Date post: | 15-Jan-2016 |
Category: |
Documents |
Upload: | dynomuhammad |
View: | 31 times |
Download: | 0 times |
ANTIFUNGAL DRUGS
dr. Agung Wiwiek Indrayani, M.Kes
Pharmacology Department Faculty of Medicine
dr. Agung Wiwiek Indrayani, M.Kes
Pharmacology Department Faculty of Medicine
Problems
+ a polyene
ergosterol
ergosterol withpore
Reduction of ergosterol synthesis by inhibition of fungal cytochrome P450
enzymes
Reduction of ergosterol synthesis by inhibition of fungal cytochrome P450
enzymes
Clinical UseMany candida species, Crytococcus neoformans , the endemic mycoses (blastomycosis, coccidiodomycosis, histoplasmosis, the dermatophytes,
aspergillus infections
Clinical UseMany candida species, Crytococcus neoformans , the endemic mycoses (blastomycosis, coccidiodomycosis, histoplasmosis, the dermatophytes,
aspergillus infections
Acetyl CoA
Squalene
Lanosterol
(ergosterol)
Allylaminedrugs
Azoles
Squalene-2,3 oxide
Squalene monooxygenase
14--demethylase
VORICONAZOLENewest triazole
Intravenous and oral formulations
Dosage 400 mg/d
Intravenous and oral formulations
Dosage 400 mg/d
Well absorbed, bioavaibility 90 %,
inhibition of P450 low
Visual disturbances 30 % patient
Less toxic > Amphotericin B
Candida species, invasive aspergillosis
Echinocandins the newest antifungal agent
Only intravenous form, a single loading dose 70 mg, dailly dose 50 mg
Water soluble, highly protein bound T1/2 9-11 hours Excretion kidneys and GIT Dosage adjustment hepatic
insufficiency Disruption cell wall inhibiting synthesis
of B (1-3) glucan Invasive aspergillosis, candida
Very insoluble ,fungistatic, from penicillium
Oral form absorption with fatty food, 1 g/d
It binds to keratin, protecting from new infection
2-6 weeks for skin and hair infectionNail infection for monthsSerum sickness, hepatitis, drug
interaction ( warfarin and phenobarbital ),
replaced by azoles and terbinafine
A synthetic allylamine , fungicidal, oral formulation, 250 mg/d
Dermatophytoses, onychomycosis Keratophilic, inhibit ergosterol
biosynthesis Accumulation of the sterol squalene
toxic organism One tablet daily 12 weeks cure rate 90
%
Acetyl CoA
Squalene
Lanosterol
(ergosterol)
Allylaminedrugs
Azoles
Squalene-2,3 oxide
Squalene monooxygenase
14--demethylase
RATIONALE FUNGAL DRUGS
THANK YOUTHANK YOU