2010/06/23

Tavanic

Composition, structure and packing

Coated tablets pale yellowish-pink, oblong, biconvex, with a dividing groove.

1 tab.

levofloxacin gemigidrat 256.23 mg

which corresponds to the content of levofloxacin 250 mg.

Excipients: krospovidon, methylhydroxypropylcellulose, microcrystalline cellulose, sodium stearyl fumarate, macrogol 8000, talc, titanium dioxide (E171), iron oxide red (E172), iron oxide yellow (E172).

Coated tablets pale yellowish-pink, oblong, biconvex, with a dividing groove.

1 tab.

levofloxacin gemigidrat 512.46 mg

which corresponds to the content of levofloxacin 500 mg.

Excipients: krospovidon, methylhydroxypropylcellulose, microcrystalline cellulose, sodium stearyl fumarate, macrogol 8000, talc, titanium dioxide (E171), iron oxide red (E172), iron oxide yellow (E172).

Solution for infusion transparent, greenish-yellow.

1 ml of levofloxacin gemigidrat 5.12 mg.

which corresponds to the content of levofloxacin 5 mg.


1 vial. levofloxacin gemigidrat 512.46 mg

which corresponds to the content of levofloxacin 500 mg.

Excipients: sodium chloride, concentrated hydrochloric acid, sodium hydroxide, water d / and.

Clinico-pharmacological group: antibacterial fluoroquinolone group.

Pharmacological action

Antimicrobial group of fluoroquinolones, ofloxacin isomer levogyrate. It has a wide spectrum of antimicrobial action. Levofloxacin blocks DNA-gyrase (topoisomerase II) and topoisomerase IV, and crosslinking violates supercoiling of DNA, inhibits DNA synthesis, causes profound morphological changes in the cytoplasm, cell wall and membranes.

Levofloxacin is active against most strains of microorganisms in the conditions in vitro, and in vivo. In vitro sensitive (IPC ≤ 2mg/ml) aerobic Gram-positive microorganisms: Corynebacterium diphtheriae, Enterococcus spp. (Including Enterococcus faecalis), Listeria monocytogenes, Staphylococcus spp. (Coagulase metitsillin-chuvstvitelnye/metitsillin-umerenno sensitive strains), Staphylococcus aureus (methicillin-sensitive strains), Staphylococcus epidermidis (methicillin-chuvstvitelnye strains), Staphylococcus spp. (CNS), Streptococcus spp. Group C and G (including Streptococcus agalactiae, Streptococcus pneumoniae (penitsillin-chuvstvitelnye/umerenno sensitive / resistant strains), Streptococcus pyogenes, Streptococcus viridans (penitsillin-chuvstvitelnye/rezistentnye strains), aerobic gram-negative microorganisms: Acinetobacter baumannii, Acinetobacter spp ., Actinobacillus actinimycetemcomitans, Citrobacter freundii, Eikenella corrodens, Enterobacter aerogenes, Enterobacter agglomerans, Enterobacter spp. (including Enterobacter cloacae), Escherichia coli, Gardnerella vaginalis, Haemophilus ducreyi, Haemophilus influenzae (ampitsillin-chuvstvitelnye/rezistentnye strains), Haemophilus parainfluenzae, Helicobacter pylori, Klebsiella spp. (including Klebsiella oxytoca, Klebsiella pneumoniae), Moraxella cattaralis (producing strains and β-lactamase neprodutsiruyuschie), Morganella morganii, Neisseria gonnorrhoeae (producing strains and neprodutsiruyuschie penicillinase), Neisseria meningitidis, Pasteurella spp. (including Pasteurella conis, Pasteurella dagmatis, Pasteurella multocida), Proteus mirabilis, Proteus vulgaris, Providencia spp. (including Providencia rettgeri, Providencia stuartii), Pseudomonas spp. (in t. h. Pseudomonas aeruginosa), Salmonella spp., Serratia spp. (Serratia marcescens); anaerobic microorganisms: Bacteroides fragilis, Bifidobacterium spp., Clostridium perfringens, Fusobacterium spp., Peptostreptococcus spp., Propionibacterum spp., Veilonella spp.; other microorganisms: Bartonella spp., Chlamydia pneumoniae, Chlamydia psittaci, Chlamydia trachomatis, Legionella pneumophila, Legionella spp., Mycobacterium spp. (including Mycobacterium leprae, Mycobacterium tuberculosis), Mycoplasma hominis, Mycoplasma pneumoniae, Rickettsia spp., Ureaplasma urealyticum.

Levofloxacin is moderately active (IPC ≥ 4 mg / L) against aerobic gram-positive microorganisms: Corynebacterium urealiticum, Corynebacterium xerosis, Enterococcus faecium, Staphylococcus epidermidis (methicillin-resistant strains), Staphylococcus haemolyticus (methicillin-resistant strains), aerobic gram-negative organisms: Burkholderia cepacia , Campilobacter jejuni, Campilobacter coli; anaerobic microorganisms: Bacteroides thetaiotaomicron, Bacteroides vulgatus, Bacteroides ovaius, Prevotella spp., Porphyromonas spp. By levofoloksatsinu resistant (IPC ≥ 8 mg / l) aerobic Gram-positive microorganisms: Corynebacterium jeikeium, Staphylococcus aureus (methicillin-resistant strains), Staphylococcus spp. (Coagulase-negative methicillin-resistant strains), aerobic gram-negative bacteria: Alcaligenes xylosoxidans; other microorganisms: Mycobacterium avium.

Pharmacokinetics

Absorption

After oral levofloxacin rapidly and almost completely absorbed from the gastrointestinal tract. Eating little effect on the speed and completeness of absorption.

When a single dose of 500 mg C max in plasma is achieved through 1.3 h and is 5.2-6.9 mg / ml. Bioavailability - 100%.

After i / in the 60-minute infusion of levofloxacin 500 mg healthy volunteers the mean C max in plasma was 6.2 ± 1.0 pg / ml, Tmax - 1.0 ± 0.1 h. The pharmacokinetics of levofloxacin is linear and predictable after a single and multiple injections of the drug. Plasma concentration profile of levofloxacin following to / in the introduction is similar to that in the pill.

Therefore, oral and / in route of administration may be interchanged.

Distribution

Binding to plasma proteins - 30-40%.

Well into the organs and tissues: lungs, bronchial mucosa, sputum, organs and urinary system, reproductive organs, bone, cerebrospinal fluid, prostate gland, polymorphonuclear leukocytes, alveolar macrophages.

The average Vd levofloxacin ranges from 89 to 112 l after single and multiple in / at a dose of 500 mg.

Metabolism

In the liver, a small part of levofloxacin is oxidized and / or dezatsetiliruetsya.

Withdrawal

When you receive a single dose of 500 mg of T1 / 2 is 6-8 hours

After a single in / in a dose of 500 mg of T1 / 2 - 6.4 ± 0.7 h.

Write mainly by the kidneys by glomerular filtration and tubular secretion.

The mean final T1 / 2 from 6 to 8 h after single and repeated administration.

About 87% of the dose excreted in the urine unchanged within 48 hours Less than 4% found in feces for the period 72 hours

Pharmacokinetics in special clinical situations

In renal insufficiency, reducing clearance of the drug and its excretion by the kidneys depends on the degree of reduction of QA.

Statement

Infectious-inflammatory diseases of mild to moderate severity caused by microorganisms sensitive to the drug:
Acute sinusitis (Oral);
exacerbation of chronic bronchitis (Oral);
infections of skin and soft tissues (for oral);
in the complex therapy of drug-resistant tuberculosis (Oral);
community-acquired pneumonia (for both dosage forms);
Complicated infections of the kidneys and urinary tract infections, including pyelonephritis (for both dosage forms);
uncomplicated urinary tract infections (for both dosage forms);
prostatitis (for both dosage forms);
septicemia / bacteremia associated with the above readings (for both dosage forms);
intra-abdominal infection (for both dosage forms). .

Dosage regimen

The drug taken by mouth or injected i / v at 250-500 mg 1-2 times / day.

Doses are determined by the nature and severity of infection, as well as the sensitivity of the parasite.

Patients with normal or slightly impaired renal function (CC> 50 ml / min) the drug is recommended to appoint the following doses.

Sinusitis: inside 2 tablets of 250 mg or 1 tablet of 500 mg (500 mg levofloxacin) 1 times / day. The treatment course - 10-14 days.

Exacerbation of chronic bronchitis: the interior of a tablet of 250 mg (250 mg levofloxacin), or 2 tablets of 250 mg or 1 tablet of 500 mg (500 mg levofloxacin) 1 times / day. The treatment course - 7-10 days.

Community-acquired pneumonia: the interior of 2 tablets of 250 mg or 1 tablet of 500 mg 1-2 times / day. (500-1000 mg of levofloxacin /) or in / - 500 mg 1-2 times / sut.Kurs treatment - 7 -14 days.

Uncomplicated urinary tract infection: the interior of a tablet 250 mg (250 mg levofloxacin) 1 times / day., Or a / c - 250 mg 1 time / sut.Kurs treatment - 3 days.

Complicated urinary tract infections (including pyelonephritis): inside of a 250-mg tablets (250 mg levofloxacin) 1 times / day., Or a / c - 250 mg 1 time / day. In severe infections dosage for i / v administration may be increased. The treatment course - 7-10 days.

Prostatitis: mouth 2 tablets of 250 mg or 500 mg 1 tablet (500 mg levofloxacin) 1 times / day., Or a / c - 500 mg 1 time / day. The course of treatment - 28 days.

Septicemia / bacteremia: inside of 2 tablets of 250 mg or 1 tablet of 500 mg 1-2 times / day. (500-1000 mg of levofloxacin /) or in / - 500 mg 1-2 times / sut.Kurs treatment - 10-14 days.

Intra-abdominal infection: inside the 2 tablets of 250 mg or 1 tablet of 500 mg (500 mg levofloxacin) 1 times / day., Or in / in - 500 mg 1 time / day. The treatment course - 7-14 days in combination with antibacterial drugs, acting on the anaerobic flora.

Infections of skin and soft tissue: the interior of a 250-mg tablets (250 mg levofloxacin) 1 times / day. Or 2 tablets of 250 mg or 1 tablet of 500 mg (500 mg levofloxacin) 1-2 times a day. (Respectively 500 -1000 mg of levofloxacin in the day). The treatment course - 7-14 days.

In the combined therapy of drug-resistant forms of tuberculosis tavanic designate the interior of 1-2 tablets 500 mg 1-2 times / day. (500-1000 mg of levofloxacin /) up to 3 months.

For elderly patients with normal renal function correct dosing regimen is not required.

If abnormal liver function does not require a special selection of doses, since tavanic metabolized in the liver in a very limited degree.

Tablets should be taken without chewing and drinking plenty of fluids (from 0.5 to 1 cup). In the selection of doses of the pills can be broken on the separation groove. The drug can be taken before meals or at any time between meals.

Tavanic drug in solution is introduced into / in drip slowly.

Duration of drug administration in a dose of 500 mg (100 ml infusion rastvora/500 mg levofloxacin) should be at least 60 minutes. The solution of the drug tavanic 500 mg/100 ml, compatible with the following infusion solutions: 0.9% sodium chloride, 5% dextrose, 2.5% Ringer's solution with dextrose, Combined Solution for parenteral nutrition (amino acid, carbohydrates, electrolytes). The solution of the drug should not be mixed with heparin or solutions with an alkaline reaction (eg, with a solution of sodium bicarbonate).

When the positive dynamics of the clinical condition of the patient within a few days of treatment to move from the i / v drip to oral medication tavanic in the same dose.

Duration of treatment with a / in the introduction, depending on the course of the disease is not more than 14 days. As the use of other antibiotics, treatment for drug tavanic for oral or in / infusion should continue for at least 48-72 h after normalization of body temperature or after the eradication of reliable agent.

If you missed taking the drug should be as soon as possible to resume the reception and then continue to take tavanic on the recommended scheme.

Patients should be cautioned against self-interruption or early termination of therapy without a doctor's instructions.

Side effect

The frequency of side effects is determined according to the following table:

often in patients 1-10 out of 100

sometimes less than 1 patient out of 100

rarely less than 1 patient in 1000

rarely less than 1 patient out of 10 000

in some cases even less

Allergic reactions: sometimes - itching and redness of the skin; rare - anaphylactic and anaphylactoid reactions (manifesting symptoms such as urticaria, bronchospasm and the possibility of severe asthma) are very rare - swelling of the skin and mucous membranes (eg, in the face, throat), sudden fall in blood pressure, shock, allergic pneumonitis, vasculitis, and in some cases - Stevens-Johnson syndrome, toxic epidermal necrolysis (Lyell's syndrome) and erythema multiforme exudative.

Dermatologic reactions: very rare - photosensitization.

On the part of the digestive system: common - nausea and diarrhea, increased ALT, AST, and sometimes - loss of appetite, vomiting, abdominal pain, digestive disorders, rarely - increase of bilirubin in the blood serum, diarrhea with blood (in very rare cases it may be a sign of inflammation of the intestine or pseudomembranous colitis); very rarely - hepatitis.

On the part of metabolism: very rarely - hypoglycemia (manifested by a sharp increase in appetite, nervousness, sweating, trembling). Experience with other quinolones suggests that they can exacerbate existing porphyria, in some cases, this effect is not excluded the application of the drug tavanic.

From the side of the central nervous system and peripheral nervous system: sometimes - headache, dizziness and / or stiffness, drowsiness and sleep disorders are rarely - depression, anxiety, psychotic reactions such as hallucinations, paresthesias in the hands, trembling, excited state, seizures and confusion; very rare - and hearing impairment, violation taste and smell sensitivity, reduction of tactile sensitivity.

Since the cardiovascular system: rarely - tachycardia, falling blood pressure, very rarely - vascular collapse, and in some cases - lengthening the interval QT.

From the Musculoskeletal System: rare - the defeat of the tendons (including tendonitis), joint and muscle pain, very seldom - tendon rupture, such as Achilles tendon (may be bilateral in nature and occur within 48 h after treatment), muscle weakness ( is of particular importance for patients suffering from asthenic bulbar paralysis), in some cases - rhabdomyolysis.

From the urinary system: rarely - increases in serum creatinine in serum, very rarely - the deterioration of renal function until the acute renal failure (eg, due to allergic reactions - interstitial nephritis).

On the part of the hemopoietic system: sometimes - eosinophilia, leucopenia, rarely - neutropenia, thrombocytopenia (increased tendency to hemorrhage or bleeding) is very rare - agranulocytosis and the development of severe infection (accompanied by persistent or recurrent fever, inflammation of the tonsils and persistent deterioration of the well-being, in individual cases - hemolytic anemia, pancytopenia.

Other: sometimes - asthenia, very rarely - fever, allergic pneumonitis. Any antibiotic can cause changes in the microflora (bacteria and fungi), which is normally present in humans.

Local reactions: often - pain at the injection site, redness, phlebitis.

Contraindications
epilepsy;
tendon injury associated with hosting quinolones in history;
childhood and adolescence to 18 years;
Pregnancy
lactation (breastfeeding);
hypersensitivity to levofloxacin or other quinolones.

Precautions should use the drug in elderly patients due to high likelihood of concomitant reduction of renal function, with deficit of glucose-6-phosphate dehydrogenase.

Pregnancy and lactation

The drug is contraindicated during pregnancy and lactation (breastfeeding).

Application for violations of liver function

If abnormal liver function does not require a special selection of doses, since tavanic metabolized in the liver in a very limited degree.

Cautions

In appointing the drug elderly patients should be borne in mind that this group of patients often have renal dysfunction. During treatment with tavanic possible development of an attack of convulsions in patients with previous brain damage (including stroke or severe brain injuries). Cramping may increase readiness and while applying fenbufena similar with NSAIDs or theophylline.

In applying the drug in patients with diabetes should be borne in mind that tavanic can cause hypoglycemia.

In severe pneumonia caused by pneumococcus, the use of the drug tavanic may be insufficiently effective. Nosocomial infections caused by Pseudomonas aeruginosa, may require the use of combination therapy. Despite the fact that photosensitization observed in the application of levofloxacin is very rare, to prevent its development patients must avoid exposure to sunlight or UV-irradiation.

Suspicion of pseudomembranous colitis should be lifted immediately tavanic and start appropriate treatment. In such cases, can not be applied drugs, which suppress motility.

Elderly patients when using the drug tavanic likely to develop tendonitis increases. In the application of SCS, apparently, increases the risk of tendon rupture. If you suspect tendonitis should be lifted immediately tavanic and start appropriate treatment, providing a quiescent state in defeat.

Precautions should be administered simultaneously with tavanic probenecid and cimetidine, which block the tubular secretion; under their influence excretion of levofloxacin slightly slower. This interaction has little clinical significance and may focus mainly on patients with impaired renal function.

With simultaneous application tavanic and vitamin K antagonists should monitor the status of the blood coagulation system.

If an antibiotic can be observed changes in the microflora (bacteria, fungi), which is normally present in humans. For this reason, perhaps increased multiplication of bacteria and fungi that are resistant to antibiotics (secondary infection and superinfection), which in rare cases may require additional treatment.

Experience with other quinolones suggests that they can exacerbate porphyria. Such an effect is not excluded in the application of the drug tavanic.

In the application of quinolones in patients with deficiency of glucose-6-phosphate dehydrogenase possible hemolysis. Given this, treatment tavanic this category of patients should be conducted with extreme caution.

It should strictly adhere to the recommended duration of administration, which must be at least 60 minutes for 100 ml infusion solution. Experience with levofloxacin shows that during the infusion may experience tachycardia and transient drop in blood pressure. In rare cases it may be vascular collapse. If during infusion observed pronounced decrease in BP, the introduction of an immediate cease.

Use in pediatrics

Tavanic contraindicated for the treatment of children and adolescents because of the probability of destruction of articular cartilage.

Effects on ability to drive vehicles and management mechanisms

Tavanic may cause dizziness or stiffness, drowsiness, visual disturbances, and reduce ability to concentrate attention and psychomotor speed of reaction that should be considered in need of the drug in patients whose activities are related to driving, maintenance of machinery, the performance of work in unstable situation. This is especially true cases of drug interaction with alcohol.

Overdose

Symptoms: confusion, dizziness, impaired consciousness and seizures seizures by type of epileptic seizures, nausea, erosive lesions of mucous membranes. In clinical pharmacological studies with the use of levofloxacin at doses higher than average therapeutic, was observed lengthening of the interval QT.

Treatment: perform symptomatically. Levofloxacin is not displayed by dialysis. Specific antidote exists. The erroneous admission of one extra tablet of 250 mg tavanic no negative actions.

Drug Interactions

Quinolone can enhance the ability of drugs (including fenbufena and similarities with NSAIDs, theophylline), lower the threshold of convulsive readiness. The action of the drug tavanic significantly reduced, while the use of sukralfatom, magnesium or aluminum containing antacid, as well as salts of iron (the interval between doses tavanic and these drugs should be at least 2 h). Since calcium carbonate interaction was not detected.

Stain (renal clearance) levofloxacin slightly slower under the influence of cimetidine and probenecid, which has virtually no clinical significance. Tavanic causes a slight increase in T1 / 2 cyclosporine from plasma.

Simultaneous reception from the SCS increases the risk of tendon rupture.

Terms and Conditions of storage

The drug in the form of coated tablets should be stored in a dry place at temperatures not above 25 ° C.

Shelf life - 5 years

Do not use the drug after the expiration date stated on the packaging.

The drug in the form of solution for injection should be stored in a dry, dark place at temperatures not above 25 ° C.

Shelf life - 3 years.

When room lighting solution can be stored without svetozaschity no more than 3 days.

The drug should be stored out of reach of children.