Leflox

Lefloxacin belongs to a subgroup of antibacterial drugs from the category of fluoroquinolones with quinolones.

The therapeutic effect is developed due to the effect exerted by the active component of the drug – levofloxacin. This is an artificial antibacterial substance, which is also the S-enantiometer of the racemic mixture of ofloxacin. The drug also has an effect on topoisomerase 4 and DNA gyrase. [ 1 ]

The severity of the antibacterial effect is determined by the drug levels in the blood serum. [ 2 ]

There is a potential for cross-resistance with other fluoroquinolones, but no cross-resistance has been observed with antibiotics from other categories. [ 3 ]

Indications Leflox

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

• active phase of sinusitis;
• exacerbation of chronic bronchitis;
• pneumonia (community-acquired or hospital-acquired);
• infections of the urethra, developing with or without complications (including uncomplicated cystitis and pyelonephritis);
• lesions of the subcutaneous layers and epidermis;
• chronic stage of prostatitis of bacterial origin.

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 a packaging plate or 5 or 7 pieces inside a jar (tablet volume - 0.5 and 0.75 g).

Pharmacodynamics

Resistance to levofloxacin is manifested by phased mutation of target sites within both type 2 topoisomerases, topoisomerase 4, and DNA gyrase. Sensitivity to levofloxacin is also altered by other resistance mechanisms, such as changes in cell membrane permeability (found in Pseudomonas aeruginosa) and cellular efflux.

Pharmacokinetics

Absorption.

After oral administration, levofloxacin is almost completely and rapidly absorbed, reaching plasma levels of Cmax within 1-2 hours. Absolute bioavailability is approximately 99-100%. Food intake has little effect on the absorption of levofloxacin.

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

Distribution processes.

Approximately 30-40% of the drug is synthesized with whey protein. The distribution values of the drug are on average 100 l with a single or multiple intravenous administration of 0.5 g of the substance. This indicates that levofloxacin passes well into organs and tissues.

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

Exchange processes.

Levofloxacin is poorly metabolized; its metabolic components (including desmethyl levofloxacin and levofloxacin N-oxide) account for only <5% of the portion excreted in urine.

The medicinal substance has stereochemical stability and is not subject to chiral inversion processes.

Excretion.

When administered intravenously or orally, the drug is excreted from the blood plasma rather slowly (the half-life is 6-8 hours). Excretion is mostly carried out by the kidneys (over 85% of the dose taken).

The systemic clearance of the drug after 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 the drug are practically the same.

The pharmacokinetic parameters of the drug are linear over a dosage range of 50-1000 mg.

Dosing and administration

The medication is taken orally. The dosage portion is selected by the attending physician, taking into account the severity of the pathology.

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

In case of exacerbation of chronic bronchitis, 0.25-0.5 g of the medication is taken once a day; therapy continues for 7-10 days.

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

During urinary tract infections (without complications), 0.25 g of the drug is administered once a day. The therapy cycle lasts 3 days.

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

In case of urinary tract infections 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 subcutaneous tissue and epidermis infections, 0.5-1 g of the medicine is taken 1-2 times per day. Treatment continues for 1-2 weeks.

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

Persons with liver dysfunction and the elderly can be prescribed standard doses of the medication.

The duration of the therapeutic cycle is selected individually and is determined by the attending physician.

• Application for children

The medication cannot be prescribed in pediatrics (damage to articular cartilage may develop).

Use Leflox during pregnancy

The medication should not be used during pregnancy.

Breastfeeding should be discontinued during treatment with Lefloxacin.

Contraindications

Main contraindications:

• severe intolerance associated with the action of the constituent elements of the drug;
• epilepsy;
• history of tendon injury associated with quinolone use.

Side effects Leflox

Side effects include:

• mycosis or candidiasis;
• myalgia with arthralgia, damage to articular cartilage tissue, tendinitis and damage to the ligaments (may even lead to ruptures);
• thrombocyto-, leuko- or pancytopenia, agranulocytosis and eosinophilia;
• anaphylaxis;
• hypoglycemia and anorexia;
• nervousness, agitation, insomnia, hallucinations and anxiety;
• tremor, dysgeusia, seizures, anosmia and ageusia;
• tinnitus and vertigo;
• decreased blood pressure, tachycardia and prolongation of the QT interval;
• dyspnea, bronchial spasm and allergic pneumonitis;
• dyspepsia, nausea, diarrhea and vomiting;
• jaundice or hepatitis;
• Quincke's edema, itching, rashes and hyperhidrosis;
• pyrexia, asthenia and pain in the back, sternum and limbs;
• weakening of renal function, which may lead to acute renal failure (associated with tubulointerstitial nephritis);
• attacks of porphyria.

Overdose

Poisoning results in the following symptoms: loss of consciousness, dizziness, prolongation of the QT interval and seizures.

In case of intoxication, it is necessary to monitor the patient's condition - primarily 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 information about the intensive reduction of the seizure threshold when using quinolones with drugs that reduce 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 Lefloxacin is greatly reduced when used in combination with sucralfate (a substance that protects the gastric mucosa). The same effect occurs when administered with aluminum- or magnesium-containing antacids (medicines used for gastralgia or heartburn), and also with Fe salts (medicines used for anemia). The medication should be administered at least 2 hours before or after the administration of these drugs.

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

Use in combination with vitamin K antagonists requires monitoring of blood coagulation function.

Intrarenal drug clearance rates are slightly slowed down by cimetidine (by 24%) and probenecid (by 34%). It should be taken into account that such interactions are practically insignificant. However, in the case of administration of substances such as cimetidine with probenecid, which block one of the excretion pathways (excretion through the tubules), levofloxacin should be used with great caution. This mainly applies to people with problems in renal function.

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

Levofloxacin, like other fluoroquinolones, should be used with extreme caution in people taking medications that can prolong the QT interval (including tricyclics, macrolide antipsychotics, and antiarrhythmic drugs from subclasses 1a and 3).

Storage conditions

Leflox should be stored in a place closed to small children and moisture penetration. Temperature level – no more than 25°С.

Shelf life

Leflox can be used within 36 months from the date of manufacture of the medicinal substance.

Analogues

Analogues of the drug are Remedia, Leflobact with Tavanic, Glevo and Flexid with Lebel, and also Lefoxin and Levolet with Eleflox. Also on the list are Levofloxacin, Oftaquix and Haileflox.