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Definition
allylamines (topical mucocutaneous infection)
MOA: block ergosterol biosynthesis by inhibiting squalene-2,3-epoxidase enzyme
USE: creams for tinia cruris and corporis
-broad spectrum antifungals |
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Term
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Definition
azole (topical mucocutaneous infection)
MOA: inhibit 14-alpha-sterol demethylase (microsomal CYP enzyme essential for ergosterol biosynthesis)
USE: cutaneous application-dermatophytic infections (tinea pedis, corporis, and cruris); shampoo form-seborrheic dermatitis and pityriasis versicolor; vaginal application-vaginal candidiasis
MOR: mutations in gene encoding 14-alpha-sterol demethylase |
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Term
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Definition
polyene antibiotic (topical mucocutaneous infection)
-same MOA and cross-resistance with amphotericin B
-not absorbed from GI, skin, vagina
USE: mucocutaneous candidal infections; stomatitis, vaginitis |
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Term
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Definition
azole (systemic mucocutaneous infection)
MOA: inhibit 14-alpha-sterol demethylase (microsomal CYP enzyme essential for ergosterol biosynthesis)
USE: similar spectrum of activity as itraconazole
MOR: mutations in gene encoding 14-alpha-sterol demethylase
TOX: visual disturbances (blurring and changes in color brightness or vision)-symptoms appear soon after admin and disappear after ~30 min |
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Term
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Definition
azole (systemic mucocutaneous infection)
MOA: inhibit 14-alpha-sterol demethylase (microsomal CYP enzyme essential for ergosterol biosynthesis)
USE: DOC treatment and secondary prophylaxis of C meningitis, IV treatment equiv to amphotericin B in candidemia in ICU pts with normal WBCs
MOR: mutations in gene encoding 14-alpha-sterol demethylase
PK: oral or IV, well absorbed from GI, good CSF penetration
-prophylactic use reduce fungal disease in bone marrow transplant and AIDS pts
TOX: relatively non-toxic |
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Term
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Definition
systemic mucocutaneous infection
MOA: similar to griseofulvin, but fungicidal agent; similar to azoles-inhibits ergosterol biosynthesis (inhibits fungal enzyme squalene epoxidase)
USE: dermatophytoses, particularly onychomycosis (cured in pts-1 tablet/d/12 weeks)
TOX: rare-GI, headaches |
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Term
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Definition
systemic mucocutaneous infection
-fungistatic
MOA: deposited in newly forming skin -> binds to keratin protecting skin from new infection
USE: dermaphytosis (given 2-6 weeks), nail infections (given for months)
PK: poor solubility, GI absorption enhanced when given in microcrystalline form and fatty foods |
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Term
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Definition
echinocandin (systemic infection)
MOA: inhibit synthesis of beta(1,3)D-glucan -> disrupt cell wall structure
USE: esophageal candidiasis, candidema, and salvage therapy of aspergilliosis; azole resistant fungi susceptible to caspofungin
MOR: mutation in one of genes encoding beta(1,3)D-glucan
PK: only IV admin
TOX: generally well tolerated, SEs-GI disturbances, flushing |
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Term
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Definition
azole (systemic and mucocutaneous infection)
MOA: inhibit 14-alpha-sterol demethylase (microsomal CYP enzyme essential for ergosterol biosynthesis)
USE: replaced ketaconazole, broad spectrum; DOC for dimorphic fungi histoplasma, blastomyces, sporothrix
PK: oral or IV admin, absorption inc by food and low gastric pH, poor CSF penetration; interacts with hepatic microsomal enzymes, bioavail lowered when taken with rifamycins
MOR: mutations in gene encoding 14-alpha-sterol demethylase
TOX: relatively non-toxic
DI: interact with number of drugs -> fatal cardiac arrythmias |
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Term
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Definition
azole (systemic and mucocutaneous infection)
MOA: inhibit 14-alpha-sterol demethylase (microsomal CYP enzyme essential for ergosterol biosynthesis)
USE: only used when cost is primary determinant, broad spectrum
MOR: mutations in gene encoding 14-alpha-sterol demethylase
TOX: relatively non-toxic |
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Term
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Definition
cytosine analog (systemic infection)
MOA: toxic to fungal cells only when transported by cytosine permease into fungal cell; 5-FU -> 5-FUMP -> 5-FUTP (inhibit RNA synthesis) or 5-F-dUMP (inhibit DNA synthesis)
USE: narrow spectrum of action-cryptococcus neoformans, some candida, some molds; combo w/ amphotericin B for cryptoccal meningitis or w/ intraconazole for chromoblastomycosis
MOR: loss of cytosine permease enzyme, dec. activity of UPRTase or cytosine deaminase
PK: well absorbed from GI, widely distributed inc. CSF, renal excretion
TOX: renal insufficiency and AIDs-removed by dialysis, GI disturbances, leukopenia, thrombocytopenia, toxic enterocolitis, azotemia in AIDS pts
DI: synergy with amphotericin B and azoles |
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Term
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Definition
polyene antibiotic (systemic infection)
MOA: binds to ergosterol altering cell permeability by forming pores
USE: broad spectrum antifungal agent, yeasts, molds, fungi-causing endemic mycoses, initial induction regime for serious fungal infections -> replaced by azole drug for chronic therapy or relapse prevention; VERY IMPORTANT for immunosupp. pts, sever fungal pneumonia, crytococcal meningitis (intrathecal admin); corneal ulcer, keratitis, fungal arthritis, candiduria
PK: admin slow IV infusion, poorly absorbed from GI
MOR: alterations in ergosterol binding
TOX: immediate rxn-fever, chills, muscle spams, hypotension; culm. rxn-renal impairment, anemia, renal toxicity; hypersens. rxn and phlebitis @ site of injection; CNS SEs, hypokalemia, hypomagnesia, fever, pain, abnormal liver function test; intrathecal admin-seizures, chemical arachnoiditis |
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