates, electrolytes).

Levofloxacin solution for I/V administration should not be mixed with heparin and solutions having an alkaline reaction.

Pregnancy and lactation:

Levofloxacin is contraindicated during pregnancy and lactation (breastfeeding).

Side effects:

From the digestive system: nausea, vomiting, diarrhea, anorexia, abdominal pain, pseudomembranous enterocolitis, increased activity “liver” transaminases, hyperbilirubinemia, hepatitis, goiter.

From the side of cardiovascular system: decrease in blood pressure, vascular collapse, tachycardia.

From the metabolic: hypoglycemia (increased appetite, sweating, tremor).

CNS and peripheral nervous system: headache, dizziness, weakness, drowsiness, insomnia, paresthesia, anxiety, fear, hallucinations, confusion, depression, movement disorders, seizures.

From the sensory organs: visual impairment, hearing, olfactory, gustatory and tactile sensitivity.

From the side of musculoskeletal system: arthralgia, myalgia, tendon rupture, muscular weakness, tendonitis.

From the urinary system: gipercreatininemia, intersticialny jade.

With the hematopoietic system: eosinophilia, hemolytic anemia, leukopenia, neutropenia, agranulocytosis, thrombocytopenia, pancytopenia, hemorrhage.

Dermatological reactions: photosensitivity, itching, swelling of the skin and mucous membranes, malignant exudative erythema (Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell’s syndrome).

Allergic reactions: urticaria, bronchospasm, dyspnea, anaphylactic shock, allergic pneumonitis, vasculitis.

Other: aggravation of porphyria, rhabdomyolysis, persistent fever, development of superinfection.

Indications:

Infections of the lower respiratory tract (chronic bronchitis, pneumonia), ENT-organs (sinusitis, otitis media), urinary tract and kidney (including acute pyelonephritis), genitals (including urogenital chlamydia), skin and soft tissues (festering atheroma, abscess, boils).

Contraindications:

Hypersensitivity, epilepsy, lesions of the tendons at the earlier treatment quinolones, pregnancy, lactation, childhood and adolescence to 18 years.

Special instructions:

With careful use of levofloxacin in elderly patients (high probability of having a concomitant loss of kidney function).

After normalization of temperature it is recommended to continue the treatment for at least 48-78 hours long in/in infusion 500 mg (100 ml infusional solution) must be at least 60 min. During treatment should avoid sunlight and artificial UV radiation to avoid damage to the skin (photosensitization). When signs of tendinitis levofloxacin immediately cancelled. It should be borne in mind that patients with brain damage in medical history (stroke, severe injury) may develop convulsions, in case of insufficiency of glucose-6-phosphate dehydrogenase – the risk of hemolysis.

Effects on ability to drive vehicles and management mechanisms

During treatment should refrain from activities potentially hazardous activities, require high concentration and psychomotor speed reactions.