GRISEOFULVIN: CLINICAL APPLICATION AND MECHANISM OF ACTION

Griseofulvin is a naturally synthesized antifungal agent that is produced by Penicillium species (particularly P. griseofulvin). Griseofulvin is available both for topical and oral administration, but the drug is mainly used for topical treatment of superficial mycoses. The drug is poorly absorbed by the gastrointestinal tract (GIT), and this limits their usage for oral administration. The structure of griseofulvin is shown in Figure 1.

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CLINICAL APPLICATION OF GRISEOFULVIN

Griseofulvin is mainly used to treat superficial mycoses caused by dermatophytes. Dermatophytes are fungal cells that cause skin infections or diseases. 

Figure 1. Chemical structure of griseofulvin. Photo courtesy: https://www.microbiologyclass.com

They are a group of fungal organisms that can degrade the keratin layers or tissues of animals and humans. Dermatophytes mainly affect the nails, skin and hair causing a range of infections generally known as dermatophytosis (e.g. ringworm). Typical examples of dermatophytes are Microsporum species, Epidermophyton species and Trichophyton species. Griseofulvin exists only as creams or solutions which are applied topically on the site of the infection. Fungal infections of the hairs, skin, scalp and ringworm are best treated with griseofulvin. However, griseofulvin is also available for oral administration but the drug is poorly absorbed by the GIT.

MECHANISM OF ACTION OF GRISEOFULVIN

The mechanism of action of griseofulvin is mainly based on its ability to interfere with cell division (particularly mitosis) in fungal cells. Particularly, griseofulvin disrupts microtubule formation or mitotic spindle and this interferes with mitosis in fungi, thus affecting the biosynthetic machinery of other molecules such as the synthesis of DNA, RNA and proteins in fungi. 

SIDE EFFECTS AND FUNGAL RESISTANCE TO GRISEOFULVIN

Hypersensitivity is one of the notable side effects of the topical application of griseofulvin for treating fungal infections. Other untoward effects associated with the clinical use of griseofulvin include headache and stomach upset. Resistance to griseofulvin is rare.

FURTHER READING

Ashutosh Kar (2008). Pharmaceutical Microbiology, 1st edition. New Age International Publishers: New Delhi, India. 

Block S.S (2001). Disinfection, sterilization and preservation. 5th edition. Lippincott Williams & Wilkins, Philadelphia and London.

Courvalin P, Leclercq R and Rice L.B (2010). Antibiogram. ESKA Publishing, ASM Press, Canada.

Denyer S.P., Hodges N.A and Gorman S.P (2004). Hugo & Russell’s Pharmaceutical Microbiology. 7th ed. Blackwell Publishing Company, USA. Pp.152-172.

Ejikeugwu Chika, Iroha Ifeanyichukwu, Adikwu Michael and Esimone Charles (2013). Susceptibility and Detection of Extended Spectrum β-Lactamase Enzymes from Otitis Media Pathogens. American Journal of Infectious Diseases. 9(1):24-29.

Finch R.G, Greenwood D, Norrby R and Whitley R (2002). Antibiotic and chemotherapy, 8th edition. Churchill Livingstone, London and Edinburg.

Russell A.D and Chopra I (1996). Understanding antibacterial action and resistance. 2nd edition. Ellis Horwood Publishers, New York, USA.

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