Absorption, Distribution and Excretion
In children with acute or chronic/recurrent secretory otitis media, cefuroxime is distributed into the middle ear effusion after oral administration of cefuroxime axetil. A study in children aged 1–4 years with acute secretory otitis media showed that 2–5 hours after a single dose of 15 mg/kg cefuroxime axetil oral suspension, the concentration of cefuroxime in the middle ear effusion ranged from 0.2–3.6 μg/mL; the serum concentration was 2.8–7.3 μg/mL. In pharmacokinetic studies of cefuroxime axetil oral suspension in children, the drug was administered after meals or with food; data on absorption of this suspension in children on an empty stomach are currently unavailable. In children aged 3 months to 12 years (mean age: 23 months), a single oral dose of 10, 15, or 20 mg/kg of commercially available cefuroxime axetil oral suspension, taken concurrently with milk or dairy products, resulted in peak serum cefuroxime concentrations reached approximately 3.6, 2.7, or 3.1 hours post-administration, with mean concentrations of 3.3, 5.1, or 7 mcg/mL, respectively. A study in healthy adults demonstrated bioequivalence of cefuroxime axetil oral suspensions at concentrations of 125 mg/5 mL or 250 mg/5 mL. In healthy adults, administration of 250 mg cefuroxime axetil suspension (concentrations of 125 mg/5 mL and 250 mg/5 mL, respectively) with food resulted in peak plasma cefuroxime concentrations of 2.4 μg/mL and 2.2 μg/mL, respectively, both reached 3 hours post-administration.
In adults, after an oral single dose of 125 mg, 250 mg, 500 mg, or 1 g of commercially available cefuroxime axetil tablets immediately after a meal, peak serum concentrations of cefuroxime were reached approximately 2–3 hours after administration, with average concentrations of 2.1 μg/mL, 4.1 μg/mL, 7 μg/mL, or 13.6 μg/mL, respectively; mean serum concentrations at 6 hours after administration were 0.3 μg/mL, 0.7 μg/mL, 2.2 μg/mL, or 3.4 μg/mL, respectively. The mean drug AUCs for these subjects were 6.7, 12.9, 27.4, or 50 mcg-h/mL, respectively.
For more complete data on absorption, distribution, and excretion of cefuroxime axetil (13 in total), please visit the HSDB records page.

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Metabolism/Metabolites
After oral administration, cefuroxime axetil is rapidly hydrolyzed to cefuroxime by nonspecific esterases in the intestinal mucosa and blood; the ester group is metabolized to acetaldehyde and acetic acid. Cefuroxime is not metabolized and is mainly excreted unchanged in the urine via glomerular filtration and renal tubular secretion.

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Biological Half-Life
In newborns and children, the serum half-life of cefuroxime is inversely proportional to age. ^{6 25 30}In children aged 3 months to 12 years, the average serum half-life of cefuroxime after oral administration of cefuroxime axetil suspension is 1.4–1.9 hours.
In adults, the serum or plasma half-life of cefuroxime after oral administration of commercially available cefuroxime axetil tablets or suspension is 1.2–1.6 hours.
Because cefuroxime is excreted by the kidneys, the serum half-life is prolonged in patients with impaired renal function. In a study of 20 elderly patients (mean age = 83.9 years), the mean creatinine clearance was 34.9 mL/min and the mean serum elimination half-life was 3.5 hours.

Interactions
Drugs that lower stomach acid may reduce the bioavailability of cefuroxime compared to an empty stomach and tend to counteract the effects of postprandial absorption. Taking oral probenecid shortly before or concurrently with cefuroxime typically slows the renal tubular secretion rate of cefuroxime, resulting in higher and more sustained serum cefuroxime concentrations. This effect is commonly used to treat gonorrhea. Concomitant use of probenecid has been reported to increase peak serum concentrations and half-life of cefuroxime by up to 30%; the area under the concentration-time curve (AUC) of cefuroxime has increased by approximately 50%. Concomitant use of probenecid has been reported to decrease the apparent volume of distribution of cefuroxime by approximately 20%. Cefuroxime axetil may affect the gut microbiota, leading to reduced estrogen reabsorption and decreased efficacy of oral contraceptives containing estrogen and progestin. The manufacturer notes that patients taking diuretics should use cefuroxime with caution, as concomitant use of these medications may increase the risk of adverse renal reactions. In vitro studies have shown that cefuroxime and aminoglycoside antibiotics may have additive or synergistic antibacterial activities against certain microorganisms, including Enterobacter spp., Escherichia coli, Klebsiella spp., Proteus mirabilis, and Serratia marcescens. Concomitant use of aminoglycoside antibiotics and certain cephalosporins has been reported to increase the risk of nephrotoxicity during treatment. Although there are currently no reports of cefuroxime causing nephrotoxicity, the possibility of enhanced nephrotoxicity should be considered if this drug is used in combination with aminoglycoside antibiotics.

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Non-human toxicity values
Rabbit oral LD50: 200 mg/kg
Mouse subcutaneous LD50: 1840 mg/kg
Mouse intraperitoneal LD50: 510 mg/kg
Rats subcutaneous LD50: 2500 mg/kg
Rats intraperitoneal LD50: 950 mg/kg

Cefuroxime axetil is a cephalosporin. It has been reported that cefuroxime axetil exists in the Chinese honeybee (Apis cerana), and relevant data are available. Cefuroxime axetil is a second-generation semi-synthetic cephalosporin, belonging to the β-lactam antibiotic class, and possesses bactericidal activity. The action of cefuroxime depends on its binding to penicillin-binding proteins (PBPs) located on the bacterial cell membrane. Upon binding, transpeptidase activity is inhibited, thereby preventing the cross-linking of the pentagaryl bridge to the fourth amino acid residue of the pentapeptide, and thus blocking the synthesis of peptidoglycan chains. Therefore, cefuroxime inhibits the synthesis of bacterial septa and cell walls. See also: Cefuroxime (with active moiety). Cefuroxime axetil (E) - (Note moved to). Mechanism of Action: Cefuroxime generally has bactericidal activity. Like other cephalosporins, its antibacterial activity derives from the inhibition of peptidoglycan synthesis in the bacterial cell wall.

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Therapeutic Use
Antimicrobial Agent
Cefuroxime tablets and oral suspension are indicated for acute bacterial otitis media caused by Streptococcus pneumoniae, Haemophilus influenzae (including β-lactamase-producing strains), Moraxella catarrhalis (including β-lactamase-producing strains), or Streptococcus pyogenes. (Included on the US product label)
Cefuroxime tablets and oral suspension are indicated for pharyngitis/tonsillitis caused by Streptococcus pyogenes. Note: Intramuscular penicillin is usually the first-line treatment and prevention of streptococcal infections (including prevention of rheumatic fever). Cefuroxime tablets are generally effective in clearing streptococci from the nasopharynx; however, there is currently insufficient data to confirm the efficacy of cefuroxime in the prevention of rheumatic fever. Also note that in all clinical trials, all isolates must be sensitive to both penicillin and cefuroxime. There is currently insufficient and well-controlled data to demonstrate the effectiveness of cefuroxime in treating penicillin-resistant Streptococcus pyogenes strains. /US Product Label Includes/
Cefuroxime tablets are indicated for/acute bacterial maxillary sinusitis caused by Streptococcus pneumoniae or Haemophilus influenzae (non-β-lactamase-producing strains only). Note: Due to insufficient isolation of β-lactamase-producing Haemophilus influenzae and Moraxella catarrhalis strains in clinical trials of cefuroxime tablets for the treatment of acute bacterial maxillary sinusitis, the efficacy of cefuroxime tablets against sinus infections known, suspected, or probable to be caused by β-lactamase-producing Haemophilus influenzae or Moraxella catarrhalis could not be adequately evaluated. /US Product Label Includes/
For more complete data on the therapeutic uses of cefuroxime axetil (out of 15), please visit the HSDB record page.

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Drug Warnings
Patients should be informed that antimicrobial drugs (including cefuroxime) are intended for the treatment of bacterial infections only and not for the treatment of viral infections (such as the common cold). Patients should also be informed of the importance of completing the full course of treatment, even if they feel better after a few days. Missed doses or incomplete treatment courses may reduce efficacy and increase the likelihood of bacterial resistance, potentially leading to future ineligibility for cefuroxime or other antibiotics. To reduce the development of resistant bacteria and maintain the efficacy of cefuroxime and other antibiotics, this drug should only be used to treat or prevent infections confirmed or highly suspected to be caused by susceptible bacteria. When selecting or adjusting anti-infective treatment regimens, the results of bacterial cultures and in vitro drug susceptibility testing should be considered. If such data are unavailable, local epidemiology and drug susceptibility patterns should be considered when selecting empirical anti-infective drugs. Before initiating cefuroxime treatment, a thorough inquiry should be made into the patient's history of allergic reactions to cephalosporins, penicillins, or other drugs. Cefuroxime axetil is contraindicated in patients with a history of allergy to cefuroxime or other cephalosporins, and should be used with caution in patients with a history of penicillin allergy. Patients who have experienced immediate-type (anaphylactic) hypersensitivity reactions to penicillin should avoid using cephalosporins. Prescribing cefuroxime axetil without a confirmed or highly suspected bacterial infection or indication for prophylactic use is unlikely to benefit the patient and may instead increase the risk of developing drug-resistant bacteria. For more complete data on cefuroxime axetil (18 in total), please visit the HSDB records page.

C20H22N4O10S

510.47448

510.105

C, 47.06; H, 4.34; N, 10.98; O, 31.34; S, 6.28

64544-07-6

Cefuroxime sodium;56238-63-2

6321416

White to almost white crystalline powder
White powder

1.6±0.1 g/cm3

1.665

0.85

2

12

12

35

968

2

CC(OC(OC(C1=C(CS[C@@H]2[C@H](NC(/C(/C3=CC=CO3)=N\OC)=O)C(N12)=O)COC(N)=O)=O)C)=O

KEJCWVGMRLCZQQ-YJBYXUATSA-N

InChI=1S/C20H22N4O10S/c1-9(25)33-10(2)34-19(28)15-11(7-32-20(21)29)8-35-18-14(17(27)24(15)18)22-16(26)13(23-30-3)12-5-4-6-31-12/h4-6,10,14,18H,7-8H2,1-3H3,(H2,21,29)(H,22,26)/b23-13-/t10?,14-,18-/m1/s1

1-acetyloxyethyl (6R,7R)-3-(carbamoyloxymethyl)-7-[[(2Z)-2-(furan-2-yl)-2-methoxyiminoacetyl]amino]-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylate

Cefuroxime axetil; SN 407; DRG-0157; CXM-AX

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Note: This product requires protection from light (avoid light exposure) during transportation and storage.

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

DMSO : ~125 mg/mL (~244.87 mM)

Solubility in Formulation 1: ≥ 2.08 mg/mL (4.07 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 20.8 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: ≥ 2.08 mg/mL (4.07 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 20.8 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: ≥ 2.08 mg/mL (4.07 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 20.8 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.)