ANTIFUNGALS

Although their mechanisms of action differ slightly, antifungals

often interfere with lipid biosynthesis and therefore the
integrity of the fungal membrane (Fig. 4-8). A variety of antifungals
are used to treat fungal infections, depending on
whether the infection is cutaneous or systemic. Major antifungals
include the polyenes (amphotericin B, nystatin) and the
azoles (voriconazole, ketoconazole, and fluconazole).

Polyenes

Amphotericin B
Mechanism of action
Amphotericin B is an example of a polyene type of antifungal.
Polyenes bind to fungal ergosterol (the primary sterol in
fungal cell membranes). This alters cell membrane permeability,
and intracellular components leak from the cell. Depending
on the concentration attained in the body, amphotericin B
can be either fungistatic or fungicidal.
Pharmacokinetics
Amphotericin B does not penetrate the central nervous system
well. This drug has a very long t.
Clinical use
Amphotericin B may be used to treat serious, life-threatening
systemic fungal infections. It is administered intravenously or
intrathecally for systemic fungal infections including systemic
Adverse effects
Numerous toxicities are attributed to amphotericin B
(Box 4-11). Serum creatinine, blood urea nitrogen, complete
blood counts, serum potassium, serum sodium, serum magnesium,
and liver function test results must be monitored. When
amphotericin B is used with aminoglycosides or neuromuscular
blockers, prolonged skeletal muscle paralysis may result.