What is the difference between ciprofloxacin and levofloxacin. Antibiotic Ciprofloxacin: description, indications for use and medicinal properties of the drug

Levofloxacin - synonyms

Levofloxacin eye drops have the following synonymous drugs:

• Oftakviks - eye drops;
• Signicef ​​- eye drops;
• L-Optic Rompharm - eye drops.

Levofloxacin tablets and solution for infusions have the following synonyms in the domestic pharmaceutical market:

• Vitalecin - tablets;
• Glevo - tablets;
• Ivacin - solution for infusion;
• Lebel - tablets;
• Levolet R - tablets and solution for infusion;
• Levostar - tablets;
• Levotek - tablets and solution for infusion;
• Levoflox - tablets;
• Levofloxabol - solution for infusion;
• Levofloripin - tablets;
• Leobag - solution for infusion;
• Leflobact - tablets and solution for infusion;
• Lefoktsin - tablets;
• Lefloks - solution for infusion;
• Loksof - tablets;
• Maklevo - tablets and solution for infusion;
• Remedia - tablets and solution for infusion;
• Tavanic - tablets and solution for infusion;
• Tanflomed - tablets;
• Flexid - tablets;
• Floracid - tablets;
• Hylefloks - tablets;
• Ecovid - tablets;
• Elefloks - tablets and solution for infusion.

Analogues

For citation: Belousov Yu.B., Mukhina M.A. Clinical pharmacology levofloxacin // BC. 2002. No. 23. S. 1057

RSMU

IN Currently, fluoroquinolones (FC) are considered as an important group of chemotherapeutic drugs within the class of quinolones - DNA gyrase inhibitors, characterized by high clinical efficacy (including oral administration), wide indications for use and constitute a serious alternative to other broad-spectrum antibiotics. More than 15 drugs of the PC group have been created, several new active compounds are undergoing clinical trials in order to obtain more effective drugs against gram-positive microorganisms, mycobacteria, anaerobes, atypical pathogens. An important task is also the development of drugs with minimal risk of side effects and high clinical efficacy.

Among FH, two groups of drugs are currently distinguished: early or old (norfloxacin, ciprofloxacin, ofloxacin, pefloxacin, lomefloxacin, etc.) and new or late (levofloxacin, sparfloxacin, gatifloxacin, gemifloxacin, etc.).

Ofloxacin has been used for more than 15 years, has high efficacy, good tolerance, low side effects and no significant drug interactions. From the point of view of stereochemistry, ofloxacin is a racemic mixture of two optically active isomers: left-handed (L-isomer, L-ofloxacin) and right-handed (D-isomer, D-ofloxacin).

The levorotatory isomer of ofloxacin, L-ofloxacin, is currently known as levofloxacin (LF). The drug was developed in the late 1980s in Japan and was proposed for use after multicenter clinical trials conducted in Europe, America, and Asian countries. In Russia, levofloxacin was registered and approved for use in 2000 under trade name Tavanik (oral and parenteral forms).

Levofloxacin is 8-128 times more active than D-ofloxacin. In the chemical structure of LF, two main groups play a significant role: 4-methyl-piperazinyl, which causes an increase in absorption when the drug is taken orally, an increase in its activity against gram-negative bacteria, an extension of the half-life, and an oxazine ring, which causes an expansion of the spectrum of activity against gram-positive bacteria, as well as prolongation of the half-life. Levofloxacin is characterized by 2 times greater activity than ofloxacin, and, therefore, is not inferior in activity to ciprofloxacin.

Levofloxacin has a unique, almost 100% oral bioequivalence. The pharmacokinetic profile of LF is similar to that of ofloxacin. The half-life is 4-8 hours, that is, more than that of ciprofloxacin, T max - 1.5 hours (as in ciprofloxacin and ofloxacin), C max - 5.1 mg / l (that is, 4 times more than that of ciprofloxacin), which practically corresponds to C max when administered parenterally in an equivalent dose. Levofloxacin is almost 10 times more soluble than ofloxacin.

Activity spectrum

Levofloxacin, like other PCs, has a bactericidal type of action and a wide antimicrobial spectrum. PC is active against most enterobacteria, gram-negative bacilli (Hemophilus influenzae, including b-lactamase-producing strains) and gram-negative cocci (gonnococcus, meningococcus, moraxella, including b-lactamase-producing strains), as well as Pseudomonas aeruginosa. Early PCs (ciprofloxacin, ofloxacin) have some activity against staphylococci and even less activity against streptococci and enterococci, unlike new PCs, including levofloxacin, highly active against Staphylococcus aureus (with the exception of methicillin-resistant strains), coagulase-negative staphylococci, streptococci, including pneumococcus (Tables 1, 2). The MIC range of LF for staphylococci is 0.06-64 mg/l (at MIC 90 0.25-16 mg/l), for pneumococci the MIC range is 0.25-0.2 mg/l. Antipneumococcal activity does not depend on the degree of sensitivity to penicillin. Levofloxacin is somewhat less active against enterococci, although for some strains, the MIC values ​​\u200b\u200bare 0.5-1 mg / l. The drug is highly active against Listeria monocitogenes, Сorinebacterium diphtheriae. Intracellular pathogens (chlamydia, mycoplasmas, legionella) are susceptible to all PCs. Some new PCs are active against anaerobes, LF - partially. Of particular interest is the activity of LF against mycobacteria. The activity of LF against rickettsia, bartonella and some other microorganisms is being studied.

In the past decade, resistance to fluoroquinolones in the following pathogens has been noted in the United States: MRSA, enterococci, Pseudomonas sp. In subsequent years, an increase in the resistance of Salmonella, Shigella, Acinetobacter sp., Campilobacter sp. and gonococcus. Selection of strains of Staphylococcus aureus resistant to LF is observed much less frequently than to ciprofloxacin. Data on resistance of pneumococci to PC are known. One of the lowest levels of pneumococcal resistance was noted for LF (generally 0.5% in 1997-2000 in the USA and Canada). Formation of resistance to levofloxacin is possible, but currently resistance to the drug develops most slowly and is not cross with other antibiotics .

In the past decade, resistance to fluoroquinolones in the following pathogens has been noted in the United States: MRSA, Enterococcus. In subsequent years, an increase in resistance in Salmonella, Shigella, and Gonococcus has been reported. Selection of strains of Staphylococcus aureus resistant to LF is observed much less frequently than to ciprofloxacin. Data on resistance of pneumococci to PC are known. One of the lowest levels of pneumococcal resistance was noted for LF (generally 0.5% in 1997-2000 in the USA and Canada). The formation of resistance to levofloxacin is possible, however, at present.

Pharmacokinetics

Levofloxacin has some pharmacokinetic advantages over other PCs. This is determined by the resistance of the molecule to transformation and metabolism in the patient's body. Levofloxacin, like ciprofloxacin, gatifloxacin, trovafloxacin and ofloxacin, exists in oral and parenteral forms and can be used in step therapy , unlike other PCs available only in oral form.

Long T 1/2 allows you to prescribe LF once a day which improves patient compliance. Oral bioavailability of LF reaches 100% and does not depend on food intake, which also makes it convenient to use. Excretion of most PC occurs in a double way (through the kidneys and liver). In contrast, LF is excreted mainly through the kidneys (90%), which requires dose adjustment in severe renal failure. However, the lack of metabolism by enzymes of the cytochrome p450 system causes the absence of interaction with warfarin and theophylline and other significant drug interactions. In a clinical and pharmacological study of mutual influence while prescribing LF with non-steroidal anti-inflammatory, antidiabetic, antiarrhythmic drugs of class I and III, theophylline, warfarin, cyclosporine and cimetidine, it was not noted (Simpson I., 1999).

Levofloxacin is only 5% metabolized. About 35% of LF binds to blood serum proteins, and therefore the drug is well distributed in tissues. It should be emphasized that PC, including LF, perfectly penetrate into various tissues, creating high concentrations in the kidneys, prostate, female genital organs, bile, gastrointestinal tract, bronchial secretions, alveolar macrophages, lung parenchyma, bones, and also in cerebrospinal fluid, therefore these drugs can be widely used for infections of almost any localization. In addition, good intracellular penetration ensures their activity against atypical pathogens.

The clinical efficacy of LF with a single appointment of 250-500 mg / day is a significant advantage of the drug, however, with generalized infectious processes that occur in severe form, LF is prescribed twice.

Side effects and tolerance

Side effects of levofloxacin and other PCs are known from European and other international studies. More than 5,000 patients have been studied in Europe, and approximately 130 million LF prescriptions have been administered worldwide during trials.

Levofloxacin proved to be the safest PC with a low level of hepatotoxicity (1/650,000). Levofloxacin, along with ofloxacin and moxifloxacin, is safer in terms of pathological effects on the central nervous system. Cardiovascular negative effects of LF were observed much less frequently than with other PCs (1/15 million appointments, with sparfloxacin - in 1-3% of cases). Diarrhea, nausea and vomiting are the most common side effects associated with Lf, but they are much less common than with other FH. The frequency of side effects of LF and other PC is presented in Table. 3 .

It has been shown that an increase in the dose of LF up to 1000 mg/day does not lead to an increase in the number of side effects, and their probability does not depend on the patient's age.

In general, the level of adverse reactions associated with LF is the lowest among PC, and the tolerability of LF can be regarded as very good.

Levofloxacin for lower respiratory tract infections

community-acquired pneumonia

Community-acquired pneumonia is one of the most common diseases with a serious prognosis. The incidence of pneumonia in Europe ranges from 2 to 15 cases per 1000 people per year. According to A.G. Chuchalin, the prevalence of pneumonia among the adult population of Russia is 5-8 per 1000 people. In the USA, 2-3 million cases are registered annually community-acquired pneumonia about 10 million medical visits per year. According to TsNIIOIZ of the Ministry of Health of the Russian Federation, more than 1.5 million adults annually suffer from pneumonia in Russia.

The overall mortality in pneumonia is about 20-30 cases per 100 thousand people per year. Mortality among outpatients with low risk is less than 1%, and in patients hospitalized with pneumonia - up to 14% (in critical patients up to 30-40%) (Fine et al. 1999).

Pneumococcus remains the most common causative agent of community-acquired pneumonia - 30.5% (20-60%). Common in young and middle age groups Mycoplasma pneumoniae(5-50%) and Chlamydia pneumoniae(5-15%). In older age groups, these pathogens are less common (1-3%). Legionella is a rare causative agent of pneumonia (4.8%), but it causes up to 10% of cases of severe pneumonia. Legionella pneumonia ranks second in mortality after pneumococcal pneumonia. H. influenzae more often causes pneumonia in smokers or against the background of chronic bronchitis (3-10%) and, according to some data, in Russia it ranks second in the etiology of severe pneumonia. Family representatives Enterobacteriaceae(E.coli, K.pneumoniae) occur in patients with risk factors ( diabetes, circulatory failure, etc.) in 3-10% of cases. Moraxella catarrhalis isolated in 0.5% of cases Relatively rarely isolated Str. pyogenes, Chl. psittaci, Coxiella burnetii and others. In severe pneumonia, a relatively large proportion of bacterial agents is occupied by Staphylococcus aureus, the probability of its detection increases with age or after influenza (3-10%), while the mortality rate can reach 50%. In 50% of cases, it is not possible to isolate the pathogen, and in 2-5% of cases a mixed infection is detected.

For recent years worldwide, there is a rapid increase in the resistance of pathogens of pneumonia to antibacterial drugs. Significantly increased the proportion of pneumonia caused by pneumococcal strains resistant to penicillin (up to 51.4%) and cephalosporins, as well as to macrolides (to erythromycin up to 45.9%), tetracyclines and co-trimoxazole. At the same time, in some regions, resistance to macrolides prevails over resistance to penicillin. In some countries, the incidence of resistance of pneumococci to penicillin can reach 60%. Large-scale studies of pneumococcal resistance to penicillin have not been conducted in our country. According to local studies in Moscow, the frequency of resistant strains is 2%, strains with intermediate sensitivity - about 20%. The resistance of pneumococci to penicillin is not associated with the production of b-lactamase, but with the modification of the antibiotic target in the microbial cell - penicillin-binding proteins, therefore inhibitor-protected penicillins are also inactive against these pneumococci. Pneumococcal resistance to penicillin is usually accompanied by resistance to I-II generation cephalosporins, macrolides, tetracyclines, co-trimoxazole.

The problem of pneumococcal resistance to antibiotics in Russia is not yet as relevant as in the West, but it should be remembered that the resistance of strains varies in each region. Risk factors for the development of resistance are the elderly and childhood, comorbidities, prior antibiotic therapy, stay in care homes.

The resistance of Haemophilus influenzae to penicillins reaches 10%, its resistance to new macrolides is growing.

Antibacterial therapy of pneumonia, in the vast majority of cases empirical, requires the use of drugs with a wide spectrum of action. When choosing a method of treatment, the severity of the disease and risk factors are taken into account. Empiric therapy should always cover pneumococcus, antibiotics active against mycoplasma and legionella should be considered during an influenza epidemic - S. aureus and in elderly patients Enterobacteriaceae. It is common for severe community-acquired pneumonia to begin treatment with an antibiotic combination consisting of a macrolide and an agent active against gram-negative enterobacteria, such as a cephalosporin. In addition, current guidelines recommend the use of the latest PC for the treatment of community-acquired pneumonia requiring hospitalization.

Fluoroquinolones have a wide spectrum of antimicrobial activity. These drugs show natural activity against almost all potential pathogens of community-acquired pneumonia. However the use of early FH (ciprofloxacin, ofloxacin, pefloxacin) with community-acquired pneumonia was limited due to their weak natural activity against the main causative agent of pneumonia - S. pneumoniae. The minimum inhibitory concentrations (MICs) of early PC against pneumococcus range from 4 to 8 µg/ml, and their concentration in bronchopulmonary tissue is much lower, which is insufficient for successful therapy. Cases have been described in which PC therapy in pneumococcal pneumonia was not successful. According to other data, it is possible to create a high tissue concentration of these drugs, sufficient for adequate anti-pneumococcal activity. This is confirmed by the clinical and bacteriological efficacy of ciprofloxacin in the treatment of pneumonia and other infections of the lower respiratory tract, which is not inferior to standard therapy b-lactam antibiotics. The proven efficacy of PC in lower respiratory tract infections allows to determine their place in the treatment of community-acquired pneumonia. In patients younger than 65 years of age, non-smokers, without serious chronic diseases, the causative agent of community-acquired pneumonia in 80% of cases is pneumococcus and other streptococci, less often atypical microorganisms. Fluoroquinolones in this category of patients are an alternative for the treatment of moderate to severe pneumonia, for example, when allergic to penicillins. In patients over 65 years of age, heavy smokers suffering from serious chronic somatic diseases, alcoholism, the causative agents of pneumonia are predominantly gram-negative pathogens, namely H. influenzae, M. catarrhalis, Klebsiella spp., in a third of cases pneumococcus, often atypical pathogens. Fluoroquinolones are the drugs of choice in this category of patients, especially in outpatient treatment, since they can be administered orally in moderate disease with a single dose per day, which increases the compliance of elderly patients. In the treatment of pneumonia requiring hospitalization, the advantage of PC is the possibility of using stepwise therapy, which significantly improves the pharmacoeconomic aspects of treatment.

Against the background of growing resistance of key pathogens of respiratory infections to antibiotics (in particular, the spread of strains S.pneumoniae resistant to penicillin and macrolides) new or so-called respiratory fluoroquinolones(levofloxacin, moxifloxacin, gatifloxacin). New PCs have increased, in comparison with classical fluoroquinolones (ofloxacin, ciprofloxacin), activity against S.pneumoniae. It should also be emphasized that the high anti-pneumococcal activity of new PCs is observed regardless of the sensitivity of pneumococcus to penicillin and / or to macrolides. The superiority of new PCs is also obvious in relation to atypical pathogens ( M.pneumoniae, C. pneumoniae, L.pneumophila). And finally, these antibiotics "inherited" high activity classic FH vs. H.influenzae And M.catarrhalis. There is no doubt that the new PCs are an acceptable alternative to macrolides, amoxicillin/clavulanate and oral cephalosporins in the treatment of community-acquired pneumonia. To the obvious advantages of the new PCs, one should add the possibility of taking them once a day and using them as part of a stepwise therapy.

In studies conducted to date, including incl. and patients with severe and (or) unfavorable prognostic course of the disease, convincing evidence was obtained of superior or at least comparable clinical and microbiological efficacy of LF monotherapy compared to traditional combined treatment (cephalosporins + macrolides). This circumstance, as well as the excellent safety profile, confirmed by many years of widespread clinical use, and the obvious economic advantages of monotherapy explain the presence of LF in modern treatment regimens for community-acquired pneumonia. Levofloxacin occupies a prominent place in modern treatment regimens for adult patients with community-acquired pneumonia not subject to hospitalization (Frias J., 1998; Bartlett J.G., 2000), as well as in a hospital setting (Frias J., 2000; Mandell L.A., 1997)

In community-acquired pneumonia, the clinical efficacy of LF was superior to that of therapy with ceftriaxone, cefuroxime (including in combination with erythromycin or doxycycline) and amounted to 96 and 90%, bacteriological efficacy - 98 and 85%, respectively; the differences were statistically significant (File T.M., 1997).

According to I. Harding (2001), levofloxacin was more effective in the treatment of community-acquired pneumonia than clarithromycin, benzylpenicillin, ceftriaxone, amoxicillin/clavulanic acid.

In a randomized, double-blind, multicenter study, 518 patients with community-acquired pneumonia underwent comparative analysis clinical effectiveness of the use of LF and amoxicillin / clavulanate. Clinical efficacy when taking 500 mg LF 1 time per day was 95.2%, when taking LF 500 mg 2 times a day - 93.8%, and when taking amoxicillin / clavulanate 625 mg 3 times a day - 95.3 %.

A multicenter, open, randomized study compared the efficacy of Lf and ceftriaxone in combination with erythromycin in patients with community-acquired pneumonia at high risk of adverse outcome. In 132 patients receiving LF, the drug was initially administered intravenously (500 mg 1 time per day), then orally at the same dose for 7-14 days. In the comparison group, 137 patients received intravenous or intramuscular ceftriaxone (1-2 g 1 time per day) and intravenous erythromycin (500 mg 4 times a day), followed by a switch to oral amoxicillin / clavulanate (875 mg 2 times a day) together with clarithromycin (500 mg twice a day). Clinical efficacy in group 1 was 89.5%, in group 2 - 83.1%. Thus, LF monotherapy is not inferior in effectiveness to traditional combined treatment in patients with a high probability of death.

In the course of another multicenter randomized study in 456 patients with community-acquired pneumonia (group 1 - 226 patients received levofloxacin, group 2 - 230 patients received ceftriaxone and / or cefuroxime axetil), the clinical and microbiological efficacy of Lf administered intravenously (500 mg 1 time per day) was studied and / or orally (500 mg 1 time per day), compared with ceftriaxone administered intravenously (1.0-2.0 g 1-2 times a day) and / or cefuroxime axetil administered orally (500 mg 2 times a day). day). In addition, based on the specific clinical situation, 22% of patients in the second group were prescribed erythromycin orally (1 g 4 times a day). The clinical and microbiological efficacy of LF monotherapy was significantly higher than the traditional treatment regimen. Thus, the clinical success in patients of group 1 was 96%, in patients of group 2 - 90%, and the frequency of pathogen eradication in microbiologically examined patients was 98% and 85%, respectively.

The role and place of LF in the stepwise therapy of community-acquired pneumonia compared with conventional therapy was studied in a large Canadian study ( CAPITAL Study), which included 1743 patients. To resolve the issue of the place of treatment and the method of drug administration, the M.J. scale was used. Fine et al., 1997. If the final score of the patient did not exceed 90 points, then the treatment was carried out at home with the appointment of LF (500 mg 1 time / day, orally) for 10 days. If the final score was 91 or more points, then the patient was hospitalized and initially LF (500 mg 1 time / day) was administered intravenously. Upon reaching a stable state (ability to swallow food, negative results blood cultures, body temperature 38.0°C, respiratory rate<24/мин, частота сердечных сокращений <100/мин), лечение продолжалось с назначением оральной формы ЛФ (500 мг 1 раз/сутки). Использовали унифицированные критерии для выписки больного из стационара: возможность приема антибиотика внутрь; число лейкоцитов периферической крови < 12x109/л; стабильное течение сопутствующих заболеваний; нормальная оксигенация крови.

As a result, there were no significant differences in the frequency of repeated hospitalizations, mortality and quality of life among patients who received LF as part of a stepwise therapy, or with standard treatment. At the same time, the introduction of stepwise LF therapy led to an 18% reduction in bed-days for this nosological form and a reduction in costs by $1,700 (per patient).

The clinical efficacy and safety of Lf and some new macrolides (azithromycin, clarithromycin) in the treatment of community-acquired pneumonia was compared using a meta-analysis of randomized controlled trials. The rate of complete clinical recovery was clearly higher with LF (78.9%) than macrolides (57% azithromycin, 63.3% clarithromycin). A higher incidence of adverse drug events was noted with the use of LF - 36.6% (azithromycin - 12.6%, clarithromycin - 27.1%), but, according to the authors, the safety profile of LF practically does not differ from macrolides, and levofloxacin can be recommended as an effective tool in the treatment of community-acquired pneumonia.

The presented data allow us to conclude that clinical and microbiological efficacy of levofloxacin monotherapy is no less than that of traditional regimens for the treatment of community-acquired pneumonia .

A large number of studies have confirmed not only the clinical advantage of Lf, but also its economic superiority over other antibacterial drugs.

A study conducted at the Talahas Medical Center showed economic advantage of using LF in the treatment of community-acquired pneumonia in comparison with traditional parenteral therapy. Estimated savings averaged $111 per patient.

A multicentre, randomized, controlled trial conducted in 19 Canadian hospitals assessed the economic outcome of treating adult patients with community-acquired pneumonia. Hospitals were divided into two groups: those using the study approach and those using conventional standard therapy. The studied method of management included the use of LF as the antibiotic of choice, and the use of the PSSI (Pneumonia Severity Scoring Index) pneumonia severity index, according to which patients were divided into 5 classes and the question of the method of treatment was decided (outpatient or inpatient). In hospitals using the conventional approach, hospitalization decisions, antibiotic choices (with the exception of LF), and other decisions were made by the attending physicians. The analysis included 716 patients on the study method and 1027 patients on conventional therapy. In hospitals with the studied method, there were fewer hospitalizations than in hospitals with conventional therapy (46.5% and 62.2%, respectively, p = 0.01), there was also a reduction in the length of stay of patients in the hospital by an average of 1.6 days and savings of $457-994 per patient, without compromising clinical performance or quality of life.

A study conducted by the INOVA Health System showed that levofloxacin is a cost-effective alternative to ciprofloxacin for infectious diseases of various localizations (upper and lower respiratory tract, urinary tract, skin and soft tissues, etc.) and that the use of disease risk criteria (PSI) can reduce the frequency of justified hospitalizations for community-acquired pneumonia, which also leads to cost savings. In addition, experience has demonstrated the economic and clinical benefits of stepwise therapy.

Another large, multicentre, prospective, open-label, randomized, actively controlled, phase III study included 310 outpatients and 280 inpatients with community-acquired pneumonia treated with levofloxacin or cefuroxime axetil (IV or PO). Economic evaluation was performed only for outpatients. The economic benefit of LF was found to be as high as $233 per patient (p=0.008).

A study conducted at the University of Texas Cancer Center showed that the use of levofloxacin was safe, effective, and cost-effective in the treatment of community-acquired pneumonia in adults compared to b-lactam antibiotics, as well as clarithromycin. In this study, the sensitivity to the studied antibiotics was determined using the MIC and a high level of resistance of the main pathogens of pneumonia (pneumococcus, Haemophilus influenzae, moraxella) to b-lactams, an increase in the resistance of atypical pathogens to macrolides and, in contrast, a low level of resistance to LF. The frequent occurrence of allergic reactions to b-lactams in comparison with LF and the good tolerance of the latter also showed its advantage. The second study addressed the issue of optimal antibiotic therapy for community-acquired pneumonia in patients with various comorbid conditions (COPD, diabetes, chronic heart failure, alcoholism, nursing home stay, work on livestock farms, etc.). As a result, among all PCs, only levofloxacin was recommended for the management of community-acquired pneumonia.

The next study examined the replacement of other PCs with levofloxacin in pneumonia and other infections. A microbiological study, clinical and pharmacoeconomic evaluations were carried out. As a result, the replacement of a more expensive drug (levofloxacin) with cheaper ones (ofloxacin, ciprofloxacin) turned out to be more profitable.

Chronic bronchitis in the acute phase

According to a study by C.A. DeAbate (1997), the clinical and bacteriological efficacy of LF when taken at a dose of 500 mg 1 time per day for 5-7 days is comparable to 7-10 days of taking cefuroxime at a dose of 250 mg 2 times a day. Clinical efficacy was 94.5 and 92.6%, bacteriological - 97.4 and 92.6%, respectively.

According to M.P. Habib (1998), the clinical and bacteriological efficacy of a single dose of 500 mg of LF for 5-7 days is comparable to a 7-10-day intake of cefaclor at a dose of 250 mg 3 times a day. Clinical efficacy was 91.6 and 85%, bacteriological - 94.2 and 86.5%, respectively.

Nosocomial pneumonia

Gram-negative flora predominates in the etiology of nosocomial pneumonia ( Klebsiella sp., P. mirabilis, E. coli, H. influenzae, P. aeruginosa). From Gram-positive flora are found S. aureus, rarely pneumococci, often multiresistant strains. Fluoroquinolones have long been successfully used in the treatment of this pathology. Given the antimicrobial spectrum of LF, its appointment in nosocomial pneumonia can be fully justified. However, for suspected or confirmed infection P. aeruginosa combination antibiotic therapy is required, usually with antipseudomonal b-lactam antibiotics to prevent the development of resistance.

Conclusion

The experience with levofloxacin convincingly proves that it is a highly effective drug, comparable in terms of efficiency with other new fluoroquinolones. Almost equally, levofloxacin is effective against both gram-positive and gram-negative aerobic flora, and also has high activity against atypical pathogens. Levofloxacin has almost ideal pharmacokinetic parameters and two dosage forms, oral and parenteral, which allows you to optimize doses and treatment regimens as much as possible and use it as part of suppository therapy. The high bactericidal activity of levofloxacin in combination with high maximum concentrations, good tissue penetration, and AUC values ​​provide the maximum therapeutic effect.

Among other drugs of the PC group, levofloxacin has the best tolerance with a low level of side effects.

Currently, levofloxacin is successfully used mainly for infections of the lower respiratory tract. However, given the wide antimicrobial spectrum, optimal pharmacokinetic parameters, good tolerance, levofloxacin can be used for infections of almost any localization (sinusitis, infections of the urinary tract, skin and soft tissues, small pelvis, intra-abdominal infections, severe generalized infections, intestinal infections, infections transmitted sexually, etc.).

Formation of resistance to levofloxacin is possible, however, at present, resistance to the drug develops most slowly and does not cross with other antibiotics.

Along with high clinical efficacy, levofloxacin undoubtedly has pharmacoeconomic advantages, which is relevant in the modern healthcare system.

A huge number of infectious and inflammatory diseases caused by various pathogens forces doctors to use antibacterial drugs with a wide spectrum of action to combat them. Fluoroquinolones are especially popular. Ciprofloxacin and Levofloxacin earned the trust of doctors and patients, the comparison of which helps to understand in which cases this or that drug will achieve a positive result in the shortest possible time and without harm to the general condition of the patient.

Ciprofloxacin is one of the antibacterial drugs with a wide spectrum of activity and is used as a means to combat pathogens of inflammatory processes that affect organs:

1. respiration.
2. Urinary and reproductive systems.
3. Abdominal cavity.

Ciprofloxacin is highly effective when carrying out therapeutic measures aimed at eliminating the pathological process that occurs in the human body and provokes the development of:

1. Inflammation of the bronchi and lungs.
2. Cystic fibrosis.
3. Bronchiectasis.
4. Pharyngitis and inflammation of the maxillary sinuses (sinusitis).
5. Otitis, tonsillitis and sinusitis.
6. Infections in the kidneys, urinary tract, bladder and urethra.
7. Adnexitis and prostatitis.
8. Gonorrhea and chlamydia.
9. Diseases of the gastrointestinal tract (caused by the penetration of pathogenic bacteria).
10. Infections of the dermis and soft tissues.
11. Ailments affecting the bone frame and articular apparatus (osteomyelitis, septic arthritis).

Despite the fact that fluoroquinolones have long been highly popular among ENT doctors, their use is justified in the treatment of diseases affecting the male genitourinary system. So, in the treatment of prostatitis, Ciprofloxacin is prescribed more often than other antibiotics and allows you to achieve a complete recovery of the patient in the shortest possible time.

The drug is used as an agent that destroys pathogens that are highly sensitive to ciprofloxacin and bacteria that produce beta-lactamase. The drug "Ciprofloxacin" has a bactericidal effect, inhibits the production of bacterial DNA and is distinguished by its ability to suppress DNA gyrase.

The activity of the antibiotic is manifested in relation to:

1. Staphylo- and streptococci.
2. Shigella.
3. Salmonella.
4. Neisserium.
5. Chlamydia.
6. Mycoplasmas.
7. Clostridia.

Ciprofloxacin is rapidly absorbed into the mucosa of the gastrointestinal tract (gastrointestinal tract) regardless of food intake. It is well distributed in tissues and cells of the human body.

Despite the high effectiveness of the drug, there are contraindications to its use and the risk of side effects.

Among the conditions in which treatment with Ciprofloxacin is contraindicated:

1. Pregnancy (especially the first trimester).
2. The period of breastfeeding (lactation).
3. Younger children's age.
4. Individual intolerance to the active active ingredient and a high level of sensitivity to fluoroquinolones.

It is forbidden to use Ciprofloxacin as a medicine and in cases where the patient has not reached the age of 18 years.

The use of an antibiotic should be discontinued if side effects occur:

1. Nausea and frequent urge to vomit.
2. Digestive disorders (dyspepsia).
3. Changes in stool (diarrhea).
4. Failure of the heart rhythm and increased heart rate (tachycardia).
5. Violation of the functionality of the urinary system.
6. Appearance of blood in urine.
7. Pain in the stomach.
8. An increase in the content of bilirubin.

You should immediately inform your doctor about an allergic reaction that occurs, which manifests itself in the form of skin itching and rashes. Cancellation of the drug is possible if the patient has complaints of lack of sleep and appetite, the occurrence of hallucinations and increased irritability. Among other things, other forms of negative reaction are possible. We are talking about dizziness, fainting or blurred vision.

To avoid possible troubles, you should carefully study the instructions and strictly follow the instructions received from the attending physician regarding the dosing regimen and the schedule for taking the medication.

First of all, it must be taken into account that the duration of therapy using Ciprofloxacin should not exceed 10-14 days. During this time, the drug is taken in the form of capsules or tablets twice a day at 250, 500 or 750 mg. The daily dose for adult patients is 1.5 g.

Intravenous administration is carried out 2 r / d with an interval of 12 hours. A single dose of antibiotic does not exceed 400 mg. Despite the fact that jet intravenous administration of the solution is allowed, doctors in most cases recommend using a dropper, trying to ensure a gradual slow penetration into the body of the active active ingredient.

Using Ciprofloxacin in ophthalmology, instillations are carried out at intervals of 4 hours and 2 drops of a special solution are instilled into each eye (lower conjunctival sac).

In order to achieve a quick cure for patients, doctors are increasingly prescribing broad-spectrum antibacterial drugs that affect numerous pathogens. Among the drugs that are characterized by increased efficiency, Levofloxacin, which enjoys the well-deserved trust of ophthalmologists, therapists, urologists.

It is prescribed for the treatment of such complex and dangerous diseases as:

1. Community-acquired pneumonia.
2. Chronic bronchitis in the acute stage.
3. Acute sinusitis caused by the penetration of pathogenic bacteria into the body.
4. Acute pyelonephritis.
5. Infectious inflammatory diseases of the urinary tract.
6. Chronic bacterial prostatitis.
7. Purulent lesions of soft tissues and dermis (abscesses and furunculosis).

As one of the components of complex therapy, Levofloxacin is used in therapeutic measures aimed at combating tuberculosis.

The antimicrobial bactericidal effect of the drug is provided by its active ingredient - levofloxacin hemihydrate. The drug created on its basis has the ability to block DNA gyrase and cause significant morphological changes in the membranes and cells of pathogenic bacteria. This has a detrimental effect on pathogenic microorganisms and prevents their growth and reproduction.

Susceptibility to Levofloxacin has been found in many bacteria, including:

1. Streptococcus and Enterococcus.
2. Staphylococci and Klebsiella.
3. Morganella and Neisseria.
4. Chlamydia and mycoplasmas.
5. Rickettsia and ureaplasma.

After ingestion, the antibiotic is rapidly absorbed and easily penetrates into the lungs and bronchial mucosa, organs of the genitourinary system. Most of the composition is excreted during the day through the kidneys.

They take the antibacterial drug Levofloxacin, which is produced in tablet form, with plenty of clean water, without chewing or crushing beforehand. The daily dose of the drug, which is allowed to be divided into 2 doses, should not exceed 500 mg.

The duration of therapy depends on the severity of the disease, the location of the focus of inflammation and the stage of development of the disease. Of course, the age of the patient is also of great importance. The minimum course of therapy is 3 days, and the maximum is a week (in some cases, Levofloxacin can be taken for two weeks).

Despite the positive characteristics and high degree of effectiveness of the drug, it is able to provoke the appearance of side effects in the form of:

1. Nausea and vomiting.
2. Pain in the head and abdomen.
3. Sleep disturbances and lack of appetite.
4. Dyspepsia (indigestion) and diarrhea (diarrhea).
5. Acute renal failure and arthralgia.
6. Muscle weakness and tendon rupture.
7. Tremor (trembling) of the limbs and an unreasonable feeling of fear.
8. Insomnia and anxiety.
9. Increased sweating and increased blood sugar.

You should consult a doctor with a request to cancel the drug if an allergic reaction (skin rash and severe itching) occurs. It is strictly forbidden to make an independent decision on the need to use Levofloxacin as a drug for the treatment of complex and dangerous diseases. Otherwise, the patient risks provoking the development of a negative reaction from various organs and systems, worsening his condition and complicating further treatment.

Comparative characteristics

Comparison of Ciprofloxacin and Levofloxacin allows you to make the right choice before deciding on the need to use one or another drug for adequate quality therapy. Both drugs belong to antibiotics from a number of fluoroquinolones, however, Ciprofloxacin is a first-generation drug and a large number of pathogenic bacteria were able to develop resistance to it, while Levofloxacin is a new drug with increased efficiency.

The main difference that exists between the described broad-spectrum antibiotics is the active substance:

1. The drug "Levofloxacin" was created on the basis of the component of the same name.
2. The active ingredient in ciprofloxacin is ofloxacin.

Under the influence of ofloxacin, few pathogenic bacteria die. This is due to the fact that each group of bacteria has its own level of sensitivity. It was this fact that caused the choice of medicine only by a qualified doctor.

If the newest drug has excellent compatibility with other drugs and formulations, then the first generation antibiotic under the influence of other drugs significantly reduces its level of activity and concentration. This leads to the need to extend the course of therapy.

The attending physician determines the daily and single dosage of each antibiotic, taking into account the severity of the disease, the age of the patient, the need for additional medications and the localization of the focus of inflammation. No less important is the occurrence of side effects, with complaints about which patients turn to doctors in most cases, treated with Ciprofloxacin. From this point of view, Levofloxacin has a greater degree of safety, and therefore more often highly qualified specialists make their choice in its favor.

Ofloxacin refers to fluoroquinolones of the 1st generation - highly active antibacterial drugs that have become firmly established in medical practice. This group of drugs can be considered as an alternative to broad-spectrum antibiotics. It should be noted that the drugs of this group differ in pharmacokinetic properties and specific antibacterial activity. The group of fluoroquinolones includes ofloxacin and ciprofloxacin (available in the form of tablets and solution for injection).

Due to its structure and mechanism of action, ofloxacin has a high bactericidal activity comparable to that of third-generation cephalosporins. The drug is active against gram-negative and gram-positive microorganisms, including strains resistant to other antibacterial drugs, as well as strains of atypical intracellular pathogens.

Ofloxacin has an optimal pharmacokinetic profile, is well absorbed in the digestive tract (about 100%), due to the rapid penetration into the tissues at the site of infection, a high concentration of the drug is created, the half-life is 5-7 hours.

Ofloxacin can be administered simultaneously with many antibacterial drugs (macrolides, b-lactam antibiotics, cephalosporins). Due to this property, the drug is widely used as part of combination therapy for infectious diseases. Ofloxacin, unlike ciprofloxacin, retains its activity while using inhibitors of RNA polymerase synthesis (chloramphenicol and rifampicin).

According to the chemical structure, many fluoroquinolones, including those containing more than one fluorine atom, are bicyclic derivatives. As shown by the results of numerous studies (Padeyskaya EN, 1994, 1996), additional fluoridation does not change the spectrum and severity of antibacterial activity. The physicochemical properties that determine the features of the pharmacokinetics and antimicrobial activity of drugs in this group depend to a greater extent on their structure - bicyclicity or tricyclicity.

Ofloxacin belongs to the group of tricyclic monofluoroquinolones. Unlike ciprofloxacin, it is practically not metabolized in the liver. The bioavailability of ofloxacin when administered orally and parenterally is identical. Due to this, when replacing the injection method of administering the drug with oral dose adjustment is not required (one of the significant differences between ofloxacin and ciprofloxacin).

According to WHO recommendations, 200 mg of ofloxacin corresponds to 500 mg of ciprofloxacin.

It penetrates well into target organs (for example, in chronic prostatitis - into the tissue of the prostate gland). It should be noted that with prostatitis, the capsule of the prostate gland is practically impermeable to many antibacterial drugs.

There is a linear relationship between the dose of ofloxacin used and its concentration in tissues.

Ofloxacin is prescribed 1-2 times a day. Eating does not affect its absorption, however, when eating fatty foods, the absorption of ofloxacin slows down.

Ofloxacin, to a lesser extent than ciprofloxacin, interacts with other drugs, practically does not affect the kinetics of theophylline and sodium caffeine benzoate.

Ofloxacin is excreted mainly by the kidneys (more than 80%) unchanged, that is, this drug does not have the effect of primary passage through the liver. The concentration of ofloxacin in the feces is significantly lower than that of ciprofloxacin. However, this drug is more effective in bacterial diarrhea, as well as traveler's diarrhea. This is due to its more pronounced activity against staphylococci and salmonella. The antimicrobial activity of ofloxacin is most pronounced against gram-negative bacteria and intracellular pathogens (chlamydia, mycoplasmas, ureaplasmas), against streptococci and Pseudomonas aeruginosa, ofloxacin is less active.

The bactericidal efficacy of ofloxacin manifests itself quite quickly, the resistance of microorganisms to this drug rarely develops. This is due to its bactericidal mechanism of action, affecting only one DNA gyrase gene and topoisomerase.

In clinical practice, ofloxacin is the drug of choice or first-line alternative and is recommended for empirical therapy in many urogenital infections. Due to its good tolerability (the incidence of side effects is 1.3%), the high bioavailability of the drug in the form of tablets and the optimal spectrum of action (active against 94% of pathogens that cause infections of the urogenital tract, except for protozoa and anaerobes), it can be used on an outpatient basis. A significant advantage of ofloxacin in the treatment of urinary tract infections is its high concentration both in the renal parenchyma and in the pyelocaliceal apparatus. The results of clinical studies (Padeyskaya E.N., Yakovlev V.P., 1995; Lynne C., 1996) indicate that ofloxacin, when compared with other antibiotics, has a more pronounced antibacterial effect against chlamydia, and its effectiveness is comparable to other fluoroquinolones and doxycycline against mycoplasmas and ureaplasmas.

In acute cystitis, ofloxacin is the drug of choice. This disease is more often diagnosed in women (0.5–0.7 episodes per year per 1 woman).

In chronic cystitis in young people, especially in the presence of concomitant sexually transmitted infections (20-40% of cases caused by chlamydia, mycoplasmas and ureaplasmas), ofloxacin is a priority among other fluoroquinolones.

The frequency of detection of chlamydia in patients with gynecological profile is 40%. Basically, these are young women with infertility, inflammatory diseases of the pelvic organs, patients with a history of ectopic pregnancy. In 70% of patients, chlamydia is combined with infection with other microorganisms, which aggravates the course of the inflammatory process and requires the appointment of adequate therapy (combination with ureaplasma is detected in 33% of cases, with mycoplasma - in 21%, gardnerella - approximately 14%, fungi of the genus Candida- in 12.9%. Ofloxacin is effective against all of the listed pathogens, except for fungi of the genus Candida.

Ofloxacin- the only fluoroquinolone recommended by the Association of Urogenital Medicine and the Medical Society for the Study of Sexually Transmitted Diseases (USA) as an alternative drug of first choice for the treatment of patients with non-gonococcal urethritis and chlamydial infection of the urogenital tract (1999). The Centers for Disease Control and Prevention (USA, 1993) recommends the use of ofloxacin in combination with metronidazole or clindamycin for the outpatient treatment of patients with pelvic inflammatory disease.

A new drug of the fluoroquinolone group produced by Lechiva (Czech Republic) has been introduced to the Ukrainian pharmaceutical market. OFLOKSIN 200, which is registered in our country in the form of tablets of 200 mg (10 tablets per pack). Assessing the quality of OFLOKSIN 200, I would like to note that in terms of bioequivalence it fully complies with the original standard and GMP requirements. This means that patients are less likely to return to the doctor about relapses of the disease and the development of side effects. Offering OFLOKSIN 200 to a patient, you can be sure that the choice is made correctly.

ON THE. Gorchakova, prof., Dr. med. Sciences
National Medical University. A.A. Bogomolets

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