Levoflocin

Levofloxacin is an antibacterial agent used in systemic therapy.

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Indications Levoflocin

It is used for moderate and even mild infections caused by bacteria that are sensitive to levofloxacin:

• aggravated sinusitis;
• chronic bronchitis that is in the form of an exacerbation;
• outpatient pneumonia;
• lesions of the urinary system, occurring with complications (this also includes pyelonephritis);
• lesions affecting the subcutaneous area and epidermis.

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Release form

The substance is released in tablet form; a plate contains 5 pieces. Inside a separate box there is 1 packaging plate.

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Pharmacodynamics

The drug has a wide spectrum of antibacterial activity. The high rate of development of bactericidal properties is ensured by the suppression of the activity of the bacterial enzyme inside DNA gyrase, which is part of the structure of topoisomerase-2. The result of this is the destruction of the volumetric structure of bacterial DNA and the blocking of their division processes.

Among the microbes that are susceptible to the influence of levofloxacin:

• aerobes gram(+): pyogenic streptococci, faecal forms of enterococci, golden forms of staphylococci methy-S, and along with these saprophytic staphylococci with hemolytic staphylococci methy-S, agalactiae type streptococci with streptococci of subgroups C and G and pneumococci peni-I/S/R;
• Gram(-) aerobes: Citrobacter freundii, Enterobacter cloacae, Acinetobacter baumannii, Escherichia coli with Eikenella corrodens, as well as Klebsiella oxytoca, Haemophilus influenzae ampi-S/R, Klebsiella pneumoniae with Enterobacter agglomerans and Morgan's bacilli. The list also includes Haemophilus parainfluenzae, Proteus mirabilis, Providencia stuartii, Moraxella catarrhalis b+/b-, Providencia rettgerii, Proteus vulgaris with Pasteurella multocida and Serratia marcescens with Pseudomonas aeruginosa;
• anaerobes: Clostridia perfringens with Bacteroides fragilis and Peptostreptococci;
• Others: Legionella pneumophila, Chlamydophila pneumoniae and Mycoplasma pneumoniae with Chlamydophila psittaci.

The following have irregular sensitivity to the influence of the drug:

• aerobes gram(+): hemolytic staphylococci methy-R;
• aerobes gram(-): Bukholderia cepacia;
• anaerobes: bacteria thetayotomicron with Bacteroides ovatus, Clostridium difficile together with Bacteroides vulgaris.

Aerobes Gram(+) are resistant to Levofloxacin: Staphylococcus aureus methy-R.

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Pharmacokinetics

Levofloxacin is absorbed at high speed and almost 100% in the gastrointestinal tract with plasma Cmax values observed after 1 hour from the moment of drug use. The absolute bioavailability values of the substance are almost 100%. Linear pharmacokinetics are recorded in the dosage range of 50-600 mg. Food intake has a weak effect on drug absorption.

Approximately 30-40% of the drug is synthesized with whey protein. The accumulation of the substance at a daily 1-time portion dosage of 0.5 g does not lead to the development of significant clinical effects. Insignificant, but predictable accumulation of the drug occurs with 2-times daily use of a portion of 0.5 g. Stable distribution values are noted after 3 days.

For doses over 0.5 g, the Cmax values of the drug inside the bronchial mucosa together with the epithelial secretion of the bronchi are 8.3 and 10.8 μg/ml, respectively; the values inside the lung tissue are approximately 11.3 μg/ml (determined after 4-6 hours from the moment of administration). The drug penetrates poorly into the cerebrospinal fluid.

The average values of the drug in urine over 8-12 hours from the moment of a single dose of 0.15, 0.3 and 0.5 g are equal to 44, 91 and 200 mcg/ml, respectively.

It is practically not subject to metabolic processes; metabolic products make up less than 5% of the volume of the drug excreted in the urine.

Excretion from plasma occurs at a fairly low rate (the half-life of the component ranges from 6 to 8 hours). 85% is excreted by the kidneys.

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Dosing and administration

Daily use of the drug should be carried out in 1-2 applications, not tying them to the meals. The medicine is swallowed without chewing and washed down with plain water.

Levofloxacin is taken at least 2 hours before or after taking medications that contain Fe salts, as well as sucralfate and antacids, because they can reduce the absorption of the drug. The size of the total dose is determined by the severity of the course and the form of the infection that has arisen, as well as the sensitivity of the pathogen to levofloxacin.

The therapy should last a maximum of 2 weeks. Also, for another 48-72 hours from the moment the temperature stabilizes or from the moment the microbe is destroyed (which is confirmed by microbiological analysis), the therapeutic course must be continued.

Dosage sizes for different diseases:

• acute stages of sinusitis – 1-time daily administration of 0.5 g of the medication for 10-14 days;
• exacerbation of chronic bronchitis - 1-time daily use of 0.25-0.5 g for a period of 7-10 days;
• home pneumonia – 1-2 times daily intake of 0.5 g Levofloxacin within 7-14 days;
• damage to the urinary system (with complications) - 0.25 g of the drug once a day within a 7-10-day period;
• skin lesions – 1-2 times use of 0.15-0.5 g of the drug, over a period of 1-2 weeks.

People with kidney problems (CC level below 50 ml/min) should take the full dose of the drug on the first day, and then reduce it, taking into account the CC indicators. Patients from this group should be constantly monitored by a medical specialist.

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Use Levoflocin during pregnancy

It is prohibited to use during breastfeeding and pregnancy.

Contraindications

Main contraindications:

• severe intolerance to drugs from this subcategory;
• epilepsy;
• if there are complaints of negative manifestations developing in the tendon area and associated with the use of quinolones.

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Side effects Levoflocin

Among the side effects that arise are:

• sometimes redness of the epidermis or itching appears. Occasionally, symptoms of severe intolerance with manifestations of urticaria or swelling of the epidermis and mucous membranes are noted;
• tachycardia;
• signs of dyspepsia;
• feeling drowsy, severe dizziness or headaches;
• decrease in blood pressure;
• an increase in bilirubin levels, and along with them liver enzymes and serum creatinine;
• leuko-, thrombocyto- or neutropenia and eosinophilia;
• feeling of systemic weakness;
• severe inflammation or pain in the muscular-articular area affecting the tendons.

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Overdose

In case of intoxication with Levofloxacin, signs of damage to the central nervous system often occur: severe dizziness, severe confusion, seizures and impaired consciousness.

The corresponding symptomatic measures are carried out. The active element of the drug is not excreted by dialysis. Also, the drug has no antidote.

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Interactions with other drugs

The absorption of the drug is significantly weakened when combined with Al- or Mg-containing antacids, as well as with products containing Fe salts.

The bioavailability values of the drug are significantly reduced when administered in combination with sucralfate. Therefore, a minimum 120-minute interval should be observed between their administrations.

Levofloxacin is prescribed with great caution together with substances that affect kidney secretion (cimetidine or probenecid). This is especially true for people with kidney disorders.

The half-life of the cyclosporine component increases by 33% when combined with levofloxacin.

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Storage conditions

Levofloxacin should be stored in a place closed to small children. Temperature values are in the range of 15-25°C.

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Shelf life

Levofloxacin can be prescribed for a period of 3 years from the date of release of the pharmaceutical substance.

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Application for children

Not prescribed in pediatrics (under 18 years of age).

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Analogues

The drug's analogues are Ofloxacin, Ciprolet, Glevo with Moflaxia, as well as Ciprofloxacin, Levofloxacin and Rotomax.

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