antifungal

1. Antifungal drugs
• Antifungal drugs are used for the treatment of fungal infections
(mycoses) that may be superficial or deep infections.
• Fungal infections are susceptible to the immunocompromised
patients due to chemotherapy or antibiotic use.
• Antifungal drugs can be broadly classified into systemic agent &
topical agents.
1.Systemic Agents
a.Antibiotics: Amphotericin B, Griseofulvin
b.Antimetabolites: Flucytosine (5-FC)
c.Azoles: Ketoconazole, Fluconazole, Itraconazole,Vericonazole
d.Allylamine: Terbinafine
e.Echinocandins: Caspofungin, Micafungin, Anidulafungin
2.Topical Agents
a.Polyene Antibiotics: Nystatin, Hamycin, Natamycin
b.Imidazole: Clotrimazole, Miconazole, Econazole
c.Miscellaneous: Tolnaftate, Undecylenic acid, Benzoic acid

3. Amphotericin B
• Amphotericin B is a polyene antibiotic that has antifungal action for
systemic mycoses.
Mechanism of action
• Amphotericin B binds to ergosterol present on cell membrane to
form microspore or channels that increase the permeability of the
membrane causing leakage of electrolytes (K+
) & molecules which
ultimately causes cell death.
Indications
• Candidiasis, Coccididomycosis, Aspergillosis, Blastomycosis,
Otomycosis, Leishmaniasis
Contraindications
• Patients with hypersensitivity
Adverse effects
• Acute reactions: Nausea, Vomiting, fever & chills
• Chronic reaction: Anemia, nephrotoxicity
Doses
• 250mcg/kg daily i.v. infusion (1.5 mg/kg for severe infections)

4. Griseofulvin
• Griseofulvin was the first orally effective antifungal agent extracted from
Penicillium griseofulvum effective against most dermatophytes including
Epidermophyton, Trichophyton and Microsporum, but not against Candida.
Mechanism of Action
• Griseofulvin interfere with mitosis causing abnormal metaphase
configuration, also disorients microtubules & inhibit the cell division of
fungus.
Indication
• Griseofulvin is effective against all superficial ringworm (dermatophyte)
infection.
Contraindication and Precaution
• Contraindicated in patients with hypersensitivity, prophyria, monilial
infection(vaginal candidiasis), pregnancy & lactation
Adverse Effects
• Adverse reaction include GI upset, headache, rashes, photohobia and
peripheral neuritis.
Dose:
• Adult: 125 to 250 mg QID with meal.
• Child: 10 mg/kg daily

5. Ketoconazole
• Ketoconazole was the first orally effective antifungal agents of imidazole group in
the azole derivatives.
Mechanism of Action
• It acts as an inhibitor of 14-alpha demethylase, thereby inhibits synthesis of
ergosterol, causing leakage of cellular contents.
Indication
• It is used in the treatment of systemic fungal infection, alternative to Griseofulvin,
topically used for jack itch (Tinea cruris), athlets foot, ring worm
Contraindication and Precaution
• Contraindicated in patients with hypersensitivity.
Adverse Effects
• The common side effects are nausea, vomiting, anorexia, headache, parasthesia,
rashes and hair loss.
• Gynaecomastia in male and menstrual irregulation in female can occur
Dose
• usual dose is 200 mg OD or BD with meal.
• 2% topical preparation is applied in affected area.

6. Fluconazole
• Fluconazole is more water soluble than ketoconazole and its major advantage is
its good penetration into the CSF, ocular fluid, vaginal tissue, saliva and nails.
Mechanism of Action
• Same as Ketoconazole
Indication
• It is effective in oropharyngeal candidiasis, vaginal candidiasis, cryptococcal
meningitis (caused by Cryptococcus neoformans) and histoplasmosis.
Contraindication and Precaution
• Contraindicated in patients with hypersensitivity & renal or hepatic impairment.
Adverse Effects
• It has few side effect includes, nausea, vomiting, abdominal pain, rashes,
headache & alopecia.
Dose
• Oropharyngeal candidiasis: 200 mg on the first day and then 100 mg daily for 2
week.
• Veginal candidiasis: 150 mg as a single dose.
• Cryptococcal meningitis: 200-400 mg/day for 4-12 week or more.

7. Nystatin
• It is available in the form of topical powder, oral and vaginal tablets
and oral suspension.
Mechanism of Action
• It binds to ergosterol, a major component of the fungal cell
membrane & forms pores in the membrane that lead to K+
leakage,
acidification, and death of the fungus.
Indication
• It is used to treat Candida infections of the skin including diaper
rash, thrush (mouth infection), oropharyngeal candidiasis, and vaginal
yeast infections.
Contraindication and precaution
• Contraindicated in patients with hypersensitivity & skin disorders
Adverse Effects
• GI distress, diarrhoea, nausea, vomiting, rash, itching, burning
Dose
• Adult: 5,00,000 or 10,00,000 IU 3-4 times a day
• Child: >1 months– 1,00,000 IU

8. Clotrimazole
• It is a common topical antifungal agent of imidazole derivatives.
Mechanism of Action
• Clotrimazole kills individual Candida or fungal cells by altering the permeability of
the fungal cell wall.
• It binds to phospholipids in the cell membrane and inhibits
the biosynthesis of ergosterol and other sterols required for cell membrane
production which leads to the cell's death via loss of intracellular elements.
Indication
• It is used in the topical treatment of ring worm, athlete’s foot, otomycosis (fungal
ear infection), oral/cutaneous/vaginal candidiasis as well as skin infection caused
by corynebacteria.
Contraindication and Precaution
• Contraindicated in patients with hypersensitivity & skin disorders
Adverse Effects
• Local irritation and burning skin have been reported in few patients.
Dose
• 1% cream/lotion/solution applied 4 times a day to affected area.

9. 9
Antifungals Indications Doses
Flucytosine
(5-FC)
Chromoblasto-
mycosis
cryptococcosis
100-150mg/kg/day q6h
Terbinafine Dermatophytes
Candidia
250mg OD (Oral)
1% cream (Topical)
Caspofungin Candida
Aspergillus
70mg loading dose
infused i.v for 1h
followed by 50mg i.v
daily

10. 9
Antifungals Indications Doses
Flucytosine
(5-FC)
Chromoblasto-
mycosis
cryptococcosis
100-150mg/kg/day q6h
Terbinafine Dermatophytes
Candidia
250mg OD (Oral)
1% cream (Topical)
Caspofungin Candida
Aspergillus
70mg loading dose
infused i.v for 1h
followed by 50mg i.v
daily