阿扑西林

阿扑西林用途

【用途1】
广谱半合成青霉素，对葡萄球菌属、链球菌属、肺炎球菌等革兰阳性菌有很强的抗菌作用，对大肠杆菌、流感杆菌及厌氧菌拟杆菌属等革兰阴性菌也有较好的抗菌作用。临床用于上述敏感菌引起的感染，包括败血症、细菌感染性心内膜炎、急慢性支气管炎、支气管扩张感染、外伤及手术创面等表面性感染、扁桃体炎、肺炎等。

阿扑西林名称

[ CAS 号 ]:
63358-49-6

[ 中文名 ]:
阿扑西林

[ 英文名 ]:
Aspoxicillin

[中文别名 ]:

阿朴西林

[英文别名 ]:

ASPOXICILLIN 3-HYDRATE
n(sup4)-methyl-d-asparagininylamoxicillin
Aspoxicillin
N4-Methyl-D-asparaginylamoxicillin
Doyle
Aspoxicilin
TA 058
ASPC

阿扑西林生物活性

[ 描述 ]:

Aspoxicillin 是一种广谱的抗菌剂,对分离的胸膜肺炎放线杆菌 68 菌株抑制作用的 MIC90 值 <= 0.05 μg/ml。Aspoxicillin 在小鼠血清中的半衰期为 55 分钟。

[ 相关类别 ]:

研究领域 >> 感染

信号通路 >> 抗感染 >> 细菌

[ 靶点 ]

microbe[1]

[体外研究]

阿司匹林是一种半合成的青霉素衍生物[2]阿司匹林在体外对金黄色葡萄球菌产生1.7h的抗生素后效应[2]。

[体内研究]

在中性粒细胞减少小鼠大腿感染模型中,阿昔西林对金黄色葡萄球菌Smith 5.2小时的体内诱导PAEs[2]。

[参考文献]

[1]. Yoshimura H, et al. Comparative in vitro activity of 16 antimicrobial agents against Actinobacillus pleuropneumoniae. Vet Res Commun. 2002 Jan;26(1):11-9.

[2]. Oshida T, et al. Activity of sub-minimal inhibitory concentrations of aspoxicillin in prolonging the postantibiotic effect against Staphylococcus aureus. J Antimicrob Chemother. 1990 Jul;26(1):29-38.

阿扑西林物理化学性质

[ 密度 ]:
1.5±0.1 g/cm3

[ 沸点 ]:
985.1±65.0 °C at 760 mmHg

[ 熔点 ]:
195-198° (dec)

[ 分子式 ]:
C₂₁H₂₇N₅O₇S

[ 分子量 ]:
493.533

[ 闪点 ]:
549.5±34.3 °C

[ 精确质量 ]:
493.163116

[ PSA ]:
215.87000

[ LogP ]:
-0.53

[ 蒸汽压 ]:
0.0±0.3 mmHg at 25°C

[ 折射率 ]:
1.672

[ 储存条件 ]:
2-8°C

阿扑西林毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: MB7548000

CHEMICAL NAME :: Glycinamide, N-methyl-D-asparaginyl-N-(2-carboxy-3,3-dimethyl-7-ox o-4-thia-1- azabicyclo(3.2.0)hept-6-yl)-D-2-(4-hydroxyphenyl)-, (2S-(2-alpha,5-alpha,6-beta))-

CAS REGISTRY NUMBER :: 63358-49-6

LAST UPDATED :: 199109

DATA ITEMS CITED :: 4

MOLECULAR FORMULA :: C21-H27-N5-O7-S

MOLECULAR WEIGHT :: 493.59

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: >8 gm/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: -,20,1990

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: >8 gm/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: -,20,1990

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 8 gm/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: -,20,1990

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 8 gm/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: -,20,1990

阿扑西林安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H315-H319-H335

[ 警示性声明 ]:
P261-P305 + P351 + P338

[ 个人防护装备 ]:
dust mask type N95 (US);Eyeshields;Gloves

[ 危害码 (欧洲) ]:
Xi:Irritant

[ 风险声明 (欧洲) ]:
R36/37/38

[ 安全声明 (欧洲) ]:
S26

[ 危险品运输编码 ]:
NONH for all modes of transport

[ RTECS号 ]:
MB7548000

阿扑西林制备

【方法1】
2-氨基-3-甲胺羰基丙酸和间硝基苯磺酰氯进行酰化反应，对侧链的游离氨基进行保护，和N-羟基丁二酰亚胺反应形成活性酯，利用该活性酯的高反应活性，在三乙胺存在下，对羟氨苄青霉素进行酰化，再在硫代乙酰胺作用下，脱去氨基上的保护基，即得到阿扑西林。

阿扑西林文献

[In vitro study on efficacy of combination use of aspoxicillin and beta-lactam preparations (ceftazidime, cefmetazole and aztreonam) against bacteria isolated from abdominal infections].

Jpn. J. Antibiot. 45(7) , 763-73, (1992)

An in vitro study was done to evaluate combination use of aspoxicillin (ASPC) with each of 3 beta-lactam preparations, ceftazidime (CAZ), cefmetazole (CMZ) and aztreonam (AZT). The results obtained ar...

[A clinical study of combined therapy of aspoxicillin and ceftazidime on intractable respiratory infections].

Jpn. J. Antibiot. 45(10) , 1282-94, (1992)

Both aspoxicillin (ASPC) and ceftazidime (CAZ) were administered together to 55 patients with intractable respiratory tract infections. ASPC and CAZ were administered at daily doses of 4 g and 2 to 4 ...

Separation and determination of aspoxicillin in human plasma by micellar electrokinetic chromatography with direct sample injection.

J. Chromatogr. A. 515 , 245-55, (1990)

Both the separation and determination of aspoxicillin in human plasma by micellar electrokinetic chromatography (MEKC) were investigated. Selectivity in the separation of seven penicillin antibiotics ...

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