Nitrofuran instructions for use for children. Treatment of uncomplicated urinary tract infections. The place of nitrofuran preparations in modern conditions

Preparations: furazolidone, nitrofurantoin (furadonin), furatsilin, furagin, nifuroxazide.

Mechanism of action: nitro groups of the drug under the action of bacterial enzymes to be restored to the amino group. Substances formed as a result of the reduction of the nitro group have toxic effect, block a number of biochemical processes in the bacterial cell, violate the structure and integrity of the cell membrane. In particular, there is an irreversible blockade of NADH and inhibition of the tricarboxylic acid cycle, as a result of which the cellular respiration of microorganisms, the function of the cytoplasmic membrane are disturbed, and the death of the microorganism occurs. The nitrofuran molecule, due to the ability to form complex compounds with nucleic acids, disrupts the synthesis of a number of proteins in a bacterial cell, as a result of which the growth and reproduction of microorganisms is inhibited.

Action type: dose-dependent: in low - bacteriostatic, in high - bactericidal.

Spectrum (narrow):

Gr+ cocci: Streptococcus, Staphylococcus,

Gr-bacteria: Escherichia, Salmonella, Shigella, Proteus, Klebsiella, Enterobacter,

Protozoa: Lamblia (furazolidone).

Resilience develops slowly.

Application:

urinary system infections: cystitis, pyelonephritis (nitrofurantoin);

intestinal infections: food poisoning, dysentery, (furazolidone, nifuroxazide)

giardiasis (furazolidone);

washing of wounds, cavities (furatsilin).

Side effects:

dyspeptic reactions

neurotoxicity: headache, drowsiness, polyneuropathy (more typical for nitrofurantoin)

hemolysis in patients with glucose-6 phosphate dehydrogenase deficiency

leukopenia

• skin rash

  angioedema

  teturam-like effect

Prevention side effects: to reduce dyspeptic reactions when using furazolidone, it is recommended to take it before meals and drink plenty of liquid, if necessary, reduce the dose, prescribe antihistamines and B vitamins.

Nitroimidazoles

Mechanism of action: biochemical reduction of the 5-nitro group of intracellular transport proteins of anaerobic microorganisms and protozoa; the reduced 5-nitro group interacts with the DNA of microorganism cells, inhibiting the synthesis of their nucleic acids, which leads to the death of bacteria.

Action type: bactericidal

Action spectrum:

Protozoa: Trichomonas vaginalis, Entamoeba histolytica, Giardia lamblia, Balantidium coll

Obligate anaerobes Bacteroides spp. (including Bacteroides fragilis, Bacteroides distasonis, Bacteroides ovatus, Bacteroides thetaiotaomicron, Bacteroides vulgatus), Fusobacterium spp.,

Some gram-positive anaerobic microorganisms (Eubacterium spp., Clostridium spp., Peptococcus niger, Peptostreptococcus spp.)

Helicobacter pylori (in combination with amoxicillin)

Gardnerella vaginalis,

Application:

Trichomoniasis

Amoebiasis, giardiasis

Bacterial vaginosis

Abdominal infections (peritonitis, liver abscess),

Infections of the pelvic organs (endometritis, endomyometritis, abscess of the fallopian tubes and ovaries, infections of the vaginal fornix after surgical operations),

Infections of the skin and soft tissues caused by susceptible microorganisms,

Pseudomembranous colitis associated with antibiotic use

gastritis or peptic ulcer duodenal ulcer associated with Helicobacter pylori

Cutaneous leishmaniasis

Side effects:

teturam-like effect

polyneuropathy

stomatitis, metallic taste in the mouth

• leukopenia

Metronidazole can be used to treat tumors in combination with radiation therapy - it has a radiosensitizing effect in cases where tumor resistance is due to hypoxia in tumor cells.

Independent work of students

Task number 1

Write out at home in a notebook for practical exercises in the form of medical prescriptions and indicate the indications for the use of prescribed dosage forms.

Sulfanilamide for the treatment and prevention of eye infections

A derivative of nitrofuran, poorly absorbed in the gastrointestinal tract

Ciprofloxacin hydrochloride in the table.

Metronidazole in the table. and in vials

Task number 2

Write out in the form of medical prescriptions drugs for the treatment of:

Pneumocystis pneumonia from the group of sulfonamides.

An antibacterial drug for the eradication of H. pylori.

Cystitis (from nitrofurans).

Peritonitis.

Situational tasks

Task #1

Patient V. was drinking sulfadimidine orange juice. After 2 weeks, the patient was taken to the hospital with acute renal failure. Explain the reason for the complication. What recommendation for taking sulfonamides did the patient not follow?

Task #2

A young girl was taken to the hospital with severe endometritis. The emergency room doctor prescribed ofloxacin intravenously at 400 mg 2 times a day. After the patient reported that she was suffering from epilepsy and was taking phenytoin, the doctor stopped ofloxacin and prescribed a combination of imipinem + cilastatin 500 mg IV. Why did the doctor cancel ofloxacin? Was it reasonable to make a substitution?

Task #3

Patient S. was prescribed furazolidone for the treatment of intestinal infection. During the course of treatment, the patient attended a banquet where he drank some alcohol. From there, he was taken to the hospital in serious condition: blood pressure dropped sharply, tachycardia, hyperemia of the skin and mucous membranes appeared. What complication did the patient have? Explain its mechanism.

Test control:

Specify the sulfanilamide preparation containing sulfanilamide and trimethoprim:

sulfadimidine (sulfadimidine)

inhalipt

phthalylsulfothiazole (phthalazol)

sodium sulfacetamide (sulfacyl sodium)

co-trimoxazole (biseptol)

Which of the antibiotics cause oppression of hematopoiesis (anemia, leukopenia)?

penicillins

cephalosporins

macrolides

chloramphenicol (levomycetin)

tetracyclines

Which of the antibiotics cause dysfunctionVIIIa pair of cranial nerves?

chloramphenicol (levomycetin)

tetracyclines

aminoglycosides

macrolides

penicillins

Choose a drug for the treatment of uncomplicated chlamydial infection:

penicillin G (benzylpenicillin)

azithromycin (sumamed)

penicillin V (phenoxymethylpenicillin)

ampicillin

clavulanic acid

Ciprofloxacin belongs to the group of derivatives:

naphthyridine

fluoroquinolone

oxyquinoline

nitrofuran

nitroimidazole

Specify what type of drug interaction is observed when combining amoxicillin and clavulanic acid:

antidotism

antagonism

tachyphylaxis

potentiation

inhibition

All of the following statements are correct EXCEPT:

cephalosporins, when used together, potentiate the nephrotoxic effect of aminoglycosides;

skeletal muscle paralysis caused by a high concentration of aminoglycosides is relieved by infusion of calcium gluconate;

furosemide (diuretic) increases the rate of renal elimination of aminoglycosides and thus reduces their toxic effect;

headache and dizziness are early symptoms of the neurotoxic action of aminoglycosides;

oral administration of neomycin may lead to superinfection.

All of the following statements are true EXCEPT:

metronidazole is effective against aerobic bacteria;

metronidazole is well absorbed when taken orally and penetrates into the central nervous system;

with prolonged use of metronidazole, peripheral neuropathy may occur;

in pregnant women, metronidazole should be used with caution, because. it has been shown to be teratogenic in animals;

metronidazole is an effective treatment for pseudomembranous colitis caused by anaerobic clostridia.

Trimethoprim...

less active in its antimicrobial activity than sulfamethoxazole;

inhibits the enzyme dihydropteroate synthetase;

causes undesirable effects, which can be reduced by the appointment of folic acid; +

does not cause the development of resistance in microorganisms;

stimulates the synthesis of purines.

Sulfadiazine…

is an antagonist of para-aminobenzoic acid;

has a bactericidal effect;

effective in the treatment of nocardiosis.

Answers

Task #1

Alkaline drink.

Task #2

Fluoroquinolones → CNS → convulsions (with epilepsy).

Replacement is not rational.

Task #3

Teturam-like effect.

Tests:

I. 5.VI. 4.

II. 4. VII. 3.

III. 3.VIII. 1.

IV. 2. IX. 3.

v. 2.x. 1,3.

Urinary tract infections (UTIs) are the most common bacterial infections in the world . Accordingly, UTIs are among the 20 most common causes patients' appeals to a general practitioner and therapist. However, in Europe there are no data on the impact of UTIs on the quality of life of patients, the economic costs associated with these infections. In the US, UTIs accounted for 8.6 million doctor visits in 2007 (84% of them were women). About 15% of all over $1 billion a year of antibiotics prescribed outpatiently in the United States are for UTIs. The direct and indirect costs of community-acquired UTIs exceed $1.6 billion per year. In Russia, about 36 million cases of acute cystitis are registered annually (an average of 0.5-0.7 episodes of the disease per woman per year). The incidence of acute pyelonephritis is 15.7 cases per 100,000 population per year. It should be noted that the diagnosis and treatment of uncomplicated UTI usually does not cause difficulties. However, the problem of microbiological recovery with the eradication of the uropathogen remains one of the most urgent, as it determines the prevention of relapses and exacerbations of these diseases.

The spectrum of causative agents of uncomplicated UTIs and the frequency of their resistance to antibacterial drugs

The reason for the failure of the eradication of the uropathogen, with the transition of an uncomplicated course of UTI to a complicated one, is often high level resistance of pathogens to the most widely used antibacterial agents in the region. That is why it is recommended to regularly update data on the characteristics of the sensitivity of UTI pathogens and revise the recommended treatment regimens. To this end, multicenter clinical and epidemiological studies are regularly conducted around the world. It is believed that if the level of resistance to any antimicrobial drug in the region is more than 10-20%, this is a prerequisite for limiting its use as empirical therapy.

So, according to European Association urologists (European Association of Urology, EAU), the spectrum of causative agents of uncomplicated infections of the upper and lower urinary tract is similar, while Escherichia coli is the causative pathogen in 70-95%, Staphylococcus saprophyticus- in 5-10% of cases, more rarely other enterobacteria, such as Proteus mirabilis, Klebsiella spp. (level of evidence 2a) [Urological infections, 2011]. According to US researchers E. coli causes the development of 75-95% of cases of uncomplicated cystitis and pyelonephritis. The largest international study ECO.SENS, which included 4734 patients under 65 years of age in 252 clinics in 16 European countries and Canada, revealed the following spectrum of pathogens: 77.7% of UTIs were caused by E. coli, 5.2% have Proteus mirabilis, 2.8% have Klebsiella spp., in 3.9% - other members of the family Enterobacteriaceae, 4.6% have Staphylococcus saprophyticus and 5.8% - other microorganisms. Moreover, the absence of sensitivity in the isolated strains of microorganisms to ampicillin occurred in 29.8% of cases, sulfamethoxazole - in 29.1%, trimethoprim - in 14.8% of cases. Strain resistance E. coli to ciprofloxacin, Co-amoxiclav, nitrofurans, gentamicin and fosfomycin trometamol was detected in less than 3% of patients.

In a study of the sensitivity of microorganisms isolated from UTI patients to 10 antimicrobial drugs, conducted in Russia in 1999, it was found that the lowest level of resistance of enterobacteria was to fluoroquinolones (norfloxacin and ciprofloxacin) and nitrofurantoin (the frequency of isolation of resistant strains was 2, 6-2.9%). For ampicillin and co-trimoxazole, this figure was at the level of 33.3% and 20.3%, for gentamicin and non-fluorinated quinolones it was 4.4-5.9%.

According to studies of the resistance of uropathogenic flora to antibacterial drugs conducted in Moscow and 4 cities of Russia in the early 2000s, the frequency of resistance E. coli to nalidixic acid ranged from 8.9% to 22.2%, between ciprofloxacin and levofloxacin, complete cross-resistance was noted, its frequency ranged from 4.8% to 16%. 33.9-40.6% of strains were resistant to ampicillin, 12.1-25.9% to protected penicillins, 0.8-6.8% to cefuroxime, resistance to cephalosporins III generation- 0-3.1% of strains, to nitrofurantoin - 1.2-11.6%. The highest level of resistance was noted to co-trimoxazole - 19.4-31%. Among the rarer Gram-negative UTIs ( Klebsiella spp., Proteus spp. etc.) the frequency of resistance to all antibacterial drugs was 5-7% higher.

As of 2010-2011 in the Moscow region, the main causative agents of acute uncomplicated cystitis in women of childbearing age were: E. coli (81%), Klebsiella pneumoniae (6,9%), Staphylococcus epidermidis(5.2%) and Enterococcus spp. (5.2%). The highest sensitivity of pathogens was noted to levofloxacin (98.3%), fosfomycin (94.8%) and co-trimoxazole (100%), resistance was noted Escherichia coli to amoxicillin / clavulanate and ampicillin - in 21.2% and 10.6% of cases, respectively, all uropathogens - in 22.4% and 13.8% of cases, respectively.

As part of a prospective study of the dynamics of antibiotic resistance of causative agents of community-acquired UTIs in various subpopulations of patients - DARMIS (2010-2011), 903 community-acquired strains of uropathogens from 26 centers (polyclinics and hospitals) in 18 Russian cities were analyzed. The study included strains obtained from children and adults of both sexes of all age groups with acute (and exacerbation of chronic) community-acquired UTIs, including pregnant women with asymptomatic bacteriuria when the pathogen is isolated in a diagnostically significant titer according to the recommendations of the European Association of Urology (EAU). Of the 518 strains of uropathogens obtained in the adult subpopulation, 429 strains (82.8%) were isolated from non-pregnant patients and 89 strains (17.2%) from male patients. The total proportion of family members Enterobacteriaceae amounted to 80.5%, of which E. coli— 63,5%,K. pneumoniae — 8,9%, P. mirabilis — 3,5%, Enterobacter spp. - 2.1%, others - 2.5%. In addition, the structure of UTI pathogens included: E. faecalis — 6,6%, Staphylococcus spp. — 6.2%, P. aeruginosa- 3.1%, others - 3.7%.

Most active in relation to E. coli possessed fosfomycin (98.5%), nitrofurans - 98.2% and ceftibuten - 92.7%; for all members of the family Enterobacteriaceae- fosfomycin (92.1%), ceftibuten (88.5%) and nitrofurans (86.4%). 87.5% of strains were susceptible to cefixime E. coli and 82.1% of all strains Enterobacteriaceae. In adults, there was a high frequency of isolation of resistant strains E. coli to ampicillin (46.6%), piperacillin (42.2%), inhibitor-protected penicillins - ampicillin / sulbactam (40.1%) and amoxicillin / clavulanate (41.7%), trimethoprim / sulfamethoxazole (26.8%), fluoroquinolones - ciprofloxacin (20.1%) and levofloxacin (19.5%). Resistance indicators of strains of the family Enterobacteriaceae were higher than resistance rates for strains E. coli and amounted to: for ampicillin - 54.6%, piperacillin - 44.1%, ampicillin / sulbactam - 43.6%, amoxicillin / clavulanate - 43.9%, trimethoprim / sulfamethoxazole - 26.9%, ciprofloxacin and levofloxacin - 22 .1% and 21.6%, respectively.

Based on the above data and other studies, it follows that there is a clear trend towards an increase in the resistance of uropathogenic strains, primarily E. coli, to antibacterial drugs that are traditionally widely prescribed for community-acquired UTIs. Against this background, a low level of stability remains E. coli to nitrofurans and third-generation cephalosporins.

The place of nitrofurans in the treatment of uncomplicated UTIs

In this situation, it follows that the attractiveness of nitrofurans for practical medicine is determined by a combination of high natural activity against all significant pathogens of uncomplicated UTI and low price, and high clinical efficacy, among other things, depends on patient compliance, which is largely determined by the cost of treatment.

Nitrofurans as antibacterial agents known since the 1940s. After the introduction of a number of new antimicrobial drugs into clinical practice, interest in nitrofurans fell sharply. Fluoroquinolones have significantly replaced nitrofurans in the treatment of UTIs and infections gastrointestinal tract, and nitrofurans in the West were almost forgotten. So, in 1998, the next 29th edition of the well-known in the United States guide for practitioners "Washington Guide to Medicines" did not mention at all even the most famous representative of nitrofurans - nitrofurantoin (Furadonin). However, a decade later, the 32nd edition of this guideline stated that nitrofurantoin in the treatment of UTIs is "experiencing a rebirth".

The mechanism of action of nitrofurans

The mechanism of action of nitrofurans on the microbial cell and in particular the uropathogen is multifactorial. The mechanism of action of nitrofurantoin (and, consequently, its analogue, furazidin), which is not similar to other antimicrobial agents, has been studied in the most detail. It consists in damage to the ribosomal proteins of bacteria, which leads to the disruption of many vital parameters of the bacterium at once - the suppression of protein synthesis, aerobic energy metabolism, the synthesis of nucleic acids and the cell wall. Nitrofurans are oxygen acceptors and disrupt the process of cellular respiration, in addition, they inhibit the activity of a number of cell respiratory enzymes (pyruvate oxidase, glutathione reductase, aldehyde dehydrogenase). Preparations undergo intracellular transformation: the process of reduction of the nitro group occurs under the action of bacterial flavoproteins. As a result, metabolites of nitrofurans are formed, which have a cytotoxic effect. The drugs inhibit the biosynthesis of microbial DNA and, to a lesser extent, RNA. The mechanism of action of nitrofurans is specific only for drugs of this group. In experiment in vitro a distinct antioxidant effect of Furagin (furazidin) was revealed.

Such a multifactorial disturbance of microbial cell metabolism is the basis of the main advantage of nitrofurantoin and its analogue furazidin relative to other antibacterial agents - an extremely low probability of the emergence of microbial resistance to it, which is demonstrated by the results of clinical studies presented above. The latter circumstance is the basis clinical application nitrofurantoin. It should also be taken into account that the rules of rational chemotherapy require preference for antimicrobial drugs with a narrow spectrum of activity. Thus, nitrofurantoin and furazidin have a narrower spectrum of antibacterial activity compared to fluoroquinolones, which avoids the development of intestinal microbiota disorders, especially since it is irrational to use powerful antimicrobial agents with a wide spectrum of activity in relatively mild infections to prevent the development of resistance to antibacterial drugs.

biological fluids(blood, blood serum, urine, cerebrospinal fluid, etc.) do not reduce the antibacterial activity of nitrofurans; the activity of drugs does not change in the presence of para-aminobenzoic acid and novocaine. Antagonists of nitrofurans are B vitamins, which can prevent nitrofurans from inhibiting the respiratory enzymes of the cell. Indicate antagonism between nitrofurantoin and furazidin with nalidixic acid, which may reduce therapeutic effect quinolone.

Antimicrobial spectrum of action of nitrofurans

Includes microorganisms that are important in the pathology of purulent-inflammatory processes and intestinal infections in humans. These include: 1) a large group of gram-negative aerobic bacteria - E. coli, Shigella spp., Salmonella spp., Proteus spp., Klebsiella spp., Aerobacter faecalis, Aerobacter aerogenes, Vibrio cholerae, Haemophillus spp.; 2) gram-positive aerobic bacteria Staphylococcus spp., Streptococcus spp. (first of all S. pyogenes), Corynebacterium spp.; 3) pathogenic fungi - Candida albicans, Microsporum spp., Trichophyton spp.; 4) some protozoa - Trichomonas vaginalis, Lamblia intestinalis, Entamoeba histolytica.

The problem of drug resistance in relation to nitrofurans

Resistance is cross-prone only within this class of drugs. Bacterial strains resistant to sulfonamides, β-lactams, aminoglycosides, chloramphenicol, tetracyclines, fluoroquinolones remain sensitive to nitrofurans, however, if cell transport systems are disrupted, it can be assumed that cross-resistance between nitrofurans and other classes of antibacterial drugs develops.

Accordingly, an analysis of the results of a broad study of the sensitivity of clinical strains of bacteria in UTI to a spectrum of antibacterial drugs confirms the slow development of drug resistance of bacteria to nitrofurans, despite the use of these drugs in clinical practice for more than 70 years (since 1944).

Pharmacokinetics

Most nitrofurans after oral administration are well absorbed, their bioavailability varies from 50% to 90-95%. Nifuroxazide is practically not absorbed. Nitrofurans do not provide therapeutic concentrations in the blood and tissues, as they are quickly excreted from the body, mainly by the kidneys, mainly by glomerular filtration. The half-life (T1 / 2) from the blood for most drugs is within 1 hour, respectively, their plasma concentrations are low and vary widely. Therapeutic levels of drugs (concentrations significantly higher than the minimum inhibitory concentrations - MIC) are achieved only in the urine and in the contents of the intestine. Depending on the characteristics of the metabolism of nitrofuran in the body, there is also a level active drug in urine. Drugs that are metabolized in the body to a lesser extent accumulate in the urine in very high concentrations, providing a bactericidal effect against the main pathogens of UTIs. These include nitrofurantoin and Furagin.

Nitrofurans do not pass well through histohematic barriers, some drugs (nitrofurantoin) in small amounts can penetrate into breast milk. Nitrofurans are metabolized mainly in the liver, partly in muscle tissue and the intestinal wall.

Tolerability, side effects

Nitrofurans are characterized by a narrow therapeutic latitude and are used in low therapeutic doses. Nitrofurantoin and nitrofural (Furacilin) ​​are more toxic (LD50 when administered orally at the level of 166 mg/kg), furazidin (Furagin) and furazolidone (LD50 2813 and 1807 mg/kg, respectively) are much better tolerated. Furazidin is also characterized by the highest maximum tolerated dose (2000 mg / kg with a single injection of the drug intragastrically in experiments on mice).

When used in the clinic, nitrofurans can cause pain and discomfort in epigastric region, loss of appetite, nausea, less often diarrhea and vomiting, an attack of pancreatitis, a transient increase in transaminases. Allergic reactions to nitrofurans are cross to all 5-nitrofuran derivatives and can manifest as skin rash and itching, arthralgia and myalgia, eosinophilia, fever, very rarely - anaphylactic shock. Rare adverse reactions are: 1) reactions from respiratory system(allergic pneumonitis - pain in the area chest, cough, shortness of breath, fever) more often in elderly patients, appear during the first week of treatment, usually reversible after stopping treatment; pulmonary fibrosis; 2) reactions from the nervous system in the form of dizziness, drowsiness and fatigue, headache; the occurrence of polyneuropathies (numbness, tingling, burning of the skin of the face, peripheral neuropathies, muscle weakness); 3) hematological reactions (granulocytopenia, leukopenia, anemia, decreased platelet aggregation, very rarely - hemolytic anemia).

The risk of adverse reactions increases with impaired renal function and the use of drugs that block tubular secretion. This reduces the efficiency antibiotic therapy with UTI, since the necessary therapeutic concentrations in the urine are not provided and the risk of adverse reactions increases due to an increase in the parent drug and its metabolites. With a decrease in liver function, the risk of adverse reactions increases due to a decrease in the metabolism of the drug in the liver and an increase in the concentration of free nitrofuran in the blood. risk of haematological reactions, pneumonitis, pulmonary fibrosis during therapy with nitrofurans, it increases when they are used together with drugs that depress hematopoiesis in patients with glucose-6-phosphate dehydrogenase deficiency. Nitrofurans have only minor nephrotoxicity.

It is necessary to note some features of adverse reactions depending on the drug. During therapy with Furazolidone and the simultaneous intake of alcohol, in some cases, incompatibility is possible according to the type of disulfiram-like reactions; the patient should not use alcoholic drinks during treatment and within 4 days after discontinuation of the drug. Furazolidone acts as a monoamine oxidase (MAO) inhibitor, which, if the dosage of the drug is exceeded in some patients, can cause a sudden increase in blood pressure. The drug should not be used simultaneously with MAO inhibitors, including tricyclic antidepressants, and products containing tyramine and other vasoconstrictive amines should be avoided. Not currently indicated for UTIs as it does not produce therapeutic urinary concentrations. Nitrofurantoin should not be administered simultaneously with drugs that have neurotoxic and hepatotoxic effects; when therapeutic doses are exceeded (from 10 mg / kg per day and above), a moderate delay in spermatogenesis is possible. Patients with diseases respiratory tract use with caution under medical supervision (risk of developing pneumonitis). Furazidin is similar to nitrofurantoin, but less toxic and better tolerated.

Special conditions of use

By modern ideas the use of nitrofurantoin is safe in early pregnancy, but is contraindicated from the 38th week and beyond due to potential risk development hemolytic disease newborns. The use of nitrofurantoin is allowed during breastfeeding and in children older than one month. Furazidin is distributed exclusively in the CIS and a number of countries of Eastern Europe, so it does not have the Food and Drug Administration (FDA) pregnancy risk categories. According to available data, like nitrofurantoin, furazidin is not contraindicated in either pregnant or lactating women. Mention should be made of a case-control study conducted in Hungary, which included 38,151 pregnant women who gave birth to babies without any defects (control group) and 22,865 pregnant women whose newborns or fetuses had congenital anomalies (case group) between 1980 and 1996. In both groups, 0.7% of women received furazidin. A case-control analysis did not reveal a teratogenic potential for the use of furazidin during 2-3 months of pregnancy, i.e. in critical period for the development of major congenital anomalies. In pediatrics, the use of furazidin preparations is also allowed from one month of life. Nitrofurantoin weakens the action of nalidixic acid. It is considered inappropriate to prescribe the following combinations: Furagin with Levomycetin, Furagin with sulfonamides.

Indications for use

The main field of application of nitrofurans as chemotherapeutic drugs in accordance with antimicrobial activity and pharmacokinetic properties is bacterial UTIs, primarily acute uncomplicated processes, and some acute intestinal infections - bacterial diarrhea and shigellosis. Among nitrofuran preparations, nitrofurantoin is widely used abroad, Furagin is more common in our country. According to a large number of authors, furozalidon and furazidin are recommended for the treatment of acute cystitis, long-term suppressive therapy chronic pyelonephritis. There is an opinion about the expediency of prescribing nitrofurans in acute uncomplicated pyelonephritis, as alternative means treatment of uncomplicated UTIs.

Modern recommendations in the era of global growth in the resistance of uropathogens to ampicillin and co-trimoxazole justify the appointment of a fluoroquinolone for 3 days, or fosfomycin once, or nitrofuran for 7 days as an empirical therapy for acute cystitis.

There are also recommendations that if it is necessary to carry out therapy with uroseptics for a long time, with a change of drugs every 7-10 days, it is advisable to consistently apply drugs that act on the bacterial wall and metabolism. bacterial cell: Penicillin and Erythromycin, cephalosporins and Levomycetin, cephalosporins and nitrofurans to prevent the survival of protoplast and L-forms of bacteria.

Furazidin and nitrofurantoin should also be prescribed to "vulnerable" categories of the population - children, pregnant and lactating women, since alternative drugs- fluoroquinolones are contraindicated in pediatrics (under 18 years of age), during lactation and are not completely safe during pregnancy (category C, according to the FDA classification, i.e. the risk to the fetus cannot be excluded).

Contraindications for use: allergic reactions on nitrofurans, renal failure (nitrofurantoin, furazidin); severe liver pathology (Furazolidone), deficiency of glucose-6-phosphate dehydrogenase, pregnancy - III trimester (nitrofurantoin), newborns.

Conclusion

Currently, one of the main problems in the treatment of UTIs is the high level of resistance of pathogens to the most widely used antibacterial agents. For inclusion in the treatment regimen for uncomplicated UTIs from nitrofuran derivatives, only nitrofurantoin and furazidin preparations should be used, since an analysis of the results of a wide study of the sensitivity of clinical strains of bacteria in UTIs revealed a slow development of drug resistance of bacteria to them, despite the long period of their use. At the same time, according to a large number of studies, furazidin is less toxic and better tolerated. An important factor, which, among other things, ensures high compliance of patients, is the rather low cost of the drug. From this point of view, the attention of clinicians may be attracted by the drug furazidin - Urofuragin, which combines high clinical efficacy in the treatment of UTIs due to the low frequency of resistance of the uropathogenic flora inherent in furazidin, economic availability and a high production culture in accordance with the criteria of GMP (Good Manufacturing Practice) .

Literature

1. Lokshin K. L. Treatment of acute uncomplicated lower and upper infections urinary tract(cystitis and pyelonephritis): the place of fluoroquinolones in modern conditions // Effective pharmacotherapy. 2014; 15. No. 2: 8-13.
2. Foxman B. Brown P. Epidemiology of urinary tract infections: transmission and risk factors, incidence, and costs // Infect. Dis. Clin. North Am. 2003; 17(2):227-241.
3. Arkhipov E. V., Sigitova O. N., Bogdanova O. R. Modern recommendations for the diagnosis and treatment of pyelonephritis from the standpoint evidence-based medicine// Herald of modern clinical medicine. 2015; 8 (6): 115-120.
4. Sinyakova L. A. Antibacterial therapy of acute cystitis in the era of growing resistance of pathogens // Therapeutic archive. 2014; 4:125-129.
5. Hoodon T.M. Uncomplicated urinary tract infection // New Engl J Med. 2012; 366:1028-1037.
6. Naber K. G., Schito G., Botto H. et al. Surveillance study in Europe and Brazil on clinical aspects and Antimicrobial Resistance Epidemiology in Females with Cystitis (ARESC): implications for empiric therapy // Eur Urol. 2008; 54(5): 1164-1175.
7. Foxman b. Epidemiology of urinary tract infections: incidence, morbidity, and economic costs // Am J Med. 2002; 113 (Suppl 1A): 5S-13S.
8. Laurent O. B. Epidemiological aspects of urinary tract infections. Proceedings of the international symposium "Urinary tract infections in outpatients". M., 1999. S. 5-8.
9. Palagin I. S., Sukhorukova M. V., Dekhnich A. V., Eidelstein M. V., Shevelev A. N., Grinev A. V., Perepanova T. S., Kozlov R. S.., research group "DARMIS". The current state of antibiotic resistance in pathogens of community-acquired urinary tract infections in Russia: results of the DARMIS study (2010-2011) // Klin. microbiol. and antimicrobial. chemother. 2012; 14(4): 280-302.
10. Warren J. W., Abrutyn E., Hebel J. R., Johnson J. R., Schaeffer A. J., Stamm W. E. Guidelines for antimicrobial treatment of uncomplicated acute bacterial cystitis and acute pyelonephritis in women. Infectious Diseases Society of America (IDSA) // Clin Infect Dis. 1999; 29(4): 745-758.
11. Kahlmeter G. An international survey of the antimicrobial susceptibility of pathogens from uncomplicated urinary tract infections: the ECO. SENS Project // J. Antimicrob. Chemother. 2003; 51(1): 69-76.
12. Strachunsky L. S. Norfloxacin (Nolicin) in the treatment of urinary tract infections. Urinary tract infections in outpatients. Proceedings of the international symposium, M., 1999. S. 29-32.
13. Sidorenko S. V., Ivanov D. V. Results of studying the spread of antibiotic resistance among community-acquired pathogens of urinary tract infections in Moscow. Phase I // Antibiotics and Chemotherapy 2005, 50: 3-10.
14. Rafalsky V. V., Strachunsky L. S., Krechikova O. I., Eidelstein I. A., Akhmetova L. I., Babkin P. A., Gugutsidze E. N., Ilyina V. N., Kogan M I., Kopylov V. V. et al. Resistance of causative agents of outpatient urinary tract infections according to multicenter microbiological studies UTIAP-I and UTIAP-H // Urology. 2004: 13-17.
15. Strategy and tactics rational use antimicrobial agents in outpatient practice: Russian practical recommendations / Ed. S. V. Yakovleva, S. V. Sidorenko, V. V. Rafalsky, T. V. Spichak. M.: Presto Publishing House, 2014. 121 p.
16. Lokshin K. L., Gevorkyan A. R., Evdokimov M. E. Analysis of the effectiveness of standard antibiotic therapy and the risk of recurrence of acute uncomplicated cystitis in women of childbearing age. Open randomized comparative study // Consilium medicum. 2012; 14(4):51-56.
17. Cooper D.H. et al. The Washington Manual™ of Medical Therapeutics. 32nd ed. Lippincott Williams & Wilkins, 2007. P. 354.
18. Vdovichenko V. P., Bronskaya G. M., Korshak T. A., Kazakevich D. V., Sokolov N. K., Shchevruk A. N., Akulenets E. V. Nitrofurans in the pharmacotherapy of urinary tract infections // Medical News. 2012: 3; 38-41.
19. Blyuger A.F. Nitrofurans and their application in medicine. Riga: Publishing House of the Academy of Sciences of the Latvian SSR, 1958.
20. Information about medicines for healthcare professionals. Issue. 3. Antimicrobial and antiviral medicines. USP D.I. Russian edition. M.: RC "Farmedinfo", 1998. S. 317-319, 347-351.
21. Padeyskaya E. N. Furamag in a series of antimicrobial drugs derived from 5-nitrofuran: implications for clinical practice // Consilium medicum. 2004: 6(1).
22. Pasechnikov S. P., Mitchenko M. I. The use of furamag in the treatment of acute pyelonephritis // Urology. 2002; 4:16-20.
23. Paul H. E., Paul M. F. The Nitrofurans - Chemotherapeutic properties. - Experimental Chemotherapy, Ed. Schnitzer R. J., Hawking F., vol. II, Chemotherapy of bacterial infections, Part I, Academic Press, New-York-London, 1964; 307-370.
24. Hardman J.G. et al. Goodman & Gilman's The Pharmacological Basis of Therapeutics. 9th ed. McGraw-Hill, 1996. P. 1069.
25. Katzung B.G. Basic & Clinical Pharmacology. 9th ed. McGraw-Hill, 2009. P. 820-826.
26. Makareeva E. N., Lozovskaya E. L., Tatikolov A. S., Sapezhinsky I. I. Photosensitizing properties and antioxidant activity of furagin, an antimicrobial drug, a derivative of nitrofuran // Biophysics. 1997; 42(2): 472-479.
27. Strachunsky L. S., Belousov L. B., Kozlov S. N. Modern antimicrobial chemotherapy: a guide for physicians. M.: Borges, 2002. C. 143-146.
28. Practical guide to anti-infective chemotherapy / Ed. L. S. Strachunsky, Yu. N. Belousov, S. N. Kozlov. Smolensk: MACMAH, 2007. S. 128-130.
29. Korovina N. A., Zakharova I. N., Strachunsky L. S. and etc. Practical recommendations on antibacterial therapy of infections of the urinary system of community-acquired origin in children // Klin. microbiol. and antimicrobial. chemother. 2002; 4(4):337-346.
30. Pereverzev A. S., Rossokhin V. V., Adamenko A. N. Clinical efficacy of nitrofurans in urological practice// Men's health. 2002; 3:24-26.
31. Sakharchuk V. P., Lemeshev A. F. Reference book of the doctor. Minsk: Publisher Yu. L. Gladkiy, 1994. P. 32.
32. Dovbysh M. A. The use of furamag for the treatment and prevention of infections of the upper urinary tract // Dermatovenerology. Cosmetology. Sexopathology. 2002; 1-2: 12-14.
33. Ivanov D. D., Kushnirenko S. V. Modern approaches to the treatment of recurrent urinary tract infections. Clinical immunology. 2007; 6 (11); 1-3.
34. Shatokhina O. V. Comparative efficacy of anti-relapse therapy with furagin and furamag in urinary tract infections in children. Vestn. pediatrician, pharmacology and nutrition. 2006. V. 3, No. 6. S. 10-15.
35. Tarascon Pocket Pharmacopoeia. Loma Linda, 2010. 336 p.
36. Cztizel A. E., Rockenbauer M., Sorensen H. T., Olsen J. A population-based case-control rteratologic study of furazidine, a nitrofuran-derivative treatment during pregnancy // Clin Nephrol. 2000; 53(4): 257-263.
37. Mkrtchyan V. R., Orlov V. A. The tactics of using uroseptics in general practice// Attending doctor. 2008, no. 8.
38. Lopatkin N. A., Derevianko I. I. Antibacterial therapy program for acute cystitis and pyelonephritis in adults. Infections and Antimicrobe. ter. 1999; 1(2):57-58.
39. Naber K. G., Bergman B., Bishop M. K. and other Recommendations of the European Association of Urology for the treatment of urinary tract infections and infections of the reproductive system in men // Klin. microbiol. and antimicrobial. chemother. 2002; 4(4): 347-363.
40. Gupta K., Hooton T. M., Stamm W. E. Increasing antimicrobial resistance and the management of uncomplicated community-acquired urinary tract infections // Ann Intern Med. 2001; 135:41-50.
41. Gilbert D. N., Moellering R. C., Eliopoulos G. M., Chambers H. F., Michael S., Saag M. D. The Sanford Guide to Antimicrobial Therapy, (Guide to Antimicrobial Therapy (Sanford)). 40th edition. 2010. 119 p.
42. Gomella L. G., Haist S. A. Clinician's Pocket Drug Reference. McGraw-Hill, 2004. P. 127-129.
43. Koda-Kimble M.A. et al. Handbook of Applied Therapeutics. 7th ed. Lippincott Williams & Wilkins, 2002. 44.19, 61.4, 61.5.
44. Kostowski W. Farmakologia/Podstawy farmakoterapii. wyd. II. PZWL, 2001. S. 956-958.
45. Presacco J. Medical Drug Therapy. Lippincott Williams & Wilkins, 2003. P. 339.
46. Belousov Yu. B., Moiseev V. S., Lepakhin V. K. Clinical pharmacology and pharmacotherapy. Guide for doctors. 2nd ed. correct and additional M.: Universum Publishing, 1997. 531 p.
47. Blondeau J.M. Current issues in the management of urinary tract infections // Drugs. 2004; 64(6): 611-628.
48. Hooton T. M., Besser R., Foxman B. et al. Acute uncomplicated cystitis in an era of increasing antibiotic resistance: a proposed approach to empirical therapy // Clin Infect Dis. 2004; 39:75-80.

A. N. Kazyulin,doctor medical sciences, Professor, Academician of the Russian Academy of Natural Sciences

Nitrofurans

antimicrobial agents that are chemically derivatives of 5-nitrofuran.

N. used in medical practice include furatsilin, furagin, furadonin, furazolidone and furazolin. N. have a wide spectrum of antimicrobial activity and are active against many gram-positive and gram-negative bacteria (streptococci, staphylococci, diplococci, coli, shigella, salmonella, proteus, spore-forming anaerobes, etc.), as well as trypanosomes, leptospira, coccidia, trichomonads, giardia and a number of other microorganisms, including those strains that are resistant to antibiotics (Antibiotics) and sulfanilamide preparations (Sulfanilamide preparations). to N. develops much more slowly than to antibiotics. Concerning N.'s viruses are not active. According to the spectrum of antimicrobial action and activity against a number of pathogens, drugs of the H. group differ somewhat from each other. So, furatsilin acts mainly on gram-positive and gram-negative, furazolidone is most active against gram-negative bacteria, Trichomonas and Giardia, and furazolin affects mainly gram-positive bacteria.

When taken orally, N. is absorbed from the gastrointestinal tract to an unequal degree. N. are allocated from an organism mainly through in the form of metabolites and partially in not changed look. By being excreted through the kidneys in unchanged form N. differ from each other. So, in a person with urine, 19.1-32.6% of the oral dose of furadonin, 9.6-20.9% - furagin, 6.2-9.9% - furazolidone and 1-3.1 % - furatsilina. In the body, in the process of biotransformation, the nitro group at the furan ring of the H. molecule can be reduced to an amino group, as a result of which the drugs lose their antimicrobial activity. Further N. occurs by acetylation.

Assign N. mainly externally and internally. For parenteral administration, soluble furagin is used, which is the potassium salt of furapt. Outwardly, N. is used for the treatment of purulent-inflammatory lesions of the skin and mucous membranes. Inside, drugs in this group are prescribed as chemotherapeutic agents for the treatment of mainly infections of the gastrointestinal tract and urinary tract.

Contraindications to the use of N. are increased individual to the drugs of this group, severe diseases of the heart, liver and kidneys.

When applied externally, N. usually does not cause side effects. In some cases, they develop. When taken orally, N. can cause a decrease in appetite, nausea, vomiting, and allergic reactions (exanthema, enanthema). With prolonged use, neuralgia and are possible. In the event of side effects during N. therapy, antihistamines and group B are used. side effects reduce the dose or stop taking the drug. Preparations of group N., their doses, methods of application, forms of release and storage conditions are given below.

Lifusol(Lifusolum) - aerosol containing furatsilin, linetol, resin special composition, and a mixture of refrigerants. When the solvent evaporates, it forms an elastic yellowish film on the surface treated with the preparation, which protects the wound surfaces from contamination and has an antimicrobial effect due to the presence of furacilin. Used to protect surgical wounds and postoperative sutures against infection, to protect the skin from maceration in fistulas and to protect and treat skin wounds, sealing of channels in places of an exit of drainages and catheters. applied by spraying from a special container on the surface of the skin to be treated, previously cleaned with cotton wool or gauze soaked in ether. On bleeding and weeping, the drug is not applied. Release form: in aerosol cans of 94 and 200 ml. Storage: at room temperature away from existing heating devices; protect from moisture and direct sunlight.

Ointment "Fastin"(Unguentun "Fastinum") contains furatsilin (2%), synthomycin (1.6%), anestezin (3%) and ointment base (up to 100%). Used externally for burns I-III degree, purulent wounds and. Usually applied to sterile gauze pads or directly to the affected skin surface. change after 7-10 days (more often if necessary). Release form: in orange glass jars of 50 G. Storage: in a cool place.

Furagin(Furaginum) is given orally (after meals) and topically. Inside the drug is used for urinary tract infections (pyelonephritis, cystitis, etc.) at 0.1-0.2 G 2-3 times a day courses for 7-10 days. Repeated courses of treatment are carried out with intervals of 10-15 days. Outwardly, furagin is used as a solution (1:13,000) for isotonic solution sodium chloride for washing and douching in surgical and obstetric-gynecological practice, as well as in the form eye drops(water solution 1:13,000) for the treatment of keratitis, conjunctivitis. Release form: and tablets of 0.05 G. Storage: list B, in a dry, dark place.

Furagin soluble(Furaginum solubile; synonym: furaginum potassium salt, solafur) is administered intravenously by drip (slowly) for severe infectious diseases (sepsis, pneumonia), wound and purulent infections caused by microorganisms sensitive to the drug. Daily allowance for adults 300-500 ml 1% solution of the drug. The drug is administered daily or every 1-2 days. Release form: powder. Storage: in a well-closed container, protected from light.

Furadonin(Furadoninum; synonym: nitrofurantoin, etc.) is used for urinary tract infections (pyelitis, pyelonephritis, cystitis, urethritis) and to prevent infectious complications during urological operations and manipulations. Assign inside adults at 0.1-0.15 G 3-4 times a day. The duration of the course of treatment is 5-8 days. For children, the drug is prescribed at the rate of 5-8 mg/kg per day (in 3-4 doses). Higher doses for adults inside: single 0.3 G, daily 0.6 GG and tablets, soluble in the intestine, 0.03 each (for children) and 0.1 G. Storage: in a dry, dark place.

Furazolidone(Furazolidonum; synonym: diafuror, furoxon, etc.) is used as a chemotherapeutic agent for intestinal infections ( bacillary dysentery, paratyphoid, food poisoning), as well as trichomoniasis and giardiasis. For intestinal infections, the drug is prescribed orally (after eating) for adults at 0.1-0.15 G 4 times a day for 5-10 days. For children, doses are reduced according to age. With trichomonas colpitis, furazolidone is prescribed orally at 0.1 G 3-4 times a day for 3 days and simultaneously administered in 5-6 G powder containing furazolidone with milk sugar in a ratio of 1:400 or 1:500, and in the rectum - containing 0.004-0.005 G furazolidone. Intravaginally and rectally, the drug is administered daily for 1-2 weeks. At Trichomonas urethritis in men, furazolidone is prescribed orally at 0.1 G 4 times a day for 3 days. With giardiasis, the drug is used orally for adults at 0.1 G 4 times a day, children in a daily dose at the rate of 10 mg/kg(in 3-4 doses). Higher doses for adults inside: single 0.2 G, daily 0.8 G. Release form: tablets of 0.05 G. Storage: list B; in a place protected from light.

Furazolin(Furazolinum; synonym: furaltazone, etc.) is used to treat infections caused by gram-positive and gram-negative bacteria (staphylococci, streptococci, pneumococci, etc.), such as wound infections, septicemia, erysipelas, staphylococcal enteritis, pneumonia, osteomyelitis, meningitis, etc., as well as urinary tract infections. Assign inside (after 15-20 min after meals) for adults 0.1 G 3-4 times a day. Children are prescribed depending on age: up to 1 year at 0.01-0.015 G appointment; 1-2 years at 0.02 G; 2-5 years at 0.03-0.04 G; 5-15 years at 0.05 G 3-4 times a day. The course of treatment is 5-7 days, in severe cases up to 14 days. Release form: tablets of 0.05 G. Storage: list B; in a dry place protected from light.

Furacilin(Furacilinum; synonym: furacin, nitrofural, etc.) is used mainly externally in the form of 0.02% (1:50,000) aqueous solution for the treatment of purulent wounds, bedsores, ulcers, II and III degree burns, for washing the pleural cavity after suction of pus in case of pleural empyema, as well as for washing the accessory cavities of the nose. For the treatment of conjunctivitis, furatsilin is used in the form of eye drops. With blepharitis, the edges of the eyelids are smeared with 0.2% furacilin ointment. alcohol solution furatsilina 0.066% (1:1500) is used for chronic purulent otitis media. Inside, furatsilin is prescribed for adults at 0.1 G 4-5 times a day for 5-6 days for the treatment of bacillary dysentery. If necessary, repeat after 3-4 days, assigning 0.1 G drug 4 times a day for 3-4 days. Higher doses for adults inside: single 0.1 G, daily 0.5 G. Release form: powder, tablets of 0.02 for the preparation of solutions for external use, tablets of 0.1 G for internal use, ointment 0.2%. Storage: list B; in well-corked dark glass jars, protected from light; tablets - in a place protected from light.

1. Small medical encyclopedia. - M.: Medical Encyclopedia. 1991-96 2. First health care. - M.: Great Russian Encyclopedia. 1994 3. Encyclopedic Dictionary medical terms. - M.: Soviet Encyclopedia. - 1982-1984.

See what "Nitrofurans" are in other dictionaries:

Nitrofurans are a group of antibacterial agents. Gram-positive and gram-negative bacteria, as well as chlamydia and some protozoa (Trichomonas, Giardia), are sensitive to nitrofurans. Nitrofurans usually act on microorganisms ... ... Wikipedia

Furan derivatives in which the hydrogen atom is replaced by a nitro group. N. have a wide spectrum of antimicrobial action, which is based on their ability to inhibit the respiration of microbial cells. In surgery, N. is used in the treatment of wounds and ... ... Medical Encyclopedia

Active ingredient ›› Furazidin (Furazidin) Latin name Furamag ATX: ›› J01XE Nitrofuran derivatives Pharmacological group: Other synthetic antibacterial agents Nosological classification (ICD 10) ›› L08.9 Local ... ... Medicine Dictionary

CYSTITIS- - inflammation of the bladder. Predisposing factors for the development of cystitis are trauma to its mucous membrane, stagnation of blood in the veins of the pelvis, hormonal disorders, beriberi, hypothermia, etc. Violation is of great importance ... ... Encyclopedic Dictionary of Psychology and Pedagogy

- (Greek dysentería, from dys... prefix meaning obstruction, disorder, and énteron gut) acute or chronically relapsing infection human, accompanied by a predominant lesion of the large intestine. … … Great Soviet Encyclopedia

A drug from the group of nitrofurans (See Nitrofurans); has an antimicrobial effect against staphylococci, streptococci, dysenteric bacillus, etc. It is used externally in solutions and ointments for the treatment and prevention ... ... Great Soviet Encyclopedia

Conventional name for various groups medicines used for chemotherapy and chemoprophylaxis. As H. with. use substances of natural origin (for example, a number of antibiotics) and synthetic drugs (for example, ... ... Great Soviet Encyclopedia

Nitrofurans are the second class of synthetic antibacterial drugs proposed for wide medical use after sulfonamides. They are inferior in clinical efficacy to most antibiotics and are of value mainly in the treatment of acute uncomplicated forms of urinary tract infection ( nitrofurantoin, furazidin), intestinal infections (nifuroxazide) and some protozoal infections - trichomoniasis and giardiasis (furazolidone, nifuratel).

Mechanism of action

Being oxygen acceptors, nitrofurans disrupt the process of bacterial cellular respiration and inhibit the biosynthesis of nucleic acids. Depending on the concentration, they have a bacteriostatic or bactericidal effect. Rarely develops to nitrofurans drug resistance microorganisms.

Activity spectrum

Nitrofurans are characterized by a fairly wide spectrum of action and in high concentrations. in vitro active against many Gram-negative ( E.coli, K.pneumoniae etc.) and gram-positive bacteria, some anaerobes, fungi of the genus Candida. Enterococci are insensitive. Resistant P.aeruginosa, most strains of Proteus, Serration, Providence, Acinetobacter. In addition, furazolidone and nifuratel are active against some protozoa (Giardia, Trichomonas).

Pharmacokinetics

Among nitrofurans, the pharmacokinetics of nitrofurantoin has been better studied. When taken orally, nitrofurans are well and rapidly absorbed. They do not create high concentrations in the blood and tissues (including the kidneys), as they are quickly excreted from the body (half-life within 1 hour). Nitrofurantoin and furazidin accumulate in the urine in high concentrations, furazolidone - only in the amount of 5% taken dose(because it is largely metabolized). Partially excreted in the bile and create high concentrations in the intestinal lumen. With renal failure, the excretion of nitrofurans slows down significantly.

Adverse reactions

GIT: nausea, vomiting, diarrhea.

Liver: transient increase in transaminase activity, cholestasis, hepatitis.

Allergic reactions: rash, eosinophilia, fever, arthralgia, myalgia, lupus-like syndrome, rarely anaphylactic shock.

Lungs: pneumonitis (when taking nitrofurantoin), bronchospasm, cough, chest pain.

Nervous system: dizziness, headache, general weakness, drowsiness, peripheral polyneuropathy.

Hematological reactions: leukopenia, megaloblastic or hemolytic anemia.

Indications

When combined with chloramphenicol, the risk of hematopoietic inhibition increases.

When combined with alcohol, furazolidone can cause a disulfiram-like reaction.

With the simultaneous use of furazolidone, which is an MAO inhibitor, with other MAO inhibitors, sympathomimetics, tricyclic antidepressants or food products containing tyramine, there is a risk of developing a hypertensive crisis.

Information for patients

Take orally after meals, drink enough water (100-200 ml).

Strictly follow the regimen and treatment regimen during the entire course of therapy, do not skip the dose and take it at regular intervals. If you miss a dose, take it as soon as possible; do not take if it is almost time for the next dose; do not double the dose. Maintain the duration of therapy, especially with streptococcal infections.

Consult your doctor if there is no improvement within a few days or if new symptoms appear.

Do not drink alcoholic beverages during therapy with furazolidone and within 4 days after its cancellation.

During therapy with furazolidone, foods and drinks containing tyramine (cheese, beer, wine, beans, smoked meats) should not be consumed in large quantities.

During treatment with furazolidone, you should not take medicines for the treatment of coughs and colds without a doctor's prescription.

Be careful with dizziness.

Nitrofurantoin and furazidin can stain urine rusty yellow or brownish.

Table. Preparations of the nitrofuran group.
Main characteristics and application features

* With normal kidney function

Nitrofurans are the second class of synthetic antibacterial drugs proposed for wide medical use after sulfonamides. They are inferior in clinical efficacy to most antibiotics and are mainly important in the treatment of acute uncomplicated forms of urinary tract infection (nitrofurantoin, furazidin), intestinal infections (nifuroxazide) and some protozoal infections - trichomoniasis and giardiasis (furazolidone, nifuratel).

Mechanism of action

Being oxygen acceptors, nitrofurans disrupt the process of bacterial cellular respiration and inhibit the biosynthesis of nucleic acids. Depending on the concentration, they have a bacteriostatic or bactericidal effect. Drug resistance of microorganisms rarely develops to nitrofurans.

Activity spectrum

Nitrofurans are characterized by a fairly wide spectrum of action and are active in high concentrations in vitro against many gram-negative (E.coli, K.pneumoniae, etc.) and gram-positive bacteria, some anaerobes, fungi of the genus Candida. Enterococci are insensitive. Resistant P.aeruginosa, most strains of Proteus, Serration, Providence, Acinetobacter. In addition, furazolidone and nifuratel are active against some protozoa (Giardia, Trichomonas).

Pharmacokinetics

Among nitrofurans, the pharmacokinetics of nitrofurantoin has been better studied. When taken orally, nitrofurans are well and rapidly absorbed. They do not create high concentrations in the blood and tissues (including the kidneys), as they are quickly excreted from the body (half-life within 1 hour). Nitrofurantoin and furazidin accumulate in the urine in high concentrations, furazolidone - only in the amount of 5% of the dose taken (because it is largely metabolized). Partially excreted in the bile and create high concentrations in the intestinal lumen. With renal failure, the excretion of nitrofurans slows down significantly.

Adverse reactions

gastrointestinal tract: nausea, vomiting, diarrhea.

Liver: transient increase in transaminase activity, cholestasis, hepatitis.

allergic reactions: rash, eosinophilia, fever, arthralgia, myalgia, lupus-like syndrome, rarely - anaphylactic shock.

Lungs: pneumonitis (when taking nitrofurantoin), bronchospasm, cough, chest pain.

Nervous system: dizziness, headache, general weakness, drowsiness, peripheral polyneuropathy.

Hematological reactions: leukopenia, megaloblastic or hemolytic anemia.

Indications

infections lower divisions MVP: acute cystitis, suppressive therapy of chronic infections (nitrofurantoin, furazidin).

Prevention of infectious complications during urological operations, cystoscopy, bladder catheterization (nitrofurantoin, furazidin).

Intestinal infections: acute infectious diarrhea, enterocolitis (nifuroxazide, nifuratel).

Locally - washing of wounds and cavities (furazidin).

Contraindications

Allergic reactions to nitrofurans.

Renal failure (nitrofurantoin, furazidin).

Deficiency of glucose-6-phosphate dehydrogenase.

Newborns.

Warnings

Allergy. Cross to all derivatives of nitrofuran.

Pregnancy. The use of nitrofurantoin a during pregnancy is possible only in the II trimester. There are insufficient data on the use of other nitrofurans during pregnancy to recommend their use.

Lactation. Nitrofurans are able to penetrate into breast milk. Due to the immaturity of enzyme systems in newborns and the associated risk of hemolytic anemia, it is not recommended to use nitrofurans in lactating women.

Pediatrics. Nitrofurans should not be used in newborns due to the immaturity of enzyme systems and the associated risk of hemolytic anemia.

Geriatrics. In the elderly, it should be used with caution due to possible changes in kidney function. Dose reduction may be required. The risk of developing pneumonitis and peripheral polyneuropathy increases.

Impaired kidney function. Nitrofurantoin and furazidin are contraindicated in renal failure, since in this case they do not create therapeutic concentrations in the urine, accumulate and may have a toxic effect.

Impaired liver function. With the initial pathology of the liver, the risk of hepatotoxic action increases.

Other accompanying illnesses. The risk of peripheral polyneuropathy increases with anemia, diabetes mellitus, electrolyte imbalance, hypovitaminosis B. For the purpose of prevention, B vitamins should be prescribed.

Drug Interactions

The activity of nitrofurantoin and furazidin a decreases under the influence of quinolones.

When combined with chloramphenicol, the risk of hematopoietic inhibition increases.

When combined with alcohol, furazolidone can cause a disulfiram-like reaction.

With the simultaneous use of furazolidone, which is an MAO inhibitor, with other MAO inhibitors, sympathomimetics, tricyclic antidepressants or foods containing tyramine, there is a risk of developing a hypertensive crisis.

Information for patients

Take orally after meals, drink plenty of water (100-200 ml).

Strictly follow the regimen and treatment regimen during the entire course of therapy, do not skip the dose and take it at regular intervals. If you miss a dose, take it as soon as possible; do not take if it is almost time for the next dose; do not double the dose. Maintain the duration of therapy, especially with streptococcal infections.

Consult your doctor if there is no improvement within a few days or if new symptoms appear.

Do not drink alcoholic beverages during therapy with furazolidone and within 4 days after its cancellation.

During therapy with furazolidone, foods and drinks containing tyramine (cheese, beer, wine, beans, smoked meats) should not be consumed in large quantities.

During treatment with furazolidone, you should not take medicines for the treatment of coughs and colds without a doctor's prescription.

Be careful with dizziness.

Nitrofurantoin and furazidin can stain urine rusty yellow or brownish.

Table. Preparations of the nitrofuran group.
Main characteristics and application features

* With normal kidney function