ANTIFUNGALS

Presented To :Dr.Prof. Saeedullah khattak

                             Presented by:  zunaira saeed 
               Noor E Sahar Awan
           Hannah Siddiqui
Sana Kamal
     Omyma Sajjad
Sidra Sher
Microbiology 5th (morning)
Center of Biotechnology and Microbiology
POLYENE ANTIFUNGALS
• Polyene antifungals are the only which directly targets the cell
membrane by interacting with fungal sterol I.e ergosterol.
• It includes
A. Amphotericin Click to add text

B. Nystatin
C. Hamcyin
AMPHOTERICIN B
Obtained from streptomyces nodosus
Classification based on the mechanism of
action
• Fungal cell wall synthesis inhibition: Caspofungin
• Bind to fungal cell membrane ergosterol: Amphotericin-B, Nystatin
• Inhibition of ergosterol synthesis: Terbinafine, Naftatine, Azoles
• Inhibition of Nucleic acid : Flucytosine
• Disruption of mitotic spindle and inhibition of fungal mitosis:
Griseofulvin
• Miscellaneous: undecylenic acid, topical azoles
IMIDAZOLES
Imidazoles consists of two nitrogen in structure.
It includes two categories 
• Topical antifungals
• Systemic antifungals
TOPICAL ANTIFUNGALS
It consists of 
• Miconazole
• Clotrimazole
• Oxinazole
• econazole
SYSTEMIC ANTIFUNGAL
• Ketoconazole
MICONAZOLE AND CLOTRIMAZOLE
USES : these are used for dermatophyte infections
Candida infections of vaginal, cutaneous ,oral pharyngeal
ADVERSE EFFECTS:
Local irritation, itching, burning.
ECHINOCANDINS
•  Inhibit beta-(1,3)-D-glucan synthase, an enzyme that is necessary for
the synthesis of an essential component of the cell wall of several
fungi.
•  efficacious for the treatment of esophageal candidiasis, candidemia,
and invasive candidiasis.
• It includes:
• Caspofungin
• Micafungin
• anidulafungin
CASPOFUNGIN
• Caspofungin (caspofungin acetate) is a semi-synthetic water-soluble
lipopeptide produced from a fermentation product of the
fungus Glarea lozoyensis.
• Caspofungin inhibits the synthesis of beta-(1,3)-D-glucan, an
essential component of Click
thetocell wall of Aspergillus species
add text

and Candida species. beta-(1,3)-D-glucan is not present in

mammalian cells. The primary target is beta-(1,3)-glucan synthase.
•  It is typically administered intravenously.
•  92% tissue distribution within 36-48 hours after intravenous infusion.
MICAFUNGIN
• Micafungin is a semisynthetic lipopeptide synthesized from a fermentation
product of Coleophoma empetri that works as an antifungal agent.
• Micafungin is used to treat infections caused by the Candida fungus.
Micafungin is also used to prevent Candida fungal infections in stem cell
transplant patients. Micafungin is for use in adults and children who are at
least 4 months old.
• Micafungin can be used concomitantly with a variety of other drugs,
including the HIV protease inhibitor ritonavir and the transplant
medications cyclosporine and tacrolimus.
• Micafungin is injected into a vein through an IV. 
ANIDULAFUNGIN
• Anidulafungin is a semi-synthetic lipopeptide synthesized from a
fermentation product of Aspergillus nidulans.
• For use in the treatment of the following fungal infections:
Candidemia and other forms of Candida infections (intra-abdominal
abscess, and peritonitis), Aspergillus infections, and esophageal
candidiasis.
•  Also considered an alternative treatment for oropharyngeal
canaidiasis
HETEROCYCLIC BENZOFURAN
• GRISEFULVIN
• Griseofulvin is a mycotoxic metabolic product of Penicillium spp. It was the
first available oral agent for the treatment of dermatophytoses.
•  Griseofulvin is fungistatic. It is thought to inhibit fungal cell mitosis and
nuclear acid synthesis.
•  It also binds to and interferes with the function of spindle and cytoplasmic
microtubules by binding to alpha and beta tubulin.
•  It binds to keratin in human cells, then once it reaches the fungal site of
action, it binds to fungal microtubes thus altering the fungal process of
mitosis.
• For the treatment of ringworm infections of the skin, hair, and nails, namely:
tinea corporis, tinea pedis, tinea cruris, tinea barbae, cradle cap or other
conditions caused by Trichophyton or Microsporum fungi.
ANTIMETABOLITE
   FLUCYTOSIN
• Flucytosine is an antimetabolite that acts as an antifungal agent with in
vitro and in vivo activity against Candida and Cryptococcus.
•  Flucytosine enters the fungal cell via cytosine permease; thus, flucytosine
is metabolized to 5-fluorouracil within fungal organisms. The 5-fluorouracil
is extensively incorporated into fungal RNA and inhibits synthesis of both
DNA and RNA. The result is unbalanced growth and death of the fungal
organism.
• For the treatment (in combination with amphotericin B) of serious
infections caused by susceptible strains of Candida (septicemia,
endocarditis and urinary system infections) and/or Cryptococcus
(meningitis and pulmonary infections).
ALLYLAMINES
   TERBINAFINE
• Terbinafine is an allylamine antifungal that inhibits squalene
epoxidase (also known as squalene monooxygenase) to prevent the
formation of ergosterol and cause an accumulation of squalene,
weakening the cell wall of fungal cells.
• Terbinafine hydrochloride is indicated to treat fungal skin and nail
infections caused by Trichophyton species, Microsporum
canis, Epidermophyton floccosum, and Tinea species.Terbinafine
hydrochloride also treats yeast infections of the skin caused
by Candida species and Malassezia furfur.
TOPICAL ANTIFUNGALS
   TOLNAFTATE
• Tolnaftate is a topical fungicide. Though its exact mechanism unknown, it is
believed to prevent ergosterol biosynthesis by inhibiting squalene
epoxidase. It has also been reported to distort the hyphae and to stunt
mycelial growth in susceptible organisms.
• Tolnaftate topical is used to treat skin infections such as athlete's foot, jock
itch, and ringworm infections.
• Tolnaftate is also used, along with other antifungals, to treat infections of
the nails, scalp, palms, and soles of the feet. The powder and powder
aerosol may be used to prevent athlete's foot.
UNDECYLENIC ACID
• It is an unsaturated fatty acid with a terminal double bond that is
derived from castor oil.
• It is also found naturally in the human sweat. 
• Zinc undecylenate is an example of a topical antifungal agent that
treats skin infections such as athlete’s foot and relieves itching,
burning, and irritation associated with the skin condition.