Fluconazole

Fluconazole Due to its fungistatic effect, it is used as an antimycotic in the treatment of fungal infections. The active ingredient is used in particular when a local or topical (external) therapy for fungal infections remains ineffective.

What is fluconazole?

Fungal infections of the skin and nails as well as mucous membranes (including vaginal fungus, oral thrush) can be effectively treated with the drug. For this purpose, fluconazole can e.g. can be administered in capsules or as an injection preparation.

Fluconazole is an azole antifungal agent which, as a triazole derivative, belongs to the group of imidazoles and triazoles. The active ingredient is used in the treatment of infections with fungi that are pathogenic to humans.

Fluconazole itself is a whitish, crystalline powder that is difficult to dissolve in water. The triazole derivative, through its cytostatic or fungistatic effect, inhibits the growth and multiplication of pathogens, especially yeasts of the Candida genus.

Fungal infections of the skin and nails as well as mucous membranes (including vaginal fungus, oral thrush) can be effectively treated with the drug. For this purpose, fluconazole can be administered in capsules, as an injection preparation or as a suspension.

Pharmacological effect

Fluconazole Like all representatives of the imidazoles and triazoles, it has a fungistatic effect by inhibiting (inhibiting) the structure of the cell walls of the yeast fungi and thus their growth or multiplication.

Depending on the dosage, the active ingredient can also have a fungicidal (fungicidal) effect. After application, the active ingredient enters the bloodstream either via the gastrointestinal tract (including oral intake of hard capsules) or directly (intravenously administered injection preparation) and is distributed throughout the entire organism. In contrast to the human cell membrane, which consists of cholesterol, among other things, ergosterol is the most important building block of the yeast cell membrane.

In the cytochrome P450 system, fluconazole inhibits an enzyme that is important for the synthesis of ergosterol, the so-called 14-alpha-demethylase, which blocks the conversion of lanosterol to ergosterol. The building materials modified by the blockade lead to defects in the yeast cell membrane and impair certain metabolic processes that control the division of the fungal cells.

The pathogens can no longer multiply (fungistatic effect). Fluconazole, however, has a significantly weaker inhibitory effect on demethylase in the human organism.

Medical application & use

Fluconazole is used in the context of systemic (internal) therapy of infections with yeasts of the genus Candida (so-called cadidoses), of which Candida albicans is the most important representative.

As a rule, only the skin and / or nails (nail and athlete's foot infections) or the mucous membranes (oral thrush, vaginal fungus) are affected by candidiasis. In immunocompromised people, a fungal infection can in rare cases also affect the internal organs. Correspondingly, fluconazole can also be used prophylactically to prevent fungal infections in people who have a weakened immune system as a result of chemotherapy and / or radiation therapy measures.

Fluconazole has also been shown to be effective in treating meningitis (inflammation of the meninges) caused by infections with the yeast Cryptococcus neoformans. Fluconazole can also be used prophylactically in people with HIV who have an increased prevalence of this specific fungal infection (opportunistic infection). If local or topical application of other antimycotics in vaginal candidiasis is unsuccessful, fluconazole can alternatively be used as part of systemic treatment.

In some cases (around 10 percent) the pathogens develop resistance to fluconazole, so that the active ingredient has to be replaced by other fungicidal drugs such as flucytosine or amphotericin B.

Risks & side effects

Fluconazole As a comparatively newer representative of the triazoles, it is characterized by significantly fewer side effects and interactions compared to older active ingredients of this group. Nevertheless, therapy with fluconazole is not completely risk-free and can correlate with various side effects.

Therapy with fluconazole is often associated with nausea, vomiting and gastrointestinal complaints such as abdominal pain and diarrhea. Elevated enzyme levels for alkaline phosphatase and aminotransferases are also frequently observed. In some cases, loss of appetite, digestive disorders such as constipation (constipation) or flatulence, dizziness, headaches, cramps, increased sweat production, sensory disorders such as tingling, liver impairment, jaundice, anemia, and weakness and fever can be detected.

Angioedema, liver cirrhosis, tissue necrosis and Stevens-Johnson syndrome, among others, can very rarely be associated with fluconazole therapy. Fluconazole is contraindicated in the presence of hypersensitivity to the active ingredient or other antimycotics, in the case of pronounced liver and cardiac arrhythmias as well as impaired cardiac function.

In addition, the drug must not be administered during pregnancy, as animal experiments have shown an association with fetal malformations. A parallel therapy of fluconazole with terfenadine (antihistamine) or cisapride (prokinetic) should also be excluded.