Antifungal drugs for the treatment of systemic mycoses. Antifungal drugs in tablets of a wide spectrum of action

Antifungal medicines Medicines in the form of tablets and capsules

Indications for use

Treatment of mycoses with antifungal drugs in broad-spectrum tablets is indicated for:

• The course of an unspecified infection (the symptomatology of the disease is identical with a fungal infection, but it is impossible to establish the strain of the pathogen in the laboratory);
• Mixed fungal infection;
• A large area of ​​fungal skin lesions with the formation of ulcers, abscesses, exfoliation;
• Frequent relapses of the fungus of the extremities (onychomycosis, ringworm, candidiasis);
• The absence of a positive trend of recovery with local therapy of the fungus;
• Chronic (seasonal) exacerbation of a fungal infection;
• The development of the fungus against the background of immunodeficiency (HIV, AIDS);
• Leishmaniasis;
• High risk of fungal infection as a preventive measure if one of the family members is sick.

Classification of antimycotics

Pills for fungal infections are conditionally divided into two types, containing:

• natural ingredients;
• Chemical synthesized elements.

More sparing for the body tablets of the first type, the second - provides high resistance to the fungus.

Depending on the degree of activity and clinical use, tablet preparations for the fungus are classified into the following groups.

polyene

Includes antibiotic tablets of natural origin with an antimycotic spectrum of action against yeast (Candida), yeast-like, mold (Aspergillus) fungi, cryptococci, sporotrixes, dermatomycetes, pseudoallesheria boydi.

The active substance of drugs for the fungus:

• Nystatin;
• Levorinum;
• Natamycin;
• Neomycin;
• Amphotericin.

The main components of the tablets bind the sterols of the membranes of spore cells, which leads to the inhibition of the vital activity of fungi.

Azole

The azole synthetic series of tablets is active against yeast (candida), mold (aspergillus) fungi, dermatomycetes, sporotrixes, boydi pseudoallecheria, dimorphic (histoplasma) fungi, dermatomycetes, blastomycetes, cryptococci, coccidioids.

Active ingredient of antifungal tablets:

• Ketoconazole;
• Itraconazole;
• Fluconazole.

allylamine

Synthetic antimycotics in tablets have a depressing effect on yeast (candida, chromomycosis), mold (aspergillus), dimorphic (histoplasma) fungi, blastomycetes, sporotrixes, cryptococci.

The active substance of allylamine preparations - terbinafine, in the first minutes of entering the body, inhibits the division of fungal cells and destroys them from the inside.

The broad spectrum of action of antifungal tablets (capsules) can be explained by the negative impact of their components not only on the fungal infection caused by various pathogens, but also on the reproduction of the simplest microorganisms - amoebae, trichomonas, trypanosomes, leishmania.

Fungicidal substances of antifungal agents with proven effectiveness are included in the composition of combined antiseptic, bactericidal preparations, despite the fact that they tend to enhance or inhibit the effect of other drugs.

Contraindications for use

Systemic drugs against the fungus in tablet form are characterized by the following contraindications:

• Pregnancy;
• Lactation;
• Restriction of children's age;
• Diseases of the liver, kidneys, gastrointestinal tract, cardiovascular system;
• Diabetes;
• Allergy to the constituent components of the tablets.

Rules for the use of fungicidal tablets

The effectiveness of the therapy of mycoses with broad-spectrum antifungal agents is determined by:

• Determination of the causative agent - a strain of the fungus;
• A doctor's prescription for permission to use a certain type of pill;
• Compliance with the regimen of administration (regularity, dose, time interval, duration of the treatment course);
• Taking medication with food, drinking plenty of fluids.

Used in the treatment of fungal infections, antifungal antibiotics in tablets (capsules), characterized by fungicidal and fungistatic effects, are relatively toxic. There is no other alternative to these drugs, so they should be used with extreme caution.

Even if you follow the instructions for taking antifungal agents, adverse reactions may occur:

• dizziness;
• Violations of the functions of the gastrointestinal tract;
• Increased excitability;
• Active reproduction of the fungus instead of oppression;
• Allergic reaction.

Reception of tablet antifungal agents is incompatible with the use of alcohol-containing products.

Medical treatment of mycoses

The group of antifungal antibiotics in tablets (capsules) on the domestic pharmaceutical market is represented mainly by original drugs, the name of which is identical to the active substance. Designed for the treatment of adults and children.

Natomycin

Commercial name Pimafucin. The most affordable drug (360 rubles for 1 pack of 20 pcs.). Prescribed for intestinal candidiasis. The therapeutic course lasts no more than one week. The dose is determined depending on the age of the patient.

Nystatin

An antifungal drug from a number of available ones (550 rubles for 1 pack of 20 pcs.). It is prescribed mainly for candidiasis. The course of treatment with tablets does not exceed two weeks. The dosage is determined by the age scale. It is used in the treatment of mycoses and in their prevention.

Levorin

It belongs to the group of expensive antifungal drugs (700-900 rubles for 1 pack of 25 pcs.). The drug is prescribed for oral administration with candidiasis in order to prevent the disease, as well as with severe symptoms of sexual candidiasis and intestinal candidiasis. The course of treatment with tablets is from 15 days to three months. Dose the medicine depending on the age of the patient and the severity of the course of the disease.

Ampho-Moronal

The active substance is amphotericin B. The most expensive polyene (5600 rubles for 1 pack of 20 pcs.). The drug is prescribed for severe mycoses (trichosporosis, histoplasmosis, penicilliosis, aspergillosis, sporotrichosis, pheogyphomycosis, blastomycosis, paracoccidioidomycosis). The course of treatment of the fungus - from two weeks to a year. The dosage is prescribed by age.

Nizoral

The active ingredient is ketoconazole. The cost of the drug is 1260 rubles per 1 pack. 30 pcs. Tablets are prescribed for the diagnosis of chromomycosis, blastomycosis, histoplasmosis, coccidioidomycosis, paracoccidioidomycosis, also for mycosis of the hands and feet in cases of dermatosis and skin candidiasis, when local therapy is powerless. The dosage is prescribed depending on the patient's body weight and age. The duration of the therapeutic course with tablets is up to six months or more.

Orungal

The active ingredient is itraconazole. Price 1 pack antifungal capsules 14 pcs. - 3000 rubles. Tablets are prescribed for yeast and dermatophyte onychomycosis of the nails, skin candidiasis, an unspecified strain of the fungus, histoplasmosis, sporotrichosis, blastomycosis, pityriasis versicolor. Tablets are taken in courses, the duration of one is one to three weeks. The number of courses depends on the complexity of the course of the disease and can exceed six months. The dosage and regularity of taking the drug is determined depending on the age of the patient.

Diflucan

The active substance is fluconazole. 1 pack 14 pcs. costs at least 2000 rubles. Assign capsules from the fungus of the nails, feet, hands, torso, unspecified, chronic mycosis, candidiasis of varying complexity, cryptococcosis, epidermophytosis. The course of treatment of the fungus with this drug is four to eight weeks. The dose is determined depending on the age of the patient.

Terbizil

The active substance is terbinafine. Price 1 pack 14 pcs. tablets 1600 rubles. The drug is prescribed for nail mycosis, onychomycosis, skin candidiasis of the trunk and nails, fungus of the scalp. Depending on the degree of fungal infection, the course of treatment with tablets can last from one to three months. The dose of the drug is calculated according to the age of the patient.

Antimycotic analogues

The price of original antimycotics significantly exceeds the cost of analogues. The table shows samples of inexpensive, but effective antifungal tablets.

Griseofulvin is assigned to a separate group of cheap antifungal drugs intended for the treatment of severe mycoses. A pack of tablets (20 pcs.) Costs 240 rubles. Griseofulvin therapy is effective in the diagnosis of epidermophytosis, dermatosis, trichophytosis, microsporia of hair, nails. The course of treatment of an advanced fungus with these tablets is two to four months.

Antifungal drugs are available in pharmacies without a prescription, but it is not recommended to use them without a prescription from a dermatologist.

Content

A huge number of people suffer from fungal infections. Antifungal drugs help to 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.

Tablets

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 is 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 is 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:

Video

Attention! The information provided in the article is for informational purposes only. The materials of the article do not call for self-treatment. Only a qualified doctor can make a diagnosis and give recommendations for treatment, based on the individual characteristics of a particular patient.

Discuss

Antifungal drugs - effective and inexpensive

Antimycotic (antifungal) drugs are drugs whose mechanism of action is aimed at neutralizing and completely destroying pathogenic fungi.

Such pharmaceutical products can have both chemical and natural composition. Antifungal drugs have their own classification, so it’s quite difficult to choose the right remedy for yourself.

Alas, statistics show that today the need for such medicines has increased significantly. This is due to many different factors, the impact of which is often the result of rash actions of the person himself.

It is important to remember that antimycotics have a large number of contraindications, and can cause serious side effects. This is especially true for tablets and capsules for oral use, therefore, without a doctor's prescription, it is better not to get involved in taking them. Only a specialist can accurately calculate the dosage, and choose a drug substitute if necessary.

Patients undergoing therapy with antifungal medications must strictly follow all the recommendations of the attending physician. You can not independently change the regimen of therapy and adjust the dosage. Such actions can, at best, nullify all attempts to overcome the disease, and at worst, lead to more serious health problems.

How to choose the right medicine?

When symptoms of a fungus appear, it is better not to run to the pharmacy for a medicine, but to make an appointment with a dermatologist.

The doctor can determine the type of fungal infection, the degree of skin damage, and identify symptoms associated with the disease. Based on the data obtained, a drug is selected that will be most effective in a particular situation.

But the patient will not be able to independently perform the necessary diagnostic manipulations. Based on this, you should not self-medicate.

Dosage forms of drugs for the treatment of onychomycosis

Before prescribing a specific antimycotic, it is necessary to determine the type of causative agent of mycosis. To do this, a scraping is carried out from the surface of the nail plate or skin, and the selected material is subjected to a thorough laboratory study.

Treatment of onychomycosis can be carried out:

• topical preparations (gels, ointments, creams, varnishes, solutions);
• means for oral administration - capsules, tablets.

The use of topical drugs does not always give the expected results. Their components do not penetrate well into the lower layers of the nail plate, so it is advisable to use them only for superficial fungus. In addition, before starting therapy, it is recommended to remove or cut off the affected nail, which does not always suit patients.

A good alternative to sprays and ointments are special medical varnishes. They have a versatile effect, and have a completely different mechanism of action than other local antimycotics.

Distinctive features of varnishes from fungus are:

• the presence in their composition of drying components (alcohol, oil extracts, etc.);
• the ability to penetrate into all layers of the nail and spread through them;
• preventing the penetration of air into the nail after hardening of the varnish, which contributes to the death of the fungal flora;
• the active substance of the varnish leads to destructive processes in the membrane of fungi, as well as in the enzymes produced by them;
• the formation of a protective film on the surface of the nail, which prevents its re-infection.

If onychomycosis occurs in a chronic or complicated form, then, in addition to local, systemic antimycotic drugs are also prescribed. These drugs are very toxic, so their selection is carried out for each patient separately. In this case, the role is played not only by the type of pathogen, but also by the reaction of the patient's body to a specific agent.

The scheme of therapy is based on the use of "shock" doses of drugs in short courses. After one therapeutic course, a long break follows, after which the second begins, etc.

Azoles

Azoles belong to the group of synthetic antimycotic drugs, and are used to treat fungal infections in the scalp, skin, and nails. They are also used for lichen, as well as candidal lesions of the epidermis or mucous membranes.

Below is a list of the most effective and well-known antifungal drugs in this group:

1. Ketoconazole. The drug is used to combat dimorphic and yeast-like fungi. They are used to treat folliculitis, dermatophyte, seborrheic dermatitis, chronic candidiasis, lichen. Ketoconazole is used for the fungus of the head and skin, if there is an extensive fungal infection and resistance to the infectious process. The drug can cause serious side effects, so it must be used carefully. This is especially true for children and the elderly. You can buy Ketoconazole at a price of 100 rubles.
2. Mycozoral. With the help of this ointment, diseases such as epidermophytosis, pityriasis versicolor, ringworm, seborrheic form of dermatitis, various types of candidiasis are treated. Medications based on ketoconazole are also available in the form of shampoos and oral tablets. Their price starts from 200 rubles.
3. Sebosol is a shampoo and ointment used to treat fungal infections caused by yeast-like fungi, dimorphites, staphylococci and streptococci. The medicine is suitable for the treatment of fungus of the foot, nails, head. Its cost starts from 130 rubles.
4. - a broad-spectrum drug used for skin lesions with cryptococci and candida fungi. Capsules should be taken with caution by pregnant women, as well as patients with renal and hepatic diseases. The price of the drug is from 20 rubles.

Polyena

Polyenes are a group of broad-spectrum antifungal drugs. These drugs are the most common and frequently prescribed. In most cases, they are prescribed for fungal infections of the mucous membranes, skin and digestive tract.

The most effective drugs are:

1. . It is released in the form of tablets and ointments, and is used to treat fungal infections of the skin and mucous membranes. The use of the drug is advisable for candidal lesions of the vagina, oral cavity, intestines. The medicine has almost no contraindications and rarely causes side effects. Its cost is from 40 rubles.
2. Levorin. The drug is used for candidiasis of the digestive tract and skin. It is highly effective in the fight against Trichomonas, fungi of the genus Candida, as well as Leishmania. The drug is contraindicated in pregnancy, HB, liver and kidney failure, pancreatitis, gastric ulcer and duodenal ulcer. It should not be used by children under 2 years of age. The cost of the medicine ranges from 100-130 rubles.
3. . It is effective for many types of fungi, and is prescribed for candidal lesions of the gastrointestinal tract and vagina. Pimafucin is also used to eliminate fungal infections caused by long-term use of antibiotics or corticosteroids. The price starts from 250 rubles.

Allylamines

It is advisable to use this group of drugs for dermatomycosis - fungal infections of hair, nails and skin. The most popular drug in this group is, which is released in the form of an ointment and cream. It is used to treat fungal infections of the nails and skin. Effective against dimorphic and mold fungi.

The medicine is prescribed for the treatment of the skin of the legs, head and torso. Its use is also appropriate for nail fungus. The cost is from 48 rubles.

Broad Spectrum Antifungals

This group of drugs has a fungicidal and fungistatic effect. They prevent the further development of a fungal infection, and also destroy the remaining fungi.

The mechanism of action of drugs depends on their active ingredients.

1. Ketoconazole, which prevents the synthesis of fungal cell membrane constituents. The most effective drugs are Oronazole, Mycozoral, Fungavis.
2. Griseofulvin, which stops the division of fungal cells.
3. Itraconazole - allows the formation of fungal cells. The most effective representatives of this group are Irunin, Orunit, Orungal.
4. Terbinafine interrupts the synthesis of fungal cells at the initial stage.
5. Fluconazole is a substance that prevents the formation of new fungal spores and neutralizes those that already exist. This group includes drugs: Mycomax, Diflucan and Fluxstat.

Antifungal drugs have a lot of contraindications, the most common of which include:

• chronic renal and hepatic diseases occurring in severe form;
• the period of pregnancy and GV;
• childhood;
• glucose-galactose malabsorption;
• individual lactose intolerance;
• the use of certain groups of medications;
• individual intolerance to one or more components of the drug.

Based on these contraindications, only a doctor can prescribe a systemic antimycotic.

Antifungal nail polishes

This group of antimycotic drugs can be used in isolation, or as part of complex treatment. The most effective varnishes are:

1. Mycosan. The drug can be used for extensive fungal infections of the nail plate.
2. Lotseril. The drug quickly stops the fungal infection, even in the later stages of its development.
3. Batrafen. Varnish can be used to treat advanced onychomycosis. It well eliminates the unpleasant symptoms of pathology, and has a pleasant aroma.
4. Neil Expert. It is advisable to use the tool for the defeat of nails with yeast-like fungi. It slows down the growth of microorganisms and prevents their further spread.
5. Demicten. This varnish is allowed to be used in parallel with other topical antimycotics. The drug is effective for extensive lesions of the nail plate.
6. Gazebo. The medicine is used to disinfect nails after a course of treatment for the fungus. It eliminates odor and inflammation.

Before applying varnish, the nail must be filed and treated with an antiseptic (ordinary alcohol is also suitable). After that, a medicine is applied that dries within a few minutes. How often you can apply antifungal varnish, only the attending physician can tell.

Antifungal solutions (drops) and sprays

These drugs can be used both independently and in parallel with other antimycotics. They contain active ingredients from the ansol and allylamine groups.

Often doctors resort to prescribing antifungal drops:

• Clotrimazole;
• Mycospora;
• Exoderil.

Among the sprays are very popular:

• Bifosin;
• Lamitel;
• Lamisil;
• Terbix.

It is necessary to apply drops and sprays on previously cleansed skin and nails. Multiplicity of application - 1-2 times a day. The duration of treatment is determined by the doctor individually for each patient.

How to choose the right treatment methods?

The method of treatment depends on the type of pathogen and the stage of the pathological process. So, with the defeat of the epidermis, therapy is carried out using local antimycotics.

Onychomycosis requires a comprehensive approach, although it is often treated with one of the following options: topical antifungal therapy, cleaning and filing of the affected nail, or systemic antifungal medication.

The first signs of a fungal infection of the skin and nails should be a good reason for an immediate appeal to a dermatologist. And although fungal infections do not pose a serious danger to human health, they significantly impair the quality of life. In addition, they are easily transmitted to other people, so they must be treated.

Moreover, therapy at the initial stages of the development of mycosis does not take much time, and does not require significant financial costs.

Content

Most people have experienced itching near the nails, reddening of the lateral ridges, and an unpleasant smell from the feet, but this is not the only type of fungal infection - only the most common. If the lesion covers a large area or has affected internal organs, local treatment is indispensable: tablets are needed.

What are antifungal drugs in broad spectrum tablets

Antimycotics - the so-called drugs that have a fungistatic (suppress activity) or fungicidal effect (kill) on fungal microorganisms. They can be natural or synthetic, narrowly focused or broad spectrum, meaning they are effective against several groups of fungal microorganisms. Systemically (tablets) they are prescribed for:

• severe course of the disease;
• extensive area of ​​damage;
• infection of internal organs;
• the need to protect yourself from a fungal disease (with a high risk of infection).

The main advantage of such systemic drugs is their effectiveness - they act on several different pathogens at once and do it quickly, suitable for a severe infection. The downside is high toxicity, a large number of contraindications and side effects, so you need to carefully consider the doctor's recommendations and the prescribed regimen. Broad-spectrum antifungal drugs in tablets can cause:

• liver damage (hepatotoxic);
• estrogen fluctuations;
• severe allergic reactions;
• anaphylactic shock.

How to use

Antifungal drugs with a wide spectrum of activity for systemic treatment can be used parenterally (dropper solution) or orally. The specific scheme of application depends on the active substance, the form of the disease, the patient's condition. A few key points:

• Suction allylamines does not depend on food intake, so they can be taken at any time, and azoles - always with meals. It is advisable to use antibiotics not on an empty stomach in order to reduce the likelihood of mucosal irritation.
• Antimycotics it is advisable to drink only clean water. An exception is the situation of treatment with azoles in patients with low stomach acidity: they should take the pill with an acidic liquid (tea, pasteurized milk).
• Griseofulvin should be taken with a tablespoon of vegetable oil, especially if the patient is on a low-fat diet.
• Antifungals use according to the schedule, observing the time of admission and intervals (necessarily equal intervals). If you forget, take the pill as soon as you remember, but do not increase the single dose.
• Capsules cannot be destroyed (cut, pour out the contents). The tablet can be divided if necessary to reduce the dosage.

Classification of broad-spectrum antifungal drugs in tablets

Official medicine has several ways of dividing antimycotics into categories. By origin, they are synthetic (artificial) and natural. The classification by chemical structure (active substance) is more extensive:

• Azoles: derivatives of triazole, imidazole.
• Allylamines.
• Echinocandins.
• polyene antibiotics.
• Preparations of other chemical groups: ciclopirox, griseofulvin, flucytosine.

Antifungal antibiotics

The widest spectrum of action and high efficiency in the fight against the fungus are antibiotics of the polyene macrolide group - they do not affect only dermatomycetes with pseudo-allescheria. They mainly destroy representatives of the genus Candida, but can also be active against filamentous and dimorphic fungi, trichomonas, amoebas, leishmania. Known polyenes in tablets:

• Amphotericin B;
• Levorin;
• Nystatin;
• Mycoheptin;
• Natamycin.

All of them work by binding to the fungal cell membrane with ergosterol, which leads to a violation of its integrity and subsequent lysis (death) of the cell. Each of the polyene antibiotics has its own spectrum of activity and a list of organisms sensitive to it, so they are not interchangeable. When taking tablets, active substances from the gastrointestinal tract are almost not absorbed. A highly effective antifungal drug of this type is Pimafucin, which does not have a systemic effect, working only in the digestive tract:

• Active ingredient: natamycin.
• Indications: non-invasive intestinal candidiasis (treatment / prevention), including those caused by drug therapy.
• Side effects: in the first days of use, diarrhea, nausea.
• Contraindications: intolerance to the active substance.

A powerful representative of polyenes is Levorin, which is active against yeast-like fungi, is prescribed for a long course (for 10-12 days). If necessary, the treatment is carried out twice. Features of Levorin:

• Active ingredient: levorin.
• Indications: gastrointestinal candidiasis, carriage of fungi of the genus Candida.
• Side effects: diarrhea, nausea, vomiting, loss of appetite, headache.
• Contraindications: liver or kidney failure, hypersensitivity, pancreatitis, ulcers, acute bowel disease (not fungal etiology), pregnancy. With caution, it is allowed to use Levorin in children under 2 years of age and while breastfeeding.

Nystatin is a cheap polyene antibiotic based on the active substance of the same name, which can be prescribed not only for the active treatment of a fungal infection, but also for the prevention of infection. Key points:

• Active ingredient: nystatin.
• Indications: candidiasis of the skin, mucous membranes, internal organs. Long-term treatment with antimicrobial agents (prophylaxis).
• Side effects: nausea, vomiting, pruritus, fever.
• Contraindications: peptic ulcer, pancreatitis, liver problems, pregnancy, sensitivity to the composition.

Among the antifungal antibiotics of the non-polyene group, doctors single out the drug Griseofulvin: it works on a substance of the same name that has a fungistatic effect. It is produced by mold fungi, causes disruption of cell wall synthesis, inhibits cell division and protein production. It tends to accumulate in the cells of nails, hair and skin. Features of Griseofulvin tablets:

• Active ingredient: griseofulvin.
• Indications: dermatophytosis of the scalp, epidermophytosis (trichophytosis) of the hands and feet.
• Side effects: dyspepsia, headaches, dizziness, urticaria, leukopenia, increased levels of eosinophils.
• Contraindications: uterine bleeding, malignant tumors, impaired functioning of the kidneys and liver, porphyria (impaired pigment metabolism), problems with cerebral circulation, lactation and pregnancy, systemic lupus erythematosus, changes in the composition of the blood.

Synthetic antimycotics

The appointment of polyene antibiotics (or non-polyene) is rare - mainly antifungal drugs in capsules or tablets belong to the group of synthetic antimycotics. It is represented by the following categories of drugs:

• azoles;
• allylamines;
• echinocandins;
• drugs of other drug groups (cyclopirox, flucytosine, amorolfine).

Azoles

Broad-spectrum drugs from the azole category have a fungicidal effect (destroy cells) on the fungus, if used in high doses, and fungistatic (do not allow to multiply) in low doses. These medicines are also divided into groups (the names of medicines are given for the most used active substances):

• Triazole derivatives: miconazole (Daktarin, Klion D), ketoconazole (Oronazol, Nizoral, Fungavis), isoconazole, oxinazole, clotrimazole (Candide, Antifungol), bifonazole, sertaconazole, fenticonazole.
• Imidazole derivatives: vorkinazole (Vikand, Vfend), itraconazole (Orungal, Irunit), fluconazole (Diflucan, Flucostat).

Most of the azole preparations are used in the treatment of mycoses of the scalp, arms and legs, to combat lichen and especially thrush (vaginal candidiasis), since such tablets are highly effective against the Candida fungus. Among the most popular drugs from the azole group, doctors singled out the most non-toxic and approved Flucostat during pregnancy:

• Active ingredient: fluconazole.
• Indications: candidiasis of the mucous membrane of the eye, vagina, internal organs (including prophylaxis in the treatment of antibiotics), pityriasis versicolor, mycosis of the feet.
• Side effects: dizziness, headache, diarrhea, nausea.
• Contraindications: hypersensitivity to azoles, age up to 3 years, taking hepatotoxic drugs, breastfeeding.

Mycozoral among the other azoles is considered the most powerful (concerns the central component), therefore it is used mainly where treatment with other antimycotics did not work. Key points:

• Active ingredient: ketoconazole.
• Indications: deep mycoses, lesions of the scalp with dermatophytes / mold fungi, versicolor versicolor, chronic superficial candidiasis, systemic infections (histoplasmosis, blastomycosis).
• Side effects: menstrual disorders, toxic hepatitis, loss of appetite, hemolytic anemia.
• Contraindications: liver disease, children under 3 years of age, intolerance to any component of the composition. Tablets require care when combined with other medicines.

Biflurin tablets (as well as other drugs on vorkinazole) are little known, they can be the drugs of choice in case of intolerance to other azoles (or lack of effect from them). Features of the drug:

• Active ingredient: vorkinazole.
• Indications: invasive aspergillosis, severe forms of invasive candidiasis.
• Side effects: peripheral edema, chills, fever, chest pain, nausea, vomiting, indigestion, anemia.
• Contraindications: hypersensitivity, taking rifampicin, barbiturates, efavirenzine, ergot alkaloids.

Allylamines

The elimination of dermatomycosis (on the skin of the body, head) and onychomycosis is the main effect of drugs from the allylamine group, which include only 2 substances: naftifine and terbinafine. Tablets are released only on the latter and there are a large number of them:

• Fungoterbin;
• Exifin;
• Binafin;
• Thermikon;
• Mycoferon;
• Lamisil.

In the group of allylamines, terbinafine is considered more common and effective: it has a wide spectrum of action, is able to eliminate infections caused by protozoa (leishmaniasis, trypanosomiasis), deep mycoses, pityriasis versicolor. Naftifine (Exoderil) works only locally. Allylamines act by inhibiting the synthesis of ergosterol and destroying the shell of fungal spores, which leads to the death of the infectious agent. Low dosages are effective against molds and dimorphs. The most famous allylamine is Lamisil:

• Indications: dermatophytic onychomycosis, fungal infections of the scalp, feet, legs, candidiasis. With multi-colored lichen, the effectiveness is low.
• Side effects: headache, dizziness, change in taste perception, loss of appetite, abdominal pain, urticaria.
• Contraindications: hypersensitivity to the composition, chronic / acute liver disease, impaired renal function.

Most allylamines have approximately the same spectrum of action due to the same central component in the composition (they differ only in dosages and additional substances, therefore, to replace the expensive (due to its wide popularity) Lamisil, you can purchase a more budgetary Termikon:

• Active ingredient: terbinafine.
• Indications: mycoses of the scalp (trichophytosis, microsporia), skin and nails, severe extensive ringworm of the body, superficial candidiasis (not internal organs).
• Side effects: nausea, digestive problems, stool problems, skin manifestations of allergies, muscle or joint pain.
• Contraindications: pregnancy, lactation, alcoholism, inhibition of hematopoiesis, disorders of the liver / kidneys.

Close in cost to Termikon and Exiter, which, by analogy with all tablets on terbinafine, requires careful attention to the instructions, since it can affect the cardiovascular system. Features of the drug:

• Active ingredient: terbinafine.
• Indications: mycosis of the skin and nails, candidiasis of the mucous membranes.
• Side effects: jaundice, drug-induced hepatitis, muscle, headache or joint pain, nausea, vomiting, skin rash, taste disturbances.
• Contraindications: old age, disorders of the liver / kidneys.

Echinocandins

A new category of broad-spectrum antifungal agents are echinocandins, presented in a small assortment. They have not been fully studied by specialists, therefore they are prohibited for patients under 18 years of age, during pregnancy and lactation. Echinocandins work through the blockade of the synthesis of a fungal cell component, which disrupts the process of its construction. In this category, antifungal drugs are present only in powder (tablets are not available). The most studied is Cancidas:

• Active ingredient: caspofungin.
• Indications: candidiasis (strains insensitive to azoles), aspergillosis, suspected fungus in patients with febrile neutropenia (a sharp decrease in the level of neutrophils in the blood).
• Side effects: headache, chills, fever, nausea, abdominal pain, diarrhea, anemia, increased bilirubin levels, tachycardia, shortness of breath, skin rash with itching.
• Contraindications: age up to 3 months. Persons with hepatic insufficiency should be careful when taking.

Less well-known is the drug Mikamin, presumably even less toxic for children (there is no strict ban on use in the instructions, it is allowed to use the drug for a fungal rash on the buttocks of a child). Most doctors prescribe Mikamin to patients over 16 years of age. Features of the tool:

• Active ingredient: micafungin.
• Indications: Prevention or treatment of candidiasis, including candidal stomatitis.
• Side effects: leukopenia, anemia, increased number of eosinophils and bilirubin, hypokalemia, headaches, nausea, diarrhea, abdominal pain.
• Contraindications: intolerance to any component of the composition.

Eraxis, in comparison with other echinocandins, is the most budgetary representative of this group, since 100 ml of lyophilisate cost 5700-6000 rubles. - Mikamin in the same volume will cost the consumer 15,000 rubles. Cancidas next to him (14,000 rubles for 70 g). Eraxis Features:

• Active ingredient: anidulafungin.
• Indications: candidiasis (including damage to the esophagus).
• Side effects: skin allergic reactions, bronchospasm, shortness of breath, decreased pressure (occurs rarely), diarrhea.
• Contraindications: sensitivity to any echinocandins.

Other groups

Most dermatologists, when selecting antifungal drugs in tablets or capsules for systemic treatment of an infection, choose from the categories presented above. Azoles, allylamines, echinocandins and polyenes cope with most mycoses, but in rare cases it is necessary to turn to drugs from other groups. They have a less wide spectrum of action, but are often not so dangerous for the body. The only drug for systemic intravenous use is Ankotil:

• Active ingredient: flucytosine (fluorinated pyrimidine).
• Indications for use: has a fungicidal and fungistatic effect against pathogens of candidiasis, cryptococcosis, chromoblastomycosis (the main indications for use), disrupts the synthesis of fungal DNA. For aspergillosis, it is used with amphotericin B.
• Contraindications: The drug is non-toxic, prohibited in chronic renal failure, blood diseases. The teratogenic effect was found only in rats, so the question of using Flucytosine during pregnancy is decided by the doctor.
• Side effects: nausea, vomiting, diarrhea, dry mouth, stomach bleeding, headaches, dizziness, acute renal failure, severe weakness, fatigue, allergic reactions, fever.

As an antifungal agent (but not with a wide spectrum of activity), Potassium iodide, which is available in the form of eye drops and is used externally, can also be prescribed by a doctor. The solution is not used orally, if there is no iodine deficiency established by the results of the analysis. Before use, you need to know:

• Active ingredient: potassium iodide.
• Indications: lesions of the cornea, pathological conditions of the conjunctiva, which are caused by a fungus.
• Contraindications: neoplasms of the thyroid gland, kidney disease, hypersensitivity to iodine (and its excess in the body), acne.
• Adverse reactions: increased lacrimation, burning, disruption of the thyroid gland, redness of the mucous membrane of the eyes, blurred vision.

What antifungal drugs for internal use are prescribed

The choice of drug is determined by the specific pathogen, since even broad-spectrum tablets are not absolutely universal. So azoles are mainly used for lichen, onychomycosis, lesions of the scalp, and antibiotics are needed for extensive damage or systemic infection. Self-selection of an antifungal agent is prohibited, since this can aggravate the situation - the pathogen mutates and becomes resistant. To select a medicine, you need to conduct laboratory tests and undergo an examination by a dermatologist.

For deep mycosis

The colonization of bone tissues, nervous system, internal organs, and respiratory tract by pathogenic microorganisms requires the use of immunomodulating drugs. Such severe infections include coccidioidomycosis, cryptococcosis, blastomycosis, histoplasmosis. Among the broad-spectrum antifungal agents, doctors distinguish polyene antibiotics and some azoles (miconazole, ketoconazole, itraconazole, fluconazole):

• Itraconazole- medicine in capsules, with systemic fungal infections, it is used for 2-12 months (check with your doctor). The exact dosage depends on the specific disease and condition of the patient. Mostly adults are recommended 200 mg / day one-time.
• Ketoconazole DS- the dosage is calculated according to the patient's weight: 30 kg or more - 200-400 mg, less - 4-8 mg / kg. The daily dose is taken as a single dose. Used for 4 weeks or longer (determined by physician).

Treatment with intravenous administration of medicinal solutions is considered more effective - polyenes and azoles are also used here. Vorkinazol-Sandoz was highly appreciated by doctors, the dosage of which is set individually. It is worth paying attention to:

• Flucorus (fluconazole)- 50-400 mg, the frequency of use is 1 r / day. In case of impaired renal function, the dosage is determined individually. The duration of therapy depends on the clinical picture of the disease.
• Amphotericin B (or Ampholip)- the release form is not a tablet, but a powder for infusion (intravenously), which is done at a frequency of 20-30 drops / min. The adult dosage is 250 U/kg, but the first dose is 100 U/kg. The concentration of the solution is 100-125 IU per 1 ml of water for injection. Treatment lasts 4-8 weeks with the use of the drug every other day or 2 r / week.

With epidermomycosis

Skin infection requires active local treatment - the use of systemic antifungal agents is considered an additional step in the main therapy. Here, the non-polyene antibiotic Griseofulvin, synthetic antimycotics on terbinafine, Chlornitrophenol are used. Iodine preparations (potassium iodide) are allowed. Your doctor may recommend these broad-spectrum antifungal tablets:

• Exifin (terbinafine)- is prescribed for 2-4 weeks or more, 250 mg per day after meals. In case of renal / hepatic insufficiency, reduce the dose by 2 times.
• Itraconazole- with dermatomycosis, tablets are drunk at 200 mg / day for a week or 100 mg / day for 15 days. With lichen, only a weekly version with a high dose is practiced.
• Griseofulvin- the daily dosage for adults is 500 mg (taken at a time or divided into several servings), in case of severe illness, it is determined by the doctor. The course of treatment lasts 4-6 months if mycosis is on the fingers, 2-4 weeks for the body, 4-6 weeks for the scalp and feet. It is possible to increase up to a year with a severe form of dermatomycosis.

With candidiasis

Yeast infection of the genital organs (vaginal thrush), intestines, oral mucosa is eliminated mainly with the help of 2 categories of broad-spectrum antifungal agents: polyene antibiotics and azoles. Candidiasis responds to the following medications:

• Levorin- adults from candidiasis are recommended to drink 500 thousand units up to 4 r / day. The duration of treatment is 10-12 days.
• Nystatin- dosage for adults with candidiasis of internal organs: 500 thousand units with a frequency of 4-8 r / day, therapy lasts 2 weeks. If the infection is generalized, the dose is increased to 6000 thousand units per day (divided into 4-8 doses).
• clotrimazole- vaginal tablets are used for 3 days, 1 pc. morning and evening or just before bedtime, but for a whole week. If there is no effect, the doctor must adjust the therapeutic course. If necessary, treatment is extended.
• Miconazole- used for intestinal candidiasis at a dosage of 120-240 mg with a frequency of 4 r / day, is prescribed for 10-14 days.
• Fluconazole (analogue - Diflucan)- the most famous pills for recurrent thrush, are taken at 150 mg on the 1st, 4th and 7th day, and after 50 mg weekly for six months.

The severe course of a fungal infection, especially candidiasis of the internal organs, requires the use of solutions for droppers. The following antimycotics of a wide spectrum of activity have such a dosage form:

• Fluconazole- 200-400 mg / day, treatment lasts 6-8 weeks. A dropper is placed every day once.
• Miconazole- With caution, adults are prescribed 10 mg / kg intravenously (one-time no more than 600 mg). Dilute the solution with sodium chloride. The duration of the use of droppers is determined by the doctor.
• Micafungin-Nativ- with candidiasis of the esophagus intravenously, adults are prescribed 150 mg / day. The number of procedures is set individually.

For the treatment of fungal infections in children

Pediatricians recommend treating a child with topical medications whenever possible, since most broad-spectrum antifungal tablets are toxic. Ingestion is advisable for candidal stomatitis (tablets and lozenges), large lesions for other mycoses and active progression of the infection. The doctor should prescribe the therapeutic regimen - do not select such medicines for the baby yourself. In children, systemically can be used:

• Lamisil (terbinafine)- children over 3 years of age 125 mg / day (if the weight is 20-40 kg) or 250 mg / day (weight 40 kg or more). Dosages for tablets and intravenous solution are similar. The course of treatment is individual.
• Fluconazole- single use, calculate the dose by weight: 6-12 mg / kg, with food candidiasis once 3 mg / kg. For tablets and intravenous solution, the calculation is the same. The duration of therapy is from 2 weeks.
• Amphotericin B- the initial daily dose of the solution is 0.25 mg / kg (dilute with dextrose 5%), gradually increase it to 1 mg / kg (step - 0.125 mg / kg every other day). Application once a day, the duration of use is determined by the doctor.

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Antifungal drugs, or antimycotics, are a rather extensive class of various chemical compounds, both of natural origin and obtained by chemical synthesis, that have specific activity against pathogenic fungi. Depending on the chemical structure, they are divided into several groups that differ in the specifics of the spectrum of activity, pharmacokinetics and clinical use in various fungal infections (mycoses).

Classification of antifungal drugs

Polyenes:

Nystatin

Natamycin

Amphotericin B

Amphotericin B liposomal

Azoles:

For systemic use

Ketoconazole

Fluconazole

Itraconazole

For topical application

clotrimazole

Miconazole

Bifonazole

Econazole

Isoconazole

Oxyconazole

Allylamines:

For systemic use

For topical application

Preparations of different groups:

For systemic use

Griseofulvin

Potassium iodide

For topical application

Amorolfine

Cyclopirox

The need for the use of antifungal drugs has recently increased significantly due to an increase in the prevalence of systemic mycoses, including severe life-threatening forms, which is primarily due to an increase in the number of patients with immunosuppression of various origins. More frequent invasive medical procedures and the (often unjustified) use of powerful, broad-spectrum AMPs are also important.

Polyena

Polyenes that are natural antimycotics include nystatin, levorin, and natamycin, which are applied topically and orally, as well as amphotericin B, which is used primarily for the treatment of severe systemic mycoses. Liposomal amphotericin B is one of the modern dosage forms of this polyene with improved tolerability. It is obtained by encapsulating amphotericin B in liposomes (fat vesicles formed when phospholipids are dispersed in water), which ensures the release of the active substance only upon contact with fungal cells and is intact with respect to normal tissues.

Mechanism of action

Polyenes, depending on the concentration, can have both fungistatic and fungicidal effects due to the binding of the drug to the ergosterol of the fungal membrane, which leads to a violation of its integrity, loss of cytoplasmic content and cell death.

Activity spectrum

Polyenes have the broadest spectrum of activity among antifungal drugs. in vitro.

When used systemically (amphotericin B), sensitive Candida spp. (among C. lusitaniae resistant strains are found). Aspergillus spp. ( A.terreus may be sustainable) C.neoformans, pathogens of mucomycosis ( Mucor spp., Rhizopus spp. and etc.), S.schenckii, causative agents of endemic mycoses ( B. dermatitidis, H. capsulatum, C.immitis, P. brasiliensis) and some other mushrooms.

However, when applied topically (nystatin, levorin, natamycin), they act mainly on Candida spp.

Polyenes are also active against some protozoa - Trichomonas (natamycin), Leishmania and Amoeba (amphotericin B).

Polyenes are resistant to dermatomycete fungi and pseudo-allescheria ( P. boydii).

Pharmacokinetics

All polyenes are practically not absorbed in the gastrointestinal tract and when applied topically. Amphotericin B when administered intravenously is distributed to many organs and tissues (lungs, liver, kidneys, adrenal glands, muscles, etc.), pleural, peritoneal, synovial and intraocular fluid. Poorly passes through the BBB. Slowly excreted by the kidneys, 40% of the administered dose is excreted within 7 days. The half-life is 24-48 hours, but with prolonged use it can increase up to 2 weeks due to cumulation in tissues. The pharmacokinetics of liposomal amphotericin B is generally less well understood. There is evidence that it creates higher peak blood concentrations than standard. It practically does not penetrate into the tissue of the kidneys (therefore, it is less nephrotoxic). It has more pronounced cumulative properties. The elimination half-life averages 4-6 days, with prolonged use, an increase up to 49 days is possible.

Adverse reactions

Nystatin, levorin, natamycin

(for systemic use)

Allergic reactions: rash, itching, Stevens-Johnson syndrome (rare).

(when applied topically)

Irritation of the skin and mucous membranes, accompanied by a burning sensation.

Amphotericin B

Reactions to IV infusion: fever, chills, nausea, vomiting, headache, hypotension. Preventive measures: premedication with the introduction of NSAIDs (paracetamol, ibuprofen) and antihistamines (diphenhydramine).

Local reactions: pain at the site of infusion, phlebitis, thrombophlebitis. Preventive measures: the introduction of heparin.

Kidneys: dysfunction - decreased diuresis or polyuria. Control measures: monitor clinical analysis of urine, determination of serum creatinine levels every other day during dose increase, and then at least twice a week. Preventive measures: hydration, exclusion of other nephrotoxic drugs.

Liver: possible hepatotoxic effect. Control measures: clinical and laboratory (transaminase activity) monitoring.

Electrolyte imbalances: hypokalemia, hypomagnesemia. Control measures: determination of the concentration of electrolytes in blood serum 2 times a week.

Hematological reactions: most often anemia, less often leukopenia, thrombocytopenia. Control measures: a clinical blood test with the determination of the number of platelets 1 time per week.

GIT: abdominal pain, anorexia, nausea, vomiting, diarrhea.

Nervous system: headache, dizziness, paresis, sensory disturbance, tremor, convulsions.

Allergic reactions: rash, itching, bronchospasm.

Amphotericin B liposomal

Compared to the standard drug, it rarely causes anemia, fever, chills, hypotension, and is less nephrotoxic.

Indications

Nystatin, levorin

Candida vulvovaginitis.

(Prophylactic use is ineffective!)

Natamycin

Candidiasis of the skin, oral cavity and pharynx, intestines.

Candida vulvovaginitis.

Candida balanoposthitis.

Trichomonas vulvovaginitis.

Amphotericin B

Severe forms of systemic mycoses:

invasive candidiasis,

aspergillosis,

cryptococcosis,

sporotrichosis,

mucormycosis,

trichosporosis,

fusarium,

pheogyphomycosis,

endemic mycoses (blastomycosis, coccidioidomycosis, paracoccidioidomycosis, histoplasmosis, penicilliosis).

Candidiasis of the skin and mucous membranes (locally).

Leishmaniasis.

Primary amoebic meningoencephalitis caused by N. fowleri.

Amphotericin B liposomal

Severe forms of systemic mycoses (see amphotericin B) 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.

Contraindications

For all polyenes

Allergic reactions to drugs of the polyene group.

Additionally for amphotericin B

Liver dysfunction.

Kidney dysfunction.

Diabetes.

All contraindications are relative, since amphotericin B is almost always used for health reasons.

Warnings

Allergy. Data on cross-allergy to all polyenes are not available, however, in patients with an allergy to one of the polyenes, other drugs in this group should be used with caution.

Pregnancy. Amphotericin B passes through the placenta. Adequate and well-controlled studies on the safety of polyenes in humans have not been conducted. However, in numerous reports of the use of amphotericin B at all stages of pregnancy, adverse effects on the fetus have not been registered. Recommended to be used with caution.

Lactation. Data on the penetration of polyenes into breast milk are not available. No adverse effects have been noted in breastfed children. Recommended to be used with caution.

Pediatrics. No serious specific problems associated with the appointment of polyenes to children have been registered so far. In the treatment of oral candidiasis in children under 5 years of age, it is preferable to prescribe a suspension of natamycin, since buccal administration of nystatin or levorin tablets can be difficult.

Geriatrics. Due to possible changes in kidney function in the elderly, there may be an increased risk of amphotericin B nephrotoxicity.

Impaired kidney function. The risk of amphotericin B nephrotoxicity is significantly increased, so liposomal amphotericin B is preferred.

Impaired liver function. A higher risk of hepatotoxic action of amphotericin B is possible. It is necessary to compare the possible benefit from the use and the potential risk.

Diabetes. Since amphotericin B solutions (standard and liposomal) for intravenous infusion are prepared in 5% glucose solution, diabetes is a relative contraindication. It is necessary to compare the possible benefits of the application and the potential risk.

Drug Interactions

With the simultaneous use of amphotericin B with myelotoxic drugs (methotrexate, chloramphenicol, etc.), the risk of developing anemia and other hematopoietic disorders increases.

The combination of amphotericin B with nephrotoxic drugs (aminoglycosides, cyclosporine, etc.) increases the risk of severe renal dysfunction.

The combination of amphotericin B with non-potassium-sparing diuretics (thiazide, loop) and glucocorticoids increases the risk of developing hypokalemia, hypomagnesemia.

Amphotericin B, causing hypokalemia and hypomagnesemia, can increase the toxicity of cardiac glycosides.

Amphotericin B (standard and liposomal) is incompatible with 0.9% sodium chloride solution and other solutions containing electrolytes. When using systems for intravenous administration, established for the introduction of other drugs, it is necessary to flush the system with a 5% glucose solution.

Information for patients

When using nystatin, levorin and natamycin, strictly observe the regimen and treatment regimens during the entire course of therapy, do not skip a dose and take it at regular intervals. If you miss a dose, take it as soon as possible; do not take if it is almost time for the next dose; do not double the dose. Maintain the duration of therapy.

Observe the rules for storing drugs.

Azoles

Azoles are the most representative group of synthetic antimycotics, including drugs for systemic (ketoconazole, fluconazole, itraconazole) and local (bifonazole, isoconazole, clotrimazole, miconazole, oxiconazole, econazole) use. It should be noted that the first of the proposed "systemic" azoles - ketoconazole - after the introduction of itraconazole into clinical practice has practically lost its significance due to high toxicity and has recently been more often used topically.

Mechanism of action

Azoles have a predominantly fungistatic effect, which is associated with the inhibition of cytochrome P-450-dependent 14α-demethylase, which catalyzes the conversion of lanosterol to ergosterol, the main structural component of the fungal membrane. Local preparations, when creating high local concentrations in relation to a number of fungi, can act fungicidal.

Activity spectrum

Azoles have a wide spectrum of antifungal activity. The main causative agents of candidiasis are susceptible to itraconazole ( C. albicans, C. parapsilosis, C.tropicalis, C.lusitaniae and etc.), Aspergillus spp., Fusarium spp., C.neoformans, dermatomycetes ( Epidermophyton spp., Trichophyton spp., microsporum spp.), S. schenckii, P.boydii, H. capsulatum, B. dermatitidis, C.immitis, P. brasiliensis and some other mushrooms. Resistance is common in C.glabrata and C. krusei.

Ketoconazole is similar in spectrum to itraconazole, but does not affect Aspergillus spp.

Fluconazole is most active against most pathogens of candidiasis ( C. albicans, C. parapsilosis, C.tropicalis, C. lusitaniae etc.), cryptococcus and coccidioides, as well as dermatomycetes. Blastomycetes, histoplasmas, paracoccidioides and sporotrix are somewhat less sensitive to it. Does not work on aspergillus.

Azoles used topically are active mainly against Candida spp., dermatomycetes, M.furfur. They act on a number of other fungi that cause superficial mycoses. Some gram-positive cocci and corynebacteria are also sensitive to them. Clotrimazole is moderately active against some anaerobes (bacteroids, G.vaginalis) and Trichomonas.

Pharmacokinetics

Ketoconazole, fluconazole and itraconazole are well absorbed from the gastrointestinal tract. At the same time, for the absorption of ketoconazole and itraconazole, a sufficient level of acidity in the stomach is necessary, since, reacting with hydrochloric acid, they turn into highly soluble hydrochlorides. The bioavailability of itraconazole, administered in the form of capsules, is higher when taken with food, and in the form of a solution - on an empty stomach. Peak blood concentrations of fluconazole are reached after 1-2 hours, ketoconazole and itraconazole - after 2-4 hours.

Fluconazole is characterized by a low degree of plasma protein binding (11%), while ketoconazole and itraconazole are almost 99% protein bound.

Fluconazole and ketoconazole are relatively evenly distributed in the body, creating high concentrations in various organs, tissues and secretions. Fluconazole penetrates the BBB and the blood-brain barrier. CSF levels of fluconazole in patients with fungal meningitis range from 52% to 85% of plasma concentrations. Ketoconazole does not pass well through the BBB and creates very low concentrations in the CSF.

Itraconazole, being highly lipophilic, is distributed mainly to organs and tissues with a high fat content: liver, kidneys, and greater omentum. It can accumulate in tissues that are particularly prone to fungal infection, such as the skin (including the epidermis), nail plates, lung tissue, genitalia, where its concentration is almost 7 times higher than in plasma. In inflammatory exudates, itraconazole levels are 3.5 times higher than plasma levels. At the same time, itraconazole practically does not penetrate into “aquatic” media - saliva, intraocular fluid, CSF.

Ketoconazole and itraconazole are metabolized in the liver, excreted mainly by the gastrointestinal tract. Itraconazole is partially excreted with the secretion of the sebaceous and sweat glands of the skin. Fluconazole is only partially metabolized, excreted by the kidneys mainly unchanged. The half-life of ketoconazole is 6-10 hours, itraconazole is 20-45 hours, does not change with renal failure. The half-life of fluconazole is 30 hours, with renal failure it can increase up to 3-4 days.

Itraconazole is not removed from the body during hemodialysis, the concentration of fluconazole in plasma during this procedure is reduced by 2 times.

Azoles for topical application create high and fairly stable concentrations in the epidermis and underlying affected skin layers, and the concentrations created exceed the MICs for the main fungi that cause skin mycoses. The longest lasting concentrations are characteristic of bifonazole, the half-life of which from the skin is 19-32 hours (depending on its density). Systemic absorption through the skin is minimal and has no clinical significance. With intravaginal application, absorption can be 3-10%.

Adverse reactions

Common to all systemic azoles

Gastrointestinal: abdominal pain, loss of appetite, nausea, vomiting, diarrhea, constipation.

CNS: headache, dizziness, drowsiness, visual disturbances, paresthesia, tremor, convulsions.

Allergic reactions: rash, itching, exfoliative dermatitis, Stevens-Johnson syndrome (more often when using fluconazole).

Hematological reactions: thrombocytopenia, agranulocytosis.

Liver: increased activity of transaminases, cholestatic jaundice.

Additionally for itraconazole

Cardiovascular system: congestive heart failure, arterial hypertension.

Liver: hepatotoxic reactions (rare)

Metabolic disorders: hypokalemia, edema.

Endocrine system: impaired production of corticosteroids.

Additionally for ketoconazole

Liver: severe hepatotoxic reactions, up to the development of hepatitis.

Endocrine system: impaired production of testosterone and corticosteroids, accompanied in men by gynecomastia, oligospermia, impotence, in women - menstrual irregularities.

Common to local azoles

With intravaginal use: 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.

Indications

Itraconazole

Pityriasis versicolor.

Candidiasis of the esophagus, skin and mucous membranes, nails, candidal paronychia, vulvovaginitis.

Cryptococcosis.

Aspergillosis (with resistance or poor tolerance to amphotericin B).

Pseudoallescheriosis.

Feogyphomycosis.

Chromomycosis.

Sporotrichosis.

endemic mycoses.

Prevention of mycoses in AIDS.

Fluconazole

invasive candidiasis.

Candidiasis of the skin, mucous membranes, esophagus, candidal paronychia, onychomycosis, vulvovaginitis.

Cryptococcosis.

Dermatomycosis: epidermophytosis, trichophytosis, microsporia.

Pityriasis versicolor.

Sporotrichosis.

Pseudoallescheriosis.

Trichosporosis.

Some endemic mycoses.

Ketoconazole

Candidiasis of the skin, esophagus, candidal paronychia, vulvovaginitis.

Pityriasis versicolor (systemically and locally).

Dermatomycosis (locally).

Seborrheic eczema (locally).

Paracoccidioidomycosis.

Azoles for topical use

Candidiasis of the skin, oral cavity and pharynx, vulvovaginal candidiasis.

Dermatomycosis: trichophytosis and epidermophytosis of smooth skin, hands and feet with limited lesions. With onychomycosis, they are ineffective.

Pityriasis versicolor.

Erythrasma.

Contraindications

Allergic reaction to drugs of the azole group.

Pregnancy (systemically).

Breastfeeding (systemically).

Severe liver dysfunction (ketoconazole, itraconazole).

Age up to 16 years (itraconazole).

Warnings

Allergy. Data on cross-allergy to all azoles are not available, however, in patients with an allergy to one of the azoles, other drugs in this group should be used with caution.

Pregnancy. Adequate studies of the safety of azoles in humans have not been conducted. Ketoconazole passes through the placenta. Fluconazole may interfere with estrogen synthesis. There is evidence of teratogenic and embryotoxic effects of azoles in animals. Systemic use in pregnant women is not recommended. Intravaginal use is not recommended in the first trimester, in others - no more than 7 days. For outdoor use, care should be taken.

Lactation. Azoles penetrate into breast milk, and fluconazole creates the highest concentrations in it, close to the level in blood plasma. The systemic use of azoles during breastfeeding is not recommended.

Pediatrics. Adequate safety studies of itraconazole in children under 16 years of age have not been conducted, so it is not recommended for use in this age group. In children, the risk of ketoconazole hepatotoxicity is higher than in adults.

Geriatrics. In the elderly, due to age-related changes in renal function, fluconazole excretion may be impaired, as a result of which a correction of the dosing regimen may be required.

H dysfunction of the kidneys. In patients with renal insufficiency, fluconazole excretion is impaired, which may be accompanied by its cumulation and toxic effects. Therefore, in case of renal insufficiency, a correction of the dosing regimen of fluconazole is required. Periodic monitoring of creatinine clearance is required.

Impaired liver function. Due to the fact that itraconazole and ketoconazole are metabolized in the liver, in patients with a violation of its function, their cumulation and the development of hepatotoxic effects are possible. Therefore, ketoconazole and itraconazole are contraindicated in such patients. When using these antimycotics, it is necessary to conduct regular clinical and laboratory monitoring (transaminase activity monthly), especially when ketoconazole is prescribed. Strict monitoring of liver function is also necessary in people suffering from alcoholism, or receiving other drugs that can adversely affect the liver.

Heart failure. Itraconazole may contribute to the progression of heart failure, so it should not be used for the treatment of skin fungal infections and onychomycosis in patients with impaired cardiac function.

Hypokalemia. When prescribing itraconazole, cases of hypokalemia, which was associated with the development of ventricular arrhythmias, are described. Therefore, with its long-term use, monitoring of the electrolyte balance is necessary.

Drug Interactions

Antacids, sucralfate, anticholinergics, H 2 blockers and proton pump inhibitors reduce the bioavailability of ketoconazole and itraconazole, as they reduce acidity in the stomach and disrupt the conversion of azoles into soluble forms.

Didanosine (containing a buffer medium necessary to increase gastric pH and improve drug absorption) also reduces the bioavailability of ketoconazole and itraconazole.

Ketoconazole, itraconazole and, to a lesser extent, fluconazole are inhibitors of cytochrome P-450, therefore, they can interfere with the metabolism of the following drugs in the liver:

oral antidiabetic (chlorpropamide, glipizide, etc.), the result may be hypoglycemia. Strict control of blood glucose is required, with possible adjustment of the dosage of antidiabetic drugs;

indirect anticoagulants of the coumarin group (warfarin, etc.), which may be accompanied by hypocoagulation and bleeding. Laboratory monitoring of hemostasis parameters is required;

cyclosporine, digoxin (ketoconazole and itraconazole), theophylline (fluconazole), which can lead to an increase in their concentration in the blood and toxic effects. Clinical control, monitoring of drug concentrations with possible correction of their dosage is necessary. There are recommendations to reduce the dose of cyclosporine by 2 times since the concomitant appointment of itraconazole;

terfenadine, astemizole, cisapride, quinidine, pimozide. An increase in their concentration in the blood may be accompanied by a prolongation of the QT interval on the ECG with the development of severe, potentially fatal ventricular arrhythmias. Therefore, combinations of azoles with these drugs are unacceptable.

The combination of itraconazole with lovastatin or simvastatin is accompanied by an increase in their concentration in the blood and the development of rhabdomyolysis. During treatment with itraconazole, statins should be discontinued.

Rifampicin and isoniazid increase the metabolism of azoles in the liver and lower their plasma concentrations, which may be the cause of treatment failure. Therefore, azoles are not recommended for use in combination with rifampicin or isoniazid.

Carbamazepine reduces the concentration of itraconazole in the blood, which may be the reason for the ineffectiveness of the latter.

Cytochrome P-450 inhibitors (cimetidine, erythromycin, clarithromycin, etc.) can block the metabolism of ketoconazole and itraconazole and increase their blood concentrations. The simultaneous use of erythromycin and itraconazole is not recommended due to the possible development of cardiotoxicity of the latter.

Ketoconazole interferes with alcohol metabolism and can cause disulfirap-like reactions.

Information for patients

Azole preparations, when taken orally, should be washed down with a sufficient amount of water. Ketoconazole and itraconazole capsules should be taken with or immediately after a meal. With low acidity in the stomach, these drugs are recommended to be taken with drinks that have an acidic reaction (for example, cola). It is necessary to observe intervals of at least 2 hours between taking these azoles and drugs that lower acidity (antacids, sucralfate, anticholinergics, H 2 blockers, proton pump inhibitors).

During treatment with systemic azoles, terfenadine, astemizole, cisapride, pimozide, quinidine should not be taken. In the treatment of itraconazole - lovastatin and simvastatin.

Strictly observe the regimen and treatment regimens during the entire course of therapy, do not skip the dose and take it at regular intervals. If you miss a dose, take it as soon as possible; do not take if it is almost time for the next dose; do not double the dose. Maintain the duration of therapy.

Do not use drugs that have expired.

Do not use azoles systemically during pregnancy and lactation. Intravaginal use of azoles is contraindicated in the first trimester of pregnancy, in others - no more than 7 days. When treating with systemic azoles, reliable methods of contraception should be used.

Before starting the intravaginal use of azoles, carefully study the instructions for use of the drug. During pregnancy, discuss with your doctor the possibility of using the applicator. Use only special swabs. Observe the rules of personal hygiene. It should be borne in mind that some intravaginal forms may contain ingredients that damage the latex. Therefore, you should refrain from using latex barrier contraceptives during treatment and for 3 days after its completion.

In the treatment of mycoses of the feet, it is necessary to carry out antifungal treatment of shoes, socks and stockings.

Allylamines

Allylamines, which are synthetic antimycotics, include terbinafine, applied orally and topically, and naftifine, intended for topical use. The main indications for the use of allylamines are dermatomycosis.

Mechanism of action

Allylamines have a predominantly fungicidal effect associated with a violation of the synthesis of ergosterol. Unlike azoles, allylamines block earlier stages of biosynthesis by inhibiting the enzyme squalene epoxidase.

Activity spectrum

Allylamines have a wide spectrum of antifungal activity. Dermatomycetes are sensitive to them ( Epidermophyton spp., Trichophyton spp., micro-sporum spp.), M.furfur, candida, aspergillus, histoplasma, blastomycetes, cryptococcus, sporotrix, causative agents of chromomycosis.

Terbinafine active in vitro also against a number of protozoa (some varieties of leishmania and trypanosomes).

Despite the wide spectrum of activity of allylamines, only their effect on causative agents of dermatomycosis is of clinical importance.

Pharmacokinetics

Terbinafine is well absorbed from the gastrointestinal tract, and bioavailability is practically independent of food intake. Almost completely (99%) binds to plasma proteins. Having a high lipophilicity, terbinafine is distributed into many tissues. Diffusing through the skin, as well as standing out with the secrets of the sebaceous and sweat glands, it creates high concentrations in the stratum corneum of the epidermis, nail plates, hair follicles, and hair. Metabolized in the liver, excreted by the kidneys. The half-life is 11-17 hours, increases with renal and hepatic insufficiency.

When applied topically, systemic absorption of terbinafine is less than 5%, of naftifine - 4-6%. The preparations create high concentrations in various layers of the skin, exceeding the MIC for the main pathogens of dermatomycosis. The absorbed portion of naftifine is partially metabolized in the liver, excreted in the urine and feces. The half-life is 2–3 days.

Adverse reactions

Terbinafine inside

Gastrointestinal: abdominal pain, loss of appetite, nausea, vomiting, diarrhea, changes and loss of taste.

CNS: headache, dizziness.

Allergic reactions: rash, urticaria, exfoliative dermatitis, Stevens-Johnson syndrome.

Hematological reactions: neutropenia, pancytopenia.

Liver: increased activity of transaminases, cholestatic jaundice, liver failure.

Other: arthralgia, myalgia.

Terbinafine topically, naftifine

Skin: itching, burning, hyperemia, dryness.

Indications

Dermatomycosis: epidermophytosis, trichophytosis, microsporia (with limited damage - locally, with widespread - inside).

Mycosis of the scalp (inside).

Onychomycosis (inside).

Chromomycosis (inside).

Skin candidiasis (locally).

Pityriasis versicolor (locally).

Contraindications

Allergic reaction to drugs of the allylamine group.

Pregnancy.

Lactation.

Age up to 2 years.

Warnings

Allergy. Data on cross-allergy to terbinafine and naftifine are not available, however, in patients with an allergy to one of the drugs, the other should be used with caution.

Pregnancy. Adequate safety studies of allylamines have not been conducted. Use in pregnant women is not recommended.

Lactation. Terbinafine passes into breast milk. Use in breastfeeding women is not recommended.

Pediatrics. Adequate safety studies in children under 2 years of age have not been conducted, so use in this age group is not recommended.

Geriatrics. In the elderly, due to age-related changes in renal function, terbinafine excretion may be impaired, as a result of which a correction of the dosing regimen may be required.

Impaired kidney function. In patients with renal insufficiency, the excretion of terbinafine is impaired, which may be accompanied by its cumulation and toxic effects. Therefore, in case of renal insufficiency, a correction of the dosing regimen of terbinafine is required. Periodic monitoring of creatinine clearance is necessary.

Impaired liver function. Possible increased risk of terbinafine hepatotoxicity. Adequate clinical and laboratory monitoring is required. With the development of severe liver dysfunction during treatment with terbinafine, the drug should be discontinued. Strict monitoring of liver function is necessary in alcoholism and in people receiving other drugs that can adversely affect the liver.

Drug Interactions

Inducers of microsomal liver enzymes (rifampicin, etc.) can increase the metabolism of terbinafine and increase its clearance.

Inhibitors of microsomal liver enzymes (cimetidine, etc.) can block the metabolism of terbinafine and reduce its clearance.

In the situations described, it may be necessary to adjust the dosing regimen of terbinafine.

Information for patients

Terbinafine can be taken orally regardless of food intake (on an empty stomach or after a meal), should be washed down with a sufficient amount of water.

Do not drink alcoholic beverages during treatment.

Do not use drugs that have expired.

Do not use allylamines during pregnancy and lactation.

Do not allow topical preparations to come into contact with the mucous membrane of the eyes, nose, mouth, open wounds.

Consult a doctor if improvement does not occur at the time indicated by the doctor or if new symptoms appear.

Preparations of different groups

Griseofulvin

One of the earliest natural antimycotics with a narrow spectrum of activity. It is produced by a fungus of the genus Penicillium. It is used only for dermatomycosis caused by dermatomycete fungi.

Mechanism of action

It has a fungistatic effect, which is due to the inhibition of the mitotic activity of fungal cells in the metaphase and the disruption of DNA synthesis. Selectively accumulating in the "prokeratin" cells of the skin, hair, nails, griseofulvin gives the newly formed keratin resistance to fungal infection. The cure occurs after the complete replacement of the infected keratin, so the clinical effect develops slowly.

Activity spectrum

Dermatomycetes are sensitive to griseofulvin ( Epidermophyton spp., Trichophyton spp., microsporum spp.). Other mushrooms are resistant.

Pharmacokinetics

Griseofulvin is well absorbed from the gastrointestinal tract. Bioavailability is increased when taken with fatty foods. The maximum concentration in the blood is observed after 4 hours. High concentrations are created in the keratin layers of the skin, hair, nails. Only a small part of griseofulvin is distributed to other tissues and secretions. Metabolized in the liver. Excreted with feces (36% in active form) and urine (less than 1%). The half-life is 15-20 hours, does not change with renal failure.

Adverse reactions

Gastrointestinal: abdominal pain, nausea, vomiting, diarrhea.

Nervous system: headache, dizziness, insomnia, peripheral neuritis.

Skin: rash, itching, photodermatitis.

Hematological reactions: granulocytopenia, leukopenia.

Liver: increased activity of transaminases, jaundice, hepatitis.

Other: oral candidiasis, lupus-like syndrome.

Indications

Dermatomycosis: epidermophytosis, trichophytosis, microsporia.

Mycosis of the scalp.

Onychomycosis.

Contraindications

Allergic reaction to griseofulvin.

Pregnancy.

Liver dysfunction.

Systemic lupus erythematosus.

Porfiry.

Warnings

Pregnancy. Griseofulvin crosses the placenta. Adequate safety studies in humans have not been conducted. There is evidence of teratogenic and embryotoxic effects in animals. Use in pregnant women is not recommended.

Lactation.

Geriatrics. In the elderly, due to age-related changes in liver function, the risk of hepatotoxicity of griseofulvin may be increased. Strict clinical and laboratory control is required.

Impaired liver function. Due to the hepatotoxicity of griseofulvin, its administration requires regular clinical and laboratory monitoring. In case of impaired liver function, it is not recommended to prescribe. Strict monitoring of liver function is also necessary in alcoholism and in people receiving other drugs that can adversely affect the liver.

Drug Interactions

Inducers of microsomal liver enzymes (barbiturates, rifampicin, etc.) can increase the metabolism of griseofulvin and weaken its effect.

Griseofulvin induces cytochrome P-450, therefore, it can increase metabolism in the liver and, therefore, weaken the effect of:

indirect anticoagulants of the coumarin group (control of prothrombin time is necessary, dose adjustment of the anticoagulant may be required);

oral antidiabetic drugs, (blood glucose control with possible dose adjustment of antidiabetic drugs);

theophylline (monitoring of its concentration in the blood with possible dose adjustment);

Griseofulvin enhances the effect of alcohol.

Information for patients

Griseofulvin should be taken orally during or immediately after a meal. If a low-fat diet is used, griseofulvin should be taken with 1 tablespoon of vegetable oil.

Do not drink alcoholic beverages during treatment.

Strictly observe the regimen and treatment regimens during the entire course of therapy, do not skip the dose and take it at regular intervals. If you miss a dose, take it as soon as possible; do not take if it is almost time for the next dose; do not double the dose.

Do not use drugs that have expired.

Be careful with dizziness.

Do not expose to direct insolation.

Do not use griseofulvin during pregnancy and lactation.

During treatment with griseofulvin and within 1 month after the end, do not use only estrogen-containing oral preparations for contraception. Be sure to use additional or alternative methods.

In the treatment of mycoses of the feet, it is necessary to carry out antifungal treatment of shoes, socks and stockings.

Consult a doctor if improvement does not occur at the time indicated by the doctor or if new symptoms appear.

Potassium iodide

As an antifungal drug, potassium iodide is used orally as a concentrated solution (1.0 g/ml). The mechanism of action is not exactly known.

Activity spectrum

Active against many fungi, but the main clinical significance is the effect on S.schenckii.

Pharmacokinetics

Quickly and almost completely absorbed in the gastrointestinal tract. It is distributed mainly in the thyroid gland. It also accumulates in the salivary glands, gastric mucosa, and mammary glands. Concentrations in saliva, gastric juice and breast milk are 30 times higher than in blood plasma. Excreted mainly by the kidneys.

Adverse reactions

Gastrointestinal: abdominal pain, nausea, vomiting, diarrhea.

Endocrine system: changes in thyroid function (requires appropriate clinical and laboratory monitoring).

Reactions of iodism: rash, rhinitis, conjunctivitis, stomatitis, laryngitis, bronchitis.

Others: lymphadenopathy, swelling of the submandibular salivary glands.

With the development of severe HP should reduce the dose or temporarily stop taking. After 1-2 weeks, treatment can be resumed at lower doses.

Indications

Sporotrichosis: cutaneous, cutaneous-lymphatic.

Contraindications

Hypersensitivity to iodine preparations.

Hyperthyroidism.

Tumors of the thyroid gland.

Warnings

Pregnancy. Adequate safety studies have not been conducted. Use in pregnant women is possible only in cases where the intended benefit outweighs the risk.

Lactation. Concentrations of potassium iodide in breast milk are 30 times higher than in plasma. During treatment, breastfeeding should be discontinued.

Drug Interactions

When combined with potassium preparations or potassium-sparing diuretics, hyperkalemia may develop.

Information for patients

Potassium iodide should be taken orally after meals. A single dose is recommended to be diluted with water, milk or fruit juice.

Strictly observe the regimen and treatment regimens during the entire course of therapy, do not skip the dose and take it at regular intervals. If you miss a dose, take it as soon as possible; do not take if it is almost time for the next dose; do not double the dose. Maintain the duration of therapy. Irregular use or premature termination of treatment increases the risk of relapse.

Consult a doctor if improvement does not occur at the time indicated by the doctor or if new symptoms appear.

Amorolfine

Synthetic antimycotic agent for topical use (in the form of nail polish), which is a derivative of morpholine.

Mechanism of action

Depending on the concentration, it can have both fungistatic and fungicidal effects due to a violation of the structure of the cell membrane of fungi.

Activity spectrum

It is characterized by a wide spectrum of antifungal activity. sensitive to him Candida spp., dermatomycetes, Pityrosporum spp., Cryptococcus spp. and a number of other mushrooms.

Pharmacokinetics

When applied topically, it penetrates well into the nail plate and nail bed. Systemic absorption is insignificant and has no clinical significance.

Adverse reactions

Local: burning, itching or irritation of the skin around the nail, discoloration of the nails (rarely).

Indications

Onychomycosis caused by dermatomycetes, yeasts and molds (if no more than 2/3 of the nail plate is affected).

Prevention of onychomycosis.

Contraindications

Hypersensitivity to amorolfine.

Pregnancy.

Lactation.

Age up to 6 years.

Warnings

Pregnancy.

Lactation. Adequate safety data are not available. Use during breastfeeding is not recommended.

Pediatrics.

Drug Interactions

Systemic antimycotics enhance the therapeutic effect of amorolfine.

Information for patients

Carefully study the instructions for use.

Maintain the duration of therapy. Irregular use or premature termination of treatment increases the risk of relapse.

All altered nail tissue should be regularly ground down. Files used on diseased nails should not be used on healthy nails.

Consult a doctor if improvement does not occur at the time indicated by the doctor or if new symptoms appear.

Observe storage rules.

Cyclopirox

Synthetic antifungal drug for topical use with a wide spectrum of activity. The mechanism of action has not been established.

Activity spectrum

sensitive to ciclopirox Candida spp., dermatomycetes, M.furfur, Cladosporium spp. and many other mushrooms. It also acts on some gram-positive and gram-negative bacteria, mycoplasmas and Trichomonas, but this is of no practical importance.

Pharmacokinetics

When applied topically, it quickly penetrates into various layers of the skin and its appendages, creating high local concentrations that are 20-30 times higher than the MIC for the main pathogens of superficial mycoses. When applied to large areas, it can be slightly absorbed (1.3% of the dose is found in the blood), 94–97% binds to plasma proteins, and is excreted by the kidneys. The half-life is 1.7 hours.

Adverse reactions

Local: burning, itching, irritation, peeling or flushing of the skin.

Indications

Dermatomycosis caused by dermatomycetes, yeasts and molds.

Onychomycosis (if no more than 2/3 of the nail plate is affected).

Fungal vaginitis and vulvovaginitis.

Prevention of fungal infections of the feet (powder in socks and / or shoes).

Contraindications

Hypersensitivity to ciclopirox.

Pregnancy.

Lactation.

Age up to 6 years.

Warnings

Pregnancy. Adequate safety studies have not been conducted. Use in pregnant women is not recommended.

Lactation. Adequate safety data are not available. Use during breastfeeding is not recommended.

Pediatrics. Adequate safety studies have not been conducted. Use in children under 6 years of age is not recommended.

Drug Interactions

Systemic antimycotics enhance the therapeutic effect of ciclopirox.

Information for patients

Carefully study the instructions for use of the prescribed dosage form of the drug.

Strictly observe the regimen and treatment regimens during the entire course of therapy.

Maintain the duration of therapy. Irregular use or premature termination of treatment increases the risk of relapse.

Protective impervious gloves must be worn when working with organic solvents.

In the treatment of onychomycosis, all altered nail tissue should be regularly ground down. Files used on affected nails should not be used on healthy nails.

Avoid getting the solution and cream in the eyes.

The vaginal cream must be inserted deep into the vagina using the supplied disposable applicators, preferably at night. A new applicator is used for each procedure.

Consult a doctor if improvement does not occur at the time indicated by the doctor or if new symptoms appear.

Observe storage rules.

Table. Antifungal drugs.
Main characteristics and application features

* With normal kidney function

** With intravaginal administration. When applied externally, it is practically not absorbed

*** When applied to inflamed skin