Antifungal drugs

Drugs used for treatment of fungal

infections or mycoses called as
Antifungal agents or antimycotic agents
 classification Based on chemical nature-5A& T
1) A- Allyl amines(ANT) -
Naftifine,Terbinafine
2) A-Azoles-
3) Imidazole
A-Antimetabolite- andflucytosine
(5-FC) Triazole-
4) A- Antibiotics-
a) polyenes-NAN-Nystatin,Amphotericin-B, Natamycin
b )Natural derivative- Griseofulvin
C) Echinocandins-CAM-Fungins

5) A - Acids-fatty acid- Undecylenic acid,

Topical agents - Ciclopirox,Undecylenic acid
Miscellaneous Peptide derivative- Nikkomycin
 Based on mechanism of action

1.Fungal Cell wall synthesis blockers

a)Glucan synthease inhibitors -Echinocandins–CAM
(caspofungin,Anidula fungin,Mica fungin)
b)Chitin synthease inhibitor - Nikkomycin
2. cell membrane synthesis blockers –( Ergosterol synthesis blocker)
a) By inhibiting Squalene Epoxidase enzyme- Allyl amines(ANT)
b)By inhibiting 14- alpha Demethylase enzyme- Azoles
c)By inhibiting Delta 14 reductase enzyme- Amorolfine
3. Antimiotic drug- Griseofulvin
4 Cell membrane leakagers ( cellmebrane Disruptor)
Example Polyenes – ( NAN), Nystatin, Amphotericin-B,Natamycin.
Polymyxin( antibactrial)

5.Nucleic acid synthesis blocker( antimetabolite)

Thimdylate synthease blocker- 5 FC ( flucytosine) 5-flurocytosine

6 Fungal protein synthesis blockers- TavoBorole

 1. Cell wall synthesis blockers
a) Drugs inhibiting gucan layer of fungus cell wall
Echinocandins- (CAM) -Caspofungin,Anidulafungin,Micafungin
Mechanism:

CAM inhibits glucan synthease there by prevent

formation of glucan layer of cell wall. Act as

b)bactericidal
Drugs inhibiting Chitin ( polymer of NAG) layer of fungus cell
wall
Nikkomycin inhibits chitin synthease there
by prevent formation of chitin layer of cell
wall. Act as bactericidal
Targets of antifungal drugs
2. Drugs inhibiting Ergosterol layer of fungus
cell mebrane Example-allylamines and
azoles
Squalene

Allyal amines Squalene epoxidase( ANT)

Naftifine, Terbinafine
Lanosterol

Lanosterol 14 alpha
Inhibited by
azoles demethylase
Ergosterol
Required for cell memrane rigidity
Allylamines –
Allylamines inhibits squalene epoxidase
which converts squalene to lanosterol. There by
decrease in lanosterol production, which leads to decrease
ergosterol production and affecting fungal cell
membrane synthesis and function.
Naftifine is available for topical use only in the treat-
ment of cutaneous dermatophyte and Candida infections.
Terbinafine (Lamisil®) is available for
topical and systemic use (oral tablet) in
the treatment of dermatophyte skin and
nail infections.
Antifungal Azoles( ergosterol synthesis blocker)
azoles broad-spectrum fungistatic activity .
Azoles inhibits 14 alpha demethylase enzyme so
prevent conversion of lanosterol to ergosterol
a)Imidazole s – COMET-K S
C-Clotrimazole O -Oxiconazole
M- Miconazole,E- Econazole T- Tioconazole
K- Ketoconazole
S- sertaconazole ( antiinflammatory,Antipruritic)
a)Triazole s – FIT VIP-
b)F-Fluconazole, I- Itraconazole T- Teraconazole ,
V- VoriconazoleI- Isavu conazole P-Posaconazole
3 Antifungal antibiotics
a) Antimiotic drugs
Griseofulvin is an oral fungistatic agent used
in the long-term treatment of dermatophyte infections
Produced by Penicilliumgriseofulvin,
it inhibits fungal cell mitosis
3 b) -Polyene antibiotics- (NAN)
Nystatine ,Amphotericin,Natamycin (Cellmembrane leakagers)

. Amphotericin B is a polyene antibiotic

(polyene: containing many double
bonds)
Mechanism of action
-Binding to ergosterol present in
the membranes of fungal cells

Formation of “pores” in the
membrane

Leaking of small molecules
(mainly K+) ,sugars from the
cells

- Cell death fungicidal

Amphotericin uses i.v. for treatment of Candida esopha-
gitis, cryptococcal meningitis,
Toxicity- Nephrotoxity
To reduce nephro toxicity amphotericin
formulated as liposomal amphotericin B,

Nystatin is a polyene antifungal drug with

a topical treatment of superficial
infections caused by C. albicans.
Natamycin is used as eye drops for treatment
of eye Infections
4. Anti metabolite-( nucleic acid synthesis blocker)
5 FC-fluoctosine – when enters to fungal cell converted into 5- FU (5-
flurouracil.) It is metabolized to 5Fdump which inhibits thymidylate
synthease enzyme reduce synthesis of DNA and 5 FUTP which
inhibits RNA synthesis( protein synthesis)
 Fungus cell

5-FdUMP-( 5-flurodeoxy uridine monophosphate)

5-UTP ( 5-fluro uridine triphosphate )