fluorinated bis-triazole
reduction of ergosterol synthesis by inhibition of fungal cytochrome P450 enzymes (greater affinity for fungal than for human)

Polyenes specifically target fungal membranes. They bind ergosterol, which is the principal sterol in fungal membranes as opposed to cholesterol found in host membranes. This interference creates a transmembrane channel and the resultant change in permeability allows leakage of intracellular components

Well absorbed orally

only administered IV

good CSF penetration

Poor tissue penetration. Negligable CSF or urine penetration.

Highly protein bound

not metabolized well

Metabolised by the liver

Urine unchanged

poorly characterized but does not accumulate in renal failure

N/V/D, Abdominal pain
Headache
Skin rash
Reversible alopecia
Rare: Hepatic failure, SJS
Should be avoided in Pregnancy
Drug interactions: (inhibitor of CYP3A4, CYP2C9)

Dose related nephrotoxicity
Infusion related reactions (hypotension, fever, rigors)

Candida
Cryptococcus
Coccidia
(No activity against histoplasma, blasto, sporotrichosis, Aspergillus, mucormycosis)

Broad antifungal cover including candida, Cryptococcus, aspergillus and zygomyces

ANTIFUNGAL:
AZOLE

Antifungal

Triazole

Polyene

Level 3

Level 3

Some candida species,

Decreased drug concentration
Target site alteration
Up-regulation of target enzyme
Development of bypass pathways

potent CYP inhibitors with a wide range of drug interactions (including warfarin)