头孢拉宗钠(Cefbuperazone Sodium) - 药物靶点：PBPs_在研适应症：细菌感染，支气管扩张，慢性支气管炎_专利_临床

概要

基本信息

药物类型

小分子化药

别名

Cefbuperazone、Cefbuperazone sodium (JP17)

+ [3]

靶点

PBPs

作用机制

PBPs抑制剂(细菌青霉素结合蛋白家族抑制剂)、细胞壁抑制剂

治疗领域

感染心血管疾病消化系统疾病+ [5]

在研适应症

细菌感染支气管扩张慢性支气管炎+ [15]

非在研适应症

肝胆感染泌尿道感染

原研机构-

在研机构

海口市医药总公司

福建省福抗药业股份有限公司

悦康药业集团股份有限公司

+ [1]

非在研机构

桂林医药集团有限公司

海南通用三洋药业有限公司

最高研发阶段批准上市

首次获批日期-

最高研发阶段(中国)临床1期

特殊审评-

结构

分子式C22H29N9O9S2

InChIKeySMSRCGPDNDCXFR-CYWZMYCQSA-N

CAS号76610-84-9

查看全部结构式(2)

关联

6

项与头孢拉宗钠相关的临床试验

CTR20150370 / Not yet recruiting临床1期

注射用头孢拉宗钠临床药代动力学研究

选择中国健康志愿者为受试者，开展本品临床药代动力学研究，以了解该新药在人体内的吸收、分布与消除的规律

开始日期-

申办/合作机构

悦康药业集团股份有限公司

CTR20150131 / Completed临床1期

注射用头孢拉宗钠在中国健康人体的单中心、随机、开放人体药代动力学试验

考察健康志愿者单次或多次静脉滴注由海南通用三洋药业有限公司开发的注射用头孢拉宗钠后血药浓度经时变化过程，估算相应的药代动力学参数，评价头孢拉宗在人体内的药代动力学特征，为II期临床试验方案制定提供试验依据，为临床用药的给药剂量提供依据。

开始日期2015-08-27

申办/合作机构

海南通用三洋药业有限公司

CTR20150130 / Completed临床3期

注射用头孢拉宗钠治疗中、重度呼吸和泌尿系统急性细菌感染的随机、单盲、阳性药平行对照、多中心临床试验

以注射用头孢美唑钠为对照，评价注射用头孢拉宗钠治疗中、重度呼吸和泌尿系统急性细菌感染的有效性和安全性。

开始日期2015-02-04

申办/合作机构

海南通用三洋药业有限公司

100 项与头孢拉宗钠相关的临床结果

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100 项与头孢拉宗钠相关的转化医学

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100 项与头孢拉宗钠相关的专利（医药）

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96

项与头孢拉宗钠相关的文献（医药）

2016-09-01·Journal of Pharmaceutical and Biomedical Analysis3区 · 医学

Pharmacokinetic profile of cefbuperazone in healthy Chinese volunteers after single and multiple drip intravenous infusion by HPLC–MS/MS

3区 · 医学

Article

作者: Ding, Li ; Geng, Taohua ; Wang, Yiya ; Liu, Dongbo

A selective and reproducible HPLC-MS/MS method was developed and fully validated for the determination of cefbuperazone in human plasma and urine. Samples were prepared using protein precipitation and separated on a Zorbax Eclipse Plus C18 column (2.1×50mm, 3.5μm). The API-4000 mass spectrometer was operated under multiple reaction monitoring mode (MRM) using the electrospray ionization technique. Linearity was achieved from 0.250 to 250μg/mL in plasma and 20.0-5000μg/mL in urine. The method was successfully applied to a pharmacokinetic study of cefbuperazone in healthy Chinese volunteers after drip intravenous infusion of 0.5, 1.0, 2.0g cefbuperazone sodium injection. Cefbuperazone reached a maximum concentration (Cmax) of 44.7±8.1μg/mL, 86.7±12.7μg/mL and 168±14μg/mL in 0.5, 1.0 and 2.0g dose groups respectively, at 60min after the start of infusion. The half-life (t1/2) was between 1.8-1.9h, and the elimination constant (kel) was between 0.36-0.39h(-1). The results proved that cefbuperazone showed linear pharmacokinetic profile in the dose range of 0.5-2.0g without gender difference. Drug accumulation was not observed. Cefbuperazone reached the maximum excretion rate in urine 2h after the start of infusion. About 60.0% of the administered drug was excreted via urine as unchanged form within 12h. The cumulative excretion of cefbuperazone after single drip intravenous infusion was proportional to the administered dose within the range from 0.5g to 2.0g.

2015-03-31·Journal of Lifestyle Medicine

Suspected Anaphylactic Reaction Prior to Induction of Anesthesia

作者: Do, Hye Jin ; Jeon, Yeong Gwan ; Park, Ji Hyoung ; Lim, Hyun Kyo ; Lee, Kwang Ho

Although uncommon, anaphylactic reactions during surgery are very dangerous and can result in serious morbidity. Various anesthetics can trigger anaphylactic reactions, and incidents with cephalosporin antibiotics are on the rise. In the case presented, an 84-year-old woman scheduled for calcaneus fracture surgery, was injected with cefbuperazone as a prophylactic antibiotic. On the way to the operating room, before induction of anesthesia, the patient lost consciousness and showed signs of hypoxemia, and anaphylactic reaction, which included hypotension, bronchospasm, and rash. Five hours after immediate intubation and fluid resuscitation, the patient was extubated and transferred to the general ward. Eight weeks later, the skin prick test confirmed a positive reaction to cefbuperazone.

2011-04-12·Journal of Pharmacy and Pharmacology3区 · 医学

Effects of various cephem antibiotics on ethanol metabolism and their structure-activity relations

3区 · 医学

Article

作者: Kamei, Chiaki ; Sugimoto, Yukio ; Muroi, Nobuaki ; Tasaka, Kenji

AbstractThe effects of various cephem antibiotics and related compounds on ethanol metabolism were studied in association with their chemical structures. In rats, cefoperazone, cefbuperazone, cefamandole, latamoxef, cefmetazole, cefotetan, cefmenoxime and cefminox which have the [(1-methyl-1H-tetrazol-5-yl) thio] methyl group at position 3 of the cephem ring caused a significant increase in the blood acetaldehyde concentration. In the last three compounds, disulfiram-like activity was less potent than that evaluated in the preceding compounds. Cefazolin and ceftezole having a 1H-tetrazol group at position 7 also showed a disulfiram-like activity. A single administration of 1H-tetrazol also increased the blood acetaldehyde concentration. Both blood ethanol and acetaldehyde values were increased significantly on administration of these drugs. In beagle dogs, cefoperazone induced a less remarkable but much more sustained increase in the blood acetaldehyde. These results indicate that the 1H-tetrazol group, as well as the [(1-methyl-1H-tetrazol-5-yl) thio] methyl group, is responsible for inducing a disulfiram-like action and that there is a difference in the potency of the disulfiram-like activity among the drugs having a [(1-methyl-1H-tetrazol-5-yl)thio] methyl group at position 3 of the cephem ring in relation to those in which the side chain is substituted at position 7.

100 项与头孢拉宗钠相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
D01736	头孢拉宗钠	J01DC13	DB13638

研发状态

批准上市

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适应症	国家/地区	公司	日期
细菌感染	-	-	-

未上市

10 条进展最快的记录,

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适应症	最高研发状态	国家/地区	公司	日期
肺脓肿	临床3期	中国	桂林医药集团有限公司	2014-04-02
腹膜炎	临床3期	中国	桂林医药集团有限公司	2014-04-02
肺炎	临床1期	中国	桂林医药集团有限公司	2014-04-02
肾盂肾炎	临床1期	中国	桂林医药集团有限公司	2014-04-02
胆管炎	临床前	中国	桂林医药集团有限公司	2014-04-02
心内膜炎	临床前	中国	桂林医药集团有限公司	2014-04-02
呼吸道感染	药物发现	中国	海南通用三洋药业有限公司	2015-02-04
泌尿道感染	药物发现	中国	海南通用三洋药业有限公司	2015-02-04
脓胸	药物发现	中国	桂林医药集团有限公司	2014-04-02
盆腔炎	药物发现	中国	桂林医药集团有限公司	2014-04-02