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Flashcards in Antibiotics (Antifungals) Deck (10):
1

FOR SYSTEMIC FUNGAL INFECTIONS
__________________
- polyene
- binds to ____________ in fungal cell membranes, forming artificial pores; fungicidal (Aspegillus, Blastomyces, Candida albicans, Cryptococcus, Histoplasma, Mucor)
- SE: infusion reactions, nephrotoxicity (RTA with _____________ and ______________ wasting)
- Control infusion reactions by slowing rate of infusion and premedication with __________________
- Additive nephrotoxicity with other nephrotoxic drugs (aminoglycosides)
- lipid formulations (prolonged duration of action): ambisome, amphotec, abelcet

FOR SYSTEMIC FUNGAL INFECTIONS
Amphotericin B
- polyene
- binds to ergosterol in fungal cell membranes, forming artificial pores; fungicidal (Aspegillus, Blastomyces, Candida albicans, Cryptococcus, Histoplasma, Mucor)
- SE: infusion reactions, nephrotoxicity (RTA with magnesium and potassium wasting)
- Control infusion reactions by slowing rate of infusion and premedication with antihistamines
- Additive nephrotoxicity with other nephrotoxic drugs (aminoglycosides)
- lipid formulations (prolonged duration of action): ambisome, amphotec, abelcet

2

FOR SYSTEMIC FUNGAL INFECTIONS
______________
- pyrimidine antimetabolite
- accumulated in fungal cells by the action of _____________ and converted by ______________ to 5-FU, which inhibits thymidilate synthase; fungi_________
- for cryptococcosis, systemic candidal infections, chromoblastomycosis
- Selective toxicity occurs because mammalian cells have low levels of ____________ and _____________

FOR SYSTEMIC FUNGAL INFECTIONS
Flucytosine
- pyrimidine antimetabolite
- accumulated in fungal cells by the action of permease and converted by cytosine deaminase to 5-FU, which inhibits thymidilate synthase; fungistatic
- for cryptococcosis, systemic candidal infections, chromoblastomycosis
- Selective toxicity occurs because mammalian cells have low levels of permease and deaminase

3

FOR SYSTEMIC FUNGAL INFECTIONS
Ketoconazole
- inhibits fungal P450-dependent enzymes blocking ergosterol synthesis (lanosterol->ergosterol); fungi_________
- narrow antifungal spectrum
- for chronic mucocutaneous candidiasis, dermatophytosis
- SE: gynecomastia, hepatotoxicity (azoles are hepatotoxic!)
- limited to topical use because of systemic toxicity

FOR SYSTEMIC FUNGAL INFECTIONS
Ketoconazole
- inhibits fungal P450-dependent enzymes blocking ergosterol synthesis (lanosterol->ergosterol); fungistatic
- narrow antifungal spectrum
- for chronic mucocutaneous candidiasis, dermatophytosis
- SE: gynecomastia, hepatotoxicity (azoles are hepatotoxic!)
- limited to topical use because of systemic toxicity

4

FOR SYSTEMIC FUNGAL INFECTIONS
____________
- inhibits fungal P450-dependent enzymes blocking ergosterol synthesis (_________->ergosterol); fungi_________
- has good CNS permeability
- used for candidiasis, coccidiomycosis, cryptococcal meningitis (treatment and prophylaxis)

FOR SYSTEMIC FUNGAL INFECTIONS
Fluconazole
- inhibits fungal P450-dependent enzymes blocking ergosterol synthesis (lanosterol->ergosterol); fungistatic
- has good CNS permeability
- used for candidiasis, coccidiomycosis, cryptococcal meningitis (treatment and prophylaxis)

5

FOR SYSTEMIC FUNGAL INFECTIONS
_______________
- inhibits fungal P450-dependent enzymes blocking ergosterol synthesis (lanosterol->ergosterol); fungistatic
- used for blastomycosis, sporotrichosis, dermatophytosis

FOR SYSTEMIC FUNGAL INFECTIONS
Itraconazole
- inhibits fungal P450-dependent enzymes blocking ergosterol synthesis (lanosterol->ergosterol); fungistatic
- used for blastomycosis, sporotrichosis, dermatophytosis

6

FOR SYSTEMIC FUNGAL INFECTIONS
_____________
- echinocandin
- inhibits ____________ synthase, decreasing fungal cell wall synthesis; fungi___________
- for disseminated and mucocutaneous candidiasis, salvage therapy for invasive ____________
- SE: flushing (_________ release)

FOR SYSTEMIC FUNGAL INFECTIONS
Caspofungin
- echinocandin
- inhibits beta-glucan synthase, decreasing fungal cell wall synthesis; fungistatic
- for disseminated and mucocutaneous candidiasis, salvage therapy for invasive aspergillosis
- SE: flushing (histamine release)

7

SYSTEMIC DRUGS FOR SUPERFICIAL MYCOSES
_____________
- azole
- interferes with microtubule function; inhibits synthesis and polymerization of nucleic acids; fungi________
- for dermatophytosis
- accumulates in _________; contraindicated in ___________

SYSTEMIC DRUGS FOR SUPERFICIAL MYCOSES
Griseofulvin
- azole
- interferes with microtubule function; inhibits synthesis and polymerization of nucleic acids; fungistatic
- for dermatophytosis
- accumulates in keratin; contraindicated in porphyria

8

SYSTEMIC DRUGS FOR SUPERFICIAL MYCOSES
___________
- squalene oxidase inhibitor
- interfere with ergosterol synthesis by inhibiting conversion of squalene to ___________
- for dermatophytosis, onychomycosis
- accumulates in ________

SYSTEMIC DRUGS FOR SUPERFICIAL MYCOSES
Terbinafine
- squalene oxidase inhibitor
- interfere with ergosterol synthesis by inhibiting conversion of squalene to lanosterol
- for dermatophytosis, onychomycosis
- accumulates in keratin

9

TOPICAL DRUGS FOR SUPERFICIAL FUNGAL INFECTIONS
__________
- polyene
- binds to ergosterol in fungal cell membranes, forming artificial pores; fungicidal
- for candidiasis
- SE: severe nephrotoxicity
- minimal mucocutaneous absorption
- available as a swish-and-swallow preparation

TOPICAL DRUGS FOR SUPERFICIAL FUNGAL INFECTIONS
Nystatin
- polyene
- binds to ergosterol in fungal cell membranes, forming artificial pores; fungicidal
- for candidiasis
- SE: severe nephrotoxicity
- minimal mucocutaneous absorption
- available as a swish-and-swallow preparation

10

TOPICAL DRUGS FOR SUPERFICIAL FUNGAL INFECTIONS
Clotrimazole
- azole
- for mucocutaneous candidiasis, dermatophytosis, seborrheic dermatitis, pityriasis versicolor
- limited to topical use due to systemic toxicity

TOPICAL DRUGS FOR SUPERFICIAL FUNGAL INFECTIONS
______________
- azole
- for mucocutaneous candidiasis, dermatophytosis, seborrheic dermatitis, pityriasis versicolor
- limited to topical use due to systemic toxicity

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