Leflox

Leflox belongs to the subgroup of antibacterial medicines from the category of fluoroquinolones with quinolones.

The therapeutic effect develops in connection with the effect of the active component of the drug - levofloxacin. It is an artificial antibacterial substance that is also the S-enantiometer of the ofloxacin racemic mixture. The drug also has an effect on topoisomerase 4 and DNA gyrase. [1]

The severity of the antibacterial effect is determined by the indicators of drugs inside the blood serum. [2]

There is a possibility of developing cross-resistance with other fluoroquinolones, while this is not observed with antibiotics from other categories. [3]

Indications Leflox

It is used for the treatment of inflammations, whose development is associated with the activity of microbes that are sensitive to levofloxacin. Among those:

• active phase of sinusitis ;
• exacerbation of chronic bronchitis;
• pneumonia (community or hospital);
• infections of the urethra, developing with or without complications (among them, cystitis of an uncomplicated nature and pyelonephritis);
• lesions of the subcutaneous layers and epidermis;
• chronic stage of prostatitis, which is of a bacterial nature.

Release form

The release of the therapeutic element is realized in the form of tablets - 10 pieces inside a blister pack or 5 pieces inside a jar (tablet volume - 0.25 g). Also, 10 pieces inside the packaging plate or 5 or 7 pieces inside the jar (tablet volume - 0.5 and 0.75 g).

Pharmacodynamics

Resistance to levofloxacin manifests itself in the phase of mutation of target sites within both type 2 topoisomerases, topoisomerase 4 and DNA gyrase. Sensitivity to levofloxacin also changes with the participation of other resistance mechanisms - for example, changes in the permeability of cell membranes (found in Pseudomonas aeruginosa), as well as efflux from the cell.

Pharmacokinetics

Absorption.

After oral administration, levofloxacin is practically fully absorbed and at high speed, reaching the plasma level Cmax in a period of 1-2 hours. Indicators of absolute bioavailability are approximately 99-100%. Eating food has little effect on the absorption of levofloxacin.

The substance reaches the saturation limits after 48 hours in the case of administration of 0.5 g of levofloxacin 1-2 times per day.

Distribution processes.

About 30-40% of the drug is synthesized with whey protein. The distribution values of drugs are on average 100 liters with 1-fold or multiple intravenous administration of 0.5 g of the substance. This indicates that levofloxacin passes well into organs with tissues.

It is known that the drug is determined inside the epithelial fluid, bronchial mucosa, lung tissue, alveolar macrophages, prostate tissue, epidermis (blisters), and urine, but it does not pass well into the cerebrospinal fluid.

Exchange processes.

Levofloxacin is weakly involved in metabolic processes; its metabolic components (among them desmethyl-levofloxacin with levofloxacin N-oxide) make up only <5% of the portion that is excreted in the urine.

The drug substance has stereochemical stability without undergoing chiral inversion processes.

Excretion.

With intravenous injections and oral administration, the drug is excreted from the blood plasma rather slowly (the half-life term is 6-8 hours). Excretion is mainly carried out by the kidneys (over 85% of the consumed dosage).

The systemic drug clearance with a single use of 0.5 g of levofloxacin is 175 ± 29.2 ml per minute.

Pharmacokinetic characteristics after intravenous injection and oral administration of drugs practically do not differ.

Pharmacokinetic parameters of drugs are linear with a dosage range of 50-1000 mg.

Dosing and administration

The medication is taken orally. The selection of the dosage portion is performed by the attending doctor, taking into account the severity of the pathology.

In the case of the active phase of sinusitis, 0.5 g of the drug is used once a day. The treatment cycle includes 10-14 days.

With an exacerbation of chronic bronchitis, use 1-fold, 0.25-0.5 g of medication per day; therapy lasts 7-10 days.

In the case of community-acquired pneumonia, 0.5-1 g of the substance is used 1-2 times per day. The duration of the course is 1-2 weeks.

During infections of the urethra (without complications), 0.25 g of the drug is administered 1 time per day. The cycle of therapy lasts 3 days.

In the chronic stage of prostatitis, which has a bacterial etiology, 0.5 g of the drug is administered 1 time per day. The treatment lasts 4 weeks.

In case of infections of the urinary system, proceeding with complications (for example, pyelonephritis), 0.25 g of the medication is taken once a day. The cycle duration is 7-10 days.

In case of infections of subcutaneous tissues and epidermis, 0.5-1 g of the drug is consumed 1-2 times per day. Treatment continues for 1-2 weeks.

In the case of renal dysfunction, the dosage portions of Leflox should be reduced.

Individuals with hepatic dysfunction and the elderly can be given standard doses of the medication.

The selection of the duration of the therapeutic cycle is made personally and is determined by the treating doctor.

• Application for children

You can not prescribe a medication in pediatrics (articular cartilage damage may develop).

Use Leflox during pregnancy

You can not use the medication during pregnancy.

For the period of therapy with Leflox, breastfeeding should be stopped.

Contraindications

The main contraindications:

• severe intolerance associated with the action of the constituent elements of the drug;
• epilepsy;
• a history of tendon lesions associated with the use of quinolones.

Side effects Leflox

Among the side symptoms:

• mycoses or candidiasis;
• myalgias with arthralgias, lesions of the articular cartilage tissues, tendinitis and damage in the ligamentous region (it can reach their ruptures);
• thrombocyto-, leuko- or pancytopenia, agranulocytosis and eosinophilia;
• anaphylaxis;
• hypoglycemia and anorexia;
• nervousness, agitation, insomnia, hallucinations and anxiety;
• tremor, dysgeusia, convulsions, anosmia and ageusia;
• ear ringing and vertigo;
• decrease in blood pressure, tachycardia and prolongation of the QT-interval;
• dyspnea, bronchial spasm and allergic pneumonitis;
• indigestion, nausea, diarrhea and vomiting;
• jaundice or hepatitis;
• Quincke's edema, itching, rashes and hyperhidrosis;
• pyrexia, asthenia and pain in the back, sternum and extremities;
• weakening of renal function, which can reach ARF (associated with tubulointerstitial nephritis);
• attacks of porphyria.

Overdose

Poisoning leads to the appearance of such symptoms: loss of consciousness, dizziness, prolongation of the QT interval and seizures.

In case of intoxication, it is required to monitor the patient's condition - first and foremost, the ECG readings. There is no antidote. The dialysis procedure does not have the desired effect. Symptomatic actions are performed.

Interactions with other drugs

There is evidence of an intense decrease in the seizure threshold when quinolones are used with drugs that lower the cerebral seizure threshold. This also applies to the combination of quinolones with theophylline, fenbufen or similar NSAIDs (substances used in the treatment of rheumatic diseases).

The effect of Leflox is greatly reduced when used in combination with sucralfate (substances that protect the gastric mucosa). The same effect develops when administered with aluminum or magnesium-containing antacids (medicines used for gastralgia or heartburn), and in addition with Fe salts (medicines used for anemia). The medication must be administered at least 2 hours before or after the administration of these drugs.

Administration with corticosteroids increases the likelihood of rupture in the tendon area.

The use in combination with K-vitamin antagonists requires monitoring of blood clotting function.

Intrarenal drug clearance rates are slightly slowed down under the influence of cimetidine (by 24%), as well as probenicide (by 34%). It should be borne in mind that such interaction is practically insignificant. But at the same time, in the case of the introduction of substances such as cimetidine with probenecid, which block one of the excretion pathways (excretion through the tubules), levofloxacin should be used very carefully. This mainly applies to people with renal problems.

The drug slightly prolongs the half-life of cyclosporine (up to 33%).

Levofloxacin, like other fluoroquinolones, must be used very carefully in people using medications that can prolong the QT-interval (including tricyclics, antipsychotics with macrolides and antiarrhythmic drugs from subclass 1a, as well as 3).

Storage conditions

Leflox must be kept out of the reach of small children and moisture penetration. Temperature level - no more than 25 ° С.

Shelf life

Leflox can be used within a 36-month period from the date of manufacture of the drug substance.

Analogs

The analogs of the medicine are the drugs Remedia, Leflobact with Tavanik, Glevo and Flexid with Lebel, and in addition Lefokcin and Levolet with Eleflox. Also on the list are Levofloxacin, Oftaquix and Haileflox.