DƯỢC LÍ Goodman & Gilman's The Pharmacological Basis of Therapeutics 12th, 2010

Table 57-6
Some Additional Contraindicated Azole Drug Combinations
DRUG FLUCONAZOLE VORICONAZOLE ITRACONAZOLE POSACONAZOLE
Alfuzosin x x x
Artemether x x
Bepridil
x
Clopidogrel
x
Conivaptan x x x x
Dabigatran
x
Darunavir
x
Dronedarone x x x x
Everolimus x x x x
Lopinavir
x
Lumefantrine x x
Mesoridazine
x
Nilotinib x x x x
Nisoldipine use with caution x x x
Quinine x x
Rifapentine x use with caution use with caution
Ritonavir x use with caution
Rivaroxaban x x
Salmeterol x x x
Silodosin x x x
Simvastatin use with caution x
St. John’s wort
x
Tetrabenazine x x
Thioridazine x x
Tolvaptan x x x
Tolvaptan x x
Topotecan
x
Ziprasidone x x
possessing three chiral centers. The structure is similar
to that of the imidazole ketoconazole.
Absorption, Distribution, and Excretion. Itraconazole (SPORANOX,
others) is available as a capsule and a solution in hydroxypropylβ-cyclodextrin
for oral use. The capsule form of the drug is best
absorbed in the fed state, but the oral solution is better absorbed in
the fasting state, providing peak plasma concentrations >150% of
those obtained with the capsule. Itraconazole is metabolized in the
liver. It is both a substrate for and a potent inhibitor of CYP3A4.
Itraconazole is present in plasma with an approximately equal concentration
of a biologically active metabolite, hydroxy-itraconazole.
Bioassays may report up to 3.3 times as much itraconazole in plasma
as do physical methods such as high-performance liquid chromatography,
depending on the susceptibility of the bioassay organism to
hydroxy-itraconazole. The native drug and metabolite are >99%