Anti-fungal Chemotherapy Flashcards
Voriconazole Drug class How is it made? What does it treat? Pros Cons
Triazole antifungal
Newer drug used to treat serious aspergillosis infections and some rarer infections in immunocompromised patients
Ringworm caused by what family?
Trichophyton family
Fluconazole Drug class How is it made? What does it treat? Pros Cons
Triazole antifungal
Synthetic product - inhibits CYP450-14-alpha-demethylase
Can be taken orally, absorption good at any pH
Widely distributed in the body, including the brain
Most active drug in triazole class
Treats cryptococcal infections (including cryptococcal meningitis) and severe oral and oesophageal candidiasis
High doses inhibit androgen synthesis in men
Griseofulvin Drug class How is it made? What does it treat? Pros Cons
Interferes with microtubule assembly
Used to treat skin infections in particular, but taken orally instead of topically
Natural product produced by strains of Penicillum fungi
Does not inhibit Candida
Used rarely nowadays, therapy can last a year
Pneumocystis pneumonia. When is it important? What is it treated with?
Rarely important unless AIDs patients, where it is VERY important
Treated with co-trimoxazole and anti-leishmaniasis drugs
Posaconazole Drug class How is it made? What does it treat? Pros Cons
Triazole antifungal
Normally used 2nd line
Tends to be used in immunocompromised patients
Azole drug class Mechanism of action Examples
Antifungal
Inhibits CYP450-14-alpha-demethylase enzyme
Imidazoles - ketoconazole, miconazole, ticonazole
Triazoles - only these are licensed for use in UK: fluconazole, intraconazole, voriconazole, posaconazole
Azores and polyene can’t be given together as polyene rely on ergosterol binding to work
CYP450-14-a-demethylase is an enzyme used in the conversion of squealing to ergosterol
Candida infections caused by what organism?
The yeast Candida, especially Candida albicans
Terbinafine Drug class How is it made? What does it treat? Pros Cons
Polyene
On WHO list of essential medicines
Used topically/orally for skin infections
Inhibits squalne epoxidase, a rate limiting step in ergosterol synthesis
Accumulates in skin, nails and fatty tissue as hydrophobic drug
Cryptococcosis or cryptococcal meningitis, what group does this cause a lot of death in? Treatment?
Leading cause of death in AIDs patients, in whom nearly always untreatable
Amphotericin B Drug class How is it made? What does it treat? Pros Cons
Polyene antifungal
produced by Streptomyces nodosus
Treats oral infections by local application (not absorbed by mouth)
Used IV for systemic infections
Active against most fungi + yeasts, including cryptococcosis
Toxic - especially to kidneys, and side effects common
Lipid-based formulations are less toxic
Flucocytosine Drug class How is it made? What does it treat? Pros Cons
Antimetabolic antifungal
Targets DNA+RNA synthesis
Transported into fungus via fungal cytosine permeate
Converted to 5-flurouracil by cytosine de-amidase
inhibits DNA+RNA synthesis
Mainly used in combination therapy with amphotericin B
Blastomycosis
Affects lungs of the healthy, mainly young men
Caspofungin Drug class How is it made? What does it treat? Pros Cons Similar to
Broad range, minimal drug interactions
Toxic to embroys
Hepatotoxic
Similar to anidulafungin and micafungin
They are actually fungal products produced by Aspergillus strains
They have minor semi-synthetic modifications
Active against bio films on catheters
Nystatin Drug class How is it made? What does it treat? Pros Cons
Polyene antifungal
Produced by Streptomyces noursei
Treats Candida albicans infections of skin - ointments and creams
