Yokoya Y, Ikeda F, Mine Y
Pharmacological Research Laboratories, Fujisawa Pharmaceutical Co., Ltd.
Kansenshogaku Zasshi. 1993 Sep;67(9):808-15. doi: 10.11150/kansenshogakuzasshi1970.67.808.
Since Helicobacter pylori is isolated very frequently from gastric ulcer specimens, the combination therapy of antimicrobial agent and proton pump inhibitor has recently been used. A study was made on whether cefdinir (CFDN), amoxicillin (AMPC), metronidazole (MNZ), omeprazole (OPZ), and omeprazole-M (OPZ-M) have antimicrobial activity against H. pylori and whether they can inhibit H. pylori-producing urease. 1) CFDN, AMPC and MNZ showed a potent antimicrobial activity against H. pylori, and especially, AMPC showed a marked bactericidal activity in a short time. 2) OPZ is reported to be converted to OPZ-M, and active form, in the body. OPZ and OPZ-M showed a moderate antimicrobial activity against H. pylori, and scarcely any bactericidal activity. 3) CFDN and OPZ or AMPC and OPZ in combination did not show any synergistic effect on the antimicrobial activity, but MNZ and OPZ in combination showed additive effect on the antimicrobial activity against H. pylori. 4) OPZ and OPZ-M inhibited H. pylori-producing urease and the inhibitory effect of OPZ-M was more stronger than that of OPZ. CFDN, AMPC and MNZ did not show any inhibitory effect on H. pylori-producing urease at 10 micrograms/ml. From these data, antimicrobial agents and proton pump inhibitors in combination are expected to exert the in vivo synergistic effect since these drugs eradicate H. pylori and inhibit H. pylori-producing urease.
由于从胃溃疡标本中非常频繁地分离出幽门螺杆菌,因此最近采用了抗菌剂和质子泵抑制剂的联合疗法。对头孢地尼(CFDN)、阿莫西林(AMPC)、甲硝唑(MNZ)、奥美拉唑(OPZ)和奥美拉唑 - M(OPZ - M)是否对幽门螺杆菌具有抗菌活性以及它们是否能抑制幽门螺杆菌产生脲酶进行了研究。1)CFDN、AMPC和MNZ对幽门螺杆菌显示出强大的抗菌活性,尤其是AMPC在短时间内显示出显著的杀菌活性。2)据报道,OPZ在体内会转化为其活性形式OPZ - M。OPZ和OPZ - M对幽门螺杆菌显示出中等抗菌活性,几乎没有杀菌活性。3)CFDN与OPZ联合或AMPC与OPZ联合在抗菌活性上未显示出任何协同作用,但MNZ与OPZ联合对幽门螺杆菌的抗菌活性显示出相加作用。4)OPZ和OPZ - M抑制幽门螺杆菌产生脲酶,且OPZ - M的抑制作用比OPZ更强。CFDN、AMPC和MNZ在10微克/毫升时对幽门螺杆菌产生脲酶未显示出任何抑制作用。从这些数据来看,抗菌剂和质子泵抑制剂联合使用有望发挥体内协同作用,因为这些药物可根除幽门螺杆菌并抑制幽门螺杆菌产生脲酶。