Clotrimazole

Clotrimazole

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The Clotrimazole is an antifungal medication belonging to the imidazole and triazole classes. It was introduced in 1975 under the brand name Mycelex. By inhibiting cytochrome P450 14α-demethylase, a key enzyme responsible for converting lanosterol to ergosterol, clotrimazole effectively blocks the synthesis of the fungal cell membrane. This disruption of cell membrane synthesis is the mechanism behind its antifungal effects.

Mechanism of Action

The primary action of clotrimazole involves the inhibition of cytochrome P450 14α-demethylase. This enzyme is responsible for converting lanosterol to ergosterol, an essential component of the fungal cell membrane. By inhibiting this conversion process, clotrimazole disrupts the synthesis of the cell membrane, leading to impaired growth and function of the fungi.

Types of Imidazole and Triazole Antifungals

The family of imidazole and triazole antifungals includes various drugs, all possessing a similar mechanism of action.

• Imidazoles: Apart from clotrimazole, another commonly used imidazole is ketoconazole (Nizoral), introduced in 1981.
• Triazoles: The triazoles, known for excellent oral absorption, tolerance, and tissue penetration, include fluconazole (Diflucan), itraconazole (Sporanox), posaconazole (Noxafil), and voriconazole (Vfend).

Prodrugs in Antifungal Therapy

Some triazole antifungals, such as isavuconazonium (Cresemba), are available as prodrugs. Introduced in 2016, isavuconazonium is a prodrug of isavuconazole, and it is available in both intravenous and oral forms. The use of isavuconazonium is primarily restricted to severe, invasive fungal infections, such as aspergillosis and mucormycosis.

Uses of Clotrimazole

Clotrimazole is typically used in the treatment of various fungal infections, including oral thrush, candidiasis, ringworm, and athlete's foot. It is also commonly used for the treatment of jock itch and yeast infections.

Side Effects

Side effects of clotrimazole are generally mild and can include skin irritation, stinging, swelling, or redness at the application site. In rare cases, it can cause an allergic reaction.

See Also

• Imidazole
• Triazole
• Antifungal medication
• Cytochrome P450

References

• Dailymed label info on Clotrimazole
• FDA Clotrimazole

Clotrimazole Resources
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