Name

Adverse Effects
Infusion-related
toxicity
Chills, muscle
spasms,
hypotension
Lowering infusion
rate may relieve
symptoms

Amphotericin B
(AmB)

Nystatin

Cumulative-related
toxicity
Nephrotoxicityazotemia (high
concentration of
nitrogen containing
compounds, such
as urea) and
reduced
Erythropoietin
production may
lead to anemia.
Arachnoiditis with
serious sequelae in
intrathecal therapy.
Little toxicity when

Polyenes
Indications
Drug of choice for
most severe and lifethreatening fungal
infections.
Initial induction
regimen drug before
azoles for
immunocompromised
patients, fungal
pneumonia, severe
cryptococcal
meningitis, and histoand coccidiomycoses.
In drops and topical
solution for eye and
skin mycoses.

Drug Int.

Other

Poor GI
absorption
15 day half-life
Poor CSF
penetration

Broadest spectrum
antifungal
Binds ERGOSTEROL
in fungal
membrane, forms
pores that allow ion
leakage.
Slow IV infusion

Inhaled for prophylaxis

in neutropenic lung
transplant patients
Nebulized AmB used in
allergic
bronchopulmonary
aspergiloses (ABPA)
Used in mycosis of the

Too toxic for

used TOPICALLY or
ORALLY. BAD
TASTE.

Name

Ketoconazole

Used topically for

Greater propensity
tinea versicolor and
than other azoles to
seborrheic
inhibit mammalian
dermatitis
CytP450.

Rare

Name

parenteral
administration

Azoles
Imidazoles (2 N atoms in azole ring)
Adverse Effects
Indication

Miconazole

Clotrimazole

stratum corneum of
the skin, the cornea,
and squamous
mucosa.

Drug Int.

Poor CSF
penetration

Vulvovaginal
candidiasis
Vulvovaginal
candidiasis

Available as oral
troches for oral
thrush
Triazoles (3 N atoms in azole ring)
Adverse Effects
Indication

Drug Int.

Other
First oral azole.
Imidazoles are less
specific than
triazoles. Also
available in topical
cream for
superficial
infections
These are the
topical Azoles.
Useful in
dermatophytic
infections including
tinea corporis, tinea
pedis, and tinea
cruris
Other

Itraconazole

Fluconazole

Drug of choice for

Absorption
disease caused by
increased by food
dimorphic fungi
and low gastric pH.
histoplasma, and
Reduced
infections caused
bioavailability when
by blastomyces and
taken with
sporothrix.
rifamycins such as
Rifampin.
Used extensively in
treatment of
Poor CSF
deramatophytose
penetration
s.
Drug of choice in
High oral
treatment and
bioavailability.
secondary
Good CSF
prophylaxis in
penetration
cryptococcal
MENINGITIS.
LEAST EFFECT OF
ALL AZOLES ON
Most commonly
HEPATIC
used agent in
MICROSOMAL
mucocutaneous
ENZYMES
CANDIDIASIS.
In high doses
No activity against eliminates need for
aspergillus or other intrathecal AmB for
filamentous fungi.
meningitis.
Prophylactically to
reduce disease in

Widest therapeutic
index (allows for
higher dosing)
In IV is as effective
as AmB in treating
systemic
candidemia

AIDS patients and

bone marrow
transplant
recipients.

Voriconazole

Elevated hepatic
enzymes
Photosensitive
dermatitis
Visual and color
disturbances with
IV

Treatment of choice
for INVASIVE
ASPERGILLOSIS.

Less toxic than

AmB.
Hepatic elimation.
Inhibits
mammalian
CYP3A4. Need to
lower statin
dosages.

Licensed for use in

prophylaxis in
INDUCTION
CHEMOTHERAPY
Newest triazole.
FOR LEUKEMIA
Broadest
High fat meals
Posaconazole
AND BONE
spectrum
improve absorption
MARROW
member of
TRANSPLANTS IN
azoles.
GVHD.
Effective against
most species
ALL AZOLES FUNCTION AS INHIBITORS OF FUNGAL CYT P450 AND PREVENT THE SYNTHESIS OF ERGOSTEROLS.

Name

Adverse Effects

Flucytosine (5-FC)
Indications

Drug. Int

Other

Activity restricted to
C. neoformans, some
Candida species and
molds that cause
chromoblastomycosis.
Flucytosine

BONE MARROW
TOXICITY.
Toxic enterocolitis

Given with AmB for

CRYPTOCOCCAL
MENINGITIS.
Given with
Itraconazole for
CHROMOBLASTOMYC
OSIS

Good penetration
into CSF
Kidney excretion
AmB-creats pores
through which 5FC can enter,
increasing its
uptake into fungal
cells.

Converted
intracellularly to its
active metabolites
which inhibit DNA
(FdUMP) and RNA
(FUTP) synthesis,
human cells dont
make these
metabolites, not
toxic to them.

Echinocandins
Name

Adverse Effects

Indications

Caspofungin

When combined
with cyclosporin
there have been
cases of elevated
liver enzymes

Disseminated mucocutaneous
candida.
For invasive aspergillosis ONLY
IN PATIENTS WHO DONT
RESPOND TO AmB.

Drug
Int.
Water
soluble
, highly
protein
bound.
Excret
ed in
urine
and

Other

feces
Increases levels of
Mucocutaneous candidiasis,
11-15
cyclosporine,
candidemia, and for prophylaxis
Micafungin
hr half
nifedipine and
for candida in bone marrow
life
sirolimus
transplant patients.
Histamine release
24-48
Anidulafungi
Esophageal and invasive
may occur during
hour
n
candidiasis and candidemia
IV administration
half life
INHIBIT SYNTHESIS OF 1,3-GLUCAN IN THE FUNGAL CELL WALL. CELLS DIE BY OSMOTIC LYSIS. LOW ORAL
BIOAVAILABILITY, HIGHLY PROTEIN BOUND, NO CSF PENETRATION. NO ORAL ADMINISTRATION, JUST
PARENTERAL

Name
Griseofulvin

Adverse Effects
Leukopenia,
neutropenia,
monocytosis and
hepatitis.
Estrogen-like
effects have been
observed in
children

Other Antifungal Drugs

Indications
Drug Int.
Only use in
Given in a
treatment of
crystalline for at 1
dermatophytosis
g/d
Microsporum,
Tricophyton,
Epidermophyton

Improved
absorption with
fatty foods.

FOR TINEA CAPITIS

Induces CYPs,

Other
Inihibits microtubule function
formation of mitotic spind
(Fungistatic)

Binds tightly to keratin distribu

to those areas, therefore, skin
are usually the areas to be fun
first.

in children it is the
drug of choice

Terbinafine

Tolfnaftate
(Tinactin)

Naftifine (Naftin)

Rare toxic effects,

rash headache, etc.

Used in the
treatment of
dermatophytosis,
particularly
ONYCHOMYCOSIS.
Available as topical
cream for tinea
pedis (Lamisil)
Useful in treating
NONCANDIDAL
cutaneous
mycoses.
Useful for tinea
versicolor and
cutaneous
candidiasis (topical
cream)

increasing
elimination of
warfarin and
phenobarbital.

Binds to keratin, but it is fung

Inihibits SQUALENE EPOXIDASE,
accumulation of squalene, a
intermediate.

TOPICAL ALLYLAMINES