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Posaconazole

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  • 1. POSACONAZOLE Dr.Sangeetha P
  • 2. FUNGUS
    • Yeasts
    • Filamentous fungi/moulds
    • - Dermatophytes
    • - Opportunistic fungi
    • Dimorphic fungi
  • 3. MYCOSES – CLINICAL CLASSIFICATION
    • Superficial
    • Deep
    • Opportunistic
  • 4. ANTIFUNGAL AGENTS
    • Antibiotics
    • Polyenes
    • Griseofulvin
    • Azoles
    • Imidazoles
    • Triazoles
    • Allylamines
    • Antimetabolites
    • Echinocandins
  • 5.  
  • 6.  
  • 7.
    • (-)Lanosterol demethylase
    • (-)Ergosterol synthesis
    • (-)The cell membrane
    (-)The cell membrane
  • 8.  
  • 9. WHY NEW AZOLES ?
    • Broader spectrum
    • Low toxicity
    • Oral preparations
  • 10. POSACONAZOLE
    • Latest drug in triazole group
    • Broadest spectrum azole
    • Approved by FDA on 2006
    • “ Noxafil”
  • 11. MECHANISM OF ACTION
    • (-)Lanosterol demethylase
    • (-)Ergosterol synthesis
    • (-)The cell membrane
  • 12. PHARMACOKINETICS
    • Only as oral suspension
    • Fatty food absorption
    • High tissue penetration
    • Low CSF penetration
    • Potent inhibitor of CYP-3A4
    • Mainly excreted through bile
    • No dose reduction in elderly, liver or renal ds
  • 13. SPECTRUM - AZOLES
    • Broad spectrum
    • Covers yeasts, filamentous fungi (Dermatophytes) & dimorphic fungi
    • weak against opportunistic fungi !(aspergillosis,mucor mycosis etc)
  • 14. POSACONAZOLE SPECTRUM
    • Broad spectrum like other azoles
    • covers opportunistic fungi also
  • 15. STUDIES
    • 1: Posaconazole vs Fluconazole for prophylaxis of invasive fungal infections
    • in transplant recepients
    • 2: Posaconazole vs fluconazole in neutropenic patients
  • 16. 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)
  • 17. DOSE
    • Prophylaxis of invasive fungal infections-200mg TDS(40mg/ml)
    • Oropharyngeal Candidiasis - 100mg BD
    • Refractory cases – up to 400mg BD
  • 18. CONTRAINDICATIONS
    • Children 13 yrs
    • Pregnancy
    • Nursing mother
  • 19. POSACONAZOLE ADR
    • Gastrointestinal upset
    • Hepatotoxicity
    • Neutropenia
    • Drug interactions (CYP3A4)
  • 20. AZOLES-S/E
    • Fluconazole
    • Itraconzole
    • voriconozle
    • GI upset
    • CCF,Dysrrythmias
    • Visual disturbances
  • 21. THANK YOU