Anti-fungal agents Flashcards
ALLYLAMINES Classification? Site of action? Mechanism of action? Spectrum? Uses? Side Effects? Routes? Pharmacokinetics? Example?
Classification: FUNGICIDAL Site of action: FUNGAL CELL MEMBRANE Mechanism of action: INHIBIT ERGOSTEROL BIOSYNTHESIS Spectrum: DERMATOPHYTES Uses: ATHLETE'S FOOT Side effects: TRANSIENT/MILD (GIT/skin) Routes: ORAL AND TOPICAL Pharmacokinetics: HIGHLY LIPOPHILIC Example: TERBINAFINE; LAMASIL
AZOLES: IMIDAZOLES Classification? Site of action? Mechanism of action? Spectrum? Uses? Side Effects? Routes? Resistance methods? Example?
Classification: SUPERFICIAL MUCUS MEMBRANE AND SKIN INFECTION; FUNGISTATIC
Site of action: FUNGAL CELL MEMBRANE
Mechanism of action: INHIBIT ERGOSTEROL BIOSYNTHESIS
Spectrum: BROAD
Uses: TRICHOPHYTON, MICROSPORUM, CANDIDA, AND MALASSEZIA TREATMENT
Side Effects: GIT, ANOREXIA, HEPATOTOXICITY; SUPPRESSION OF STEROID PRODUCTION; TERATOGENIC
Routes: TOPICAL ADMINISTRATION; EAR DROPS
Resistance methods: MEMBRANE CHANGES/REDUCED DRUG UP-TAKE; BIOFILM FORMATION; DRUG EFFLUX; TARGET ENZYME OVER-PRODUCED OR MUTATED
Example: CLOTRIMAZOLE, ENILCONAZOLE, MICONAZOLE
AZOLES: TRIAZOLES Classification? Site of action? Mechanism of action? Spectrum? Uses? Side Effects? Routes? Pharmacokinetics? Methods of Resistance? Example?
Classification: SYSTEMIC MYCOSE INFECTIONS; FUNGISTATIC
Site of action: FUNGAL CELL MEMBRANE
Mechanism of action: INHIBIT ERGOSTEROL BIOSYNTHESIS
Spectrum: BROAD
Uses: TREAT HISTOPLASMOSIS; CANDIDA INFECTIONS; ASPERGILLUS INFECTIONS; MICROSPORUM INFECTION IN CATS
Side Effects: GIT, ANOREXIA, HEPATOTOXICITY, TERATOGENIC
Routes: ORAL
Pharmacokinetics: ITRACONAZOLE - LIPOPHLIC/HEPATIC METABOLISM/FECES EXCRETION; FLUCONAZOLE - WATER SOLUBLE/MINIMAL METABOLISM/MAJORITY EXCRETED UNCHANGED FROM KIDNEY
Methods of Resistance: MEMBRANE CHANGES, TARGET ENZYME MUTATION OR OVER-PRODUCTION, DRUG EFFLUX DUE TO TRANSPORTERS, BIOFILM FORMATION
Example: FLUCONAZOLE, ITRACONAZOLE, VORICONAZOLE, POSACONAZOLE
POLYENES Classification? Site of action? Mechanism of action? Spectrum? Uses? Side Effects? Routes? Pharmacokinetics? Methods of Resistance? Example?
Classification: FUNGICIDAL
Site of action: FUNGAL CELL MEMBRANE
Mechanism of action: PUNCH HOLES IN MEMBRANE UPON BINDING TO ERGOSTEROL; IONS LEAK FROM CELL –> CIDAL AND OXIDATIVE DAMAGE
Spectrum: BROAD
Uses: SKIN YEAST INFECTION, OTITIS EXTERNA, EAR MITE TREATMENT
Side Effects: NEPHROTOXICITY (IV), HYPOKALEMIA, THROMBOPHLEBITIS
Routes: TOPICAL, IV
Pharmacokinetics: POOR WATER SOLUBILITY, POOR ABSORPTION FROM GUT
Methods of resistance: REDUCED ERGOSTEROL, INCREASED INTRACELLULAR CATALASE REDUCING OXIDATIVE KILLING MECHANISM, INNATE RESISTANCE
Example: AMPHOTERICIN B, NYSTATIN
GLUCAN SYNTHESIS (CELL WALL) INHIBITORS: ECHINOCANDINS Classification? Site of action? Mechanism of action? Spectrum? Uses? Side Effects? Routes? Pharmacokinetics? Methods of Resistance? Example?
Classification: SYSTEMIC MYCOSE INFECTIONS; FUNGICIDAL IN YEAST; FUNGISTATIC IN MOULDS
Site of action: FUNGAL CELL WALL
Mechanism of action: BLOCK SYNTHESIS OF BETA (1,3) GLUCAN
Spectrum: CANDIDA AND ASPERGILLUS SPECIES
Uses: TREAT BLOODSTREAM YEAST INFECTIONS
Side Effects: MINIMAL
Routes: IV
Pharmacokinetics: WATER SOLUBLE, HIGHLY PLASMA PROTEIN BOUND, ELIMINATED IN URINE AND FECES AS METABOLITES
Methods of Resistance: MUTATED ENZYMES, INHIBIT GLUCAN SYNTHASE WHICH SYNTHESIZES BETA GLUCAN
Example: CAPSOFUNGIN, ANIDULAFUNGIN, MICAFUNGIN
ANTI-METABOLITES Classification? Site of action? Mechanism of action? Spectrum? Uses? Side Effects? Routes? Pharmacokinetics? Methods of Resistance? Example?
Classification: FUNGICIDAL
Site of action: FUNGAL NUCLEUS
Mechanism of action: INTERFERES WITH DNA AND PROTEIN SYNTHESIS
Spectrum: NARROW - CRYPTOCOCCUS AND CANDIDA SPECIES
Uses: COMBINATION THERAPY FOR SEVERE YEAST INFECTIONS ONLY
Side Effects: GENERALLY WELL TOLERATED
Routes: ORAL
Pharmacokinetics: EXCRETED UNCHANGED BY KIDNEY
Methods of Resistance: MISCODED DNA OR RNA; LOSS OR REDUCTION IN ACTIVITY OF PHOSPHORYLASE ENZYMES; ALWAYS COMBINE WITH AMPHOTERICIN B FOR THERAPY
Example: FLUCYTOSINE
GRISEOFULVIN Classification? Site of action? Mechanism of action? Spectrum? Uses? Side Effects? Routes? Pharmacokinetics?
Classification: FUNGISTATIC
Site of action: FUNGAL MICROTUBULES
Mechanism of action: INHIBITS MITOSIS AND DISORGANIZES SPINDLE MICROTUBULES
Spectrum: NARROW (DERMATOPHYTES)
Uses: DERMATOPHYTE INFECTIONS ONLY. NO LONGER LICENSED FOR FOOD PRODUCING ANIMALS IN UK. ONLY HORSES.
Side Effects: IDIOSYNCRATIC REACTION IN CATS, TERATOGENIC
Routes: ORAL (WITH HIGH FAT DIET)
Pharmacokinetics: POORLY WATER SOLUBLE, HEPATIC METABOLISM, AND FECAL ELIMINATION
OTHER AGENTS: IODIDES, WHITFIELD’S OINTMENT, AND PHENOLIC ANTISEPTICS
Uses?
Iodides: ENHANCE HOST IMMUNE RESPONSE
Whitfield’s ointment: TREAT DERMATOPHYTE INFECTIONS OF THE SKIN
Phenolic antiseptics: USED FOR SUPERFICIAL SKIN INFECTIONS
