Griseofulvin is an antifungal agent used to treat infections of the skin with dermatophytes (filamentous fungi). It is a fungal toxin produced by the mold Penicillium griseofulvum.
What is griseofulvin?
As a fungal toxin, griseofulvin has antibiotic activity against filamentous fungi, which mainly affect the skin and its appendages, such as fingernails and toenails. Griseofulvin is a chemical active ingredient of the mold Penicillium griseofulvum. As a fungal toxin, it has an antibiotic effect against filamentous fungi, which mainly attack the skin and its appendages, such as fingernails and toenails. However, griseofulvin is ineffective against other fungi, including molds. Chemically, it is a benzofuran derivative that can be applied both orally and locally. It is, so to speak, a toxin produced by molds, which in turn acts against other types of fungi. Studies have also shown that griseofulvin can also fight cancer cells by inhibiting their cell division. Medically, this property is not yet significant. Currently, griseofulvin is used exclusively as an antifungal agent against dermatophytes.
Pharmacological action
The mode of action of griseofulvin is justified by its influence on cell division. It causes inhibition of mitosis (cell division), thus causing the death of the corresponding cells without the formation of subsequent cell lines. Griseofulvin binds to the intracellular protein tubulin, which is a basic building block of microtubules. These microtubules, in turn, are building blocks of the spindle fibers responsible for cell mitosis. However, if griseofulvin binds to tubulins, they can no longer be used to build the microtubules. Thus, ultimately, the formation of spindle fibers necessary for cell division is hindered, resulting in the inhibition of mitosis and intracellular transport of substances. The reason why mainly filamentous fungi that attack the skin are combated by griseofulvin is that the active ingredient is firmly bound to the keratin of the skin after oral ingestion. Its removal there is only possible again through the exfoliation of dead skin cells. Griseofulvin keratin complexes, for energetic reasons, selectively migrate into these cells in the presence of dermatophytes and disrupt their cell division. The same mechanism of action also causes the observed inhibitory effect of griseofulvin on the cell division of cancer cells.
Medical application and use
Griseofulvin is now mainly used for the treatment of children with tinea corporis and tinea capitis. For its therapy, griseofulvin is the only approved drug in Germany. It is used less frequently in the treatment of onychomycosis (nail fungus), because there are better-acting drugs for this purpose. Tinea corporis, also called ringworm, is a fungal disease of the trunk and extremities without involvement of the hands, feet and groin. This disease causes ring-shaped, circular redness with scaling and itching of the skin. Several species of dermatophytes are implicated in the development of these symptoms. Treatment is with ointments containing griseofulvin applied locally. Tinea capitis, on the other hand, is a dermatophytosis characterized by infestation of the hairy scalp with dermatophytes, especially in adolescents during puberty. It results in circular hair loss with scaly changes. Treatment is by local and systemic application of medications containing griseofulvin. The duration of therapy can be up to three months. Other skin mycoses, such as athlete’s foot, are also treated with griseofulvin, among others. Treatment of onychomycosis (nail fungus) was also frequently carried out with griseofulvin in the past. Today, griseofulvin is used less frequently here, along with other active ingredients.
Risks and side effects
Side effects may also occur with the use of griseofulvin. First of all, it should always be noted that there are people who are sensitive to certain active ingredients. In this case, of course, the use of griseofulvin is contraindicated. Otherwise, gastrointestinal disorders and skin changes have sometimes been observed. In rare cases, neurological problems and blood count changes may occur. Griseofulvin is contraindicated in liver dysfunction, collagenosis, or blood disorders such as porphyria.Furthermore, the effect of certain drugs is reduced, such as the pill or anticoagulants. Since griseofulvin affects cytochrome P 450, the use of other medications must be coordinated with the doctor. Adverse effects of griseofulvin with other drugs may include headache, fatigue, nausea, vomiting, diarrhea, allergies, or sensitivity problems.
