Itraconazole or fluconazole which is better for nail fungus. Azoles - antifungal agents

What is the best remedy for nail fungus today? Modern medicine offers us a wide choice of drugs and innovative technologies.

Nail fungus is a fairly common disease. Mycosis - this is the name of this disease, you can catch it either directly from an infected person, or if the nail plate or skin comes into contact with the patient's clothes, shoes, personal belongings or common items. The most common places of infection are baths, saunas, swimming pools, gyms, and beaches.

In order to carry out effective treatment of nail fungus, it is necessary to determine which specific species caused the lesion. Most often, these are dermatophytes Trichophyton rubrum or mentagrophytes. They account for 60 to 90 percent of all nail diseases.

However, often the infection is mixed, that is, the nail plate is affected by several types of dermatophytes, as well as yeast and mold types of fungi. It is impossible to answer what exactly a person is infected with without analysis. However, there are tools on the market that perfectly cope with a complex problem.

Nail fungus is treated in different ways

A severe lesion of the nail plate, when it is completely deformed, is called the hypercarotic form. In this case, self-medication is unacceptable. In other cases, you can get by with ointments, creams and sprays based on some kind of multi-fungal active substance.

Most often, therapy includes:

• Oral administration of antifungal drugs plus application of a similar drug to the site of the lesion.
• Removal of the affected part of the nail plate using keratolic patches Ureaplast, Microspore, Onychoplast, followed by treatment with antifungal drugs. Removing part or all of the plate speeds up the process of treatment and restoration of the nail.
• Application of antifungal varnishes. Helps in complex treatment, as a prophylactic or at the very initial stage of the disease. Trade names of varnishes: Amorolfine (Amorolfin), Loceryl (active ingredient amorolfine), Cyclopirox, Batrafen (on cyclopirox), Omorolfine.
• Application of creams, ointments, solutions and sprays based on terbinafine.
• Appointment of oral systemic antifungal drugs - Griseofulvin, Grimelan, Ketoconazole, Itraconazole, Irunin, Terbinafine, Fluconazole and others. Simultaneously with the tablets, external agents are prescribed, depending on the nature of the disease.
• With a severe course of the disease, drugs are prescribed, which include not only antifungal substances, but also antibacterial or corticosteroid components. For example, travocort includes isoconazole from fungi and diflucortolone valerate (a corticosteroid), which relieves itching and allergies. The drug Pimafucort is also good, which contains a broad-spectrum antibiotic, an antifungal drug and a corticosteroid.
• As maintenance therapy, lotions with Dimexide are prescribed - it relieves inflammation, drops and ointments with zinc, copper - accelerate the restoration of the skin and nails.

Terbinafine tablets

One of the most affordable means for oral, that is, external, administration for nail fungus is Terbinafine. The name of the drug and the active substance are the same. Also suitable for the treatment of skin, hair, mucous membranes. It is available in the form of ointments, creams, tablets, sprays, solutions. It is rarely prescribed systemically, in most cases local application is indicated. Belongs to the group of allylamines.

Terbinafine has a strong fungicidal effect on various types of dermatophytes and other fungi and yeasts. It destroys the intercellular membranes, and over time, the fungi die. This drug is prescribed for a number of diseases: nail fungus, microsporia, mycoses caused by the rubrum fungus, trichophytosis, candidal lesions of the mucous membranes and skin.

For local treatment of the fungus Terbinafine cream, ointment or spray is prescribed 1 time per day. The approximate duration of the course is 1 week. It is impossible to interrupt the course, despite the fact that the improvement will occur after the second or third use of the drug. The main contraindications to the use of drugs with this active substance are liver and kidney failure, as well as tumors of various nature, psoriasis, endocrine diseases.

It is most convenient to use sprays from various manufacturers. Alcoholic solutions of terbinafine are quickly absorbed into the nail plate, practically do not enter the bloodstream (less than 5%), and dry out instantly. So you can wear socks and shoes almost immediately after application.

Preparations for the treatment of mycoses with this active ingredient:

• Lamisil.
• Binafin.
• Thermicon.
• Terbasil.
• Fungoterbin.
• Exifin.
• Atifin and others.

All of them have the same active ingredient, the same concentration for specific forms. Only auxiliary substances differ, which are responsible for softening the plate and transporting active substances to the nail. It is worth choosing according to individual portability and price.

Itraconazole tablets

This is another drug for the treatment of fungus with a wide spectrum of action. Belongs to the group of triazoles. Itraconazole has also been used successfully to treat lesions of the nail plate, as has Terbinafine. However, it is prescribed with caution to patients with a diseased liver, kidneys.

Names of drugs based on Itraconazole:

• Irunin.
• Orungal.
• Teknazol.
• Orungamine.
• Orunit.
• Rumikoz and others.

The most affordable capsules are Irunin. The duration and course of treatment (with intervals in admission) are prescribed by the doctor strictly individually.

fluconazole tablets

It also refers to the drugs of the triazole series, that is, it acts similarly to Itraconazole. Its advantage over related drugs is that it has practically no effect on human pathogenic microflora, that is, beneficial fungi in our body.

This is a relatively expensive drug that is prescribed in rare cases when the patient has problems with the immune system. So, he can be discharged if there are tumors, immune depression, if in the near future the patient will have to undergo surgery, radiation therapy. In banal cases of fungal infection of the nail, Fluconazole is not recommended. It is worth noting that this drug has a number of unpleasant side reactions that are not characteristic of other antifungal agents.

Analogues:

• Diflucan.
• Mycosist.
• Flucostat.

All these capsule preparations are focused mainly on the systemic treatment of fungal diseases associated with the human genitourinary system.

Ketoconazole tablets

A fairly active antifungal drug that is most effective in the treatment of systemic lesions. It has practically no contraindications - only intolerance, pregnancy, lactation, serious liver diseases, but it can give a number of side effects.

Preparations containing Ketoconazole:

• Mycozoral.
• Fungikok.
• Oronazole.
• Dermazol.

Also, this active ingredient is often used in the production of medical and cosmetic shampoos, ointments. For example, it is in Nizoral shampoo and Perhotal.

Video: Antifungal drugs

Let's summarize the main drugs for nail fungus

At the slightest suspicion of nail fungus, immediately go to the doctor

Modern pharmacology can offer a number of antifungal drugs that act on many types of microfungi. Some of the drugs can be classified as specialized for the treatment of certain groups of diseases. For example, drugs based on Ketoconazole or Fluconazole act.

Most often, mycologists prescribe drugs based on Terbinafine or Itraconazole for the treatment of nail fungus. Some of the drugs based on them are widely advertised and are quite expensive. At the same time, the effect of such popular drugs is well studied, which allows doctors to recommend these particular drugs.

If the problem has not gone too far, you can try to self-medicate. To do this, soften the damaged part of the plate using special patches and remove it. Then choose an ointment, cream or spray for topical use based on Terbinafine or Itraconazole and use according to the instructions.

To eliminate discomfort, ointments with corticosteroids are suitable. Zinc and copper ointments will contribute to the restoration of the skin. If therapy does not work, a visit to the doctor is necessary. It is possible not only the loss of the nail, but the systemic damage to the body by fungi.

In recent decades, there has been a significant increase in fungal diseases. This is due to many factors and, in particular, to the widespread use in medical practice of broad-spectrum antibiotics, immunosuppressants and other groups of drugs.

In connection with the trend towards the growth of fungal diseases (both superficial and severe visceral mycoses associated with HIV infection, oncohematological diseases), the development of resistance of pathogens to existing drugs, the identification of fungal species that were previously considered non-pathogenic (currently, potential pathogens of mycoses are considered about 400 species of mushrooms), the need for effective antifungal agents has increased.

Antifungal agents (antimycotics) are drugs that have a fungicidal or fungistatic effect and are used for the prevention and treatment of fungal infections.

For the treatment of fungal diseases, a number of drugs are used, different in origin (natural or synthetic), spectrum and mechanism of action, antifungal effect (fungicidal or fungistatic), indications for use (local or systemic infections), methods of administration (orally, parenterally, externally) .

There are several classifications of drugs belonging to the group of antimycotics: according to the chemical structure, mechanism of action, spectrum of activity, pharmacokinetics, tolerability, features of clinical use, etc.

In accordance with the chemical structure, antifungal agents are classified as follows:

1. Polyene antibiotics: nystatin, levorin, natamycin, amphotericin B, mycoheptin.

2. Imidazole derivatives: miconazole, ketoconazole, isoconazole, clotrimazole, econazole, bifonazole, oxiconazole, butoconazole.

3. Triazole derivatives: fluconazole, itraconazole, voriconazole.

4. Allylamines (N-methylnaphthalene derivatives): terbinafine, naftifine.

5. Echinocandins: caspofungin, micafungin, anidulafungin.

6. Drugs of other groups: griseofulvin, amorolfine, ciclopirox, flucytosine.

The division of antifungal drugs according to the main indications for use is presented in the classification of D.A. Kharkevich (2006):

I. Means used in the treatment of diseases caused by pathogenic fungi:

1. With systemic or deep mycoses (coccidioidomycosis, paracoccidioidomycosis, histoplasmosis, cryptococcosis, blastomycosis):

Antibiotics (amphotericin B, mycoheptin);

Imidazole derivatives (miconazole, ketoconazole);

Triazole derivatives (itraconazole, fluconazole).

2. With epidermomycosis (dermatomycosis):

Antibiotics (griseofulvin);

Derivatives of N-methylnaphthalene (terbinafine);

Nitrophenol derivatives (chlornitrophenol);

Iodine preparations (alcoholic iodine solution, potassium iodide).

II. Means used in the treatment of diseases caused by opportunistic fungi (for example, with candidiasis):

Antibiotics (nystatin, levorin, amphotericin B);

Imidazole derivatives (miconazole, clotrimazole);

Bis-quaternary ammonium salts (dequalinium chloride).

In clinical practice, antifungal agents are divided into 3 main groups:

1. Preparations for the treatment of deep (systemic) mycoses.

2. Preparations for the treatment of epidermophytosis and trichophytosis.

3. Preparations for the treatment of candidiasis.

The choice of drugs in the treatment of mycoses depends on the type of pathogen and its sensitivity to drugs (it is necessary to prescribe drugs with the appropriate spectrum of action), the pharmacokinetics of drugs, the toxicity of the drug, the clinical condition of the patient, etc.

Fungal diseases have been known for a very long time, since antiquity. However, the causative agents of dermatomycosis and candidiasis were identified only in the middle of the 19th century, by the beginning of the 20th century. pathogens of many visceral mycoses have been described. Before the advent of antimycotics in medical practice, antiseptics and potassium iodide were used to treat mycoses.

In 1954, antifungal activity was discovered in a known since the late 40s. 20th century polyene antibiotic nystatin, in connection with which nystatin has become widely used for the treatment of candidiasis. The antibiotic griseofulvin proved to be a highly effective antifungal agent. Griseofulvin was first isolated in 1939 and used in fungal diseases of plants, it was introduced into medical practice in 1958 and was historically the first specific antimycotic for the treatment of dermatomycosis in humans. For the treatment of deep (visceral) mycoses, another polyene antibiotic, amphotericin B, began to be used (it was obtained in purified form in 1956). Major successes in the creation of antifungal agents date back to the 70s. XX century, when imidazole derivatives were synthesized and put into practice - second-generation antimycotics - clotrimazole (1969), miconazole, ketoconazole (1978), etc. Third-generation antimycotics include triazole derivatives (itraconazole - synthesized in 1980 ., fluconazole - synthesized in 1982), the active use of which began in the 90s, and allylamines (terbinafine, naftifine). IV generation antimycotics — new drugs already registered in Russia or under clinical trials — liposomal forms of polyene antibiotics (amphotericin B and nystatin), triazole derivatives (voriconazole — created in 1995, posaconazole — registered in Russia at the end of 2007 ., ravuconazole - not registered in Russia) and echinocandins (caspofungin).

Polyene antibiotics- antimycotics of natural origin, produced Streptomyces nodosum(amphotericin B), Actinomyces levoris Krass(levorin), actinomycete Streptoverticillium mycoheptinicum(mycoheptin), actiomycete Streptomyces noursei(nystatin).

The mechanism of action of polyene antibiotics is well understood. These drugs bind strongly to the ergosterol of the fungal cell membrane, disrupt its integrity, which leads to the loss of cellular macromolecules and ions and cell lysis.

Polyenes have the widest spectrum of antifungal activity in vitro among antimycotics. Amphotericin B, when used systemically, is active against most yeast-like, filamentous and dimorphic fungi. When applied topically, polyenes (nystatin, natamycin, levorin) act mainly on Candida spp. Polyenes are active against some protozoa - Trichomonas (natamycin), Leishmania and amoeba (amphotericin B). The causative agents of zygomycosis are insensitive to amphotericin B. Dermatomycetes (genus Trichophyton, Microsporum And Epidermophyton), Pseudoallescheria boydi and etc.

Nystatin, levorin and natamycin are used both topically and orally for candidiasis, incl. skin candidiasis, gastrointestinal mucosa, genital candidiasis; amphotericin B is used primarily for the treatment of severe systemic mycoses and is so far the only polyene antibiotic for intravenous administration.

All polyenes are practically not absorbed from the gastrointestinal tract when taken orally, and from the surface of intact skin and mucous membranes when applied topically.

Common systemic side effects of polyenes when taken orally are: nausea, vomiting, diarrhea, abdominal pain, and allergic reactions; when used topically - irritation and burning sensation of the skin.

In the 1980s, a number of new drugs based on amphotericin B were developed - lipid-associated forms of amphotericin B (liposomal amphotericin B - Ambysome, lipid complex of amphotericin B - Abelset, colloidal dispersion of amphotericin B - Amphocil), which are currently being introduced into clinical practice. practice. They are distinguished by a significant decrease in toxicity while maintaining the antifungal effect of amphotericin B.

Liposomal amphotericin B is a modern dosage form of amphotericin B encapsulated in liposomes (vesicles formed when phospholipids are dispersed in water) and is better tolerated.

Liposomes, being in the blood, remain intact for a long time; the release of the active substance occurs only upon contact with the cells of the fungus when it enters the tissues affected by the fungal infection, while the liposomes ensure the intactness of the drug in relation to normal tissues.

Unlike conventional amphotericin B, liposomal amphotericin B creates higher concentrations in the blood than conventional amphotericin B, practically does not penetrate into the kidney tissue (less nephrotoxic), has more pronounced cumulative properties, the half-life is on average 4-6 days, with long-term use may increase up to 49 days. Adverse reactions (anemia, fever, chills, hypotension), compared with the standard drug, occur less frequently.

Indications for the use of liposomal amphotericin B are severe forms of systemic mycoses in patients with renal insufficiency, with the ineffectiveness of the standard drug, with its nephrotoxicity, or severe reactions to IV infusion that cannot be stopped by premedication.

Azoles(derivatives of imidazole and triazole) - the most numerous group of synthetic antifungal agents.

This group includes:

Azoles for systemic use - ketoconazole, fluconazole, itraconazole, voriconazole;

Azoles for topical use - bifonazole, isoconazole, clotrimazole, miconazole, oxiconazole, econazole, ketoconazole.

The first of the proposed systemic azoles (ketoconazole) is currently being replaced from clinical practice by triazoles - itraconazole and fluconazole. Ketoconazole has practically lost its importance due to its high toxicity (hepatotoxicity) and is used mainly locally.

All azoles have the same mechanism of action. The antifungal effect of azoles, like polyene antibiotics, is due to a violation of the integrity of the fungal cell membrane, but the mechanism of action is different: azoles disrupt the synthesis of ergosterol, the main structural component of the fungal cell membrane. The effect is associated with inhibition of cytochrome P450-dependent enzymes, incl. 14-alpha-demethylase (sterol-14-demethylase), which catalyzes the conversion of lanosterol to ergosterol, which leads to disruption of the synthesis of ergosterol in the fungal cell membrane.

Azoles have a wide spectrum of antifungal activity, have a predominantly fungistatic effect. Azoles for systemic use are active against most pathogens of superficial and invasive mycoses, including Candida spp.(incl. candida albicans, candida tropicalis), Cryptococcus neoformans, Coccidioides immitis, Histoplasma capsulatum, Blastomyces dermatitidis, Paraccoccidioides brasiliensis. Usually not sensitive or resistant to azoles. Candida glabrata, Candida krucei, Aspergillus spp., Fusarium spp. and zygomycetes (class Zygomycetes). Azoles have no effect on bacteria and protozoa (with the exception of Leishmania major).

Voriconazole and itraconazole have the widest spectrum of activity among oral antimycotics. Both differ from other azoles in having activity against moulds. Aspergillus spp. Voriconazole differs from itraconazole in its high activity against Candida krusei And Candida grabrata, as well as greater effectiveness against Fusarium spp. And Pseudallescheria boydii.

Topically applied azoles are predominantly active against Candida spp., dermatomycetes ( Trichophyton, Microsporum, Epidermophyton) And Malassezia furfur(syn. Pityrosporum orbiculare). They also act on a number of other fungi that cause superficial mycoses, on some gram-positive cocci and corynebacteria. Clotrimazole exhibits moderate activity against anaerobes ( Bacteroides, Gardnerella vaginalis), in high concentrations - in relation to Trichomonas vaginalis.

Secondary resistance of fungi with the use of azoles rarely develops. However, with long-term use (for example, in the treatment of candidal stomatitis and esophagitis in HIV-infected patients in the later stages), resistance to azoles gradually develops. There are several ways to develop sustainability. The main mechanism of resistance in candida albicans due to the accumulation of gene mutations ERG11 encoding sterol-14-demethylase. As a result, the cytochrome gene ceases to bind to azoles, but remains available for the natural substrate, lanosterol. Cross-resistance develops to all azoles. In addition, at candida albicans And Candida grabrata resistance may be due to the removal of drugs from the cell with the help of carriers, incl. ATP dependent. It is also possible to enhance the synthesis of sterol-14-demethylase.

Topical preparations at high concentrations at the site of action may act fungicidal against some fungi.

Pharmacokinetics of azoles. Azoles for systemic use (ketoconazole, fluconazole, itraconazole, voriconazole) are well absorbed when taken orally. The bioavailability of ketoconazole and itraconazole can vary significantly depending on the level of acidity in the stomach and food intake, while the absorption of fluconazole does not depend on either gastric pH or food intake. Triazoles are metabolized more slowly than imidazoles.

Fluconazole and voriconazole are used orally and intravenously, ketoconazole and itraconazole are used only inside. The pharmacokinetics of voriconazole, unlike other systemic azoles, is non-linear - with a 2-fold increase in dose, AUC increases by 4 times.

Fluconazole, ketoconazole, itraconazole and voriconazole are distributed to most tissues, organs and body fluids, creating high concentrations in them. Itraconazole can accumulate in the skin and nail plates, where its concentrations are several times higher than plasma levels. Itraconazole practically does not penetrate into saliva, intraocular and cerebrospinal fluid. Ketoconazole passes poorly through the BBB and is determined in the cerebrospinal fluid only in small quantities. Fluconazole passes well through the BBB (its level in the cerebrospinal fluid can reach 50-90% of the plasma level) and the hemato-ophthalmic barrier.

Systemic azoles differ in the duration of the half-life: T 1/2 ketoconazole - about 8 hours, itraconazole and fluconazole - about 30 hours (20-50 hours). All systemic azoles (except fluconazole) are metabolized in the liver and excreted mainly through the gastrointestinal tract. Fluconazole differs from other antifungal drugs in that it is excreted through the kidneys (mainly unchanged - 80-90%).

Azoles for topical use (clotrimazole, miconazole, etc.) are poorly absorbed when taken orally, and therefore are used for topical treatment. These drugs create high concentrations in the epidermis and underlying skin layers that exceed the MIC for the main pathogenic fungi. The longest half-life from the skin is observed in bifonazole (19-32 hours). Systemic absorption through the skin is minimal. For example, with local application of bifonazole, 0.6-0.8% is absorbed by healthy and 2-4% by inflamed skin. With vaginal application of clotrimazole, absorption is 3-10%.

generally recognized testimony to the appointment of systemic azoles: skin candidiasis, including intertriginous candidiasis (yeast diaper rash of skin folds and inguinal region); onychomycosis, candidal paronychia; keratomycosis (pityriasis versicolor, trichosporosis); dermatophytosis, including superficial trichophytosis of the smooth skin of the face, trunk and scalp, infiltrative-suppurative trichophytosis, epidermophytosis of the groin and feet, microsporia; subcutaneous mycoses (sporotrichosis, chromomycosis); pseudoallescheriosis; vulvovaginal candidiasis, colpitis and balanoposthitis; candidiasis of the mucous membranes of the oral cavity, pharynx, esophagus and intestines; systemic (generalized) candidiasis, incl. candidemia, disseminated, visceral candidiasis (candidal myocarditis, endocarditis, bronchitis, pneumonia, peritonitis, urinary tract candidiasis); deep endemic mycoses, including coccidioidomycosis, paracoccidioidomycosis, histoplasmosis and blastomycosis; cryptococcosis (skin, lungs and other organs), cryptococcal meningitis; prevention of fungal infections in patients with reduced immunity, transplanted organs and malignant neoplasms.

Indications to the appointment of topical azoles: skin candidiasis, candidal paronychia; dermatophytosis (epidermophytosis and trichophytosis of smooth skin, hands and feet, microsporia, favus, onychomycosis); pityriasis (colorful) lichen; erythrasma; seborrheic dermatitis; candidiasis of the oral cavity and pharynx; candidal vulvitis, vulvovaginitis, balanitis; trichomoniasis.

Side effects systemic azoles include:

Gastrointestinal disorders, incl. abdominal pain, loss of appetite, nausea, vomiting, diarrhea or constipation, increased activity of hepatic transaminases, cholestatic jaundice;

From the nervous system and sensory organs, incl. headache, dizziness, drowsiness, paresthesia, tremor, convulsions, blurred vision;

hematological reactions - thrombocytopenia, agranulocytosis;

allergic reactions - skin rash, itching, exfoliative dermatitis, Stevens-Johnson syndrome.

With external use of azoles in 5% of cases, a rash, itching, burning, hyperemia, skin peeling appear, rarely - contact dermatitis.

With intravaginal use of azoles: itching, burning, hyperemia and swelling of the mucous membrane, vaginal discharge, increased urination, pain during intercourse, burning sensation in the penis of the sexual partner.

Azole interactions. Since azoles inhibit the oxidative enzymes of the cytochrome P450 system (ketoconazole > itraconazole > fluconazole), these drugs can change the metabolism of other drugs and the synthesis of endogenous compounds (steroids, hormones, prostaglandins, lipids, etc.).

Allylamines- synthetic drugs. They have a predominantly fungicidal effect. Unlike azoles, they block the earlier stages of ergosterol synthesis. The mechanism of action is due to inhibition of the enzyme squalene epoxidase, which together with squalene cyclase catalyzes the conversion of squalene to lanosterol. This leads to a deficiency of ergosterol and to intracellular accumulation of squalene, which causes the death of the fungus. Allylamines have a wide spectrum of activity, but only their effect on causative agents of dermatomycosis is of clinical importance, and therefore the main indications for the appointment of allylamines are dermatomycosis. Terbinafine is used topically and orally, naftifine - only topically.

Echinocandins. Caspofungin is the first drug from a new group of antifungal agents - echinocandins. Studies of this group of substances began about 20 years ago. Caspofungin, micafungin and anidulafungin are currently registered in Russia. Caspofungin is a semi-synthetic lipopeptide compound synthesized from a fermentation product Glarea lozoyensis. The mechanism of action of echinocandins is associated with the blockade of the synthesis of (1,3)-β-D-glucan, an integral component of the fungal cell wall, which leads to a violation of its formation. Caspofungin is active against candida spp., including strains resistant to azoles (fluconazole, itraconazole), amphotericin B or flucytosine, which have a different mechanism of action. Has activity against various pathogenic fungi of the genus Aspergillus as well as vegetative forms Pneumocystis carini. Resistance to echinocandida occurs as a result of a gene mutation FKS1 , which encodes the large subunit of (1,3)-β-D-glucan synthase.

Caspofungin is used only parenterally, because. oral bioavailability is less than 1%.

Assign caspofungin for empirical therapy in patients with febrile neutropenia with suspected fungal infection, with candidiasis of the oropharynx and esophagus, invasive candidiasis (including candidemia), invasive aspergillosis with ineffectiveness or intolerance of other types of therapy (amphotericin B, amphotericin B on lipid carriers and/or itraconazole).

Since (1,3)-β-D-glucan is not present in mammalian cells, caspofungin has an effect only on fungi, and therefore it is distinguished by good tolerance and a small number of adverse reactions (usually not requiring discontinuation of therapy), including . fever, headache, abdominal pain, vomiting. There are reports of cases of allergic reactions (rash, swelling of the face, itching, feeling of heat, bronchospasm) and anaphylaxis during the use of caspofungin.

LS of other groups. Antifungal drugs of other groups include agents for systemic (griseofulvin, flucytosine) and local (amorolfine, ciclopirox) use.

Griseofulvin - one of the first natural antifungal agents - an antibiotic produced by a mold fungus Penicillium nigricans (griseofulvum). Griseofulvin has a narrow spectrum of activity - it is effective only against dermatomycetes. It is used orally in the treatment of severe forms of dermatomycosis, which are difficult to treat with external antifungal agents.

Amorolfine is a broad-spectrum synthetic antimycotic for topical use (in the form of nail polish).

Cyclopirox is a synthetic drug for topical use.

Flucytosine is a fluorinated pyrimidine that differs in mechanism of action from other antifungal agents. It is used in / in the treatment of systemic infections, incl. generalized candidiasis, cryptococcosis, chromoblastosis, aspergillosis (only in combination with amphotericin B).

The choice of antifungal drug is based on the clinical picture and the results of laboratory tests for fungi. These studies include the following:

1. Microscopy of native preparations of sputum, exudate, blood, scrapings from the tongue, tonsils, microbiopsy, etc.

2. Microscopy of stained preparations (biosubstrates). At the same time, it is important to detect not just fungal cells, but their vegetative forms - budding cells, mycelium, pseudomycelium.

3. Cultural microscopic examination with inoculation of the material on nutrient media to identify the type and strain of the pathogen fungus.

4. Cytological examination of biosubstrates.

5. Histological examination of biopsy specimens (assessment of the invasiveness of the process).

6. Immunological diagnostic methods are used to detect antibodies to fungi, as well as sensitization, hypersensitivity to them.

7. Determination of metabolites-markers of fungi of the genus Candida using azochromatographic monitoring. The main metabolite-marker is D-arabinitol (the background concentration in the blood is from 0 to 1 µg/ml, in the cerebrospinal fluid - 2-5 µg/ml). Other markers-components of the cell wall of fungi of the genus Candida are mannose (normally in the blood serum of children - up to 20-30 μg / ml) and mannitol (normal - up to 12-20 μg / ml).

8. Detection of specific Candida antigens (by latex agglutination and by enzyme-linked immunosorbent assay to determine mannan) is typical for patients with generalized and visceral forms of candidiasis and is rarely found in superficial forms.

With deep mycoses, the use of the listed methods of laboratory diagnostics is mandatory.

The concentration of antifungal drugs in the blood is determined only in the framework of scientific studies. The exception is flucytosine - its side effect depends on the dose, and in case of renal failure, the concentration in the blood quickly reaches toxic. The efficacy and adverse effects of azoles and amphotericin B do not directly depend on their serum concentrations.

Currently, antimycotics are under development, which are representatives of already known groups of antifungal agents, as well as related to new classes of compounds: corinecandin, fuzacandin, sordarins, cispentacin, azoxybacillin.

Preparations

Preparations - 3657 ; Trade names - 204 ; Active ingredients - 35

Active substance	Trade names
Information is absent

The main condition for the effective treatment of candidiasis in women is etiotropic therapy, which is aimed directly at the elimination of Candida fungi. To do this, use tablets from thrush. The arsenal of pills is huge.

They are produced in two types:

• vaginal (local action);
• systemic action.

If the gynecologist has determined a mild degree of thrush, topical tablets are sufficient for treatment. Local tablets (vaginal) are injected directly into the vagina. As a rule, the scheme is simple: 1 tablet - 1 time per day, in the evening, at night. The duration of treatment depends on the form of the disease. For the treatment of acute candidiasis, 5-7 days are needed, the course of treatment of chronic candidiasis is at least two weeks.

The most popular and frequently prescribed local remedies by gynecologists are Pimafucin, Econazole, Livarol, Ginezol, Gino-Pevaril suppositories, tablets and suppositories based on clotrimazole.

1. Pimafucin is a popular and fairly effective drug approved for the treatment of women during pregnancy and lactation. Available in the form of tablets, suppositories and ointments. Pimafucin is well tolerated and has no allergic reactions, it is known as a non-toxic drug. Contains the active substance of a wide spectrum of action - the antifungal antibiotic natamycin.


2. Livarol is a safe and effective antifungal drug with an active substance - ketoconazole. Can be used during pregnancy (except the first trimester). The drug is sold in the form of candles. Treatment of the acute form of candidiasis lasts 5 days, chronic treatment - at least 10.
3. Clotrimazole is an antifungal drug in the form of tablets, cream, powder, ointment and solution for external use. Do not use for treatment during pregnancy and lactation.
4. Hexicon - a drug is produced in the form of suppositories, cream, external solution and gel. This antiseptic drug with the active substance chlorhexidine bigluconate shows excellent results in the treatment of candidiasis in pregnant women, it is used before childbirth for sanitation.

Treatment of the disease only with topical preparations is allowed for the first time candidiasis that occurs in an acute form. All other cases are treated comprehensively - systemic ones are connected to local drugs.

Systemic tablets

The active substance, which is contained in systemic tablets, is absorbed directly into the blood through the gastrointestinal tract, and thus disperses throughout the body, acting on the affected organs. The active substance of drugs remains in the body for a long time, after antifungal therapy is excreted from the body by the kidneys.

Candidiasis is treated with tablets that contain various active substances:

• fluconazole;
• natamycin;
• ketoconazole;
• miconazole;
• nystatin.

Pills and other drugs differ not only in doses, but also in how quickly they are absorbed in the body.

Common to all antifungal drugs is the mechanism of action: they suppress the reproduction of pathogenic fungi, and after a while the mycelium of Candida fungi is completely destroyed.

Gynecologists prefer systemic preparations based on three active substances: fluconazole, itraconazole and ketoconazole.

There are many commercial names of drugs, but there are not so many active substances on the basis of which they are produced.

Fluconazole

This remedy for candidiasis, produced in capsules, is considered to be the "gold standard" in the treatment of candidiasis. Most types of pathogenic Candida fungi, including the most common pathogen Candida albicans, are sensitive to them. The advantage of the drug: the drug does not cause fungal resistance, and is also well tolerated by patients and has a convenient dosage regimen:

• per day - 1 capsule (150 mg) - for acute candidiasis;
• 1 capsule (150 mg) - 3 days in a row - in the chronic course of the disease;
• 1 capsule (150 mg) - per week, 3 or 6 months - for prevention.

Itraconazole

Common and quite effective pills for thrush, but they are prescribed for individual intolerance to Fluconazole or when it is ineffective.

The course of admission and the scheme depend on the form of the disease:

• in the acute form of candidiasis - 200 mg once a day for 3 days in a row;
• with chronic - 100-200 mg per day - a week in a row;
• in the prevention of relapse - 100 mg on the first menstrual day - 3 months.

Ketoconazole

This drug for thrush, like the previous one, is considered to be a reserve remedy. What does it mean? With both Itraconazole and Ketoconazole, treatment is never prescribed, they are used only if there is no effective effect from Fluconazole. This drug is used according to a simple scheme exclusively for the treatment of thrush:

• 1 tablet of the drug (200 mg) 2 times a day or 2 tablets (400 mg) - once a day, 5 days in a row.

Prevention of relapses with Ketoconazole tablets is not carried out. Other systemic remedies for thrush are also available - the list can be extended.

No matter how popular and effective tablets, ointments, capsules and suppositories from thrush are, if used incorrectly, they will only cause harm, for example, they will transfer the disease from an acute form to a chronic one. That is why the treatment of candidiasis should be prescribed only by a doctor. Self-treatment and self-diagnosis are unacceptable for any diseases.

Does soda help?

Douching with soda is a popular and proven method at home in the fight against thrush. The soda solution cleanses the vagina of bacteria and fungi. Candida fungi in the acidic environment of the vagina feel great. Turning an acidic environment into an alkaline one is easy: douching with soda (soda is alkaline).

The soda solution prevents the reproduction of fungi by destroying their microfibers. Douching with soda also helps with external manifestations of thrush: soda solution reduces itching and burning, removes unpleasant vaginal discharge.

Is it possible to cure thrush with soda? Doctors prescribe douching with soda as an additional treatment in the complex treatment of candidiasis. The most effective effect is achieved if douching with soda is carried out in combination with the use of antifungal drugs: suppositories, ointments, tablets.

The effect of douching will increase if you use an ointment with levorin or nystatin after the procedure.

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General information about the disease and drugs

The disease, known as thrush, is provoked by fungi of the genus Candida. Rapid reproduction on the mucous membranes of the mouth, nasopharynx, external genitalia leads to the appearance of a characteristic white curdled plaque, thanks to which the name of the disease appeared. In addition to external signs of the presence of fungal flora, a focus of local inflammation is formed with the development of symptoms of itching, burning, redness and soreness. It is believed that the provoking factors can be a violation of the immune system, non-compliance with hygiene standards, trauma to the mucous membranes and the transfer of infection from an infected person.

Practitioners for a long time remember that a few decades ago, to eliminate thrush, it was necessary to undergo a long course of conservative therapy, which included mechanical cleansing of the affected surfaces, the appointment of antibacterial and anti-inflammatory drugs, stimulation of the immune system and vitaminization. The discovery of fluconazole, an active ingredient effective against several varieties of Candida, marked the beginning of a new era in the treatment of an unpleasant disease. A good and fast result, as well as the almost complete absence of side effects caused a stir in the medical community.

The first drug containing fluconazole in oval-shaped capsules for internal use appeared in France and was called Diflucan. The patent for the invention, according to the principle common to all pharmacological discoveries, was bought out by several dozen manufacturing pharmaceutical companies. Generics appeared - products with a similar composition, but different names, among which are domestic products - Fluconazole.

Each manufacturer independently determines the pricing policy for the cost of medicines. Diflucan is much more expensive than Fluconazole. The Russian drug is produced on the territory of the country, which excludes the cost of delivery and customs fees. The average price in a pharmacy, depending on the region, ranges from 20 to 50 rubles, which is 4 times cheaper than the original product in the same dosage and represents a significant difference.

Given the equal amount of the same active ingredient in Diflucan and Fluconazole capsules, one can initially conclude that the funds presented are equivalent and choose a cheaper Russian drug. According to patients, there are still differences that make one think about the correctness of the first impression.

Similar Specifications

To compare the principle of action and scope of Diflucan and Fluconazole will help the instructions that are in the packaging of all pharmacological agents. First of all, you should pay attention to similar characteristics:

• The amount of active ingredient. Capsules are available with different contents of fluconazole - from 25 to 150 mg. For the treatment of complex generalized infections, there is a release form in the form of a solution.
• Indications for appointment. Diseases caused by fungi of the genus Candida with a predominant lesion of the mucous membranes, as well as the addition of a fungal infection to the course of the inflammatory process of a bacterial or viral nature. The active substance of the Russian Fluconazole and the French Diflucan is equally effective against the symptoms of thrush.
• Bioavailability. The mechanism of absorption of the active substance is the same for both drugs. In small concentrations, fluconazole is found in saliva, sweat, blood, tears, semen, urine and breast milk, that is, in all biological fluids of the human body.
• Withdrawal. The destruction of decay products and residual molecules occurs by filtration in the kidneys, after which the agent leaves the body as part of the final urine.

Action speed. The maximum concentration of the drug is reached in the blood within 30 minutes after taking the capsule with the drug.

Side effects. The instructions for preparations containing fluconazole as the main active ingredient contain the same information about negative effects. There may be problems with digestion, flatulence, manifestations of intestinal dysbacteriosis. Both drugs are recommended with caution in chronic diseases of the liver and kidneys.

Contraindications. The presence of pregnancy, breastfeeding and children under 4 years of age limit the appointment of Fluconazole and Diflucan, which is described in the annotation for medicines of any production.

There are no visible differences between Diflucan and Fluconazole, however, many doctors recommend that their patients opt for a French drug, which is caused by the existing differences, which, in a superficial comparison, may be ignored.

Drug differences

Re-reading the instructions will allow you to find out some points that clearly demonstrate the difference between the two drugs based on fluconazole:

• Auxiliary components. The annotation to the French Diflucan describes in detail the additional substances that make up the capsule. The Russian manufacturer did not consider it necessary to indicate which ingredients were used.
• Clarification on the scope. Mushrooms of the genus Candida are represented by several varieties, and the active component is effective against all except Crusei, which is warned by the instructions for the original drug and the annotation to the generic is silent.
• Treatment of children. If it is necessary to give a drug to a child, detailed information can be easily found in the instructions for Diflucan, and the manufacturers of Fluconazole did not consider it necessary to amend the description.
• Clinical Trials. The original French medicine has passed a lot of preliminary trials and tests, without which it is impossible to obtain an international patent. There is no data on such checks of the Russian drug.
• Package. It is very difficult to fake Diflucan. A multi-stage protection system, original design, a special blister format - all this speaks of quality and protection against fakes. Fluconazole has a cardboard box and a soft blister pack with a low degree of protection.
• Price. The price matters, especially if the treatment requires a course of medication. Fluconazole in this case has an advantage, since it costs 4 times cheaper than Diflucan.

Based on detailed information about two effective drugs of different production, you can draw an independent conclusion and choose the most appropriate treatment for thrush.

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Mechanism of action and pharmacological effects of azoles

Azoles have a fungistatic effect. They inhibit the synthesis of fungal cell membrane ergosterol at the level of formation of dimethylergostatrienol from lanosterol by inhibiting the cytochrome P450-dependent C14-a-dimethylation reaction (Fig. 1). This pathway of sterol biosynthesis is characteristic only of fungi. Due to the higher affinity for the enzyme catalyzing the synthesis of ergosterol in fungi than for the enzyme catalyzing the synthesis of cholesterol in humans, the selectivity of the action of triazoles on fungal cells is much higher (for fluconazole - 10,000 times) than on mammalian cells. Fluconazole has the highest selectivity. At very high concentrations of azoles, rarely achieved with systemic treatment, severe membrane damage leads to a fungicidal effect. In fungicidal concentrations (when applied topically), azoles interact with mitochondrial and peroxidase enzymes, resulting in an increase in the concentration of hydrogen peroxide to a toxic level, which leads to the death of a fungal cell at the proliferation stage.
Itraconazole after voriconazole has the broadest spectrum of action of all oral antimycotics. It is fundamentally different from other azoles (with the exception of voriconazole) by the presence of activity against mold fungi Aspergillus spp. (MIC 0.5-10 µg/ml). The main pathogens of candidiasis are also sensitive to itraconazole (C. dlbicans, C. lusitaniae, C. parapsilosis, C. tropicalis) (MIC 0.1-5 μg / ml), dermatophytosis (Epidermophyton spp., Trichophyton spp., Microsporum spp.) (MIC 0.1-1 μg / ml), multi-colored, or pityriasis, lichen (Malassezia furfur, or Pityrosporum ovale, Pityrosporum orbiculare), subcutaneous mycoses (Sporotrix schensckii), deep mycoses (Cryptococcus neoformans, Blastomyces dermatitidis, Coccidiodes immitis, Paracoccidiodes brasiliensis, Histoplasma capsulatum), as well as Cladosporium carrionii, Pseudallescheria boydii, Fusarium spp., Fonsecaea spp., Penicillium marneffei. C. krusei and C. glabrata are often resistant to it. Cross-resistance to all azoles is possible. Highly sensitive to itraconazole are strains of Candida spp., having an MIC up to 0.125 μg / ml, strains with intermediate sensitivity - MIC 0.25-0.5 μg / ml, resistant - MIC above 1 μg / ml.
Voriconazole has a spectrum of action similar to that of itraconazole, but differs in the presence of high activity against C. krusei and C. glabrata, greater efficiency against Pseudallescheria boydii, Fusarium spp.
Fluconazole has a fungistatic effect against Candida dlbicans, a number of strains of Candida nondlbicans (C. guilliermondii, C. pseudotropicalis, C. torulopsis, C. kefyr, C. stellatoidea) (MIC about 1 μg / ml), dermatophytes (Microsporum spp., Trichophyton spp.) (MIC more than 5 μg / ml), multi-colored, or pityriasis, lichen (Malassezia furfur, or Pityrosporum ovale, Pityrosporum orbiculare), as well as pathogens of deep mycoses (Cryptococcus neoformans, Coccidiodes immitis, Pseudallescheria boydii). Less sensitive are Blastomyces dermatitidis, Histoplasma capsulatum, Paracoccidiodes brasiliensis, Sporotrix schensckii. Aspergillus spp. and C. krusei are naturally resistant to fluconazole. Most strains of C. glabrata, C. lusitaniae, C. parapsilosis, C. tropicalis are also resistant to the drug. Rarely, AIDS patients receiving long-term therapy have acquired resistance to Cryptococcus neoformans. The activity of fluconazole against molds is less than against yeasts. Highly sensitive to fluconazole are strains with an MIC up to 8 µg/material; strains with intermediate sensitivity - IPC 16-32 µg/material; resistant - IPC 32-64 kg / ml and above.
Ketoconazole is similar in spectrum to itraconazole, but does not affect aspergillus. The MIC of ketoconazole in relation to dermatophytes is 0.1-0.2 μg / ml, for Candida Olbicans - 0.5 μg / ml. For Candida spp. Ketoconazole sensitivity is defined as MIC less than 8 µg/mL, resistance is greater than 16 µg/mL. Many mold fungi - causative agents of non-dermatophyte onychomycosis - are resistant to ketoconazole. Occasionally there are strains of Candida Olbicans resistant to ketoconazole. The drug is moderately active against staphylococci and streptococci.
Comparative data on the sensitivity of the main species of fungi of the genus Candida to systemic antimycotics are shown in Table 4.
Azoles applied topically are active mainly against candida, mold fungi (Aspergillus ferrus, Scopulariopsis brevicaulis), dermatophytes (Epidermophyton spp., Trichophyton spp., Microsporum spp.), the causative agent of multi-colored, or pityriasis, lichen, as well as some gram-positive cocci ( streptococci, staphylococci) and corynebacteria - causative agents of erythrasma (Corynebacterium minutissimum). Clotrimazole has a moderately pronounced effect on some anaerobes (bacteroids, gardnerella) and Trichomonas. The MIC of bifonazole in relation to C. minutissimum is 0.5-2 μg / ml, in relation to gram-positive cocci, with the exception of enterococcus, 4-16 μg / ml.
All azoles are inactive against zygomycetes (Mucor spp., Rhizopus spp., etc.), as well as Rhodotorula spp. and Trichoderma spp.

Table 4 Sensitivity Candida spp. to systemic antimycotics based on NCCLS standards

View	Amphotericin B		Fluconazole		Itraconazole		Ketoconazole
	MIC, mcg/ml	% sensitive strains	MIC, mcg/ml	% sensitive strains	IPC, mcg/ml	% sensitive strains	IPC, mcg/ml	% sensitive strains
C. guilliermondii

Pharmacokinetics

Azoles, when applied topically, create high and fairly stable concentrations in the epidermis and dermis, which exceed the MICs of the main pathogenic fungi. The therapeutic concentration of bifonazole is maintained the longest, the half-life of which from the skin is 19-32 hours. Systemic absorption through the skin is minimal (when bifonazole is applied to healthy skin - 0.6-0.8%, to inflamed skin - 2-4%). With vaginal application of clotrimazole, absorption is 3-10%. Less than 1% of econazole is excreted in the urine and bile.
Miconazole can be used not only topically, but also inside and intravenously. It is 93% bound to plasma proteins. It is distributed mainly in the connective tissue, penetrates through the synovial membranes. It passes poorly into the fiber of the eye and through the BBB. Therapeutic concentration in the blood is maintained for 4-6 hours. T^2 - 24 hours. It is metabolized by microsomal liver enzymes, undergoing oxidative dealkylation.

Fluconazole, unlike other oral antimycotics, is a hydrophilic compound. Ketoconazole and itraconazole are used topically or orally, fluconazole and voriconazole are used orally or intravenously. Ketoconazole, fluconazole and itraconazole are well absorbed from the gastrointestinal tract. Under the influence of hydrochloric acid of the stomach, ketoconazole and itraconazole pass into well-soluble hydrochlorides. Food reduces the absorption of ketoconazole, but does not affect the absorption of fluconazole. The pharmacokinetics of fluconazole when administered orally and intravenously are similar. When administered orally, the bioavailability of ketoconazole is 75%, voriconazole - 96%, fluconazole - 80-90% and above, itraconazole - variable (average 70%): in capsules - from 40-55% (on an empty stomach) to 90-100% (with food), in solution - from 55% (with food) to 90-100% (on an empty stomach). Itraconazole undergoes 85% first-pass biotransformation in the liver. The main of its more than 30 metabolites, hydroxyitraconazole is active, its plasma level exceeds the concentration of itraconazole. The maximum concentration of fluconazole in the blood is reached after 0.5-2 hours, itraconazole and ketoconazole - after 2-4 hours, voriconazole - after 1-2 hours. The maximum concentration of fluconazole after taking 50 mg is 1 μg / ml, 100 mg - 1, 9-
2 μg / ml, 150 mg - 2.44-3.58 μg / ml, 400 mg - 6.7 μg / ml. The maximum concentration after taking 100, 200 and 400 mg of itraconazole in capsules is 0.1-0.2 (average 0.127) μg / ml, 0.25-1 (average 0.272) μg / ml and 1.2 μg / ml , respectively. After taking 100, 200 and 400 mg of ketoconazole, it is 1.6 μg / ml, 1.7-4.5 μg / ml (average
3 µg/ml) and 5-6 µg/ml. The maximum concentration after taking 100 mg of voriconazole is 3.1-4.8 mcg / ml. The concentration of drugs in the blood is directly proportional to the dose taken.
The equilibrium concentration of ketoconazole is established on the 3-4th day, fluconazole - by the 4-7th day with a daily intake of 1 r / day. When used on the 1st day of a double dose, the equilibrium concentration of fluconazole is reached by the 2nd day. The equilibrium concentration of itraconazole is established after 1-2 weeks and is 0.4 μg / ml at 100 mg / day, 1.1 μg / ml at 200 mg / day, 2 μg / ml at 400 mg / day. Voriconazole is characterized by non-linear pharmacokinetics - when doubling the dose, AUC increases by 4 times. Communication with plasma proteins of fluconazole - 10-12%, itraconazole and ketoconazole - 99%, voriconazole - 58%. Fluconazole, voriconazole and ketoconazole are relatively evenly distributed throughout the body. The volume of distribution of ketoconazole - 0.3-0.4 l, fluconazole - 5.6-6.4 l, voriconazole - 4.6 l.
Fluconazole concentrations in saliva, sputum, joint and peritoneal fluids, vaginal secretions, breast milk are similar to those in blood plasma, in most tissues they are about 50% of the plasma level. The concentration of fluconazole in the liquor is 50-90% (on average 70-80%) of the level in the blood plasma, with meningitis - from 52 to 85-93%. Fluconazole also penetrates the hematoophthalmic barrier. All azoles pass through the placenta, are excreted in breast milk, and fluconazole is in the highest concentration, close to the level in blood plasma. In the stratum corneum of the skin, epidermis, dermis, sweat fluid and urine, fluconazole concentrations reach values ​​10 times higher than the level in blood plasma. The concentration of fluconazole in the stratum corneum one week after taking 150 mg is 23.4 mcg / g, one week after taking the 2nd same dose - 71 mcg / g, and after 12 days of use at a dose of 50 mg 1 r / day - 73 mcg / g. Already on the 1st day of treatment in the distal part of the nail plate, fluconazole is detected at a concentration of 1.3 µg/g. Its concentration in the nails after 4 months of use at a dose of 150 mg 1 r / week is 4.05 μg / g in healthy and 1.8 μg / g in affected nails. At the end of 6-12 months of treatment, it reaches 8.5 mcg/g. The drug is determined in the nails within 6 months after completion of therapy: after 3 months at a concentration of 1.7 mcg / g, after 6 months - 1.4 mcg / g.
Itraconazole, being a highly lipophilic compound, is distributed mainly in organs and tissues with a high fat content: in the liver, kidneys, and greater omentum. In the lungs, stomach, liver, spleen, kidneys, skeletal muscles and bones, the level of itraconazole is 2-3 times higher than the serum level. In the tissues of the external genital organs and inflammatory exudates, its concentration is 7 times higher than in the blood plasma. At the same time, itraconazole almost does not penetrate into aqueous media - saliva, intraocular and cerebrospinal fluid. However, it accumulates in the skin, incl. in the epidermis and nails (at concentrations 4 times higher than serum levels), a day later it is found in secret by
tovy glands. On the 4th day of treatment, the concentration of antimycotic in sebum exceeds plasma levels by 5-10 times. Itraconazole appears in the distal part of the nail plate a week after the start of administration. Once in the nails, it does not return to the systemic circulation. The concentration of antimycotic in the nail increases during treatment and increases 10 times with an increase in the dose from 100 to 200 mg / day. With 3-month treatment in the nails of the feet, it is 10 μg / g 2 months after withdrawal, 0.67 μg / g - after 6 months, and from the 10th month it is no longer determined. Effective concentrations in the skin persist for 2-4 weeks after discontinuation of the drug.
The concentration of ketoconazole in the epidermis at a dose of 200 mg / day is 3 μg / g, at a dose of 600 mg / day - 5 μg / g. In the skin and secretion of sweat glands, it is found 1 hour after ingestion. The drug penetrates into the nails through the matrix and the nail bed, it can be detected on the 11th day from the start of treatment. Fungicidal concentrations of ketoconazole in the vaginal mucosa are created on the 3rd-4th day. Ketoconazole passes poorly through the BBB (the concentration in the cerebrospinal fluid is 2-7% of serum).
T1 / 2 fluconazole - 20-35 hours (average 27-30 hours), itraconazole - two-phase (final phase - 20-45 hours, average 30-40 hours), ketoconazole - from 2-4 hours (initial phase) to 6-10 hours (final phase). Itraconazole is metabolized in the liver, excreted in the bile (3-18% - unchanged). 35-40% of itraconazole metabolites and 0.03% of the unchanged drug are excreted in the urine. Ketoconazole also undergoes biotransformation in the liver (oxidative deoxylation, aromatic hydroxylation), but is excreted by 70% in the urine (mainly in the form of metabolites, 5% unchanged). T1 / 2 of these drugs in renal failure does not change. Voriconazole is excreted in urine and bile. Fluconazole is only partially biotransformed in the liver. Excreted by the kidneys, 70-90% - unchanged. The concentration in the urine is more than 100 mcg / ml. Clearance of ketoconazole 2 ml / min / kg. Fluconazole clearance is high and proportional to creatinine clearance. With renal failure, its T1 / 2 can increase up to 3-4 days. The concentration of fluconazole in plasma can be reduced by dialysis (by 50% within 3 hours). Itraconazole is not removed from the body during hemodialysis.

Place in therapy

Indications for the appointment of topical azoles:
skin candidiasis, candidal paronychia;
Dermatophytosis (epidermophytosis and trichophytosis of smooth skin, hands and feet, microsporia, favus, onychomycosis);
pityriasis (colorful) lichen;
erythrasma;
· seborrheic dermatitis;
Candidiasis of the oral cavity and pharynx;
Candidiasis vulvitis, vulvovaginitis, balanitis;
trichomoniasis.
Indications for the appointment of systemic azoles:
skin candidiasis, including intertriginous candidiasis (yeast diaper rash of the skin folds and inguinal region);
onychomycosis, candidal paronychia;
Keratomycosis (pityriasis versicolor, trichosporosis);
Dermatophytosis, including superficial trichophytosis of the smooth skin of the face, trunk and scalp, infiltrative-suppurative trichophytosis, epidermophytosis of the groin and feet, microsporia;
subcutaneous mycoses (sporotrichosis, chromomycosis);
Pseudo-allescheriasis
Vulvovaginal candidiasis, colpitis and balanoposthitis;
candidiasis of the mucous membranes of the oral cavity, pharynx, esophagus and intestines;
systemic (generalized) candidiasis, including candidemia, dissemi
nirovanny, visceral candidiasis (candidiasis myocarditis, endocarditis, bronchitis, pneumonia, peritonitis, urinary tract candidiasis);
deep endemic mycoses, including coccidioidomycosis, paracoccidioidomycosis, histoplasmosis and blastomycosis;
cryptococcosis (skin, lungs and other organs), cryptococcal meningitis;
prevention of fungal infections in patients with reduced immunity, transplanted organs and malignant neoplasms.

Indications for the appointment of itraconazole is also aspergillosis, in which its effectiveness is 75%, as well as pheogyphomycosis. With systemic therapy with itraconazole for onychomycosis, clinical and mycological cure is observed in 87-90% of cases (in 85-100% of patients with onychomycosis of the hands and in 73-98% with onychomycosis of the feet). When taking itraconazole for 1 week, recovery is observed in 85% of patients with mycoses of the feet. Itraconazole was also highly effective in the treatment of ophthalmomycosis. In the treatment of patients with subcutaneous mycoses with itraconazole, recovery is observed in 97% of cases of sporotrichosis and in 75% of cases of chromomycosis. Efficiency in patients with deep mycoses is 96% for paracoccidioidomycosis, 76% for histoplasmosis. Itraconazole cures 64% of cases of leishmaniasis.
Voriconazole is indicated mainly for systemic aspergillosis and candidiasis, fusarium and pseudoalescheria. It is also used in empirical antifungal therapy.
Fluconazole is the most effective drug for candidiasis of any localization. It is used orally or intravenously 1 r / day. The duration of treatment with fluconazole for skin candidiasis is 2-6 weeks, for oropharyngeal candidiasis - 7-14 days, for candidiasis of other localization (candiduria, candidal esophagitis and non-invasive broncho-pulmonary candidiasis) - 14-30 days, for onychomycosis - 3-6 months with damage to the nails of the fingers and 6-12 months - with damage to the nails of the toes (before replacing the infected nail), with candidal balanoposthitis or vaginal candidiasis - once, with candidal vulvovaginitis - up to 7 days, with chronic recurrent (3-4 r / year or more often) vulvovaginal candidiasis 3-4 doses at 3-7-day intervals, sometimes up to 12 times at monthly intervals, with candidemia, disseminated candidiasis - 7-14 days or more, with deep endemic mycoses - up to 2 years: 11-24 months with coccidiomycosis, 2-17 months - with paracoccidiomycosis, 1-16 months - with sporotrichosis, 3-17 months - with histoplasmosis, with cryptococcal meningitis - up to 6-8 weeks, with cryptococcal infections of other localization - 7-14 days. For the prevention of fungal infections, fluconazole is prescribed throughout the entire period of antibacterial, glucocorticosteroid, cytostatic or radiation therapy. The clinical efficacy of fluconazole is 83-100% for fungal lesions of the mucous membranes, skin and its appendages, 74-83.4% for urogenital candidiasis, 74.7% for candidal bronchitis, 66.7% for candidal pneumonia, and candidemia - 64-70%, with generalized candidiasis in children - 60-80%, with local candidiasis in children (stomatitis, gingivitis, esophagitis, vulvovaginitis, intestinal candidiasis) - 90%.
Ketoconazole, due to its high toxicity (hepatotoxicity), has now largely lost its significance as a systemic antimycotic and is used more often topically. Inside, ketoconazole is prescribed for candidiasis of the skin and dermatophytosis for 2-8 weeks, for onychomycosis of the hands - for 4-6 months, for onychomycosis of the feet - for 8-18 months, for candidiasis of the oral cavity, gastrointestinal tract and genitourinary system - for 4-6 weeks, with deep mycoses - within a few months. With oral administration of ketoconazole, its clinical efficacy is 25-52% for skin candidiasis, 55-80% for dermatophytosis, 50-55% for onychomycosis, 90% for candidal vaginitis, 52% for histoplasmosis, and 80% for paracoccidioidomycosis. %.
Miconazole orally is prescribed for candidiasis of the oral cavity, pharynx, gastrointestinal tract. In / in or intrathecally, it is currently practically not used due to the presence of low-toxic fluconazole, highly effective when administered orally and parenterally.
Clotrimazole remains the main drug for local (external or intravaginal) use.

Tolerability, side effects of azoles

Among the azoles of systemic action, fluconazole is the least toxic. It is well tolerated, does not affect steroid metabolism, but can sometimes cause the following side effects.
From the digestive system: loss of appetite, abdominal pain, flatulence, nausea, vomiting, diarrhea, constipation, increased activity of "liver" transaminases and alkaline phosphatase, hyperbilirubinemia, cholestasis.
On the part of the nervous system in rare cases: headache, dizziness, drowsiness, insomnia, impaired consciousness, vision, hallucinations, paresthesia, tremor, convulsions.
On the part of the hematopoietic system: in some patients - hypoplastic anemia, leukopenia, neutropenia, agranulocytosis, thrombocytopenia.
Other undesirable effects: allergic reactions, skin rash, itching, alopecia, hypercholesterolemia, hypertriglyceridemia. Severe reactions are sometimes possible in AIDS patients and cancer patients: hepatotoxic, nephrotoxic and myelotoxic effects, Stevens-Johnson syndrome and toxic epidermal necrolysis.
Itraconazole and ketoconazole, in addition to the side effects listed for fluconazole, can cause hypercreatininemia, have a pronounced hepatotoxic effect (monthly monitoring of transaminase activity is required), reduce the biosynthesis of glucocorticoids and sex hormones, which is manifested in men by gynecomastia, oligospermia, decreased libido, impotence, and in women - violation of the menstrual cycle. So, with oral administration of ketoconazole, an asymptomatic increase in transaminase activity is observed in 5-10% of cases, hepatitis - in 0.1% of cases. Risk factors for hepatitis are a previous liver disease, taking hepatotoxic drugs, and long-term use of the drug. Ketoconazole leads to a decrease in the level of testosterone in the blood at a dose of 800 mg / day. Itraconazole, in addition, can cause congestive heart failure, increased blood pressure, edema, hypokalemia and ventricular arrhythmia.
Miconazole, when taken orally, can cause nausea, diarrhea, allergic reactions; when administered intravenously, thrombophlebitis, chills, rhinitis, skin rash, anorexia, nausea, diarrhea, tachycardia, arrhythmias, hyperlipidemia, increased erythrocyte aggregation, allergic reactions.
With external use of azoles in 5% of cases, a rash, itching, burning, hyperemia, peeling of the skin appear, in rare cases, contact dermatitis may develop.
When administered intravaginally, azoles can cause itching, burning, hyperemia and swelling of the mucous membrane, vaginal discharge, and increased urination.
Contraindications
Azoles of local action are contraindicated in the first trimester of pregnancy and with allergies to them. Data on cross-allergy to all azoles are not available. Azoles of systemic action are contraindicated in the following cases:
hypersensitivity;
severe liver dysfunction (for itraconazole and ketoconazole);
pregnancy (for itraconazole, voriconazole and ketoconazole);
· lactation;
children's age (for itraconazole).
Cautions
When treating with topical azoles, contact with the eyes should be avoided.
In the treatment of systemic azoles, the use of alcohol should be excluded.
Special selection of doses of fluconazole for elderly patients is not required, if kidney function is not depressed (creatinine clearance less than 40-50 ml / min).
In patients with renal insufficiency, a correction of the dosing regimen of fluconazole is required, depending on the clearance of endogenous creatinine (with a creatinine clearance of 50 ml / min, the dose does not change, at 11-50 ml / min the dose is halved). For external use and a single oral dose adjustment is not required.
As shown by animal experiments and clinical studies on 625 pregnant women, the course use of fluconazole in the first trimester of pregnancy and later at a dose of 150 mg / day does not increase the incidence of congenital developmental defects, fetal malnutrition and premature birth. In contrast, ketoconazole and flucytosine have been shown to be embryotoxic and teratogenic. Nevertheless, the use of fluconazole in pregnant women should be avoided, except in cases of severe and potentially life-threatening fungal infections, when the expected benefit of treatment outweighs the possible risk to the fetus.

Interactions

Antacids, M-anticholinergics, H2-histamine blockers and proton pump inhibitors reduce the bioavailability of itraconazole and ketoconazole, as they reduce acidity in the stomach and prevent the conversion of azoles into soluble forms. The absorption of azoles in the intestine is also reduced by adsorbents and enveloping agents. Ketoconazole reduces the absorption of rifampicin. Rifampicin and isoniazid accelerate the biotransformation of azoles in the liver, lower their plasma levels and reduce the effectiveness of treatment (rifampicin reduces T1 / 2 of fluconazole by 20%, AUC by 25%). Carbamazepine and phenytoin reduce the concentration of itraconazole in the blood. Hydrochlorothiazide increases the plasma concentration of fluconazole by 40%. The combination of itraconazole with statins is accompanied by an increase in their concentration in the blood with the possible development of rhabdomyolysis. Cytochrome P450 inhibitors (cimetidine, erythromycin, clarithromycin, etc.) can inhibit the metabolism of itraconazole and ketoconazole and increase their serum concentrations. Ketoconazole in combination with alcohol can cause disulfiram-like reactions. Ketoconazole, itraconazole and, to a lesser extent, fluconazole are inhibitors of cytochrome P450, therefore, they can interfere with the metabolism in the liver of the following drugs:
oral hypoglycemic agents (sulfonylurea derivatives) with the possible development of hypoglycemia;
Indirect anticoagulants with an increase in their action, prolongation of prothrombin time (when taking fluconazole - by 12%) and an increased risk of bleeding;
cyclosporine and digoxin (when prescribing itraconazole or ketoconazole, the dose of cyclosporine should be halved);
eophyllin, phenytoin, zidovudine, rifampicin and rifabutin (fluconazole);
midazolam, triazolam, calcium antagonists from the group of derivatives
Amphotericin B, nystatin, natamycin reduce the effectiveness of azoles when applied topically.
dihydropyridine, vincristine (itraconazole);
chlordiazepoxide, methylprednisolone (ketoconazole);
oral contraceptives levonorgestrel and ethinylestradiol (high doses of fluconazole cause an increase in the AUC of these drugs); terfenadine, astemizole, cisapride, quinidine, pimozide with an increase in their concentration in the blood, which may be accompanied by a prolongation of the QT interval on the ECG with the development of severe ventricular arrhythmias (combinations of systemic azoles with these drugs are unacceptable).
Antagonism of action is noted between ketoconazole, miconazole and amphotericin B.

lekmed.ru

Itraconazole: a brief description

Itraconazole is an antifungal agent related to azole derivatives of systemic action. It has two dosage forms of release: capsules and solution. The active substance is itraconazole.

Indications for use

Itraconazole is advisable to use for the treatment of the skin from various fungal infections and inflammatory processes.

In addition, it is effective for:

• dermatoses;
• candidiasis;
• lichen planus;
• mycotic eczema (with the defeat of large areas of the skin);
• dermatophytosis;
• sporotrichosis;
• onychomycosis.

Side effects

In general, Itraconazole was well tolerated by patients, but in some it provoked:

• failure in the functionality of the gastrointestinal tract;
• increased blood pressure;
• deterioration in the condition of the hair, their loss;
• decreased sexual activity;
• fast fatigue;
• headaches and vertigo;
• skin rashes, itching and burning;
• swelling of the face and limbs.

Application features

Itraconazole is taken by mouth. It is better to drink capsules before eating, the solution - after eating. The daily rate and duration of the therapeutic course is determined by the attending physician.

Fluconazole: a brief description

The drug has the same active ingredient. Produced by domestic and foreign pharmaceutical companies. It has two dosage forms: capsules and suspension. Designed for oral use. Popular analogues of Fluconazole: Terbinafine, Pimafucin, Nystatin and Itraconazole. Only a qualified specialist should decide whether it is possible to take Itraconazole instead of Fluconazole, or replace the latter with another analogue.

Side effects and overdose

Some women noted that fluconazole therapy was accompanied by:

• allergic manifestations: erythema, rashes on the epithelium, urticaria and swelling;
• severe pain in the head;
• convulsive lesions of the limbs;
• dizziness;
• disorders of taste buds;
• diarrhea
• nausea and vomiting;
• impaired functionality of the kidneys and liver.

If you take a large dose of fluconazole, it can provoke hallucinations and paranoia.

Is it possible to combine

Since these two drugs belong to the same pharmaceutical group, many patients wonder if it is possible to take Fluconazole and Itraconazole at the same time? Doctors say no, explaining that such a combination can provoke the development of side effects and adversely affect the patient's health.

What to choose

Comparing Itraconazole and Fluconazole, it can be initially noted that the difference between the drugs lies in the price: the first will cost the patient 390-460 rubles, the second - only 35-55 rubles. Both drugs have a broad action and fungicidal properties. They should not be taken during pregnancy and while breastfeeding, but both rarely cause side effects.

If the patient suffers from acute thrush, but the disease was diagnosed on time, it is enough for her to drink one tablet of Fluconazole. Itraconazole in a similar situation should be taken for a week. If we compare drugs in the fight against chronic thrush, then the use of Fluconazole is performed according to the scheme every 72 hours for nine days, and Itraconazole should be used once a day for 5-7 days.

It is up to the attending physician to decide which of these two drugs is better for the patient, based on the results of the diagnosis.

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pillsman.org

Classification of antifungal (antimycotic) drugs

In order to treat diseases caused by a fungus of the genus Candida, drugs of the following pharmacological groups can be used:

• antibiotics of the polyene group: levorin, nystatin, natamycin, amphotericin-B;
• imidazole derivatives: clotrimazole, isoconazole, voriconazole, ketoconazole, fenticonazole, butoconazole and others;
• thiazole derivatives: fluconazole;
• bis-quaternary ammonium salts: dequalinium chloride;
• N-methylnaphthalene derivatives: terbinafine.

Let's consider each group in more detail.

Antibiotics of the polyene group

They are natural antifungals. The mechanism of their action has been studied quite well and it consists in binding the drugs of this group with the ergosterol of the membrane of fungal cells, as a result, the integrity of this membrane is violated, which leads to the dissolution (lysis) of the cell.

The spectrum of activity of polyenes, in addition to Candida, also includes some protozoa: Trichomonas, Amoebas and Leishmania.

When ingested in the organs of the digestive tract, as well as from the surface of healthy, intact skin, these drugs are practically not absorbed. They are low toxic.

Most drugs are applied topically and orally, amphotericin B - intravenously.

Against the background of taking polyenes, undesirable effects such as allergic reactions, nausea, vomiting, abdominal pain, and diarrhea may develop.

Currently, drugs of this group for the treatment of thrush are rarely used, since other, more modern and effective drugs for this purpose have already been developed. The most common antifungal antibiotic is nystatin.

Nystatin

Produced in the form of tablets for oral administration and vaginal tablets, ointments, rectal suppositories (candles).

It is used to treat candidiasis of the mucous membranes of the mouth, skin and internal organs, as well as to prevent these diseases in case of long-term antibiotic therapy.

Adults are recommended to take the drug 250 thousand units 6-8 times a day or 500 thousand units 3-4 times a day. The average daily dose is 1.5-3 million units, and the maximum is 4-6 million units. You can use 2 dosage forms of nystatin - tablets and ointment - at the same time. The course of treatment is usually 10-14 days. With recurrent candidiasis, repeated courses of treatment are recommended - after 2-3 weeks from the previous one.

Vaginal tablets are administered 1-2 pieces (100-200 thousand units) deep into the vagina for 1.5-3 weeks.

Rectal suppositories are injected into the rectum 1-2 pieces (250-500 thousand units) twice a day for 10-14 days.

Nystatin preparations are contraindicated in case of increased individual sensitivity to this substance.

Side effects are nausea, vomiting, chills, fever, allergic reactions. In the event of these symptoms, it is recommended to reduce the dose of the drug. When using vaginal tablets, local irritation and soreness in the vagina may occur.

Nystatin is also part of combined antibacterial and antifungal drugs, such as Polygynax, Terzhinan.

Derivatives of imidazole and thiazole

The mechanism of action of drugs in this group is due to their effect on the synthesis of ergosterol, which is a structural component of the fungal cell membrane. Due to a violation of the production of this substance, the integrity of the cell membrane of the pathogen (the fungus that caused the disease) is violated, the cell dissolves, the fungus dies.

Different representatives of imidazole derivatives have their own spectrum of activity, that is, they affect a different number of fungal species.

They are applied systemically - inside - and locally.

Systemic drugs are ketoconazole, fluconazole, voriconazole and itraconazole.

For the purpose of local treatment, isoconazole, miconazole, clotrimazole, econazole, ketoconazole and others can be used.

Resistance (resistance, immunity) of the fungus to the action of these drugs develops quite rarely, but in certain clinical situations, for example, in the treatment of HIV-infected patients for a long time, resistance may develop.

When taken orally, imidazole and thiazole derivatives (azoles) are well absorbed by the organs of the gastrointestinal tract. They are distributed in most organs and tissues, creating high concentrations in them. Some drugs, in particular, itraconazole, penetrate into saliva, cerebrospinal fluid and intraocular fluid in extremely small quantities. The half-life of different drugs is different and varies between 8-30 hours. Reaching the liver, they undergo a number of biochemical changes in it. They are excreted mainly with feces. Fluconazole is excreted mainly through the kidneys.

Azoles for topical use when taken orally are absorbed poorly, and are effective only when applied topically. In the skin, they create high concentrations. The maximum half-life is noted for bifonazole and it is 19-32 hours. Absorbed into the bloodstream in a minimal amount.

Side effects of systemic azoles are as follows:

• nausea, vomiting, constipation or diarrhea, pain in the abdomen, cholestatic jaundice (one that is associated with stagnation of bile in the biliary tract), increased activity of liver enzymes;
• dizziness, headache, drowsiness, irritability, tremor (involuntary trembling), paresthesia (numbness), convulsions, visual disturbances;
• a decrease in the level of platelets in the blood (agranulocytosis);
• allergic reactions in the form of a skin rash, accompanied or not accompanied by itching, burning;
• peeling of the skin, contact dermatitis.

When taken intravaginally (locally - in the vagina), there may be burning, itching, swelling and redness of the vaginal mucosa, increased discharge from it, pain during intercourse, increased urination.

Clotrimazole (Canesten, Candibene, Candide, Candid-B6, Clotrimazole)

Available in the form of vaginal tablets, gels and ointments for vaginal use.

When applied intravaginally, only 5-10% of the drug is absorbed, therefore it acts only locally, and does not affect the body as a whole. The concentration necessary for the implementation of the therapeutic effect is stored in the vagina for another 3 days after the use of the drug. The part of the active substance that has been absorbed into the blood is modified in the liver and excreted in the bile.

In case of skin candidiasis, it is used in the form of gels or ointments: the drug is applied 1-3 times a day to the affected areas and rubbed into the skin for some time. The duration of treatment is from 1 week to 1 month. In the case of a fungal infection of the feet, in order to reduce the likelihood of a recurrence of the disease, treatment is extended to 3 weeks.

With urogenital candidiasis, 1 tablet per day is injected into the vagina for 7 days, plus the skin of the perineum and external genital organs are lubricated with clotrimazole cream. Alternative tablet regimens are 200 mg three days in a row or 500 mg once.

The vaginal gel is administered at bedtime deep into the vagina, 1 full applicator (which is 5 g) for 6 days.

Vaginal suppositories are administered 1 time per day at bedtime for 6 days.

Treatment of urogenital candidiasis (fungal infection of the genitourinary system) should be carried out outside of menstruation.

Clotrimazole is contraindicated in case of individual intolerance to it, as well as in the first 12-16 weeks of pregnancy.

When used simultaneously with polyenes, it reduces their effectiveness. Cannot be used with nystatin.

Econazole (Santequin, Gino-pevaril, Econazole)

Release form - pessaries, vaginal suppositories, gel and cream for external use.

When applied topically for 3 days causes the death of the fungus.

When applied to the skin creates therapeutic concentrations in the dermis and epidermis. Absorbed into the blood in a minimal amount; that part of the drug that has been absorbed is excreted in the urine and feces.

Outwardly: apply a small amount of cream or gel to the affected area of ​​the skin, rub it until completely absorbed; the multiplicity of application is 2 times a day. Duration of treatment - 14 days, in the treatment of mycosis of the feet - up to 6 weeks.

Intravaginally injected 1 time per day (before going to bed) deep into the vagina. The course of treatment is 3 days. If this is not enough, the course is continued for another 3 days and repeated after 10 days. Can be used during menstruation.

Pessaries are inserted into the posterior fornix of the vagina, 1 piece 1 time per day, in the supine position, at bedtime.

Econazole is contraindicated in case of hypersensitivity of the patient's body to it.

Use with caution in the first 12-16 weeks of pregnancy, as well as during lactation. With vulvovaginal candidiasis, simultaneous treatment of the sexual partner is mandatory.

Isoconazole (Gyno-Travogen)

Used locally. From the surface of the skin is absorbed in small quantities.

The cream is applied once a day to the affected areas of the skin for at least 4 weeks. With the localization of mycoses in the interdigital spaces after applying the cream, a gauze bandage should be applied between them.

Side effects occur quite rarely and are manifested by the occurrence of burning and itching in the first 12-24 hours after the administration of the suppository. When using the cream, allergic reactions are extremely rare, as well as skin irritation and a slight burning sensation.

Within 1 week after the introduction of the suppository, douching should not be performed.

Ketoconazole (Ketodine, Livarol, Ketoconazole)

Available in the form of vaginal suppositories, pessaries.

Applied locally.

Suppositories are injected 1 piece deep into the vagina in a squatting position or lying on your back with legs bent at the knees, before going to bed. The course of treatment is 3-5 days, but if necessary, it can be extended until the patient recovers completely. In chronic candidiasis, the course of treatment is 10 days.

Side effects are extremely rare, standard.

In the first 12-16 weeks of pregnancy, the drug is not used, in the 2nd and 3rd trimester and during lactation, it is used only after assessing the benefit for the mother-risk for the child.

Fenticonazole (Lomexin)

Release form - vaginal capsules and cream, cream for external use.

The absorption of the drug through the skin is minimal, a small amount of it is absorbed by the vaginal mucosa. Not phototoxic. Does not affect the function of the female and male gonads.

Vaginal cream is administered in the amount of 1 applicator deep into the vagina, applied before bedtime, if necessary - in the morning.

In order to prevent reinfection (re-infection), the sexual partner should also be treated with an antifungal drug.

The cream is applied to the skin 1-2 times a day, gently rubbing.

It is usually well tolerated, side effects occur only in a small proportion of patients.

Fenticonazole is not recommended during pregnancy and lactation.

Butoconazole (Ginofort)

Available in the form of a vaginal gel.

5 g of the drug (contains 100 mg of the active ingredient) is injected deep into the vagina once, preferably at bedtime.

Side effects are standard.

During pregnancy and lactation, use only on the advice of a doctor.

Release form - vaginal suppositories, cream.

Candles are administered 1 time per day, preferably at bedtime, deep into the vagina. Suppositories containing 150 mg of the active substance are administered for 6 days, 300 - 3 days, 900 mg - once. It is advisable to start the course of treatment after menstruation. During treatment and for 7 days after its completion, it is not recommended to douche.

The cream is applied in a thin layer to the affected area of ​​the skin and gently rubbed. Multiplicity of application - 1-2 times a day. The course of treatment is from 14 days to one and a half months. The drug should be used for another 7 days after the disappearance of the symptoms of the disease.

Use with caution during pregnancy and lactation.

Sertaconazole (Zalain, Zalain Ovuli)

Available in the form of a cream for external use and in the form of vaginal suppositories.

Enter 1 suppository deep into the vagina at bedtime 1 time per day once. If signs of the disease persist, you can enter again after 1 week.

The cream is applied evenly to the affected area of ​​the skin 1-2 times a day for 1 month.

Side effects are standard, rarely observed.

During the period of treatment with the drug, you should refrain from sexual intercourse, use cotton underwear, do not douche. You can carry out therapy during menstruation.

During pregnancy and lactation, the drug should be used with caution.

There are a number of combined topical preparations containing 2 or 3 antimicrobial / antifungal components at once. This:

• Klion-D 100 (vaginal tablets; contains 100 mg of miconazole and metronidazole);
• Klevazol (vaginal cream, 1 g of which contains 20 mg of clindamycin and miconazole);
• Metromicon-neo (vaginal suppositories containing 500 mg of metronidazole and 100 mg of miconazole);
• Neo-penotran (vaginal suppositories containing 750 mg of metronidazole and 200 mg of miconazole).

Fluconazole (Difluzol, Diflucan, Mikosist, Fluzamed, Fluzak, Futsis, Diflazon, Difluzol, Mikomax and others)

Release form: capsules, tablets, solution for infusions and injections, powder for suspensions, gel.

Well absorbed in the digestive tract after oral administration. Eating does not affect absorption. The maximum concentration in the blood is determined after 0.5-1.5 hours. The half-life is 30 hours.

When injected into a vein, the pharmacokinetics are similar to those when taken orally. It penetrates well into all body fluids. Excreted with urine.

It is used for candidiasis of any localization. In case of a severe course of the disease, it is administered parenterally (into the muscle) or intravenously (drip).

With disseminated (common) candidiasis, 400 mg per day are taken orally, then 200 mg per day. The duration of treatment is determined individually. The dose of the drug administered parenterally varies depending on the severity and characteristics of the course of the disease.

For vaginal candidiasis, take 150 mg of fluconazole once. In order to reduce the frequency of relapses, the drug should be taken at 150 mg every month. The duration of therapy in this case is from 4 to 12 months.

Fluconazole is contraindicated in case of hypersensitivity to it or compounds similar in chemical structure, as well as in the case of treatment with terfenadine.

Side effects are similar to those of other triazole derivatives.

If the patient shows signs of liver damage, treatment with this drug should be discontinued. Pregnant women and women during lactation should not use the drug.

Itraconazole (Funit, Eszol, Itracon, Itrungar, Mikokur, Orungal, Sporagal)

Release form: capsules, tablets, vaginal suppositories.

When taken orally, it is well absorbed. The maximum concentration in the blood is determined 3-4 hours after ingestion. Distributed in many organs and tissues of the body. Excreted with bile.

For vaginal candidiasis, 200 mg twice a day for 1 day or 200 mg 1 time per day for three days are used.

With oral candidiasis - 100 mg 1 time per day for 15 days.

With systemic candidiasis (damage by fungi of the genus Candida) - 100-200 mg 1 time per day, the course of treatment ranges from 3 weeks to 7 months.

The drug is contraindicated in case of hypersensitivity to itraconazole.

During treatment with the drug, the following side effects may occur:

• nausea, vomiting, abdominal pain, constipation, increased activity of liver enzymes, in some cases - hepatitis;
• dizziness, headache, peripheral neuropathy;
• allergic reactions.

During pregnancy and lactation, the drug is prescribed only in case of systemic mycoses.

Voriconazole (Vfend, Voritab)

Release form: tablets, powder for solution for infusion.

After oral administration, it is absorbed quickly and almost completely. The maximum concentration in the blood is determined 1-2 hours after administration. Absorption of the drug does not depend on the acidity of gastric juice. It penetrates the blood-brain barrier (the physiological barrier between the circulatory system and the brain) and is found in the cerebrospinal fluid. The elimination half-life depends on the dose and averages 6 hours.

It is used in case of severe candidal infections, with candidiasis of the esophagus.

The dosage of the drug varies widely depending on the course of the disease, age and body weight of the patient.

Contraindicated while taking certain drugs, such as terfenadine, astemizole, quinidine, rifampicin, carbamazepine, ritonavir, ergot alkaloids, as well as in case of individual intolerance to voriconazole.

Use this drug with caution in people suffering from severely impaired liver and kidney function. Treatment should be carried out under the control of indicators of liver function.

During pregnancy and lactation, the drug is not used. During the period of treatment, a woman should be reliably protected.

Posaconazole (Noxafil)

Powerful antifungal agent.

With oropharyngeal candidiasis (fungal infection of the oral cavity and pharynx), it is used in patients with reduced immunity or low efficacy of topical preparations.

On the first day of therapy, take 200 mg of the drug 1 time per day with meals, then 100 ml 1 time per day for 13 days.

Contraindications for Noxafil are similar to those for voriconazole.

During pregnancy and lactation is not used.

Dequalinium chloride (Fluomizin)

Release form - vaginal tablets.

It has a wide spectrum of antimicrobial activity, in particular, it has a negative effect on fungi of the genus Candida. The mechanism of action of this drug is to increase the permeability of the cell membrane, which leads to cell death.

When administered intravaginally, it is absorbed into the blood in a small amount.

It is used in case of vaginal candidiasis.

It is recommended that in the supine position, with legs slightly bent, insert 1 tablet deep into the vagina. The frequency of administration is 1 time per day, the duration of treatment is 6 days. Treatment with a shorter course may lead to relapse.

The drug is contraindicated in case of individual hypersensitivity to its components, in case of ulcers in the vagina and cervix, as well as in girls before reaching puberty.

Side effects are rare. In some cases, patients note burning, itching, hyperemia of the vaginal mucosa. Allergic reactions are possible.

The drug is approved for use during pregnancy and lactation. However, care should be taken when prescribing it in the 1st trimester of pregnancy.

Terbinafine (Lamisil, Mycofin, Terbizil, Terbinorm, Fungotek, Exifin and others)

Release form: tablets, cream, gel, skin spray.

In relation to Candida, it has both fungicidal (causes the death of fungi) and fungistatic (inhibits their growth) activity (depending on the type of fungus).

The drug inhibits the synthesis of ergosterol in the fungal cell, which ultimately leads to the death of its cell.

When administered orally, it accumulates in the skin, nails, hair in the concentration necessary to achieve a fungicidal effect.

Terbinafine is used for various fungal infections, in particular for candidiasis.

Cream or gel 1-2 times a day is applied to cleansed dry skin at the site of the lesion, capturing and adjacent healthy areas, lightly rubbed. The duration of treatment is approximately 7 days.

The drug is contraindicated in case of hypersensitivity to its components.

Against the background of the use of terbinafine, the following side effects may develop:

• nausea, vomiting, loss of appetite, abdominal pain, diarrhea;
• allergic reactions - skin rashes with or without itching, extremely rarely - Stevens-Johnson syndrome;
• violations of taste sensations in some cases;
• when applied topically - redness, itching or burning at the site of application.

Patients with severe liver and / or kidney disorders are recommended to prescribe a half dose of the drug.

Terbinafine should not be taken during pregnancy and lactation.

Above, you were able to get acquainted with the majority of drugs used to treat candidiasis (thrush) of various localizations. We draw your attention to the fact that you should not self-medicate, choosing a drug based on data taken on the Internet - if you have symptoms characteristic of a fungal disease, you should seek qualified medical help as soon as possible.

Which doctor to contact

For fungal infections of the skin or nails, it is best to consult a dermatologist. Candidiasis of the oral mucosa will be cured by a dentist, and vaginal - by a gynecologist. With recurrent candidiasis, consultation with an immunologist is necessary, since this disease is a frequent companion of immunodeficiencies. In case of systemic candidiasis with damage to internal organs, an infectious disease specialist or mycologist, as well as a specialized doctor, is involved in the treatment of the patient.

myfamilydoctor.com

A huge number of people suffer from fungal infections. Antifungal drugs help get rid of them - special tablets, ointments, creams, suppositories, sprays and solutions for treatment, the action of which is aimed at destroying pathogens and preventing their reproduction. Now there are a huge number of such funds on the market. Not a single person is immune from damage by different types of fungi, so everyone should know what antimycotic drugs exist.

What are antifungal drugs

This is the name of all drugs that exhibit specific activity against pathogenic fungi, suppressing their activity and destroying them. Antifungal agents are divided into different groups according to the structure of the chemical compound and the spectrum of activity. May contain both natural and chemical ingredients. Available in the form of tablets, ointments, creams, suppositories, sprays. The action of drugs is aimed at destroying pathogens without causing harm to the patient.

The use of antifungal drugs

There are a huge number of types of mycoses. They can affect the skin, nails, mucous membranes. Antifungal drugs are designed specifically to destroy the pathogens of the fungus, to stop its negative impact on the human body. List of the most common mycotic diseases:

• candidiasis;
• pityriasis versicolor;
• cryptococcal meningitis;
• pseudoallescheriosis;
• ringworm;
• dermatomycosis;
• lesions of the nail plates, skin;
• aspergillosis;
• candidal and trichomonas vulvovaginitis;
• sporotrichosis;
• fusarium.

Kinds

There are many types of antifungal drugs. They are divided into groups according to:

• origin (synthetic, natural);
• method of application (internal, external, parenteral);
• mechanism and spectrum of action;
• indications for use (systemic or local infections);
• effect of exposure (fungistatic, fungicidal);
• activity level (broad and narrow spectrum).

Ointments

Local preparations of this type are prescribed, as a rule, in the initial stages of mycotic diseases. Antifungal ointments fight the infection caused by the pathogen, relieve unpleasant symptoms. The advantages of their use:

• a wide range of antifungal agents, both at affordable prices and more expensive;
• ease of use;
• the possibility of acquiring without a doctor's prescription (in most cases).

There are certain groups of ointments according to the area of ​​​​application. General medicines:

1. Zalain. Ointment with sertaconazole. Prevents the spread of pathogens. The course of treatment is a month.
2. Exoderil. Effective ointment, the substances of which do not penetrate into the blood. It cures the fungus in one to two months, but can cause side effects: allergic reactions, headache, bloating, diarrhea, hives, nausea, vomiting.
3. Candide. Suitable for any area of ​​the skin. Can be used during pregnancy, lactation. Treatment course, lasts up to six months. Contraindicated in case of individual intolerance to the components.
4. Salicylic ointment. Suitable for treating affected skin areas and applying compresses.
5. Ketoconazole. The drug is effective against many fungi, but dangerous because of its toxicity.
6. Mycosan. Contains ketoconazole. Very quickly relieves itching, and the rest of the symptom in about a month.
7. Zinc ointment. The drug has no side effects. It is used until the symptoms of the fungus are completely eliminated.
8. Lamisil. Contains terbinafine. Eliminates the symptoms of the fungus in a month.

There are a number of drugs in the form of ointments that are designed to treat mycosis in the intimate area:

1. Clotrimazole. This ointment is allowed to be applied not only to the skin, but also to the mucous membranes. The course of treatment is a maximum of 1 month.
2. Nitrofungin. Ointment with chlornitrophenol, which inhibits the growth of the fungus and has an antiseptic effect.
3. Ketoconazole. It is applied to skin and mucous membranes. The course of treatment is 2-4 weeks.

Pills

Mycosis, especially in advanced stages, will not go away without systemic treatment. Pills for fungal diseases can destroy the pathogen or block its action, so they are more effective than any local drugs. Such funds are allowed to be taken only as directed by a doctor and at the same time strictly follow his instructions, because they have many contraindications and side effects. The list of drugs in tablets is very wide, so it is most convenient to divide them into groups according to the active substance.

1. with ketoconazole. Prevents the growth of fungi. Antimycotic drugs with this active substance in the composition: Nizoral, Ketozol, Dermazol, Ketozoral, Ketoconazole, Mycozoral.
2. with itraconazole. This substance is especially effective against dermatophytes, molds and yeasts. It contains such tablets: Itraconazole, Itrungar, Orungal, Sporagal, Itracon, Eszol, Isol.
3. with terbinafine. A substance that disrupts the viability of a fungus. Taking drugs with it is effective for dermatomycosis of any part of the body. It is a part of such tablets: Lamisil, Binafin, Terbinafine, Lamikon.
4. with fluconazole. The substance is a derivative of triazole with a pronounced antifungal effect. Fluconazole tablets are especially effective against yeast fungi. Suitable for the treatment of onychomycosis, candidiasis of the mucous membranes. The list of tablets with this substance: Fluzon, Fluconazole, Medoflucon, Futsis, Mikosist, Difluzol, Diflucan.
5. Griseofulvin. Tablets have the same name as the main active ingredient in their composition. The systemic drug is effective against trichophytons, microsporums, epidermophytons. Suppresses the process of cell division of the fungus. Contraindicated in pathologies of the heart, renal failure, disorders of the nervous system.

Creams

Preparations in this form of release have a local effect. Creams differ from ointments in that they contain less fat in the composition. They are quickly absorbed and soften the skin. List of effective antifungal creams:

1. Nizoral.
2. Tinedol. Contains climbazole and many excipients. Restores skin cells, heals, disinfects. Suitable for the treatment of fungus and prevention.
3. Microspore.
4. Terbinafine. Helps with fungal infections of the feet, skin, mucous membranes, nails. Apply a thin layer to the infected area. The duration of treatment, depending on the severity of the lesion, can range from several weeks to six months.
5. Lamisil.
6. Naftifin. Effective for inguinal epidermophytosis, onychomycosis, candidiasis.
7. Ketoconazole.
8. Clotrimazole. Helps against mold, yeast fungi, dermatophytes. It is not recommended for use during pregnancy and in case of hypersensitivity to the components. Cream treatment is a month and a half.
9. Lotseril.

Capsules

Preparations released in this form practically do not differ in the principle of action from tablets. What antifungal capsules exist:

• Fluconazole;
• Orungal;
• Rumikoz;
• Itrazol;
• Irunin;
• Diflazon;
• Diflucan;
• Mycomax;
• Mycosist;
• Flucostat;
• Forkan.

Candles

Preparations in this form are prescribed to women from thrush. The disease is caused by yeast-like fungi. Its symptoms appear in the intimate area. Vaginal (in rare cases, rectal) suppositories help to get rid of them as quickly as possible. They are made from medicinal and additional components that allow suppositories to remain solid at room temperature. Suppositories are convenient to use. They act locally and do not harm the kidneys, liver, organs of the digestive system.

List of the most effective candles:

• Pimafucin;
• Zalain;
• Livarol;
• Ginezol 7;
• Guino-Pevaril;
• Hexicon;
• Betadine;
• Metronidazole;
• Osarbon;
• Nystatin;
• Gino-Dactanol;
• Ketoconazole;
• Viferon;
• Klion-D;
• Terzhinan;
• Polygynax;
• Lomeksin.

Classification

There are many features by which antimycotic drugs are categorized. It is more common to combine them by chemical group and pharmacological activity. This classification helps the specialist to choose and recommend to the patient the drug that will be most effective in treating the diagnosed type of fungus. Allocate antifungal agents of a wide and narrow spectrum of action.

Azole group

Synthetic antifungal agents that have fungicidal and fungistatic effects. They help in the treatment of mycoses of the skin, nails, mucous membranes, scalp. Group representatives:

1. Ketoconazole (analogues of Fungavis, Oronazole, Nizoral, Mycozoral). Effective against yeast-like, dimorphic, higher fungi, dermatophytes.
2. Voriconazole (Vfend, Biflurin, Vikand). Drugs effective for candidiasis, versicolor, aspergillosis, deep subcutaneous mycoses.
3. Itraconazole (Irunin, Orunit, Itrazol, Rumikoz, Itrazol, Orungal, Kanditral). They are prescribed for severe lesions of mold, candida fungi.
4. Fluconazole (Diflucan, Mikoflucan, Medoflucon, Mikosist, Diflazon, Mikoflucan, Mykosist, Mikomax). Drugs that inhibit the growth and reproduction of fungi.

Polyene antibiotics

This group of drugs has the widest spectrum of action. They are prescribed to patients who have a weakened immune system. Representatives:

1. Nystatin. Effective against candidiasis of the skin, oral cavity and pharynx, intestines.
2. Levorin. A drug with a wide range of indications, especially effective against candidiasis and protozoan fungi.
3. Pimafucin. A drug that has a fungicidal effect on molds and pathogenic yeast fungi.
4. Amphotericin B (Ambizom, Fungizone, Amphoglucamine, Ampholip, Amphocil). It is used for progressive fungal infections that pose a serious threat to life.

Allylamine group

Synthetic antifungal agents effective against dermatomycosis affecting nails, hair, skin. Allylamine group drugs:

1. Terbinafine (Lamisil, Terbinox, Bramisil, Terbizil, Exitern). It is effective in dermatomycoses that have affected areas of the body that are significant in size.
2. Naftifin (Exoderil). Effective in fungal diseases of nails and skin caused by sensitive pathogens.

Antifungals for children

The child's body is at an increased risk of mycotic lesions because their immune system is still defective. However, not all drugs are suitable for the treatment of pediatric patients. If the child has become infected, then the doctor should select the antifungal medicine for him, determining the type of pathogen and conducting additional diagnostics. What drugs can be prescribed to children:

1. Local. Mycosan, Nystatin, Amorolfine, Lamisil.
2. Systemic. Griseofulfin, Mikoseptin, Flucytosine, Terbinafine, Flucytosine, Fluconazole.

Broad Spectrum Antifungals

Such drugs have both fungicidal and fungistatic effects. They prevent the reproduction of the fungus and destroy existing pathogens. Depending on the active substance, each drug works in its own way:

1. Ketoconazole (Oronazol, Fungavis, Mycozoral). Interferes with synthesis of components of a cellular membrane of a fungus.
2. Griseofulvin. Prevents the division of fungal cells.
3. Itraconazole (Irunin, Orunit, Orungal). Prevents the formation of ergosterol (a component of a fungal cell).
4. Terbinafine. Prevents the synthesis of ergosterol at the initial stage.
5. Fluconazole (Diflucan, Fluxstat, Mycomax). Prevents the formation of new spores and eliminates existing ones.

How to choose

If you find a fungus, then the most reasonable thing to do would be to consult a dermatologist. The specialist will determine the type of pathogen, assess the degree of damage and the general condition of the body. After analyzing the data, he will develop a therapy strategy, recommend you the most effective and safe drugs. Self-medication can not only not give a positive effect, but also harm your body.

Price

You can order drugs in an ordinary pharmacy, buy in an online store, choosing the option that suits you in the catalog. The price depends on a wide range of factors. The approximate cost of some drugs can be found in the table below:

Name of the antifungal drug

Approximate price in rubles Video

20.06.2017

Product characteristics

Release form: Capsules, vaginal suppositories, ointment

Indications for use:Fungus of various types

Side effects:Disorder of the gastrointestinal tract and nervous system

Contraindications:Individual intolerance

Price: 350-450 rubles

One of the effective antimycotic agents is Itraconazole. It is a synthetic drug with the active substance a derivative of triazole. Allows you to cope with various types of fungi. Itraconazole capsules are easy to use and allow the drug to be almost completely absorbed when taken orally. If necessary, an ointment is prescribed for external use.

Indications and contraindications

This remedy is prescribed for various mycoses that spread to the skin, mucous membranes or nails. These can be diseases localized on the mucous membranes of the oral cavity, genital organs, systemic processes, pityriasis versicolor and some others.

Treatment makes sense only when the fungal nature of the disease is established, therefore it is not worth prescribing Itraconazole to yourself without consulting a doctor and certain studies.

Like any drug, this drug has certain contraindications. The main one is individual intolerance. The instructions for use of Itraconazole also indicate that contraindications are periods of childbearing and breastfeeding.

This drug has a negative effect on the development of the fetus during pregnancy, therefore, if it is prescribed to a woman of childbearing age, she needs to be protected and prevent pregnancy for some time after the end of therapy.

Itraconazole capsules should be used with caution in the following conditions:

• chronic renal failure;
• cirrhosis of the liver;
• children and old age;
• heart failure.

Forms of release and action of the drug

Forms of release of Itraconazole - capsules, vaginal tablets, suppositories, ointment. Each form has its own range of applications.

Capsules and tablets Itraconazole

The mechanism of action of this drug is based on the inhibition of the production of ergosterol, which is an important component of the cell membrane of pathogens of fungal diseases. In simple terms, the active substance prevents the development of fungi, and they die. Clinical results begin to appear after some time, some earlier, some later, depending on the individual response. In the treatment of mycosis of the nails on the legs and hands, the final results can be seen only after a complete change of the affected nails, that is, after about six months.

What conditions are treated with Itraconazole?

1. vulvovaginal candidiasis;
2. systemic mycoses;
3. pityriasis versicolor;
4. onychomycosis, which you can read more about;
5. dermatomycosis;
6. cryptococcosis;
7. histoplasmosis;
8. sporotrichosis;
9. blastomycosis.

Dose, frequency of administration and duration of treatment depend on the type of disease. Usually Itraconazole is prescribed 100-200 mg in one or two doses. Treatment can last only three days with vulvovaginal candidiasis, that is, with thrush. With pityriasis versicolor, it lasts a week, for therapy and candidiasis of the oral mucosa it takes 15 days, onychomycosis is treated for 3 months, and aspergillosis - 5. With systemic candidiasis, the course of treatment can range from three weeks to seven months.

With mycosis of the nails, repeated treatment will be required to obtain a lasting effect. If mycosis has spread only to the nail plates of the hands, then two courses per week of taking the drug with a three-week break are needed. With mycosis of the toenails, three such courses are required.

Itraconazole is taken in the prescribed dose after a meal, it is desirable that it was not just a snack, but a normal solid meal. It is very important to clearly maintain the dosage, frequency and duration of treatment. If you do not follow the doctor's recommendations, then the development of mycosis can go in a new circle, and therapy will have to be started anew.

When treating with Itraconazole, side effects are possible, which can manifest themselves in varying degrees. If they are, it is worth informing your doctor about this, because in some cases it is necessary to cancel the drug or replace it with a drug with another active substance. Side effects can occur from the gastrointestinal tract, the nervous system, various manifestations of allergies are likely.

Possible negative reactions

• violation of the digestive tract;
• stomach ache;
• dizziness;
• headache;
• allergic manifestations from the skin;
• puffiness;
• disruption of the menstrual cycle.

Candles Itraconazole

Indications for the use of candles - genital candidiasis. This remedy is effective in both chronic and recurrent forms of the disease. In mild forms, you can limit yourself to using only one suppository at night for 1-3 days. However, in more severe cases, suppository therapy is additional and should be combined with oral tablets or capsules. Candles are prescribed one at a time for six days. In this case, it is necessary to take Itraconazole orally 200 mg once.

Recurrent forms of genital candidiasis are associated with a decrease in immunity, therefore, along with treatment, it is necessary to take measures to strengthen the body's defenses. In some forms of genital candidiasis, exacerbations can occur at the beginning of the menstrual cycle. To prevent them, one dose (200 mg) of Itraconazole is prescribed on the first day of the cycle.

Since suppositories are a topical agent, the active substance practically does not penetrate into the systemic circulation. For this reason, it is safer than capsules or tablets, side effects are only local manifestation.

Possible negative reactions

1. Itching and a slight burning sensation immediately after the introduction of the candle.
2. Local allergic reactions.
3. During menstruation, candle treatment is interrupted, continuing or replacing it with tablets or capsules.

Ointment Itraconazole

Itraconazole ointment or cream is applied topically to the affected areas. It is prescribed for pityriasis versicolor, ringworm of various parts of the body, trichophytosis, erythrasma. If mycosis has extensive localization, as well as with onychomycosis, oral administration of the drug is usually indicated, since it is more effective.

Local treatment with Itraconazole can cause discomfort such as itching and burning at the site of application. Other negative reactions, as a rule, are not observed.

The cost of the drug and its analogues

Today, pharmacology offers us several analogues of Itraconazole. Some have the same active ingredient, others have the same antifungal effect, but their composition is different, and the main component is a different substance. There are analogues cheaper than Itraconazole, there are more expensive ones. The price depends on the form of release and the volume of packaging. For example, a package of 14 capsules of this drug will cost 350-450 rubles, depending on which city and pharmacy to buy it in.

What are analogues for? Thanks to them, you can choose a drug that will have the maximum effect with minimal negative consequences or without them at all.

Almost identical in composition and has the same active substance Orungal. The main component is itraconazole, Orungal also contains excipients: sucrose, hypromellose, macrogol. This drug is the most expensive of all analogues. Its cost per pack of 14 capsules is about 2500-3000 rubles. Itrazol

Interaction with other drugs

In the treatment of mycoses with drugs containing itraconazole, it is necessary to take into account their compatibility and interaction with other drugs. General recommendation: do not combine treatment with these drugs with any medication, because the likelihood of negative side effects increases. For example, erythromycin increases the bioavailability of antimycotic agents, that is, enhances their systemic effects on the body. With the simultaneous use of hydrocortisone, the effect of both this hormonal drug and Itraconazole increases several times, and this can be dangerous. All antifungal drugs linger in the body for a long time, this should also be taken into account when prescribing other drugs.