Levofloxacin-Vertex pills 500mg, 5pcs

Composition

1 film-coated tablet contains

Active ingredient:

levofloxacin hemihydrate in terms of levofloxacin-500.00 mg

Excipients (core):

microcrystalline cellulose — 60.00 mg,

sodium carboxymethyl starch-35.00 mg,

povidone (polyvinylpyrrolidone) – 30.00 mg,

magnesium stearate-10.00 mg,

croscarmellose sodium-16.54 mg,

colloidal silicon dioxide-6.00 mg.

Excipients (shell):

Opadray White-30.00 mg, including polyvinyl alcohol-14.070 mg, macrogol 3350-7.080 mg, talc-5.220 mg, titanium dioxide-3.630 mg

Pharmacological action

The optically active levorotatory isomer of ofloxacin is L-ofloxacin (S-(-)-enantiomer). It has a wide spectrum of antimicrobial activity. Blocks bacterial topoisomerase IV and DNA gyrase (topoisomerase II). Disrupts supercoiling and crosslinking of DNA breaks, causes deep morphological changes in the cytoplasm and cell wall. In concentrations equivalent to or exceeding the minimum suppressive concentrations (MPC), it most often has a bactericidal effect. The main mechanism of resistance development is associated with a mutation of the gyr-A gene with the possible development of cross-resistance between levofloxacin and other fluoroquinolones. Cross-resistance between levofloxacin and other classes of antibacterial drugs usually does not occur.

Sensitive microorganisms: aerobic gram-positive microorganisms-Corynebacterium diphtheriae, Enterococcus spp., including Enterococcus faecalis, Listeria monocytogenes, Staphylococcus spp. (coagulasepositive methicillinsusceptible / lactosylceramide / moderately sensitive strains), including Staphylococcus aureus (methicillinsusceptible strains), Staphylococcus epidermidis (methicillinsusceptible strains), Streptococcus spp. groups C and G, Streptococcus agalactiae, Streptococcus pneumoniae (penicillinsusceptible / moderately sensitive / resistant strains), Streptococcus pyogenes, Streptococcus spp. viridans group (penicillinsusceptible / resistant strains); aerobic gram – negative microorganisms Acinetobacter spp., including Acinetobacter baumannii, Acinetobacillus actinomycetecomitans, Citrobacter freundii, Eikenella corrodens, Enterobacter spp., including Enterobacter aerogenes, Enterobacter agglomerans, Enterobacter cloacae, Escherichia coli, Gardnerella vaginalis, Haemophilus ducreyi, Haemophilus influenzae (ampicillinampicillin / resistant strains), Haemophilus parainfluenzae, Helicobacter pylori, Klebsiella spp., including Klebsiella oxytoca, Klebsiella pneumoniae, Moraxella catarrhalis (producing and reproducirse beta-lactamase strains), Morganella morganii, Neisseria gonorrhoeae (and reproducirse producing penicillinase strains), Neisseria meningitidis, Pasteurella spp., including Pasteurella canis, Pasteurella dagmatis, Pasteurella multocida, Proteus vulgaris, Providencia spp., including Providencia rettgeri, Providencia stuartii, Pseudomonas spp., including Pseudomonas aeruginosa, Serratia spp., including Serratia marcescens, Salmonella spp. ; anaerobic microorganisms Bacteroides fragilis, Bifidobacterium spp., Clostridium perfringens, Fusobacterium spp., Peptostreptococcus spp. Propionibacterium spp. Veilonella spp. ; other micro – organisms Bartonella spp. Chlamydia pneumoniae, Chlamydia psittaci, Chlamydia trachomatis, Legionella pneumophila, Legionella spp., Mycobacterium leprae, Mycobacterium tuberculosis, Mycoplasma hominis, Mycoplasma pneumoniae, Rickettsia spp., Ureaplasma urealyticum.

Moderately sensitive micro-organisms (MPC greater than 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-Burkhoideria cepacia, Campylobacter jejuni Campylobacter coli; anaerobic microorganisms-Bacteroides thetaiotaomicron, Bacteroides vulgatus, Bacteroides ovatus, Prevotella spp., Porphyromonas spp.

Resistant microorganisms (MPC greater than 8 mg / l): aerobic gram-positive microorganisms-Corynebacterium jeikeium, Staphylococcus aureus (methicillin-resistant strains), other Staphylococcus spp. (coagulase-negative methicillin-resistant strains); aerobic gram – negative microorganisms – Alcaligenes xylosoxidane; other microorganisms-Mycobacterium avium.

Indications

Infectious and inflammatory diseases caused by microorganisms sensitive to levofloxacin:

– infections of the lower respiratory tract (acute exacerbation of chronic bronchitis, community-acquired pneumonia);

– acute maxillary sinusitis;

– uncomplicated urinary tract infections;

– complicated urinary tract infections (including acute pyelonephritis);

infections of skin and soft tissues (festering of sebaceous cysts, abscesses, boils);

chronic bacterial prostatitis;

– intra-abdominal infection;

– complex therapy of drug-resistant forms of tuberculosis.

Contraindications

Hypersensitivity to levofloxacin and other fluoroquinolones, epilepsy, tendon damage during previous treatment with quinolones, pregnancy, breastfeeding, children and adolescents (up to 18 years).

With caution

Advanced age (high probability of concomitant decline in renal function), glucose-6-phosphate dehydrogenase deficiency.

Side effects

From the digestive system: nausea, vomiting, diarrhea (including blood), digestive disorders, decreased appetite, abdominal pain, pseudomembranous colitis, increased activity of “liver” transaminases, hyperbilirubinemia, hepatitis, dysbiosis.

From the cardiovascular system: reduced blood pressure, vascular collapse, tachycardia, increased Q-T interval on the cardiogram, atrial fibrillation.

From the side of metabolism: hypoglycemia (increased appetite, increased sweating, trembling, nervousness), hyperglycemia (dry mouth, thirst, increased urination, fatigue, blurred vision, dry or itchy skin, arrhythmia).

Nervous system disorders: headache, dizziness, weakness, drowsiness, insomnia, restlessness, paresthesia in the hands, fear, hallucinations, confusion, depression, motor disorders, convulsions, peripheral sensory neuropathy, peripheral sensory-motor neuropathy, mental disorders with behavioral disorders with self-harm, including suicidal thoughts and suicide attempts, extrapyramidal disorders, agitation (agitation), nighttime sleep disorders nightmares.

From the side of the senses: visual, hearing, olfactory, taste and tactile sensitivity disorders, tinnitus.

Musculoskeletal disorders: arthralgia, muscle weakness, myalgia, tendon rupture, tendinitis, rhabdomyolysis.

From the urinary system: hypercreatininemia, interstitial nephritis, acute renal failure.

Hematopoietic disorders: eosinophilia, hemolytic anemia, leukopenia, neutropenia, agranulocytosis, thrombocytopenia, pancytopenia, hemorrhages.

Allergic reactions: pruritus and hyperemia of the skin, edema of the skin and mucous membranes, urticaria, malignant exudative erythema (Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell’s syndrome), bronchospasm, anaphylactic shock, allergic pneumonitis, vasculitis.

Others: asthenia, acute porphyria, photosensitization, persistent fever, leukocytoclastic vasculitis, development of superinfection.

Interaction

Quinolones can enhance the ability of drugs, including theophylline, nonsteroidal anti-inflammatory drugs to lower the threshold of convulsive readiness. When taken concomitantly with fenbufen, higher concentrations of levofloxacin are observed than with motor therapy.

The effect of levofloxacin is reduced by drugs that inhibit intestinal motility, sucralfate, magnesium-or aluminum-containing antacids, iron and zinc salts.

Taking glucocorticosteroids increases the risk of tendon rupture.

Levofloxacin enhances the anticoagulant activity of warfarin.

Elimination (renal clearance) of levofloxacin is slightly slowed down by cimetidine and probenecid due to possible blocking of the tubular secretion of levofloxacin in the kidneys. It should be noted that this interaction is of clinical significance, primarily for patients with impaired renal function.

Levofloxacin increases the elimination half-life of cyclosporine.

Simultaneous use of levofloxacin and hypoglycemic agents leads to changes in the concentration of glucose in blood plasma (hypoglycemia and hyperglycemia).

When used concomitantly with drugs that prolong the Q-T interval (class IA and III antiarrhythmics, tricyclic and tetracyclic antidepressants, neuroleptics, macrolides, antifungal agents, imidazole derivatives, some antihistamines, including astemizole, terfenadine, ebastine), the Q-T interval may be prolonged.

How to take it, course of administration and dosage

The drug should be administered orally during meals or in between meals, without chewing, with a sufficient amount of liquid.

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

Recommended dose for adults with normal renal function (creatinine clearance (KK)>50 ml / min):

In acute bacterial sinusitis-500 mg once a day for 10-14 days;

In case of exacerbation of chronic bronchitis-250-500 mg once a day for 7-10 days;

For community-acquired pneumonia-500 mg 1 or 2 times a day for 7-14 days;

For uncomplicated urinary tract and kidney infections-250 mg once a day for 3 days;

For complicated urinary tract infections-250 mg once a day for 7-10 days;

For chronic bacterial prostatitis-500 mg once a day for 28 days;

For skin and soft tissue infections-250-500 mg 1-2 times a day for 7-14 days;

Intraabdominal infections-500 mg once a day for 7-14 days (in combination with antibacterial drugs acting on anaerobic flora);

Tuberculosis (complex therapy of drug-resistant forms — – 500 mg 1-2 times a day, the course of treatment is up to 3 months.

Overdose

Symptoms:

confusion, dizziness, impaired consciousness, convulsions, possible nausea, vomiting and erosive lesions of the mucous membranes. Studies have shown that when levofloxacin is used in doses higher than the average therapeutic dose, it is possible to prolong the Q-T interval.

Treatment:

if necessary, conduct symptomatic therapy. Levofloxacin is not excreted during hemodialysis, peritoneal dialysis, and permanent peritoneal dialysis. There is no specific antidote.

Special instructions

The drug should be used at least 2 hours before or 2 hours after taking iron, zinc, antacids and sucralfate preparations.

During treatment with the drug, it is necessary to avoid sun and artificial UV radiation in order to avoid damage to the skin (photosensitization).

If signs of tendonitis, pseudomembrane colitis, or allergic reactions appear, the drug is immediately discontinued.

It should be borne in mind that patients with a history of brain damage (stroke, severe injury) may develop convulsions, with insufficient glucose-6-phosphate dehydrogenase — the risk of developing hemolysis.

When levofloxacin and warfarin are co-administered, careful monitoring of prothrombin time and other coagulation parameters is necessary.

It is recommended to carefully monitor the concentration of glucose in the blood plasma when using the drug simultaneously with hypoglycemic drugs.

Since levofloxacin is mainly excreted by the kidneys, patients with impaired renal function require mandatory monitoring of renal function, as well as adjustment of the dosage regimen. Prolongation of the Q-T interval has been reported in patients treated with fluoroquinolones, including levofloxacin. When using fluoroquinolones, including levofloxacin should be used with caution in patients with known risk factors lengthening of the Q-T interval: older age; electrolyte imbalance (hypokalemia, hypomagnesemia); the syndrome of congenital lengthening of the Q-T interval; heart disease (heart failure, myocardial infarction, bradycardia); simultaneous reception of drugs that can prolong the interval Q-T.

Patients receiving fluoroquinolones, including levofloxacin, have experienced sensory and sensorimotor peripheral neuropathy, which may start quickly. If the patient develops symptoms of neuropathy, levofloxacin should be discontinued. This minimizes the possible risk of irreversible changes.

Storage conditions

Store the drug in a dry place, protected from light, at a temperature not exceeding 25°C. Keep out of reach of children.

Shelf life

2 years

Active ingredient

Levofloxacin

Conditions of release from pharmacies

By prescription

Dosage form

Tablets

Indications

Urinary Tract Infections, Pyelonephritis, Bronchitis, Prostatitis, Pneumonia, Sinusitis, Skin Infections