Levofloxin

Levoflocin is an antibacterial agent used in systemic therapy.

[1], [2], [3], [4]

Indications Levofloxin

It is used in patients with moderate and, in addition, light stage infections caused by the activity of bacteria, marked by sensitivity to levofloxacin:

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

[5], [6], [7], [8], [9], [10]

Release form

Release of the substance produced in tablet form; The plate contains 5 pieces. Inside a separate box - 1 packing plate.

[11], [12]

Pharmacodynamics

The drug has a large 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 bulk structure of bacterial DNA and blocking the processes of their division.

Among the microbes that are influenced by levofloxacin:

• aerobic Gram (+): pyogenic streptococci, fecal shape enterococci, gold forms staphylococci methy-S, and together with this saprophytic staphylococci with hemolytic staphylococci methy-S, streptococcus type agalactia with streptococci C and G subgroups and pneumococci peni-I / S / R;
• aerobic Gram (-): tsitrobakter Freund, Enterobacter cloaca akinetobakterii Baumann, coliform bacteria with Eikenella corrodens, and furthermore Klebsiella oxytoca, Haemophilus ampi-S / R, Klebsiella pneumoniae and Enterobacter agglomerans with bacteria Morgan. The list also includes Haemophilus parainfluenze, Proteus Mirabilis, Stuart Providences, Moraksella Cataralys b + / b-, Retger's Providences, Vulgar Proteas with Multhotside Pasteurella and Serrations of Marzescense with Blue-Potential Chopsticks;
• anaerobic bacteria: clostridia perfringens with fragilis bacteroids and peptostreptokokki;
• other: legionella pneumophilus, chlamydophilia pneumonia, and mycoplasma pneumonia with chlamydophilia psittaci.

Irregular sensitivity regarding the effects of drugs have:

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

Relatively resistant Levoflotsina possess aerobic Gram (+): S.aureus methy-R.

[13], [14], [15], [16], [17]

Pharmacokinetics

Levoflotsin is absorbed at high speed and practically 100% inside the gastrointestinal tract with plasma Cmax indices, noted after the expiration of the 1st hour from the moment of using the drug. Values of absolute bioavailability of a substance are almost 100%. Registered linear pharmacokinetics with a dosage range of 50-600 mg. Eating has a weak effect on drug absorption.

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

When serving more than 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 time of use). In the liquor drug penetrates poorly.

The average indices of drugs inside the urine for 8–12 hours from the moment of 1 single dose of 0.15, 0.3, and 0.5 g of the portions are, respectively, 44th, 91st, and 200 μg / ml.

The exchange processes are practically not exposed; metabolic products make up less than 5% of the volume of medication excreted in urine.

Excretion from plasma occurs at a rather low speed (the half-life of the component varies in the range of 6-8 hours). 85% excreted by the kidneys.

[18], [19]

Dosing and administration

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

Levoflocin is consumed at least 2 hours before or after the use of drugs that contain Fe salts, as well as sucralfate and antacids, because they can reduce the absorption of the drug. The size of the total portion is determined by the severity of the course and the form of the infection, and in addition the sensitivity of the causative organism with respect to levofloxacin.

Therapy should last a maximum of 2 weeks. Also, for another 48-72 hours after the temperature stabilizes, or since the destruction of the microbe (as confirmed by microbiological analyzes), it is required to continue the therapeutic course.

Dosage sizes for different diseases:

• acute stages of sinusitis - 1 daily administration of 0.5 g of the drug for 10-14 days;
• exacerbated stage of chronic bronchitis - 1-fold daily use of 0.25-0.5 g in the period of 7-10 days;
• home pneumonia - 1-2 times daily intake of 0.5 g of Levoflocin within 7-14 days;
• lesion of the urinary system (with complications) - 0.25 g of drug 1-fold per day within a 7-10-day period;
• skin lesions - 1-2 times a day use of 0.15-0.5 g of the drug, over a period of 1-2 weeks.

Persons with problems in the activity of the kidneys (the level of QC below 50 ml / minute) on the first day is required to take a full dose of drugs, and further reduce it, taking into account the indicators of QC. Patients from this group should be constantly supervised by a medical specialist.

[28], [29], [30], [31]

Use Levofloxin during pregnancy

It is forbidden to use during breastfeeding and pregnancy.

Contraindications

Main contraindications:

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

[20], [21], [22], [23]

Side effects Levofloxin

Among the emerging side signs:

• sometimes there is redness on the epidermis or itching. Occasionally, symptoms of severe intolerance with manifestations of urticaria or swelling of the epidermis and mucous membranes;
• tachycardia;
• signs of dyspepsia;
• drowsiness, marked dizziness or headaches;
• decrease in blood pressure;
• an increase in bilirubin values, as well as liver enzymes and serum creatinine;
• leuco-, thrombocyto-or neutropenia and eosinophilia;
• sense of systemic weakness;
• pronounced inflammation of the tendons or pain in the muscular-articular zone.

[24], [25], [26], [27]

Overdose

When intoxication with levoflotsinom often appear signs of damage to the central nervous system: severe dizziness, severe confusion, seizures, convulsions and disorder of consciousness.

Corresponding symptomatic measures are performed. The active element of drugs is not excreted by dialysis. Also, the drug does not have an antidote.

[32], [33]

Interactions with other drugs

The absorption of the drug is significantly weakened when it is combined with Al-or Mg-containing antacids, and in addition with the means, which include Fe salts.

The values of bioavailability of drugs significantly reduced with the combined administration with sucralfate. Therefore, at least a 120-minute interval should be observed between their injections.

With great care, Levoflocin is prescribed together with substances that affect the secretion of the kidneys (cimetidine or probenecid). This is especially true for people with renal impairment.

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

[34], [35]

Storage conditions

Levoflocin is required to keep in a closed place from small children. Temperatures - in the range of marks 15-25 ° C.

[36], [37], [38]

Shelf life

Levoflocin can be administered over a 3-year period from the time a pharmaceutical substance is released.

[39], [40]

Application for children

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

[41], [42], [43], [44], [45]

Analogs

Analogues of the drug are the means Ofloxacin, Tsiprolet, Glevo with Moflaksii, and in addition Ciprofloxacin, Levofloxacin and Rotomax.

[46], [47], [48], [49], [50], [51]