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Wednesday, 22 June 2016

ANTIFUNGAL AGENTS-PART-III-Continued...

ANTI-FUNGAL AGENTS

In this post, we will see some antifungal agents which are used only for superficial infections. These agents are meant for external as well as internal use.

1.Griseofulvin:-

Griseofulvin is practically insoluble in water.
Griseofulvin inhibits fungal growth in vitro and hence it is fungistatic. It is acting in vitro against dermatophytes, Microsporum, Epidermophyton, and Trichophyton. The drug has no effect against bacteria or other fungi which cause systemic infections.
Resistance is developed frequently against ringworm infections.
Griseofulvin enters into the fungal cell and impairs the microtubule functions. In long term therapy, this drug accumulates in the newly synthesized outer protective layer of the human epidermis (stratum corneum) and making the skin undesirable for the fungus and inhibits its growth.
Kinetics
Griseofulvin is absorbed well orally. Griseofulvin should be taken with high fatty food for good intestinal absorption. It is well distributed in the keratin containing stratum corneum of the epidermis.
It is metabolized in the liver and excreted in bile.
Side effects
1.Headache
2.Liver damage
3.Nausea, vomiting, and diarrhea. 

2.Nystatin:-

Similar to amphotericin-B nystatin is also a polyene derivative with similar action.
Nystatin is meant only for topical use.
It is used for local Candida infections. 

3.Miconazole, Econazole, and Clotrimazole:-

These are the drugs available for external use only.
They are widely used only for skin infections.
In all aspects, structure, chemistry, and mechanism of actions, they are very similar to ketoconazole. 

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