| Structure/Class |
- Imidazoles – ketoconazole, miconazole, clotrimoxazole
- Triazoles – fluconazole, voriconazole
|
| Pharmacodynamics |
- Inhibits fungal CYP 450, therefore reducing ergosterol synthesis.
- Specificity comes from the fact that azoles have greater affinity for fungal CYP than human CYP.
- Imidazoles are less selective and hence more toxic.
- Spectrum of activity
- Broad – candida, mycoses, aspergillus
- Toxicity
- Minor GI upset
- Rarely, clinically significant hepatitis.
|
| Pharmacokinetics |
- Fluconazole has interesting pharmacokinetics
- Can be given PO/IV (good bioavailability)
- It has high CSF penetration and can be used un fungal meningitis (other anti-fungals do not)
- It is an inhibitor of CYP 450 enzyme, and has drug interactions as such.
- Widest therapeutic index.
|
