青霉素
青霉素用途
青霉素作用
青霉素是细菌繁殖期杀菌剂,主要通过干扰细菌细胞壁的合成而产生抗菌作用。它能抑制细菌细胞壁的基础成分黏肽的合成,造成细胞壁缺损,使水分渗入细菌胞浆,导致菌体肿胀、变形,最后裂解而死亡。由于革兰阳性菌的细胞壁黏肽含量较革兰阴性菌高,所以对前者作用较强。人和动物的细胞没有细胞壁,所以青霉素对其几乎无毒性。
临床上主要用于革兰阳性菌引起的各种感染,如败血症、肺炎、肾炎、乳腺炎、子宫内膜炎、创伤感染、猪丹毒、猪淋巴结肿胀、兔和禽葡萄球菌病、链球菌病、炭疽、恶性水肿、气肿疽、马腺疫等。青霉素也可用于治疗放线菌及钩瑞螺旋体病。青霉素还可局部应用,如乳管内、子宫内及关节腔内注入,以治疗乳房炎、子宫内膜炎及关节炎等。另外,我国有人与链霉素合用,注射产后亲鱼,防治继发性感染。青霉素也用于治疗肠球菌感染性心包炎、梭状芽胞杆菌所致的破伤风和气性坏疽、流行性脑脊髓炎、李氏杆菌病等。在手术或术后,为了预防炎症的发生,青霉素也作为首选药物。
本品不耐酸,也不耐酶,不宜内服给药。在水溶液中稳定性差,降解迅速,禽病防治一般不宜采用自由混饮给药,但可采用“口渴法”混饮给药,用于肠道局部感染,如坏死性肠炎、溃疡性肠炎,球虫病以及病毒性疾病的继发细菌感染。
青霉素属窄谱的杀菌性抗生素,抗菌作用很强。青霉素对多种革兰阳性菌(包括链球菌、肺炎球菌、敏感的葡萄球菌和杆菌)、部分革兰阴性球菌(包括脑膜炎球菌、淋球菌)、螺旋体和放线菌有强大抗菌活性,对革兰阳性杆菌包括白喉杆菌、炭疽杆菌及革兰阳性厌氧杆菌,如破伤风杆菌、产气荚膜杆菌等敏感; 但对革兰阴性杆菌作用很弱,对结核杆菌、立克次体、病毒等无效。
青霉素是细菌繁殖期杀菌剂,主要通过干扰细菌细胞壁的合成而产生抗菌作用。它能抑制细菌细胞壁的基础成分黏肽的合成,造成细胞壁缺损,使水分渗入细菌胞浆,导致菌体肿胀、变形,最后裂解而死亡。由于革兰阳性菌的细胞壁黏肽含量较革兰阴性菌高,所以对前者作用较强。人和动物的细胞没有细胞壁,所以青霉素对其几乎无毒性。
临床上主要用于革兰阳性菌引起的各种感染,如败血症、肺炎、肾炎、乳腺炎、子宫内膜炎、创伤感染、猪丹毒、猪淋巴结肿胀、兔和禽葡萄球菌病、链球菌病、炭疽、恶性水肿、气肿疽、马腺疫等。青霉素也可用于治疗放线菌及钩瑞螺旋体病。青霉素还可局部应用,如乳管内、子宫内及关节腔内注入,以治疗乳房炎、子宫内膜炎及关节炎等。另外,我国有人与链霉素合用,注射产后亲鱼,防治继发性感染。青霉素也用于治疗肠球菌感染性心包炎、梭状芽胞杆菌所致的破伤风和气性坏疽、流行性脑脊髓炎、李氏杆菌病等。在手术或术后,为了预防炎症的发生,青霉素也作为首选药物。
本品不耐酸,也不耐酶,不宜内服给药。在水溶液中稳定性差,降解迅速,禽病防治一般不宜采用自由混饮给药,但可采用“口渴法”混饮给药,用于肠道局部感染,如坏死性肠炎、溃疡性肠炎,球虫病以及病毒性疾病的继发细菌感染。
青霉素名称
[ CAS 号 ]:
61-33-6
[ 中文名 ]:
青霉素
[ 英文名 ]:
Penicillin-G
[中文别名 ]:
[英文别名 ]:
- penicillin, benzyl-
- cilloral
- MFCD00036193
- benzyl penicillin
- cosmopen
- dropcillin
- cilopen
- abbocillin
- Penicillinic acid, benzyl-
- galofak
青霉素生物活性
[ 描述 ]:
[ 相关类别 ]:
[参考文献]
青霉素物理化学性质
[ 密度 ]:
1.4±0.1 g/cm3
[ 沸点 ]:
663.3±55.0 °C at 760 mmHg
[ 分子式 ]:
C16H18N2O4S
[ 分子量 ]:
334.390
[ 闪点 ]:
355.0±31.5 °C
[ 精确质量 ]:
334.098724
[ PSA ]:
112.01000
[ LogP ]:
1.67
[ 外观性状 ]:
powder
[ 蒸汽压 ]:
0.0±2.1 mmHg at 25°C
[ 折射率 ]:
1.655
[ 储存条件 ]:
通风低温干燥
[ 水溶解性 ]:
H2O: 100 mg/mL
青霉素毒性和生态
CHEMICAL IDENTIFICATION
- RTECS NUMBER :
- XH9400000
- CHEMICAL NAME :
- 4-Thia-1-azabicyclo(3.2.0)heptane-2-carboxylic acid, 3,3-dimethyl-7-oxo-6- (2-phenylacetamido)-
- CAS REGISTRY NUMBER :
- 61-33-6
- BEILSTEIN REFERENCE NO. :
- 0044740
- LAST UPDATED :
- 199612
- DATA ITEMS CITED :
- 24
- MOLECULAR FORMULA :
- C16-H18-N2-O4-S
- MOLECULAR WEIGHT :
- 334.42
- WISWESSER LINE NOTATION :
- T45 ANV ESTJ CMV1R& F F GVQ
HEALTH HAZARD DATA
ACUTE TOXICITY DATA
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Parenteral
- SPECIES OBSERVED :
- Human - child
- DOSE/DURATION :
- 15000 units/kg
- TOXIC EFFECTS :
- Sense Organs and Special Senses (Ear) - changes in cochlear structure or function Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - dyspnea
- TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Oral
- SPECIES OBSERVED :
- Rodent - rat
- DOSE/DURATION :
- 8 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 - rat
- DOSE/DURATION :
- 9 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 :
- >5 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 :
- Intraperitoneal
- SPECIES OBSERVED :
- Rodent - mouse
- DOSE/DURATION :
- 3500 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 :
- 329 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 :
- Intracerebral
- SPECIES OBSERVED :
- Rodent - mouse
- DOSE/DURATION :
- 5700 ug/kg
- TOXIC EFFECTS :
- Brain and Coverings - other degenerative changes
- TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Unreported
- SPECIES OBSERVED :
- Rodent - mouse
- DOSE/DURATION :
- 7800 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 :
- Intracerebral
- SPECIES OBSERVED :
- Mammal - dog
- DOSE/DURATION :
- 1118 ug/kg
- TOXIC EFFECTS :
- Brain and Coverings - other degenerative changes
- TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Unreported
- SPECIES OBSERVED :
- Mammal - dog
- DOSE/DURATION :
- 4940 ug/kg
- TOXIC EFFECTS :
- Brain and Coverings - other degenerative changes
- TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Intracerebral
- SPECIES OBSERVED :
- Rodent - rabbit
- DOSE/DURATION :
- 653 ug/kg
- TOXIC EFFECTS :
- Brain and Coverings - other degenerative changes
- TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Unreported
- SPECIES OBSERVED :
- Rodent - guinea pig
- DOSE/DURATION :
- 38 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 :
- Oral
- SPECIES OBSERVED :
- Rodent - hamster
- DOSE/DURATION :
- 24 mg/kg
- TOXIC EFFECTS :
- Behavioral - somnolence (general depressed activity) Behavioral - food intake (animal) Gastrointestinal - hypermotility, diarrhea
- TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Subcutaneous
- SPECIES OBSERVED :
- Rodent - hamster
- DOSE/DURATION :
- 96 mg/kg
- TOXIC EFFECTS :
- Behavioral - somnolence (general depressed activity) Behavioral - food intake (animal) Gastrointestinal - hypermotility, diarrhea
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Intraperitoneal
- SPECIES OBSERVED :
- Rodent - mouse
- DOSE/DURATION :
- 104 ku/kg/4D-I
- TOXIC EFFECTS :
- Blood - changes in other cell count (unspecified) Biochemical - Enzyme inhibition, induction, or change in blood or tissue levels - dehydrogenases
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Intramuscular
- SPECIES OBSERVED :
- Rodent - mouse
- DOSE/DURATION :
- 750 units/kg/5D-I
- TOXIC EFFECTS :
- Blood - changes in serum composition (e.g. TP, bilirubin, cholesterol) Immunological Including Allergic - decrease in humoral immune response Biochemical - Enzyme inhibition, induction, or change in blood or tissue levels - phosphatases
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Subcutaneous
- SPECIES OBSERVED :
- Rodent - rat
- DOSE/DURATION :
- 2600 mg/kg/65W-I
- TOXIC EFFECTS :
- Tumorigenic - equivocal tumorigenic agent by RTECS criteria Tumorigenic - tumors at site of application
MUTATION DATA
- TYPE OF TEST :
- Mutation test systems - not otherwise specified
- TEST SYSTEM :
- Microorganism - not otherwise specified
- DOSE/DURATION :
- 20 ug/L
- REFERENCE :
- AMACCQ Antimicrobial Agents and Chemotherapy. (American Soc. for Microbiology, 1913 I St., NW, Washington, DC 20006) V.1- 1972- Volume(issue)/page/year: 17,572,1980 *** OCCUPATIONAL EXPOSURE LIMITS *** OEL-RUSSIA:STEL 0.1 mg/m3 JAN 1993 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - X3134 No. of Facilities: 151 (estimated) No. of Industries: 1 No. of Occupations: 5 No. of Employees: 2695 (estimated) No. of Female Employees: 1750 (estimated)
青霉素安全信息
[ 危害码 (欧洲) ]:
Xn
[ 风险声明 (欧洲) ]:
R42/43
[ 安全声明 (欧洲) ]:
S36/37
[ WGK德国 ]:
2
[ RTECS号 ]:
XH9700000
[ 海关编码 ]:
32041900
青霉素合成路线
青霉素上下游产品
青霉素上游产品
青霉素下游产品
青霉素海关
[ 海关编码 ]: 32041900
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