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替卡西林二钠

替卡西林二钠用途

Ticarcillin二钠盐主要用于抗革兰氏阴性菌, 尤其是绿脓杆菌, 也是少数能够治疗嗜麦芽感染的抗生素。

替卡西林二钠名称

[ CAS 号 ]:
4697-14-7

[ 中文名 ]:
替卡西林二钠

[ 英文名 ]:
Ticarcillin disodium salt

[中文别名 ]:

[英文别名 ]:

Ticillin Disodium Salt
Neoanabactyl
CSL Ticillin,Tarcil
Timentin sodium
Ticalpenin
TIMENTIN
ticarpen
MFCD07787410
Ticarcillin disodium
Disodium Ticarcillin

替卡西林二钠生物活性

[ 描述 ]:

Ticarcillin二钠盐主要用于抗革兰氏阴性菌, 尤其是绿脓杆菌, 也是少数能够治疗嗜麦芽感染的抗生素。

[ 相关类别 ]:

信号通路 >> 抗感染 >> 细菌

研究领域 >> 感染

[相关活性小分子]

替卡西林二钠物理化学性质

[ 沸点 ]:
768.3ºC at 760 mmHg

[ 分子式 ]:
C₁₅H₁₄N₂Na₂O₆S₂

[ 分子量 ]:
428.391

[ 闪点 ]:
418.4ºC

[ 精确质量 ]:
428.008881

[ PSA ]:
183.21000

[ 外观性状 ]:
结晶粉末

[ 储存条件 ]:
2-8°C

替卡西林二钠毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: XM9410000

CHEMICAL NAME :: 3-Thiophenemalonamic acid, N-(2-carboxy-3,3-dimethyl-7-oxo-4-thia-1-azabicylo(3. 2.0) hept-6-yl)-, disodium salt

CAS REGISTRY NUMBER :: 4697-14-7

LAST UPDATED :: 199707

DATA ITEMS CITED :: 18

MOLECULAR FORMULA :: C15-H14-N2-O6-S2.2Na

MOLECULAR WEIGHT :: 428.41

WISWESSER LINE NOTATION :: T45 ANV ESTJ GVO CMVYVO&- CT5SJ &-NA- 2

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 16 gm/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Gastrointestinal - hypermotility, diarrhea

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 12,556,1978

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 7200 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Gastrointestinal - ulceration or bleeding from stomach Gastrointestinal - ulceration or bleeding from small intestine

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 12,556,1978

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 10 gm/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Gastrointestinal - ulceration or bleeding from small intestine

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 12,556,1978

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 5350 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Kidney, Ureter, Bladder - other changes

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 12,556,1978

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: >16 gm/kg

TOXIC EFFECTS :: Gastrointestinal - ulceration or bleeding from small intestine

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 12,556,1978

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 7800 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Gastrointestinal - ulceration or bleeding from small intestine Kidney, Ureter, Bladder - other changes

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 12,556,1978

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 10700 mg/kg

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

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 12,556,1978

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 5200 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity)

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 12,556,1978

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 7 gm/kg

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

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 12,556,1978

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: >4 gm/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Gastrointestinal - nausea or vomiting

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 12,556,1978

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rabbit

DOSE/DURATION :: >11 gm/kg

TOXIC EFFECTS :: Gastrointestinal - ulceration or bleeding from stomach

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 12,556,1978

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rabbit

DOSE/DURATION :: >8 gm/kg

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

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 12,556,1978 ** OTHER MULTIPLE DOSE TOXICITY DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 60 gm/kg/30D-C

TOXIC EFFECTS :: Liver - changes in liver weight Endocrine - changes in thymus weight Blood - changes in leukocyte (WBC) count

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 12,556,1978

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 26 gm/kg/30D-I

TOXIC EFFECTS :: Endocrine - changes in spleen weight Endocrine - changes in thymus weight Blood - normocytic anemia

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 12,556,1978

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 91 gm/kg/26W-C

TOXIC EFFECTS :: Endocrine - changes in adrenal weight Endocrine - changes in thymus weight Blood - changes in serum composition (e.g. TP, bilirubin, cholesterol)

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 12,556,1978 ** REPRODUCTIVE DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

DOSE :: 5500 mg/kg

SEX/DURATION :: female 7-17 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus) Reproductive - Specific Developmental Abnormalities - musculoskeletal system

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 12,556,1978

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

DOSE :: 5500 mg/kg

SEX/DURATION :: female 7-17 day(s) after conception

TOXIC EFFECTS :: Reproductive - Specific Developmental Abnormalities - musculoskeletal system

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 12,556,1978 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - X2885 No. of Facilities: 535 (estimated) No. of Industries: 2 No. of Occupations: 9 No. of Employees: 14268 (estimated) No. of Female Employees: 10723 (estimated)

替卡西林二钠安全信息

[ 符号 ]:

GHS07, GHS08

[ 信号词 ]:
Danger

[ 危害声明 ]:
H315-H319-H334-H335

[ 警示性声明 ]:
P261-P305 + P351 + P338-P342 + P311

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

[ 危害码 (欧洲) ]:
Xi:Irritant;

[ 风险声明 (欧洲) ]:
R36/37/38;R42;R43

[ 安全声明 (欧洲) ]:
S26-S36/37

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

[ WGK德国 ]:
2

[ RTECS号 ]:
XM9410000

替卡西林二钠制备

方法1:1.38g(5mmol)(噻吩-3-基)丙二酸单苄酯(Ⅰ)和2.5ml二氯亚砜，在50~55℃下加热1h，再在60~65℃下加热10min。在减压和低于30℃下，除去过剩的二氯亚砜，最后可以加入1ml苯，在高真空下利用共沸去除痕量的二氯亚砜，剩下的是黄色油状的(噻吩-3-基)丙二酸单苄酯酰氯(Ⅱ)。把该酰氯9Ⅱ)溶于10ml干燥丙酮，在搅拌和蒸汽浴上，加入1.08g(55mmol)6-APA、15ml1mol/L碳酸氢钠和5ml丙酮的混合溶液。当反应开始进行后，将反应液在室温下继续搅拌45min。反应液用乙醚(3×25ml)洗后，再用约11ml1mol/L盐酸酸化至PH＝2，然后用乙醚(3×15ml)萃取该酸性水溶液。萃取液用活性炭和硫酸镁一起脱色5min。过滤，摇晃淡黄色的滤液和约4ml1mol/L碳酸氢钠，得到PH值为7~7.5的水
溶性萃取液。该水溶性萃取液在低温低压浓缩后，剩余物加入异丙醇一起搅拌，直到混合物中含10％水为止。此时开始结晶，在0℃下放置过夜使结晶完全。得白色结晶的α-(苄氧羰基)-3-噻吩甲基青霉素钠(Ⅲ)，收率50％。

10.65g5％载于碳酸钙的钯催化剂悬浮于32ml水中，预先氢化1h，然后加入2.13g(4.3mmol)上面得到的钠盐(Ⅲ)溶于30ml水的溶液，在略高于大气压的压力下氢化1.5h。用装有Dicalite(一种硅藻土)的装置进行过滤。澄清的滤液在低温低压下浓缩，剩余物在五氧化二磷存在下真空燥，得白色固体的替卡西林钠。

方法2:2-噻吩-2-苄氧羰基乙酰氯(Ⅱ)对6-APA的苄酯进行酰化，得到化合物(Ⅳ)，再氢解脱去两个苄基保护基，然后用碳酸氢钠中和即可得到替卡西林钠。

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