克霉唑（拜耳b 5097）：体外及临床药理学研究。
Clotrimazole (Bay b 5097): in vitro and clinical pharmacological studies.
作者信息
Burgess M A, Bodey G P
出版信息
Antimicrob Agents Chemother. 1972 Dec;2(6):423-6. doi: 10.1128/AAC.2.6.423.
Abstract
Clotrimazole (Bay b 5097) is a new synthetic antifungal drug with in vitro activity against Candida spp., Torulopsis glabrata, and Saccharomyces spp. Pharmacological studies in man after the oral administration of 1.5 and 3 g of clotrimazole produced mean peak concentrations in the serum of 1.16 and 1.29 mug/ml, respectively, 2 hr after administration. In six patients taking 1.5 g of clotrimazole every 6 hr, there was a progressive decline in the serum concentrations after administration of a dose on days 1, 4, and 8. Nine other patients begun on a similar schedule manifested gastrointestinal symptoms attributed to the clotrimazole and were unable to complete the study. Concentrations of active drug in the urine were less than 1% of the administered dose.
摘要
克霉唑（拜耳b 5097）是一种新型合成抗真菌药物，对念珠菌属、光滑球拟酵母菌和酿酒酵母属具有体外活性。口服1.5克和3克克霉唑后，人体药理学研究显示给药后2小时血清中的平均峰值浓度分别为1.16微克/毫升和1.29微克/毫升。在6名每6小时服用1.5克克霉唑的患者中，在第1天、第4天和第8天给药后血清浓度呈逐渐下降趋势。另外9名开始采用类似给药方案的患者出现了归因于克霉唑的胃肠道症状，无法完成研究。尿液中活性药物的浓度低于给药剂量的1%。
相似文献
1
Clotrimazole (Bay b 5097): in vitro and clinical pharmacological studies.克霉唑（拜耳b 5097）：体外及临床药理学研究。
Antimicrob Agents Chemother. 1972 Dec;2(6):423-6. doi: 10.1128/AAC.2.6.423.
2
Laboratory assessment of the antimycotic drug clotrimazole.抗真菌药物克霉唑的实验室评估。
J Clin Pathol. 1972 Dec;25(12):1089-97. doi: 10.1136/jcp.25.12.1089.
3
A comparison of bifonazole (BAY H 4502) with clotrimazole in vitro.联苯苄唑（BAY H 4502）与克霉唑的体外比较。
Sabouraudia. 1982 Dec;20(4):313-23.
4
In vitro sensitivity of Torulopsis glabrata to amphotericin B, 5-fluorocytosine, and clotrimazole (Bay 5097).光滑球拟酵母对两性霉素B、5-氟胞嘧啶和克霉唑（Bay 5097）的体外敏感性
Appl Microbiol. 1971 Jul;22(1):93-5. doi: 10.1128/am.22.1.93-95.1971.
5
Superficial mycoses and in vitro sensitivity of dermatophytes and Candida species to tolciclate and clotrimazole.
Indian J Med Res. 1981 Sep;74:365-71.
6
[Mechanism of action of clotrimazole. I. Study of the principal action on Candida albicans].
Nihon Saikingaku Zasshi. 1973 Nov;28(6):513-21.
7
[Mechanisl of action of clotrimazole. 2. Effects on the cell membrane of Candida albicans].[克霉唑的作用机制。2. 对白色念珠菌细胞膜的影响]
Nihon Saikingaku Zasshi. 1974 Mar;29(2):379-85.
8
In vitro antifungal activity of clotrimazole (Bay b 5097).克霉唑（拜耳b 5097）的体外抗真菌活性。
Infect Immun. 1971 Aug;4(2):143-8. doi: 10.1128/iai.4.2.143-148.1971.
9
The therapy of candida vaginitis and candida vulvovaginitis with a new antimycotic substance, clotrimazole.
Curr Med Res Opin. 1973;1(9):540-6. doi: 10.1185/03007997309111719.
10
Topical treatment with clotrimazole in dermatomycosis.克霉唑局部治疗皮肤真菌病。
Curr Ther Res Clin Exp. 1974 Jan;16(1):27-31.
引用本文的文献
1
Identification of Clotrimazole Derivatives as Specific Inhibitors of Arenavirus Fusion.鉴定克霉唑衍生物为沙粒病毒融合的特异性抑制剂。
J Virol. 2019 Mar 5;93(6). doi: 10.1128/JVI.01744-18. Print 2019 Mar 15.
2
Cavamax W7 composite ethosomal gel of clotrimazole for improved topical delivery: development and comparison with ethosomal gel.克霉唑 Cavamax W7 复合醇质体凝胶经皮给药系统的构建及其与醇质体凝胶的比较
AAPS PharmSciTech. 2012 Mar;13(1):344-55. doi: 10.1208/s12249-012-9754-y. Epub 2012 Jan 27.
3
Antifungal resistance and new strategies to control fungal infections.抗真菌耐药性与控制真菌感染的新策略。
Int J Microbiol. 2012;2012:713687. doi: 10.1155/2012/713687. Epub 2011 Dec 1.
4
The changing face of febrile neutropenia-from monotherapy to moulds to mucositis. Management of mycoses in neutropenic patients: a brief history, 1960-2008.发热性中性粒细胞减少症的变迁——从单一疗法到霉菌感染再到黏膜炎。中性粒细胞减少患者真菌病的管理：简史，1960 - 2008年。
J Antimicrob Chemother. 2009 May;63 Suppl 1(Suppl 1):i23-6. doi: 10.1093/jac/dkp079.
5
Decreased susceptibility of the cytochrome P450 2B6 variant K262R to inhibition by several clinically important drugs.细胞色素P450 2B6变体K262R对几种临床重要药物抑制作用的敏感性降低。
Drug Metab Dispos. 2009 Mar;37(3):644-50. doi: 10.1124/dmd.108.023655. Epub 2008 Dec 12.
6
New antifungal therapy in ophthalmology.眼科领域的新型抗真菌治疗方法。
Trans Am Ophthalmol Soc. 1973;71:233-42.
7
Potent antimalarial activity of clotrimazole in in vitro cultures of Plasmodium falciparum.克霉唑在恶性疟原虫体外培养中具有强大的抗疟活性。
Proc Natl Acad Sci U S A. 2000 Jan 4;97(1):331-6. doi: 10.1073/pnas.97.1.331.
8
Inhibition and killing of Candida albicans in vitro by five imidazoles in clinical use.临床使用的五种咪唑类药物对白色念珠菌的体外抑制和杀灭作用
Antimicrob Agents Chemother. 1984 Apr;25(4):450-4. doi: 10.1128/AAC.25.4.450.
9
Therapy of fungal infections.真菌感染的治疗
Bull N Y Acad Med. 1982 Nov;58(8):721-32.
10
Collaborative evaluation in seven laboratories of a standardized micromethod for yeast susceptibility testing.七个实验室对酵母药敏试验标准化微量方法的协同评估。
J Clin Microbiol. 1988 Nov;26(11):2307-12. doi: 10.1128/jcm.26.11.2307-2312.1988.
本文引用的文献
1
AMPHOTERICIN B TOXICITY; CHANGES IN RENAL MORPHOLOGY.两性霉素B毒性；肾脏形态学变化。
Ann Intern Med. 1964 Aug;61:349-54.
2
[1st clinical experience with a new oral antimycotic in systemic mycoses].
Dtsch Med Wochenschr. 1969 Jun 27;94(26):1365-7 passim. doi: 10.1055/s-0028-1111224.
3
Bay B 5097, a new orally applicable antifungal substance with broadspectrum activity. Preliminary clinical and laboratory experiences in children.Bay B 5097，一种新的具有广谱活性的口服抗真菌物质。儿童的初步临床和实验室经验。
Acta Paediatr Scand. 1971 May;60(3):341-5. doi: 10.1111/j.1651-2227.1971.tb06668.x.
4
In vivo studies with Bay b 5097.使用Bay b 5097进行的体内研究。
Antimicrob Agents Chemother (Bethesda). 1970;10:169-74.
5
Persistent fungemia caused by Torulopsis glabrata: treatment with amphotericin B.光滑假丝酵母菌引起的持续性真菌血症：两性霉素B治疗
Am J Clin Pathol. 1970 Aug;54(2):205-8. doi: 10.1093/ajcp/54.2.205.
6
Saccharomyces fungemia.酵母菌血症
Chest. 1970 Aug;58(2):173-5. doi: 10.1378/chest.58.2.173.
7
BAY b 5097, a new orally applicable antifungal substance with broad-spectrum activity.
Antimicrob Agents Chemother (Bethesda). 1969;9:271-4.
8
Fungal infections complicating acute leukemia.急性白血病合并真菌感染。
J Chronic Dis. 1966 Jun;19(6):667-87. doi: 10.1016/0021-9681(66)90066-x.
9
In vitro sensitivity of Torulopsis glabrata to amphotericin B, 5-fluorocytosine, and clotrimazole (Bay 5097).光滑球拟酵母对两性霉素B、5-氟胞嘧啶和克霉唑（Bay 5097）的体外敏感性
Appl Microbiol. 1971 Jul;22(1):93-5. doi: 10.1128/am.22.1.93-95.1971.
10
Pulmonary aspergillomata in a child treated with clotrimazole.用克霉唑治疗的儿童肺曲菌球。
Br Med J. 1971 Dec 4;4(5787):599-600. doi: 10.1136/bmj.4.5787.599.
Zotero 插件