Ceftizoxime is a novel derivative of parenteral cephalosporin. It is more effective against different types of leather than cephalosporins and cephalomycins, such as cefotiam, cefamandole, cefuroxime, cefotaxime, and cefmetazole. More active are lamb-negative bacilli, which include opportunistic infections like Enterobacter, Citrobacter, and Serratia marcescens. Broad-spectrum antibacterial activity of ceftizoxime is demonstrated against both aerobic Gram-positive and Gram-negative bacteria [1].

Ceftizoxime and cefotaxime had nearly identical therapeutic effects on mice infected with modest inoculums [1]. Serum, urine, and tissue homogenates are biological fluids in which ceftizoxime is stable, but rat tissue homogenates are unstable with cefotaxime. Among all antibiotics, ceftizoxime had the lowest binding to serum proteins across all species: 31% in rats, 17% in dogs, and 31% in humans [2].

Absorption, Distribution and Excretion
Cefotaxime is excreted almost unchanged via the kidneys within 24 hours. The mean apparent volume of distribution is between 15 and 28 liters. Metabolism/Metabolites Cefotaxime is not metabolized and is excreted almost unchanged via the kidneys within 24 hours.

Effects During Pregnancy and Lactation
◉ Overview of Use During Lactation
Limited information suggests that low concentrations of cefotaxime in breast milk are not expected to have adverse effects on breastfed infants. There are reports that cephalosporins occasionally disrupt the infant's gut microbiota, leading to diarrhea or thrush, but these effects have not been fully assessed. Cefotaxime is safe for use by breastfeeding women.
◉ Effects on Breastfed Infants
No published information found as of the revision date.
◉ Effects on Lactation and Breast Milk
No published information found as of the revision date.

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Protein Binding
The protein binding rate is 30% within the standard concentration range.

[1]. Kamimura T, et al. Ceftizoxime (Ceftizoxime), a new parenteral cephalosporin: in vitro and in vivo antibacterial activities. Antimicrob Agents Chemother. 1979 Nov;16(5):540-8.
[2]. Murakawa T, et al. Pharmacokinetics of ceftizoxime in animals after parenteral dosing. Antimicrob Agents Chemother. 1980 Feb;17(2):157-64

Cefotaxime is a third-generation cephalosporin for injection, containing a 2-(2-amino-1,3-thiazolyl-4-yl)-2-(methoxyimino)acetyl]amino group at the 7β position. It is an antibacterial drug and the conjugate acid of cefotaxime (1-). It is a semi-synthetic cephalosporin antibiotic, administered intravenously or as a suppository. This drug exhibits high resistance to various β-lactamases but is effective against a wide range of aerobic and anaerobic Gram-positive and Gram-negative bacteria. Cefotaxime has few side effects and has been reported to be safe and effective in elderly patients and patients with hematologic disorders. Cefotaxime is a cephalosporin antibiotic. Cefotaxime is a semi-synthetic, broad-spectrum, β-lactamase-resistant third-generation cephalosporin with antibacterial activity. Cefotaxime binds to and inactivates penicillin-binding proteins (PBPs) located on the inner membrane of bacterial cell walls. PBPs are enzymes involved in the final stages of bacterial cell wall assembly and in the remodeling of the cell wall during bacterial growth and division. Inactivation of PBPs interferes with the cross-linking of peptidoglycan chains, which is crucial for maintaining the strength and rigidity of the bacterial cell wall. This leads to weakening of the bacterial cell wall, ultimately resulting in cell lysis. Cefotaxime is a semi-synthetic cephalosporin antibiotic, administered intravenously or via suppository. This drug exhibits high resistance to various β-lactamases and is effective against a wide range of aerobic and anaerobic Gram-positive and Gram-negative bacteria. It has few side effects and has been reported to be safe and effective in elderly patients and patients with hematologic disorders. Drug Indications Cefotaxime has previously been approved for the treatment of infections caused by susceptible bacterial strains. Mechanism of Action Cefotaxime is an aminothiazole cephalosporin with broad-spectrum antibacterial activity against a variety of Gram-negative nosocomial pathogens. It exhibits excellent β-lactamase stability and demonstrates good antibacterial activity against Haemophilus influenzae, Neisseria gonorrhoeae, and Klebsiella pneumoniae in vitro. Cefotaxime, like penicillins, belongs to the β-lactam antibiotic class. Cefotaxime inhibits the third and final stage of bacterial cell wall synthesis by binding to a specific penicillin-binding protein (PBP) located within the bacterial cell wall. Subsequently, bacterial cell wall autolysins (such as autolysins) mediate cell lysis; cefotaxime may interfere with the action of autolysin inhibitors.

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Pharmacodynamics
Cefotaxime exhibits high resistance to various β-lactamases and is effective against a wide range of aerobic and anaerobic Gram-positive and Gram-negative bacteria. It has few side effects and has been reported to be safe and effective in elderly patients and patients with hematologic disorders.

C13H13N5O5S2

383.4028

383.035

68401-81-0

Ceftizoxime sodium;68401-82-1

6533629

White to off-white solid powder

1.9±0.1 g/cm3

227 °C(dec.)

1.849

0.59

3

10

5

25

669

2

S1C([H])([H])C([H])=C(C(=O)O[H])N2C([C@]([H])([C@@]12[H])N([H])C(/C(/C1=C([H])SC(N([H])[H])=N1)=N\OC([H])([H])[H])=O)=O

NNULBSISHYWZJU-LLKWHZGFSA-N

InChI=1S/C13H13N5O5S2/c1-23-17-7(5-4-25-13(14)15-5)9(19)16-8-10(20)18-6(12(21)22)2-3-24-11(8)18/h2,4,8,11H,3H2,1H3,(H2,14,15)(H,16,19)(H,21,22)/b17-7-/t8-,11-/m1/s1

(6R,7R)-7-[[(2Z)-2-(2-amino-1,3-thiazol-4-yl)-2-methoxyiminoacetyl]amino]-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light.

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

DMSO : ~25 mg/mL (~65.21 mM)

Solubility in Formulation 1: ≥ 2.5 mg/mL (6.52 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

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Solubility in Formulation 2: ≥ 2.5 mg/mL (6.52 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.

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Solubility in Formulation 3: ≥ 2.5 mg/mL (6.52 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.

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 (Please use freshly prepared in vivo formulations for optimal results.)