Composition Levofloxacin:
Levofloxacin - 250 mg; Aux.-va: MCC, sodium carboxymethyl starch, povidone, magnesium stearate, croscarmellose sodium, colloidal silicon dioxide
general description Levofloxacin:
Antimicrobial - fluoroquinolone
Special conditions Levofloxacin:
Levofloxacin cannot be used to treat children and adolescents because of the likelihood of damage to articular cartilage.
When treating patients of senile age, it should be borne in mind that patients of this group often suffer from impaired renal function (see section "Dosage and administration").
In severe pneumonia caused by pneumococci, levofloxacin may not give the optimal therapeutic effect. Hospital infections caused by certain pathogens (P. aeruginosa) may require combination treatment.
During treatment with Levofloxacin, it is possible to develop an attack of seizures in patients with a previous brain damage due to, for example, a stroke or severe trauma.
Despite the fact that photosensitization is rarely observed with levofloxacin, in order to avoid it, patients are not recommended to undergo strong sunlight or artificial ultraviolet radiation without special need.
If pseudomembranous colitis is suspected, levofloxacin should be immediately withdrawn and appropriate treatment should be initiated. In such cases, drugs that inhibit intestinal motility should not be used.
Rarely observed with the use of the drug Levofloxacin tendonitis (primarily inflammation of the Achilles tendon) can lead to rupture of tendons. Elderly patients are more prone to tendonitis. Treatment with glucocorticosteroids in all likelihood increases the risk of tendon rupture. If you suspect a tendonitis, you should immediately stop treatment with Levofloxacin and begin appropriate treatment for the affected tendon.
Patients with glucose-6-phosphate dehydrogenase deficiency (a hereditary metabolic disorder) can respond to fluoroquinolones by destroying red blood cells (hemolysis). In this regard, the treatment of such patients with levofloxacin should be carried out with great care.
Influence on the ability to drive vehicles and control mechanisms
Side effects of Levofloxacin, such as dizziness or numbness, drowsiness, and visual impairment (see also the section “Side effects”), may impair reactivity and ability to concentrate. This may pose a certain risk in situations where these abilities are of particular importance. (for example, when driving a car, when servicing machines and mechanisms, when performing work in an unstable position).
Overdose Levofloxacin:
Symptoms of an overdose of Levofloxacin are manifested at the central nervous system level (confusion, dizziness, impaired consciousness and bouts of seizures, such as epiprippacks). In addition, gastrointestinal upsets (for example, nausea) and erosive lesions of the mucous membranes, prolongation of the Q-T interval can be noted.
Treatment should be symptomatic. Levofloxacin is not excreted by dialysis (hemodialysis, peritoneal dialysis and permanent peritoneal dialysis). There is no specific antidote.
Drug Interactions Levofloxacin:
Levofloxacin increases T1 / 2 of cyclosporine.
The effect of levofloxacin is reduced by drugs that inhibit intestinal motility, sucralfate, magnesium and aluminum-containing antacids and iron salts (a break between taking at least 2 hours is necessary).
With the simultaneous use of NSAIDs, theophylline increases convulsive readiness, GCS - increase the risk of tendon rupture.
Cimetidine and drugs that block tubular secretion slow down the excretion of levofloxacin.
The solution of levofloxacin for iv administration is compatible with 0.9% sodium chloride solution, 5% dextrose solution, 2.5% Ringer's solution with dextrose, combined solutions for parenteral nutrition (amino acids, carbohydrates, electrolytes).
A solution of levofloxacin for iv administration cannot be mixed with heparin and solutions that have an alkaline reaction.
Pharmacodynamics Levofloxacin:
An antimicrobial drug from the group of fluoroquinolones, the levorotatory ofloxacin isomer. It has a wide range of antimicrobial effects. Levofloxacin blocks DNA gyrase (topoisomerase II) and topoisomerase IV, disrupts supercoiling and cross-linking of DNA breaks, inhibits DNA synthesis, and causes deep morphological changes in the cytoplasm, cell wall and bacterial membranes. Effective against most strains of microorganisms in vitro and in vivo. Sensitive to the action of the drug: in vitro sensitive (minimal inhibitory concentration of aerobic gram-positive microorganisms: Corynebacterium diphtheriae, Enterococcus spp. (Including Enterococcus faecalis), Listeria monocytogenes, Staphylococcus spp. (Coagulase-sensitive strain-sensitive methicillins) (methicillin-sensitive strains), Staphylococcus epidermidis (methicillin-sensitive strains), Staphylococcus spr. (leukotoxin-containing); Streptococcus spp. groups C and G, Streptococcus agalactiae, Streptococcus susceptible, streptococcus susceptible, moderately sensitive penicillocensitive, resistant penicillin-susceptible / resistant strains); aerobic gram-negative microorganisms: Acinetobacter spp. (including Acinetobacter baumannii), Actinobacillus actinomycetemcomitans, Citrobacter freundii, Eikenella corrodens, Enterobacter aerogenes, Enterobacter, enterobacter ns, Enterobacter spp. (including Enterobacter cloacae), Escherichia coli, Gardnerella vaginalis, Haemophilus ducreyi, Haemophilus influenzae (ampicillin-sensitive / resistant strains), Haemophilus parainfl uenzae, Helicobacter pylori, Klebsiella spp. (including Klebsiella oxytoca, Klebsiella pneumoniae), Moraxella catarrhalis (producing and non-producing beta-lactamase strains), Morganella morganii, Neisseria gonorrhoeae (producing and
penicillinase non-producing strains), Neisseria meningitidis, Pasteurella spp. (including Pasteurella canis, Pasteurella dagmatis, Pasteurella multocida), Proteus mirabilis, 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, Bifi dobacterium spp., Clostridium perfringens, Fusobacterium spp., Peptostreptococcus spp., Propionibacterium spp., Veilonella spp .; other microorganisms: Bartonella spp., Chlamydia pneumoniae, Chlamydia psittaci, Chlamydia trachomatis, Legionella spp. (including Legionella pneumophila), Mycobacterium spp. (including Mycobacterium leprae, Mycobacterium tuberculosis), Mycoplasma hominis, Mycoplasma pneumoniae, Rickettsia spp., Ureaplasma urealyticum. Moderately sensitive microorganisms: 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. Resistant microorganisms: aerobic gram-positive microorganisms: Corynebacterium jeikeium, Staphylococcus aureus (methicillin-resistant strains), other Staphylococcus spp. (coagulase-negative methicillin-resistant strains); aerobic gram-negative microorganisms: Alcaligenes xylosoxidans; other microorganisms: Mycobacterium avium.
Pharmokinetics Levofloxacin:
Levofloxacin is rapidly and almost completely absorbed after oral administration. Eating little effect on the speed and completeness of absorption. The bioavailability of 500 mg of levofloxacin after oral administration is almost 100%.
After taking a single dose of 500 mg of Levofloxacin, Cmax is 5.2-6.9 μg / ml, the time to reach Cmax is 1.3 hours, T1 / 2 is 6-8 hours.
Communication with plasma proteins - 30-40%. It penetrates well into organs and tissues: lungs, mucous membrane of the bronchi, sputum, organs of the genitourinary system, bone tissue, cerebrospinal fluid, prostate gland, polymorphonuclear leukocytes, alveolar macrophages.
In the liver, a small portion is oxidized and / or deacetylated. It is excreted mainly by the kidneys by glomerular filtration and tubular secretion. After oral administration, approximately 87% of the dose taken is excreted unchanged in the urine within 48 hours, less than 4% with feces within 72 hours.
Indications Levofloxacin:
Infectious and inflammatory diseases caused by microorganisms sensitive to Levofloxacin:
lower respiratory tract infections (exacerbations of chronic bronchitis, community-acquired pneumonia); acute maxillary sinusitis
uncomplicated urinary tract infections
complicated urinary tract infections (including acute pyelonephritis)
infections of the skin and soft tissues (suppurating atheroma, abscess, boils)
chronic bacterial prostatitis
intra-abdominal infection
complex therapy of drug-resistant forms of tuberculosis.
Contraindications Levofloxacin:
- hypersensitivity to levofloxacin or to other quinolones;
- renal failure (with creatinine clearance less than 20 ml / min. - due to the impossibility of dosing this dosage form);
- epilepsy;
- tendon lesions with previous treatment with quinolones;
- childhood and adolescence (up to 18 years);
- pregnancy and lactation.
Caution should be used in the elderly due to the high likelihood of a concomitant decrease in renal function, as well as with a deficiency of glucose-6-phosphate dehydrogenase.
Pregnancy and lactation
Contraindicated in pregnancy and lactation.
Side effects Levofloxacin:
The frequency of a side effect is determined by
following table:
Incidence 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
very rare: less than 1 patient out of 10,000
individual cases less than 0.01%
Allergic reactions: sometimes - itching and redness of the skin; rarely, general hypersensitivity reactions (anaphylactic and anaphylactoid reactions) with symptoms such as urticaria, narrowing of the bronchi and possibly severe suffocation; very rarely - swelling of the skin and mucous membranes (for example, in the face and pharynx), a sudden drop in blood pressure and shock, increased sensitivity to solar and ultraviolet radiation (see "Special Instructions"), allergic pneumonitis, vasculitis; in some cases, severe rashes on the skin with the formation of blisters, for example, Stevens-Johnson syndrome, toxic epidermal necrolysis (Lyell syndrome) and exudative erythema multiforme. General hypersensitivity reactions can sometimes be preceded by milder skin reactions. The above reactions may develop after the first dose several minutes or hours after administration of the drug Levofloxacin.
From the digestive system: often - nausea, diarrhea, increased activity of liver enzymes (for example, alanine aminotransferase and aspartate aminotransferase); sometimes - loss of appetite, vomiting, abdominal pain, digestive disorders; rarely - diarrhea with an admixture of blood, which in very rare cases can be a sign of intestinal inflammation and even pseudomembranous colitis (see "Special instructions").
From the side of metabolism: very rarely - a decrease in blood glucose concentration, which is of particular importance for patients suffering from diabetes mellitus (possible signs of hypoglycemia: increased appetite, nervousness, perspiration, trembling). The experience of using other quinolones suggests that they can cause exacerbation of porphyria in patients already suffering from this disease. A similar effect is not excluded with the use of the drug levofloxacin.
From the nervous system: sometimes - headache, dizziness and / or numbness, drowsiness, sleep disturbances; rarely - anxiety, paresthesia in the hands, trembling, psychotic reactions such as hallucinations and depressions, excited state, convulsions and confusion; very rarely - visual and hearing impairment, violation of taste sensitivity and smell, decreased tactile sensitivity.
From the cardiovascular system: rarely - increased heart rate, lowering blood pressure; very rarely - vascular (shock-like) collapse; in some cases, lengthening of the Q-T interval.
From the musculoskeletal system: rarely - tendon lesions (including tendonitis), joint and muscle pain; very rarely - tendon rupture (for example, Achilles tendon); this side effect can be observed within 48 hours after the start of treatment and can be bilateral in nature (see "Special Instructions"), muscle weakness, which is of particular importance for patients with bulbar syndrome; in some cases, muscle damage (rhabdomyolysis).
From the urinary system: rarely - increased levels of bilirubin and creatinine in blood serum; very rarely - impaired renal function up to acute renal failure, interstitial nephritis.
From the hemopoietic organs: sometimes - an increase in the number of eosinophils, a decrease in the number of leukocytes; rarely - neutropenia, thrombocytopenia, which may be accompanied by increased bleeding; very rarely - agranulocytosis and the development of severe infections (persistent or recurrent fever, worsening of well-being); in some cases, hemolytic anemia; pancytopenia.
Other: sometimes - general weakness; very rarely - fever.
Any antibiotic Levofloxacin therapy can cause changes in microflora, which is normally present in humans. For this reason, increased reproduction of bacteria and fungi that are resistant to the antibiotic used may occur, which in rare cases may require additional treatment.
Ways of application Levofloxacin:
The drug is taken orally 1 or 2 times a day. Do not chew the tablets and drink plenty of fluids (from 0.5 to 1 cup), you can take before meals or between meals. Doses are determined by the nature and severity of the infection, as well as the sensitivity of the putative pathogen.
