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泊沙康唑是第二代三唑类抗真菌药,该口服液通过抑制细胞色素P450依赖的14α-脱甲基酶(CYP51)发挥抗真菌活性。泊沙康唑口服生物利用度变异大,随高脂餐同服吸收率最高,分次给药可增加其生物利用度。在体内蛋白结合率达98%,单次给药后5～8 h血药浓度达峰。泊沙康唑的表观分布容积与给药方案相关,组织分布广泛,穿透力强,口服给药后7～10 d达稳态血药浓度,通过尿苷二磷酸葡萄糖醛酸转移酶途径代谢。泊沙康唑是细胞色素酶CYP3A4的抑制剂,经此通路代谢的药物可受泊沙康唑的影响,血药浓度升高。泊沙康唑主要经消化道清除,清除半衰期20～66 h,口服耐受性良好,不良反应轻微。
Posaconazole is a second-generation triazole antifungal agent that exerts anti-fungal activity by inhibiting cytochrome P450-dependent 14α-demethylase (CYP51). Posaconazole oral bioavailability of variation, with the same high-fat meal with the highest absorption rate, divided doses can increase its bioavailability. In vivo protein binding rate of 98%, after a single administration of 5-8 h plasma concentration peak. The apparent volume of distribution of posaconazole is related to the dosing regimen. The tissue distribution is broad and has strong penetrating power. The steady-state plasma concentration is reached at 7-10 d after oral administration, and the urinary diphosphate glucuronosyltransferase metabolism. Posaconazole is an inhibitor of cytochrome CYP3A4, and drugs that are metabolized by this pathway can be affected by posaconazole with elevated plasma concentrations. Posaconazole mainly through the digestive tract clearance half-life of 20 ~ 66 h, good oral tolerance, minor adverse reactions.