Fluconazole
Class
Azole
Dose
Prophylaxis: 100-400mg od
Tx: 400-800mg od
Mechanism
Cidal
MoA
Inhibits the fungal cytP450 enzyme that syntheses ergosterol
Inhibits cell memb formation
Leakage -> cell death
Time v Conc
Concentration
Spectrum
Covers
Doesnt
C Albicans
Cryptococcus
C Gabralta
C Krusei (Kompletely resistant)
Indications
PK
A
Rapid, complete 100% OBA
D
CNS 50-90% of absorbed levels.
Wide distribution
Good urine penetration can be used for candida cystitis
M
Hepatic
E
Excreted in kidneys
80% unchanged
AE
Hepatic toxicity
Watch LFTs; hepatic failure, hepatitis, abnormal LFTs
CVS
Angioedema, QT prolongation
CNS
Headache, dizziness
Haem
Thrombocytopenia, leukopenia
Derm
Skin rashes, alopecia
Resistance
Non Albicans Candidas
Most other fungi
Monitoring
LFT