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Until relatively recently, the latest generation of fluoroquinolones—moxifloxacin and levofloxacin—were not seriously considered as treatments for severe infections (with the exception of severe pneumonia). Arguments against their use were the lack of a pronounced effect against some current pathogens (Pseudomonas aeruginosa, anaerobes - levofloxacin), the presence of effective antibiotics among drugs of other classes, and most importantly, the need to accumulate reliable material on the effectiveness of these drugs for “non-respiratory” diseases. However, it is now becoming clear that with increased attention to antimicrobial rotation as a factor in preventing pathogen resistance, these fluoroquinolones may be potentially useful in empirical antibiotic regimens and severe infections.

Fluoroquinolones in general and ciprofloxacin, which has the greatest activity against Pseudomonas aeruginosa in particular, have been successfully used for a long time to treat serious hospital infections [1, 2]. In terms of its antimicrobial spectrum, ciprofloxacin is generally comparable to aminoglycosides, but does not have the inherent nephro- and ototoxicity of the latter. At the same time, it is characterized by low activity against streptococci and no effect against actual anaerobes. Moxifloxacin belongs to the group of extended-spectrum fluoroquinolones. It exhibits increased activity against pneumococci, streptococci and staphylococci, is comparable to ciprofloxacin in its effect on Enterobacteriaceae (although it is inferior to it in its effect on Pseudomonas aeruginosa), but unlike ciprofloxacin it has a high bactericidal index against anaerobes, comparable to the “standard” antianaerobic agent - metronidazole [3]. Its activity against anaerobes does not differ from amoxicillin/clavulanate [4] and even carbapenems. This spectrum of action allows us to consider moxifloxacin as a promising antimicrobial agent for the treatment of mixed (including nosocomial) infections.

The effectiveness of moxifloxacin against P. aeruginosa is less than that of ceftazidime and other antibiotics with targeted “antipseudomonas” activity [5]. In principle, it is also less than that of ciprofloxacin. However, recently, evidence has been accumulating that the minimum inhibitory concentration (MIC) of ciprofloxacin for this pathogen is increasing, which indicates the formation of resistance and predetermines attempts to replace this drug with other antimicrobial agents.

Moxifloxacin inhibits enzymes of the topoisomerase class – DNA gyrase (topoisomerase II) and topoisomerase IV, which are the targets of fluoroquinolones in the bacterial cell and are responsible for changes in the spatial configuration of bacterial DNA IV [6]. DNA gyrase supercoils bacterial DNA, and topoisomerase IV separates daughter chromosomes during replication. The key point in the action of moxifloxacin is the formation of a three-component complex, bacterial DNA - enzyme - quinolone, which prevents the replication of bacterial DNA.

The level of bacterial activity of fluoroquinolones is determined by the degree of their affinity for topoisomerases. To suppress the vital activity of a microbial cell, it is sufficient to inhibit the activity of only one enzyme. This feature explains the fact that for all fluoroquinolone drugs it is possible to distinguish a primary and secondary target of action. The primary target is the enzyme for which a given fluoroquinolone exhibits the greatest affinity. In gram-negative bacteria, fluoroquinolones exhibit the greatest affinity for DNA gyrase, making this enzyme the primary target. In Gram-positive bacteria, the primary target of most drugs in this class is topoisomerase IV [7].

Only moxifloxacin has the same affinity for the two enzymes, which most contributes to the bactericidal effect and prevents the selection of resistant strains [8]. The main mechanism of resistance to fluoroquinolones is a change in the structure of topoisomerase as a result of mutations in the corresponding genes and amino acid substitutions in enzyme molecules. In the vast majority of cases, stability is formed in stages. After the occurrence and selection of mutations in the genes that control the enzyme that is the primary target, the MIC of fluoroquinolones increases 4–8 times. If you continue to administer the drugs, the second enzyme (secondary target) is suppressed, and the MIC increases another 4–8 times.

It is believed that it is the affinity for both topoisomerases that allows moxifloxacin to avoid the formation of stepwise mutations in bacteria and provide an almost constant effect on sensitive strains. This advantage of the drug is relevant for intensive care units, since it is the rapid selection of resistant strains of bacteria that poses the main threat to effective treatment of infection. The reliable effect of the drug is also confirmed by in vitro data. Its activity decreases only slightly with shifts in the pH of the environment in the range of 5.6–8.4 and remains virtually unchanged at inoculum values of 104–106 CFU/ml [9]. This circumstance is extremely important, since during infectious inflammation the pH values of the environment undergo fluctuations over a wide range, and the inoculum tends to rapidly increase.

It is believed that the maximum therapeutic effect of fluoroquinolones and a reduction in the risk of developing microbial resistance to them are achieved when the ratio of peak concentration to MIC is > 8–10, and the ratio of the area under the concentration-time curve (AUC) to MIC should be £ 125 for gram-negative microorganisms and Ћ 30 for gram-positive pathogens [10].

Even more accurate is to take into account the ratio of the AUC of the free fraction of the drug to the MIC. As is known, it is the free fraction of fluoroquinolones, not bound to proteins, that has pharmacological activity. With this approach, the optimal ratio for eliminating microorganisms and preventing microbial resistance is considered to be Ћ 25. For moxifloxacin, this figure is more than 50 (for ciprofloxacin, only 7); when it is reached, the elimination of sensitive microorganisms occurs within 12 hours [11].

Moxifloxacin is registered in Russia under the commercial name Avelox in dosage forms for enteral and intravenous administration. The bioavailability of moxifloxacin when taken orally is close to 100%, i.e. its concentrations after oral and intravenous administration are identical, which determines the same severity of the bactericidal effect in tissues [12]. In addition, it has a clinically significant post-antibiotic effect, which prolongs the effect of the drug up to 24 hours. The convenient mode of administration – once a day and the availability of enteral and parenteral dosage forms makes moxifloxacin one of the drugs of choice for “stepped” treatment tactics – first parenterally, then orally [13].

The results of the clinical use of moxifloxacin indicate its high effectiveness and good tolerability in pneumonia, exacerbation of chronic bronchitis, urogenital infections, and infections of the pelvic organs in women [14]. There are individual reports of the successful use of this drug in surgery, in particular for complicated infectious processes in ENT practice [15]. Particular attention is paid to the issues of “stepwise” use of moxifloxacin, which reduces the cost of treatment. It has been shown that the effectiveness of this method of use in severe pneumonia is comparable to the results of a parenteral course of beta-lactam antibiotics or their combination with antianaerobic agents.

The following features of the pharmacodynamics and pharmacokinetics of moxifloxacin allow us to count on its effectiveness for the prevention and treatment of surgical infections:

wide spectrum of antibacterial action against gram-positive and gram-negative aerobic and anaerobic bacteria;
simple and convenient dosing regimen – 400 mg once a day;
the ability to choose between intravenous or oral administration at the same dose and (if necessary and/or possible) conducting “stepped” therapy;
favorable safety and tolerability profile.

Let us note that if in outpatient practice the use of all fluoroquinolones in children is still contraindicated, then in the treatment of severe infections in a hospital, this restriction, in our opinion, should not be approached so strictly.

Moxifloxacin was officially included in the recommendations for the management of septic patients with community-acquired surgical infections of the abdominal cavity, as well as with a primary bacterial focus in the kidneys [16]. At the same time, we should not forget about the leading role of this drug in the treatment of severe respiratory tract infections. It is significant that in case of aspiration pneumonia with the formation of a cavity in the lung, moxifloxacin has advantages over many antibiotics and their combinations. Its effect extends to the anaerobic flora that occurs during this process; the drug penetrates well into this cavity [17]. The effectiveness of “stepped” therapy with moxifloxacin (intravenously for 3–4 days, then orally for 4–10 days) and those carried out using a combination therapy method that included amoxicillin/clavulanate and clarithromycin was almost equal (88 and 83%, respectively) [18]. Of course, monotherapy treatment should be considered preferable from a compliance point of view. In addition, it is better tolerated by patients.

Moxifloxacin demonstrates good activity against hospital strains of methicillin-sensitive staphylococci (in some cases against methicillin-resistant strains) and satisfactory activity against enterococci and even Pseudomonas aeruginosa with low MIC90 values [19]. It is the increased activity against gram-positive microorganisms that is considered one of the important advantages of moxifloxacin over previous generations of fluoroquinolones.

In cases of polymicrobial etiology of lung diseases (after artificial ventilation) with higher MIC90 values for moxifloxacin, it is recommended to combine this fluoroquinolone with amikacin [20]. Treatment with moxifloxacin after mechanical ventilation is also justified because after intravenous administration of the drug at a dose of 400 mg during the day, high bactericidal concentrations are established in the lung tissue, which cannot be achieved by administering some beta-lactam antibiotics and vancomycin [21].

Recently, Stenotrophomonus maltophilia has become one of the current causative agents of nosocomial infections. It is found in critically ill patients who have undergone massive antibiotic therapy with broad-spectrum drugs. The resistance of this pathogen is largely determined by the formation of antibiotic efflux. Moxifloxacin has good MIC90 values against S. maltophilia - 0.0625–0.5 μg/ml, surpassing ciprofloxacin in this regard (0.5–2 μg/ml). Suppression of the growth of this bacterium by moxifloxacin after a single dose is 1.5–2 times longer than by ciprofloxacin, and the number of mutated strains formed is several times less [22]. In addition, this problematic pathogen is able to protect itself from beta-lactam antibiotics using the biofilm it forms, which makes it impossible for these drugs to penetrate the microbial cell, which makes it impossible to ensure effective eradication. As recently shown, moxifloxacin, even at low concentrations (equal to half the MIC90), inhibits biofilm growth and provides a reliable bactericidal effect [23].

Moxifloxacin is considered as one of the effective agents for severe infections of the skin and soft tissues [24]. It is of particular relevance in patients with concomitant diabetes mellitus, with lesions of the skin and underlying structures, when there are polymicrobial associations of gram-positive aerobic and anaerobic flora.

It should be noted that there are no generic drugs of moxifloxacin on the domestic pharmaceutical market (contrast with “ciprofloxacins”), which guarantees all the above-described characteristics of action when using the original drug Avelox.

In conclusion, I would like to emphasize the authors’ understanding of the importance of the position according to which practical recommendations, in particular for the use of moxifloxacin for sepsis and other severe infections, should be based on the results of large international studies assessing the effectiveness and tolerability of the drug. However, given the great importance of the problem of treating these infections, the article makes an attempt, even before obtaining data from this type of research, to draw the attention of clinicians to the potential opportunities inherent in moxifloxacin, a modern antibacterial drug with a wide spectrum of action. Discovering these possibilities seems to be an urgent task for the specialists themselves, who in their daily work are faced with the problem of treating severe infections.

How to use

The daily dose of the drug is 400 mg. No dosage adjustment is required for patients with chronic pathologies of the liver and kidneys.

The tablets are swallowed without chewing and washed down with water. The medicine can be taken at any time, since food intake does not affect the absorption of the active component.

The infusion solution is administered once a day, preferably at approximately the same time each time. Eye drops are applied one drop 3 times a day.

The duration of the course depends on the type of pathogen and the location of inflammation. For chronic bronchitis, treatment lasts 5–10 days, for pneumonia - 10 days; Therapy for acute sinusitis continues for a week. For diseases of the pelvic organs, the medicine is taken daily for 2 weeks.

Moxifloxacin during pregnancy and breastfeeding

Due to the possibility of a destructive effect on the cartilage tissue of the fetus, taking pills while carrying a child is strictly contraindicated. If the mother's health is in danger, infusion administration is possible. In this case, the attending physician must carefully weigh the risks of such treatment.

Due to insufficient research on the danger of active components passing into breast milk during breastfeeding, antibiotics are not taken. In case of urgent need, feeding is interrupted.

Frequently asked questions about Moxifloxacin

Why is Moxifloxacin prescribed?

Antibacterial therapy is indicated in the treatment of acute and chronic inflammatory processes provoked by pathogenic microorganisms. The medicine is used in the treatment of sinusitis, bronchitis, pneumonia and diseases of the pelvic organs.

What group of antibiotics does Moxifloxacin belong to?

Moxifloxacin belongs to synthetic antibacterial agents from the group of fluoroquinolones. The drug is indicated for the treatment of infectious diseases caused by gram-positive and gram-negative bacteria.

How much should I take Moxifloxacin?

The course of treatment depends on the type of infection that caused the disease. As a rule, therapy lasts from 5 to 14 days.

How to replace Moxifloxacin?

The drug has a number of analogues with the same active ingredient. At Pharmacy 9-1-1 you can buy Moximac, Timoxi, Avelox tablets, Moxiflox, Moflax infusion solution, Tamveler eye drops, etc. Targeted delivery is possible for our clients.