Absorption, Distribution and Excretion
Oral bioavailability is approximately 95%. 0.23 L/kg 3 mL/min/kg [Fasting subjects] Metabolisms/Metabolites Cefprozil is primarily excreted via the kidneys. Biological Half-Life 1.3 hours

Effects During Pregnancy and Lactation
◉ Overview of Use During Lactation
Limited information currently available indicates that cefprozil concentrations in breast milk are low and 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. Cefprozil 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 Rate
36%

Cefprozil is a semi-synthetic second-generation cephalosporin with a propenyl group at position 3 and an (R)-2-amino-2-(4-hydroxyphenyl)acetamide group at positions 7 of its cephalosporin backbone. It is used to treat bronchitis and ear, skin, and other bacterial infections. It is an antibacterial drug. It is a semi-synthetic cephalosporin derivative. Cefprozil is a commonly used cephalosporin antibiotic used to treat various bacterial infections, including ear and skin infections, bronchitis, etc. Cefprozil is a semi-synthetic cephalosporin β-lactam antibiotic with bactericidal activity. The action of cefprozil depends on its binding to penicillin-binding proteins (PBPs) located on the bacterial cell membrane. After binding to transpeptidase, cefprozil inhibits its activity, thereby preventing the cross-linking of the pentaglycine bridge to the fourth amino acid residue of the pentapeptide, and thus blocking the synthesis of peptidoglycan chains. Therefore, cefprozil inhibits the synthesis of bacterial septa and cell walls. Anhydrous cefprozil (E) is an anhydrous E-isomer of a semi-synthetic cephalosporin β-lactam antibiotic with bactericidal activity. Cefprozil's action depends on its binding to penicillin-binding protein (PBP) located on the bacterial cell membrane. Upon binding, transpeptidase activity is inhibited, preventing the cross-linking of the pentaglycine bridge to the fourth amino acid residue of the pentapeptide, thereby blocking peptidoglycan chain synthesis. Therefore, cefprozil inhibits the synthesis of bacterial septa and cell walls. Anhydrous cefprozil is the anhydrous form of cefprozil, a semi-synthetic broad-spectrum second-generation cephalosporin with antibacterial activity. Cefprozil binds to and inactivates penicillin-binding protein (PBP) located on the inner membrane of the bacterial cell wall. PBP is an enzyme involved in the final stages of bacterial cell wall assembly and in remodeling the cell wall during growth and division. Inactivation of PBP interferes with the cross-linking of peptidoglycan chains, which is crucial for the strength and rigidity of the bacterial cell wall. This leads to weakening of the bacterial cell wall and causes cell lysis.
A second-generation cephalosporin antibiotic. Cefprozil has a benzene ring at the C-3 position of its cephalosporin core.
Indications

For the treatment of infections caused by the following bacteria (respiratory, skin, soft tissue, urinary tract, ear, nose, and throat): Streptococcus pneumoniae, Haemophilus influenzae, Staphylococcus, Streptococcus pyogenes (Group A β-hemolytic streptococci), Escherichia coli, Proteus mirabilis, Klebsiella spp., and coagulase-negative staphylococci.
FDA label
Mechanism of action

Cefprozil, like penicillin antibiotics, is a β-lactam antibiotic. It inhibits the third (and final) stage of bacterial cell wall synthesis by binding to specific penicillin-binding proteins (PBPs) located within the bacterial cell wall. Subsequently, bacterial cell wall autolysins (such as autolysins) mediate cell lysis; cefprozil may interfere with autolysin inhibitors.

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Pharmacodynamics
Cefprozil is a semi-synthetic second-generation cephalosporin used to treat otitis media, soft tissue infections, and respiratory infections.

C18H19N3O5S

389.43

389.104

92665-29-7

Cefprozil monohydrate;121123-17-9

5281006

Typically exists as solid at room temperature

1.5±0.1 g/cm3

803.1±65.0 °C at 760 mmHg

76°C

439.5±34.3 °C

0.0±3.0 mmHg at 25°C

1.718

0.06

4

7

5

27

699

3

C(C1=C(C=CC)CS[C@@H]2[C@@H](C(N12)=O)NC(=O)[C@@H](C1C=CC(O)=CC=1)N)(=O)O

WDLWHQDACQUCJR-ZAMMOSSLSA-N

InChI=1S/C18H19N3O5S/c1-2-3-10-8-27-17-13(16(24)21(17)14(10)18(25)26)20-15(23)12(19)9-4-6-11(22)7-5-9/h2-7,12-13,17,22H,8,19H2,1H3,(H,20,23)(H,25,26)/b3-2+/t12-,13-,17-/m1/s1

(6R,7R)-7-[[(2R)-2-amino-2-(4-hydroxyphenyl)acetyl]amino]-8-oxo-3-[(E)-prop-1-enyl]-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid

Brisoral; Cefprozil anhydrous; Cefprozil

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

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

May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples

Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.

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Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)
*Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution.
Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline)
Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil)
Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals).

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Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)]
*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.
Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin → 500 μL Saline)
Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO → 100 μLPEG300 → 200 μL castor oil → 650 μL Saline)
Injection Formulation 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (i.e. 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline)
Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline
Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH → 900 μL Corn oil)
Injection Formulation 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline)

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Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium)
Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose
Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals).

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Oral Formulation 3: Dissolved in PEG400
Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose
Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose
Oral Formulation 6: Mixing with food powders

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Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.

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