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53 Cards in this Set
- Front
- Back
Broad spectrum antifungals
|
-amphotericin
-azoles -terbinafine |
|
Narrow spectrum antifungals
|
-grieofulvin
|
|
-Aspergillus spectrum
|
-amphotericin
-itraconazole -voriconazole -terbinafine |
|
Therapeutic drug angle for antifungals
|
-patient
-drug -fungus |
|
Amphotericin B
-organism derived from |
-Streptomyces nodosus
|
|
Amphotericin B
-mechanism of action |
-bind to ergosterol in the cell wall
-increases cell permeability resulting in cell death |
|
Amphotericin B
-adverse effects |
-nephrotoxic at high concentration
-tremors, anorexia, vomiting, pyrexia, phlebitis |
|
Amphotericin B
-oral bioavailability |
-poor
|
|
Amphotericin B
-opthalmic penetration |
-good penetration into aqueous humor
-poor penetration into vitreous humor and CNS |
|
Amphotericin B
-half-life |
-long
|
|
Amphotericin B
-route of elimination |
-hepatic metabolism (renal toxicity if liver disease present)
|
|
Amphotericin B
-efficacy spectrum |
-broad
-Aspergillus & Leishmania |
|
Amphotericin B
-when to use in horses |
-when systemic disease is not responsive to fluconazole
|
|
Azole
-mechanism of action |
-reduce ergosterol through fungal Cyt P450 inhibition
|
|
Azole
-adverse effects |
-nausea, vomiting, anorexia
-hepatotoxicity -CYP inhibition |
|
Ketoconazole
-Spectrum of efficacy |
Broad spectrum
-Aspergillus mostly resistant -Leishmania -Staphylococcus |
|
Ketoconazole should not be used in _______
|
horses
|
|
Ketoconazole
-bioavailability |
Dependent on acid environment
-don't administer w/ acid suppression therapy (PPIs, H2 antagonists, antacids, sucralfate -give with food to increase acid and biliary secretion |
|
Ketoconazole
-route of elimination |
-hepatic metabolism
|
|
Ketoconazole
-adverse effects |
-nausea, anorexia, vomiting, hepatotoxicity
-dec. cortisol synthesis -cataracts -hair coat lightening |
|
Ketoconazole
-Drug interactions |
CYP 3A inhibitor
-drug exposure of time increases because it inhibits its own metabolism P-gp Inhibitor |
|
Itraconazole
-adverse effects |
-CYP inhibition
-minimal effect on steroid synth. -anorexia, vomiting, nausea, hepatotoxicity |
|
Itraconazole
-spectrum of efficacy |
Broad
-Aspergillus (slightly higher than ketoconazole) -Leishmania |
|
Should Itraconazole be used in horses? Why?
|
No, Poor bioavailability making it very expensive to treat with
|
|
Why should compounded formulas of Itraconazole not be used?
|
very unstable
|
|
Itraconazole
-route of elimination |
-hepatic metabolism
|
|
Itraconazole
-dosing |
-daily for systemic fungals
-pulse dosing for dermatophytes |
|
Fluconazole
-efficacy spectrum |
Broad
-Leishmania |
|
Fluconazole
-oral bioavailability |
-Good (even horses)
|
|
Fluconazole
-adverse effects |
-hepatotoxicity
|
|
Fluconazole
-Route of Elimination |
-renal (active in urine)
|
|
Voriconazole
-derivative of |
Fluconazole
|
|
Voriconazole
-efficacy spectrum |
Aspergillus & Fusarium (treatment of choice)
Equine Fungal keratitis |
|
Voriconazole
-bioavailability |
Good oral absorption (even horses)
|
|
Drug of choice for CNS and Aqueous humor penetration
|
Fluconazole
|
|
Voriconazole
-how to administer for accessing aqueous humor |
-topically
|
|
Voriconazole
-adverse effects |
-transient visual distrurbances
-rash -hepatotoxicity |
|
Terbinafine
-mechanism of action |
-Inhibit squalene epoxidase
-decrease ergosterol synthesis |
|
Terbinafine
-efficacy spectrum |
Broad
-Aspergillus -Malassezia |
|
Terbinafine
-CNS penetration |
-poor
|
|
Terbinafine
-route of elimination |
hepatic metabolism
|
|
Terbinafine
-adverse effects |
-vomiting, anorexia
-hepatitis |
|
Griseogulvin
-mechanism of action |
deposition in skin keratin to inhibit fungal mitosis
|
|
Griseofulvin
-efficacy spectrum |
narrow
-dermatophytes |
|
Griseofulvin
-dosing |
-administer with a fatty meal
|
|
Griseofulvin
-route of elimination |
hepatic metabolism
|
|
Griseofulvin
-adverse effects |
-Teratogen (abortion causing)
-anemia, leukopenia (in FIV cats) -Anorexia, depression, vomiting, diarrhea |
|
Topical use only antifungals
-drugs |
-nystatin
-micronazole -clotrimazole -terbinafine |
|
Nystatin
-efficacy spectrum |
Broad
-similar to amphotericin |
|
Nystatin
-primary use |
Malassezia otitis in dogs
|
|
Nystatin
-adverse effects |
renal toxicity with systemic administration
|
|
Miconazole & Clotrimazole
-efficacy spectrum |
Broad
-similar to ketoconazole & Itraconazole |
|
Miconazole & Clotrimazole
-primary uses |
-Malassezia otitis
-local dermatophyte infection -nasal sinus treatment of Aspergillus |