Mucosal Candidiasis Medication

Updated: Aug 28, 2017
  • Author: Surbhi Gupta; Chief Editor: William D James, MD  more...
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Medication

Medication Summary

The goals of pharmacotherapy are to reduce morbidity and to prevent complications.

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Azoles

Class Summary

Azoles are synthetic antifungals with broad-spectrum fungistatic activity against yeasts and fungi, including candidal species. By blocking fungal cytochrome P450-dependent enzymes, azoles disrupt the synthesis of ergosterol, which is the principal sterol in fungal cell membranes. The two subclasses of azoles are imidazoles (eg, clotrimazole, miconazole, econazole, ketoconazole) and triazoles (eg, fluconazole, itraconazole).

The most common adverse effect of topical azoles is local skin and mucous membrane irritation. The most common adverse effects of systemic azoles are gastrointestinal distress, morbilliform rash, and hepatotoxicity. Most azoles have additional adverse effects specific to each drug, and these are listed below. Diazoles (eg, ketoconazole, miconazole) have a stronger effect on human cytochromes than triazoles (eg, fluconazole, itraconazole) and therefore tend to have more severe adverse effects.

Azoles are effective antifungals, but resistance is occasionally reported. Development of cross-resistance of C albicans to different azoles during treatment with a single azole derivative has been described.

Clotrimazole (Lotrimin, Mycelex, Femizole, Gyne-Lotrimin)

Clotrimazole is available as topical therapy. As a 10-mg troche, clotrimazole is effective against oral candidiasis in some patients who are immunocompromised. It is less effective than other azoles in patients with HIV infection. 

Fluconazole (Diflucan)

Fluconazole is available as systemic therapy. Compared with other azoles, it has lower toxicity while maintaining a half-life of 30 hours in patients with normal renal function. Fluconazole is active against most C albicans, although resistance is occasionally seen. It is less active against other species, such as C glabrata, and it has no activity against C krusei.

Itraconazole (Sporanox)

Itraconazole is available as systemic therapy. Itraconazole is active against all Candida species. Therefore, it may be advantageous in patients who are immunocompromised and in whom other antifungals may predispose to selection and overgrowth of resistant species. It may interact with terfenadine, astemizole, and cisapride to produce dysrhythmias and to increase the activity of anticoagulants, cyclosporine, midazolam, and sulfonylureas. Adverse effects include hepatotoxicity, hypokalemia, and peripheral neuropathy.

Voriconazole (Vfend)

Voriconazole is available as systemic therapy. It is effective against organisms that demonstrate resistance to fluconazole, including C krusei. The associated adverse effects include phototoxicity, arrhythmia, and visual disturbances.

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Polyenes

Class Summary

This class of antifungals includes the drugs amphotericin B and nystatin. Amphotericin B is available as a systemic therapy, and nystatin is available as topical therapy. Polyenes irreversibly bind to the cell membrane sterol, ergosterol, causing disruption by increasing cell membrane permeability. They are fungistatic at low concentrations and become fungicidal at higher concentrations.

Amphotericin, in particular, is notorious for its adverse effects. It can cause fevers, electrolyte disturbances, nephrotoxicity, arrhythmias, as well as a number of skin eruptions. Severe reactions from amphotericin include seizures, agranulocytosis, and hepatotoxicity.

Amphotericin B deoxycholate (Amphotericin B (conventional), Fungizone)

This is one of the oldest antifungals and has been in use for more than 40 years; it is the criterion standard of antifungal therapy. Lipid formulations have been developed. The total dose must be adjusted depending on the type of candidal infection being treated. Most patients receive a total dose of 0.5-1.5 g.

Nystatin (Mycostatin, Nilstat, Nyamyc)

This is a fungicidal and fungistatic antibiotic obtained from Streptomyces noursei. It is effective against various yeasts and yeastlike fungi. It changes the permeability of the fungal cell membrane after binding to cell membrane sterols, causing cellular contents to leak. Membrane channel activity is increased at lower doses, and pores are formed at higher concentrations.

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