Antifungal (Antimycotic) Drugs

BY
KENNETH CHISAMANGA
PHARMACIST
 These are drugs that are used for treatment of
different fungal infections.
 They are categorised into five of the following
basic group:
a. Polyene
b. Antimetabolite
c. Synthetic Triazoles
d. Imidazole
e. Superficial Antifungal
A. AMPHOTERICIN B
 This drug potency has made it the most widely
used antifungal agent for severe systemic
fungal infection.
 After intravenous (I.V) administration ,
Amphotericin B is distributed through out the
body and excreted by the kidneys.
 Again after I.V. Amphotericin B has immediate
onset of action.
 These irreversibly binds to STEROLS in the
membranes of the fungal cell and produces
pores or channels that increase cell membrane
permeability.
 The permeability allows leakage of intracellular
components, which prevent the fungal cell
from functioning normally as barrier.
 Amphotericin B usually acts as a
FUNGISTATIC agent but can become
FUNGICIDAL if it reaches high concentration
in the fungi.
 Severe Systemic Fungal infections
 Meningitis
 Others include candida, Paracoccidioides
brasiliensis, Blastomyces dermatitidis etc.
 Amphotericin B therapy usually begins with a
test dose that is increased daily until the
desired dosage is reached.
 Duration of therapy depends on the maturity
and severity of the infection.
 Life-threatening systemic fungal infections and
Meningitis, 0.25mg to 1mg/kg I.V. daily
infused over 4 to 6 hours.
 OR you may give, 1.5mg/kg every other day.
 Nephrotoxicity (Use Lyofilised Amphotericin B
in case of toxicity or suspected toxicity).
 Hypokalemia
 Abdominal pain
 Hypersensitivity reaction
 Chills, fever, anorexia and joint pain
 headache
1. Refridgerate Amphotericin B until it is used.
2. Dilute Amphotericin B for infusion or injection
in a dextrose 5% in water solution with pH
greater than 4.2 or in sterile water. The drug is
not compatible with electrolyte solution.
3. Shake the vial vigorously for at least 3 minutes
before administration to assure particle
dispersion.
4. Do not administer the solution if it contains
precipitate.
5. Monitor the patient’s Blood Urea Nitrogen
(BUN) and serum creatinine levels before
beginning therapy, every other day during initial
therapy, and once every week after the optimal
dosage is reached.
6. Monitor the patient’s fluid intake and output,
and observe for signs of nephrotoxicity.
7. Always cover the Amphotericin B in the
infusion set with a cloth to avoid ultraviolet rays.
 Nystatin is used only orally or topically to treat
local infections because it is extremely toxic
when administered parenterally.
 Oral Nystatin undergoes little or no absorption,
distribution, or metabolism.
 Nystatin binds to the STEROLS in fungal cell
membranes and alters the permeability of the
membranes, leading to loss of essential cell
components.
 It can act as fungicidal or fungistatic agent
depending on the organism present.
 Used primarily to treat fungal skin infections.
 The drug is effective against Candida albicans,
C. guillier-mondii and other Candida.
 Topical Nystatin is used to treat cutaneous or
mucocutaneous candidal infection, such as oral
thrush, diaper rash, vulvovaginitis
 Oral Nystatin is used to treat intestinal
candidiasis and may be used as an adjunct to
vaginal application in treating vulvovaginitis.
 Diarrhoea
 Abdominal pain
 Bitter Taste
 Skin irritation
 Hypersensitivity
DOSE
 500,000IU either tid or qds orally (Adult)
 100,000IU inserted vaginally once or twice

daily for 14 days.
1. Monitor for diarrhoea, nausea, vomiting and
abdominal pain in patient receiving high doses
of Nystatin.
2. Inspect the patient’s skin regularly for signs of
irritation. Expect to discontinue the drug if
skin irritation occurs.
FLUCYTOSINE
 This is the only Antimetabolite with Antimycotic
activities.
 It is used primarily with another antimycotic agent
such as Amphotericin B to treat systemic fungal
infection.
MoA
 It penetrates fungal cells where it is converted to its
active metabolite FLUOROURACIL, a metabolic
antagonist.
 Fluorouracil then is incorporated into the RNA of the
fungal cells, altering their protein synthesis and
causing cell death.
 It is used in combination with Amphotericin B
to reduce the dosage and risk of toxicity.
 The combination therapy is the treatment of
choice for cryptococcal meningitis.
 Flucytosine can be used alone to treat lower
urinary tract candida infections because it
reaches high urinary concentration.
 It can also be used effectively to treat infections
caused by T. glabratta, Phialophora, Asergillus
and Cladosporium.
 Bone Marrow Suppression which occurs when
the Flucytosine concentration
exceeds100mcg/ml may lead to leukopenia,
thrombocytopenia, Anaemia etc.
 Abdominal distention, diarrhoea and anorexia
 Hepatoxicity
 Increased BUN and creatinine levels
 Crystaluria, Azotemia
 Renal Failure
 Adult: 50mg to 150mg/kg P.O. daily in four
equally divided doses and administered every
6 hours.
1. Monitor the patient’s fluid’s intake and
output. Notify the primary health Care
provider if the patient develops Azotemia,
crystaluria, or decreased urine output, all of
which may indicate renal failure.
2. Monitor also the patient’s hematologic values,
liver function test and the BUN and creatine
levels. Notify the doctor if test resultsare
abnormal.
3. Inspect patient’s skin for rash which may
indicate hypersensivity.
FLUCONAZOLE
 It is broad spectrum bistriazole antifungal.
 After oral administration, about 90% is absorbed

and distributed into all body fluids while 80% of
the drug is excreted unchanged in urine.
MoA
 A selective inhibitor of fungal cytochrome P450
and sterol C-14 alpha – demethylation.
 It causes fungal cell to lose normal sterols, thereby
promoting cell death.
 To treat Oropharyngeal and Oesophargeal
candidiasis and serious systemic candidal
infections, including urinary tract infection,
peritonitis and pneumonia.
 It can also be used to treat cryptococcal
meningitis.
 Dizziness
 Diarrhoea
 Rash
 Hypokalemia
 Increased BUN and Creatinine Levels
 Transient elevation of Aspartate
aminotransferase (AST), Alanine
Aminotransferase (ALT), Alkaline phosphatase
and Bilirubin levels.
 Adult: 400mg P.O or I.V. on the first day,
followed by 200mg daily for 2 weeks
 Monitor the patient who develops rash; be
prepared to discontinue treatment if symptoms
continues.
 Do not administer an I.V. infusion of greater
than 200mg/hour by continuous infusion.
 Monitor Hydration if the patient experiences
Nausea and Vomitting or diarrhoea.
Administer an antiemetic or antidiarrhoea
agent as needed.
Examples of drugs under this group include:
 Ketoconazole
 Clotrimazole
 Miconazole
 Itraconazole
 Econazole
 This is the Broad spectrum antimycotic drug
which is more effective orally.
 It undergoes extensive hepatic metabolism and
is excreted through the bile and faeces
MoA
It interferes with STEROL synthesis, damaging
the cell membrane and increasing its
permeability.
 Hepatotoxicity
 Dermatitis
 Insomia
 Dizziness
 Rash
 Impotence
 Pruritus
 etc
 200mg to 400mg p.o. once daily or twice
NURSING APPLICATION
 Monitor the patient’s liver function test
 Administer it on an empty stomach to promote

absorption
 Do not administer it with drugs that decreases
gastric acidity such as antiacids and
anticholinergics.
GRISEOFULVIN
 This comes as an oral tablet or capsule of either
125mg/ tablet or 250mg/tablet and 500mg.
USES
 Fungal infections of the skin, scalp, hair and
nails where topical treatment has failed or is
inappropriate.
 Adult: 0.5 – 1g (but not less than 10mg/kg)
daily with food in single or divided doses.
 Child: 10mg/kg daily with food in single or
divided doses.
NOTE.
 Duration of treatment depends on the infection
and thickness of keratin at the site of infection.
At least 4 weeks for skin and hair: at least 6
weeks for scalp ringworm and in severe
infection upto 3 months; 6 months for
fingernails and 12 months or more for toenails.
 Diarrhoea
 Dry Mouth
 Peripheral neuropathy
 Confusion and impaired coordination
 Toxic epidermal necrolysis
 Hepatic and renal impairement.
 Closely monitor hepatic function throughout
treatment.
 Monitor blood count weekly during the first
month of treatment
 Avoid pregnancy during and for 1 month after
treatment; men should not father children
within 6 months of treatment

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 100,000IU inserted vaginally once or twice

 After oral administration, about 90% is absorbed

 Administer it on an empty stomach to promote

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