The value of levofloxacin for respiratory and urogenital infections in outpatient practice


Contraindications and indications for taking Levofloxacin

The instructions for use of the tablets indicate the following indications:

  • acute forms of sinusitis;
  • infectious lesions of the genitourinary tract without complications;
  • gastrointestinal infections;
  • chronic bronchitis in the acute stage;
  • community-acquired pneumonia;
  • infection of soft tissues and dermis;
  • infection of the urinary ducts with complications;
  • bacterial infection of the blood.

Solutions are used to treat pathologies of the skin, respiratory and urinary tract, and genital organs. Eye drops are prescribed for superficial bacterial diseases of the organs of vision.

Levofloxacin is not used:

  • for minors;
  • people with allergies to the component composition;
  • patients with renal failure, epilepsy;
  • during pregnancy, breastfeeding and tendon damage during treatment with quinolones.

Particular caution is required when prescribing medication to elderly people with a deficiency of G6PD.

The value of levofloxacin for respiratory and urogenital infections in outpatient practice

The first fluoroquinolone drugs appeared in clinical practice in the early 1980s. They were characterized by a wide spectrum of antimicrobial activity and favorable tissue pharmacokinetics (concentrations in most tissues exceeded serum levels). The unique mechanism of action of fluoroquinolones on microbial cells (inhibition of DNA gyrase or topoisomerase IV) explained the lack of cross-resistance with other classes of antimicrobial agents.

The most well-studied early fluoroquinolones are ciprofloxacin and ofloxacin. Fluoroquinolones have taken leading positions in the treatment of various bacterial infections, primarily nosocomial ones, the main pathogens of which are gram-negative bacteria.

The disadvantage of early fluoroquinolones is their low natural activity against gram-positive microorganisms, primarily Streptococcus pneumoniae, which did not allow these drugs to be recommended for the treatment of community-acquired respiratory infections.

At the end of the 1990s. drugs of the fluoroquinolone group appeared, fundamentally different in antimicrobial properties from earlier drugs. These differences are, first of all, characterized by significantly higher natural activity against gram-positive bacteria (pneumococci, staphylococci) and atypical microorganisms (chlamydia, mycoplasmas). These drugs were called "new fluoroquinolones" or "respiratory fluoroquinolones." The first of the respiratory fluoroquinolones was levofloxacin, later other drugs appeared (gemifloxacin, moxifloxacin).

Due to the high activity of the new fluoroquinolones against Gram-positive microbes, including S. pneumoniae, resistant to other antibiotics, they were mainly marketed for the treatment of community-acquired respiratory tract infections, and therefore they are sometimes called “respiratory fluoroquinolones.” Also, new fluoroquinolones, along with increased activity against gram-positive bacteria, retain, and in some cases exceed, the high activity of earlier fluoroquinolones against gram-negative bacteria.

Levofloxacin is characterized by high natural activity against all pathogens of community-acquired respiratory infections. In addition, levofloxacin is characterized by good tissue pharmacokinetics, in particular, high tissue and intracellular concentrations of the drug are maintained at therapeutic levels for 24 hours.

A large number of controlled clinical studies have shown:

  • Levofloxacin is not inferior in effectiveness to β -lactam antibiotics for community-acquired respiratory infections;
  • Levofloxacin in monotherapy is not inferior in effectiveness to combined regimens ( β -lactam + macrolide) for pneumonia of any severity;
  • Levofloxacin is characterized by higher efficacy in monotherapy compared to the ceftriaxone/macrolide combination in severe community-acquired pneumonia;
  • Higher effectiveness of levofloxacin compared to macrolide antibiotics for community-acquired legionella pneumonia;
  • The advantage of levofloxacin compared to macrolide antibiotics in exacerbation of COPD both in eradication of Haemophilus influenzae and in the duration of the relapse-free period.

The most common causative agents of urinary tract infections are Escherichia coli and other enterobacteriaceae; gram-positive microorganisms are less common. Levofloxacin is characterized by high natural activity against these pathogens, comparable to the activity of ciprofloxacin, and superior to it against staphylococci and enterococci.

In recent years, in almost all regions of the world, there has been an increase in the resistance of urogenital strains of Escherichia coli and other enterobacteria to almost all antimicrobial drugs, including fluoroquinolones. The decrease in the sensitivity of enterobacteria to levofloxacin is compensated by high concentrations of the drug in the urine (250-300 μg/ml), which is many times higher than the MIC90 values. It is also characterized by good penetration into the tissues of the genitourinary system, where its concentrations are 2-5 times higher than serum concentrations. This explains the fact that, despite some reduction in the sensitivity of uropathogens, levofloxacin continues to demonstrate high efficacy against urogenital infections in controlled clinical trials.

Levofloxacin also has good penetration into the secretions and tissue of the prostate gland, which are difficult to reach for most antibiotics. An hour after a single dose of 250 mg, the concentration of levofloxacin in the prostate secretion averaged 0.89 mcg/ml, in the seminal fluid -3.25 mcg/ml, with an average concentration in the blood of -1.7 mcg/ml. The clinical effectiveness of levofloxacin has been confirmed in controlled clinical studies.

Levofloxacin has advantages over earlier fluoroquinolones in the treatment of chronic bacterial prostate and urogenital chlamydia, both in tissue pharmacokinetics and higher natural activity against some actual pathogens, primarily Enterococcus faecalis, Ureaplasma urealyticum, Chlamydia trachomatis.

Thus, along with community-acquired respiratory infections, levofloxacin can be positioned as a drug of choice in the treatment of complicated urinary infections, bacterial prostatitis and some other sexually transmitted diseases.

Recommendations for wider use of levofloxacin for respiratory and urinary infections in outpatient practice are supported by data on the good tolerability and safety of the drug.

Possible adverse reactions to Levofloxacin

Undesirable non-standard effects during therapy are numerous and affect many internal systems and organs. Patients complain:

  • for diarrhea, nausea, loss of appetite;
  • insomnia, cephalgia, abdominal pain;
  • digestive problems, skin hyperemia;
  • general weakness, tremor, muscle discomfort;
  • unreasonable anxiety, tremors, convulsions;
  • depression, joint pain, bleeding;
  • blood particles in the stool, increased heart rate.

Less common:

  • swelling of the face, blisters on the dermis;
  • problems with taste, vision, smell, tactile sensitivity;
  • formation of persistent infections, tendon ruptures, drop in blood pressure;
  • increased sensitivity to ultraviolet radiation, muscle weakness;
  • febrile syndrome, vasculitis, vascular collapse.

The antibacterial agent provokes dysbacteriosis and increased activity of fungal infections. In parallel with Levofloxacin, it is necessary to take drugs that stabilize the intestinal microflora and antifungal drugs.

Treatment with eye drops provokes:

  • mucus formation, burning sensation;
  • swelling of the eyelid tissues, obsessive itching;
  • redness of the white membranes of the eyes;
  • contact dermatitis, allergic reactions;
  • decreased visual acuity and headaches;
  • blepharitis, irritation, fear of light, runny nose.

Drops can cause the growth of papillae located on the conjunctiva.

Levofloxacin

Nosocomial infections caused by Pseudomonas aeruginosa

), may require combination treatment.

The prevalence of acquired resistance in cultured strains of microorganisms may vary by geographic region and over time. In this regard, information on drug resistance in a specific country is required.

For the treatment of severe infections or if treatment is ineffective, a microbiological diagnosis must be established with the isolation of the pathogen and determination of its sensitivity to levofloxacin.

Disability and potential irreversible serious adverse reactions associated with fluoroquinolones

The use of fluoroquinolones, including levofloxacin, has been associated with disability and the development of irreversible serious adverse reactions from various body systems that can develop simultaneously in the same patient.

Adverse reactions caused by fluoroquinolones include tendonitis, tendon rupture, arthralgia, myalgia, peripheral neuropathy, and nervous system side effects (hallucinations, anxiety, depression, insomnia, headaches, and confusion).

These reactions may develop from several hours to several weeks after starting levofloxacin therapy. The development of these adverse reactions was observed in patients of any age or without the presence of previous risk factors. If the first signs or symptoms of any serious adverse reactions occur, use of levofloxacin should be discontinued immediately. Fluoroquinolones, including levofloxacin, should be avoided in patients who have experienced any of these serious adverse reactions.

Methicillin-resistant streptococcus aureus

There is a high likelihood that methicillin-resistant Staphylococcus aureus will be resistant to fluoroquinolones, including levofloxacin. Therefore, levofloxacin is not recommended for the treatment of known or suspected infections caused by methicillin-resistant Staphylococcus aureus if laboratory tests have not confirmed the sensitivity of this microorganism to levofloxacin.

Patients predisposed to developing seizures

Like other quinolones, levofloxacin should be used with great caution in patients with a predisposition to seizures.

Such patients include patients with previous lesions of the central nervous system, such as stroke, severe traumatic brain injury; patients simultaneously receiving drugs that lower the seizure threshold of the brain, such as fenbufen and other similar non-steroidal anti-inflammatory drugs or other drugs that lower the seizure threshold, such as theophylline (see section "Interaction with other drugs").

Pseudomemdranosus colitis

Diarrhea that develops during or after treatment with levofloxacin, especially severe, persistent and/or bloody, may be a symptom of pseudomembranous colitis caused by Clostridium difficile

. If pseudomembranous colitis is suspected, treatment with levofloxacin should be stopped immediately and specific antibiotic therapy (vancomycin, teicoplanin or oral metronidazole) should be started immediately. Drugs that inhibit intestinal motility are contraindicated.

Tendinitis and tendon rupture

Rarely observed, tendonitis with quinolones, including levofloxacin, can lead to rupture of tendons, including the Achilles tendon. This side effect can develop within 48 hours after starting treatment and can be bilateral. Elderly patients are more prone to developing tendonitis. The risk of tendon rupture may be increased when taking corticosteroids concomitantly. If tendinitis is suspected, treatment with Levofloxacin should be stopped immediately and appropriate treatment of the affected tendon should be initiated, for example by providing sufficient immobilization (see sections “Contraindications” and “Side effects”).

In addition, post-transplant patients have an increased risk of developing tendonitis, so it is recommended to be careful when prescribing fluoroquinolones to this category of patients.

In patients with impaired renal function, the daily dose should be adjusted based on creatinine clearance.

Application for airborne anthrax infection

The use of levofloxacin in humans for this indication is based on susceptibility data from Bacillus anthracis obtained from in vitro and experimental animal studies, as well as limited data from the use of levofloxacin in humans. Treating physicians should refer to national and/or international documents that reflect the collectively developed point of view on the treatment of anthrax.

Hypersensitivity reactions

Levofloxacin can cause serious, potentially fatal, hypersensitivity reactions (angioedema, anaphylactic shock), further with initial doses (see section "Side effects"). Patients should immediately stop taking the drug and consult a doctor.

Severe bullous reactions

Cases of severe bullous skin reactions such as Stevens-Johnson syndrome or toxic epidermal necrolysis have been observed while taking levofloxacin (see section "Side effects"). In case of development of any reactions from the skin or mucous membranes, the patient should immediately consult a doctor and not continue treatment until his consultation.

Disorders of the liver and biliary tract

Cases of hepatic necrosis, including the development of fatal liver failure, have been reported with the use of levofloxacin, mainly in patients with severe underlying diseases, such as sepsis (see section "Side effects").

Patients should be warned to stop treatment and seek immediate medical attention if signs and symptoms of liver damage occur, such as anorexia, jaundice, dark urine, itching and abdominal pain.

Patients with kidney failure

Since levofloxacin is excreted mainly through the kidneys, patients with impaired renal function require mandatory monitoring of renal function, as well as adjustment of the dosage regimen (see section "Dosage and Administration"). When treating elderly patients, it should be borne in mind that patients in this group often have impaired renal function (see section “Dosage and Administration”).

Preventing the development of photosensitivity reactions

Although photosensitivity develops very rarely with the use of levofloxacin, to prevent its development, patients are not recommended to be unnecessarily exposed to strong solar or artificial ultraviolet irradiation (for example, visiting a solarium) during treatment and for 48 hours after the end of treatment with levofloxacin.

Superinfection

As with the use of other antibiotics, the use of levofloxacin, especially for a long time, can lead to increased proliferation of microorganisms (bacteria and fungi) that are insensitive to it, which can cause changes in the microflora that is normally present in humans. As a result, superinfection may develop. Therefore, during treatment, it is imperative to re-evaluate the patient’s condition, and, if superinfection develops during treatment, appropriate measures should be taken.

QT prolongation

Very rare cases of QT prolongation have been reported in patients taking fluoroquinolones, including levofloxacin.

When using fluoroquinolones, including levofloxacin, caution should be exercised in patients with known risk factors for prolongation of the QT interval: in patients with uncorrected electrolyte disturbances (with hypokalemia, hypomagnesemia); with congenital long QT syndrome; with heart disease (heart failure, myocardial infarction, bradycardia); while taking medications that can prolong the QT interval, such as class IA and III antiarrhythmic drugs, tricyclic antidepressants, macrolides, antipsychotics.

Elderly and female patients may be more sensitive to drugs that prolong the QT interval. Therefore, fluoroquinolones, including levofloxacin, should be used with caution (see sections “With caution”, “Dosage and administration”, “Side effects” and “Overdose”, “Interaction with other drugs”).

Patients with glucose-6-phosphate dehydrogenase deficiency

Patients with latent or manifest glucose-6-phosphate dehydrogenase deficiency are predisposed to hemolytic reactions when treated with quinolones, which should be taken into account when treated with levofloxacin.

Hypo- and hyperglycemia (dysglycemia)

As with the use of other quinolones, cases of hyperglycemia and hypoglycemia have been observed with the use of levofloxacin, usually in patients with diabetes mellitus receiving concomitant treatment with oral hypoglycemic drugs (for example, glibenclamide) or insulin preparations. Cases of hypoglycemic coma have been reported.

In patients with diabetes mellitus, monitoring of blood glucose concentrations is required (see section "Side effects").

Peripheral neuropathy

Sensory and sensorimotor peripheral neuropathy, which may have a rapid onset, has been reported in patients taking fluoroquinolones, including levofloxacin. If the patient develops symptoms of neuropathy, levofloxacin should be discontinued. This minimizes the possible risk of developing irreversible changes.

Exacerbation of pseudoparalytic myasthenia gravis (myasthenia gravis)

Fluoroquinolones, including levofloxacin, have neuromuscular blocking activity and may increase muscle weakness in patients with myasthenia gravis. Adverse reactions, including pulmonary failure requiring mechanical ventilation and death, have been reported with the use of fluoroquinolones in patients with myasthenia gravis.

The use of levofloxacin in a patient with an established diagnosis of pseudoparalytic myasthenia gravis is not recommended (see “Side Effects”).

Psychotic reactions

With the use of quinolones, including levofloxacin, the development of psychotic reactions has been reported, which in very rare cases progressed to the development of suicidal thoughts and behavior disorders with self-harm (sometimes after taking a single dose of levofloxacin (see section "Side effects")). reactions, treatment with levofloxacin should be discontinued and appropriate therapy should be prescribed.

The drug should be prescribed with caution to patients with psychosis or patients with a history of mental illness.

Visual impairment

If any visual impairment develops, immediate consultation with an ophthalmologist is necessary (see section “Side Effects”).

Effect on laboratory tests

In patients taking levofloxacin, the determination of opiates in urine may lead to false-positive results, which should be confirmed by more specific methods.

Levofloxacin may inhibit the growth of Mycobacterium tuberculosis

and subsequently lead to false-negative results of the bacteriological diagnosis of tuberculosis.

Dosages, features of use of Levofloxacin from the instructions

The tablets are taken 1 to 2 times a day, with a full glass of water. The dose is taken before or after meals, the dosage depends on the complexity of the pathological process.

For patients with normal kidney function:

  • for exacerbations of chronic bronchitis - 0.25-0.5 g per day, up to 10 days in a row;
  • sinusitis – 0.5 g, with treatment for 2 weeks;
  • for uncomplicated infectious lesions of the urinary tract - 0.25 g, for 3 days; in case of complications, the dose is doubled, treatment lasts for a week;
  • community-acquired pneumonia – 0.5 g, with therapy from 7 to 10 days;
  • prostatitis – 0.5 g, for one calendar month;
  • infection of the dermis - 0.25-0.5 g for 1-2 weeks.

For bacteriological blood damage and septic conditions, Levofloxacin is prescribed at 0.25-0.5 g per day, therapeutic procedures take from 1 to 2 weeks.

An intravenous solution is administered 250-500 ml dropwise, up to two times a day.

During the first 48 hours, eye drops are instilled every two hours, up to 8 procedures per day. The following days - four times a day, every 4 hours. The duration of course therapy is determined by the attending physician.

Levolet P (levofloxacin) has a broad spectrum of antimicrobial action. It is part of a new group of fluoroquinolones, the distinctive feature of which, along with high activity against many gram-negative bacteria, is increased activity against gram-positive microbes, atypical microorganisms and anaerobes. An important property of the drug is its high activity against intracellular pathogens [5].

Levofloxacin blocks DNAgyrase (topoisomerase II) and topoisomerase IV, disrupts supercoiling and cross-linking of DNA breaks, inhibits DNA synthesis, and causes profound morphological changes in the cytoplasm, cell wall and membranes. Like other fluoroquinolones, levofloxacin has a pronounced post-antibiotic effect - the continuation of the antimicrobial effect after the drug is removed from the environment, the duration of which depends on the type of microorganism and the value of the previously effective concentration [5]. Levofloxacin has favorable pharmacokinetic properties.

It is important to emphasize that the pharmacokinetic parameters of dosage forms for oral and parenteral administration do not differ significantly, and this makes it possible to effectively use the drug in a stepwise manner. When taken orally, levofloxacin is rapidly and almost completely absorbed. Bioavailability is 99% and does not depend on food intake. Levofloxacin is characterized by a low degree of binding to plasma proteins - 30–40%. It has a large volume of distribution, accumulates in many organs and tissues: lungs, bronchial mucosa, alveolar macrophages, fluid lining the alveoli, skin, kidney parenchyma, prostate gland, etc., creating in them levels several times higher than the minimum inhibitory concentration for potential pathogens [3, 4].

The drug is excreted primarily in the urine (70%), which creates high concentrations sufficient to suppress microflora sensitive to it for a long time [5]. Long-term circulation of the drug in the body in therapeutic concentrations allows it to be used once a day [5]. As a rule, levofloxacin is well tolerated by patients.

Side effects (3–10% of cases) include nausea, vomiting, diarrhea, constipation, headache, phototoxicity, hypersensitivity reactions, prolongation of the QT interval on the electrocardiogram, tendonitis. Contraindications to taking the drug include hypersensitivity, age under 18 years, pregnancy, breastfeeding, epilepsy, glucose-6-phosphate dehydrogenase deficiency [5].

Levofloxacin is used in urological practice to treat diseases such as uncomplicated and complicated urinary tract infections (UTIs), bacterial prostatitis, nonspecific urethritis and some types of specific urethritis (caused by sexually transmitted infections), as well as orchitis and epididymitis.

Uncomplicated urinary tract infections

Acute uncomplicated UTI is an episode of acute infection of the lower (urethritis, cystitis) or upper (pyelonephritis) urinary tract in patients in the absence of any disturbances in the outflow of urine from the kidneys and bladder, structural changes in the organs of the urinary system and serious underlying diseases that may aggravate its course or lead to ineffectiveness of the therapy.

Recurrent uncomplicated UTI is the occurrence of more than two episodes of UTI within six months or three episodes per year.

Asymptomatic bacteriuria - the presence of two consecutive (with an interval of a week) positive results of bacteriological examination of urine, in which the same strain of the UTI pathogen was detected; There are no clinical manifestations of the disease [2].

Uncomplicated UTIs are more common in women. Every second woman in the world experiences an episode of UTI at least once in her life, of which 25–40% of women experience a recurrence of the disease over the next 6–12 months.

Treatment of acute uncomplicated UTIs can be carried out on an outpatient basis; Hospitalization is necessary only in serious cases. For acute uncomplicated cystitis, levofloxacin is prescribed orally at a dose of 250–500 mg once a day for 3–5 days. Treatment of acute uncomplicated mild pyelonephritis consists of taking levofloxacin orally at a dose of 250–500 mg once a day for 7–14 days. In the absence of improvement or if the patient's condition worsens, hospitalization is indicated for additional examination, identification of complicating factors, drainage of the urinary tract and possible surgical treatment. Hospitalization is also indicated for initial moderate and severe acute uncomplicated pyelonephritis, the presence of symptoms of intoxication, and urosepsis [2].

For acute uncomplicated pyelonephritis of moderate and severe course, levofloxacin is administered intravenously at a dose of 500 mg once a day for 3–5 days, then orally at a dose of 500 mg once a day (total course of treatment is 2–3 weeks).

Uncomplicated UTIs (excluding sexually transmitted diseases) are rare in young, healthy men aged 15 to 50 years. Typically, UTIs in men are complicated and are caused by urological abnormalities, bladder outlet obstruction, instrumental interventions and urinary tract drainage [2]. Nonspecific urethritis in young men is treated with levofloxacin, taken orally at a dose of 250–500 mg once a day for 7 days.

In case of exacerbation of recurrent uncomplicated UTI, it is possible to use levofloxacin according to the regimens given above. However, long-term use of the drug as maintenance therapy is often unjustified due to the high risk of developing dysbiosis.

Complicated urinary tract infections

Complicated UTI develops against the background of structural or anatomical abnormalities of the genitourinary organs, as well as concomitant diseases that reduce the body's defenses and increase the risk of ascending infection or treatment failure.

A complicated UTI is characterized by the presence of one or more of the following:

  • the presence of a permanent bladder catheter, catheter-stent, drainage; intermittent catheterization of the bladder;
  • presence of residual urine;
  • obstructive uropathy (infravesical obstruction, neurogenic bladder, stones, urinary tract tumors, etc.);
  • vesicoureteral reflux and other functional abnormalities;
  • reconstructive surgeries on the urinary tract;
  • chemical or radiation damage to the urothelium;
  • peri- and postoperative UTI;
  • renal failure, diabetes mellitus, kidney transplantation, immunodeficiency states [2].

Treatment tactics depend on the severity of the disease and the ability to eliminate complicating factors. Otherwise, the UTI may not be completely cured. Treatment of complicated UTI often requires hospitalization of the patient. In this case, it is advisable to carry out antibacterial therapy under the control of bacteriological examination of urine. Of the antibacterial agents, the most effective are fluoroquinolones, which are excreted primarily by the kidneys, have a wide spectrum of antimicrobial action and reach high concentrations both in the urine and in the tissues of the genitourinary system.

In the presence of kidney or bladder stones, eradication of the pathogen can help inhibit their growth. If complete stone removal is not possible, the patient requires long-term antimicrobial therapy.

The addition of infection against the background of obstruction of the upper urinary tract is extremely dangerous and requires emergency drainage. Active antimicrobial therapy can be started only after the obstruction has been eliminated due to the high risk of developing bacteriotoxic shock.

Treatment of asymptomatic bacteriuria in patients with permanent catheters or drainages in the urinary tract, as well as intermittent catheterization of the bladder, is not recommended, since it leads to the selection of resistant strains of microorganisms and is not effective for the eradication of microorganisms that are part of the biofilm. If clinical manifestations are present, such patients are prescribed 7–10-day courses of broad-spectrum antibiotic therapy. The presence of diabetes mellitus or immunodeficiency is an indication for treatment of even asymptomatic bacteriuria. For complicated UTIs (except for cases of resistance), levofloxacin is used intravenously at 500 mg once a day for 7–14 days. If indicated, the duration of treatment can be increased to 3 weeks.

When using levofloxacin in patients with renal failure, it should be taken into account that if glomerular filtration decreases to <20 ml/min, it is necessary to adjust the dose or increase the intervals between doses of the drug. In the urology clinic of the First Moscow State Medical University named after. THEM. Sechenov, levofloxacin was prescribed to 75 patients with uncomplicated and 32 with complicated (acute obstructive pyelonephritis) aged from 20 to 68 years (average 44 years). Among patients with uncomplicated infections, 50 women had acute cystitis, and 25 had acute non-obstructive pyelonephritis. The drug was prescribed to patients at a dosage of 500 mg per day for 10 days for uncomplicated infections and 14 days for complicated UTIs. Treatment results were assessed based on subjective assessment of the effectiveness and safety of treatment by patients and physicians, as well as analysis of objective indicators: monitoring of blood and urine tests, ultrasound monitoring. Lack of clinical effect of treatment was defined as persistence or worsening of clinical manifestations after 2 days of therapy.

According to the data obtained during the study, a positive clinical and bacteriological effect of treatment was achieved in 90% of patients with uncomplicated and in 81% of patients with complicated UTIs. During a control bacteriological examination performed 2 weeks after treatment, no growth of the pathogen was detected in patients with a good clinical effect of antibiotic therapy. Side effects when using levofloxacin were noted in 3% of patients. The most common adverse reactions were nausea and diarrhea. It should be noted that the above phenomena had an extremely low degree of severity. None of the patients required special treatment due to the above adverse reactions, and none of them dropped out of the study.

Thus, fluoroquinolones currently retain their leading position in the treatment of UTIs. In terms of clinical effectiveness, these drugs are comparable to aminoglycosides and new generation cephalosporins, and in some cases (for mixed infections) superior to them. The effect of fluoroquinolones is predominantly pathogenetic in nature, and is aimed at eliminating infectious agents from the body.

Bacterial prostatitis

With inflammation of the prostate gland (prostatitis), which can be acute or chronic, symptoms persist for more than 3 months [2]. Treatment of prostatitis should be comprehensive; in addition to antimicrobial therapy, adequate drainage of the excretory ducts of the prostate acini is necessary (for chronic prostatitis, prostate massage is performed), as well as the use of various physical methods (physiotherapy) in order to improve blood flow and provide a more effective anti-inflammatory effect.

When choosing antibacterial agents, one should take into account the spectrum of their antimicrobial activity, as well as their ability to penetrate prostate tissue. Fluoroquinolones have good tissue penetration, a wide spectrum of antimicrobial activity and are the drug of choice in the treatment of prostatitis. In the urology clinic of the First Moscow State Medical University named after. THEM. Sechenov's effectiveness of levofloxacin was assessed in 38 patients with chronic bacterial prostatitis. To confirm the diagnosis of chronic prostatitis, all patients underwent microscopy of prostate secretions. In rare cases (about 10%), when it was not possible to obtain prostate juice, a spermogram was performed.

The material for bacteriological culture was always sperm collected in the morning on the day of the study in a sterile jar. This analysis was not performed on all patients. The selection criterion for the study was a long history of treatment for chronic prostatitis, which could be the cause of multiple antibiotic resistance of the pathogen.

The criterion for exclusion from the study was multidrug-resistant flora identified during bacteriological examination.

The pathogens identified during bacteriological examination in patients of the main and control groups were sensitive to most drugs, including fluoroquinolones.

The effectiveness of the drug was assessed 1 month after the start of treatment. The control examination included a microscopic examination of prostate secretions, a bacteriological examination of sperm, and a PCR examination of scrapings from the urethra.

After treatment of patients with chronic bacterial prostatitis, complaints were completely absent in 35 (92%) patients. One patient experienced a decrease in clinical symptoms. In 2 patients, complaints persisted, but during a control microscopic examination of prostate secretions there were no signs of inflammation. The proportion of patients in whom pathogens were not identified during the control examination was 89.4%.

The clinical effectiveness of levofloxacin in patients with chronic bacterial prostatitis was 92%, microbiological effectiveness - 89.4%.

For acute bacterial prostatitis, the following treatment regimen is used: levofloxacin 500 mg intravenously once a day for 2–4 weeks, then orally 500 mg once a day for 2 weeks. For chronic bacterial prostatitis, levofloxacin is prescribed orally at a dose of 500 mg once a day for 3–4 weeks.

Epididymitis and orchitis

When choosing an antibiotic for the treatment of epididymitis (inflammation of the testicle) and orchiepididymitis (combined inflammation of the testicle and epididymis) in young sexually active men, it is necessary to remember that in 2/3 of cases the disease can be caused by chlamydial infection. In elderly patients with benign prostatic hyperplasia and urinary dysfunction, uropathogenic microorganisms may be the causative agents. Fluoroquinolones are the drugs of choice due to their wide spectrum of antimicrobial activity and good interstitial penetration [2].

Depending on the severity of the inflammatory process, fluoroquinolones are used orally or parenterally. For orchitis, epididymitis, or mild orchiepididymitis, levofloxacin is prescribed orally at a dose of 500 mg once a day for 2 weeks. Orchitis, epididymitis, orchiepididymitis of moderate and severe course are treated with levofloxacin intravenously at a dose of 500 mg once a day for a week, then orally at a dose of 500 mg once a day also for a week.

Sexually transmitted diseases

A special place in the recommendations of the WHO, CDC (Centers for Disease Control), and European recommendations for the management of patients with sexually transmitted diseases (STDs) is occupied by fluoroquinolones, which have a bactericidal effect, a wide spectrum of antimicrobial activity, high efficiency, and good tolerability with long-term use. An important factor in the treatment of a number of STDs is the effect of fluoroquinolones on microorganisms that are resistant to drugs of other classes, high activity against microorganisms with intracellular localization, and a long-term post-antibiotic effect [1]. Therapy for chlamydial and mycoyes ureaplasma urethritis includes taking levofloxacin at a dose of 500 mg once a day for 7–10 days.

Thus, due to its unique qualities, levofloxacin is the drug of choice for the treatment of a wide range of urological diseases.

Information about the authors: Elena Anatolyevna Sultanova – Candidate of Medical Sciences, urologist at the Russian-Israeli Medical Center RAMBAM. Tel.; Shpot Evgeniy Valerievich – Candidate of Medical Sciences, urological clinic, associate professor of the Department of Urology of the State Educational Institution of Higher Professional Education “First Moscow State Medical University named after. THEM. Sechenov” Ministry of Health and Social Development. Email

Levofloxacin 500 mg 10 pcs. tablets in Voronezh

Nosocomial infections caused by Pseudomonas aeruginosa

), may require combination treatment.

The prevalence of acquired resistance in cultured strains of microorganisms may vary by geographic region and over time. Therefore, country-specific information on levofloxacin resistance is required. For the treatment of severe infections or if treatment is ineffective, a microbiological diagnosis must be established with the isolation of the pathogen and determination of its sensitivity to levofloxacin.

There is a high likelihood that methicillin-resistant Staphylococcus aureus will be resistant to fluoroquinolones, including levofloxacin. Therefore, levofloxacin is not recommended for the treatment of known or suspected infections caused by methicillin-resistant Staphylococcus aureus if laboratory tests have not confirmed the sensitivity of this microorganism to levofloxacin.

Like other quinolones, levofloxacin should be used with great caution in patients with a predisposition to seizures. Such patients include patients with previous CNS lesions, such as stroke, severe traumatic brain injury; patients concomitantly taking drugs that lower the seizure threshold of the brain, such as fenbufen and other similar NSAIDs or other drugs that lower the seizure threshold, such as theophylline

Diarrhea that develops during or after treatment with levofloxacin, especially severe, persistent and/or bloody, may be a symptom of pseudomembranous colitis caused by Clostridium difficile. If pseudomembranous colitis is suspected, treatment with levofloxacin should be stopped immediately and specific antibiotic therapy (vancomycin, teicoplanin or oral metronidazole) should be started immediately. Drugs that inhibit intestinal motility are contraindicated.

Tendonitis has been reported rarely with quinolones, including levofloxacin, and can sometimes lead to rupture of tendons, including the Achilles tendon. This side effect can develop within 48 hours after starting treatment and can be bilateral. Elderly patients are more prone to developing tendonitis; in patients taking fluoroquinolones, the risk of tendon rupture may increase with concomitant use of corticosteroids. In addition, post-transplant patients have an increased risk of developing tendonitis, so it is recommended to be careful when prescribing fluoroquinolones to this category of patients. If tendonitis is suspected, treatment with levofloxacin should be stopped immediately and appropriate treatment of the affected tendon should be initiated, for example by providing adequate immobilization.

Levofloxacin may cause serious, potentially fatal hypersensitivity reactions (angioedema, anaphylactic shock), even with initial doses. In such cases, you should immediately stop using levofloxacin and consult a doctor.

Cases of severe bullous skin reactions such as Stevens-Johnson syndrome or toxic epidermal necrolysis have been observed with the use of levofloxacin. In case of development of any reactions from the skin or mucous membranes, the patient should immediately consult a doctor and not continue treatment until his consultation.

Cases of liver necrosis, including fatal liver failure, have been reported with the use of levofloxacin, mainly in patients with severe underlying diseases, such as sepsis. Patients should be warned to stop treatment and seek immediate medical attention if signs and symptoms of liver damage occur, such as anorexia, jaundice, dark urine, itching and abdominal pain.

Since levofloxacin is excreted mainly through the kidneys, patients with impaired renal function require mandatory monitoring of renal function, as well as adjustment of the dosage regimen. When treating elderly patients, it should be taken into account that patients in this group often have impaired renal function.

Although photosensitivity occurs very rarely with the use of levofloxacin, to prevent its development, patients are not recommended to be exposed to strong solar or artificial ultraviolet radiation (for example, visiting a solarium) during treatment and for 48 hours after the end of treatment with levofloxacin.

As with the use of other antibiotics, the use of levofloxacin, especially for a long time, can lead to increased proliferation of microorganisms (bacteria and fungi) that are insensitive to it, which can cause changes in the microflora that is normally present in humans. As a result, superinfection may develop. Therefore, during treatment, it is imperative to re-evaluate the patient’s condition, and, if superinfection develops during treatment, appropriate measures should be taken.

Very rare cases of QT prolongation have been reported in patients taking fluoroquinolones, including levofloxacin.

When using fluoroquinolones, including levofloxacin, caution should be exercised in patients with known risk factors for prolongation of the QT interval: in patients with uncorrected electrolyte disturbances (with hypokalemia, hypomagnesemia); with congenital long QT syndrome; with heart disease (heart failure, myocardial infarction, bradycardia); with simultaneous use of drugs that can prolong the QT interval, such as class IA and III antiarrhythmic drugs, tricyclic antidepressants, macrolides, antipsychotics.

Elderly and female patients may be more sensitive to drugs that prolong the QT interval. Therefore, fluoroquinolones, including levofloxacin, should be used with caution in this category of patients.

Patients with latent or manifest glucose-6-phosphate dehydrogenase deficiency are predisposed to developing hemolytic reactions when treated with quinolones, which should be taken into account when treating with levofloxacin.

As with the use of other quinolones, cases of hyperglycemia and hypoglycemia have been observed with the use of levofloxacin. During therapy with levofloxacin, dysglycemia occurred more often in elderly patients and patients with diabetes mellitus receiving concomitant therapy with oral hypoglycemic drugs (for example, glibenclomide) or insulin. When using levofloxacin in such patients, the risk of developing hypoglycemia, including hypoglycemic coma, increases. It is necessary to inform patients about the symptoms of hypoglycemia (confusion, dizziness, ravenous appetite, headache, nervousness, palpitations or increased heart rate, pale skin, perspiration, trembling, weakness). If the patient develops hypoglycemia, treatment with levofloxacin should be stopped immediately and appropriate therapy should be initiated. In these cases, it is recommended to switch to therapy with an antibiotic other than a fluoroquinolone, if possible. When treating with levofloxacin in elderly patients and patients with diabetes mellitus, careful monitoring of blood glucose concentrations is recommended.

Sensory and sensorimotor peripheral neuropathy, which may have a rapid onset, has been reported in patients taking fluoroquinolones, including levofloxacin. If the patient develops symptoms of neuropathy, levofloxacin should be discontinued. This minimizes the possible risk of developing irreversible changes.

Fluoroquinolones, including levofloxacin, have neuromuscular blocking activity and may increase muscle weakness in patients with myasthenia gravis. Adverse reactions, including pulmonary failure requiring mechanical ventilation and death, have been associated with the use of fluoroquinolones in patients with myasthenia gravis. The use of levofloxacin in a patient with an established diagnosis of pseudoparalytic myasthenia gravis is not recommended.

The use of airborne anthrax is based on data on the sensitivity of Bacillus anthracis to it from in vitro and experimental studies in animals, as well as on limited data from the use of levofloxacin in humans. Treating physicians should refer to national and/or international documents that reflect the collectively developed point of view on the treatment of anthrax.

Psychotic reactions, including suicidal ideation/attempts, have been reported in patients taking fluoroquinolones, including levofloxacin, sometimes after a single dose. In case of development of any side effects from the central nervous system, including mental disorders, treatment with levofloxacin should be stopped immediately and appropriate therapy should be prescribed. In these cases, it is recommended to switch to therapy with an antibiotic other than a fluoroquinolone, if possible. The drug should be prescribed with caution to patients with psychosis or patients with a history of mental illness.

In patients taking levofloxacin, the determination of opiates in urine may lead to false-positive results, which should be confirmed by more specific methods.

Levofloxacin may inhibit the growth of Mycobacterium tuberculosis, which may subsequently lead to false-negative results of the bacteriological diagnosis of tuberculosis.

When carrying out intravenous infusion, the recommended duration of administration should be strictly adhered to. Experience with the use of levofloxacin shows that increased heart rate and a transient decrease in blood pressure may occur during infusion. In rare cases, vascular collapse may develop. If a pronounced decrease in blood pressure is observed during the intravenous infusion of levofloxacin, then its administration is immediately stopped.

Impact on the ability to drive vehicles and machinery

During the treatment period, it is necessary to refrain from engaging in potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

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