GRISEOFULVIN: CLINICAL USE & MECHANISM OF ACTION

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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. 

CLINICAL APPLICATION OF GRISEOFULVIN

Griseofulvin is mainly used to treat superficial mycoses caused by dermatophytes. And the antifungal agent 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 (Figure 1) 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. 

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

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

Anaissie E.J, McGinnis M.R, Pfaller M.A (2009). Clinical Mycology. 2nd ed. Philadelphia, PA: Churchill Livingstone Elsevier. London.

Baumgardner D.J (2012). Soil-related bacterial and fungal infections. J Am Board Fam Med, 25:734-744.

Calderone R.A and Cihlar R.L (eds). Fungal Pathogenesis: Principles and Clinical Applications. New York: Marcel Dekker; 2002.

Champoux J.J, Neidhardt F.C, Drew W.L and Plorde J.J (2004). Sherris Medical Microbiology: An Introduction to Infectious Diseases. 4th edition. McGraw Hill Companies Inc, USA.       

Gladwin M and Trattler B (2006). Clinical Microbiology Made Ridiculously Simple. 3rd edition. MedMaster, Inc., Miami, USA.

Larone D.H (2011). Medically Important Fungi: A Guide to Identification. Fifth edition. American Society of Microbiology Press, USA.

Madigan M.T., Martinko J.M., Dunlap P.V and Clark D.P (2009). Brock Biology of Microorganisms, 12th edition. Pearson Benjamin Cummings Inc, USA.

Stephenson S.L (2010). The Kingdom Fungi: The Biology of Mushrooms, Molds and Lichens. First edition. Timber Press.

Sullivan D.J and Moran G.P (2014). Human Pathogenic Fungi: Molecular Biology and Pathogenic Mechanisms. Second edition. American Society of Microbiology Press, USA.

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