Table 2.
Representative antifungal drugs approved by FDA. Rx: prescription drug; OTC: over-the-counter drug.
| Categories | Antifungal Drugs | Mechanism of Action | Dosage Forms | Administration Routes | Need of prescription |
|---|---|---|---|---|---|
| Polyene | Amphotericin B | Directly binds to ergosterol in the cell membrane of susceptible fungi, forms transmembrane channels, and alters the cell permeability that result in cytoplasm leakage. | Lyophilized powder with sodium desoxycholate for injection | Intravenous | Rx only |
| Lyophilized lipid-complex for injection | |||||
| Lyophilized liposomal for injection | |||||
| Nystatin | Tablet | Oral | Rx only | ||
| Suspension | |||||
| Powder | Topical | ||||
| Cream | |||||
| Ointment | |||||
| Suppository | Vaginal | ||||
| Tablet | |||||
| Natamycin | Suspension | Ophthalmic | Rx only | ||
| Azoles | Fluconazole | Selectively inhibit the fungal cytochrome P450-dependent enzyme, lanosterol 14-α-demethylase, which convert lanosterol to ergosterol. | Injection | Intravenous | Rx only |
| Tablet | Oral | ||||
| Powder for suspension | |||||
| Itraconazole | Capsule | Oral | Rx only | ||
| Solution | |||||
| Clotrimazole | Lozenge | Buccal | Rx only | ||
| Solution | Topical | OTC | |||
| Lotion | |||||
| Cream | Topical; Vaginal | ||||
| Miconazole | Tablet | Buccal | Rx only | ||
| Ointment | Topical | Rx only | |||
| Cream | Vaginal | OTC | |||
| Suppository | |||||
| Insert | |||||
| Echinocandins | Caspofungin | Noncompetitively inhibits the β-1,3-D-glucan synthase, resulted in compromised synthesis of glucan and instability of fungal cell wall. | Lyophilized powder for injection | Intravenous | Rx only |
| Micafungin | Lyophilized powder for injection | Intravenous | Rx only | ||
| Pyrimidine analogs | Flucytosine | After taken up by the fungi, it is converted to fluorouracil, and the active metabolites inhibit cellular metabolism via incorporation into RNA or inhibition of thymidylate synthetase. | Capsule | Oral | Rx only |
| Mitotic inhibitor | Griseofulvin | Inhibits the function of mitotic spindle microtubule. | Tablet | Oral | Rx only |
| Suspension | |||||
| Allylamines | Terbinafine | Inhibits the biosynthesis of ergosterol on squalene epoxidase enzyme. The accumulation of high concentrations of squalene results in increased membrane permeability. |
Tablet | Oral | Rx only |
| Granule | |||||
| Cream | Topical | OTC | |||
| Gel | |||||
| Spray solution | |||||
| tRNA synthetase inhibitor | Tavaborole | Inhibits protein synthesis by inhibition of leucyl-tRNA synthetase. | Solution | Topical | Rx only |
| Hydroxypyridone | Ciclopirox | Chelates polyvalent cations such as Fe3+ and Al3+, resulting in the inhibition of some metal-dependent enzymes related to antioxidant defense. | Gel | Topical | Rx only |
| Cream | |||||
| Suspension | |||||
| Shampoo | |||||
| Nail lacquer |