Pai Manjunath P, Samples Marie L, Mercier Renee-Claude, Spilde Michael N
College of Pharmacy, MSC09 5360, 1 University of New Mexico, Albuquerque, NM 87131, USA.
Antimicrob Agents Chemother. 2008 Jul;52(7):2367-76. doi: 10.1128/AAC.01557-07. Epub 2008 Apr 21.
In vitro pharmacodynamic model (PDM) simulation of serum antifungal concentrations may predict the value of combination antifungal regimens against Candida sp. endocarditis. We investigated the effects of combinations of flucytosine (5FC), micafungin (Mica), and voriconazole (Vor) against Candida-infected human platelet-fibrin clots, used as simulated endocardial vegetations (SEVs). Single clinical bloodstream isolates of Candida albicans, Candida glabrata, Candida parapsilosis, and Candida tropicalis were used. All four isolates were susceptible to 5FC, while C. glabrata was resistant to Vor and C. tropicalis had a paradoxical resistance phenotype to Mica. The SEVs were prepared with an initial inoculum of 1 x 10(6) CFU/g of SEV and added to a PDM, which utilized yeast nitrogen broth-2% glucose and incubation at 35 degrees C and simulated antifungal pharmacokinetic profiles. Fungal densities in the SEVs were determined in quadruplicate over 72 h. Scanning electron microscopy (SEM) was used to evaluate treatment and control SEVs. Vor was the least active single agent against all Candida spp. except for C. parapsilosis, where it was comparable to Mica. In contrast, 5FC was the most active against all Candida spp. except for C. tropicalis, where it was comparable to Mica. The combination of 5FC plus Vor was superior to either agent alone against C. parapsilosis. The combination of Vor plus Mica was inferior to the use of Mica alone against C. tropicalis. The triple combination of 5FC plus Vor plus Mica was no better than single or dual agents against any of the Candida spp. The ultrastructural features of infected SEVs were unique for each Candida sp., with C. parapsilosis in particular manifesting friable biofilm clusters. In general, 5FC and Mica were superior in their rates and extents of fungal burden reduction compared to Vor against Candida-infected SEVs. Evaluation of 5FC and Mica in animal models of Candida endocarditis is warranted.
血清抗真菌浓度的体外药效学模型(PDM)模拟可预测联合抗真菌方案治疗念珠菌性心内膜炎的价值。我们研究了氟胞嘧啶(5FC)、米卡芬净(Mica)和伏立康唑(Vor)联合用药对念珠菌感染的人血小板 - 纤维蛋白凝块(用作模拟心内膜赘生物(SEV))的影响。使用了白色念珠菌、光滑念珠菌、近平滑念珠菌和热带念珠菌的单株临床血流分离株。所有这四种分离株对5FC敏感,而光滑念珠菌对Vor耐药,热带念珠菌对Mica表现出矛盾的耐药表型。制备初始接种量为1×10(6) CFU/g SEV的SEV,并将其添加到PDM中,该模型使用酵母氮肉汤 - 2%葡萄糖,在35℃下孵育并模拟抗真菌药代动力学特征。在72小时内对SEV中的真菌密度进行四次测定。使用扫描电子显微镜(SEM)评估治疗组和对照组的SEV。除近平滑念珠菌外,Vor对所有念珠菌属的活性最低,在近平滑念珠菌中其活性与Mica相当。相比之下,5FC对除热带念珠菌外的所有念珠菌属活性最高,在热带念珠菌中其活性与Mica相当。5FC加Vor的联合用药对近平滑念珠菌的效果优于单独使用任何一种药物。Vor加Mica的联合用药对热带念珠菌的效果不如单独使用Mica。5FC加Vor加Mica的三联用药对任何念珠菌属的效果都不比单药或双药更好。感染SEV的超微结构特征因每种念珠菌属而异,特别是近平滑念珠菌表现出易碎的生物膜簇。总体而言,与Vor相比,5FC和Mica在降低念珠菌感染SEV的真菌负荷的速率和程度方面更具优势。有必要在念珠菌性心内膜炎动物模型中评估5FC和Mica。