What is the MOA for azole antifungal? 3
- Inhibit fungal P450 enzymes
- Inhibits ergosterol synthesis by inhibiting 14-demethylase
- Results in fungistasis
What is the primary indication for flucanazole use? 3
- Systemic candidiasis
- Vaginal and oropharyngeal candidiasis
- Cryptococcal meningitis
What are the routes of administration for flucanazole? 2
- IV
- Oral
What adverse effects are assoicated with fluconazole? 3
- Nausea
- Vommiting
- Rash
What PK are important to fluconazole?
- Good CSF penetration
- Least effect on hepatic enzymes
What is the primary indication for itraconazole? 4
- Oropharyngeal and oesophageal candidiasis
- Dematophytes
- Onychomycosis
- Dimorphic fungi infecs
What is the route of administration for itraconazole?
Oral/ oral solution
What are the adverse effects of itraconazole?
Hepatotoxic
What are the drug interaction for itraconazole? 3
- Inhibit P450 enzymes
- antacids
- PPI
PK notes on itraconazole?
Requires acid medium for absorption; avoid antacids
What is primary indication for voriconazole?
- Aspergiliosis
- Candidiasis
What is the route of administration for voriconazole?
oral
What are the adverse effects associated with voriconazole? 3
- Visual disturbance
- Hepatotoxic
- PS dermatitis
What is the primary indication for ketoconazole?
Dermatophytes:
- Seborrhoeic dermatitis
- Pityriasis vericolor
What is the route of administration for ketoconazole?
Topical
What is the indication for clotrimazole? 3
- Dermatophytes
- Oral candidiasis
- Vaginal candidiasis
PK about clotrimazole
clotrimazole lozenges are pleasent tasting alt to nyastatin
What are the routes of administration for clotrimazole? 3
- Topical
- Lozenges
- Vaginal cream
What are the adverse effects associated with azoles? 6
- Hepatotoxic
- Nausea
- Vommiting
- Diahorrea
- Headache
- Skin rash
What are the contrai-indications on azole use?
Pregnancy: teratogenic
List the azoles. 5
FICKV
- Fluconazole
- Itraconazole
- Voriconazole
- Ketoconazole
- Clotriconazole
What is the MOA for polyene macrolide antifungals?
Bind to ergosterol and forms pores in the fungal cell membrane
List the polyene macrolides 2
- Amphotericin B
- Nystatin
What is the primary indication for amphotericin b?
- Drug of choice for most serious systemic infection (broad sprectrum):
- Systemic candida
- cryptococcus
- aspergilus
- histoplasma
- blastomyces
- coccidiosis
- Used as induction therapy and then replaced by a newer azole drug of choice once fungal burden is reduced
What is the route of administration for amphotericin b?
IV
What are the adverse effects of amphotericin B? 10
- NEPHROTOXIC
Adverse effects can be groups as:
Infusion reactions:
- Fever
- Chills
- Headache
- Myalgia
- Nausea and vommiting and
- Hypotension
Cumulative toxicity:
- Renal impairment
- Renal tubular acidosis: hypokalaemia and hypomagensaemia
- Anaemia
What are the drug interactions? 5
- Aminglycosides
- Tenofovir
- Ciclosporin
- Diuretics
- Digoxin
What is primary indication for nystatin use?
Superfiicial candidiasis (oral and vaginal)
What is the route of administration for nystatin? 4
- Topical
- Topical oral solution
- Vaginal tablet
- Vaginal cream
What are the adverse effect of nystatin?
unpleasant taste
