The antibiotic cefpodoxime (cefpodoxime acid) has a minimum inhibitory concentration (MIC) of 0.125–4 mg/L against Gram-negative anaerobic bacteria (Bacteroidetesceae). MIC values of 0.25-8 mg/L are observed for cefpodoxime's inhibition of Veillonella parvum. Cefpodoxime inhibits Peptostreptococcus glycolytica, Peptostreptococcus parvum, and Ruminococcus brucei, at a minimum inhibitory concentration (MIC) of less than two milligrams per liter [1]. Cefpodoxime, or cefpodoxime acid, inhibits the populations of Streptococcus pneumoniae and Streptococcus pyogenes bacteria. units for colony formation[2].

Mice respond well to cephalosporins (2.5 to 50 mg/kg; oral; once every 8 hours; for 48 hours straight) in terms of treatment [3].

Animal/Disease Models: Female Swiss CD1 mice [3]
Doses: 2.5, 5, 10, 25, 40 and 50 mg/kg
Route of Administration: Oral;
Route of Administration: Oral. Every 8 hrs (hrs (hours)); 48 hour
Experimental Results: Efficacy value >350 obtained.

Absorption, Distribution and Excretion
Cefpodoxime proxetil is a prodrug that is absorbed from the gastrointestinal tract and then deesterified to its active metabolite, cefpodoxime. In fasting subjects, approximately 50% of the administered dose of 100 mg cefpodoxime proxetil is absorbed systemically. Within the recommended dose range (100 to 400 mg), approximately 29% to 33% of the administered dose is excreted unchanged in the urine within 12 hours. Biological Half-Life 2.09 to 2.84 hours

Effects During Pregnancy and Lactation
◉ Overview of Use During Lactation
Limited information suggests that low concentrations of cefpodoxime in breast milk are not expected to have any 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 adequately assessed. Cefpodoxime 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
A 40-year-old non-pregnant woman developed hyperprolactinemia and bilateral galactorrhea after taking cefpodoxime 200 mg twice daily for two days. Seven days after discontinuation of the medication, the galactorrhea resolved, and serum prolactin levels significantly decreased to the normal range. One month later, prolactin levels decreased further. Since no other cause was found, the authors believe that the galactorrhea and hyperprolactinemia were most likely caused by cefpodoxime. A 22-year-old woman was taking extended-release venlafaxine 150 mg/day for 3 months. Two weeks ago, she started taking cefpodoxime 200 mg/day for 14 days. Afterward, she experienced bilateral breast engorgement and galactorrhea, lasting for 3 days. Laboratory tests and a head CT scan were normal, with only a slight increase in alkaline phosphatase and elevated serum prolactin levels. Within two weeks, her galactorrhea began to lessen and disappeared after three weeks, during which time the venlafaxine dose remained unchanged. Her serum prolactin levels also returned to normal. The authors believe that her symptoms and hyperprolactinemia were likely caused by cefpodoxime. Prolactin levels in mothers who have established lactation may not affect their ability to breastfeed. Serum protein binding rate: 22% to 33%, plasma protein binding rate: 21% to 29%.

[1]. Werner H, et, al. Comparative in vitro activity of cefpodoxime against anaerobes other than Bacteroides fragilis. Infection. 1991 Sep-Oct;19(5):377-9.
[2]. Valentini S, et, al. In-vitro evaluation of cefpodoxime. J Antimicrob Chemother. 1994 Mar;33(3):495-508.
[3]. Pérez-Trallero E, et, al. Prediction of in-vivo efficacy by in-vitro early bactericidal activity with oral beta-lactams, in a dose-ranging immunocompetent mouse sepsis model, using strains of Streptococcus pneumoniae with decreasing susceptibilities to penicillin. J Chemother. 2001 Apr;13(2):118-25.

Cefpodoxime is a third-generation cephalosporin antibiotic. Its cephalosporin skeleton has methoxymethyl and (2Z)-2-(2-amino-1,3-thiazolyl)-2-(methoxyimino)acetamino substituents at positions 3 and 7, respectively. It is administered orally as an ester prodrug for the treatment of acute otitis media, pharyngitis, and sinusitis. It is an antibacterial drug. It belongs to the cephalosporin and carboxylic acid classes. Cefpodoxime is an oral third-generation cephalosporin antibiotic effective against most Gram-positive and Gram-negative bacteria. Cefpodoxime proxetil is commonly used to treat acute otitis media, pharyngitis, and sinusitis. It is a prodrug that is deesterified into cefpodoxime after absorption through the intestinal mucosa. Cefpodoxime is a cephalosporin antibacterial drug. Cefpodoxime is a third-generation semi-synthetic cephalosporin and also a β-lactam antibiotic with bactericidal activity. Cefpodoxime's mechanism of action involves binding to penicillin-binding proteins (PBPs) 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, cefpodoxime inhibits the synthesis of bacterial septa and cell walls. Cefpodoxime is a third-generation cephalosporin antibiotic. Its cephalosporin core contains a methoxy group at the C-3 position. See also: cefpodoxime proxetil (active ingredient); cefpodoxime sodium (active ingredient). Indications: For the treatment of mild to moderate infections caused by susceptible strains of specified microorganisms. FDA Label: Cefpodoxime is effective against a variety of Gram-positive and Gram-negative bacteria. Cefpodoxime is stable in the presence of β-lactamases. Therefore, many microorganisms resistant to penicillin and cephalosporins due to the production of β-lactamases may be sensitive to cefpodoxime. Cefpodoxime is inactivated by certain extended-spectrum β-lactamases. The bactericidal activity of cefpodoxime stems from its inhibition of cell wall synthesis. The active metabolite of cefpodoxime preferentially binds to penicillin-binding protein 3, thereby inhibiting the synthesis of peptidoglycan (a major component of bacterial cell walls).

---

Pharmacodynamics
Cefpodoxime is effective against most Gram-positive and Gram-negative bacteria, but ineffective against Pseudomonas aeruginosa, Enterococcus, and Bacteroides fragilis.

C15H17N5O6S2

427.46

427.062

80210-62-4

Cefpodoxime-d3;2477791-28-7

6335986

White to off-white solid powder

1.8±0.1 g/cm3

200-202ºC

1.780

0.94

3

11

7

28

744

2

C(C1=C(COC)CS[C@@H]2[C@@H](C(N12)=O)NC(=O)/C(/C1=CSC(N)=N1)=N\OC)(=O)O

WYUSVOMTXWRGEK-HBWVYFAYSA-N

InChI=1S/C15H17N5O6S2/c1-25-3-6-4-27-13-9(12(22)20(13)10(6)14(23)24)18-11(21)8(19-26-2)7-5-28-15(16)17-7/h5,9,13H,3-4H2,1-2H3,(H2,16,17)(H,18,21)(H,23,24)/b19-8-/t9-,13-/m1/s1

5-Thia-1-azabicyclo(4.2.0)oct-2-ene-2-carboxylic acid, 7-(((2-amino-4-thiazolyl)(methoxyimino)acetyl)amino)-3-(methoxymethyl)-8-oxo-, (6R-(6alpha,7beta(Z)))-

U76253AR-3746 U-76253AR3746 R 3763 U 76253AR-3763 R3763

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, avoid exposure to moisture.

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

DMSO : ~250 mg/mL (~584.85 mM)

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.

---

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).

View More

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)

---

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).

View More

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

---

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.

---

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