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Antifungal drugs
These are drugs used for superficial and deep(systemic) fungal
infection
CLASSIFICATION
1. Antibiotics : Amphotericin B (AMB), Nystatin Hamycin, Griseofulvin
2. Antimetabolite : Flucytosine (5-FC)
3. Azoles
A. Imidazoles (topical): Clotrimazole, Miconazole, Oxiconazole
(systemic): Ketoconazole
B. Triazoles (systemic): Fluconazole,Itraconazole,
4. Allylamine : Terbinafine
5. Other topical agents
Tolnaftate, , Benzoic acid,, Ciclopirox olamine, Butenafine.
Griseofulvin
• MOA- fungistatic;deposited in keratin precursor cells and is tightly
bound to new keratin,and this inceases resistance to fungal invasion.
Griseofulvin is active against most
dermatophytes,including,Epidermophyton,Trichophyton,Microsporum
, etc., but not against Candida and other fungi causing deep mycosis.
• USE- fungal infection of hair,nail,foot, dose 125-250mg qid with
meals,no topical preparation only oral.
• A/E-headache,g.i.t. disturbance,peripheral neuritis rashes,leukopenia
Clotrimazole
• MOA-inhibit the fungal cytochromeP450 enzyme ‘lanosterol 14demethylase’
impair ergosterol synthesis
membrane abnormalities in the fungus.
• USE- 1.ring worm
2.oropharyngeal/cutaneous/vaginal candidiasis
• A/E- local irritation,stinging and burning sensation
• Preparation-candid 1%gel,cream,lotion,powder
Miconazole
• MOA-similar to clotrimazole
• USE- highly efficacious[>90%cure rate] in tinea infections,pityriasis
versicolar ,otomycosis,cutaneous and vulvovaginal candidiasis
• A/E- local irritation
• Preparation-1%ear drop,2%powder cream gel
Ketoconazole
• Use- ring worm,recurrent cases of vaginal candidiasis,systemic
mycosis,kala-azar,cushing syndrome
• A/E- nausea,vomiting,loss of appetite,rashes,paresthesia
Gynecomastia,loss of hair and libido,menstrual irregularities
• C/I- pregnancy and nursing women
• Preparations-nijral cream 2%,shampoo,tab 200mg
fluconazole
• MOA-similar to other azoles
• USE-1.tinea(ring worm)infections
2.oropharyngeal, cutaneous,vaginal candidiasis
3.crytococcal meningitis
• A/E- nausea vomiting abd pain rash headache
• C/I- pregnancy and lactating mothers
Itraconazole
• broader spectrum of activity than fluconazole,no antiandrogenic side
effects
• Use –similar to fluconazole
• A/E –g.i.t. disturbance,pruritis headache
Terbinafin
• orally and topically active drug against dermatophytes and candidiasis
• Most commonly used topical drugs
• Fungicidal unlike azole
• USE-all types of tinaea infections[250mg tab,1% cream]

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Antifungal drugs.pptx

  • 1. Antifungal drugs These are drugs used for superficial and deep(systemic) fungal infection CLASSIFICATION 1. Antibiotics : Amphotericin B (AMB), Nystatin Hamycin, Griseofulvin 2. Antimetabolite : Flucytosine (5-FC) 3. Azoles A. Imidazoles (topical): Clotrimazole, Miconazole, Oxiconazole (systemic): Ketoconazole B. Triazoles (systemic): Fluconazole,Itraconazole, 4. Allylamine : Terbinafine 5. Other topical agents Tolnaftate, , Benzoic acid,, Ciclopirox olamine, Butenafine.
  • 2.
  • 3. Griseofulvin • MOA- fungistatic;deposited in keratin precursor cells and is tightly bound to new keratin,and this inceases resistance to fungal invasion. Griseofulvin is active against most dermatophytes,including,Epidermophyton,Trichophyton,Microsporum , etc., but not against Candida and other fungi causing deep mycosis. • USE- fungal infection of hair,nail,foot, dose 125-250mg qid with meals,no topical preparation only oral. • A/E-headache,g.i.t. disturbance,peripheral neuritis rashes,leukopenia Clotrimazole • MOA-inhibit the fungal cytochromeP450 enzyme ‘lanosterol 14demethylase’ impair ergosterol synthesis membrane abnormalities in the fungus. • USE- 1.ring worm 2.oropharyngeal/cutaneous/vaginal candidiasis • A/E- local irritation,stinging and burning sensation • Preparation-candid 1%gel,cream,lotion,powder
  • 4. Miconazole • MOA-similar to clotrimazole • USE- highly efficacious[>90%cure rate] in tinea infections,pityriasis versicolar ,otomycosis,cutaneous and vulvovaginal candidiasis • A/E- local irritation • Preparation-1%ear drop,2%powder cream gel Ketoconazole • Use- ring worm,recurrent cases of vaginal candidiasis,systemic mycosis,kala-azar,cushing syndrome • A/E- nausea,vomiting,loss of appetite,rashes,paresthesia Gynecomastia,loss of hair and libido,menstrual irregularities • C/I- pregnancy and nursing women • Preparations-nijral cream 2%,shampoo,tab 200mg
  • 5. fluconazole • MOA-similar to other azoles • USE-1.tinea(ring worm)infections 2.oropharyngeal, cutaneous,vaginal candidiasis 3.crytococcal meningitis • A/E- nausea vomiting abd pain rash headache • C/I- pregnancy and lactating mothers Itraconazole • broader spectrum of activity than fluconazole,no antiandrogenic side effects • Use –similar to fluconazole • A/E –g.i.t. disturbance,pruritis headache
  • 6. Terbinafin • orally and topically active drug against dermatophytes and candidiasis • Most commonly used topical drugs • Fungicidal unlike azole • USE-all types of tinaea infections[250mg tab,1% cream]