Antimycotics for the treatment of onychomycosis

In the natural microflora of humans and animals, pathogenic fungi are not present. Fungi are eukaryotes without chlorophyll and incapable of photosynthesis. Most fungi are saprophytes of the environment (heterotrophs) and need to be fed ready-made organic substances. The body of the fungus is represented by the mycelium - a network of thin, branched tubular filaments called hyphae. Mushrooms multiply by spores. Entering the tissues of a susceptible host during accidental inoculation, onto their favorable nutrient substrates, fungi can cause various diseases of the skin, mucous membranes, and internal organs. Fungal diseases are called mycoses (from the Greek. Mykes - fungus).

healthy and fungal nail

The causative agents of mycoses are microscopic parasitic fungi of the genus: Arthroderma, Aspergillus, Amanita, Microsporum, Penicillium, Candida, Saccharomyces, Trichophyton, Epidermophyton, etc. Systemic mycoses of internal organs are very difficult and can affect, in addition to the skin, muscles, bones, internal organs and the nervous system. Actinomycosis is a serious disease caused by actinomycetes radiating fungi, blastomycosis is a deep skin mycosis, the causative agent is a pathogenic dimorphic fungus. Other diseases also belong to deep (visceral) mycoses. Superficial mycoses affect the stratum corneum, scalp, nail plates and mucous membranes.

The most common keratomicosis, which affects only the stratum corneum; dermatomycoses affect smooth skin, the epidermis and its attachments: hair, nails.

Depending on the type of pathogenic fungus and the location of the pathological process, there are:

  • epidermophytosis - skin mycoses of the inguinal folds, leg, interdigital folds, brushes;
  • trichomycosis (Greek trichos - hair) - damage to the scalp, vellum hair on the body;
  • trichophytosis (mycosis), microsporia, favirus (crust);
  • onychomycosis (Greek onico - nail) - lesion of the nail plates on the hands or feet with dermatophytes (less often mold or yeast).

For diseases caused by various types of pathogenic or opportunistic fungi, antifungal medications are used. Depending on the location of the pathogenic fungi, antifungals are classified into drugs for treatment:

  • systemic mycoses;
  • candidiasis;
  • superficial mycoses.

The chemical classification divides antifungal drugs into:

antibiotics:

  • polyene antibiotics (amphotericin B, amphoglucamine, natamycin, nystatin);
  • non-polyenic antibiotics (griseofulvin);

synthetic drugs:

  • imidazole derivatives (bifonazole, isoconazole, ketoconazole, clotrimazole, miconazole, oxiconazole, omoconazole, sertaconazole);
  • triazole derivatives (itraconazole, fluconazole, thermoconazole, tioconazole);
  • allylamine derivatives (terbinafine, naphthyfine);
  • morpholine derivatives (amorolphine);
  • derivatives of different chemical groups: undecylenic acid, ciclopirox, flucytosine, potassium iodide, etc.

onychomycosis

Onychomycosis is caused by infection of the nail plate. Most of the infection occurs in public baths, saunas, swimming pools. The scales, which contain fungal spores and mycelium, falling on patients with onychomycosis, fall to the floor, countertops, trellises, paths, rugs and sheets. In conditions of high humidity, mushrooms can not only persist for a long time (years) but also multiply, making them an intense source of infection. A person who moves on the floor in bare feet or touches household items with such scales may well become infected because they stick to their skin and are fixed. The infection develops after the fungus penetrates the nail structures. In the future, they start to activate, multiply and form tunnels, passages. When affected, the nails thicken, crumble, turn yellow and break. Sometimes the process also affects the skin, which is accompanied by itchy, scaly rashes in the interdigital area. These diseases are characterized by a long and persistent course.

The probability of susceptibility to infection increases with age, especially in the elderly over 65 years, due to the presence of chronic diseases such as vegetative-vascular pathology, diabetes mellitus, peripheral circulatory disorders, foot osteoarthropathy, etc. Nail boards.

Treatment of onychomycosis is carried out strictly according to a certain scheme for a long period - from 2 to 4 months. In therapy, antimycotics are used, which have a fungistatic and fungicidal effect and affect various stages of the vital activity and metabolism of pathogens. There are three main mechanisms of antimycotic action of antifungals, which manifest their activity as a result:

  • violations of fungal cell wall structure and function (imidazoles, triazoles);
  • violation of eukaryotic cell mitosis, by inhibiting the synthesis of nucleic acids (griseofulvin);
  • inhibition of transmembrane exchange processes across the fungal cell membrane (ciclopirox).

drugs of choice

griseofulvinGuide (Griseofulvinum). 125 mg is an antibiotic produced by the fungus Penicillium nigricans (griseofulvum), was isolated in 1939 and is a spiro derived from benzofuran in structure. The drug has fungistatic properties against all types of fungi - trichophytes and epidermophytes. The fungistatic mechanism of action is based on the drug's ability to inhibit cell division of filamentous fungi in metaphase, causing characteristic morphological changes (torsion, increased branching and curvature of the hyphae), disorganizing the structure of the mitotic spindle and cell wall synthesis . To a small extent, the drug inhibits the synthesis and polymerization of nucleic acids. The drug has no antibacterial activity.

To create a sufficient concentration of the drug in the skin, a long-term treatment is needed - 2-3 months min. Only in new and grown nails will the first symptoms of the treatment's effectiveness be noticeable.

Important! Side effects when taking the drug include: dyspeptic disorders, dizziness, sometimes insomnia, allergic reactions, leukopenia. Griseofulvin is contraindicated in suppressing hematopoiesis, hepatic and renal failure, as well as in children and pregnant women. You should not prescribe the drug to transport drivers, people involved in work at high altitudes or who require greater attention, rapid mental and motor reactions. Patients should be made aware of the development of possible cross-sensitivity to penicillin and the increased effect of alcohol.

Ketoconazole(Ketoconazole) - a broad spectrum active drug of the imidazole group with fungicidal and fungistatic activity; effective when taken orally with systemic and superficial mycoses, dermatomycosis and candidiasis. It is prescribed by a physician for the treatment and prevention of 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 dyspeptic symptoms (nausea, vomiting, diarrhea), very rarely allergic reactions in the form of urticaria and rash, headache, dizziness, gynecomastia, impotence. With the simultaneous use of the drug with other drugs (fentanyl, tamsulosin, carbamazepine, salmeterol, etc. ), its concentration may increase with the increase of side effects.

Contraindicated in severe cases of liver, kidney, pregnancy, breastfeeding and drug hypersensitivity.

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

itraconazole(Itraconazole) caps. 100mg; 10 mg / ml solution - 150 ml bottle - the drug has a broad spectrum of action, selectively and specifically inhibiting the enzyme that catalyzes the synthesis of fungal sterols. Scope: Various infections caused by dermatophytes and/or fungal and yeast fungi, such as candidiasis of the mucous membranes (including the vagina), skin mycoses, onychomycosis, epidermomycosis, fungal lesions of the eyes (keratitis), peritoneum and other locations. Taking itraconazole capsules immediately after meals increases their bioavailability; the maximum concentration in blood 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, digestive system side effects may occur: dyspepsia (nausea, vomiting, diarrhea, constipation, loss of appetite), abdominal pain, impaired taste; headache, dizziness, allergic reactions, alopecia, of Organs hematopoietic organs (rarely) - leucopenia, thrombocytopenia. Use is contraindicated in case of hypersensitivity to itraconazole and any of the drug's components, children under 3 years of age, pregnancy and lactation.

For optimal absorption of the drug, it is necessary to take the capsules without chewing, immediately after a meal, to swallow them whole. A course of pulse therapy for onychomycosis consists of a daily intake of 2 capsules. the drug twice a day for a week. For the treatment of fungal infections of the nail plates on the hands, two courses are recommended. For the treatment of fungal infections of the nail plates of the feet, three courses are recommended. The interval between courses, during which you do not need to take the medication, is 3 weeks.

terbinafine(Terbinafine) - produced in the form: tab. 250mg; 1% ointment 15. 0 g; 1% cream - 10, 15, 30 g tube; 1% spray, 20 ml. The drug is known as allylamines and is prescribed for both systemic and external use. The mechanism of action of terbinafine is associated with the inhibition of the initial phase of the biosynthesis of ergosterol (the main cellular sterol in the fungal membrane) by inhibiting the specific enzyme squalene-2, 3-epoxidase in the fungal membrane. The drug is effective against many fungi pathogenic to humans. With local treatment, terbinafine is more effective than azole drugs, imidazole derivatives, but comparable to itraconazole and, when given orally, is more effective than griseofulvin and itraconazole. Terbinafine is characterized by lipoidophilia, it diffuses rapidly in the stratum corneum of the epidermis, dermis, subcutaneous tissue, accumulates in the sebaceous glands, hair follicles and nail plate in concentrations that provide a fungicidal effect. 1 guide. Once-daily terbinafine results in higher cure rates and better outcomes for each efficacy criterion (including mycological cure) than intermittent intraconazole therapy.

naftif(Naftifine) cream 1% - 15. 30 g; The 1% solution of 10, 20, 30 ml is a derivative of allylamines. The mechanism of action is associated with inhibition of squalene-2, 3-epoxidase enzyme activity, inhibition of ergosterol biosynthesis, which leads to violation of cell wall synthesis. Naftifine has a broad spectrum of action, acting as a fungicide against dermatophytes (such as Trichophyton, Epidermophyton, Microsporum), mold (Aspergillus spp. ), yeast-like fungi (Candida spp. , Pityrosporum) and other fungi, for example (escorotrichosis Sphenor) . . . The drug has an anti-inflammatory effect, reduces itching. When applied externally, it penetrates well into the skin, creating stable antifungal concentrations in its various layers.

The duration of treatment with Naftifin ranges from 2 weeks to 6 months. When using the drug, skin dryness and redness, a burning sensation may occur, all these side effects are reversible and do not require cancellation.

Amorolfine(Amorolfine) 5% enamel - 2, 5 and 5 ml, - a preparation for external use, it has a broad spectrum of action, providing fungistatic and fungicidal action due to damage to the cytoplasmic membrane of the fungus by interrupting the biosynthesis of sterols, by inhibiting enzymes 14– gamma demethylase and 7 gamma isomerase. The drug is active against the most common and rare pathogens of dermatophyte nail fungal infections: Trichophyton spp. , Microsporum spp. , Epidermophyton spp. ;molds: Alternaria spp. , Scopulariopsis spp. , Hendersonula sppi. ;fungi of the Dematiaceae family: Cladopsorium spp. , Fonsecaea spp. , Wangiella spp. ; dimorphic fungi Coccidioides spp. , Histoplasma spp. , Sporothrix spp.

When applied to the nails, the drug penetrates the nail plate and subsequently the nail bed, almost completely within the first 24 hours. The effective concentration remains on the affected nail plate for 7 to 10 days. after the first application. Systemic absorption is negligible. It is applied externally. The medicine is applied to damaged fingers or fingers 1 to 2 times a week. The duration of treatment is determined individually and depends on the indications for use. Side effects are rare and appear in the form of itching, burning at the application site. Not prescribed for young children and infants.

undecylenic acidand its salts - antifungals for external use, which have a fungistatic and fungicidal effect against dermatophytes, when combined with zinc or copper salts - zinc undecylenate or copper undecylenate - the activity increases. Zinc, which is part of the drug, has an astringent effect, reduces the appearance of signs of skin irritation and promotes faster healing.

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

The preparations are applied to a clean, dry surface of the affected skin twice a day (morning and evening). The duration of treatment is 4 to 6 weeks and depends on the nature, effectiveness and evolution of the disease. After the clinical signs of the disease have disappeared, they continue to be used once a day. For preventive purposes - 2 times a week.

Important! The contraindication to the use of the drug is hypersensitivity to undecylenic acid and its derivatives.

Cyclopirox(Ciclopirox) 8% enamel, fl. 3g, is a broad-spectrum antifungal agent that inhibits the capture of precursors for the synthesis of macromolecules in the cell membrane. Externally applied for the treatment and prevention of fungal infections of the skin, mucous membranes, nails, fungal vaginitis and vulvovaginitis.

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

Treatment of onychomycosis should be carried out under the strict supervision of a dermatologist. As a rule, a rational etiotropic complex therapy is used. A decrease or disappearance of clinical symptoms is usually seen a few days after administration of an antimycotic. However, to avoid relapses of the disease, the course of treatment must be carried out completely. In the context of clinical cure, anti-relapse therapy is often performed, with the aim of preventing reinfection.