Anti-Fungal Agents Flashcards
Bacterial derivative of Amphotericin B
Streptomyces nodosus
MOA of Amphotericin B
Binding to ergosterol to create pores leading to increased cell permeability and lysis
Therapeutic uses of amphotericin B
Used as induction regime and treatment of all life-threatening mycotic infections; immunosuppressed individuals
Adverse effects of amphotericin B
Nephrotoxicity (decreased EPO) causing anemia; infusion related toxicity
New AMB Formulations
AMB Lipid Complex (ABLC)
AMB colloidal dispersion (ABCD)
Liposomal AMB
Drug of choice for nearly all life-threatening mycotic infections
New AMB formulations
New AMB formulation that deliver AMB to reticuloendothelial cells in the liver and spleen
Liposomal AMB
These drugs produce lower AMB levels
ABLC and ABCD
Polyene macrolide active against Candida spp.
Nystatin
Therapeutic usage of nystatin
Oropharyngeal thrush, vaginal candidiasis and intertriginous candidal infections
Pharmacokinetics of nystatin
use only as topical agent “swish and spit or swish and swallow”
MOA of azoles
inhibit lanosterol 14-demethylase leading to decreased ergosterol synthesis
Azole type with lesser degree of specificity causing higher drug interactions and side effects
Imidazole
Azole type with lower toxicity and less propensity to inhibit mammalian sterol synthesis
Triazole
Common effect of azole groups
Both groups affect CYP450 causing a drug-drug interaction
Azole with 3 nitrogen atoms with good oral absorption and high propensity to inhibit mammalian CYP450
Ketoconazole
Adverse effects of Ketoconazole
Reduction in testosterone synthesis and suppression of estradiol synthesis
Drugs that decrease absorption of ketoconazole
H2 blockers, PPI, and antacids
Drugs that decrease efficacy and induce metabolism of ketoconazole
Rifampicin
Phenobarbital
Carbamazepine
Phenytoin