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Griseofulvin: An Updated Overview of Old and Current Knowledge

Griseofulvin is an antifungal polyketide metabolite produced mainly by ascomycetes. Since it was commercially introduced in 1959, griseofulvin has been used in treating dermatophyte infections. This fungistatic has gained increasing interest for multifunctional applications in the last decades due to its potential to disrupt mitosis and cell division in human cancer cells and arrest hepatitis C virus replication. In addition to these inhibitory effects, we and others found griseofulvin may enhance ACE2 function, contribute to vascular vasodilation, and improve capillary blood flow.

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Articles of Interest

Griseofulvin, Terbinafine, Echinocandins

Griseofulvin is effective against dermatophytic infections, including tinea corporis, tinea pedis, and tinea cruris owing to its accumulation in keratin-rich tissues. It acts by binding to fungal cell microtubules, leading to a halt in mitosis. However, it can cause adverse effects, including activation of the cytochrome P-450 system of the liver

Setting The Record Straight With Griseofulvin

There is a safety or comfort level with this drug because it has been used for so long whereas you don’t have as much of a comfort with the newer agents. So I think griseofulvin does have the advantage of being a tried and tested agent with a very good safety profile. In my opinion, griseofulvin has a relatively favorable drug interaction profile.

What is Griseofulvin used for?

Griseofulvin, a well-known antifungal medication, has been a cornerstone in the treatment of various fungal infections for decades. Originally discovered in the 1930s by researchers at the University of Oxford, Griseofulvin is a natural compound isolated from the mold Penicillium griseofulvum. Over the years, this drug has been marketed under several trade names, including Gris-PEG, Fulvicin, and Grifulvin V. It primarily targets dermatophytes, a type of fungi that infect the skin, hair, and nails. Typically, Griseofulvin is prescribed for conditions such as tinea corporis (ringworm), tinea capitis (scalp ringworm), tinea pedis (athlete's foot), and onychomycosis (fungal nail infections). Despite its long history, ongoing research continues to explore new formulations and delivery methods to enhance its efficacy and reduce side effects.

Antitumor properties of griseofulvin and its toxicity

Griseofulvin (GF), which is mainly extracted from Penicillium griseofulvum, is a heat-resistant, chlorine-containing non-polyene antifungal antibiotic. Previous research shows that GF has a variety of pharmacological effects, such as anti-inflammatory, antifungal, antiviral, and antitumor effects. In recent years, GF has received extensive attention for its antitumor effects as a natural compound, offering a low price, a wide range of uses, and other beneficial characteristics.

Griseofulvin

The antifungal activity is explained by its ability to inhibit cell mitosis in fungi, causing the formation of multiple-nuclei, defective cells. The spectrum of antifungal activity of griseofulvin includes dermatophyte infections of the skin, nails, and scalp. It is ineffective against deep systemic mycotic infection. It is also ineffective for can-didomycoses. It is possible to develop resistance to it.

Griseofulvin in Children: Revisiting the Vintage Drug

Griseofulvin is a natural spirocyclic polyketide produced mainly by ascomycetes. It is the first systemic antifungal licensed for dermatophytosis in children. Even after several years of its discovery, it remains one of the widely used antifungals due to the cost-effective and safe treatment option for dermatophytosis.

Griseofulvin inhibits Fungal Mitosis

GRISEOFULVIN is an antifungal antibiotic widely used for the treatment of human and animal dermatophytic infections. The in vivo antifungal activity of griseofulvin is a reflexion of its peculiar pharmacological properties for, after oral administration, it is specifically localized and concentrated in the keratinized cells of the skin, hair and nails. The invasive growth of dermatophytes parasitizing these tissues is inhibited and the infected tissue is removed by desquamation and the growth of new epidermal layers.

Griseofulvin remains a valuable tool in treating dermatophyte infections

Discovered in the 1930s, griseofulvin was one of the first systemic antifungal agents and played a crucial role in treating dermatophyte infections before the advent of newer antifungals.

Griseofulvin-Induced Red and Hot Ears

Griseofulvin is a natural product, first isolated in 1939 from Penicillium griseofulvum and was first commercially introduced in 1959. It is a polyketide that is derived from acetyl and malonyl coenzyme A precursor molecules to form dehydrogriseofulvin. It inhibits microtubule assembly, affects the formation of the mitotic spindle, and finally inhibits mitosis in dermatophytes. Griseofulvin is mainly used for dermatophytes; however, other uses include anti-inflammatory, cardiovascular, antitumor, and antiviral activity. It has mainly gastrointestinal side effects, but other adverse effects can also be noticed, such as photosensitivity, urticaria, and petechia.

Griseofulvin: A New Look at an Old Drug

Griseofulvin is the oral antifungal agent of choice for the treatment of dermatophytoses. This article reviews the history, pharmacokinetics, adverse reactions traditional therapeutic applications of griseofulvin. In addition, reports since 1960 of the use of the drug in the treatment of Raynaud's phenomenon, progressive systemic sclerosis, lichen planus, mycosis fungoides, herpes zoster, eosinophilic fasciitis molluscum contagiosum are discussed, noting the varying degree of therapeutic success.

Now that griseofulvin is not available, what to do with tinea capitis treatments?

Griseofulvin, discovered in 1939 and commercially available since 1959, was the first oral antifungal agent effective against dermatophytosis, particularly tinea capitis. Although it was eventually superseded by azole antifungals due to its long treatment duration and reliance on keratopoiesis, griseofulvin remains notable for its effectiveness and safety in treating tinea capitis, especially when caused by Microsporum canis. However, due to a decline in cases and commercial unavailability, alternative treatments are now required.

Side Effects of Gris-Peg (griseofulvin)

Gris-Peg (griseofulvin) is an oral antibiotic used to treat fungal infections of the skin, body, hair/beard, or nails. Common side effects of Gris-Peg include hypersensitivity reactions (including rashes, itching, and redness), swelling under the surface of the skin (angioedema), numbness of the hands and feet, oral thrush, nausea, vomiting, upset stomach, diarrhea, headache, tiredness, dizziness, difficulty sleeping (insomnia), protein in the urine (proteinuria), and reduced white blood cell count (leukopenia). Gris-Peg is known to cause birth defects and should be avoided during pregnancy. The manufacturer recommends against the use of Gris-Peg in breastfeeding mothers.

What is Griseofulvin & Why is it used in the Treatment of Fungal Infections?

Griseofulvin has earned a spot on the World Health Organization’s List of Essential Medicines and has been approved by the U.S. Food and Drug Administration since 1962 under the drug class of antifungal agents. This medicine is utilized for the treatment of a number of skin infections such as ringworm, athletes’ foot, and other nail and skin fungi that do not respond to creams or lotions.

What is the best medication for a fungal infection of the toenail?

We found high-quality evidence that compared to placebo, terbinafine and azoles are effective treatments for the mycological and clinical cure of onychomycosis, with moderate-quality evidence of excess harm. However, terbinafine probably leads to better cure rates than azoles with the same risk of adverse events (moderate-quality evidence). Azole and griseofulvin were shown to probably have a similar effect on cure, but more adverse events appeared to occur with the latter (moderate-quality evidence). Terbinafine may improve cure and be associated with fewer adverse effects when compared to griseofulvin (low-quality evidence).

Resources

American Osteopathic College of Dermatology

Griseofulvin is an antifungal antibiotic used in the treatment of several fungal dermatologic infections. It is produced by a specific species fungus called penicillium. The drug was first isolated in 1939 and initially was used as a treatment for ringworm in cattle. It was officially approved by the FDA in 1959. It is marketed in several oral formulations including microsize and ultramicrosize. Griseofulvin is metabolized in the liver and excreted in the feces, urine and perspiration.

DermNet

Griseofulvin has been available since 1958 to treat ringworm (tinea). It is not effective against yeasts such as candida or malassezia. Griseofulvin has been withdrawn from the market in New Zealand (2002) and other countries, as it has been superceded by more effective and safer antifungal drugs. Griseofulvin comes from the mould, Penicillium griseofulvum. It stops fungal cells dividing (i.e. it is fungistatic) but does not kill them outright. This means treatment needs to be continued for several weeks or months. For many fungal infections, especially of the nail (tinea unguium), newer drugs work better than griseofulvin.

StatPearls

Griseofulvin is also indicated in onychomycosis, although newer antifungals such as terbinafine, itraconazole, and fluconazole have largely replaced it.