Levocin

Levocin is an antibacterial substance from the fluoroquinolone category.

Indications Levocin

It is used in cases of infectious lesions that have a different severity, which appeared due to the activity of microbial strains that are sensitive to levofloxacin:

• having an acute degree of sinusitis (this includes sinusitis);
• acute phase of bronchitis chronic course;
• home or hospital pneumonia ;
• urethral lesions, with or without complications (mild or mild stages).

[1]

Release form

The release of the component is implemented in tablet form - 10 pieces inside the plate. Pack 1 such plate in a pack.

[2], [3]

Pharmacodynamics

The fluoroquinolone antibiotic has a wide range of therapeutic effects. Contains the active element - levofloxacin (ofloxacin isomer of levorotatory type). This component blocks the activity of DNA gyrase, destroys the processes of stitching microbial DNA breaks and supercoiling, and also slows down DNA binding and leads to the development of strong morphological changes in the areas of membranes, cell walls and cytoplasm.

Shows the activity of a relatively large number of microbial strains:

• Gram (+) aerobes: enterococci (fecal among them), staphylococci (sensitive to methicaciuses and cohulase-negative), diphtheria corynebacterium, streptococcus agalactia, listeria monocytogenes with golden forms of staphylococci (sensitive to methicillin, and lycillin lycillins, which are sensitive to those with methicillin, which are sensitive to methicillins, which are sensitive to methicillins, which are sensitive to methicillins; ) and coagulase-negative staphylococcus. In addition, the list includes pyogenic streptococci, streptococci from subcategories C and G, as well as Streptococcus viridans with pneumococci (the last two are resistant, have moderate sensitivity and are influenced by penicillin);
• Gram (A): Arobe Ducrey. In addition, the list of moraccella cataris (producing β-lactamase or not), hemophilic sticks (sensitive or resistant against ampicillin), Haemophilus parainfluenzae, Klebsiella (among those of pneumonia and oxytoc), protei vulgaris and mirabilis, salmonella, cattle races, chromosolla, parasiticus, parasites, chromsyella (ophthalmic) and sensitive to the effects of penicillin), Providence (Rettgera and Stewart), meningococci with pasteurella (multocycid, canis and dagmatis), as well as serration (among them marzescense) and pseudomonads (among them blue-pied sticks);
• anaerobic bacteria: clostridia perfringens and propionibacteria with bacteroids fragilis, peptostreptokokki with bifidobacteria and fuzobakterii with veillonellas;
• other bacteria: legionella (among them pneumophilus), Bartonella spp., chlamydophilus pneumonia with chlamydophilia psittaci and Chlamydia trachomatis, and besides this mycoplasma pneumonia, mycobacteria (among them Hansen bacilli and Koch sticks), rickettsia, and there is a need;

[4]

Pharmacokinetics

Absorption.

Levofloxacin taken orally at high speed and almost 100% absorbed. Eating almost no effect on the severity and rate of absorption. The level of absolute bioavailability is approximately 100%. When 1-time use of drugs in a dose of 0.5 g, the values of Cmax are 5.2-6.9 μg / ml; determined after 1.3 hours.

Distribution processes.

Intlasma protein synthesis - 30-40%.

The substance is distributed within many tissues with organs: bone tissue, lungs, bronchial mucosa with sputum, cerebrospinal fluid, leukocytes, as well as the prostate and organs of the urogenital system with alveolar macrophages.

Exchange processes and excretion.

Inside the liver, a small part of the drug is deacetylated or oxidized.

Excretion proceeds mainly through the kidneys - the processes of filtration of the glomeruli and the secretion of tubules. About 87% of the oral dose taken is excreted unchanged along with urine (after 48 hours), and less than 4% with feces (after 72 hours). Plasma half-life of levofloxacin is 6-8 hours.

[5], [6]

Dosing and administration

The dosage of the drug is selected, taking into account the severity of the lesion and the nature of its occurrence, and at the same time the sensitivity of the pathogen.

Apply the drug is required before eating or between meals. Chew tablets should not be - they are swallowed, washed down with plain water (0.5-1 glass).

During sinusitis, 0.5 g of the drug is consumed 1 time a day (the treatment cycle lasts 10-14 days).

The exacerbated phase of chronic bronchitis is treated by taking 0.5 g of the drug 1 time per day (1 week course).

Hospital and home pneumonia is required to be treated by applying 0.5 g of Levocin 1-fold per day over a 1-2-week period.

Uncomplicated lesions of the urinary system are treated by injecting 0.5 g of the substance one time per day (3-day period). The same portion with a similar frequency should be consumed if the infection has complications, but such a cycle should last 10 days.

The lesions of the subcutaneous tissue with the epidermis occurring without complications eliminate with 1-fold daily intake of 0.5 g of the drug over a period of 7-10 days. If this disease is accompanied by complications, a dosage of 0.5 g is used 2 times a day, and the cycle lasts 1-2 weeks.

If necessary, the portion may increase, taking into account the severity of manifestations and the type of pathological lesion.

The maximum allowed size of 1-fold dosage is 0.5 g. Per day, no more than 1000 mg of the substance can be taken.

Portions of doses in patients with renal impairment:

• QC values in the range of 50-20 ml / minute - after the 1st dose of 0.5 g per day, the patient is transferred to receive 0.25 g per day; after the 1st dose of 0.75 g per day, then take 0.75 g for 48 hours;
• the level of QC in the range of 19-10 ml / minute - after the 1st daily portion of 0.25 g, 0.25 g is then used in 48 hours; at the 1st day portion of 0.5 g - 0.25 g for 48 hours; at the 1st daily portion of 0.75 g - 0.5 g for 48 hours;
• KK values <10 ml / min (this also includes CAPD and hemodialysis) - the first portion of 0.25 g per 24 hours, and then 0.25 g per 48 hours; The first portion of 0.5 g per day - further by 0.25 g for 48 hours; The first dosage of 0.75 g per day - later, at 0.5 g per 48 hours.

Use Levocin during pregnancy

Levocin should not be given to pregnant or lactating women.

Contraindications

Main contraindications:

• epileptic seizures;
• severe intolerance associated with elements of the drug or other quinolones.

[7],

Side effects Levocin

Among the observed side effects:

• lesions of the digestive activity: diarrhea or nausea often occurs, and the enzyme activity inside the liver and blood serum also increases. Vomiting, indigestion, loss of appetite and pain in the abdominal area can sometimes be observed. Occasionally, an increase in serum levels of bilirubin and bloody diarrhea is recorded. Hepatitis or enterocolitis appears singly (among them, pseudomembranous colitis);
• allergy symptoms: sometimes skin flushing or itching. Occasionally, anaphylactoid or anaphylactic manifestations are observed (with bronchial spasm, urticaria, or severe suffocation). Puffiness on the mucous membranes or epidermis (for example, facial or pharyngeal), intolerance to sunlight and UV radiation and pneumonitis of an allergic nature appear singularly, and the level of blood pressure and subsequent shock sharply decreases. Development of TEN, SSD, a vasculitis or MEE is possible;
• disorders of the central nervous system: sometimes there are sleep disorders, dizziness, a feeling of severe sleepiness and headaches. The feeling of psychomotor agitation, anxiety, anxiety or confusion, as well as depression, tremor, psychotic symptoms, convulsive syndrome and paresthesias affecting the hands, are rarely noted;
• disorders of the sense organs function: gustatory and olfactory disorders, auditory and visual disorders appear individually, and besides, tactile sensitivity is weakened;
• lesions of the hematopoietic system: leukopenia or eosinophilia sometimes occurs. Neutro-or thrombocytopenia rarely develops (sometimes bleeding increases). Agranulocytosis spontaneously appears or infections of a severe nature develop (recurrent or sustained increase in temperature, deterioration of health). Pancytopenia or anemia of hemolytic nature may occur;
• problems with the activity of the cardiovascular system: occasionally low blood pressure or heartbeat disorders occur. Possible prolongation of the QT-interval or vascular collapse;
• dysfunction of muscles and bones: occasionally affects the tendons (for example, tendonitis) and pain in the area of the joints with muscles. The tendon rupture, for example, Achilles (a similar symptom develops within 48 hours from the start of therapy and may be bilateral) or muscle weakness, which is extremely important for people with bulbar paralysis, are rarely noted. Possible development of muscle damage (rhabdomyolysis);
• urinary function disorders: serum creatinine increases occasionally. The case of OPN (tubulointerstitial nephritis) is rarely observed;
• manifestations in the endocrine system: hypoglycemia appears alone (diabetics should be taken into account), accompanied by such signs as a feeling of nervousness, shivering with sweat and a very strong appetite;
• others: sometimes asthenia develops. A feverish state, a superinfection or infection of a secondary nature, is sporadic.

[8]

Overdose

Drug poisoning leads to dizziness or seizures, confusion or disorder of consciousness, and also vomiting, erosion of mucous membranes and nausea.

Symptomatic procedures are performed. The drug has no antidote and is not excreted during dialysis.

[9], [10]

Interactions with other drugs

The effectiveness of levofloxacin is significantly reduced when combined with antacids such as Mg- and Al-containing, sucralfate and Fe drugs, therefore between their uses a minimum 120-minute interval should be observed.

A slight decrease in renal clearance of drugs is noted in the case of a combination with probenecid or cimetidine (almost does not have clinical value, but it is necessary to use this combination with caution, especially in people with renal disorders).

Probenecid with cimetidine increase the half-life and AUC values of the drug, and also reduce its clearance indicators (but you do not need to adjust the portion when they are combined).

Taking it with the medicine does not significantly increase the half-life of cyclosporine.

There is evidence of a noticeable decrease in the convulsive threshold with a combination of quinolones with agents that weaken this threshold. This also applies to the combined use of quinolone with theophylline and fenbufen or similar NSAIDs.

The combined use of the drug with theophylline requires careful monitoring of the values of the latter and a corresponding change in portion, in order to prevent the appearance of side symptoms (for example, seizures).

The use of indirect effects together with anticoagulants requires careful monitoring of the PTV indices and other coagulation data, and at the same time tracking possible bleeding symptoms.

The combination with Levocin can potentiate the effects of warfarin; in this case, an increase in the PTV level may be supplemented by the appearance of bleeding.

The combination of drugs with NSAIDs increases the likelihood of stimulating the activity of the central nervous system and the development of seizures.

In diabetics who ingest antidiabetic drugs or insulin, administration of the drug may lead to hyper- or hypoglycemic conditions (it is necessary to closely monitor the blood sugar values).

Combining the drug with the SCS increases the likelihood of tendon rupture.

[11], [12]

Storage conditions

Levocin is kept in a child-free, dark and dry place. Temperature range - within the limits of 15-30 ° C.

[13],

Shelf life

Levocin is allowed to use within a 5-year term from the time the therapeutic agent is manufactured.

Application for children

Not used in pediatrics (category under 18 years of age).

[14], [15]

Analogs

Analogues of the substance are drugs such as Alevo, Levozin with Levomak, Glevo and Levoxin, and in addition Levobact with Levolet.