Cephalothin sodium
(Synonyms: 头孢噻吩钠; Cefalotin sodium) 目录号 : GC38664A cephalosporin antibiotic
Cas No.:58-71-9
Sample solution is provided at 25 µL, 10mM.
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Cefalothin is a β-lactam cephalosporin antibiotic.1,2 It inhibits the growth of various Gram-positive and Gram-negative bacteria, including several strains of S. pyogenes, S. aureus, C. tetani, N. gonorrhoeae, Salmonella, and Shigella (MICs = 0.1-0.2, 0.312-0.625, 0.078, 1.25, 1.56-6.25, and 3.12-12.5 μg/ml, respectively).1 Cefalothin binds to E. coli penicillin-binding proteins (PBPs; IC50s = <0.25, 16, 37, and 1 μg/ml for PBP1a, 1bs, 2, and 3, respectively, in a radioligand binding assay), which interferes with bacterial morphogenesis.2 It exhibits antibacterial activity in mouse models of infection with S. pyogenes, D. pneumoniae, and S. aureus.1 Formulations containing cefalothin were previously used in the prophylaxis and treatment of bacterial infections.
1.Boniece, W.S., Wick, W.E., Holmes, D.H., et al.In vitro and in vivo laboratory evaluation of cephalothin, a new broad spectrum antibioticJ. Bacteriol.841292-1296(1962) 2.Curtis, N.A.C., Orr, D., Ross, G.W., et al.Affinities of penicillins and cephalosporins for the penicillin-binding proteins of Escherichia coli K-12 and their antibacterial activityAntimicrob. Agents Chemother.16(5)533-539(1979)
Cas No. | 58-71-9 | SDF | |
别名 | 头孢噻吩钠; Cefalotin sodium | ||
Canonical SMILES | O=C(C(N12)=C(COC(C)=O)CS[C@]2([H])[C@H](NC(CC3=CC=CS3)=O)C1=O)[O-].[Na+] | ||
分子式 | C16H15N2NaO6S2 | 分子量 | 418.42 |
溶解度 | Water: 50 mg/mL (119.50 mM); DMSO: 50 mg/mL (119.50 mM) | 储存条件 | Store at 2-8°C |
General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。 为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。 |
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Shipping Condition | 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。 |
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1 mg | 5 mg | 10 mg | |
1 mM | 2.3899 mL | 11.9497 mL | 23.8994 mL |
5 mM | 0.478 mL | 2.3899 mL | 4.7799 mL |
10 mM | 0.239 mL | 1.195 mL | 2.3899 mL |
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% DMSO % % Tween 80 % saline | ||||||||||
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1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
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Quantitation of carbenicillin disodium, cefazolin sodium, Cephalothin sodium, nafcillin sodium, and ticarcillin disodium by high-pressure liquid chromatography
J Pharm Sci 1980 Nov;69(11):1264-7.PMID:7452453DOI:10.1002/jps.2600691108.
High-pressure liquid chromatographic (HPLC) methods for the quantitation of carbenicillin, cefazolin, cephalothin, nafcillin, and ticarcillin were developed. The stability of 2% solutions of the antibiotics in normal saline and in 5% dextrose in water were studied at 24 and 5 degrees. The assays were conducted using a previously reported colorimetric method, and some assays also were performed using HPLC. For discolored solutions of cephalothin, the colorimetric method was not stability indicating. The percent relative standard deviations by HPLC based on six injections were 1.69, 0.94, 1.30, 1.59, and 1.6 for carbenicillin, cefazolin, cephalothin, nafcillin, and ticarcillin, respectively. Both carbenicillin and ticarcillin apparently may be mixtures of two isomers at equilibrium with each other. The shelflives recommended by the manufacturers at 5 degrees may be too conservative.
A trial of Cephalothin sodium in colon surgery to prevent wound infection
Arch Surg 1977 Oct;112(10):1169-73.PMID:334110DOI:10.1001/archsurg.1977.01370100023003.
A double-blind trial of preoperative and perioperative Cephalothin sodium in patients undergoing colonic surgery was carried out to test the value of this drug in reducing wound infection rates. Two studies were performed. In the first trial, 1 gm of Cephalothin sodium or a placebo was given intravenously at the beginning of operation, and 1 gm one hour later. In the second trial, the dose of cephalothin or placebo was increased to 2 gm. There was no significant reduction in wound infections in either study in the groups receiving cephalothin, although over two thirds of the organisms cultured from the infected wounds were sensitive to cephalothin. It is suggested that meticulous attention to technique to avoid gross contamination remains the most important factor in the prevention of wound infections after colon surgery.
Transferability of cephalothin to the alveolar cavity in thoroughbreds
J Vet Med Sci 1999 Mar;61(3):209-12.PMID:10331190DOI:10.1292/jvms.61.209.
Five Thoroughbreds were classified into 4 groups according to the administration method used for saline solution (saline), ambroxol, and Cephalothin sodium (cephalothin). In group A, cephalothin was injected intravenously after oral administration of ambroxol. In group B, cephalothin was injected intravenously after oral administration of saline. Groups C and D were used as control groups. The dose of cephalothin or ambroxol was clinically administrated. Venous blood and bronchoalveolar lavage fluid (BALF) were sampled from each group. In groups A and B, cephalothin concentrations in plasma reached their maximum level 5 min after cephalothin administration and then declined over time. In plasma obtained from groups A and B, there were no significant differences in pharmacokinetic parameters (T1/2, Kel, Vd). By contrast, cephalothin concentrations in BALF reached their peak at 180 min after cephalothin administration in both groups A and B and maintained a relatively high level even after 300 min. These findings indicate that cephalothin requires a relatively long period of time to move from the blood stream to the alveolar cavity, but once transferred to the alveolar cavity, it is preserved for a long time. In groups A and B, cephalothin concentrations in BALF were approximately at the same level. However, in group A, total protein in BALF was lower at 60, 180, and 300 min than the other groups. Then, cephalothin concentration was adjusted to total protein in BALF. After adjustment to total protein in BALF, group A showed a concentration level of cephalothin approximately 1.5-fold higher than that of group B. This suggests that the transferability of cephalothin to the alveolar cavity improves as a result of the oral administration of ambroxol.
Nephrotoxicity associated with cephalothin administration
Arch Intern Med 1975 Jun;135(6):797-801.PMID:1130924doi
Variable degrees of acute renal failure developed in three patients receiving therapy with Cephalothin sodium. The course and findings were consistent with acute tubular necrosis of the oliguric and nonoliguric types. One patient had protracted oliguria, a second experienced transient oliguria, and one had normal urine output. All had urinary sediment changes consistent with tubular necrosis, and the two oliguric patients had elevated urine sodium concentrations. No other causes for renal failure could be detected, and all recovered after discontinuation of cephalothin therapy, although peritoneal dialysis was required in one patient. These observations indicate that cephalothin is capable of inducing renal damage in man.
Nephrotoxicity of combined cephalothin-gentamicin regimen
Arch Intern Med 1975 Jun;135(6):850-2.PMID:1130930doi
Two patients developed acute tubular necrosis, characterized clinically by acute oliguric renal failure, while they were receiving a combination of Cephalothin sodium and gentamicin sulfate therapy. Patients who are given this drug regimen should be observed very carefully for early signs of nephrotoxicity. High doses of this antibiotic combination should be avoided especially in elderly patients. Patients with renal insufficiency should not be given this regimen.