Antifungal drugs for the treatment of onychomycosis

There are no pathogenic fungi in the natural microbiota of humans and animals. Fungi are eukaryotes that lack chlorophyll and cannot perform photosynthesis. Most fungi are environmental saprophytes (heterotrophic bacteria) and need to be fed with readily available organic materials. The body of a fungus is represented by mycelium-a network of subdivided tubular filaments called hyphae. Mushrooms reproduce through spores. Entering the tissues of susceptible hosts during accidental inoculation, fungi can cause various diseases of the skin, mucous membranes, and internal organs in its beneficial nutritional matrix. Fungal diseases are called fungal diseases (from Greek. Mykes-fungus).

Healthy and fungal nails

The pathogens of fungal diseases are parasitic microscopic fungi of the following genera: Arthroderma, Aspergillus, Amanita, Microsporum, Penicillium, Candida, Saccharomyces, Trichophyton, EpidermophytosisWait. , Muscles, bones, internal organs and nervous system. Actinomycosis is a serious disease caused by actinomycetes and radiation fungi. Blastomycosis is a deep skin mycosis. The pathogen is a pathogenic dimorphic fungus. Other diseases are also deep (visceral) fungal diseases. Superficial mycosis affects the stratum corneum, scalp, nail plate and mucous membranes.

The most common corneal mycosis affects only the stratum corneum; dermatomycosis affects smooth skin, epidermis and appendages: hair and nails.

According to the type of pathogenic fungus and the location of the pathological process, there are:

  • Epidermophytosis-fungal disease of groin folds, calf, interdigital folds, brush skin;
  • tricomycosis (from the Greek trichos-hair)-damaged scalp, vellus hair on the body;
  • Trichophytonosis (tinea), microsporum, favus (scab);
  • Onychomycosis (from the Greek word onychos-nail)-the nail plate on the hands or feet is damaged by dermatophytes (less mold or yeast).

For diseases caused by various pathogenic or opportunistic fungi, antifungal drugs are used. According to the location of pathogenic fungi, antifungal drugs are divided into therapeutic drugs:

  • Systemic mycosis;
  • Candidiasis;
  • Superficial fungal disease.

The chemical classification divides antifungal drugs into:

antibiotic:

  • Polyene antibiotics (amphotericin B, dimeglumine, natamycin, nystatin);
  • Non-polyene antibiotics (Greroslavin);

Synthetic drugs:

  • Imidazole derivatives (bifonazole, isoconazole, ketoconazole, clotrimazole, miconazole, oxyconazole, oconazole, sertaconazole);
  • Triazole derivatives (Itraconazole, Fluconazole, Reconazole, Sulconazole);
  • Allylamine derivatives (terbinafine, naftifine);
  • Morpholine derivative (Amorolfine);
  • Derivatives of different chemical groups: undecylenic acid ciclopirox, flucytosine, potassium iodide, etc.

Onychomycosis

Onychomycosis is caused by an infection of the nail plate. Most infections occur in public baths, saunas, and swimming pools. The scales contain fungal spores and mycelium, which fall off on onychomycosis patients and fall on floors, benches, trellises, paths, carpets, and bedding. Under high humidity conditions, mushrooms can not only survive for a long time (several years), but can also reproduce, which makes them a strong source of infection. A person who moves barefoot on the floor or touches household items with such scales is likely to be infected because they stick to his skin and are fixed. Infection occurs after fungus invades the nail structure. In the future, they will start to activate, multiply and form tunnels and passages. When affected, nails thicken, chip, turn yellow and break. Sometimes, the process can also affect the skin and is accompanied by an itchy flaky rash in the area between the fingers. This type of disease is characterized by a long and continuous course.

Due to the existence of chronic diseases such as vegetative vascular disease, diabetes, peripheral circulation disorders, and foot osteoarthropathy, the possibility of infection susceptibility increases with age, especially for the elderly over 65. Nail board.

The treatment of onychomycosis is carried out in strict accordance with a certain plan for a long time-from 2 to 4 months. In the treatment, antifungal agents are used, which have antibacterial and fungicidal effects and affect the life activities and metabolism of pathogens at various stages. The antifungal effects of antifungal drugs mainly have the following three mechanisms, and the results show their activity:

  • Violation of the structure and function of fungal cell walls (imidazole, triazole);
  • Disrupt the mitosis of eukaryotic cells by inhibiting the synthesis of nucleic acid (griseofulvin);
  • Inhibits the process of transmembrane exchange through fungal (ciclopirox) cell membranes.

First choice drug

Griseofulvin(Greroslavin) label. 125mg is an antibiotic produced by the black mold Penicillium (Grerospora). It was isolated in 1939 and is structurally a spiro derivative of benzofuran. The drug has antibacterial properties against all types of fungi-Trichophyton and Epidermophyton. The antibacterial action mechanism is based on the ability of the drug to inhibit the cell division of filamentous fungi in the metaphase, causing characteristic morphological changes (hyphae distortion, branching increase and bending), destroying the structure of the mitotic spindle and cell wall synthesis. The drug inhibits the synthesis and polymerization of nucleic acids to a lesser extent. The drug has no antibacterial activity.

To produce a sufficient concentration of the drug in the skin requires long-term treatment-2-3 months and minutes. Only on new, regenerated nails will the initial symptoms of the treatment effect become apparent.

important! Side effects when taking the drug include: indigestion, dizziness, sometimes insomnia, allergic reactions, and leukopenia. Griseofulvin is contraindicated in inhibiting hematopoietic function, liver and kidney failure, infants and pregnant women. You should not prescribe this medicine to drivers, people who work at high altitudes, or people who need more attention, quick mental and exercise reactions. Patients should be warned of possible cross-sensitivity to penicillin and increased effects of alcohol.

Ketoconazole(Ketoconazole)-an active broad-spectrum drug from the imidazole class with fungicidal and antifungal activity; effective when taken orally for systemic and superficial mycoses, dermatophytes and candidiasis. It is prescribed by a doctor to treat and prevent fungal infections of the skin, hair, nails, and genitals caused by drug-sensitive pathogens.

When administered orally, the drug is well absorbed, dissolved and absorbed in an acidic environment.

important! The drug is well tolerated by patients, but can cause indigestion symptoms (nausea, vomiting, diarrhea), urticaria and rash, headache, dizziness, gynecomastia, impotence and other allergic reactions rarely occur. With the simultaneous use of this drug with other drugs (fentanyl, tamsulosin, carbamazepine, salmeterol, etc. ), the concentration of the latter may increase as side effects increase.

Severe liver, kidney, pregnancy, breastfeeding, and drug allergies are prohibited.

Ketoconazole is provided in the table. 200 mg suppository. 400 mg; 2% ointment, 15 mg; cream 20 mg/g-15 g. It is used in the form of shampoo. The duration of treatment is determined individually.

Itraconazole(Itraconazole) cap. 100 mg; solution 10 mg/ml-150 ml vial-The drug has a wide range of effects, selectively and specifically inhibiting the enzyme that catalyzes the synthesis of fungal sterols. Scope of application: various infections caused by dermatophytes and/or yeasts and molds, such as mucosal (including vagina) candidiasis, dermatomycosis, onychomycosis, epidermal mycosis, ocular mycosis (keratitis), Peritoneum and other parts. Taking itraconazole capsules immediately after meals can increase its bioavailability; the maximum concentration in plasma is reached within 3-4 hours. After ingestion. The drug is well distributed in tissues susceptible to fungal infections.

important! When using the drug, there may be side effects of the digestive system: indigestion (nausea, vomiting, diarrhea, constipation, loss of appetite), abdominal pain, impaired taste; headache, dizziness, allergic reactions, hair loss, from the blood-forming organs (rarely)-Leukopenia, thrombocytopenia. If you are allergic to itraconazole and any component of the drug, children under 3 years of age, pregnancy and lactation, this use is contraindicated.

For the best absorption of the drug, it is necessary to take the capsule without chewing and swallow the entire capsule immediately after a meal. A course of pulse therapy for onychomycosis involves taking 2 capsules per day. This medicine is given twice a day for a week. For the treatment of fungal infections of the finger nail plate, two courses of treatment are recommended. For the treatment of fungal infections of the nail plates of the feet, three courses are recommended. You do not need to take medication at the interval of 3 weeks.

Terbinafine(Terbinafine)-Produced in the following form: label. 250 mg; 1% ointment 15. 0 g; 1% cream-10, 15, 30 g tubes; 1% spray, 20 ml. The drug is called allylamine and is used for systemic and topical use. The mechanism of action of terbinafine is related to the inhibition of the initial stage of the biosynthesis of ergosterol (the main cytosterol of fungal membranes) by inhibiting the specific enzyme squalene-2, 3-epoxidase on fungal membranes. The drug is effective against many fungi that are pathogenic to humans. For topical treatment, terbinafine is more effective than azole drugs and imidazole derivatives, but comparable to itraconazole, and more effective than griseofulvin and itraconazole when taken orally. Terbinafine is characterized by lipophilicity, which rapidly spreads to the stratum corneum of the epidermis, dermis, and subcutaneous tissues, and accumulates in the sebaceous glands, hair follicles and nail plates to provide fungicidal concentration. 1 label. Compared with intermittent endoconazole treatment, terbinafine once a day has a higher cure rate and better results in each efficacy standard (including mycological cure).

Naftifine(Naffine) Cream 1%-15, 30 g; 10, 20, 30 ml of 1% solution, which is a derivative of allylamine. The mechanism of action is related to inhibiting the activity of squalene-2, 3-epoxidase and inhibiting the biosynthesis of ergosterol, which leads to the destruction of cell wall synthesis. Naftifine has a broad spectrum of action against dermatophytes (such as Trichophyton, Epidermophyton, Microsporum), molds (Aspergillus), yeast-like fungi (Candida, Pityrosporum) and other fungi (such as Sphenor scorotrichosis)) Has a bactericidal effect. . . . The drug has an anti-inflammatory effect and reduces itching. When used externally, it can penetrate well into the skin and produce a stable antifungal concentration in its various layers.

The duration of treatment with Naftifin ranges from 2 weeks to 6 months. When using the drug, the skin is dry and red, and a burning sensation may occur. All these side effects are reversible and do not need to be cancelled.

Amorolfine(Amorolfine) nail polish 5%-2. 5 and 5 ml, -topical preparation, has a wide range of effects, due to its inhibitory effect, destroys the cytoplasmic membrane of fungi by disrupting sterol biosynthesis, thereby providing antibacterial and fungicidal enzymes 14-γ Demethylase and 7 γ isomerase. The drug is active against the most common and rare pathogens of dermatophytes nail fungal infections: Trichophyton, Microsporum, Epidermophyton; molds: Alternaria spp. , Scopulariopsis spp. , Hendersonula sppi. ; from DematiaceaeFungi of the family: Cladopsorium spp. , Fonsecaea, Wangiella; biphasic fungi, Coccidioides, Histoplasma, and Sporothrix.

When applied to the nail, the drug penetrates the nail plate and further penetrates into the nail bed, almost completely infiltrating within the first 24 hours. The effective concentration remains in the affected nail plate for 7-10 days. After the first application. Systemic absorption is negligible. It is for external use. The drug is used on damaged fingers or toenails 1-2 times a week. The duration of treatment is determined individually and depends on the indication used. Side effects are rare and appear in the form of itching, burning at the application site. Not suitable for toddlers and babies.

Undecylenic acidIts salt-an antifungal drug for external use, has antibacterial and fungicidal effects on dermatophytes. When combined with zinc or copper salts-zinc undecylenate or copper undecylenate-its activity increases. Zinc is part of the medicine and has an astringent effect, reducing the appearance of skin irritation and promoting faster healing.

  • Undecylenic acid + zinc undecylenate (TN, ointment 30 g tube, ointment 25 g bottle);
  • Undecylenic acid + copper undecylenate + HCV glycerin-used to treat and prevent fungal skin diseases caused by drug-sensitive fungi (dermatophytes).

Apply the preparation to the clean, dry surface of the affected skin twice a day (morning and evening). The duration of the treatment course is 4-6 weeks, depending on the nature, effectiveness and duration of the disease. After the clinical symptoms of the disease disappear, continue to use it once a day. For prevention purposes-2 times a week.

important! The contraindication for the use of the drug is allergy to undecylenic acid and its derivatives.

Ciclopirox(Ciclopirox) nail polish 8%, Florida. 3g is a broad-spectrum antifungal drug that can inhibit the capture of precursors used to synthesize macromolecules in cell membranes. External use is used to treat and prevent fungal infections of the skin, mucous membranes, nails, fungal vaginitis and vulvovaginitis.

The drug should be applied to the affected nail 1-2 times a day. The duration of use depends on the severity of the lesion, but should not exceed 6 months.

The treatment of onychomycosis should be carried out under the strict supervision of a dermatologist. Usually, use reasonable symptomatic compound therapy. The reduction or disappearance of clinical symptoms is usually observed a few days after taking antifungal drugs. However, in order to avoid the recurrence of the disease, the treatment process should be carried out thoroughly. In the context of clinical cure, anti-relapse treatment is often performed to prevent re-infection.