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核糖霉素、达地米星、地贝卡星、卡那霉素、阿米卡星、妥布霉素、庆大霉素、西索米星和奈替米星对豚鼠内耳的比较耳毒性

Comparative ototoxicity of ribostamycin, dactimicin, dibekacin, kanamycin, amikacin, tobramycin, gentamicin, sisomicin and netilmicin in the inner ear of guinea pigs.

作者信息

Kitasato I, Yokota M, Inouye S, Igarashi M

机构信息

Research and Development, Meiji Seika Kaisha, Ltd., Tokyo, Japan.

出版信息

Chemotherapy. 1990;36(2):155-68. doi: 10.1159/000238762.

Abstract

Nine aminoglycoside antibiotics, ribostamycin (RSM), dactimicin (DAC), dibekacin (DKB), kanamycin (KM), amikacin (AMK), netilmicin (NTL), tobramycin (TOB), gentamicin (GM) and sisomicin (SISO) were administered intramuscularly to guinea pigs for 4 weeks, and ototoxicity and drug concentration in the inner ear fluid were determined. RSM and DAC showed the weakest ototoxicity against the cochlea and vestibular organs. AMK and KM were more toxic to cochlea than vestibular organs. DKB, TOM, GM and SISO were equally toxic to vestibular organs and cochlea. NTL was more toxic to vestibular organs than cochlea. As judged from the pinna reflex response and hair cell damage in the cochlea, the order of auditory toxicity was the following: SISO greater than GM greater than TOB greater than AMK greater than DKB greater than KM greater than NTL, DAC RSM, whereas the vestibular toxicity was in the following order: SISO greater than GM greater than DKB greater than TOB greater than NTL greater than AMK greater than KM greater than DAC, RSM. RSM, causing the weakest ototoxicity, showed a low drug concentration in the inner ear fluid, while GM, causing severe ototoxicity, showed the highest drug level under the same conditions.

摘要

将九种氨基糖苷类抗生素,即核糖霉素(RSM)、达地米星(DAC)、双去氧卡那霉素(DKB)、卡那霉素(KM)、阿米卡星(AMK)、奈替米星(NTL)、妥布霉素(TOB)、庆大霉素(GM)和西索米星(SISO),对豚鼠进行肌肉注射,持续4周,然后测定其耳毒性以及内耳液中的药物浓度。RSM和DAC对耳蜗和前庭器官的耳毒性最弱。AMK和KM对耳蜗的毒性大于对前庭器官的毒性。DKB、TOB、GM和SISO对前庭器官和耳蜗的毒性相同。NTL对前庭器官的毒性大于对耳蜗的毒性。从耳廓反射反应和耳蜗毛细胞损伤判断,听觉毒性顺序如下:SISO>GM>TOB>AMK>DKB>KM>NTL>DAC>RSM,而前庭毒性顺序如下:SISO>GM>DKB>TOB>NTL>AMK>KM>DAC>RSM。引起最弱耳毒性的RSM在内耳液中的药物浓度较低,而引起严重耳毒性的GM在相同条件下药物水平最高。

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