β-lactam

Absorption, Distribution and Excretion
CEPHALOTHIN ENTERS AQUEOUS HUMOR AFTER SUBCONJUNCTIVAL INJECTIONS YIELDING PEAK LEVELS CA 1-2 HR AFTER DOSING. RATIO OF AQ HUMOR:SERUM ANTIBIOTIC LEVELS RANGES FROM 4.0 TO 67.0 DURING 5 HR AFTER DOSING, & LOSS OF ANTIBIOTIC FROM AQ HUMOR OCCURS BY BIPHASIC PROCESS.
...CEPHALOTHIN...WERE SHOWN...TO PENETRATE INTO BONE TO VERY LIMITED EXTENT AFTER SC OR ORAL DOSES TO RATS. RATIOS OF BONE TO SERUM CONCN AVG 1:4 FOR CEPHALOTHIN... DESPITE DIFFERENCES IN CONCN, T/2 IN BONE & SERUM WERE SIMILAR.
DRUGS RECENTLY SHOWN TO ACTIVELY CROSS HUMAN PLACENTA INCL...CEPHALOTHIN...
Concn of cephalothin present in urine after admin of 1 g range from 0.7 to 5 mg/mL. Excretion is delayed in presence of decr renal function ...
For more Absorption, Distribution and Excretion (Complete) data for CEPHALOTHIN (11 total), please visit the HSDB record page.

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Metabolism / Metabolites
Metabolized to a less active desacetyl metabolite, although 50-75% of the drug is eliminated unchanged in the urine.
Approx 25% of cephalothin dose admin was eliminated in urine as deacetylcephalothin.
Cephalothin ... /is/ deacetylated in vivo, and these metabolites have less antimicrobial activity than the parent cmpd ... The deacetylated metabolites also are excreted by the kidneys.

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Biological Half-Life
30 minutes
Half-life = 0.6 hr /by/ injection /From table/

Protein Binding
65-80%

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Interactions
Concurrent administration with probenecid may prolong the serum half-life of cephalothin.
ANIMAL STUDIES INDICATED THAT FUROSEMIDE ENHANCES NEPHROTOXICITY OF...CEPHALOTHIN...
...CEPHALOSPORINS...MAY BE AFFECTED BY CONCURRENT USE OF SULFINPYRAZONE. DIMINISHED TUBULAR SECRETION OF...WEAK ACIDS COULD RESULT IN HIGHER & MORE SUSTAINED SERUM LEVELS & HENCE, INTENSIFICATION OF DRUG ACTIVITY. /CEPHALOSPORINS/
NON-IONIC, ANIONIC, & ZWITTERIONIC SURFACTANTS INDUCED RAPIDLY REVERSIBLE HYPER-ABSORPTIVE STATE IN THOMAS CANINE FUNDIC POUCH FOR...CEPHALOTHIN...
For more Interactions (Complete) data for CEPHALOTHIN (10 total), please visit the HSDB record page.

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Non-Human Toxicity Values
LD50 Rat oral >10,000 mg/kg /sodium salt/
LD50 Rat ip 7716 mg/kg /sodium salt/
LD50 Mouse oral >20,000 mg/kg /sodium salt/
LD50 Mouse ip 5670 mg/kg /sodium salt/

[1]. Structure-based optimization of cephalothin-analogue boronic acids as beta-lactamase inhibitors. Bioorg Med Chem. 2008 Feb 1;16(3):1195-205. Epub 2007 Nov 7.

Cefalotin is a semisynthetic, first-generation cephalosporin antibiotic with acetoxymethyl and (2-thienylacetyl)nitrilo moieties at positions 3 and 7, respectively, of the core structure. Administered parenterally during surgery and to treat a wide spectrum of blood infections. It has a role as an antimicrobial agent and an antibacterial drug. It is a semisynthetic derivative, a beta-lactam antibiotic allergen, a cephalosporin, a carboxylic acid, a member of thiophenes and an azabicycloalkene. It is a conjugate acid of a cefalotin(1-).
Cefalotin is a cephalosporin antibiotic.
Cephalothin has been reported in Bos taurus with data available.
Cephalothin is a semisynthetic, beta-lactam, first-generation cephalosporin antibiotic with bactericidal activity. Cephalothin binds to and inactivates penicillin-binding proteins (PBP) located on the inner membrane of the bacterial cell wall. PBPs participate in the terminal stages of assembling the bacterial cell wall, and in reshaping the cell wall during cell division. Inactivation of PBPs interferes with the cross-linkage of peptidoglycan chains necessary for bacterial cell wall strength and rigidity. This results in the weakening of the bacterial cell wall and causes cell lysis.
A cephalosporin antibiotic.

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Drug Indication
Used to prevent infection during surgery and to treat many kinds of infections of the blood, bone or joints, respiratory tract, skin, and urinary tract.

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Mechanism of Action
The bactericidal activity of cefalotin results from the inhibition of cell wall synthesis via affinity for penicillin-binding proteins (PBPs). The PBPs are transpeptidases which are vital in peptidoglycan biosynthesis. Therefore, their inhibition prevents this vital cell wall compenent from being properly synthesized.
Bactericidal; action depends on ability to reach and bind penicillin-binding proteins located in bacterial cytoplasmic membranes. Cephalosporins inhibit bacterial septum and cell wall synthesis, probably by action of membrane-bound transpeptidase enzymes. This prevents cross-linkage of peptidoglycan chains, which is necessary for bacterial cell wall strength and rigidity. Also, cell division and growth are inhibited, and elongation of susceptible bacteria and lysis frequently occur. Rapidly dividing bacteria are those most susceptible to the actin of cephalosporins. /Cephalosporins/

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Therapeutic Uses
Since, among the cephalosporins, cephalothin is the most impervious to attack by Staphylococcal beta-lactamase, it is very effective in severe Staphylococcal infections, such as endocarditis.
Mesh Heading: anti-bacterial agents
Use should be restricted to treatment of serious infections caused by susceptible organisms, most commonly when patient is hypersensitive to penicillins. /Sodium/
... Cephalosporin is ... drug of first choice ... for Klebsiella infections ... They are useful as alternative choices to penicillin. /Cephalosporins/
For more Therapeutic Uses (Complete) data for CEPHALOTHIN (28 total), please visit the HSDB record page.

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Drug Warnings
Excretion is delayed in presence of decr renal function, and intervals between doses must be lengthened when renal failure is severe.
Cephalothin should not be used to treat bacterial meningitis.
Infections due to Enterococci are usually unaffected by these cmpd ... Enterococcal endocarditis cannot be cured with cephalosporin even when it is given concurrently with gentamicin or streptomycin. /Cephalosporins/
Patients with a history of a mild or a temporally distant reaction to penicillin appear to be at low risk of rash or other allergic reaction following the admin of a cephalosporin ... Patients who have had a recent severe, immediate reaction to a penicillin should be given a cephalosporin with great caution, if at all. /Cephalosporin/
For more Drug Warnings (Complete) data for CEPHALOTHIN (21 total), please visit the HSDB record page.

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Pharmacodynamics
Cefalotin (INN) or cephalothin (USAN) is a semisynthetic first generation cephalosporin having a broad spectrum of antibiotic activity that is administered parenterally.

C16H16N2O6S2

396.44

396.044

C, 48.47; H, 4.07; N, 7.07; O, 24.21; S, 16.18

153-61-7

Cephalothin sodium;58-71-9

6024

White to off-white solid powder

1.6±0.1 g/cm3

757.2±60.0 °C at 760 mmHg

160-161ºC

411.8±32.9 °C

0.0±2.7 mmHg at 25°C

1.676

1.45

166.55

2

8

7

26

680

2

S1C([H])([H])C(C([H])([H])OC(C([H])([H])[H])=O)=C(C(=O)O[H])N2C([C@]([H])([C@@]12[H])N([H])C(C([H])([H])C1=C([H])C([H])=C([H])S1)=O)=O

XIURVHNZVLADCM-IUODEOHRSA-N

InChI=1S/C16H16N2O6S2/c1-8(19)24-6-9-7-26-15-12(14(21)18(15)13(9)16(22)23)17-11(20)5-10-3-2-4-25-10/h2-4,12,15H,5-7H2,1H3,(H,17,20)(H,22,23)/t12-,15-/m1/s1

(6R,7R)-3-(acetyloxymethyl)-8-oxo-7-[(2-thiophen-2-ylacetyl)amino]-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid

Cefalotin; Cephalothin; Cephalotin; Cefalothin; Cefalotina; Monosodium Salt, Cephalothin; Normon Brand of Cephalothin Sodium; Salt, Cephalothin Monosodium; Seffin; Sodium Cephalothin; Spaly Brand of Cephalothin Sodium;

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

注意： (1). 本产品在运输和储存过程中需避光。  (2). 请将本产品存放在密封且受保护的环境中（例如氮气保护），避免吸湿/受潮。

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

DMSO : 79~100 mg/mL ( 199.27~252.24 mM)

配方 1 中的溶解度: ≥ 2.5 mg/mL (6.31 mM) (饱和度未知) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将100 μL 25.0 mg/mL澄清DMSO储备液加入到400 μL PEG300中，混匀；然后向上述溶液中加入50 μL Tween-80，混匀；加入450 μL生理盐水定容至1 mL。
*生理盐水的制备：将 0.9 g 氯化钠溶解在 100 mL ddH₂O中，得到澄清溶液。

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配方 2 中的溶解度: ≥ 2.5 mg/mL (6.31 mM) (饱和度未知) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将 100 μL 25.0 mg/mL澄清DMSO储备液加入900 μL 20% SBE-β-CD生理盐水溶液中，混匀。
*20% SBE-β-CD 生理盐水溶液的制备（4°C，1 周）：将 2 g SBE-β-CD 溶解于 10 mL 生理盐水中，得到澄清溶液。

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配方 3 中的溶解度: ≥ 2.5 mg/mL (6.31 mM) (饱和度未知) in 10% DMSO + 90% Corn Oil (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将 100 μL 25.0 mg/mL 澄清 DMSO 储备液加入到 900 μL 玉米油中并混合均匀。

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配方 4 中的溶解度: 10% DMSO+40% PEG300+5% Tween-80+45% Saline: ≥ 2.5 mg/mL (6.31 mM)

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请根据您的实验动物和给药方式选择适当的溶解配方/方案：
1、请先配制澄清的储备液(如：用DMSO配置50 或 100 mg/mL母液(储备液));
2、取适量母液，按从左到右的顺序依次添加助溶剂，澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明，并不一定代表此产品 的实际溶解配方):
10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline);
假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀/澄清；向上述体系中加入50 μL Tween-80，混合均匀/澄清；然后继续加入450 μL ddH2O (或 saline)定容至 1 mL；
3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例;
4、 如产品在配制过程中出现沉淀/析出，可通过加热(≤50℃)或超声的方式助溶;
5、为保证最佳实验结果，工作液请现配现用！
6、如不确定怎么将母液配置成体内动物实验的工作液，请查看说明书或联系我们;
7、 以上所有助溶剂都可在 Invivochem.cn网站购买。