it is about anti fungal drugs

1. ANTI FUNGAL AGENTS
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2. ANTI FUNGAL AGENTS
THESE ARE DRUGS USED FOR
SUPERFICIAL AND DEEP
(SYSTEMIC) FUNGAL
INFECTIONS
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3. ANTI FUNGAL AGENTS
CLASSIFICATION
1.ANTIBOITICS
POLYENES
Amphotericin B(amb)
Nystatin
Hamycin
Natamycin
HETEROCYCLIC BENZOFURAN
Grieseofulvin
2.ANTIMETABOLITES
Flucytosine (5-fc)
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4. ANTI FUNGAL AGENTS
CLASSIFICATION
3.AZOLES
IMIDAZOLES
TOPICAL : Clotrimazole,econazole,
Miconazole, Oxiconazole
Systemic : Ketaconazole
TRIAZOLES
SYSTEMIC : Fluconazole, Itraconazole
4.ALLYLAMINE
TERBINAFIN
5.OTHER TOPICAL AGENTS
Tolnaftate, Undecyclenic Acid,benzoic Acid,
Quiniodochlor, Butenafine, Sod.Thiosuphate
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5. POLYENE ANTIBIOTICS
The name polyene is derived from their highly
double-bonded structure
AMPHOTERICIN B
Obtained from STREPTOMYCES N0DOSUS
MOA :
» +
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POLYENES
ERGOSTEROL
MICROPORE
FORMATION
↑CELL
PERMIABILITY
CHOLESTROL
TOXICITY

6. AMPHOTERICIN B

7. POLYENE ANTIBIOTICS
AMPHOTERICIN B
Chemistry and MOA:
Macrocyclic ring, one side of which
has several double bond while the
other side is hydrophilic with many –
OH groups.

8. POLYENE ANTIBIOTICS
AMPHOTERICIN B

9. POLYENE ANTIBIOTICS
AMPHOTERICIN B
Cholesterol binding -with lesser
affinity.
Thus the selectivity is low.
Active Against Wide Range Of
Fungi And Yeast.

10. POLYENE ANTIBIOTICS
AMPHOTERICIN B
Uses
AMB can be applied topically for oral,
vaginal and cutaneous candidiasis and
otomycosis
Systemic mycosis
Leishmaniasis: AMB is the most
effective drug for resistant cases of
kala azar and mucocutaneous
leishmaniasis.
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11. HETEROCYCLIC BENZOFURAN
GRISEOFULVIN
It was one of the early antibiotic Extracted
from Pencillium griseofulvum. However bcoz of
lack of antibacterial activity , little attention
was paid to it.
Dermatophytes actively concentrates it
Bacterias are insensitive
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13. GRISEOFULVIN
MOA : interferes with mitosis.
It causes abnormal metaphase configuration
and daughter nuclei fails to move apart or move
only a short distance.
PK:
A: GIT absorption is poor bcoz of its very low
water solubility . Absorption is improved by
microfining the drug particles.
Now ultramicrofine particles prepn from which
absorption is still better are available.

14. P/K
D: Griseofulvin get deposited in keratin
forming cells of skin, hair and nails.
It is fungistatic and not cidal
M: Griseofulvin is largely metabolized by
methylation and excreted in urine.
P t1/2 = 24hrs
Bcoz it is fungistatic not cidal, fungi persist in
already infected keratin till it is shed off. Thus
duration of treatment is dependent upon the
site of infection, thickness of infected keratin
& its turnover rate

15. Use and Dose
Uses: It is ineffective topically
It is used orally only for Dermatophytosis
Dose: 125-250mg QID with meals
Duration depends on the site of infections(turn
over rate of keratin)
Body skin 3weeks
Palm and sole 4 – 6 weeks
Finger nails 4 – 6 months
Toe nails 8 – 12 months

16. IMIDAZOLES ANDTRIAZOLES
These are presently the most
extensively used antifungal drugs
They have broad spectrum of activity
covering dermatophytes, candida,
other fungi involved in deep mycosis.
Nocardia, some gr+ve and anaerobic
bacteria. Eg; Staph.aureus,
strep.faecalis and Leishmania.

17. IMIDAZOLES ANDTRIAZOLES
MOA: They inhibits the fungal
cytochrome P450 enzyme ‘lanosterol-
14-demethylase’ and thus impair
ergosterol synthesis leading to a
cascade of membrane abnormalities
in the fungus.
Lower host toxicity is due to its low
affinity for mammalian CYP450
enzymes.

18. IMIDAZOLES AND TRIAZOLES
KETOCONAZOLE
It is the first orally effective broad
spectrum anti-fungal drug useful in both
Dermatophytosis and deep mycosis
Oral absorption is facilitated by gastric
acidity bcoz it is more stable at lower pH
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19. IMIDAZOLES AND TRIAZOLES
KETOCONAZOLE
USES
ORAL : DERMATOPHYTOSIS, SYSTEMNIC
MYCOSIS- administered orally, but now a days
Itraconazole and fluconazole being more active
with fewer SE have largely replaced it.
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