Cefazolin ??

Cefazolin MSDS

Cefazolin

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Cefazolin has the natural acetyl side chain at C-3 replaced by a thio-linked thiadiazole ring. Although this group is an activating leaving group, the moiety is not subject to the inactivating host hydrolysis reaction that characterizes cephapirin. At C-7, it possesses a tetrazoylmethylene unit. Cefazolin is less irritating on injection than its cohort in this generation of drugs and has a longer half-life than cephapirin. Its dosing should be reduced in the presence of renal impairment. It is comparatively unstable and should be protected from heat and light.

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Cefazolin is an antibacterial compound derived from 7-amino-cephalosporanic acid.

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ChEBI: A cephalosporin compound having [(5-methyl-1,3,4-thiadiazol-2-yl)sulfanyl]methyl and (1H-tetrazol-1-ylacetyl)amino side-groups.

Antimicrobial activity

Enterobacter, Klebsiella, Providencia, Serratia spp. and Pr. vulgaris are all resistant. B. fragilis is resistant, but other anaerobes are susceptible.

Pharmacokinetics

Distribution
The volume of distribution is the smallest of the cephalosporins in group 1, perhaps an indication of relative confinement to the plasma space. It crosses inflamed synovial membranes, but the levels achieved are well below those of the simultaneous serum levels and entry to the CSF is poor. In patients receiving 10 mg/kg by intravenous bolus, mean concentrations in cancellous bone were 3.0 mg/kg when the mean serum concentration was 33 mg/L, giving a bone:serum ratio of 0.09. Some crosses the placenta, but the concentrations found in the fetus and membranes are low.
Metabolism and excretion
It is not metabolized. Around 60% of the dose is excreted in the urine within the first 6 h, producing concentrations in excess of 1 g/L. Excretion is depressed by probenecid. The renal clearance is around 65 mL/min and declines in renal failure, when the half-life may rise to 40 h, although levels in the urine sufficient to inhibit most urinary pathogens are still found. It is moderately well removed by hemodialysis and less well by peritoneal dialysis.
Levels sufficient to inhibit a number of enteric organisms likely to infect the biliary tract are found in T-tube bile (17–31 mg/L after a 1 g intravenous dose), but this is principally due to the high serum levels of the drug and the total amounts excreted via the bile are small.

Clinical Use

Cefazolin has been widely used in surgical prophylaxis, especially in biliary tract (because of the moderately high concentrations achieved in bile), orthopedic, cardiac and gynecological surgery.

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Side effects are those common to other cephalosporins ,including rare bleeding disorders and encephalopathy in patients in whom impaired excretion or direct instillation leads to very high CSF levels. Neutropenia has been described and hypoprothrombinemic bleeding has been attributed to the side chain.

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Shaanxi Xianhe Biotech Co., Ltd	+86-17709210191; +86-17709210191	Jerry@xhobio.com	China	901	58
Henan Tianfu Chemical Co.,Ltd.	+86-0371-55170693 +86-19937530512	info@tianfuchem.com	China	21531	55
Xiamen AmoyChem Co., Ltd	+86-86-5926051114	sales@amoychem.com	China	6361	58
HubeiwidelychemicaltechnologyCo.,Ltd	18627774460	faith@widelychemical.com	CHINA	738	58
BOC Sciences	+1-631-485-4226	inquiry@bocsci.com	United States	19935	58
CONIER CHEM AND PHARMA LIMITED		sales@conier.com	China	49906	58
career henan chemical co	+86-0371-86658258	factory@coreychem.com	China	29780	58
Antai Fine Chemical Technology Co.,Limited	18503026267	info@antaichem.com	CHINA	9631	58
SIMAGCHEM CORP	+86-5922680277 +86-13806087780	sale@simagchem.com	China	17339	58
TargetMol Chemicals Inc.	+1-781-999-5354; +1-00000000000	marketing@targetmol.com	United States	32431	58

Cefazolin ?? ??: