泊沙康唑属于第二代三唑类抗真菌药物，其抗菌谱和药物代谢过程有别于其他三唑类药物，口服混悬液、肠溶片和注射剂分别于2005、2013和2014年经美国食品药品监督管理局批准先后上市。沙康唑与其他三唑类抗真菌药物作用机制相似，主要通过抑制细胞色素P450依赖的14α-脱甲基酶进而抑制麦角甾醇的合成，导致真菌细胞膜的生物合成障碍，细胞膜通透性改变，从而抑制真菌生长。

Posaconazole belongs to the second generation of triazole antifungal drugs, whose antibacterial spectrum and drug metabolic process are different from other triazole drugs. Oral suspension, enteric-coated tablet and injection were approved by THE US Food and Drug Administration in 2005, 2013 and 2014 respectively. The mechanism of action of saconazole is similar to that of other triazole antifungal drugs, which mainly inhibits the synthesis of ergosterol by inhibiting cytochrome P450-dependent 14α -demethylase, leading to the biosynthesis disorder of fungal cell membrane and the change of cell membrane permeability, thus inhibiting the growth of fungi.

泊沙康唑

　　泊沙康唑在三唑类母环基础上延伸出一条侧链，苯环中氟取代氯，同时侧链进行羟基化，一系列结构改造使其和真菌亲和力更强，稳定性更高，细胞毒性增加，在保留药物亲脂性的同时水溶性增加，更容易进入组织并释放。另外，长侧链结构增加了药物对靶点(CYP51)的亲和力，对人类细胞色素P450酶影响更小，仅是CYP3A4抑制剂，药物活性更高、更安全，而且受14α-脱甲基酶密码子突变的影响更小，与跨膜转运蛋白(外排泵)的结合力更低，更不容易耐药。

　　泊沙康唑的吸收会因剂型不同而有差异，主要在胃部溶解，在十二指肠部位吸收。口服混悬液口服后3 h达血药峰浓度(Cmax)，7～10 d达稳态血药浓度，其吸收不受性别、年龄、种族和体质量等因素影响，而服用时间、方法、次数和某些药物则会明显影响其吸收。国外PK研究显示，餐后服用、分4次服用、与营养液同服、与碳酸饮料同服，药物吸收将分别增加了约3.6倍、1.5倍、0.6倍、和0.8倍；而与质子泵抑制剂类药物和甲氧氯普胺同服，药物吸收则将分别减少了约2/5和1/5；此外泊沙康唑的吸收还受腹泻、胃肠道黏膜炎等机体状态影响。

The absorption of Posaconazole varies depending on the dosage form and is mainly dissolved in the stomach and absorbed in the duodenum. The absorption of the suspension was not affected by gender, age, race and body weight, but by time, method, frequency and some drugs. Foreign PK studies showed that drug absorption increased by about 3.6 times, 1.5 times, 0.6 times and 0.8 times when taken after meals, divided into 4 times, taken with nutrient solution, and taken with carbonated drinks, respectively. When taken with proton pump inhibitors and metoclopramide, absorption was reduced by about two-fifths and one-fifth, respectively. In addition, the absorption of Posaconazole is also affected by diarrhea and gastrointestinal mucositis.