Date post: | 07-May-2015 |
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Health & Medicine |
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POSACONAZOLE
Dr.Sangeetha P
FUNGUS Yeasts Filamentous fungi/moulds - Dermatophytes - Opportunistic fungi Dimorphic fungi
MYCOSES – CLINICAL CLASSIFICATION
Superficial Deep Opportunistic
ANTIFUNGAL AGENTS
Antibiotics Polyenes Griseofulvin Azoles Imidazoles Triazoles Allylamines Antimetabolites Echinocandins
(-)Lanosterol demethylase (-)Ergosterol synthesis (-)The cell membrane
(-)The cell membrane
WHY NEW AZOLES ?
Broader spectrum
Low toxicity Oral preparations
POSACONAZOLE
Latest drug in triazole groupBroadest spectrum azoleApproved by FDA on 2006“Noxafil”
MECHANISM OF ACTION (-)Lanosterol demethylase
(-)Ergosterol synthesis
(-)The cell membrane
PHARMACOKINETICSOnly as oral suspensionFatty food absorptionHigh tissue penetrationLow CSF penetration Potent inhibitor of CYP-3A4Mainly excreted through bileNo dose reduction in elderly, liver or
renal ds
SPECTRUM - AZOLES Broad spectrumCovers yeasts, filamentous fungi (Dermatophytes) & dimorphic fungi
weak against opportunistic fungi !(aspergillosis,mucor mycosis etc)
POSACONAZOLE SPECTRUM
Broad spectrum like other azoles
covers opportunistic fungi also
STUDIES
1:Posaconazole vs Fluconazole for prophylaxis of invasive fungal infections
in transplant recepients
2:Posaconazole vs fluconazole in neutropenic patients
INDICATIONS Prophylaxis of invasive candidiasis (fluconazole/low dose polyene)Rx of refractory oropharyngeal candidiasis
( fluconazole /itraconzole)Prophylaxis & Rx of invasive aspergillosis
(secondary to voriconozle)Mucor mycosis –the only azole active against Mucor!
(high dose iv amph B)
DOSE Prophylaxis of invasive fungal infections-200mg TDS(40mg/ml)
Oropharyngeal Candidiasis - 100mg BD
Refractory cases – up to 400mg BD
CONTRAINDICATIONS
Children 13 yrsPregnancyNursing mother
POSACONAZOLE ADRGastrointestinal upset Hepatotoxicity Neutropenia Drug interactions (CYP3A4)
AZOLES-S/E
Fluconazole
Itraconzole
voriconozle
GI upset
CCF,Dysrrythmias
Visual disturbances
THANK YOU