Levocin

Levocin is an antibacterial substance from the fluoroquinolone category.

Indications Levocina

It is used for infectious lesions of varying severity that have appeared due to the activity of microbial strains sensitive to levofloxacin:

• acute sinusitis (this includes sinusitis);
• acute phase of chronic bronchitis;
• home or hospital pneumonia;
• lesions of the urinary organs, with or without complications (moderate or mild stages).

[ 1 ]

Release form

The component is released in tablet form - 10 pieces inside a plate. One such plate is packed in a pack.

[ 2 ], [ 3 ]

Pharmacodynamics

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

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

• gram(+) aerobes: enterococci (including faecal), staphylococci (methicillin-sensitive and coagulase-negative), diphtheria corynebacteria, Streptococcus agalactiae, Listeria monocytogenes with Staphylococcus aureus (methicillin-sensitive), Staphylococcus epidermidis (also susceptible to methicillin) and coagulase-negative Staphylococci. In addition, the list includes pyogenic streptococci, streptococci of subcategories C and G, as well as Streptococcus viridans with pneumococci (the last two are resistant, have moderate sensitivity and are susceptible to penicillin);
• Gram(-) aerobes: Acinetobacter (including Acinetobacter baumannii), Enterobacter (including Cloacae, Aerogenes and Agglomerans), Helicobacter pylori, Aggregatibacteria actinomycetemcomitans, Citrobacter freundii and Escherichia coli, as well as Eikenella corrodens, Morgan's bacteria, Gardnerella vaginalis and Ducrey's bacilli. In addition, the list includes Moraxella catarrhalis (producing β-lactamase or not), Haemophilus influenzae (sensitive or resistant to ampicillin), Haemophilus parainfluenzae, Klebsiella (including pneumonia and oxytoca), Proteus vulgaris and mirabilis, Salmonella and gonococci (resistant, weakly susceptible and sensitive to the influence of penicillin), Providencia (Rettger and Stuart), Meningococcus with Pasteurella (Multocida, Canis and Dagmatis), as well as Serratia (including Marciescens) and Pseudomonas (including Pseudomonas aeruginosa);
• anaerobes: Clostridia perfringens and Propionibacteria with Bacteroides fragilis, Peptostreptococci with Bifidobacteria and Fusobacteria with Veillonella;
• other bacteria: legionella (including pneumophila), Bartonella spp., chlamydophila pneumoniae with chlamydophila psittaci and Chlamydia trachomatis, as well as mycoplasma pneumoniae, mycobacteria (including Hansen's bacillus and Koch's bacillus), rickettsia, mycoplasma hominis and ureaplasma urealyticum.

[ 4 ]

Pharmacokinetics

Absorption.

Levofloxacin taken orally is absorbed at a high rate and almost 100%. Food intake has almost no effect on the expression and rate of absorption. The level of absolute bioavailability is approximately 100%. With a single use of the drug in a portion of 0.5 g, the Cmax values are 5.2-6.9 mcg / ml; determined after 1.3 hours.

Distribution processes.

Intraplasmic protein synthesis – 30-40%.

The substance is distributed within many tissues and 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.

Metabolic processes and excretion.

Within the liver, a small portion of the drug is deacetylated or oxidized.

Excretion occurs primarily through the kidneys – glomerular filtration and tubular secretion processes. About 87% of the orally administered dose is excreted unchanged in the urine (after 48 hours), and less than 4% in the feces (after 72 hours). The plasma half-life of levofloxacin is 6-8 hours.

[ 5 ], [ 6 ]

Dosing and administration

The dosage of the medication is selected taking into account the severity of the lesion and the nature of its progression, as well as the sensitivity of the pathogenic microbe.

The medicine should be taken before or between meals. The tablets should not be chewed – they should be swallowed with plain water (0.5-1 glass).

During sinusitis, 0.5 g of the drug is taken once a day (the therapy cycle lasts 10-14 days).

The acute phase of chronic bronchitis is treated by taking 0.5 g of the medicine once a day (1-week course).

Hospital and home pneumonia should be treated with 0.5 g of Levocin once a day for a 1-2 week period.

Uncomplicated urinary tract infections are treated by administering 0.5 g of the substance once a day (3-day period). The same dose should be taken with the same frequency if the infection has complications, but such a cycle should last 10 days.

Uncomplicated lesions of the subcutaneous tissue with the epidermis are eliminated by taking 0.5 g of the drug once daily for 7-10 days. If such a disease is accompanied by complications, the dosage of 0.5 g is used 2 times a day, and the cycle itself lasts 1-2 weeks.

If necessary, the dose can be increased, taking into account the severity of the symptoms and the type of pathological lesion.

The maximum permitted size of a single dosage is 0.5 g. No more than 1000 mg of the substance can be taken per day.

Portion dose sizes for individuals with renal impairment:

• CC values within 50-20 ml/minute - after the 1st dose of 0.5 g per day, the patient is transferred to taking 0.25 g per day; after the 1st dose of 0.75 g per day, then take 0.75 g every 48 hours;
• the level of CC within 19-10 ml/minute - after the 1st daily portion of 0.25 g, 0.25 g is then used for 48 hours; with the 1st daily portion of 0.5 g - 0.25 g for 48 hours; with the 1st daily portion of 0.75 g - 0.5 g for 48 hours;
• CC values <10 ml/minute (this also includes CAPD and hemodialysis) – 1st portion 0.25 g over 24 hours, then 0.25 g over 48 hours; 1st portion 0.5 g per day – then 0.25 g over 48 hours; 1st dose 0.75 g per day – later 0.5 g over 48 hours.

Use Levocina during pregnancy

Levocin should not be prescribed to pregnant or breastfeeding women.

Contraindications

Main contraindications:

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

[ 7 ]

Side effects Levocina

Among the observed side effects are:

• digestive disorders: diarrhea or nausea often appear, and enzyme activity in the liver and blood serum increases. Vomiting, indigestion, loss of appetite and abdominal pain may sometimes occur. Increased serum bilirubin levels and bloody diarrhea are occasionally recorded. Hepatitis or enterocolitis (including pseudomembranous colitis) may appear occasionally;
• allergy symptoms: sometimes skin hyperemia or itching occurs. Rarely, anaphylactoid or anaphylactic manifestations are observed (with bronchial spasm, urticaria or severe suffocation). Occasionally, swelling of the mucous membranes or epidermis (for example, facial or pharyngeal), intolerance to sunlight and UV radiation and allergic pneumonitis appear, and blood pressure levels drop sharply with subsequent shock. Development of TEN, SJS, vasculitis or MEE is possible;
• CNS disorders: sometimes sleep disorders occur, dizziness, a feeling of intense drowsiness and headaches appear. Occasionally, a feeling of psychomotor agitation, restlessness, anxiety or confusion is noted, as well as depression, tremor, psychotic symptoms, convulsive syndrome and paresthesia affecting the hands;
• disorders of the sensory organs: taste and smell disorders, auditory and visual disorders appear sporadically, and in addition, tactile sensitivity is weakened;
• damage to the hematopoietic system: sometimes leukopenia or eosinophilia occurs. Occasionally, neutro- or thrombocytopenia develops (at times, bleeding increases). Agranulocytosis appears sporadically or severe infections develop (recurrent or persistent increase in temperature, deterioration in health). Pancytopenia or hemolytic anemia may occur;
• problems with the cardiovascular system: blood pressure occasionally decreases or heart palpitations occur. Prolongation of the QT interval or vascular collapse is possible;
• muscle and bone dysfunction: tendons are occasionally affected (for example, tendinitis) and pain appears in the area of the joints with muscles. A rupture of a tendon is noted sporadically, for example, the Achilles tendon (a similar symptom develops within 48 hours from the start of therapy and can be bilateral) or muscle weakness, which is extremely important for people with bulbar palsy. Muscle damage (rhabdomyolysis) may develop;
• urinary dysfunction: serum creatinine levels occasionally increase. ARF (tubulointerstitial nephritis) is observed sporadically;
• manifestations in the endocrine system: hypoglycemia appears sporadically (this should be taken into account by diabetics), accompanied by such symptoms as a feeling of nervousness, trembling with sweating and a very strong appetite;
• Others: sometimes asthenia develops. Feverish condition, superinfection or secondary infection occur sporadically.

[ 8 ]

Overdose

Poisoning with the drug leads to dizziness or convulsions, confusion or impaired consciousness, as well as vomiting, erosions on the mucous membranes and nausea.

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

[ 9 ], [ 10 ]

Interactions with other drugs

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

A slight decrease in renal clearance of the drug is observed in the case of combination with probenecid or cimetidine (it has almost no clinical significance, but such a combination should be used with caution, especially in individuals with renal disorders).

Probenecid with cimetidine increases the half-life and AUC values of the drug, and also reduces its clearance rates (but there is no need to adjust the dose when combining them).

Taking the drug together does not significantly increase the half-life of cyclosporine.

There is evidence of a significant decrease in the seizure threshold when quinolones are combined with agents that weaken this threshold. This also applies to the combined use of quinolones with theophylline and fenbufen or similar NSAIDs.

The concomitant use of the drug with theophylline requires careful monitoring of the latter's values and appropriate dose adjustments to prevent the occurrence of adverse effects (eg, seizures).

Use with indirect anticoagulants requires careful monitoring of PT and other coagulation data, as well as monitoring for possible bleeding symptoms.

The combination with Levocin may potentiate the effect of warfarin; in this case, the increase in the level of PTT may be accompanied by the occurrence of bleeding.

The combination of the drug with NSAIDs increases the likelihood of stimulation of the central nervous system and the development of seizures.

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

Combining the drug with GCS increases the risk of tendon rupture.

[ 11 ], [ 12 ]

Storage conditions

Levocin is stored in a dark and dry place, out of reach of children. The temperature range is within 15-30°C.

[ 13 ]

Shelf life

Levocin is allowed to be used within a 5-year period from the date of production of the therapeutic agent.

Application for children

Not for use in pediatrics (under 18 years of age).

[ 14 ], [ 15 ]

Analogues

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