Otitis

What are the names of the drugs cephalosporins and fluoroquinolones. Respiratory fluoroquinolones – expanding therapeutic options in the treatment of respiratory infections

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Fluoroquinolones - drugs belong to the group of quinolones and have antibacterial properties. Used in clinical practice of pulmonology, otolaryngology, urology, nephrology, dermatology, ophthalmology. The breadth of application is due to the spectrum of action and effectiveness of these drugs. However, they have a number of negative influences. Timely prescription of antibiotics strictly according to indications, in proper dosages, taking into account contraindications ensures the effectiveness and safety of therapy.

Approaches to systematization

The list of drugs of various fluoroquinolones and quinolones includes about 4 dozen drugs. They are divided by the presence or absence of a fluorine atom, by its quantity in the molecule (monophthoquinolones, diphthoquinolones), by the predominant spectrum of action (gram-negative, anaerobic), and area of application (respiratory).

The most complete picture is contained in the classification of quinolones into separate generations. This is the approach that is common in practice.

General classification of quinolones:

1st generation (non-fluorinated): nalidixic acid, oxolinic acid;
2nd generation (gram-negative): ciprofloxacin, norfloxacin, ofloxacin, lomefloxacin;
3rd generation (respiratory): levofloxacin, sparfloxacin, gatifloxacin;
4th generation (respiratory and antianaerobic): moxifloxacin, gemifloxacin.

Differences in chemical characteristics, spectrum of pathogens, and interaction with the patient’s body determine the place of each drug in therapy.

Pharmacological features

The mechanism of action of the drugs is due to the effect on bacterial enzymes involved in the formation of DNA and RNA. The result is an irreversible disruption of the synthesis of protein molecules of the microbial cell. Its viability decreases, the activity of toxic and enzymatic structures decreases, and the likelihood of the bacterial cell being captured by a phagocyte (an element of the human defense system) increases.

Fluoroquinolones prevent bacterial cell division

Representatives of all groups of fluoroquinolones influence the active bacterial cell and are also capable of disrupting any stage of its life cycle. They act on growing microorganisms and on cells at rest, when most medications are ineffective.

The therapeutic effect of fluoroquinolones is due to:

bactericidal effect;
penetration into the bacterial cell;
continuation of the antimicrobial effect after cessation of contact with the drug molecule;
creating high concentrations in the patient’s tissues and organs;
long-term removal of the drug from the body.

Nalidixic acid is the first member of the quinolones. The second drug was oxolinic acid, which had 3 times more activity than its predecessor. However, after the creation of 2nd generation fluoroquinolones (ciprofloxacin, norfloxacin), this drug is practically not used.

Of the quinolones, only nalidixic acid (nevigramone) is currently used. Indicated for urinary tract infections (pyelitis, cystitis, prostatitis, urethritis), to prevent intraoperative complications on the kidneys, ureter, bladder. Take up to 4 times a day (tablets).

Fluoroquinolones, like the next generation of quinolones, show changes in the spectrum of sensitive microbes, as well as pharmacokinetic properties (absorption, distribution and excretion from the body).

General advantages of fluoroquinolones compared to quinolones:

broad antimicrobial activity;
effective concentrations in internal organs when using tablet forms, independent of food intake;
good penetration into the respiratory organs, kidneys, urinary system, ENT organs;
to maintain therapeutic concentrations in the affected tissues, it is enough to prescribe 1-2 times a day;
side effects in the form of disruption of the digestive organs and nervous system occur less frequently;
are used for impaired renal function, although their excretion slows down with this pathology.

Today there are four generations of representatives of this group.

Application in clinical practice

The drugs have a very wide spectrum and act on most microorganisms. 2nd generation drugs primarily affect aerobic gram-negative bacteria (Salmonella, Shigella, Campylobacter, gonorrhea pathogen), and gram-positive bacteria (Staphylococcus aureus, tuberculosis pathogen).

At the same time, pneumococcus, opportunistic microorganisms (chlamydia, legionella, mycoplasma), as well as anaerobes are insensitive to them. Since pneumococcus is the main causative agent of pneumonia and often affects the ENT organs, the use of these drugs in otolaryngology and pulmonology has limitations.

Norfloxacin (2nd generation) has a wide spectrum of effects, but creates high therapeutic concentrations only in the urinary system. Therefore, the scope of its application is limited to nephrological and urological pathology.

Respiratory fluoroquinolones (3rd generation) have the same spectrum of influence as the drugs of the previous group, and also have an effect on pneumococci, including resistant forms, and on atypical microbes (chlamydia, mycoplasma). This made it possible to widely begin to use this group for the treatment of the respiratory system (breathing organs), as well as in general therapeutic practice.

Third generation fluoroquinolones are used to treat infections:

respiratory system;
kidney tissue;
urinary system;
eye;
paranasal sinuses;
skin and fatty tissue.

Fluoroquinolones of the 4th generation, the latest generation to date, have an effect on gram-positive, gram-negative flora, and are also effective against anaerobes that are not capable of sporulation. This expands the scope of their application, allowing them to be used for deep skin lesions with the development of anaerobic infection, aspiration pneumonia, intra-abdominal, and pelvic infections.

The advantage of modern fluoroquinolones is the ability to use only this medicine (monotherapy).

They are indicated for the same diseases as respiratory fluoroquinolones. At the same time, moskifloxacin affects resistant strains of staphylococci, and therefore can be used in the treatment of the most severe hospital-acquired pneumonia.

The great advantage of a number of these drugs (levofloxacin, pefloxacin) is the possibility of their use not only for oral administration, but also for intravenous administration. This ensures rapid delivery of the drug to the affected tissues, which can be decisive for severe patients. It is also possible to use so-called step therapy. When, upon receiving a positive result from the infusion method of administering the medication, they switch to tablet forms. The high availability of fluoroquinolones with this route of administration ensures effectiveness and helps avoid the negative consequences of administering large volumes of drugs intravenously.

Undesirable effects and contraindications for use

Like any medicine, fluoroquinolone antibiotics have a number of side effects. They must be distinguished from changes in the patient's condition that are caused by the underlying disease (for example, a temporary increase in body temperature) and indicate the therapeutic effect of medications.

List of side effects:

discomfort, pain in the stomach, loss of appetite, heartburn, nausea, vomiting, bowel disorders such as diarrhea;
sleep disturbances, headaches, dizziness, blurred vision and hearing, changes in sensitivity, convulsive twitching;
inflammation of cartilage tissue, tendon ruptures;
muscle pain;
transient inflammation of the renal tissue, mainly the interstitium (nephritis);
changes in the electrocardiogram, which may result in arrhythmias;
skin rash, which may be accompanied by itching, allergic swelling;
development of increased sensitivity to sunlight;
disturbances in the structure of the microbial flora of the body, the development of fungal infections of the oral mucosa and genital organs.

It is also extremely rare that pseudomembranous colitis develops with severe dysbacteriosis or intestinal damage by clostridia. This is a serious and dangerous intestinal disease. Therefore, if there are changes in stool, bloody or other impurities in the stool, or a wave of temperature that cannot be explained by the underlying disease, you should urgently consult a doctor.

Contraindications:

pregnancy at any stage;
breastfeeding period;
age less than 18 years;
allergy or reaction to taking quinolones and fluoroquinolones in the past.

Fluoroquinolones are not used to treat children due to the pronounced negative effect on the cartilage tissue of the growing body.

If necessary, these drugs are replaced with medications with a similar spectrum of influence on pathogens.

In case of heart disease with a threat of development of ventricular arrhythmias, in case of pathology of the liver and kidneys, it is necessary to carefully monitor the condition of these organs.

The spectrum of possible negative effects differs for different drugs. Therefore, the use of these drugs should be under the strict supervision of a physician.

The use of fluoroquinolones in diseases of the ENT organs

For inflammatory diseases of the nasal passages, oropharynx, tonsils, paranasal sinuses, and ear of an infectious nature, penicillin drugs, macrolides, cephalosporins and fluoroquinolones are used. 3rd and 4th generation drugs are used: levofloxacin, moxifloxacin, sparfloxacin. The advantage of these generations of drugs is that they affect pneumococci. It is these streptococci that in most cases are the causative agents, either alone or together with other microbes, of inflammatory diseases of the ENT organs and respiratory system.

Used for acute and chronic inflammatory processes caused by fluoroquinolone-sensitive antibiotics.

Most often used in therapy:

diseases of the paranasal sinuses;
rhinitis;
rhinosinusitis.

Fluoroquinolones are used when there is no effect from treatment with beta-lactams (penicillins and cephalosporins) and macrolides.

Thus, drugs of the fluoroquinolone group are among the most widely used in modern antibacterial therapy for adults. A thorough examination of the patient, identification of risks of negative effects, the most accurate selection of the drug for the microbial spectrum of pathogens of a particular disease, determination of the method and mode of administration ensures the positive effect of therapy, as well as its safety.

In recent years, synthetic antibacterial drugs have been increasingly used to treat various infections. This is due to the fact that many microorganisms develop resistance to antibiotics of natural origin. In addition, infectious diseases are becoming more and more severe, and it is not always possible to immediately determine the pathogen. Therefore, there is an increasing need for broad-spectrum antibacterial drugs to which most microorganisms are sensitive. One of the groups of the most effective drugs with such properties are fluoroquinolones. These drugs are obtained synthetically and have been widely known since the 80s of the 20th century. Clinical results from the use of these agents have proven that they are more effective than most known antibiotics.

What is a group of fluoroquinolones

Antibiotics are drugs that have antimicrobial activity and are most often of natural origin. Formally, fluoroquinolones are not classified as antibiotics. These are drugs of synthetic origin, obtained from quinolones by adding fluorine atoms. Depending on their quantity, they have different effectiveness and elimination period.

Once in the body, drugs from the fluoroquinolone group are distributed throughout all tissues, entering fluids, bones, penetrating the placenta and blood-brain barrier, as well as bacterial cells. They have the ability to suppress the work of the main enzyme of microorganisms, without which DNA synthesis stops. This unique action leads to the death of bacteria.

Because these drugs are quickly distributed throughout the body, they are more effective than most other antibiotics.

What microorganisms are fluoroquinolones active against?

These are broad-spectrum drugs. They are believed to be effective against most gram-positive and gram-negative bacteria, mycoplasmas, chlamydia, mycobacterium tuberculosis, and some protozoa. They destroy intestinal, pseudomonas and hemophilus influenzae, pneumococci, salmonella, shigella, listeria, meningococci and others. Intracellular microorganisms are also sensitive to them, which are difficult to deal with with other drugs.

Only various fungi and viruses, as well as the causative agents of syphilis, are insensitive to these drugs.

The advantage of using these drugs

Many severe and mixed infections can be cured only by fluoroquinolones. The drugs previously used for this purpose are now increasingly becoming ineffective. In comparison, fluoroquinolones are easier to tolerate by patients, are quickly absorbed, and microorganisms cannot yet develop resistance to them. In addition, medications in this group have other advantages:

What effect do fluoroquinolones have?

Antibiotics are drugs that cause many side effects. And now many microorganisms have become insensitive to such agents. Therefore, fluoroquinolones have become an excellent alternative to antibiotics in the treatment of infectious diseases. They have the unique property of stopping the reproduction of bacterial cells, which leads to their final death. This may explain the high effectiveness of drugs from the fluoroquinolone group. The peculiarities of their action also include high bioavailability. They penetrate into all tissues, organs and fluids of the human body in 2-3 hours. These drugs are excreted mainly in the urine. And they cause side effects much less often than antibiotics.

Indications for use

Antibacterial drugs of the fluoroquinolone group are widely used for nosocomial infections, severe infectious diseases of the respiratory tract and genitourinary system. Even such serious infections as anthrax, typhoid fever, and salmonellosis are easily treatable. They can replace most antibiotics. Fluoroquinolones are effective for the treatment of the following diseases:

chlamydia;
gonorrhea;
infectious prostatitis;
cystitis;
pyelonephritis;
typhoid fever;
dysentery;
salmonellosis;
pneumonia or chronic bronchitis;
tuberculosis.

Instructions for use of these drugs

Fluoroquinolones are most often available in tablet form for oral administration. But there is a solution for intramuscular administration, as well as drops in the eyes and ears. To obtain the desired therapeutic effect, you must follow all the doctor’s recommendations regarding dosage and characteristics of taking medications. The tablets must be taken with water. It is important to maintain the required interval between taking two doses. If it turns out that one dose of the drug is missed, you need to take the medicine as soon as possible, but not at the same time as the next dose.

When taking drugs from the fluoroquinolone group, you must follow your doctor's recommendations regarding their compatibility with other medications, because some of them can both reduce the antibacterial effect and increase the possibility of developing side effects. It is not recommended to stay in direct sunlight for a long time during treatment.

Special instructions for use

Currently, fluoroquinolones are considered the safest bactericidal agents. These drugs are prescribed to many categories of patients for whom other antibiotics are contraindicated. But there are still certain restrictions on their use. Fluoroquinolones are prohibited in the following cases:

children under 3 years old, and for some new generation drugs – up to 2 years old, but in childhood and adolescence they are used only in extreme cases;
during pregnancy and breastfeeding;
with atherosclerosis of cerebral vessels;
in case of individual intolerance to the components of the drugs.

When fluoroquinolones are prescribed together with anticidal agents, their effectiveness is reduced, so a break of several hours is needed between them. If these drugs are used together with methylxanthines or iron supplements, the toxic effect of quinolones increases.

Possible side effects

Of all the antibacterial agents, fluoroquinolones are the easiest to tolerate. These drugs can occasionally cause only the following side effects:

abdominal pain, heartburn, intestinal disorders;
headaches, dizziness;
sleep disorders;
convulsions, muscle tremors;
decreased vision or hearing;
tachycardia;
impaired liver or kidney function;
fungal diseases of the skin and mucous membranes;
increased sensitivity to ultraviolet radiation.

Classification of fluoroquinolones

There are now four generations of drugs in this group.
They began to be synthesized in the 60s, but they gained fame only at the end of the century. There are 4 groups of fluoroquinolones depending on the time of appearance and effectiveness.

The first generation are agents with low effectiveness against gram-positive bacteria. These fluoroquinolones include drugs containing oxolinic acid or nalidixic acid.
Second generation drugs are active against bacteria that are insensitive to penicillins. They also act on atypical microorganisms. These fluoroquinolones are often used for severe infections of the respiratory tract and digestive tract. Drugs in this group include the following: “Ciprofloxacin”, “Ofloxacin”, “Lomefloxacin” and others.
3rd generation fluoroquinolones are also called respiratory, as they are especially effective against infections of the upper and lower respiratory tract. These are Sparfloxacin and Levofloxacin.
The 4th generation of drugs in this group has appeared recently. They are active against anaerobic infections. So far, only one drug is widespread - Moxifloxacin.

1st and 2nd generation fluoroquinolones

The first mentions of drugs in this group can be found in the 60s of the 20th century. At first, such fluoroquinolones were used against infections of the genital tract and intestines. The drugs, the list of which is now known only to doctors, since they are almost never used, had low effectiveness. These are drugs based on nalidixic acid: “Negram”, “Nevigramon”. These first generation drugs were called quinolones. They caused many side effects, and many bacteria were insensitive to them.

But research on these drugs continued, and 20 years later, 2nd generation fluoroquinolones appeared. They got their names due to the introduction of fluorine atoms into the quinolone molecule. This increased the effectiveness of the drugs and reduced the number of side effects. The second generation of fluoroquinolones include:

3rd and 4th generation drugs

Research on these drugs has continued. And now modern fluoroquinolones are considered the most effective. The list of 3rd and 4th generation drugs is not yet very large, since not all have yet passed clinical trials and are approved for use. They are highly effective and have the ability to quickly penetrate all organs and tissues. Therefore, these drugs are used for severe infections of the respiratory tract, genitourinary system, digestive tract, skin and joints. These include Levofloxacin, also known as Tavanic. It is even effective in treating anthrax. Fourth-generation fluoroquinolones include Moxifloxacin (or Avelox), which is active against anaerobic bacteria. These new drugs do not have most of the disadvantages of other drugs, are easier to tolerate by patients and are more effective.

Fluoroquinolones are one of the most effective drugs for the treatment of severe infectious diseases. But they can only be used after a doctor’s prescription.

13. CLINICAL AND PHARMACOLOGICAL CHARACTERISTICS OF FLUOROQUINOLONES

Fluoroquinolones are one of the most common and used groups of antimicrobial drugs due to their high activity against a wide range of gram-negative and some gram-positive pathogens. In terms of the number of drugs included in this group, they are second only to beta-lactams

antibiotics. Fluoroquinolones are the result of “pure” chemical synthesis.

The first fluoroquinolones began to be used clinically

practice in the early 80s of the last century. It only took a quarter of a century for them to occupy one of the leading places in the chemotherapy of infections of various origins and localizations.

There are a number of classifications, the vast majority of which include quinolones. One of the common classifications proposed by Quintilliani R. et al. in 1999, presented in table. 1.

The classification reflects, on the one hand, the generation, and on the other, the expansion of the spectrum of antimicrobial action of fluoroquinolones with an emphasis on microbes that are less susceptible or not prone to the action of fluoroquinolones of previous generations.

Table 1

Pharmacokinetics

Fluoroquinolones are well absorbed from the gastrointestinal tract, reaching a maximum concentration in the body's media in the first 3 hours and circulating in them in therapeutic concentrations for 5–10 hours, which allows them to be prescribed 2 times a day. Eating slows down absorption, but does not affect its completeness. The bioavailability of fluoroquinolones when taken orally reaches 80–100%. The only exception is norfloxacin with a bioavailability of 35–40%. Fluoroquinolones penetrate well into various tissues of the body, creating concentrations close to or exceeding serum concentrations. This is due to their physicochemical properties: high lipophilicity and low protein binding. In the tissues of the gastrointestinal tract, genitourinary and respiratory tract, kidneys, synovial fluid, their concentration is more than 150% relative to serum, the penetration rate of fluoroquinolones into sputum, skin, muscles, uterus, inflammatory fluid and saliva is 50–150%, and in the spinal brain fluid, fat and eye tissue - less than 50%.

Fluoroquinolones penetrate well not only into the cells of the human body (polymorphonuclear neutrophils, macrophages, alveolar macrophages), but also into microbial cells, which is important in the treatment of infections with intracellular localization of microbes.

Elimination of fluoroquinolones in the body is carried out renal and extrarenal(biotransformation in the liver, excretion in bile, excretion in feces, etc.) by. Ofloxacin and lomefloxacin are excreted almost completely by the renal route, predominantly by extrarenal mechanisms - pefloxacin and sparfloxacin; other drugs occupy an intermediate position.

Pharmacodynamics

The mechanism of action of fluoroquinolones is based on inhibition of DNA gyrase or microbial topoisomerase IV, which explains the lack of cross-resistance with other classes of antimicrobial drugs. Resistance to fluoroquinolones develops relatively slowly. It is associated with mutations in the genes encoding DNA gyrase or topoisomerase IV, as well as with disruption of their transport through porin channels in the outer cell membrane of the microbe or removal from it by activation of efflux proteins.

Antimicrobial spectrum

The spectrum of antimicrobial action of fluoroquinolones covers aerobic and anaerobic bacteria, mycobacteria, chlamydia, mycoplasma, rickettsia, borelia and some protozoa.

Table 2

Fluoroquinolones have natural activity against gram-negative bacteria of the families Enterobacteriaceae (Citrobacter, Enterobacter, Escherichia coli, Klebsiella, Proteus, Providencia, Salmonella, Shigella, Yersinia), Neisseriae (gonorrhoeae, meningitidis), Haemophilus and Moraxella, and are highly active against Legionella, Mycoplasma and Chlamydia , and also exhibit, although less, activity against non-fermenting gram-negative bacteria, gram-positive cocci, mycobacteria and anaerobes. Different fluoroquinolones have different effects on both different groups and individual types of microbes.

Most streptococci are insensitive to second generation fluoroquinolones(in particular pneumococcus), enterococci, chlamydia, mycoplasma. They have no effect on spirochetes, listeria and most anaerobes.

III generation fluoroquinolones compared to the 2nd generation they have more high activity against pneumococci(including penicillin-resistant) and atypical pathogens(chlamydia, mycoplasma).

Fluoroquinolones IV generation by antipneumococcal activity and effect on atypical pathogens superior to drugs of previous generations, also showing high activity against non-spore-forming anaerobes, due to which they are also used for intra-abdominal and pelvic infections, even as monotherapy.

Indications for use in clinical practice

First generation quinolones:

– Urinary tract infections: acute cystitis, anti-relapse therapy for chronic forms of infections (should not be used for acute pyelonephritis).

– Intestinal infections: shigellosis, bacterial enterocolitis (nalidixic acid).

Fluoroquinolones:

– Upper respiratory tract infections: sinusitis, especially caused by multidrug-resistant strains, malignant otitis externa.

– Lower respiratory tract infections: exacerbation of chronic bronchitis, community-acquired and nosocomial pneumonia, legionellosis.

– Intestinal infections: shigellosis, typhoid fever, generalized salmonellosis, yersiniosis, cholera.

– Anthrax.

– Intra-abdominal infections.

– Infections of the pelvic organs.

– Urinary tract infections (cystitis, pyelonephritis).

- Prostatitis.

- Gonorrhea.

– Infections of the skin, soft tissues, bones and joints.

– Eye infections.

– Meningitis caused by gram-negative microflora ( ciprofloxacin).

- Sepsis.

– Bacterial infections in patients with cystic fibrosis.

– Neutropenic fever.

– Tuberculosis (ciprofloxacin, ofloxacin and lomefloxacin in combination therapy for drug-resistant tuberculosis).

Norfloxacin, taking into account the pharmacokinetics, is used only for intestinal infections, urinary tract infections and prostatitis.

An important advantage of fluoroquinolones is the high effectiveness of monotherapy for infections caused by a wide range of aerobic gram-negative bacteria and pathogens with intracellular localization. However, for mycobacteriosis, aerobic-anaerobic and streptococcal (from various groups of streptococci) infections, they should be used only in combination therapy regimens.

It should be remembered that fluoroquinolones are not indicated for enterococcal infections, protozoal diseases, mycoses, viral infections, syphilis and some other conditions.

Second-generation fluoroquinolones, due to their low natural activity against gram-positive microbes, primarily Streptococcus pneumoniae, are not recommended for the treatment of community-acquired respiratory infections. On the contrary, fluoroquinolones of the III and IV generations, in addition to high antimicrobial activity, are characterized by free penetration into the non-cellular and cellular structures of the respiratory tract, due to which their concentrations here are higher than in blood serum, which

Fluoroquinolones of III and IV generations have bactericidal activity

with a post-antibiotic effect and are characterized by long-term circulation in the body with a long half-life. Thanks to this, they are prescribed only once a day, which is very convenient in practice.

Table 3

Preparation

Dosage form

Dosage regimen

Nalidixova

Capsules 0.5 g.

Table 0.5 g

Adults: 0.5–1.0 g every 6 hours.

Children over 3 months: 55 mg/kg per day. in 4 doses

Ciprofloxacin

(Ciprofloxacinum)

Table 0.25 g; 0.5 g;

0.75 g; 0.1 g.

0.2% Solution for inf. (0.1 and

0.2 g) per bottle. 50 ml and 100 ml.

Conc. d/inf. 0.1 g

in amp. 10 ml.

Eye/ear

drops 0.3% in dropper bottles of 5 and 10 ml.

Eye ointment 0.3% in tubes of 3 and 5 g.

Adults: 0.25–0.75 g every 12 hours;

for acute cystitis in women - up to 0.5 g every 12 hours for 7-14 days;

for acute gonorrhea – 0.5 g once.

Adults: 0.4–0.6 g every 12 hours.

Administer by slow infusion over 1 hour.

Eye drops: instill 1-2 drops. into the affected eye every 4 hours, in severe cases - every hour until improvement.

Ear drops are instilled in 2-3 drops. into the affected ear 4-6 times a day, in severe cases - every 2-3 hours, gradually reducing until improvement.

Eye ointment is placed behind the lower eyelid of the affected eye 3-5 times a day.

Levofloxacin

Table 0.25 g; 0.5 g

5% Solution for inf.

into the bottle 100 ml each

Orally (without chewing, with water).

Adults: 0.25–0.5 g every 12–24 hours; for pneumonia and severe forms of infections - 0.5 g every 12 hours for up to 14 days.

Adults: 0.25–0.5 g every 12–24 hours. Administer by slow infusion over 1 hour.

Side effects

Fluoroquinolones are generally well tolerated both when administered orally and intravenously. Side effects are rare, but if they occur, they are most often from the digestive tract and the central nervous system.

In the first case, this is nausea, vomiting, diarrhea, heartburn, pain, disorders

taste, constipation, dyspepsia, glossitis, stomatitis, candidiasis and others. In the second - dizziness, headache, sleep disturbance, paresthesia, tremors, convulsions, hearing impairment, nervousness, dreams.

Dangerous side effects, the manifestation of which requires discontinuation of the drug:

1) Epilepsy, seizures (especially while taking NSAIDs)

2) Based on experimental data on animals, the use of quinolones is not recommended during the formation of the osteoarticular system (inhibition of the development of cartilage tissue). Oxolinic acid is contraindicated in children under 2 years of age, pipemidic acid - up to 1 year, nalidixic acid - up to 3 months.

3) Tendinitis (there are reports of isolated cases of rupture of skeletal muscle tendons (mainly in elderly patients taking steroid drugs)).

4) Risk of photosensitivity.

5) Prolongation of the QT interval - risk of ventricular arrhythmias

6) Allergic reactions are possible in the form of itching, rash, angioneurotic edema.

In patients with carbohydrate metabolism disorders, primarily diabetes mellitus, renal failure, as well as in the elderly, it is recommended to use antimicrobial drugs of other groups instead of IV generation fluoroquinolones.

Contraindications

For all quinolones:

– Allergic reaction to drugs of the quinolone group. Cross to all drugs of the quinolone group!!!

– Glucose-6-phosphate dehydrogenase deficiency.

- Pregnancy.

Additionally for first generation quinolones:

– Severe liver and kidney dysfunction.

– Severe cerebral atherosclerosis.

Additionally for all fluoroquinolones:

– Children's age.

– Breastfeeding. Quinolones pass into breast milk in small quantities. According to some reports, they can cause hemolytic anemia in newborns whose mothers took nalidixic acid during breastfeeding. Therefore, nursing mothers are recommended to transfer their child to artificial feeding during treatment with quinolones.

Prescription to children is allowed only for health reasons (exacerbation of infection in cystic fibrosis; severe infections of various localizations caused by multidrug-resistant strains of bacteria;

infections with neutropenia).

Diseases of the central nervous system. Quinolones excite the central nervous system and are not recommended for use in patients with a history of seizures.

When using nalidixic acid, intracranial pressure may increase.

Impaired kidney and liver function. First generation quinolones cannot be used in cases of renal and hepatic failure, since the risk of toxic effects increases due to the accumulation of drugs and their metabolites. Doses of fluoroquinolones in severe renal failure are subject to adjustment.

Drug interactions

When used simultaneously with antacids and other drugs containing magnesium, zinc, iron, bismuth ions, may bioavailability decreases quinolones due to the formation of non-absorbable chelate complexes.

Pipemidic acid, ciprofloxacin, norfloxacin and pefloxacin may slow down the elimination of methylxanthines(theophylline, caffeine) and increase the risk of their toxic effects.

The risk of neurotoxic effects of quinolones increases when combined with NSAIDs, nitroimidazole derivatives and methylxanthines.

Quinolones exhibit antagonism with nitrofuran derivatives, so combinations with these drugs should be avoided.

First generation quinolones ciprofloxacin and norfloxacin may interfere with the metabolism of indirect anticoagulants in the liver, which leads to an increase in prothrombin time and the risk of bleeding. If used concomitantly, dose adjustment of the anticoagulant may be required.

Fluoroquinolones should be administered with caution concomitantly with drugs that prolong the QT interval, as the risk of developing cardiac arrhythmias increases.

When used simultaneously with GCS, the risk of tendon rupture increases, especially in the elderly.

When using ciprofloxacin, norfloxacin and pefloxacin together with drugs that alkalinize the urine (carbonic anhydrase inhibitors, citrates, sodium bicarbonate), the risk of crystalluria and nephrotoxic effects increases.

Even a schoolchild knows why antibiotics are needed in our time. But the phrase “broad spectrum” sometimes raises questions among patients. Why “wide”? Perhaps there will be less harm from an antibiotic with a “narrow” spectrum?

Bacteria are very ancient, most often unicellular, nuclear-free microorganisms that live in soil, water, humans and animals. “Good” bifidobacteria and lactobacilli live in the human body, these bacteria form human microflora.

Together with them, there are other microorganisms, they are called conditionally pathogenic. During illness and stress, the immune system malfunctions and these bacteria become completely unfriendly. And of course, various microbes enter the body and cause diseases.

Scientists divided bacteria into two groups, gram-positive (Gram +) and gram-negative (Gram -). Corynebacteria, staphylococci, listeria, streptococci, enterococci, clostridia belong to the gram-positive group of bacteria. Pathogens of this group, as a rule, cause diseases of the ear, eyes, bronchi, lungs, nasopharynx, etc.

Gram-negative bacteria negatively affects the intestines and the genitourinary system. Such pathogens include Escherichia coli, Moraxella, Salmonella, Klebsiella, Shigella, etc.

Based on this bacterial separation, antibacterial therapy is prescribed to treat diseases caused by certain pathogens. If the disease is “standard” or there is a result of bacterial culture, the doctor prescribes an antibiotic that will cope with pathogens belonging to one of the groups. When there is no time for analysis and the doctor doubts the identity of the pathogen, then antibiotics that have a wider spectrum of action are prescribed for treatment. These antibiotics are bactericidal against a large number of pathogens.

Such antibiotics are divided into groups. One of them is the group of fluoroquinolones.

Quinolones and fluoroquinolones

Drugs of the quinolone class began to be used in medical practice since the early 60s of the last century. Quinolones are divided into non-fluorinated quinolones and fluoroquinolones.

Non-fluorinated quinolones have an antibacterial effect mainly on gram-negative bacteria.
Fluoroquinolones have a much wider spectrum of action. In addition to influencing a number of Gram bacteria, fluoroquinolones also successfully fight Gram-positive bacteria. Fluoroquinolone antibiotics show a high bactericidal effect, thanks to this, medications for topical use (drops, ointments) have been developed, which are used in the treatment of diseases of the ears and eyes.

Four generations of drugs

1st generation quinolones are called non-fluorinated quinolones. It consists of oxolinic, nalidixic and pipemidic acids. For example, uroantiseptic drugs Negram and Nevigramon are produced based on nalidixic acid. These antibiotics are bactericidal against Salmonella, Klebsiella, Shigella, but do not cope well with anaerobic bacteria and Gram+ bacteria.
The 2nd generation of fluoroquinolone drugs consists of the following antibiotics : norfloxacin, lomefloxacin, ofloxacin, pefloxacin, and ciprofloxacin. With the introduction of fluorine atoms into quinolone molecules, the latter became known as fluoroquinolones. 2nd generation fluoroquinolones fight well against a large number of Gram-cocci and bacilli (Shigella, Salmonella, gonococci, etc.). With gram-positive bacilli (listeria, corynebacteria, etc.), legionella, staphylococcus, etc. Ciprofloxacin, lomefloxacin and ofloxacin suppress the increase in mycobacteria that cause tuberculosis, but at the same time show little activity in the fight against pneumococci, chlamydia, mycoplasmas and anaerobic bacteria.

Names of drugs containing 2nd generation fluoroquinolones

Ciprofloxacin(Tsiprolet, Floximet) is prescribed for the treatment of otitis media and sinusitis. For diseases of the genitourinary system - cystitis, prostate, pyelonephritis. For the treatment of gastrointestinal diseases, for example, bacterial diarrhea. In gynecology - adnexitis, endometritis, salpingitis, pelvic abscess. For purulent arthritis, cholecystitis, peritonitis, gonorrhea, etc. In drop form, it is used for eye diseases, such as ceraconjunctivitis and keratitis, blepharitis, etc.
Pefloxacin(Perti, Abaktal, Unikpef) is prescribed for the treatment of urinary tract infections. Relevant for the treatment of severe forms of gastrointestinal diseases, for example, salmonellosis. Effective for bacterial prostatitis and gonorrhea. It is used in the treatment of patients whose immune status is impaired. It is used to treat diseases of the nasopharynx, throat, lower respiratory tract, etc. It passes through the physiological barrier between the circulatory and central nervous systems better than other fluoroquinolones.
Ofloxacin(Uniflox, Floxal, Zanotsin) treats sinusitis and otitis media. Active against bacteria that cause urinary tract diseases. Suitable for the treatment of gonorrhea, chlamydia, meningitis. With local treatment with a drop form of an antibiotic or ointment, eye diseases such as barley, corneal ulcers, conjunctivitis, etc. are treated. Among 2nd generation antibiotics, Ofloxacin is most effective against pneumococci and chlamydia.
Lomefloxacin(Lomflox, Lomatsin). Some groups of streptococcus and anaerobic bacteria are resistant to the drug, but this antibiotic is highly active against a large number of microorganisms even in the smallest concentrations. It is used to treat patients with tuberculosis as part of complex therapy. Prescribed for the treatment of diseases of the genitourinary system, for topical use in the treatment of diseases in ophthalmology, etc. It has little activity in the fight against pneumococci, mycoplasmas and chlamydia.
Norfloxacin(Norbactin, Normax, Norphlogexal) are used in the treatment of diseases in ophthalmology, urology, gynecology, etc.

3rd generation fluoroquinolones

3rd generation fluoroquinolones are also called respiratory fluoroquinolones. These antibiotics have the same wide spectrum of influence as the fluoroquinolones of the previous generation, and are also superior to them in the fight against pneumococci, chlamydia, mycoplasmas and other pathogens of respiratory infections. Due to this, the 3rd generation of fluoroquinolone drugs is often used to treat diseases of the respiratory system.

Names of drugs containing 3rd generation fluoroquinolones

Levofloxacin(Floracid, Levostar, Levolet R) is 2 times more potent against bacteria than its 2nd generation predecessor ofloxacin. It is used in the treatment of infections of the lower respiratory system and ENT organs (otitis media, sinusitis). Prescribed for diseases of the genitourinary tract, chronic prostatitis, sexually transmitted diseases, and in the treatment of acute pyelonephritis. In the form of drops, this antibiotic is used in ophthalmology for eye infections. Better tolerated than the 2nd generation antibiotic ofloxacin.
Sparfloxacin(Sparflo, Sparbakt) in terms of the breadth of the spectrum of activity, this antibiotic is closest to Levofloxacin. It is highly effective in the fight against mycobacteria. The duration of action is longer than that of other fluoroquinolones. Used to fight bacteria in the paranasal sinuses and middle ear. In the treatment of diseases of the kidneys, reproductive system, bacterial damage to the skin and soft tissues, infections of the gastrointestinal tract, bones, joints, etc.

4th generation

4th generation fluoroquinolone drugs include the following the most famous drugs: moxifloxacin, gemifloxacin, gatifloxacin.

Medicines containing 4th generation fluoroquinolones

Gemifloxacin (Faktiv) is used in the treatment of pneumonia, chronic bronchitis, sinusitis, etc.
Gatifloxacin (Zymar, Gatispan, Zarquin). The bioavailability of this antibiotic is very high, about 96%, when taken orally. Quite large concentrations are recorded in the lung tissue, middle ear, lining of the bronchi, sperm, mucous membrane of the paranasal sinuses, and ovaries. Prescribed for the treatment of diseases of the ENT organs, sexually transmitted diseases, diseases of the skin and joints. The drug is used to treat bronchitis, pneumonia, cystic fibrosis, bacterial conjunctivitis and other diseases caused by antibiotic-sensitive bacteria.
Moxifloxacin (Avelox, Vigamox). In vitro studies have shown that this antibiotic is better than other fluoroquinolones in treating infections caused by pneumococci, chlamydia, mycoplasmas, and anaerobes. Prescribed by doctors for bronchitis, pneumonia, sinusitis, infectious lesions of the skin and soft tissues. Treats inflammation of the pelvic organs. In the form of a liquid, it is used in ophthalmology for the local treatment of barley, conjunctevitis, blepharitis, and corneal ulcers. The superiority of this latest generation fluoroquinolone over previous generations is also determined by its pharmacokinetic properties:
1. High bactericidal concentrations in various organs and tissues are ensured by its good penetration.
2. The antibiotic can be used up to once a day due to its long circulation in the body.
3. The absorption of this fluoroquinolone is not affected by food intake.
4. The absolute bioavailability of the drug after oral administration ranges from 85% to 93%.

Several fluoroquinolone drugs, namely moxifloxacin, gatifloxacin, ciprofloxacin, lomefloxacin, levofloxacin, ofloxacin, sparfloxacin, were included in the list vital and essential medicines, approved by the Government of the Russian Federation.

What should a doctor do if his patient is allergic to antibiotics? Until recently, this question perplexed almost every therapist. Since the 60s of the last century, the answer to it has been found: quinolones. In modern medicine, drugs based on their derivatives are used - fluoroquinolones. How they work and how they differ from antibiotics will be discussed in the article below.

What are fluoroquinolones

This is a group of medications with a pronounced antimicrobial effect. Medicines in this category are used as antibiotics with a wide range of applications. However, these substances are not antibiotics in the full sense of the word. They have no natural analogue and differ from them in their structure.

A special feature of fluoroquinolones is the presence of a fluorine atom in the structure. This is where the name of the group came from. The second distinguishing feature in the structures is the presence of a piperazine ring.

Fluoroquinolones are called second generation quinolones. Compared to their predecessors, fluoroquinolones have a high degree of activity.

Classification

Fluoroquinolones are classified by generation:

I generation: nalidixic and oxolinic acids. They belong to non-fluorinated quinolones.
II generation: ofloxacin, norfloxacin, lomefloxacin, ciprofloxacin. Gram-negative substances.
III generation: sparfloxacin, levofloxacin and gatifloxacin. Respiratory fluoroquinolones.
IV generation: gemifloxacin and moxifloxacin. They belong to the category of antianaerobic and respiratory substances.

List of drugs

Gatifloxacin

According to the list of fluoroquinolone drugs by generation, this substance belongs to the 4th generation. Release form: tablets and solution. Main substance: gatifloxacin. Indications for use: acute forms of otitis and sinusitis, gonorrhea, pneumonia, infections of joints, skin and bones, bronchitis, cystic fibrosis.

Contraindications: minor children, pregnancy, allergy to the drug.

Side effects: fever, sweating, tachycardia, gastrointestinal disorders, arrhythmia, hematuria, visual impairment.

Analogues: Gatispan, Tekvin, Tabris, Zarquin, Gatimak, Gatigem, Zikvin.

Gemifloxacin

A pharmacological drug with this name is not officially registered. Gemifloxacin is the name of the active substance in many medicines. Indications for use: infectious diseases, exacerbation of chronic bronchitis, sinusitis in the acute stage.

Contraindications: hypersensitivity to the substance, pregnancy and breastfeeding, increased QT interval on the electrocardiogram, age under 18 years.

Side effects: allergic reactions, disorders of the central nervous system (dizziness, tremors of the limbs, fear), changes in the functioning of the senses, renal failure.

Medicine containing gemifloxacin: tablets Faktiv.

Grepafloxacin

This active substance is available in medications under different trade names. Indications for use: pneumonia (including atypical), gonorrhea, exacerbation of bronchitis, cervicitis and urethritis.

Contraindications: epilepsy, conditions predisposing to heart rhythm disturbances, pregnancy and lactation, allergies, age less than 18 years.

Side effects: allergies, dizziness, states of panic and fear, disturbances in the functioning of the organs of vision, hearing and taste, vomiting, loss of appetite, constipation.

Medicine containing grepafloxacin: Raksar.

Levofloxacin

An antibacterial drug from the fluoroquinolone group, belonging to the 3rd generation. Active ingredient: levofloxacin. Release form: tablets, eye drops, injection solution.

Indications for use: tablets are used to treat infectious diseases of the upper and lower respiratory tract, prostatitis, skin and urinary tract infections, bacteremia. Eye drops are used to treat eye infections. The solution is used to treat infections of the upper and lower respiratory tract and ENT organs.

Contraindications: pregnancy and lactation, renal failure, age under 18 years, epilepsy.

Side effects: diarrhea, increased activity of liver enzymes, nausea.

Analogues:

for drops - Tsipromed, Ophthalmol;
for tablets - Xenaquin, Sparflo, Levoflox, Remedy, Hyleflox, Tanflomed, Maklevo, Lefoccin, Glevo;
for solution - Basijen, Cipronate, Leflobact.

Lomefloxacin

A Russian drug based on the active substance is lomefloxacin. Release form: tablets. Indications: osteomyelitis, infections of the gastrointestinal tract, respiratory system, skin, urinary and biliary tract, as well as gonorrhea and chlamydia.

Contraindications: age under 18 years, pregnancy and lactation, allergy to the drug.

Side effects: cough, bronchospasm, gastrointestinal disorders, vasculitis, back and joint pain, disorders in the central nervous system, cardiovascular and genitourinary systems, allergic reactions.

Analogues: Abactal, Quintor, Pefloxacin, Maxaquin, Lofox, Lomacin, Xenaquin, Lomflox.

Moxifloxacin

Active ingredient: moxifloxacin. Release form: tablets. Indications for use: urogenital infections, infections of the upper or lower respiratory tract, skin infections. In combination it is used to treat tuberculosis.

Contraindications: tendency to seizures, liver failure, allergies, pseudomembranous colitis, age under 18 years, pregnancy.

Side effects: anemia, gastrointestinal disorders, hyperglycemia, tachycardia, shortness of breath, hallucinations, convulsions.

Analogues: Avelox, Moxy Fluorine 400, Tevalox, Plevilox, Moximac, Moxin and Vigamox.

Nalidixic acid

The active substance - nalidixic acid - is included in many drugs. Indications for use: cystitis, pyelitis, pyelonephritis, cholecystitis, inflammation of the middle ear.

Contraindications: depression of the respiratory center, impaired liver function, first trimester of pregnancy, age up to 2 years.

Side effects: vomiting, nausea, diarrhea, allergic reactions.

Nevigramon, Cystidix, Nilidixan, Nogram, Urodixin, Vintomilon, Negram. Release is carried out in tablets or capsules.

Norfloxacin

Release form: eye and ear drops, tablets. Active substance: norfloxacin. Indications: used for infections of bacterial origin of the urinary tract, reproductive system, gastrointestinal tract, gonorrhea and traveler's diarrhea.

Contraindications: age under 18 years, pregnancy and lactation, intolerance to components.

Side effects: nausea, abdominal pain, diarrhea, vomiting, urethral bleeding, dizziness, headaches, tachycardia, tremor, arthralgia.

Analogues: Nolicin, Norilet, Normax, Sophasin, Chibroxin, Norbactin, Yutibid, Norfatsin, Noroxin, Renor.

Oxolinic acid

Acid is part of antimicrobial drugs. Active substance: oxolinic acid. Indications for the use of fluoroquinolone: prostatitis, pyelonephritis, pyelitis, prevention of infection during instrumental studies (for example, catheterization).

Contraindications: pregnancy, lactation, renal or liver failure, epilepsy, allergies, age under 2 years, old age.

Side effects: gastrointestinal disorders, allergic reactions, general weakness, dizziness, blurred vision, photosensitivity.

Preparations containing acid: Dioxacin and Gramurin (available in tablets).

Ofloxacin

One of the respiratory drugs is fluoroquinolones. Release form: ointment, tablets, solutions for infusion (drops). Active substance: ofloxacin. Indications for use: diseases of the ENT organs, urinary tract and kidney infections, pneumonia, chlamydia, prostatitis, gonorrhea, conjunctivitis, blepharitis and others.

Contraindications: pregnancy, lactation, age under 18 years, epilepsy, allergies.

Side effects: nausea, vomiting, flatulence, loss of appetite, diarrhea.

Analogues:

tablets - Zanotsin, Ofloxin, Oflocid, Glaufos, Zoflox;
solutions - Tarivid, Oflo;
ointment - Floxal (eye);
drops for eyes and ears - Dancil and Uniflox.

Pefloxacin

Domestic antimicrobial medicine. Active ingredient: pefloxacin. Release form: solution, tablets. Indications: typhoid fever, sepsis, prostatitis, gonorrhea, cholecystitis, eye infections, middle ear lesions, infectious lesions of the pharynx and larynx.

Contraindications: hemolytic anemia, epilepsy, pregnancy and breastfeeding, allergies, age under 18 years.

Side effects: headaches, fatigue, diarrhea, flatulence, dysuria, edema (allergic, including Quincke's edema), tachycardia and others.

Analogues: Leflocin, Perti, Pelox-400, Unikpef, Pefloxabol.

Pipemidic acid

Release form: capsules, tablets, vaginal suppositories, suspension (for children). Active substance: pipemidic acid. Indications for use: urinary tract infections (diseases in acute or chronic form).

Contraindications: pregnancy, kidney failure.

Side effects: allergic skin reactions, nausea, photosensitivity, abdominal pain.

Analogues: Balurol, Naril, Pipefort, Pimidel, Pipem, Palin.

Sparflo

Active ingredient: Sparfloxacin is a poorly soluble substance of the fluoroquinolone group, which has an antibacterial effect. Release form: tablets. Indications: prostatitis, genital diseases, ENT infections, abdominal infections, sepsis, skin infections, leprosy, gonorrhea.

Contraindications: epilepsy, tendency to change heart rhythm, pregnancy and lactation, renal failure, age under 18 years, allergies.

Side effects: headaches, tremors, convulsions, fear, shortness of breath, vomiting, fever, hyperglycemia, hot flashes, hepatitis and others.

Ciprofloxacin

Active substance: ciprofloxacin. Release form: drops (for eyes and ears), tablets. Indications for use: blepharitis, keratitis, barley, infections brought into the eye by foreign bodies, conjunctivitis, otitis - for drops. Tablets are prescribed for diseases of the otolaryngological organs and respiratory tract infections, prostatitis, pyelonephritis, cystitis, peritonitis, sepsis.

Contraindications: viral keratitis, allergy. Eye drops should not be used by children under one year of age. For tablets: pregnancy and lactation, renal failure, epilepsy, age under 18 years.

Side effects: itching, slight burning, lacrimation, decreased vision or hearing, the appearance of white spots in patients with ulcerative eye lesions, allergic reactions. For tablets – gastrointestinal disorders, allergic reactions, dysfunction of the central nervous system.

Analogues: Tsifran, Tsipromed, Siflox, Floximed, Cipro, Tsiprinol, Microflox, Recipro, Tseprova, Quintor.

Indications

Fluoroquinolone group drugs are used in cases where conventional antibiotics will not cope:

anthrax;
typhoid fever;
pneumonia and bronchitis;
gonorrhea;
salmonellosis;
pyelonephritis;
chlamydia;
dysentery;
cystitis.

Fluoroquinolones are widely used in gynecology, urology (for example, for prostatitis), ophthalmology, otolaryngology and other areas of medicine.

Mechanism of action

During clinical trials, it was found that fluoroquinolones, unlike conventional antibiotics, do not weaken harmful bacteria, but kill them. This occurs by penetration of the active substance into the structure of the harmful microorganism and stopping the process of cell reproduction.

Fluoroquinolones penetrate the body faster. For several hours, the substances enter all tissues or fluids. After passing through all the systems of the human body, drugs leave it through the urinary tract.

Methods of application

When taking drugs from this group, it is important to understand that they are more likely to cause side effects if taken incorrectly than antibiotics.

The frequency, dose and duration of the course are determined by the doctor. You should strictly follow his recommendations and maintain equal intervals between doses. If a dose is missed, take a single dose as quickly as possible. But you shouldn’t do this when the next appointment is approaching. Doubling the dose is strictly prohibited. The tablets are taken with a sufficient amount of water.

It is worth adjusting the course of taking fluoroquinolones if other drugs are prescribed in combination. It is best to do this in case additional medications interact negatively with fluoroquinolones.

Contraindications

Medicines from the fluoroquinolone class are generally safe, but they have their own contraindications:

pediatric diseases (all drugs are not used in children under 2 years of age, some are limited to 18 years of age);
pregnancy and lactation;
allergy to quinolone substances.

Side effects

Negative effects occur less frequently than with antibiotics, but if taken incorrectly, they appear much more often:

gastrointestinal disorders (nausea, diarrhea, vomiting);
tachycardia, arrhythmia;
disturbances in the functioning of the sense organs (vision, smell, taste);
unstable functioning of the central nervous system (dizziness, headaches, tremors, convulsions);
fungus on the mucous membranes of the genitals and mouth;
tendon rupture, inflammation of cartilage tissue;
sleep disturbance;
periodic pain in the muscles;
nephritis;
painful photosensitivity;
allergic reactions (itching, urticaria, swelling);
pseudomembranous colitis (appears rarely, only against the background of severe dysbacteriosis or intestinal clostridia infection).

Dear pharmaceutical workers, hello!

Recently we looked at the most popular groups.

Today I would like to dwell on another group of extremely popular antibacterial agents. I'm talking about fluoroquinolones.

They are not antibiotics because they have no natural analogues. But in terms of efficiency they are in no way inferior.

How many generations of fluoroquinolones are currently on the market?
Name at least one drug from each generation of this group.
How do generations differ from each other?
Which fluoroquinolones are used primarily for genitourinary tract infections?
Name a rare side effect that is caused by drugs in this group.
At what age can fluoroquinolones be used and why?

So how? Did you manage?

If not, let's continue the conversation.

From the history of fluoroquinolones

The “parents” of fluoroquinolones are quinolones - nalidixic acid (Negram, Nevigramon), pipemidic acid (Palin), etc.

I'm sure you can tell when they are used.

Right. Mainly for urinary tract infections. Quinolones are essentially uroseptics, i.e. drugs that free the bladder, kidneys, and ureters from bacterial invaders.

Recently, these drugs have been prescribed less and less often, since much more effective drugs have appeared on the market.

Quinolones were synthesized by accident during the study of an antimalarial drug called Chloroquine.

A few years after their discovery, one of the scientists came up with the idea of adding a fluorine atom to the quinolone formula and seeing what would happen. What has emerged is a completely new group of antibacterial agents, which is comparable in effectiveness to

Group of fluoroquinolones. Features of generations

In some publications, quinolones are considered together with fluoroquinolones and are classified as their first generation.

It turns out to be some kind of rubbish: quinolones are the 1st generation of fluoroquinolones.

But the group turned out to be completely different, with different characteristics and indications!

So I will speak as common sense tells me.

Today there are 3 generations of fluoroquinolones:

Generations of fluoroquinolones differ from each other in their spectrum of antibacterial activity.

Each new generation is superior in some way to the previous one.

1st generation is called " gram negative ", since drugs belonging to this generation act on a wide range of gram-negative bacteria. And of the gram-positive ones, only a small handful: several varieties of staphylococcus, listeria, corynebacterium, tuberculosis bacillus.

Let me remind you of gram-negative bacteria: Pseudomonas aeruginosa, Gonococcus (the causative agent of gonorrhea), meningococcus (the causative agent of purulent meningitis), Escherichia coli, Salmonella, Shigella, Proteus, Klebsiella, Enterobacter, Haemophilus influenzae, etc.

1st generation drugs can be divided into 2 groups:

System: Ciprofloxacin, Lomefloxacin and Ofloxacin. They penetrate various organs and tissues, therefore they are used for infections of various locations: respiratory tract, ear, eye, genitourinary tract, gastrointestinal tract, skin, bones, etc.

Uroseptics: Norfloxacin and Pefloxacin. These drugs create high concentrations in the urine, so they are most often used for infections of the genitourinary system.

But drugs of this generation have little effect on pneumococcus, chlamydia, mycoplasma, and anaerobes.

Norfloxacin is also included in eye and ear drops called Normax.

The 2nd generation was called " respiratory ", since the drugs related to it act not only on those pathogens of the 1st generation, but also on most pathogens of respiratory tract infections (pneumococcus, Mycoplasma pneumoniae, etc.).

They deal well with the same enemies of the people as the 1st generation, but also with pneumococci, chlamydia, and mycoplasmas.

I will call the 3rd generation “ storm of anaerobes».

While I was collecting material for the article, I met several representatives of this generation, but did not see them in the assortment of pharmacies. I don’t see any point in talking about “dead souls”. So I name the most popular: Moxifloxacin (trade name Avelox).

The drugs, or rather the drug, of the third generation of fluoroquinolones act on the same pathogens as the previous two, plus they are able to destroy anaerobic bacteria. Do you remember who they are?

These are unpretentious microbes that, unlike their intelligent brothers, do not need oxygen to live a full life.

They cause severe infections. Their toxins are extremely aggressive, capable of affecting vital organs and causing peritonitis, abscesses of internal organs, sepsis, osteomyelitis and other serious diseases.

Anaerobic bacteria are also the culprits of tetanus, gas gangrene, botulism,

Thus, from generation to generation the spectrum of antibacterial activity of fluoroquinolones expands.

Advantages of the fluoroquinolones group

You have probably noticed that many doctors love drugs from this group, which is why they are prescribed quite often.

What good did they find in them?

Let's list their advantages.

Fluoroquinolones:

They have a wide spectrum of action.
Penetrates deeply into various tissues.
They have a long half-life, so they can be used 1-2 times a day.
They are well absorbed from the gastrointestinal tract, so they are available in oral forms, which is more convenient and enjoyable for many patients.
Highly effective.
Well tolerated.

Mechanism of action of fluoroquinolones

Fluoroquinolones have a bactericidal effect. They inhibit enzymes that are necessary for the synthesis of DNA in daughter bacterial cells. What is DNA? This is the “heart” of the cell, its genetic code, “instructions” on how to live and make good money. No “instructions” - no life.

Indications for the use of fluoroquinolones

Fluoroquinolones have a wide, I would even say the widest, range of indications:

Diseases of the upper and lower respiratory tract.
Urinary tract and prostate infections: urethritis, pyelonephritis, prostatitis. Norfloxacin and pefloxacin work especially well against them.
Gonorrhea, chlamydia, mycoplasmosis.
Intra-abdominal infections (peritonitis, cholecystitis, etc.).
Intestinal infections (salmonellosis, dysentery, cholera, etc.).
Infections of the skin, soft tissues, bones and joints.
Sepsis.
Meningitis.
Tuberculosis.
, external ear (norfloxacin).

The choice of fluoroquinolone drug depends on the type and severity of the disease, its duration, the type of pathogen and the effectiveness of previously used drugs.

Each drug has its own advantages. For example:

Ciprofloxacin- the most active of the fluoroquinolones against gram-negative bacteria. It is superior to its “colleagues” in its effect on Pseudomonas aeruginosa. Used in combination therapy of drug-resistant forms of tuberculosis.

Ofloxacin- of the 1st generation, the most active against pneumococci and chlamydia, but weaker than drugs of the 2nd and 3rd generations.

Norfloxacin And pefloxacin especially good for urinary tract and prostate infections.

Pefloxacin In addition, it penetrates the blood-brain barrier better than other fluoroquinolones, therefore it is used for meningitis (for this there is a concentrate form for intravenous administration).

Sparfloxacin superior to other drugs in this group in terms of duration of action. Apply once a day.

Levofloxacin - an isomer of ofloxacin, 2 times more active and better tolerated.

Moxifloxacin of the entire group, it is the most active against pneumococci, chlamydia, mycoplasmas, and anaerobes. It can be used empirically (that is, blindly, without culturing bacteria) for severe infections of various localizations.

Contraindications to the use of fluoroquinolones

Common to all:

Pregnancy.
Breastfeeding.
Allergic reactions to fluoroquinolones.
Childhood and adolescence.

Fluoroquinolones contraindicated under 18 years of age, since in animal experiments researchers noted a delay in the development of cartilage tissue. Therefore, as a rule, they are not prescribed until the formation of the skeleton is completed. Although, in some cases, doctors prescribe fluoroquinolones to children on their own responsibility. For example, with cystic fibrosis or intolerance to other antibacterial agents.

The most common side effects of fluoroquinolones

From the gastrointestinal tract: abdominal pain, nausea, vomiting. Therefore, advise taking them after meals.
Central nervous system disorders: dizziness, convulsions (in people suffering from epilepsy).
Photodermatoses, i.e. increased skin sensitivity to ultraviolet rays. When exposed to the sun, fluoroquinolones are broken down, free radicals are formed and cause skin damage.

This means that when selling a drug from this group, it is necessary to offer it especially in summer and in sunny regions.

Lomefloxacin (Lomflox) and sparfloxacin (Sparflo) differ more than others in their ability to cause photodermatoses.

Increased liver transaminases. This means that the drugs are hepatotoxic. Therefore, it would be a good idea to take a drug from the fluoroquinolone group in conjunction with. Rarely, drug-induced hepatitis does occur.
Increased QT interval on ECG. For healthy people this is not scary. And if the drug is taken by a person who has serious heart problems, there may be arrhythmia. But this happens when taking large doses of the drug.

A rare side effect is tendonitis, i.e. inflammation of the tendon and its rupture. Most often, the Achilles tendon is affected. This happens mainly in older people.

Tendonitis occurs because fluoroquinolones inhibit the activity of an enzyme necessary for the synthesis of collagen protein. And it forms the basis of tendons, and connective tissue in general.

Important:

If fluoroquinolones are taken simultaneously with an antacid and insoluble compounds are formed, the drug will not have the desired effect. Therefore, the break between doses should be at least 4 hours.

Now let’s remember all of the above and draw up a list of recommendations for the buyer.

5 recommendations for the buyer when selling a fluoroquinolone drug

If you sell a drug from the fluoroquinolone group:

Offer sunscreen. Say something like this: “This drug makes your skin more sensitive to sunlight and may cause a rash. Therefore, I advise you to purchase another product to protect your skin from the sun.”
If a person refuses point 1, warn: “Avoid exposure to the sun throughout the entire treatment period and for another 3 days after its completion.”
Offer a hepatoprotector (“Did your doctor prescribe anything to protect your liver with this drug?”)
Tell them to take the medicine after meals, with plenty of liquid to reduce its irritating effect on the stomach.
If a person, along with a drug from the fluoroquinolone group, also purchases an antacid drug or a vitamin-mineral complex, recommend dividing their intake in time (a break of at least 4 hours).

Is everything clear?

If you have anything to add or comment, write in the comments box below.

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Still didn't work? Write. Let's figure it out!

Even a schoolchild knows why antibiotics are needed in our time. But the phrase “broad spectrum” sometimes raises questions among patients. Why "wide"? Perhaps there will be less harm from an antibiotic with a “narrow” spectrum?

Gram-negative bacteria negatively affects the intestines and the genitourinary system. Such pathogens include Escherichia coli, Moraxella, Salmonella, Klebsiella, Shigella, etc.

Such antibiotics are divided into groups. One of them is the group of fluoroquinolones.

Quinolones and fluoroquinolones

Drugs of the quinolone class began to be used in medical practice since the early 60s of the last century. Quinolones are divided into non-fluorinated quinolones and fluoroquinolones.

Non-fluorinated quinolones have an antibacterial effect mainly on gram-negative bacteria.
Fluoroquinolones have a much wider spectrum of action. In addition to influencing a number of Gram bacteria, fluoroquinolones also successfully fight Gram-positive bacteria. Fluoroquinolone antibiotics show a high bactericidal effect, thanks to this, medications for topical use (drops, ointments) have been developed, which are used in the treatment of diseases of the ears and eyes.

Four generations of drugs

Names of drugs containing 2nd generation fluoroquinolones

3rd generation fluoroquinolones

Names of drugs containing 3rd generation fluoroquinolones

4th generation

4th generation fluoroquinolone drugs include the following the most famous drugs: moxifloxacin, gemifloxacin, gatifloxacin.

Medicines containing 4th generation fluoroquinolones

For quotation: Zaitsev A.A., Sinopalnikov A.I. “Respiratory” fluoroquinolones in the treatment of respiratory tract infections // RMZh. 2010. No. 30. S. 1883

Introduction The emergence of quinolone antibiotics dates back to the discovery in 1962 of nalidixic acid during the synthesis of chloroquine (Fig. 1). For two decades, nalidixic acid and its derivatives (pipemidic and oxolinic acids), which are active against gram-negative microorganisms, have been successfully used to treat urinary tract infections. The second wave of development of quinolones (1980s) is associated with the emergence of fluorinated compounds with higher activity against gram-negative, some gram-positive bacteria and intracellular microorganisms, with improved pharmacokinetics, the presence of forms for parenteral administration (ciprofloxacin, ofloxacin, fleroxacin, lomefloxacin, norfloxacin ) . However, the low antipneumococcal activity of second-generation quinolones drugs currently makes their use impossible for most respiratory tract infections. The next stage in the development of quinolones (1990s) is associated with the emergence of di- and trifluorinated compounds with enhanced activity against gram-positive bacteria (especially Streptococcus pneumoniae) and intracellular pathogens. This quality determined the name of these drugs - “respiratory” fluoroquinolones, which according to the modern classification are classified as III (sparfloxacin, levofloxacin) and IV (moxifloxacin, gatifloxacin, garenoxacin) generations of quinolones. Three drugs are registered in the Russian Federation: levofloxacin, moxifloxacin and gemifloxacin.

The emergence of quinolone antibiotics dates back to the discovery of nalidixic acid in the process of chloroquine synthesis in 1962 (Fig. 1). For two decades, nalidixic acid and its derivatives (pipemidic and oxolinic acids), which are active against gram-negative microorganisms, have been successfully used to treat urinary tract infections. The second wave of development of quinolones (1980s) is associated with the emergence of fluorinated compounds with higher activity against gram-negative, some gram-positive bacteria and intracellular microorganisms with improved pharmacokinetics, the presence of forms for parenteral administration (ciprofloxacin, ofloxacin, fleroxacin, lomefloxacin, norfloxacin ) . However, the low antipneumococcal activity of second-generation quinolones drugs currently makes their use impossible for most respiratory tract infections. The next stage in the development of quinolones (1990s) is associated with the emergence of di- and trifluorinated compounds with enhanced activity against gram-positive bacteria (especially Streptococcus pneumoniae) and intracellular pathogens. This quality determined the name of these drugs - “respiratory” fluoroquinolones, which according to the modern classification are classified as III (sparfloxacin, levofloxacin) and IV (moxifloxacin, gatifloxacin, garenoxacin) generations of quinolones. Three drugs are registered in the Russian Federation: levofloxacin, moxifloxacin and gemifloxacin.
“Respiratory” fluoroquinolones are highly effective against all potential pathogens of community-acquired pneumonia (CAP) (Table 1), have a bactericidal effect and have a pronounced post-antibiotic effect, which averages 2 hours.
All “respiratory” fluoroquinolones have a long half-life, which allows them to be taken once a day, and are characterized by high bioavailability and rapid absorption. The antimicrobial effect of fluoroquinolones depends on the antibiotic concentrations created, with the best pharmacodynamic parameter correlating with bacterial eradication being the ratio of AUC (non-protein bound fraction of the antibiotic) to MIC. A reliable predictor of eradication of S. pneumoniae is a free AUC/MIC ratio of ≥ 25. For levofloxacin, moxifloxacin and gemifloxacin, this indicator is 40, 96 and 97-127, respectively (Table 2).
“Respiratory” fluoroquinolones have high tissue penetration, creating concentrations in alveolar macrophages, bronchial mucosa and the fluid lining the epithelium of the respiratory tract that significantly exceed the MIC of pathogens of respiratory infections that are sensitive to them.
The resistance of microorganisms relevant for respiratory tract infections to “respiratory” fluoroquinolones throughout the world, with the exception of a number of countries in Southeast Asia, remains low. Thus, in Europe, more than 97% of S. pneumoniae strains are sensitive to “respiratory” fluoroquinolones, and in Russia, until now, only one strain with moderate resistance to levofloxacin and moxifloxacin has been isolated. To date, not a single strain of H. influenzae resistant to “respiratory” fluoroquinolones has been isolated in the Russian Federation.
The history of the creation and subsequent clinical use of fluoroquinolones is an illustrative illustration of the fact that as the spectrum expands and the antimicrobial effect increases, the frequency of serious adverse events increases, which was the reason for the withdrawal of certain drugs from the pharmaceutical market (grepafloxacin, trovafloxacin, clinafloxacin, etc.). Levofloxacin (Tavanic) is known to have no serious safety concerns during its use in more than 300 million patients worldwide. On the contrary, for gemifloxacin this problem is the main one, since during its use the appearance of a skin rash (maculopapular) has been registered with long-term courses of its use in women under 40 years of age and in postmenopausal women on hormone replacement therapy. In this regard, it is not recommended to prescribe the drug in courses of more than 7 days. Gemifloxacin may lead to QT prolongation and is therefore not recommended for use in patients with a history of QT prolongation, electrolyte imbalance, and taking class IA and III antiarrhythmic drugs. In addition, the still short period of clinical use of the drug does not allow us to fully assess the safety of its use.
Levofloxacin (Tavanic) and moxifloxacin have dosage forms for both oral and parenteral use, which allows them to be used in step-down therapy, for example, in patients with moderate to severe pneumonia. Gemifloxacin is only available for oral administration, which limits its use to mild forms of the disease.
Clinical Application
"respiratory" fluoroquinolones
Community-acquired pneumonia
In the etiology of CAP, Streptococcus pneumoniae is of primary importance, accounting for 30-50% of cases of the disease. “Atypical” microorganisms - Chlamydophila pneumoniae, Mycoplasma pneumoniae, Legionella pneumophila - are responsible for the development of 8-30% of cases of CAP. Typical pathogens include Haemophilus influenzae, Staphylococcus aureus, Klebsiella pneumoniae, responsible for 3-5% of cases of CAP; cases of the disease associated with other enterobacteria and non-fermenting gram-negative microorganisms are less common. The etiological structure of CAP may vary depending on the age of the patients, the severity of the disease, and the presence of concomitant pathology. In patients hospitalized in the therapeutic department, pneumococci predominate in the etiology of CAP; Chlamydophila and Mycoplasma pneumoniae account for a total of about 25%. On the contrary, the latter are not significant in the etiology of severe CAP requiring treatment in the intensive care unit (ICU); at the same time, in this category of patients the role of Legionella spp., as well as S. aureus and gram-negative enterobacteria, increases.
Antibacterial therapy for CAP should be carried out immediately after the diagnosis of the disease is established; a delay in starting antibiotic therapy leads to a worsening prognosis of the disease. In the vast majority of cases, the antibiotic is prescribed empirically, which requires knowledge of the spectrum of the most likely pathogens and the local epidemiology of resistance.
When choosing a specific antibiotic, the following factors must be taken into account: antimicrobial activity against potential pathogens of CAP; high bioavailability taking into account the age characteristics of the patient; acceptable safety profile; optimal dosage regimen (frequency of administration does not exceed 2 times/day, otherwise the risk of non-compliance with the treatment regimen increases); minimal level of drug interactions.
Recommendations for empirical antibiotic therapy for CAP are presented in Figure 2. Among patients with non-severe CAP (treatment on an outpatient basis), there are 2 groups that differ in the etiological structure and tactics of antibacterial therapy. The first group included patients without concomitant diseases who had not taken any medication in the last 3 months. antibacterial drugs, i.e. patients without so-called risk factors for therapeutic failure. Amoxicillin or “modern” macrolide antibiotics are recommended as the means of choice in this situation. Macrolides should be preferred in case of intolerance β -lactam antibiotics or if an atypical etiology of the disease is suspected (M. pneumoniae, C. pneumoniae).
The second group included patients who received in the last 3 months. antibacterial drugs and patients with concomitant diseases (COPD, diabetes mellitus, congestive heart failure, liver disease, alcohol abuse, drug addiction, underweight, smoking). Taking into account the likelihood of participation in the etiology of the disease by gram-negative microorganisms (including those with some mechanisms of antibiotic resistance), as well as co-infection, combination therapy is recommended for patients in this group - “protected” aminopenicillin + macrolide. It is also possible to use “respiratory” fluoroquinolones (Tavanic, moxifloxacin, gemifloxacin).
In patients hospitalized in a general hospital, combination therapy is recommended β -lactam + macrolide, since the presence of a drug active against “atypical” microorganisms in the initial treatment regimen improves the prognosis and reduces the length of patient stay in the hospital. In case of ineffectiveness of the therapy, in the presence of risk factors for antibiotic-resistant microorganisms (old age, concomitant pathology, immunosuppression, etc.), patients with risk factors for gram-negative enterobacteria, previous treatment β -lactam antibiotics, pneumonia in patients living in nursing homes, it is advisable to use “respiratory” fluoroquinolones in a stepwise therapy regimen.
Combination therapy is recommended for patients with severe disease β IV lactam + IV macrolide, or parenteral forms of “respiratory” fluoroquinolones in combination with III-IV generation cephalosporins (cefotaxime, ceftriaxone, cefepime).
The greatest difficulties in the treatment of CAP arise in the presence of antibiotic-resistant strains of pneumococcus, in severe pneumonia (the role of S. aureus and the Enterobacteriaceae family), as well as in elderly and senile patients. It is in the above situations that the ineffectiveness of antibacterial therapy, the development of disease complications, and high mortality are most often noted. Risk factors for drug-resistant/problematic pathogens of community-acquired pneumonia are presented in Figure 3. It is worth noting that, according to current available data, clinically significant levels of S. pneumoniae resistance to penicillin are observed in strains with an MIC of at least 4 mg/l. It is important that, according to the results of individual studies, resistance to macrolides and fluoroquinolones (ciprofloxacin) can be the cause of therapeutic failure, while at the same time, cases of ineffectiveness of therapy for CAP with “new” fluoroquinolones (levofloxacin, moxifloxacin, gemifloxacin) due to antibiotic resistance have not been registered.
In this regard, these situations require the preferential administration of “respiratory” fluoroquinolones. If there are risk factors for P. aeruginosa, the drug of choice is levofloxacin (Tavanic).
The prospects for the use of “respiratory” fluoroquinolones are associated with a number of studies in which it has been shown that the use of these drugs is accompanied by less treatment failure compared to other antibiotic regimens (Table 3). It is obvious that the use of “respiratory” fluoroquinolones provides a better outcome of the disease due to its high activity against all potential pathogens of CAP, including “atypical” microorganisms (C. pneumoniae, M. pneumoniae and L. pneumophila), as well as due to pronounced antipneumococcal activity, including drug-resistant strains of this microorganism. In this regard, interesting data are obtained from a study showing that the use of levofloxacin in patients with severe pneumococcal pneumonia is accompanied by a shorter time to clinical stability than antibiotic therapy with ceftriaxone.
Exacerbation of COPD
Chronic obstructive pulmonary disease (COPD) is one of the most pressing problems of modern healthcare, due to its widespread prevalence with a clear tendency to increase the number of patients and mortality. The most important factor determining the rate of progression of bronchial obstruction, as well as the quality of life of patients and the amount of economic costs is the frequency of exacerbations. Patients with COPD experience from 1 to 4 or more exacerbations during the year, with more than half of the cases requiring hospital treatment.
In the overwhelming majority of cases (75-80%), exacerbation of COPD is of an infectious nature. The main pathogens are H. influenzae, S. pneumoniae and Moraxella catarrhalis (Table 1). Less commonly, Haemophilus parainfluenzae, S. aureus, P. aeruginosa and members of the Enterobacteriaceae family are isolated from sputum samples of COPD patients. The share of “atypical” pathogens - M. pneumoniae and C. pneumoniae - in the development of exacerbations is about 5%. About 30% of exacerbations of COPD are viral in nature. Most often, rhinoviruses are detected - 20-25%, less often influenza viruses - 3-10%. Among other things, it has been proven that a viral infection serves as a “conductor” for the development of exacerbation in more than 50% of cases.
The severity of exacerbation of COPD corresponds to the type of infectious agent. In patients with mild exacerbation of COPD, exacerbation is most often caused by S. pneumoniae; as the disease progresses (decrease in forced expiratory volume in 1 s - FEV1, frequent exacerbations throughout the year, smokers) H. influenzae, M. catarrhalis and Enterobacteriaceae are identified. In cases of severe exacerbation, P. aeruginosa is often found. Risk factors for Pseudomonas aeruginosa infection are severe bronchial obstruction (FEV1< 35%); бронхоэктатическая болезнь; хроническое гнойное отделяемое; предшествующее выделение P. aeruginosa из мокроты; недавняя госпитализация (продолжительность ≥ 2 дней в течение прошлых 90 дней); частое применение антибиотиков (≥ 4 курсов в течение года).
Empirical antibiotic therapy for infectious exacerbation of COPD involves the selection of drugs that are active against the most likely bacterial pathogens, taking into account the prevalence of mechanisms of acquired resistance to various classes of antibiotics. Taking into account the above requirements, in the treatment of infectious exacerbation of COPD, β -lactam antibiotics, macrolides and “respiratory” fluoroquinolones. The evolution of attitudes towards the above classes of antibiotics begins with a meta-analysis performed by Siempos I. et al., 2007, which conducted a comparative assessment of the effectiveness and safety of the use of macrolides, “respiratory” fluoroquinolones and amoxicillin/clavulanate in the treatment of exacerbations of COPD. As a result of the meta-analysis, all of the listed antibiotics demonstrated comparable clinical effectiveness, and it was noted that the use of “respiratory” fluoroquinolones was characterized by higher microbiological effectiveness and a lower frequency of disease relapses compared to macrolides, while the use of amoxicillin/clavulanate was accompanied by the highest incidence of adverse events compared to other drugs.
It is obvious that at the present time the most important criterion for the effectiveness of antibiotic therapy for COPD is the duration of the period between exacerbations. From this point of view, the greatest prospects are associated with the use of “respiratory” fluoroquinolones, which has been proven in a number of clinical studies. The presence of high bactericidal activity in this group of antibiotics against gram-positive and gram-negative microorganisms, including drug-resistant strains of S. pneumoniae, ensures the maximum degree of eradication of pathogens that cause exacerbation of COPD. An important feature of “respiratory” fluoroquinolones is the ability to have a bactericidal effect on dormant forms of bacteria that form biofilms. A similar effect has been demonstrated against H. influenzae and P. aeruginosa (for levofloxacin).
Domestic experts currently propose an approach to the management of patients with infectious exacerbation of COPD, presented in Figure 4. The antibiotics of choice for patients with simple/uncomplicated exacerbation of COPD1 are amoxicillin, “modern” macrolides (azithromycin, clarithromycin) and cefuroxime axetil. On the contrary, in the group of patients undergoing a complicated exacerbation of COPD2, the use of “respiratory” fluoroquinolones (Tavanic, moxifloxacin, gemifloxacin) or inhibitor-protected penicillins is recommended. The presence of risk factors for Pseudomonas aeruginosa infection (FEV1< 35% от должных значений, хроническое отделение гнойной мокроты, наличие бронхоэктазов, предшествующее выделение P. aeruginosa из мокроты) определяет выбор в пользу левофлоксацина .
Compliance problem
patients in the treatment of respiratory tract infections
An important feature of “respiratory” fluoroquinolones is the possibility of taking them once a day, which ensures high patient compliance. It is known, including the example of the treatment of respiratory tract infections, that the greatest compliance is observed with a single dose of an antibiotic; on the contrary, a more frequent antibiotic dosing regimen leads to frequent deviations from medical prescriptions. The possibility of using “respiratory” fluoroquinolones in short courses (≤ 5 days) for mild CAP and uncomplicated exacerbation of COPD also leads to improved patient compliance.

1 Infrequent (<4) обострения заболевания в течение 12 мес., возраст до 60 лет, отсутствие серьезной сопутствующей патологии, незначительные или умеренные нарушения бронхиальной проходимости - ОФВ1 ≥ 50% от должных значений.
2 Presence of ≥ 1 sign (patient age ≥ 60 years and/or severe impairment of pulmonary ventilation function - FEV1< 50% от должных значений, и/или наличие серьезных сопутствующих заболеваний - сахарный диабет, застойная сердечная недостаточность, заболевания печения и почек с нарушениями их функции и др. и/или ≥ 4 обострения в течение 12 мес., и/или госпитализации по поводу обострения в предшествующие 12 мес., и/или использование системных глюкокортикостероидов или антибиотиков в предшествующие 3 мес.).

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