ANTIFUNGAL, CS Flashcards
Terbinafine
• Allylamine
Fungicidal
Terbinafine Blocks the biosynthesis of
inhibits
ergosterol, a sterol essential to the integrity
of the fungal cell membrane;
squalene epoxidase (fungal inhibited 4X more than mammalian)
Terbinafin AND synthesis of steroid hormones, prostaglandins, and drug metabolism
Does not interfere with
Terbinafine with liver dysfunction
slow elimination by 30%
Terbinafine lesser degree efficacy
cutaneous candidiasis
Terbinafine and ?cytochrome p450 superfamily
does not inhibit
Itraconazole, Fluconazole, keto Triazole
• Inhibits
14-α-demethylase, blocking lanosterol conversion to ergosterol
Itraconazole is Highly lipophilic
• Bioavailability increased
• Needs environment for absorption
postprandially
acid
Itraconazole Adr
hypertriglyceridemia, edema, hypertension, leukopenia, elevated LFTs, nephrotic syndrome
Itraconazole , Keto, FLUCO
Inhibits cytochrome P450
→ elevates
inhibits, Small affinity for incr digoxin, cyclosporine, triazolam, fluco Elevates phenytoin, warfarin, nortriptyline, midazolam, triazolam, and tacrolimus
Ketoconazole by interfering with androgen
and glucocorticoid synthesis
gynecomastia and
impotence,
acid environment for absorption
enhanced by food intake
lipophilic
Ketoconazole itraconazole
Ketoconazole common effects on liver (fulminant hepatitis and transient increases in LFTs)
•
FALSE
Fluconazole Rarely elevated LFTs
T
Fluconazole for prolonged use at 400 mg
Alopecia