Anti-fungal medication

Synonyms in a broader sense

Fungi, fungal diseases, candida, yeast, amphotericin B, athlete's foot

introduction

Antifungal drugs (Antifungal agents) are medicines for fungal infections. Fungi are multicellular organisms that feed on organic material. Around 100,000 species of fungi are known, but only around 50 species can be dangerous to humans. A distinction is made between sprouts and yeasts (e.g. Candida and Cryptococcus species) from filamentous or mold fungi (e.g. Aspergillus). The cell wall of the fungi made of chitin, glucans and cellulose are important targets for antimycotics. Antimycotics (antifungal agents) can stop the fungi from growing (fungistatic effect) or kill the fungi (fungicidal effect) (antifungal agents).

Classification

The classification of antifungal drugs (Anti-fungal agents) takes place on the basis of the point of attack:

  • Inhibition of ergosterol synthesis by allylamines, azoles and morpholines
  • Disruption of membrane function by polyenes
  • Antimetabolites such as flucytosine
  • Disturbance of the microtubules by griseofulvin
  • Glucan synthesis inhibitors such as echinocandins

Please also read our article on the genre Mushrooms.

Medicines for fungal infections in the mouth

If a doctor has diagnosed a fungal infection in the mouth and on the tongue, treatment should be carried out with an agent that contains an anti-fungal agent. In many cases, miconazole or nystatin are suitable. The medication should be taken for a few days after the symptoms have subsided to prevent the fungi from spreading again. In many cases, other measures are also indicated to counteract a fungal infection. For example, patients with asthma who use a spray containing cortisone should rinse their mouth thoroughly after each use, as the cortisone in the mouth promotes the growth of fungi.

People with a set of teeth should clean them thoroughly every evening and not keep them in their mouths all the time, as they are also a common cause of fungal infections on the tongue or in the mouth. In general, adequate oral hygiene must be observed. Smoking and the consumption of alcohol as well as spicy foods should be avoided completely if you have a fungal infection in the mouth, as this also encourages the fungi to spread. Patients who have a very dry mouth, such as cancer patients after chemotherapy, can use a saliva replacement solution, which can also counteract a fungal infection.

Read more on the topic: Oral thrush

Medicines for fungal infections in the intestines

In the case of a medically proven fungal infection in the intestine, treatment with medication to cure it is usually unavoidable. For example, those with the active ingredient nystatin or, alternatively, amphotericin B or natamycin, which are taken either as lozenges or in liquid form, are suitable. In addition to regular and consistent use, the correct method of application is particularly important. With a fungal infection in the intestine, these usually colonize the entire digestive tract, including the oral cavity and esophagus. If you just swallow the medication, the fungi in the intestine are killed. As soon as you stop taking medication, oral fungi that you swallow with food colonize the intestines again. It is therefore important to keep the medication in your mouth for as long as possible. With a solution or suspension, it should be moved around the mouth and pulled through the teeth. As long as you do not choke, it is most effective to do this even while lying down, as the active ingredient also reaches the back of the throat. Nystatin should be used four to six times a day, especially after meals. You can obtain precise information on the type and frequency of use from your doctor or pharmacy.

Medicines for vaginal thrush

Vaginal thrush is a fairly common fungal infection that, while harmless in most cases, can be very distressing and should therefore be treated. There are several effective drugs that can be used to do this. Products with the active ingredient clotrimazole are used most frequently. It is applied as an ointment to the affected areas of the skin and mucous membranes, where it has a direct inhibitory effect on fungal growth. However, it is important that it is definitely a fungal infection and not another disease. Therefore, women who have the symptoms of an infection for the first time, such as pronounced itching and usually whitish, quark-like discharge, should be examined by a gynecologist. Even if the fungal infection is by far the most common cause of the symptoms mentioned, there may also be another disease which must then be treated with other drugs in a targeted manner.

Read more about this at: Symptoms of vaginal thrush

Fungal infection in pregnancy

A fungal infection during pregnancy can in most cases be treated well with effective medication without any danger to mother and child. Even though a fungal infection can basically occur anywhere on the body and any organ, a fungal infection of the vagina is by far the most common in pregnant women. The pregnancy hormones change the sugar content in the cells of the vaginal lining, which makes it easier for fungal infections to occur. Drugs with the active ingredient clotrimazole are often used. This is applied as a cream to the affected areas. This drug poses no danger to the unborn child. On the contrary, it is even important to treat the irritating but harmless vaginal yeast infection during pregnancy. Otherwise, if left untreated, the fungal infestation can spread to the child at birth. In rare cases, this can even be life-threatening in premature babies. If fungal infections of other organs or areas of the body occur during pregnancy, treatment with other medications may be necessary. Medicines that are applied to the skin are usually harmless. In severe cases, it is necessary to take a drug that is also absorbed through the blood and thus possibly also affects the child's organism. Whether treatment is indicated in individual cases, which medication is suitable and whether it can affect the child, must be discussed with the doctor.

Read more about this at: Vaginal fungus in pregnancy

Ergosterol synthesis inhibitors

Ergosterol is a specific component of the fungal cell membrane and is essential for optimal cell function and growth. Since ergosterol is produced in several steps, the ergosterol synthesis inhibitors intervene at different points in the synthesis sequence. The most important drug groups among the ergosterol synthesis inhibitors are allylamines, azoles and morpholines (Antifungal agents).

Allylamines

Active ingredients and mechanism of action:
The allylamines (anti-fungal agents) include the active ingredients terbinafine (Lamisil ®) and the locally used naftifin (Exoderil®). These antifungal drugs (Antifungal agents) intervene in a very early step of the ergosterol synthesis and inhibit a very specific enzyme (squalene epoxidase). This inhibits growth in most types of fungus. It only has a fungicidal effect on skin fungi (dermatophytes). Terbinafine is taken orally, is well absorbed from the intestine into the circulation and accumulates mainly in the skin, nails and fatty tissue (remedy for fungal diseases).

Use and side effects:
Terbinafine is mainly used for skin infections caused by dermatophytes. The drug is broken down in the liver and the breakdown products are excreted via the kidneys and intestines. Therefore, terbinafine should not be given in the case of liver dysfunction. It is actually quite well tolerated. Unwanted skin symptoms or digestive disorders are rare (remedies for fungal diseases).

Azoles

Azoles (Antifungal agents) disrupt the ergosterol synthesis in a later step than the allylamines. They have an inhibiting effect on fungal growth (fungistatic).
Classification and application:
With the azoles (Antifungal agents) a distinction is made between active ingredients that can only be applied locally (e.g. as a cream or ointment) and active ingredients that can be administered locally and systemically. Clotrimazole (Canesten®) used for fungal infections of the skin, oral mucosa, genitals and skin folds. Other locally applied active ingredients are ketoconazole (Nizoral®), Bifonazole (Mycospor®), Miconazole (Daktar®), Isoconazole (Travocort®), Oxiconazole (Myfungar®) and fenticonazole (Fenizolan®).
Active substances that can also be administered systemically include fluconazole (Diflucan®), Itraconazole (Sempera®), Posaconazole (Noxafil®) and voriconazole (Vfend®). They are quite wide, i.e. effective against different types of fungi (remedies against fungal diseases).

Side effects and contraindications:
Gastrointestinal disorders such as nausea or abdominal pain are most likely to be observed as undesirable effects. Headaches, dizziness or skin rashes can also occur. The liver is rarely affected, which results in an increase in liver values ​​(Liver enzymes), but can also extend to severe functional disorders. Patients with liver disease and children in general should not be treated with azoles.
Drug interactions by azoles:
Azoles (drugs against fungal diseases) affect certain enzymes in the liver that belong to the so-called cytochrome P450 system (CYP450 enzymes). On the one hand, azoles are metabolized by CYP450 enzymes, on the other hand, azoles also inhibit some of these enzymes. These antiymcotics (antifungal agents) affect the activation or breakdown of some other drugs. If other active substances such as rifampicin, phenytoin, carbamazepine or phenobarbital are administered at the same time, they are broken down more quickly by azoles, which leads to a loss of effectiveness of these substances.
On the other hand, azoles should not be given with drugs that alter stomach acid. This leads to a reduced absorption of azoles from the gastrointestinal tract. These include, for example, H2 blockers such as ranitidine or drugs to neutralize acidic gastric juice (antacids).
The active ingredients itraconazole and voriconazole can lead to cardiac arrhythmias if terfenadine, an antihistamine drug, is given at the same time.

Amphotericin B

Another group among the antifungal agents (Antifungal agents) are the polyenes. For the active ingredients amphotericin B (Amphotericin B®), nystatin (Moronal®) or natamycin (Pimafucin®) the point of attack is also on the cell membrane of the fungi. The cell membrane protects, among other things before charged particles (ions, electrolytes) exchange between the inside of the cell and the environment. The interaction with the membrane results in the formation of channels. The consequence is an uncontrolled exchange of the electrolytes with a disruption of the cell function, which in the case of amphotericin B causes a killing (fungicidal effect) and in the case of natamycin an inhibition of the growth (fungistatic effect) of the fungi (agent against fungal diseases).

Use, side effects and contraindications:
Amphotericin B can only be given as an infusion because it is not absorbed from the gastrointestinal tract into the bloodstream when given orally. It works well against a wide variety of different fungi. However, since it can damage the kidneys (nephrotoxic) and is only slowly excreted by the kidneys, it is only used for severe, life-threatening fungal infections. Sometimes an inflammation of the vein (thrombophlebitis) occurs at the point of insertion of the infusion needle. Other side effects can include fever and other flu-like symptoms. In addition to disturbances in the gastrointestinal tract, the composition of the blood components can also change, above all a reduced number of blood platelets (thrombocytopenia), which affects the ability of the blood to clot. Amphotericin B should therefore not be used for liver or kidney diseases and their function and blood values ​​should be checked regularly during treatment. In the event of intolerance, there is the possibility of using liposomal amphotericin B, an active ingredient packed in fats, so to speak. With the same effectiveness, the lipid formulation has significantly fewer side effects (anti-fungal agents).

Drug interactions:
Amphotericin B also interacts when certain other drugs are administered at the same time. Amphotericin B strengthens the effect of certain heart medications (cardiac glycosides), muscle relaxants (muscle relaxants) and drugs against cardiac arrhythmias (antiarrhythmics). Furthermore, the kidney-damaging effect of other kidney-damaging drugs is increased.

Antimetabolites

Antimetabolites are building blocks that are built into the DNA or RNA and, due to their structure, then disrupt them. The DNA describes the genetic material and is present as a long, double-stranded thread, consisting of individual components that are joined together in a chain. As a rule, the structure is changed in such a way that the antimetabolites can be incorporated, but cannot be extended because of the lack of a certain chemical structure. This is also called chain termination. RNA is basically a part of the DNA that is needed to produce a certain protein or enzyme. RNA has the same structural components as DNA, but in contrast to DNA it is only present as a single strand. This means that proteins and enzymes that the fungi need to survive cannot be produced or can only be produced incorrectly. The fungi cannot multiply because of the inhibition of cell division. The active ingredient flucytosine (Ancotil®) is a so-called.Cytosine antimetabolite. It gets into the fungal cell and is then converted by a certain enzyme (cytosine desmainase) before it is incorporated into the genetic material of the fungal cells. It has a fungistatic effect, i.e. it inhibits the multiplication of fungi (anti-fungal agents).

Flucytosine (Antifungal agents) is given as an infusion and only works on fungi that contain a certain enzyme (Cytosine deaminase) own. This is how it will be Candida, cryptococci and black fungiwhich attack the skin and subcutaneous tissue. Usually it will be with the polyene Amphotericin B combined.

Side effects:
The side effects are reversible and affect the Gastrointestinal tract, Increase in liver values (Liver enzymes) as well as changes in blood composition. It shouldn't be at Kidney, liver and blood formation disorders given (antifungal agents).

Griseofulvin

Another drug among the antifungal drugs (Antifungal agents) is griseofulvin. It is taken orally and is directed against microtubules. This is understood to mean protein structures in the cells. They are tubular and serve on the one hand for stabilization and transport within the cells, on the other hand they have an important role in the division of cells (spindle apparatus). Griseofulvin interferes with the production and function of these important proteins. It is deposited in the skin, nails and hair and is effective against fungal infections that attack these structures (dermatomycoses).
The main side effects observed so far are gastrointestinal disorders and skin changes. There are seldom disorders in the central nervous system or changes in the blood count (Neutropenia).
It should not be used for liver dysfunction, connective tissue diseases (Collagenoses) or certain blood disorders (porphyria).
In addition, the effects of anticoagulants (anticoagulants) and the pill (Contraceptives) decreased. When taking griseofulvin, alcohol consumption should be avoided.