Floracid - instructions for use, doses, side effects, contraindications

Excipients: crospovidone - 14.0 mg or 28.0 mg, magnesium stearate - 3.9 mg or 7.8 mg, sodium lauryl sulfate - 5.0 mg or 10.0 mg, povidone - 15.0 mg or 30, 0 mg, microcrystalline cellulose - 98.2 mg or 196.4 mg, silicon dioxide colloid (aerosil) - 3.9 mg or 7.8 mg.

Shell Composition: Foam II (sepia 85): (polyvinyl alcohol partially hydrolysed, titanium dioxide E 171, macrogol-3350, talc, iron dye oxide yellow E 172, iron oxide red oxide E 172) 20.0 mg or 40.0 mg.

Description:The tablets covered with a film cover of a pinkish-cream color, oblong, biconcave with risk on one side. Two layers are visible on the cross-section.

Pharmacotherapeutic group:Antimicrobial agent - fluoroquinolone

ATX: & nbsp

J.01.M.A Fluoroquinolones

J.01.M.A.12 Levofloxacin

Pharmacodynamics:

A broad-spectrum antimicrobial agent from the group of fluoroquinolones, the left-handed isloxacin isomer. Levofloxacin blocks the DNA-gyrase (topoisomerase II) and topoisomerase IV, disrupts supercoiling and cross-linking of DNA gaps, inhibits DNA synthesis,causes profound morphological changes in the cytoplasm, cell wall and membranes.

Levofloxacin is active against most strains of microorganisms both in conditions in vitro, and in vivo.

In vivo effective at respect 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 influenzae, 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, Providencia stuartii, Serratia marcescens, Clostridium perfringens.

In vitro:

Sensitive microorganisms (IPC < 2 mg / ml).

Aerobic Gram-positive microorganisms: Corynebacterium diphtheriae, Enterococcus spp., Listeria monocytogenes, Staphylococcus spp. (coagulase-negative methicillin-sensitive / methicillin-moderately sensitive strains), Staphylococcus spp. (FROMNS), Streptococcus spp. group C and G.

Aerobic Gram-negative microorganisms: Acinetobacter spp., Actinobacillus actinomycetemcomitans, Eikenella corrodens, Enterobacter spp., Gardnerella vaginalis, Haemophilus ducreyi, Helicobacter pylori, Klebsiella spp., Neisseria gonorrhoeae (strains, producing and non-reducing penicillinase), Neisseria meningitidis, Pasteurella spp. (at Tom number of Pasteurella conis, Pasteurella dagmatis, Pasteurella multocida), Providencia spp., Pseudomonas spp., Salmonella spp., Serratia spp.

Anaerobic microorganisms: Bacteroides fragilis, Bifidobacterium spp., Fusobacterium spp., Peptostreptococcus spp., Propionibacterium spp., Veilonella spp.

Other microorganisms: Bartonella spp., Chlamydia psittaci, Chlamydia trachomatis, Legionella spp., Mycobacterium spp. (at Tom number of Mycobacterium leprae, Mycobacterium tuberculosis), Mycoplasma hominis, Rickettsia spp., Ureaplasma urealyticum.

Levofloxacin is moderately active (MIC> 4 mg / l):

Aerobic Gram-positive microorganisms: Corynebacterium urealyticum, Corynebacterium xerosis, Enterococcus faecium, Staphylococcus epidermidis (methicillin-resistant strains), Staphylococcus haemolyticus (methicillin-resistant strains).

Aerobic Gram-negative microorganisms: Burkholderia cepacia, Campilobacter jejuni, Campilobacter coli.

Anaerobic microorganisms: Bacteroides thetaiotaomicron, Bacteroides vulgatus, Bacteroides ovatus, Prevotella spp., Porphyromonas spp.

To levofoloxacin are stable (MIC> 8 mg / l):

Aerobic Gram-positive microorganisms: Corynebacterium jeikeium, Staphylococcus aureus (methicillin-resistant strains), Staphylococcus spp. (coagulase-negative methicillin-resistant strains).

Aerobic Gram-negative microorganisms: Alcaligenes xylosoxidans.

Other microorganisms: Mycobacterium avium.

Pharmacokinetics:

After oral administration levofloxacin quickly and almost completely absorbed from the gastrointestinal tract. Food intake has little effect on the speed and completeness of absorption. Bioavailability of 500 mg of levofloxacin is 100%. With a single dose of 500 mg of levofloxacin, the maximum concentration (Cmah) in blood plasma is 5.2 - 6.9 μg / ml, the time to reach the maximum concentration (TCmah) - 1.3 hours, half-life (T1/2) - 6-8 hours.

The connection with plasma proteins is 30-40%. It penetrates well into organs and tissues: lungs, bronchial mucosa, sputum, urinary system organs, bone tissue, cerebrospinal fluid, prostate gland, polymorphonuclear leukocytes, alveolar macrophages.

In the liver, a small portion is oxidized and / or deacetylated.

It is excreted from the body mainly by the kidneys through glomerular filtration and tubular secretion. About 87% of the dose is excreted by the kidneys unchanged for 48 hours, less than 4% is excreted through the intestine within 72 hours.

Indications:

Infectious-inflammatory diseases caused by microorganisms sensitive to the preparation:

- Acute sinusitis;

- exacerbation of chronic bronchitis;

- community-acquired pneumonia;

- Complicated infections of the kidneys and urinary tract (including pyelonephritis);

uncomplicated urinary tract infections;

- bacterial prostatitis;

- infections of the skin and soft tissues;

- intra-abdominal infection;

- for complex treatment of drug-resistant forms of tuberculosis.

Contraindications:

- hypersensitivity to levofloxacin or other quinolones;

- epilepsy;

- lesions of tendons during the previous treatment with quinolones;

- children and adolescence (up to 18 years);

- pregnancy and lactation.

Carefully:

In elderly people due to the high likelihood of concomitant decline in kidney function, with a deficiency of glucose-6-phosphate dehydrogenase.

Dosing and Administration:

Inside, before meals or between meals. Tablets can not be chewed and washed down with a sufficient amount of liquid (0.5 to 1 cup). Doses are determined by the nature and severity of the infection, as well as the suspected pathogen susceptibility.

Patients with normal or moderately reduced renal function (creatinine clearance> 50 mL / min) are recommended the following dosing regimen:

Sinusitis: 500 mg once a day. Duration of treatment is 10-14 days.

Exacerbation of chronic bronchitis: 250 mg or 500 mg once a day. The duration of treatment is 7-10 days.

Community-acquired pneumonia: 500 mg 1-2 times a day. The duration of treatment is 7-14 days.

Uncomplicated urinary tract infections: 250 mg once a day. Duration of treatment - 3 days.

Prostatitis 500 mg once a day. Duration of treatment is -28 days.

Complicated urinary tract infections, including pyelonephritis 250 mg once a day. The duration of treatment is 7-10 days.

Infections of the skin and soft tissues: 250 mg once a day or 500 mg 1-2 times a day. Duration of treatment is 7-14 days.

Intraabdominal infection: 500 mg once a day. The duration of treatment is 7-14 days (in combination with antibacterial drugs acting on anaerobic flora).

Complex treatment of drug-resistant forms of tuberculosis: 500 mg 1-2 times a day. Duration of treatment - up to 3 months.

Dosing regimen in patients with impaired renal function.

Creatinine clearance	250 mg / 24 h	500 mg / 24 h	500 mg / 12 h
Creatinine clearance	first dose: 250 mg	first dose: 500 mg	first dose: 500 mg
50-20 ml / min	then: 125 mg / 24 h	then: 250 mg / 24 h	then: 250 mg / 12h
19-10 ml / min	then: 125 mg / 48 h.	then: 125 mg / 24h	then: 125 mg / 12 h
<10 ml / min (including hemodialysis and	then: 125 mg /	then: 125 mg /	then: 125 mg /
CAPD¹	48 h	24h	24 h

¹permanent ambulatory peritoneal dialysis.

After hemodialysis or permanent ambulatory peritoneal dialysis (CAPD), no additional doses are required.

If the liver function is not required, a special dose selection is required, as Floracid® is only metabolized to a very small extent in the liver.

For elderly patients, there is no need to change the dosage regimen, except for cases of low creatinine clearance.

As with the use of other antibiotics, treatment with Floracid® is recommended to continue for at least 48-72 hours after the normalization of body temperature or after a reliable eradication of the pathogen.

If the drug is missed, it should be resumed as soon as possible and continue to take Floracid® according to the recommended schedule.

Side effects:

The frequency of the side effect is determined using the following table:

Frequency	The appearance of side effects
often:	in 1-10 patients out of 100
sometimes:	less than 1 patient out of 100
rarely:	less than 1 patient out of 1,000
rarely:	less than 1 patient out of 10 000
in some cases:	less than 0.01%

Allergic reactions:

Sometimes: itching and redness of the skin.

Rarely: urticaria, bronchospasm, asphyxiation.

Rarely: swelling of the skin and mucous membranes (for example, in the face and larynx), anaphylactic shock; allergic pneumonitis; vasculitis.

In some cases: Stevens-Johnson syndrome, toxic epidermal necrolysis (Lyell's syndrome), and exudative erythema multiforme.

From the digestive system:

Often: nausea, diarrhea, increased activity of alanine aminotransferase (ALT), aspartate aminotransferase (ACT).

Sometimes: loss of appetite, vomiting, abdominal pain, digestive disorders.

Rarely: increased serum bilirubin levels, diarrhea with blood (in very rare cases it can be a sign of inflammation of the intestine and pseudomembranous colitis), dysbiosis.

Rarely: hepatitis.

From the side of metabolism:

Rarely: hypoglycemia (manifested by a sharp increase in appetite, nervousness, sweating, trembling). The experience with the use of other quinolones indicates that they are capable of causing porphyria exacerbation, in some cases this effect is not excluded even when levofloxacin is used.

From the side of the neutral nervous system and the peripheral nervous system:

Sometimes: headache, dizziness and / or numbness, drowsiness, sleep disturbances.

Rarely: depression, anxiety, psychotic reactions (for example, hallucinations), paresthesia in the hands, trembling, nervous state, convulsions and confusion.

Rarely: visual and hearing impairments, violation of taste sensitivity and smell, reduction of tactile sensitivity.

From the cardiovascular system:

Rarely: tachycardia, lowering blood pressure.

Rarely: cardiovascular collapse.

In some cases: interval lengthening QT.

From the musculoskeletal system:

Rarely: affections of tendons (including tendonitis), joint and muscle pain.

Rarely: rupture of tendons (for example, Achillov's tendons can be observed within 48 hours after the beginning of treatment and can be bilateral); arthralgia, myalgia, muscle weakness, which is of particular importance for patients with bulbar syndrome.

In some cases: muscle damage (rhabdomyolysis).

From the urinary system:

Rarely: increased serum creatinine levels.

Rarely: impaired renal function up to acute renal failure, interstitial nephritis.

From the hematopoiesis:

Sometimes: eosinophilia, leukopenia.

Rarely: neutropenia; thrombocytopenia, hemorrhage.

Rarely: agranulocytosis.

In some cases: hemolytic anemia; pancytopenia.

Other

Sometimes: asthenia.

Rarely: development of superinfections, fever, photosensitivity.

Overdose:

Symptoms: confusion, dizziness, impaired consciousness and seizures as epi-seizures, nausea, erosive lesions of the mucous membranes, lengthening of the interval QT.

Treatment: symptomatic. Levofloxacin not output by dialysis.

There is no specific antidote.

Interaction:

Quinolones can enhance the ability of drugs (including non-steroidal anti-inflammatory drugs, theophylline) to lower the threshold of convulsive readiness. The effect of levofloxacin is significantly reduced when used simultaneously with sucralfate, magnesium or aluminum containing antacid agents, as well as with iron salts (the interval between taking levofloxacin and these medicines should be at least 2 hours). Calcium carbonate was not detected in the interaction. Elimination (renal clearance) of levofloxacin slightly slowed down by the action of cimetidine and probenecid, which has practically no clinical significance. Levofloxacin slightly increases the half-life (T1/2) cyclosporine from the blood plasma.

Simultaneous reception with glucocorticosteroids increases the risk of rupture of tendons.

Special instructions:

When prescribing Floracid® to elderly patients, it should be borne in mind that patients of this group often have impaired renal function.

In severe pneumonia caused by pneumococcus, Floracid® may not be effective enough. Hospital infections caused by Pseudomonas aeruginosa, may require combined treatment.

During treatment with Floracid®, an episode of seizures may develop in patients with previous brain damage due to, for example, a stroke or severe trauma.

Despite the fact that photosensitivity is noted with the use of the preparation Floracid ® very rarely, patients should avoid exposure to sun or ultraviolet irradiation in order to avoid its development.

If suspected pseudomembranous colitis, immediately discontinue Floracid® and begin appropriate treatment. In such cases, drugs that depress intestinal motility should not be used.

In elderly patients with the use of Floracid®, the likelihood of tendonitis increases. When using glucocorticosteroids, the risk of rupture of tendons increases. If suspected of tendonitis, Floracid® should be immediately discontinued and appropriate treatment initiated, ensuring a state of rest in the area of the lesion.

With the simultaneous use of vitamin K antagonists, control over the blood coagulation system is necessary.

Hemolysis is possible in patients with insufficiency of glucose-6-phosphate dehydrogenase.

Effect on the ability to drive transp. cf. and fur:

During the treatment period, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Form release / dosage:

Film-coated tablets, 250 and 500 mg.

Packaging:

5 or 10 tablets in a contour mesh box made of polyvinylchloride film and aluminum foil printed lacquered.

1 circuit cell pack together with the instruction for use is placed in a pack of cardboard.

Storage conditions:In the dark place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

2 years. Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:LS-000061

Date of registration:11.02.2010

The owner of the registration certificate:VALENTA PHARM, PAO VALENTA PHARM, PAO Russia

Manufacturer: & nbsp

VALENTA PHARMACEUTICS, JSC Russia

Information update date: & nbsp09.10.2015

Illustrated instructions

Instructions

Floracid® (Floracyd®)