LEVOLET P (Pills, Film-coated)

Active material: Levofloxacin
When ATH: J01MA12
CCF: Fluoroquinolone antibacterial drug
When CSF: 06.17.02.01
Manufacturer: DR. REDDY`S LABORATORIES LTD. (India)

DOSAGE FORM, COMPOSITION AND PACKAGING

Pills, Film-coated white or nearly white, kapsulovidnoy form, lenticular, Embossed “RDY” on one side and “279” – another.

[Ring] microcrystalline cellulose (Avicel PH 101 и Avicel PH 102), corn starch, colloidal silicon dioxide, krospovydon, gipromelloza (15 cps), magnesium stearate.

The composition of the shell: colorant Opadry White OY 58900 (gipromelloza 5 cP, Titanium dioxide, macrogol 400).

10 PC. – blisters (1) – packs cardboard.

Pills, Film-coated white or nearly white, kapsulovidnoy form, lenticular, Embossed “RDY” on one side and “280” – another.

[Ring] microcrystalline cellulose (Avicel PH 101 и Avicel PH 102), corn starch, colloidal silicon dioxide, krospovydon, gipromelloza (15 cps), magnesium stearate.

The composition of the shell: colorant Opadry White OY 58900 (gipromelloza 5 cP, Titanium dioxide, macrogol 400).

10 PC. – blisters (1) – packs cardboard.

DESCRIPTION OF ACTIVE SUBSTANCES

Pharmacological action

Ftorxinolon, antimicrobial is a broad spectrum bactericidal action. Blocks of DNA gyrase (topoisomerase II) and topoisomerase IV, crosslinking violates supercoiling and DNA breaks, It inhibits DNA synthesis, It causes profound morphological alterations in the cytoplasm, cell wall and membranes. Effective against Enterococcus faecalis, Staphylococcus aureus, Staphylococcus epidermidis, Streptococcus pneumoniae, Streptococcus pyogenes и 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 is wonderful, Pseudomonas aeruginosa, Pseudomonas fluorescens, Chlamydia pneumoniae, Mycoplasma pneumoniae, Acinetobacter anitratus, Acinetobacter baumannii, Acinetobacter calcoaceticus, Bordetella pertussis, Citrobacter different, Citrobacter freundii, Morganella morganii, Proteus vulgaris, Rettgeri Providence, Providcncia stuartii, Serratia wilting, Clostridium perfringens.

Pharmacokinetics

If ingestion is absorbed from the gastrointestinal tract rapidly and almost completely. Food intake has little effect on the rate and completeness of absorption. Bioavailability is 99%. C_max achieved through 1-2 hours and at the reception 250 mg 500 mg of 2.8 and 5.2 ug / ml, respectively. Plasma protein binding – 30-40%. Well into the organs and tissues: lungs, bronchial mucosa, sputum, organs of the urogenital system, polymorphonuclear leukocytes, alyveolyarnыe macrophages. In the liver, a small portion is oxidized and / or deacetylated. Renal clearance is 70% total clearance.

T_1/2 – 6-8 no. Excreted from the body mainly by the kidneys by glomerular filtration and tubular secretion. Less 5% Levofloxacin is excreted as metabolites. Unchanged in the urine within 24 h output 70% and for 48 no – 87%; in coil 72 h detected 4% an oral dose. After the on / in Infusion 500 mg for 60 мин C_max – 6.2 ug / ml. The on / in single and repeated administration of the apparent V_d after administration of the same dose of 89-112 l, C_max – 6.2 ug / ml, T_1/2 – 6.4 no.

Testimony

Infections of the lower respiratory tract (chronic bronchitis, pneumonia), ENT (sinusitis, otitis media), urinary tract and kidney (incl. acute pyelonephritis), genital (incl. urogenital chlamydiosis), skin and soft tissue (festering atheroma, abscess, boils).

Dosage regimen

Inside, before a meal or in between meals, without chewing, drinking plenty of fluids. B /, slowly. In sinus – inside, by 500 mg 1 time / day; an exacerbation of chronic bronchitis – by 250-500 mg 1 time / day. When pneumonia – inside, by 250-500 mg 1-2 times / day (500-1000 mg / day); I / – by 500 mg 1-2 times / day. With infections of the urinary tract – inside, 250 mg 1 times / day, or in / at the same dose. With infections of the skin and soft tissues – by 250-500 mg orally 1-2 times / day, or on / in, by 500 mg 2 times / day. After the on / in a few days, a transition to the ingestion of the same dose.

When kidney disease dose reduced according to the degree of dysfunction: with CC = 20-50 ml / min – by 125-250 mg 1-2 times / day, with CC = 10-19 ml / min – 125 mg 1 once every 12-48 no, at CC<10 ml / min – 125 mg after 24 or 48 no. Length of treatment – 7-10 (to 14) days.

Side effect

From the digestive system: nausea, vomiting, diarrhea, anorexia, abdominal pain, pseudomembranous enterocolitis, activity increase “Hepatic” transaminases, giperʙiliruʙinemija, hepatitis, dysbiosis.

Cardio-vascular system: decrease in blood pressure, vascular collapse, tachycardia.

Metabolism: gipoglikemiâ (increased appetite, Sweating, tremor).

From the central and peripheral nervous system: headache, dizziness, weakness, drowsiness, insomnia, paresthesia, anxiety, fear, hallucinations, confusion, depression, movement disorders, convulsions.

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

On the part of the musculoskeletal system: arthralgia, myalgia, tendon rupture, muscular weakness, Tendinitis.

From the urinary system: giperkreatininemiя, interstitsialnyi Jade.

From the hematopoietic system: eozinofilija, gemoliticheskaya anemia, leukopenia, neutropenia, agranulocytosis, thrombocytopenia, pancytopenia, gemorragii.

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

Allergic reactions: hives, bronchospasm, suffocation, anaphylactic shock, hypersensitivity pneumonitis, vasculitis.

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

Contraindications

Hypersensitivity, epilepsy, defeat tendons at the earlier treatment quinolones, pregnancy, lactation, childhood and adolescence up 18 years.

Pregnancy and lactation

Levofloxacin is contraindicated during pregnancy and lactation (breast-feeding).

Cautions

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

After normalization of temperature, it is recommended to continue treatment for at least 48-78 no. Duration / in infusion 500 mg (100 ml solution infuzioinogo) must be at least 60 m. During treatment should avoid sunlight and artificial UV radiation to prevent damage to the skin (photosensitivity). If signs of tendinitis levofloxacin immediately cancel. It will be appreciated, In patients with brain damage history (stroke, severe injury) may develop seizures, at insufficiency glyukozo 6-fosfatdegidpogenazy – the risk of hemolysis.

Effects on ability to drive vehicles and management mechanisms

In the period of treatment should refrain from activities potentially hazardous activities, require high concentration and speed of psychomotor reactions.

Drug Interactions

Levofloxacin increases T_1/2 cyclosporine.

Effect of levofloxacin reduces preparations, suppress intestinal motility, sucralfate, magnesium- and aluminum-containing antacid and an iron salt (needed a break between the reception of at least 2 no).

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

Cimetidine and drugs, block tubular secretion, slow removal of levofloxacin.

Levofloxacin solution for i / v administration is compatible with 0.9% sodium chloride solution, 5% dextrose, 2.5% Ringer's 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.