In pharmacology, nitrofuran derivatives are widely used. They are most relevant in identifying purulent processes and inflammation.
The most famous medicines
The following nitrofuran derivatives are most widely used in modern medical practice:
- Furagin.
- Furazolidone.
- Furacilin.
All of these medicines can be used as local antiseptics, oral forms have been developed. Preparations derived from nitrofuran are approved for use, including by patients suffering from low tolerance to antimicrobial agents, sulfonamides.
Important Features
5-nitrofuran derivatives show a pronounced bacteriostatic effect. You can combine such products with antibiotics of the following categories:
- tetracycline series;
- erythromycin;
- drugs on oleandomycin.
Nitrofuran derivatives are not intended for the treatment of persons undergoing therapy with:
- levomycetin;
- drugs containing ristomycin;
- drugs with sulfonamides.
This is dueincreased negative impact on the hematopoietic system of the body.
How does it work?
Nitrofuran derivatives are often used to treat cystitis. This is due to the specifics of the metabolism of the antimicrobial compound: the function falls on the kidneys, in which the drug accumulates. This makes it effective against a wide range of diseases specific to the urinary system. This group of antibiotics helps well with various types of pyelonephritis.
Do not simultaneously use nitrofuran derivatives and antiseptics created with the participation of nalidixic acid, as these two drugs inhibit the action of each other. The indicated uroantiseptic is on sale by the names:
- Nevigramon.
- "Negro".
Therapy program
Antiseptics (nitrofuran derivatives) are usually used three times daily in the amount of 0.1 g. The duration of such a program varies: at least 10 days, but not more than two weeks. It is known that in the treatment of Proteus, invasion of Pseudomonas aeruginosa, the effectiveness of the remedy is relatively low, but a pronounced effect is observed when the harmful coccal flora is eliminated.
If the infection is associated with the ingestion of gram-negative microscopic life forms, it is recommended to use nalidixic acid. The course of treatment lasts from 10 to 12 days, the remedy is used daily with a two-gram dose. This method of treatment is allowed if required.antibacterial treatment of bile ducts.
Is there an alternative?
You can replace 5-nitrofuran derivatives with other synthetic medicines that can fight harmful microflora. Most commonly used:
- made with 8-hydroxyquinoline;
- based on quinoxaline;
- Products containing bis-quarter ammonium compounds.
On sale, these groups are represented by names:
- "5-NOC".
- Mexaform.
- Dioxidine.
- Dekamin.
- "Enteroseptol".
Regarding the described group of drugs, these medicines have a different chemical structure and a fundamentally different composition. Nevertheless, the effectiveness against initiators of infection is similar. In many ways, therapy is justified by the lack of cross-resistance. You can resort to these drugs if the patient has intolerance to nitrofuran derivatives.
Treatment of fungal invasion
To achieve maximum efficiency, nitrofuran derivatives are combined with agents such as:
- Nystatin.
- Levorin.
Dosage is the same as selected for antimicrobials. You can additionally use the antibacterial, antimycotic drug "Dekamin".
When generalized candidiasis is detected, nitrofuran derivatives are enhanced with levrine sodium s alt, used twice or thrice daily. An alternative option is the use of Amphoglucamine orally, Amphotericin B parenterally.
How to choose?
The doctor chooses a specific set of medications, focusing on the characteristics of a particular infection and the tendency to intolerance to certain groups of drugs used in medicine. Not all pathogens show a sufficient level of sensitivity to nitrofuran derivatives so that the choice in favor of this category is always justified. It is important to take into account the toxicity of a group of drugs and the ability to distribute in body tissues, which varies significantly depending on the name.
Nitrofuran derivatives are generally highly compatible with other medicines, but when patients undergo treatment, it is imperative to notify the doctor about all the drugs taken for possible adjustment of the program. All allergic reactions and toxic effects characteristic of nitrofuran derivatives are officially recorded. A special handbook has been released for doctors, detailing how to mitigate the negative results of use.
Issue Features
Nitrofuran derivatives include Furadonin, produced in the form of tablets. There are two dosage options: 0.05 g and twice as much. Recommended for use in a course lasting 5-8 days. Apply three or four times daily.
"Furazolidone" on sale is represented by a form for oral administration, dosage - 0.05 g. Recommended for use in a course of durationfrom five days to twice as long. Every day, the remedy is taken 4 times.
Furagin also belongs to nitrofuran derivatives. The form is tablets, the dosage is similar to that described above - 0.05 g. The duration of the course, the frequency of administration per day is also the same.
Finally, Solafur. In pharmacies, you can buy ampoules with a concentration of the active substance in a solution of 0.1%. The volume of one ampoule varies from 25 to 100 ml. The drug is intended for use through a dropper, the duration of the course is up to seven infusions (but not less than five), a single volume is 300-500 ml. It is recommended to put droppers every other day or every day.
All of the listed drugs belong to the category of a wide spectrum of effectiveness, are excreted in the urine, while disinfecting the ways in which the drug leaves the body. It is known that taking this kind of medication can provoke dyspepsia, allergies. One of the important advantages is the very slow acquisition of resistance by the microflora to all nitrofuran derivatives. In addition to antiseptic, such drugs have chemotherapeutic properties.
Technical aspects
Briefly, the mechanism of action of nitrofuran derivatives can be described as follows: the active substance inhibits the enzymes responsible for the cycling of tricarboxylic acids, while NADH is blocked. In the cell of the microbe, both aerobic oxidative processes with the participation of carbohydrate compounds and anaerobic ones are equally blocked. At a low concentration of the drug in the body, a bacteriostatic effect is observed. Increasing the dose givesbactericidal effect.
Drugs in dentistry practice
Indications for the use of nitrofuran derivatives in dental practice:
- stomatitis (ulcerative, aphthous);
- presence of carious cavities in need of treatment;
- need for decontamination of root canals.
The group of antimicrobial agents is effectively used in the treatment of not only caries, but also the complications provoked by it. This category of drugs is used if microscopic life forms are expected to be resistant to sulfonamides and other antibiotic compounds.
Dentists use nitrofuran derivatives to disinfect the oral mucosa, pockets caused by periodontal disease, cavities provoked by caries. Such treatment is necessary when wounds, infectious lesions are detected. The product is used externally in the form of a solution with an active ingredient concentration of 0.02%.
Some Features
When used externally, nitrofuran derivatives can provoke negative reactions, but in practice this is observed in a vanishingly small percentage of cases. There is a possibility of an allergy. If a patient is hypersensitive to a specific drug from the group of nitrofuran derivatives, this class of drugs cannot be used.
On sale means are presented not only with solutions, tablets, but also with an ointment with an active substance concentration of 0.2%. All preparations are intended for storage in a place protected from sunlight andthe influence of high temperatures. An aqueous solution of nitrofuran derivatives retains its antiseptic qualities for a very long time period.
Quality control
Currently, the problem of drug counterfeiting is quite acute, including popular antimicrobial formulations. To identify the authenticity, it is necessary to make a series of reactions, tracing the results. Classical results are known for this group when interacting with different reagents. For individual drugs, there are also specific methods for quality detection.
To prove the authenticity of 5-nitrofuran derivatives, the result of the reaction with the participation of an alkali solution is determined. This method belongs to the general group and is considered basic. As a rule, the mixture turns red, somewhat less often - red with an orange tint. The nature and intensity of the color are determined by the substituents present in the furan core. It is known that a number of drugs give a change in shade only at a very high alkaline index, others may show a reaction with an increase in temperature, and others - with a decrease.
An alternative group-wide approach - a chemical reaction involving an alkaline solution, which should lead to the release of ammonia. To do this, increase the temperature and use zinc dust, processing samples of preparations with it.
Private Methods
The most widely used method is to create a solution of water with heavy metal s alts. Complex compounds have a specific color that changes during the course of the reaction. Furacilin, when combined with a ten percent copper sulfate solution, will give a dark red precipitate, furadonin will show itself as a brown precipitate, and furazolidone - green.
Alkaline alcohol solutions created using organic solvents can be used to identify the authenticity (a fairly wide range of compounds are allowed). The most common solvents are:
- dimethylformamide;
- acetone.
All nitrofuran derivatives in such substances dissolve quickly and well, and the shade changes for each drug individually. The saturation of the color and the speed of the reaction depend on the concentration of the alkaline compound, the drug being tested.
Medicines: how did they appear?
Currently, the classification of nitrofuran derivatives is based on the effectiveness of these drugs, they distinguish drugs that are well and poorly absorbed from the gastrointestinal tract, as well as combined ones, in which nitrofuran-based components are included as one of the elements of a complex system. But it was not always so. The first developments of a synthetic nature, as is known from official documentation, appeared back in the nineteenth century, when organic chemistry was still in its infancy, but only in the second half of the last century was it possible to develop the idea to such an extent that it became possible to create effective drugs. In many ways, this was facilitated by Butlerov's theories, on the basis of which it was possible to formulate heterocycles with five elements. In this momentall the prerequisites for working with furan compounds appeared.
Officially, the first successful synthesis of furan compounds was recorded in 1818, when work was carried out on mucic acid. A by-product of the reaction in liquid form was obtained, fixed, but not investigated, so the discovery of furan did not take place at that moment - humanity was waiting for more than half a century. In 1832 Dobereiner quite accidentally discovered furfural while trying to make formic acid using sugar and starch. Manganese dioxide and sulfuric acid took part in the reaction. Furfural was rediscovered in 1840. This time, the reaction was carried out over oatmeal, which was treated with the same sulfuric acid. The second attempt to isolate that substance produced enough volumes to begin scientific research, and it was then that Stenhouse formulated an empirical formula, and was also able to discover key properties of a new substance for chemists.
Terminology and history
In 1845, furfural was officially obtained from bran, and the name used to this day is assigned to the new compound. It is formed from the Latin words "bran", "oil" and is intended to reflect the manufacturing method, special external properties. Furfural is the word from which the terms "furan", "furfuran" and other derivatives came from.
Chemists continued experiments to discover what could be used to extract a new compound. It was possible to produce aldehyde derivatives with the participation of ammonia in laboratory conditions. They have been named"furfurin", "furfuramide". In 1870, scientists repeated the experiment of 1818 again, which made it possible to discover furan. Seven years later, Bayer developed his cyclic formulas for furan.
Physics and chemistry: properties of active ingredients
Furan is a powder formed by colorless crystals. Melts when heated to 85 degrees Celsius, boils at 32 degrees. This is a pronounced acidophob, when interacting with sulfuric acid in an increased concentration, a polymerization reaction is observed. If the acid is used in dilute form, the furan ring is cleaved, leading to the formation of 1,4-dicarbonyl compounds. The substance has a tendency to electrophilic substitution. Experiments have shown that furan enters into such reactions even easier and easier than benzene.
The production of furan at present is the synthesis based on furfural. This compound can be obtained from fairly affordable products - waste products of agricultural activity. The classic source is sunflower husks or corn cobs.
What does it look like?
Normal, nitrofuran derivatives are powders created by crystal elements. They have no taste or are slightly bitter. Shades are yellowish, determined by the specificity of the side chain. Some compounds are light yellow or even orange, while others are brown with a touch of yellow. They mostly dissolve poorly in water, but this ability can be increased by heating the mixture.
It is known that nitrofuran derivatives are highly soluble in alcohol. You can use a seriesother organic substances, including dimethylformamide, propylene glycol. Medicines are characterized by increased sensitivity to sunlight, so even water, alcohol (and other) solutions of drugs should be hidden from daylight. An extremely negative effect is observed from ultraviolet radiation - the molecule is almost instantly destroyed. This imposes restrictions on storage options: strictly glass dark containers are used.
"Furagin": application features
This drug can be safely ranked among the most popular derivatives of nitrofuran in our time. This is largely due to the possibility of combining with other antimicrobial drugs. The tool shows a pronounced effect on invasion:
- staphylococci;
- Klebsiell;
- shigella.
The active substance causes irreparable damage to the bacterial protein, due to which DNA molecules cannot be produced, respiratory processes are disturbed. Under the influence of such a reaction, the microbe that provoked the infection cannot produce the same amount of toxins as a he althy cell, which quickly leads to an improvement in well-being. Doctors pay attention: it is unacceptable to stop treatment before the course recommended by the doctor is completed, since good he alth is not an indicator of the elimination of pathogenic microflora.
