Antifungal Flashcards
Three forms of fungal infections
Superficial, subcutaneous, systemic
Griseofulvin- source
Penicillin
Griseofulvin method-
Fungistatic
Griseofulvin- effective against
Dermatophytosis- Microsporum, epidermophyton, trichophyton- no effect on others!
Most common fungal disease in cats
Dermatophytosis
Griseofulvin- mechanism
Active on growing cells, binds to intracellular microtubules to inhibit mitosis, nucleic acid and protein synthesis, chitin synthesis
Griseofulvin- how does it reach skin
In sweat, incorporated in keratin loosely- undetectable in skin 2-3 days
Griseofulvin- time to reach skin after admin’n
4-8 hours
Griseofulvin- absorption dependent on
Formulation (microsize or ultramicrosize particles in polyethylene glycol) and food (increase absorption with fatty meal)
Griseofulvin- metabolism
Oxidation by hepatic enzyme; 6 times faster than in people
Griseofulvin- duration of tx
min 4 weeks, sometimes over 3 months
Griseofulvin- interactions
phenobarb decreases absorption
Griseofulvin- adverse
Bad taste- nausea, V, D; bone marrow suppression in cats with FIV or persians/himalayans/siamese/abyss - CBC q 2 weeks
Griseofulvin- Contraindications
HIGHLY teratogenic- DO NOT GIVE TO PREGNANT ANIMALS - brain and skeletal malformations, eye issues, absence of nostrils, soft palate
Amphotericin B- method
static or cidal depending on dose; Punches holes in cell membrane by binding to sterols (fungal and mammalian = not specific)- leakage until death
Amphotericin B- uses
Cryptococcosis, blasto, histoplasmosis, coccidiomycosis - only in serious cases due to possible toxicity due to lack of sterol specificity (Think ampho blasto histo, cocco)
Amphotericin B- route
IV only- no oral absorption
Amphotericin B- cautions
Dehydration increases toxicity so administer in 5% dextrose after saline diuresis; max cumulative dose before danger
Amphotericin B- metabolism
KIDNEY- high protein binding, 24 hour half life
Amphotericin B- limit
4-8 mg/kg (higher if done subcutaneous)
Amphotericin B-best formulations
liposomal- better brain penetration and longer half life leads to less dose needed
Amphotericin B- side effects
Thrombophlebitis, nephrotixicity (vasoconstriction and renal tubule toxicity), hypokalemia, resistance over time
Ketoconazole- method
static/cidal
Ketoconazole- mechanism
Inhibit lanosterol 12-demethylase; suppresses p450!!!!!
All azoles do what?
Interfere with p450- ex. cyclosporin dose lowered when on azole