苯唑西林
苯唑西林用途
苯唑西林是一种口服活性合成青霉素,对葡萄球菌和其他革兰氏阳性病原体具有良好的杀菌活性[1]。
苯唑西林名称
[ CAS 号 ]:
66-79-5
[ 中文名 ]:
苯唑西林
[ 英文名 ]:
OXACILLIN
[中文别名 ]:
[英文别名 ]:
- OXACILLIN
- Oxazina
- Penstapho
- (5-methyl-3-phenyl-isoxazol-4-yl)-penicillin
- Bactocil
- oxazocillin
苯唑西林生物活性
[ 描述 ]:
苯唑西林是一种口服活性合成青霉素,对葡萄球菌和其他革兰氏阳性病原体具有良好的杀菌活性[1]。
[ 相关类别 ]:
[体外研究]
苯唑西林抑制革兰氏阳性病原体,对A组链球菌、肺炎链球菌、敏感葡萄球菌和青霉素耐药葡萄球菌的MIC分别为0.05、0.09、0.32和0.80μg/mL[1]。耐苯唑西林菌株对其他青霉素具有高度抗性[1]。
[体内研究]
苯唑西林(50-800 mg/kg；皮下注射；一次)在感染金黄色葡萄球菌埃文斯的小鼠中显示出253.3 mg/kg的治疗剂量(CD50)。苯唑西林的口服CD50为187.2 mg/kg[2]。动物模型：感染金黄色葡萄球菌埃文斯的CD-1株雄性白化小鼠[2]剂量：50、100、200、400和800 mg/kg给药：皮下注射,一次结果：显示CD50为253.3 mg/kg的治疗活性。
苯唑西林物理化学性质
[ 熔点 ]:
188ºC
[ 分子式 ]:
C19H19N3O5S
[ 分子量 ]:
401.43600
[ 精确质量 ]:
401.10500
[ PSA ]:
138.04000
[ LogP ]:
2.22410
[ 外观性状 ]:
白色至灰白色自由流动结晶粉末
苯唑西林毒性和生态
CHEMICAL IDENTIFICATION
- RTECS NUMBER :
- XH9000000
- CHEMICAL NAME :
- 4-Thia-1-azabicyclo(3.2.0)heptane-2-carboxylic acid, 3,3-dimethyl-6-(5-methyl-3-phenyl-4- isoxazolecarboxamide)-7-oxo-
- CAS REGISTRY NUMBER :
- 66-79-5
- LAST UPDATED :
- 199606
- DATA ITEMS CITED :
- 12
- MOLECULAR FORMULA :
- C19-H19-N3-O5-S
- MOLECULAR WEIGHT :
- 401.47
- WISWESSER LINE NOTATION :
- T45 ANV ESTJ F1 F1 GVQ CMV- DT5NOJ C1 FR
HEALTH HAZARD DATA
ACUTE TOXICITY DATA
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Oral
- SPECIES OBSERVED :
- Human - woman
- DOSE/DURATION :
- 200 mg/kg/10D-I
- TOXIC EFFECTS :
- Gastrointestinal - other changes
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Intravenous
- SPECIES OBSERVED :
- Human - man
- DOSE/DURATION :
- 3800 mg/kg/19D-I
- TOXIC EFFECTS :
- Blood - agranulocytosis
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Intravenous
- SPECIES OBSERVED :
- Human - child
- DOSE/DURATION :
- 2550 mg/kg/17D-I
- TOXIC EFFECTS :
- Blood - agranulocytosis
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Intravenous
- SPECIES OBSERVED :
- Human - infant
- DOSE/DURATION :
- 3800 mg/kg/19D-I
- TOXIC EFFECTS :
- Blood - agranulocytosis
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Intravenous
- SPECIES OBSERVED :
- Human - woman
- DOSE/DURATION :
- 5560 mg/kg/20D-I
- TOXIC EFFECTS :
- Blood - agranulocytosis
- TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Unreported
- SPECIES OBSERVED :
- Rodent - rat
- DOSE/DURATION :
- 10 gm/kg
- TOXIC EFFECTS :
- Details of toxic effects not reported other than lethal dose value
- TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Oral
- SPECIES OBSERVED :
- Rodent - mouse
- DOSE/DURATION :
- 6500 mg/kg
- TOXIC EFFECTS :
- Details of toxic effects not reported other than lethal dose value
- TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Intravenous
- SPECIES OBSERVED :
- Rodent - mouse
- DOSE/DURATION :
- 1490 mg/kg
- TOXIC EFFECTS :
- Details of toxic effects not reported other than lethal dose value
- TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Unreported
- SPECIES OBSERVED :
- Rodent - mouse
- DOSE/DURATION :
- 28 gm/kg
- TOXIC EFFECTS :
- Details of toxic effects not reported other than lethal dose value
- TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Unreported
- SPECIES OBSERVED :
- Rodent - guinea pig
- DOSE/DURATION :
- 120 mg/kg
- TOXIC EFFECTS :
- Details of toxic effects not reported other than lethal dose value
MUTATION DATA
- TYPE OF TEST :
- Mutation test systems - not otherwise specified
- TEST SYSTEM :
- Microorganism - not otherwise specified
- DOSE/DURATION :
- 4 mg/L
- REFERENCE :
- JOBAAY Journal of Bacteriology. (American Soc. for Microbiology, 1913 I St., NW, Washington, DC 20006) V.1- 1916- Volume(issue)/page/year: 170,1831,1988 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - X3709 No. of Facilities: 231 (estimated) No. of Industries: 1 No. of Occupations: 5 No. of Employees: 11502 (estimated) No. of Female Employees: 9533 (estimated)
苯唑西林合成路线
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