Pharmacodynamics and pharmacokinetics
Nifuratel is broad-spectrum antibacterial agent The drug is active against gram-positive and gram-negative microorganisms : staphylococci , Citrobacter spp., Enterococcus faecium, salmonella , Escherichia coli, Klebsiella, Enterococcus faecalis, Bacillus subtilis, Shigella flexneri, Enterobacter spp., Shigella sonnei, Serratia spp., Morganella spp., Pragia fontium, Rachnella aquatilis; Giardia and protozoa ; Rettgerella spp., Budvicia aquatica, Acinetobacter spp.; fungi of the genus Candida and Trichomonas vaginalis.
The medicine is less active against Pseudomonas aeruginos, Proteus mirabilis and Proteus vulgaris.
The substance is quite effective against trichomoniasis and has a detrimental effect on the fungal and antibacterial flora accompanying the disease. Symptoms of vaginitis go away quickly. The drug is also effective in the treatment of gastrointestinal lesions caused by the bacterium Helicobacter pylori, resistant to metronidazole .
After the tablet enters the gastrointestinal tract, the active substance is quickly and almost completely absorbed through the walls of the stomach. The drug crosses the blood-brain barrier and is excreted in breast milk. Metabolism occurs in the liver and muscle tissue. The medicine is eliminated through the kidneys. About 30-50% of the substance is excreted unchanged.
Nifuratel-SZ
Dosage form
film-coated tablets
Compound
1 tablet contains:
active substance
: nifuratel – 200 mg;
Excipients
: corn starch – 90.7 mg, gelatin – 2.3 mg, polyethylene glycol 6000 (macrogol) – 15.0 mg, talc – 9.0 mg; magnesium stearate – 3.0 mg;
shell composition:
hypromellose – 5.37 mg, polysorbate-80 (Tween-80) – 1.50 mg, talc – 1.50 mg, titanium dioxide E 171 – 1.13 mg, aluminum varnish based on quinoline yellow dye – 0.50 mg .
Description
Yellow film-coated tablets, round, biconvex. In a cross section, the core of the tablet is yellow.
ATX code
G01AX05
Pharmacological properties
Pharmacodynamics
Nifuratel is an antimicrobial agent from the nitrofuran group; has antiprotozoal, antifungal and antibacterial effects.
Nifuratel has high efficiency and low toxicity, which determines a wide range of its clinical use.
Highly effective against Papiliobacter and Helicobacter pylori, gram-positive and gram-negative microorganisms.
The spectrum of action includes: Enterococcus faecalis, Enterococcus faecium, Staphylococcus aureus, Bacillus subtilis, Escherichia coli, Shigella flexneri 2a, Shigella flexneri 6, Shigella sonnei, Salmonella typhi, Salmonella typhimurium, Salmonella enteridis, Klebsiella spp., Enterobacter sph., Serratia spp. , Citrobacter spp., Morganella spp., Rettgerella spp., Pragia fontium, Budvicia aquatica, Rachnella aquatilis and Acinetobacter spp., other atypical enterobacteria, as well as protozoa (Trichomonas, amoebas, Giardia); less active against Proteus mirabilis, Proteus vulgaris, Pseudomonas aeruginosa.
It is the drug of choice for the treatment of salmonellosis, shigellosis and other acute intestinal bacterial infections.
Active against Trichomonas vaginalis, highly active against fungi of the genus Candida.
Particularly effective against Helicobacter pylori strains resistant to metronidazole.
Pharmacokinetics
When taken orally, it is quickly absorbed from the gastrointestinal tract. Penetrates the blood-brain and hematoplacental barrier and is excreted in breast milk. Metabolized in the liver and muscle tissue. It is completely excreted from the body by the kidneys (30-50% unchanged), providing a strong antibacterial effect in the urinary tract.
Indications for use
- Vulvovaginal infections caused by pathogens sensitive to the drug (pathogenic microorganisms, Candida fungi, Trichomonas, bacteria, chlamydia).
- Pyelonephritis, urethritis, cystitis, pyelitis and other diseases of the urinary system.
- Intestinal amebiasis and giardiasis. Chronic inflammatory diseases of the upper gastrointestinal tract associated with Helicobacter pylori infection.
Contraindications
Hypersensitivity to the active substance or any component of the drug.
Children under 3 years of age and weighing less than 20 kg.
Use during pregnancy and breastfeeding
Pregnancy
When administered orally, Nufuratel does not have a teratogenic effect in preclinical studies in mice, rats and rabbits.
There are no clinical studies in pregnant women. It is not recommended to use the drug during pregnancy. The drug should be prescribed only under the supervision of a physician after careful evaluation of the benefits versus the possible risks. Nifuratel penetrates the hematoplacental barrier, so the use of the drug is possible only under strict indications, if the expected effect of therapy for the mother exceeds the potential risk to the fetus. If you suspect pregnancy, it is recommended to consult a doctor.
Breast-feeding
Nifuratel is excreted into breast milk, therefore, if it is necessary to prescribe the drug during breastfeeding, the issue of stopping breastfeeding should be decided.
Directions for use and doses
The drug is taken orally following the recommendations.
Vaginal infections:
Adults: 1 tablet 3 times a day after meals for 7 days (both sexual partners should take the drug).
Children over 3 years of age and weighing more than 20 kg: the recommended dose is 10 mg/kg body weight daily for 10 days. The recommended dose should be taken in two divided doses.
Urinary tract infections:
Adults: depending on the severity of the disease, 1-2 tablets 3 times a day for 7-14 days.
Children over 3 years of age and weighing more than 20 kg: recommended dose of 30-60 mg/kg body weight. The recommended dose should be taken in two divided doses.
On the recommendation of a doctor, the course of treatment for urinary tract infections can be extended or repeated.
Intestinal amoebiasis:
Adults: 2 tablets 2-3 times a day for 10 days.
Children over 3 years of age and weighing more than 20 kg: the recommended dose is 10 mg/kg body weight 3 times a day.
Giardiasis:
Adults: 2 tablets 2-3 times a day for 7 days.
Children over 3 years of age and weighing more than 20 kg: recommended dose of 15 mg/kg body weight 2 times a day for 7 days.
Inflammatory diseases of the upper gastrointestinal tract associated with Helicobacter pylori:
Adults: 2 tablets 2-3 times a day for 7 days.
Children over 3 years of age and weighing more than 20 kg: recommended dose of 15 mg/kg body weight 2 times a day for 7 days.
Side effect
Dyspeptic disorders
: nausea, vomiting, bitterness in the mouth, diarrhea, heartburn.
Allergic reactions:
skin rash, itching.
Overdose
There have been no cases of overdose.
Interaction with other drugs
Strengthens the antifungal effect of nystatin.
special instructions
When treating vaginal infections only with oral therapy with Nifuratel-SZ, it is recommended to increase the daily dosage of the drug to 4-6 tablets.
During the treatment period you should abstain from sexual intercourse.
Impact on the ability to drive vehicles and operate machinery
The drug does not affect the ability to drive vehicles or engage in potentially hazardous activities that require increased concentration and speed of psychomotor reactions.
Release form
Film-coated tablets, 200 mg.
10 tablets per blister pack.
30 tablets per BP type polymer jar made of low-density polyethylene with a high-density polyethylene lid or in a polymer bottle made of low-density polyethylene with a high-density polyethylene lid.
Each jar, bottle, 2, 3 cell contour packages along with instructions for use are placed in a cardboard box.
Best before date
3 years. Do not use after the expiration date stated on the package.
Storage conditions
In a place protected from light, at a temperature not exceeding 25 ° C.
Keep out of the reach of children.
Vacation conditions
Dispensed by prescription.
Prescription drug
Prescription drug
Indications for use
With the help of an antibacterial agent, diseases caused by microorganisms sensitive to the action of the substance are treated:
- vulvovaginitis , trichomoniasis ;
- genitourinary infections, cystitis , pyelonephritis , urethritis , pyelitis ;
- giardiasis , gastroduodenitis , enterocolitis , amoebiasis , cholecystopancreatitis ;
- chronic diseases of the upper gastrointestinal tract caused by the Helicobacter .
The use of nifuratel in the treatment of mixed intestinal infections
In a retrospective analysis, nifuratel demonstrated 95% effectiveness in the treatment of intestinal giardiasis combined with intestinal dysbiosis, as well as high efficiency in the fight against opportunistic species Escherichia coli, Citrobacter spp. and Klebsiella spp. Most patients noted an improvement in their well-being after treatment, which was manifested primarily by normalization of the frequency and shape of stools, a decrease in flatulence, the disappearance of abdominal discomfort, improved appetite and a decrease in fatigue. Nifuratel can be considered the drug of choice when giardiasis is combined with bacterial intestinal dysbiosis and helicobacteriosis of the digestive tract.
Table. Laboratory confirmed effectiveness of nifuratel in the treatment of intestinal giardiasis and microbial overgrowth in patients (n = 42) with mixed intestinal infections
The problem of mixed infectious intestinal lesions in modern gastroenterology is very relevant. Clinicians and laboratory doctors have to solve difficult problems in the diagnosis and treatment of diseases caused simultaneously by Helicobacter pylori
(gastritis, peptic ulcer, gastric neoplasms, etc.),
Lamblia
(asthenic, allergic and dyspeptic syndromes) and other opportunistic microorganisms involved in dysbiotic conditions of the intestine - opportunistic microorganisms of the genera
Candida, Escherichia, Klebsiella, Proteus, Citrobacter, Staphylococcus aureus
, etc. (irritable bowel syndrome, immunodeficiency and allergic syndromes).
Since 1981, the World Health Organization has classified pathogens of the genus Lamblia
classified as definitely pathogenic intestinal protozoa [1]. Intestinal dysbiosis syndrome is diagnosed in a significant proportion of patients who seek help from medical institutions.
In the Russian industry standard “Protocol for the management of patients. “Intestinal dysbiosis” (OST 91500.11.0004-2003) intestinal dysbiosis is understood as a clinical and laboratory syndrome associated with changes in the qualitative and/or quantitative composition of the intestinal microflora with the subsequent development of metabolic and immunological disorders with the possible occurrence of gastrointestinal disorders. Correction of intestinal dysbiosis involves the use of enteroseptic agents to suppress opportunistic microbiota in the intestinal biofilm. This in turn creates conditions for colonization of the intestine by normal microflora, mainly lactobacilli and bifidobacteria.
At the stage of developing treatment tactics, there is an acute problem of choosing an antimicrobial drug, the action of which would be directed against all participants in the infectious process [2–4]. In this regard, it is important to study the drug nifuratel (Macmiror), a drug characterized by a wide spectrum of activity against pathogens of infectious lesions of the gastrointestinal tract (including bacterial and protozoan). Macmiror is a starting therapy drug in the treatment of giardiasis according to the protocol approved at the 20th Congress of Pediatric Gastroenterologists of Russia and the CIS Countries.
Materials and research methods
A retrospective study assessed the effectiveness of nifuratel (Macmiror) in the treatment of intestinal giardiasis associated with intestinal dysbiosis in 42 patients (26 women and 18 men) observed in the consultative and diagnostic department of the mycological clinic of the St. Petersburg Medical Academy of Postgraduate Education (SPbMAPO) in 2009–2010, outpatient records of patients aged 18 to 65 years (mean age 32 ± 4 years) were analyzed.
The study did not include data from outpatient records of patients suffering from diabetes mellitus types 1 and 2 and cancer, as well as those receiving other antimicrobial and/or glucocorticosteroid drugs at the same time.
All patients with mixed intestinal infections noted symptoms of intestinal irritation, as well as asthenic and allergic syndromes (with varying frequencies). Symptoms of intestinal irritation (usually unformed, pasty stools alternating with constipation, bloating, abdominal pain syndrome) were noted by 27 (64%) patients, asthenic syndrome (weakness, fatigue, loss of appetite) - 19 (45%) patients, allergic diseases in the phase exacerbations (urticaria or atopic dermatitis) – 11 (26%) patients.
The diagnosis of giardiasis and control of the cure of this infection were based on the results of a laboratory parasitological study of feces using enrichment methods - formaldehyde-ether sedimentation and flotation (carried out in the clinical laboratory of the Research Institute of Medical Mycology of St. Petersburg MAPO). The diagnosis was made by detecting vegetative forms and/or protozoan cysts, indicating the number of parasites in the field of view. The cure of giardiasis was confirmed by double stool examination with an interval of 5–7 days. Serological methods for diagnosing and monitoring the cure of giardiasis were not used.
Intestinal dysbiosis was detected using standard bacteriological methods for examining feces developed by R.V. Epstein-Litvak and F.V. Vilshanskaya, with determination of the number of CFU in 1 g of feces in terms of the decimal logarithm. The growth of opportunistic intestinal microbiota was considered excessive at values ≥ 10,000 CFU/g feces. Simultaneously with the control examination of stool for protozoa, a control analysis of stool for dysbacteriosis was carried out.
With the discovery of Giardia, excessive growth in the feces of opportunistic Escherichia coli (hemolytic, lactose-negative) was revealed - in 17 patients, fungi of the genus Candida
– in 13,
Citrobacter
– in 11,
Klebsiella
– in 10,
Proteus
– in 6, S.
aureus
– in 5, others – in 5. Control of cure was carried out in the same laboratory (bacteriological laboratory of the mycological clinic).
Macmiror was prescribed 400 mg (2 tablets) 3 times a day in courses of 7 days (a total of 40 tablets per course, or a total of 8 g of nifuratel). At the same time, all patients were recommended to limit the intake of fatty and fried foods and completely eliminate the intake of alcoholic beverages. Most patients received probiotics or prebiotics along with nifuratel. According to the principles of the Declaration of Helsinki, all patients received full information about the prescribed treatment and the properties of the drugs used. The frequency and nature of side effects of therapy with nifuratel (MacMirror) were assessed clinically (survey, objective examination during the second visit). Statistical processing of the obtained data was carried out using the SPSS software package, version 12. Parametric and nonparametric comparison methods were used based on the nature of the distribution of numerical data. Frequency characteristics of qualitative variables were compared using contingency tables. The correlation between characteristics was studied. Differences at p were considered significant.
results
The results of a retrospective analysis of outpatient records of patients treated with nifuratel concern changes in the clinical picture and control stool tests. During the follow-up survey, 59 (92.2%) of 64 patients noted an improvement in their state of health after the course of treatment. This was manifested primarily by the normalization of the frequency and shape of stools, a decrease in flatulence and the disappearance of abdominal discomfort. In addition, most patients noted improved appetite and decreased fatigue. Of 16 patients with symptoms of atopic dermatitis or urticaria, 12 (75%) reported a significant decrease in the severity of skin itching and rashes. At the same time, only 6 (9.4%) of 64 patients noted undesirable side effects - a feeling of moderate intensity discomfort in the epigastric region that occurs on an empty stomach, and a feeling of heaviness after eating. These symptoms were short-lived, did not require cessation of therapy and disappeared spontaneously after its completion. There were no adverse events in the form of skin itching, rashes and bronchospasm in the patients.
The results of laboratory monitoring of feces (the presence of Giardia on microscopy and the growth of opportunistic bacterial flora) are shown in the table. As we can see, nifuratel showed 95% effectiveness in the treatment of intestinal giardiasis combined with intestinal dysbiosis. The high effectiveness of nifuratel was most likely due to the pharmacodynamics of the drug - good accumulation of the active substance both in the intestinal biofilm and in the epithelial layer of the intestine. We were also able to demonstrate the high (up to 100%) effectiveness of nifuratel against opportunistic species E. coli, Citrobacter spp
.
and Klebsiella spp
. According to the results of the analysis, nifuratel can be considered the drug of choice for the combination of giardiasis with bacterial intestinal dysbiosis and helicobacteriosis of the digestive tract.
At the same time, the effectiveness of nifuratel in the treatment of candida, Proteus and staphylococcal dysbiosis turned out to be significantly lower: the use of nifuratel 800 mg/day for 7 days led to the sanitation of the intestines from yeast-like fungi in 6 out of 21 patients, Proteus - only in 3 out of 9, and Staphylococcus aureus – in 5 out of 8 patients. This may be due to the specificity of the causative agents of such dysbiosis. Widespread resistance of Candida spp., Proteus spp
.
and S. aureus
to many antimicrobial drugs. Apparently, the treatment of these variants of intestinal dysbiosis requires either prolonged courses of taking nifuratel or the use of other enteroseptics.
conclusions
Based on the study, the following conclusions were made.
1. The effectiveness of nifuratel (Makmiror) in the treatment of giardiasis in adults, according to the results of double control fecal samples, reaches 95%.
2. The effectiveness of nifuratel (Makmiror) in correcting dysbiosis syndrome in adults reaches 100%.
3. Macmiror can be recommended as a drug of choice with a good safety profile for intestinal giardiasis associated with intestinal dysbiosis.
Nifuratel, instructions for use (Method and dosage)
The drug is prescribed orally. Depending on the disease, the dosage and treatment regimen are different.
Instructions for Nifuratel
The standard daily dosage for an adult is from 600 mg to 1.2 g. The amount of medicine that a child needs to take during the day is calculated according to the principle of 10-30 mg per kg of weight.
The duration of treatment and frequency of administration depends on the indications and is determined by the attending physician.
Other dosage forms (suppositories and ointment) are used in accordance with the manufacturer's recommendations.
Medicines containing (Nifuratel analogues)
Level 4 ATC code matches:
Acylact
Iodoxide
Furazolidone
Kolposeptin
Lactonorm
Hexicon
Ecofemin
Lactozhinal
Depanthol
McMirror
Dafnedjin
Analogs of Nifuratel: Macmiror , Nifuratel tablets, Macmiror Complex suppositories and cream (in combination with nystatin ).
