QUESTIONS AND ANSWERS
azoles: a group of drugs used to treat fungal infections
Candida: fungus that is normally found on mucous membranes; can cause yeast
infections or thrush of the gastrointestinal (GI) tract and vagina in
immunosuppressed patients; can cause serious systemic infection that can affect
multiple organs in the body
fungus: a cellular organism with a hard cell wall that contains chitin and many
polysaccharides, as well as a cell membrane that contains ergosterols
AZOLE ANTIFUNGALS
fluconazole
OTHER ANTIFUNGALS
amphotericin B
nystatin
An infection caused by a fungus is called a mycosis. Fungi differ from bacteria in
that a fungus has a rigid cell wall that is made up of chitin and various
polysaccharides and a cell membrane that contains ergosterol, which is a steroid-
type protein similar in configuration to adrenal hormones and testosterone. The
composition of the protective layers of the fungal cell makes the organism
resistant to antibiotics. Conversely, because of their cellular makeup, bacteria are
resistant to antifungal drugs.
,The incidence of fungal infections has increased with the rising number of
immunocompromised individuals—patients with AIDS and AIDS-related complex;
those taking immunosuppressant drugs; people who have undergone
transplantation surgery or cancer treatment; and members of the increasing older
adults population, whose bodies have diminished protection from the many fungi
that are found throughout the environment.
For example, Candida, a fungus that is normally found on mucous membranes,
can cause yeast infections or “thrush” in the gastrointestinal (GI) tract and yeast
infections or “vaginitis” in the vagina. Candida can also cause serious systemic
infections affecting multiple organs in the body.
The azoles are a large group of antifungals used to treat systemic and topical
fungal infections.
The azoles include fluconazole (Diflucan), itraconazole (Sporanox), ketoconazole
(Nizoral), posaconazole (Noxafil), voriconazole (Vfend), and isavuconazonium
(Cresemba).
Although azoles are considered less toxic than some other antifungals, such as
amphotericin B, they may also be less effective in very severe and progressive
infections.
Older Adults
Older patients may be more susceptible to the adverse effects associated with
these drugs and should be monitored closely.
Patients with hepatic dysfunction are at increased risk for worsening hepatic
problems and toxic effects of many of these drugs (ketoconazole, itraconazole,
, griseofulvin). If hepatic dysfunction is expected (extreme age, alcohol abuse, use
of other hepatotoxic drugs), the dose may need to be lowered and the patient
monitored more frequently.
Other agents are associated with renal toxicity (amphotericin B, flucytosine,
griseofulvin); these should be used cautiously in the presence of renal
impairment. Patients at risk for renal toxicity should be monitored carefully. With
fluconazole, the dose should be reduced in the presence of renal dysfunction to
prevent adverse effects related to accumulation of the medication.
Azoles bind to sterols and can cause cell death (a fungicidal effect) or interfere
with cell replication (a fungistatic effect), depending on the type of fungus being
affected and the concentration of the drug.
Ketoconazole, fluconazole, and itraconazole work by blocking the activity of a
sterol in the fungal wall.
In addition, they may block the activity of human steroids, including testosterone
and cortisol.
Older Adults
Older patients may be more susceptible to the adverse effects associated
with Azoles and should be monitored closely.
Patients with hepatic dysfunction are at increased risk for worsening hepatic
problems and toxic effects of many of these drugs (ketoconazole, itraconazole,
griseofulvin). aIf hepatic dysfunction is expected (extreme age, alcohol abuse,
use of other hepatotoxic drugs), the dose may need to be lowered and the patient
monitored more frequently.