Te Dorsthorst D T A, Verweij P E, Meis J F G M, Punt N C, Mouton J W
Department of Medical Microbiology and Infectious Diseases, Canisius Wilhelmina Hospital, Weg door Jonkerbos 100, 6532 SZ Nijmegen, The Netherlands.
Antimicrob Agents Chemother. 2004 Jun;48(6):2007-13. doi: 10.1128/AAC.48.6.2007-2013.2004.
Combination therapy of flucytosine (5FC) with other antifungal agents could be of use for the treatment of invasive aspergillosis. However, interpretation of the results of in vitro interactions is problematic. The fractional inhibitory concentration (FIC) index is the most commonly used method, but it has several major drawbacks in characterizing antifungal drug interaction. Alternatively, a response surface approach using the concentration-effect relationship over the whole concentration range instead of just the MIC can be used. We determined the in vitro interactions between amphotericin B (AMB), itraconazole, and 5FC against 21 Aspergillus isolates with a broth microdilution checkerboard method that employs the dye MTT [3-(4,5-dimethyl-2-thiazolyl)-2,5-diphenyl-2H-tetrazolium bromide]. FIC indices based on three different MIC endpoints (MIC-0, MIC-1, and MIC-2) and the interaction coefficient alpha were determined, the latter by estimation from the response surface approach described by Greco et al. (W. R. Greco, G. Bravo, and J. C. Parsons, Pharmacol. Rev. 47:331-385, 1995). The value obtained for the FIC index was found to be dependent on the MIC endpoint used and could be either synergistic, indifferent, or antagonistic. The response surface approach gave more consistent results. Of the three combinations tested, the AMB-5FC combination was the most potent in vitro against Aspergillus spp. We conclude that the use of the response surface approach for the interpretation of in vitro interaction studies of antifungals may be helpful in order to predict the nature and intensity of the drug interaction. However, the correlation of these results with clinical outcome remains difficult and needs to be further investigated.
氟胞嘧啶(5FC)与其他抗真菌药物联合治疗可用于侵袭性曲霉病的治疗。然而,体外相互作用结果的解读存在问题。分数抑菌浓度(FIC)指数是最常用的方法,但在表征抗真菌药物相互作用方面存在几个主要缺点。另外,可以使用一种响应面方法,该方法利用整个浓度范围内的浓度-效应关系,而不仅仅是最低抑菌浓度(MIC)。我们采用肉汤微量稀释棋盘法,使用染料MTT [3-(4,5-二甲基-2-噻唑基)-2,5-二苯基-2H-四氮唑溴盐],测定了两性霉素B(AMB)、伊曲康唑和5FC对21株曲霉分离株的体外相互作用。基于三个不同的MIC终点(MIC-0、MIC-1和MIC-2)确定了FIC指数,并通过Greco等人(W. R. Greco、G. Bravo和J. C. Parsons,Pharmacol. Rev. 47:331-385,1995)描述的响应面方法估计了相互作用系数α。发现FIC指数的值取决于所使用的MIC终点,可能是协同、无关或拮抗的。响应面方法给出了更一致的结果。在所测试的三种组合中,AMB-5FC组合在体外对曲霉属最有效。我们得出结论,使用响应面方法解释抗真菌药物的体外相互作用研究可能有助于预测药物相互作用的性质和强度。然而,这些结果与临床结果的相关性仍然难以确定,需要进一步研究。