CEFAZOLIN- cefazolin sodium injection, solution
Baxter Healthcare Corporation
To reduce the development of drug-resistant bacteria and maintain the effectiveness of Cefazolin Injection, USP and other antibacterial drugs, Cefazolin Injection, USP should be used only to treat or prevent infections that are proven or strongly suspected to be caused by bacteria.
Cefazolin Injection, USP is a semi-synthetic cephalosporin for parenteral administration. It is the sodium salt of (6R ,7R)-3-[[(5-methyl-1,3,4-thiadiazol-2-yl)thio]methyl]-8-oxo-7-[2-(1H -tetrazol-1-yl)acetamido]-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid.
Image of Structural Formula for Cefazolin Injection, USP
(click image for full-size original)
The sodium content is 46 mg per gram of cefazolin.
Dextrose Hydrous, USP structural (molecular) formula:
Dextrose Hydrous, USP structural (molecular) formula
The molecular weight of Dextrose Hydrous, USP is 198.17.
The chemical name is D-Glucose, Monohydrate.
Cefazolin Injection, USP is a frozen, premixed, iso-osmotic, sterile, nonpyrogenic 50 mL solution containing cefazolin sodium equivalent to 1 g of Cefazolin, USP. Dextrose, USP has been added to adjust osmolality (2 g as dextrose hydrous).
The pH of Cefazolin Injection, USP has been adjusted with sodium bicarbonate. The solution is intended for intravenous use after thawing to room temperature.
This GALAXY container (PL 2040 Plastic) is fabricated from a specially designed multilayer plastic (PL 2040). Solutions are in contact with the polyethylene layer of this container and can leach out certain chemical components of the plastic in very small amounts within the expiration period. However, the suitability of the plastic has been confirmed in tests in animals according to the USP biological tests for plastic containers, as well as by tissue culture toxicity studies.
Studies have shown that following intravenous administration of cefazolin to normal volunteers, mean serum concentrations peaked at approximately 185 mcg/mL and were approximately 4 mcg/mL at 8 hours for a 1-gram dose.
The serum half-life for cefazolin is approximately 1.8 hours following intravenous administration.
In a study (using normal volunteers) of constant intravenous infusion with dosages of 3.5 mg/kg for 1 hour (approximately 250 mg) and 1.5 mg/kg the next 2 hours (approximately 100 mg), cefazolin produced a steady serum level at the third hour of approximately 28 mcg/mL.
Studies in patients hospitalized with infections indicate that cefazolin produces mean peak serum levels approximately equivalent to those seen in normal volunteers.
Bile levels in patients without obstructive biliary disease can reach or exceed serum levels by up to 5 times; however, in patients with obstructive biliary disease, bile levels of cefazolin are considerably lower than serum levels (<1.0 mcg/mL).
In synovial fluid, the level of cefazolin becomes comparable to that reached in serum at about 4 hours after drug administration.
Studies of cord blood show prompt transfer of cefazolin across the placenta. Cefazolin is present in very low concentrations in the milk of nursing mothers.
Cefazolin is excreted unchanged in the urine. In the first 6 hours approximately 60% of the drug is excreted in the urine and this increases to 70% to 80% within 24 hours.
In patients undergoing peritoneal dialysis (2 L/hr.), cefazolin produced mean serum levels of approximately 10 and 30 mcg/mL after 24 hours instillation of a dialyzing solution containing 50 mg/L and 150 mg/L, respectively. Mean peak levels were 29 mcg/mL (range 13 to 44 mcg/mL) with 50 mg/L (3 patients), and 72 mcg/mL (range 26 to 142 mcg/mL) with 150 mg/L (6 patients). Intraperitoneal administration of cefazolin is usually well tolerated.
Controlled studies on adult normal volunteers, receiving 1 gram 4 times a day for 10 days, monitoring CBC, SGOT, SGPT, bilirubin, alkaline phosphatase, BUN, creatinine, and urinalysis, indicated no clinically significant changes attributed to cefazolin.
Mechanism of Action
Cefazolin is a bactericidal agent that acts by inhibition of bacterial cell wall synthesis.