Nontoxic Dose of Antimicrobials for Intravitreal Use in Endophthalmitis.

用于眼内炎玻璃体内使用的无毒剂量的抗菌药物。

• 批准号: 01570972
• 负责人: KAWASAKI Kazuo
• 金额: $ 1.41万
• 依托单位: Kanazawa University
• 依托单位国家: 日本
• 项目类别: Grant-in-Aid for General Scientific Research (C)
• 财政年份: 1989
• 资助国家: 日本
• 起止时间: 1989 至 1991
• 项目状态: 已结题
• 来源: https://kaken.nii.ac.jp/grant/KAKENHI-PROJECT-01570972/
• 关键词: electroretinogram; visually evoked potential; ocular infection; intravitreal injection; vitrectomy; ocular kinetics; antimicrobials; フルコナゾ-ル; BVaraU; ノフロキサシン; 眼内移行; ロメフロキサシン; オフロキサシン; セフタジジム; ガンシクロビル; フロモキセフ

Recently, Propionibacterium acnes, methicfllin-resistant Staphylococcus epidermidis, methicillin-resistant Staphylococcus aureus and gram-positive organisms have become important pathogens in bacterial endophthalmitis after extracapsular cataract extraction with posterior chamber lens implantation or vitrectomy for proliferative diabetic retinopathy. The incidence of viral retinitis and endogenous fungal endophthalmitis has increased with use of immunosuppressive therapy. Therefore the treatment of these disorders is now very important. The treatment with systemically administered antimicrobials is often unsuccessful because of poor penetration into the eye. Therefore, intravitreal administration is needed. The purpose of the present research is to establish the nontoxic intravitreal dose of antimicrobials. Effects of topically applied antimicrobials on the retina were studied in rabbits with electroretinogram, visually evoked potential and histological examination after intravitreal i … More njections or irrigation of an antimicrobial-containing solution. We also studied the intraocular penetration of intravenously injected antimicrobials such as flomoxef, lomefloxacin, ceftazidime and fluconazole under surgical conditions, and intraocular pharmacokinetics of flomoxef, lomefloxacin, ceftazidime and BVaraU after a single intravitreal injection.Our recommended one-shot intravitreal dose of antimicrobials for clinical use is as follows : flomoxef 200-400 mug/0.1 ml, lomeflox ; acin 200 mug/0. I ml, norfloxacin 50 mug/0. I ml, ceftazidime 200-400mug/0. I ml and ganciclovir 100-200mug/0.1 ml. Our recommended concentration of antimicrobials for an intravitreal irrigation solution during vitrectomy is as follows : ofloxacin 50 mug/ml and BVaraU 20 mug/ml. The intravitreal flomoxef or ceftazidime concentration was low in nominal eyes one hour after intravenous injection, and high in vitrectomized eyes when injected immediately after surgery. The lorinefloxacin concentration was low in normal eyes and also in vitrectomized eyes. The high intraocular penetration of fluconazole-was observed in normal eyes as well as in vitrectomized eyes after intravenous administration. Intraocular penetration of fluconazole was not increased by vitrectomy. The half-life in the vitreous humor after intravitreal injection was 4.4 hours for flomoxef, 2.8 hours for lomefloxacin, 7.4 hours for ceftazidime and 2.5 hours for B VaraU. Less

近年来，痤疮丙酸杆菌、耐甲氧西林表皮葡萄球菌、耐甲氧西林金黄色葡萄球菌和革兰氏阳性菌已成为白内障囊外摘除联合后房型透镜植入术或玻璃体切除术治疗增殖性糖尿病视网膜病变后细菌性眼内炎的重要致病菌。病毒性视网膜炎和内源性真菌性眼内炎的发病率随着免疫抑制治疗的使用而增加。因此，这些疾病的治疗现在非常重要。全身给药的抗菌药物治疗通常不成功，因为对眼睛的渗透性较差。因此，需要玻璃体内给药。本研究的目的是确定玻璃体内抗菌药物的无毒剂量。用视网膜电图、视觉诱发电位和组织学检查，观察了局部应用抗菌药物对兔眼玻璃体内注射后视网膜的影响。 ...更多信息 注射或冲洗含抗菌剂的溶液。我们还研究了手术条件下静脉注射氟氧头孢、洛美氟哌酸、头孢他啶和氟康唑等抗菌药物的眼内渗透性，以及单次玻璃体内注射后氟氧头孢、洛美氟哌酸、头孢他啶和BVaraU的眼内药代动力学。我们推荐的临床使用的抗菌药物玻璃体内一次性剂量如下：氟氧头孢200-400 μ g/0.1 ml，洛美氟哌酸; acin 200 mug/0. I ml，诺氟沙星50 μ g/0. I ml，头孢他啶200- 400 μ g/0. 1 ml和更昔洛韦100- 200 μ g/0.1 ml。我们推荐的玻璃体切除术期间玻璃体内冲洗液的抗菌剂浓度如下：氧氟沙星50 μ g/ml和BVaraU 20 μ g/ml。玻璃体内氟氧头孢或头孢他啶的浓度在静脉注射后1小时在标称眼中较低，而在手术后立即注射时在玻璃体切除眼中较高。在正常眼和玻璃体切除眼中，氯氟沙星浓度较低。静脉给药后，在正常眼和玻璃体切除眼中观察到氟康唑的高眼内渗透性。玻璃体切除术不会增加氟康唑的眼内渗透性。玻璃体内注射后，氟氧头孢在玻璃体液中的半衰期为4.4小时，洛美沙星为2.8小时，头孢他啶为7.4小时，B VaraU为2.5小时。少

项目成果

河崎 一夫,鳥崎 真人,望月 清文,山下 陽子,小松 雅樹,棚橋 俊郎,大平 光彦: "フロメキサシン硝子体内注入後の眼内動態" あたらしい眼科. 8. 937-940 (1991)

Kazuo Kawasaki、Masato Torisaki、Kiyofumi Mochizuki、Yoko Yamashita、Masaki Komatsu、Toshiro Tanahashi、Mitsuhiko Ohira：“玻璃体内注射氟美沙星后的眼内动力学”新眼科学 8. 937-940 (1991)。

河崎 一夫,望月 清文,山下 陽子,鳥崎 真人,小松 雅樹: "オキサセフェム系抗生剤の眼内クリアランスーフロモキセフナトリウムー" あたらしい眼科. 7. 415-418 (1990)

Kazuo Kawasaki、Kiyofumi Mochizuki、Yoko Yamashita、Masato Torizaki、Masaki Komatsu：“氧头孢烯抗生素 - 氟氧头孢钠的眼内清除”新眼科杂志 7. 415-418 (1990)。

K.Kawasaki,K.Mochizuki,M.Torisaki,Y.Yamashita,Y.Shirao,K.Wakabayashi and J.Tanabe: "Electroretinographical Changes due to Antimicrobials" Lens and Eye Toxicity Research. 7. 693-704 (1990)

K.Kawasaki、K.Mochizuki、M.Torisaki、Y.Yamashita、Y.Shirao、K.Wakabayashi 和 J.Tanabe：“抗菌药物引起的视网膜电图变化”晶状体和眼睛毒性研究。

河崎 一夫,鳥崎 真人,望月 清文,山下 陽子,小松 雅樹,棚橋 俊郎: "Lomefloxacin硝子体内注入の家兎網膜に及ぼす影響" あたらしい眼科. 7. 1239-1241 (1990)

Kazuo Kawasaki、Masato Torisaki、Kiyofumi Mochizuki、Yoko Yamashita、Masaki Komatsu、Toshiro Tanahashi：“玻璃体内注射洛美沙星对家兔视网膜的影响”新眼科学 7. 1239-1241 (1990)。

Yohko Yamashita, Kiyofumi Mochizuki, Makoto Torisaki, Masaki Komatsu, Kazuo Kawasaki and Shigeo Matsuda: "Pharmacokinetics of Intravitreal Flomoxef in Albino Rabbit." Journal of the Eye (Atarashii Ganka). 7. 415-418 (1990)

Yohko Yamashita、Kiyofumi Mochizuki、Makoto Torisaki、Masaki Komatsu、Kazuo Kawasaki 和 Shigeo Matsuda：“白化兔玻璃体内注射氟氧头孢的药代动力学。”