SOCI 3630 Chapter Notes - Chapter 1.9: Hematopoietic Stem Cell Transplantation, Amphotericin B, Lanosterol
4 Jun 2020
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Ketoconazole: substituted imidazole that blocks demethylation of lanosterol, and prevents ergosterol from being made-it affects fungal membrane function and permeability. Miconazole, clotrimazole and econazole are closely related but only used topically. Pharmacokinetics: given orally, well absorbed (but we should avoid food and antacids, acidic drinks increase uptake) Highly bound to serum proteins, does not enter cerebral-spinal fluid. Metabolized by liver, excreted in bile, which inhibits cypp450 3a4. Should never be used with amphotericin b (because ketoconazole blocks ergosterol synthesis, amphotericin b binds to ergosterol-so the amphotericin b would be attacking our cells!). But we"ve given them both in studies and they both work. Potentiates the effects of cyclosporine, phenytoin, terfenadine, astemizole. Fluconazole: inhibits lanosterol conversion to ergosterol, but it doesn"t disrupt endocrine function (like ketoconazole does. Can be used prophylactically for bone marrow transplant. It was good at suppressing infections bone transplant people got. (ie. cryptococcus, candidiasis, histoplasmosis) Does not coat plasma proteins, will cross into csf easily.
