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 de-esterified to its active metabolite, cefpodoxime. Following oral administration of 100 mg of cefpodoxime proxetil to fasting subjects, approximately 50% of the administered cefpodoxime dose was absorbed systemically.
Over the recommended dosing range (100 to 400 mg), approximately 29 to 33% of the administered cefpodoxime dose was excreted unchanged in the urine in 12 hours.

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Biological Half-Life
2.09 to 2.84 hours

Effects During Pregnancy and Lactation
◉ Summary of Use during Lactation
Limited information indicates that cefpodoxime produces low levels in milk and is not be expected to cause any adverse effects in breastfed infants. Occasionally disruption of the infant's gastrointestinal flora, resulting in diarrhea or thrush have been reported with cephalosporins, but these effects have not been adequately evaluated. Cefpodoxime is acceptable in nursing mothers.
◉ Effects in Breastfed Infants
Relevant published information was not found as of the revision date.
◉ Effects on Lactation and Breastmilk
Hyperprolactinemia and bilateral galactorrhea occurred in a nonpregnant, 40-year-old woman taking cefpodoxime 200 mg twice daily for 2 days. Seven days after stopping the drug, galactorrhea ceased and the serum prolactin dropped markedly into the normal range. One month later it had dropped further. Because no other cause could be found, the authors determined that the galactorrhea and hyperprolactinemia were probably caused by cefpodoxime.
A 22-year-old woman who had been taking slow-release venlafaxine 150 mg daily for 3 months reported bilateral breast engorgement and galactorrhea for 3 days after being prescribed cefpodoxime 200 mg twice daily for 14 days 2 weeks prior. Laboratory and head CT results were normal except for a slight elevation in alkaline phosphatase and an elevated serum prolactin level. Her galactorrhea began decreasing within 2 weeks and disappeared in 3 weeks with no change in venlafaxine dosage. Her serum prolactin level also returned to normal. The authors felt that her symptoms and hyperprolactinemia were probably caused by cefpodoxime.
The prolactin level in a mother with established lactation may not affect her ability to breastfeed.

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Protein Binding
22 to 33% in serum and from 21 to 29% in plasma.

[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 with methoxymethyl and (2Z)-2-(2-amino-1,3-thiazol-4-yl)-2-(methoxyimino)acetamino substituents at positions 3 and 7, respectively, of the cephem skeleton. Given by mouth as its proxetil ester prodrug, it is used to treat acute otitis media, pharyngitis, and sinusitis. It has a role as an antibacterial drug. It is a cephalosporin and a carboxylic acid.
Cefpodoxime is an oral third generation cephalosporin antibiotic with effectiveness against most Gram positive and Gram negative bacteria. Commonly used to treat acute otitis media, pharyngitis, and sinusitis, cefpodoxime proxetil is a prodrug which is absorbed and de-esterified by the intestinal mucosa to Cefpodoxime.
Cefpodoxime is a Cephalosporin Antibacterial.
Cefpodoxime is a third generation semi-synthetic cephalosporin and a beta-lactam antibiotic with bactericidal activity. Cefpodoxime's effect is dependent on its binding to penicillin-binding proteins (PBPs) located in the bacterial cytoplasmic membrane. Binding results in the inhibition of the transpeptidase enzymes, thereby preventing cross-linking of the pentaglycine bridge with the fourth residue of the pentapeptide and interrupting consequent synthesis of peptidoglycan chains. As a result, cefpodoxime inhibits bacterial septum and cell wall synthesis formation.
A third-generation cephalosporin antibiotic. Cefpodoxime contains a methoxy group at C-3 of its cephalosporin core.
See also: Cefpodoxime Proxetil (active moiety of); Cefpodoxime Sodium (is active moiety of).

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Drug Indication
Indicated for the treatment of patients with mild to moderate infections caused by susceptible strains of the designated microorganisms.
FDA Label

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Mechanism of Action
Cefpodoxime is active against a wide spectrum of Gram-positive and Gram-negative bacteria. Cefpodoxime is stable in the presence of beta-lactamase enzymes. As a result, many organisms resistant to penicillins and cephalosporins, due to their production of beta-lactamase, may be susceptible to cefpodoxime. Cefpodoxime is inactivated by certain extended spectrum beta-lactamases. The bactericidal activity of cefpodoxime results from its inhibition of cell wall synthesis. The active metabolite of cefpodoxime binds preferentially to penicillin binding protein 3, which inhibits production of peptidoglycan, the primary constituent of bacterial cell walls.

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Pharmacodynamics
Cefpodoxime is shown to be effective against most Gram positive and Gram negative bacteria, except Pseudomonas aeruginosa, Enterococcus, and Bacteroides fragilis.

C15H17N5O6S2

427.46

427.062

80210-62-4

Cefpodoxime-d3;2477791-28-7

6335986

Typically exists as solid at room temperature

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.

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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.)