Delving into the Latest Updates on Cefbuperazone Sodium with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Cefbuperazone, Cefbuperazone sodium (JP17)

+ [3]

Target

PBPs

Mechanism

PBPs inhibitors(Bacterial penicillin-binding protein inhibitors), Cell wall inhibitors

Therapeutic Areas

Infectious DiseasesCardiovascular DiseasesDigestive System Disorders+ [5]

Active Indication

Bacterial InfectionsBronchiectasisBronchitis, Chronic+ [15]

Inactive Indication

Hepatobiliary infectionUrinary Tract Infections

Originator Organization-

Active Organization

Fujian Fukang Pharmaceutical Co. Ltd.

Yuekang Pharmaceutical Group Co., Ltd.Haikou Pharmaceutical Co. Ltd.

+ [1]

Inactive Organization

Guilin Pharmaceutical Group Co., Ltd.

Hainan General Sanyang Pharmaceutical Co. Ltd.

Drug Highest PhaseApproved

First Approval Date-

Regulation-

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Structure

Molecular FormulaC22H29N9O9S2

InChIKeySMSRCGPDNDCXFR-CYWZMYCQSA-N

CAS Registry76610-84-9

View All Structures (2)

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。

[Translation]

To investigate the time-dependent changes in blood concentration of cefoperazone sodium for injection developed by Hainan General Sanyo Pharmaceutical Co., Ltd. in healthy volunteers after single or multiple intravenous infusions, estimate the corresponding pharmacokinetic parameters, evaluate the pharmacokinetic characteristics of cefoperazone in humans, provide experimental basis for the formulation of Phase II clinical trial plans, and provide basis for clinical drug dosage.

Start Date27 Aug 2015

Sponsor / Collaborator

Hainan General Sanyang Pharmaceutical Co. Ltd.

CTR20150130 / CompletedPhase 3

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

[Translation] A randomized, single-blind, positive-drug parallel-controlled, multicenter clinical trial of cefuroxime sodium for injection in the treatment of moderate to severe acute bacterial infections of the respiratory and urinary systems

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。

[Translation]

To evaluate the efficacy and safety of cefoperazone sodium for injection in the treatment of moderate to severe acute bacterial infections of the respiratory and urinary systems, using ceftriaxone sodium for injection as a control.

Start Date04 Feb 2015

Sponsor / Collaborator

Hainan General Sanyang Pharmaceutical Co. Ltd.

100 Clinical Results associated with Cefbuperazone Sodium

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100 Translational Medicine associated with Cefbuperazone Sodium

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100 Patents (Medical) associated with Cefbuperazone Sodium

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96

Literatures (Medical) associated with Cefbuperazone Sodium

01 Sep 2016·Journal of Pharmaceutical and Biomedical AnalysisQ3 · MEDICINE

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

Q3 · MEDICINE

Article

Author: 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.

31 Mar 2015·Journal of Lifestyle Medicine

Suspected Anaphylactic Reaction Prior to Induction of Anesthesia

Author: 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.

12 Apr 2011·Journal of Pharmacy and PharmacologyQ3 · MEDICINE

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

Q3 · MEDICINE

Article

Author: 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 Deals associated with Cefbuperazone Sodium

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External Link

KEGG	Wiki	ATC	Drug Bank
D01736	Cefbuperazone Sodium	J01DC13	DB13638

R&D Status

Approved

10 top approved records.

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Indication	Country/Location	Organization	Date
Bacterial Infections	-	-	-

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Respiratory Tract Infections	Phase 1	CN	Hainan General Sanyang Pharmaceutical Co. Ltd.	04 Feb 2015
Urinary Tract Infections	Phase 1	CN	Hainan General Sanyang Pharmaceutical Co. Ltd.	04 Feb 2015
Cholangitis	Phase 1	CN	Guilin Pharmaceutical Group Co., Ltd.	02 Apr 2014
Cholecystitis	Phase 1	CN	Guilin Pharmaceutical Group Co., Ltd.	02 Apr 2014
Cystitis	Phase 1	CN	Guilin Pharmaceutical Group Co., Ltd.	02 Apr 2014
Empyema	Phase 1	CN	Guilin Pharmaceutical Group Co., Ltd.	02 Apr 2014
Endocarditis	Phase 1	CN	Guilin Pharmaceutical Group Co., Ltd.	02 Apr 2014
Pelvic Inflammatory Disease	Phase 1	CN	Guilin Pharmaceutical Group Co., Ltd.	02 Apr 2014
Peritonitis	Phase 1	CN	Guilin Pharmaceutical Group Co., Ltd.	02 Apr 2014
Pyelonephritis	Phase 1	CN	Guilin Pharmaceutical Group Co., Ltd.	02 Apr 2014