Name | Hydroxy Itraconazole |
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Synonyms | Itraconazole metabolite Hydroxy Itraconazole |
Description | Itraconazole metabolite Hydroxy Itraconazole is an active metabolite of Itraconazole (ITZ), which is a triazole antifungal agent. |
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Related Catalog | |
Target |
Antifungal[1] |
In Vitro | Hydroxy Itraconazole (OH-ITZ) is an active metabolite of Itraconazole (ITZ). Although OH-ITZ is also reported to have antifungal activity in vitro, its pharmacokinetics in humans has been studied less than that of ITZ. ITZ and OH-ITZ have a triazole ring and inhibit CYP3A. Their half-lives can be extended by 26-60% with repeated administration compared to single administration[1]. |
In Vivo | The plasma concentration of OH-ITZ is weakly dependent on the dose of ITZ, most likely because the process that forms OH-ITZ is saturated. Serum albumin and GFR may alter the pharmacokinetics of ITZ and OH-ITZ. Antifungal activity should be discussed while taking into account not only the plasma concentration of ITZ but also that of OH-ITZ. However, the pharmacokinetics of OH-ITZ is similar to that of ITZ in immunocompromised patients taking an oral solution of ITZ. Since the plasma concentrations of ITZ and OH-ITZ are closely correlated, determining the plasma concentration of either should be sufficient from a clinical point of view[1]. |
References |
Density | 1.44g/cm3 |
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Boiling Point | 884.7ºC at 760mmHg |
Melting Point | 76-78ºC |
Molecular Formula | C35H38Cl2N8O5 |
Molecular Weight | 721.63 |
Flash Point | 488.8ºC |
PSA | 103.95000 |
LogP | 4.96710 |
Vapour Pressure | 0mmHg at 25°C |
Index of Refraction | 1.687 |
Storage condition | 2-8℃ |