This document discusses various classes of anti-fungal drugs including antifungal antibiotics like polyenes such as amphotericin B and nystatin, antimetabolites like flucytosine, and azoles including imidazoles like ketoconazole and triazoles like fluconazole and itraconazole. It provides details on their mechanisms of action, effectiveness against different fungal infections, routes of administration, and common adverse effects.

1. ANTI-FUNGAL DRUGS
Yogapriya.v
B.Opt(IIIyr)

2. INTRODUCTION
• Fungal infections may be systemic and superficial
• They may occur as primary disease or secondary to treatment with
antibiotics,anticancer drugs or due to HIV infection

3. CLASSIFICATION OF ANTI FUNGAL
DRUGS
ANTIFUNGAL ANTIBIOTICS
i)POLYENES Amphotericin B
Nystatin
Hamycin
ii)OTHERS Griseofulvin
ANTIMETABOLITES Flucytosine(5 FC)
AZOLES
i)IMIDAZOLE Clotrimazole
Miconazole
Ketaconazole
Econazole
ii)TRIAZOLES Fluconazole
Itraconazole
teraconazole
ALKYLAMINES Terbinafine
OTHER TOPICAL AGENTS Tolnaftate
Benzoic acid
ciclopirox

4. AMPHOTERICIIN B
• It is a polyene antibiotic
• It is obtained from Streptomyces nodosus
• it is fungistatic at low and fungicidal at high concentration
• Amphotericin is not absorbed orally.it is given I.V and it is widely distributed
in the body
Adverse effect
• Fever,chills,muscle spasm,vomiting,hypotension and headache on I.V infusion
• Pain and thrombophlebitis at the site of injection
• Also renal impairment,neurotoxicity and anemia

5. NYSTATIN
• It is obtained from Streptomyces noursei
• It has action similar to amphotericin B
• But it is too toxicfor systemic use
• So it is used topically
• It is used in local cnandidial infections like oral thrush and vaginal candidias
HAMYCIN
• It is another polyene antibiotic
• It is used topically for cutaneous candidias and otomycosis

6. GRISEOFULVIN
• It is a fungistatic
• It is obtained from penicillium griseofulvum
• It is given orally for superficial dermatophytosis
• It acts by binding to micro tubular protein in the nucleus
• This distrupts mitotic spindle and inhibits mitosis in the fungus
• Griseofulvin is poorly water soluble
• Also bioavailability is poor microfined particles or fatty food enhance its
absorption
• It binds to keratin of the skin
Adverse effect
• Allergic reactions,hepatitis and nephrotoxicity

7. ANTIMETABOLITES
FLUCYTOSINE
• It is a fluorinated pyrimidine
• It is effective agaist Cryptococcus neoformans and candida
• It is converted to 5-fluorouracil which inhibits DNA synthesis
Adverse effects
• Bone marrow depression and GI disturbances
Uses
• It is used in cryptococcal meningitis and systemic candidias

8. AZOLES
IMIDAZOLES & TRIAZOLES
• Azoles are newer synthetic antifungals
• They are orally effective and less toxic
• They have broad spectrum antifungal activity
KETOCONAZOLE
• It is orally effective and is well absorbed
• Food and low gastric pH enchance its absorption

9. Adverse effect
• Gastric irritation,nausea,vomiting,headache and allergic reactions
• Inhibition of adrenal and gonadal steroid synthesis
• This results in gynecomastia,infertility,loss of libido and azoospermia
Uses
• Mucocutaneous candidiasis and dermatophytosis
• Cushing syndrome
• Deep mycosis

10. ITRACONAZOLE
• It is the most potent azole
• It is given orally
• Absorption is increased by food and gastric acid
• Less effect on hepatic microsomal enzymes
• Also it does not affect steroid synthesis
• It is available both for oral and I.V use

11. TERBINAFINE
• It is a synthetic anti fungal effective against dermatophytes and candida
• It is fungicidal and orally effective
• It gets concentrated in keratin it acts by inhibiting ergosrerol synthesis
Adverse effect
• GI disturbances,rashes and headache

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