Dr.Muhammad Fahd Mushtaq

1. ANTIFUNGAL DRUGS
Dr. Muhammad Fahd Mushtaq
M.Phil pharmacology (GCUF)

2. Antifungal Drugs
• Infectious diseases caused by fungi are called mycoses, Many common
mycotic infections are superficial and only involve the skin (cutaneous
mycoses), but fungi may also penetrate the skin, causing subcutaneous
infections.
Classification
• Antibiotics
A. Polyenes: Amphotericin B (AMB), Nystatin, Hamycin
B. Echinocandins:Caspofungin, Micafungin, Anidulafungin
C. Heterocyclic benzofuran: Griseofulvin
2. Antimetabolite Flucytosine (5-FC)
3. Azoles
A. Imidazoles
Topical: Clotrimazole, Econazole, Miconazole, Oxiconazole
Systemic: Ketoconazole

3. • B. Triazoles: Fluconazole,
• (systemic) Itraconazole,
• Voriconazole,
• Posaconazole
• 4. Allylamine Terbinafine
• 5. Other topical agents
• Tolnaftate, Undecylenic acid, Benzoic acid,

4. POLYENE ANTIBIOTICS
Amphotericin B
M.O.A

5. Antifungal spectrum
• Candida albicans, Histoplasma capsulatum, Cryptococcus
neoformans, Blastomyces dermatitidis, Coccidioides immitis,
Torulopsis, Rhodotorula, Aspergillus, Sporothrix.
Adverse effects
Fever, chills,tachypnea, Nephrotoxicity, hypokalemia and
hypomagnesemia

6. Nystatin
SAME m.o.a like amphotericin B
• It is too toxic for parenteral administration and is only used topically.
Nystatin is currently available in creams, ointments, suppositories, and
other forms for application to skin and mucous membranes nystatin
little toxicity, although oral use is often limited by the unpleasant taste.
• indications include oropharyngeal thrush, vaginal candidiasis, and
intertriginous candidal infections.
ECHINOCANDINS
Caspofungin
• active mainly against Candida and Aspergillus. Strains of candida that
have become resistant to azoles are susceptible to caspofungin

7. M.O.A
• Echinocandins act at the level of the fungal cell wall by inhibiting the
synthesis of β(1–3)-glucan . This results in disruption of the fungal cell
wall and cell death.
• Clinical Uses
candida infections, febrile neutropenia, aspergillosis
A.D.R’S
• Minor gastrointestinal side effects and flushing and pruritis.

8. Griseofulvin
Griseofulvin is fungistatic for most dermatophytes
• mechanism of action at the cellular level is unclear, but it is deposited in newly forming skin
where it binds to keratin, protecting the skin from new infection. Because its action is to
prevent infection of these new skin structures,
• Adverse effects
• allergic syndrome much like serum sickness, hepatitis,
HETEROCYCLIC BENZOFURAN

9. Antimetabolite
Flucytosine
• synthetic pyrimidine antimetabolite that is often used in combination
with amphotericin B. This combination of drugs is administered for the
treatment of systemic mycoses and for meningitis caused by
Cryptococcus neoformans and Candida albicans.
M.O.A

10. Antifungal spectrum
• is effective in combination with itraconazole for treating
chromoblastomycosis and in combination with amphotericin B for
treating candidiasis or cryptococcosis.
• Resistance
• Resistance due to decreased levels of any of the enzymes in the
conversion of 5-FC to 5-fluorouracil (5-FU) and beyond, or increased
synthesis of cytosine, can develop during therapy.
Adverse effects
bone marrow depression, gastrointestinal disturbances, Liver
dysfunction, enteritis and diarrhoea

11. Imidazoles and Triazoles
The imidazoles and triazoles have broadspectrum antifungal activity
covering dermatophytes, Candida, other fungi involved in deep mycosis
(except mucor), Nocardia and Leishmania.
M.O.A

12. Resistance
• reduction of ergosterol synthesis by inhibition of fungal cytochrome
P450 enzymes.
Adverse effects
• abnormalities in liver enzymes and, very rarely, clinical hepatitis.
Allylamine
Terbinafine
• used in the treatment of dermatophytoses, especially onychomycosis
• M.O.A
• inhibits the fungal enzyme squalene epoxidase. This leads to the
accumulation of the sterol squalene, which is toxic to the organis