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Antifungal Drugs 3
Antifungal Drugs 3
2- Deep infections
1- Antifungal Antibiotics :
Griseofulvin
Polyene macrolide : Amphotericin- B &
Nystatin
2- Synthetic :
Azoles :
A) Imidazoles : Ketoconazole , Miconazole
B) Triazoles : Fluconazole , Itraconazole
Flucytosine
Squalene epoxidase inhibitors : e.g.
Terbinafine & Naftifine.
Systemic :
Griseofulvin , Amphotericin- B , Ketoconazole ,
Fluconazole , Terbinafine.
Topical
In candidiasis :
Imidazoles : Ketoconazole , Miconazole.
Triazoles : Terconazole.
Polyene macrolides : Nystatin , Amphotericin-B
Gentian violet : Has antifungal & antibacterial.
In Dermatophytes :
Amphotericin B
Pharmacokinetics
Mechanism of action
Resistance to amphotericin B
Adverse Effects
2- Slower toxicity
Clinical uses
Routes of Administration
Liposomal preparations of
amphotericin B
Nystatin
Clinical uses
Azoles
Mechanism of Action
Azoles
Imidazoles
Ketoconazole
Miconazole
Clotrimazole
They lack selectivity ,they inhibit human
gonadal and steroid synthesis leading to
decrease testosterone & cortisol production.
Also, inhibit human P-450 hepatic enzyme.
Ketoconazole
Ketoconazole (cont.)
Clinical uses
Adverse Effects
Contraindicated in :
Prgnancy, lactation ,hepatic dysfunction
Interact with enzyme inhibitors , enzyme
inducers.
H2 blockers & antacids decrease its absorption
Triazoles
Fluconazole
Itraconazole
Voriconazole
They are :
Selective
Resistant to degradation
Causing less endocrine disturbance
Itraconazole
Itraconazole (cont.)
Fluconazole
Water soluble
Completely absorbed from GIT
Excellent bioavailability after oral
administration
Bioavailability is not affected by food or
gastric PH
Conc. in plasma is same by oral or IV route
Has the least effect on hepatic microsomal
enzymes
Fluconazole (cont.)
Clinical uses
Candidiasis
( is effective in all forms of mucocutaneous
candidiasis)
Cryptococcus meningitis
Histoplasmosis, blastomycosis, , ring worm.
Not effective in aspergillosis
Side effects
Voriconazole
Flucytosine
Mechanism of action
Converted within the fungal cell to 5fluorouracil( Not in human cell ) by cytosine
deaminase, that inhibits thymidylate
synthetase enzyme that inhibits DNA synthesis.
Phrmacokinetics
Clinical uses
Adverse Effects
Caspofungin
Clinical uses
Griseofulvin
Griseofulvin(cont.)
CLOTRIMAZOLE
ITRACONAZOLE
TOLNAFTATE
NAFTIFINE
TERBINAFINE