Active Pharmaceutical Ingredients

Cefuroxime Axetil is a second-generation cephalosporin antibiotic. It is the acetoxyethyl ester of cefuroxime. It can inhibit several Gram-positive and Gram-negative organisms. It is suitable for the treatment of infections caused by sensitive strains.

Molecular Formula:C20H22N4O10S

Molecular Weight: 510.474

CAS No.: 64544-07-6

Description

Cefuroxime Axetil is a white or almost white powder with slight odor and bitter taste. It is easily soluble in dioxane, more easily soluble in methanol, slightly soluble in ethanol, very slightly soluble in ether and almost insoluble in water.

Application

Cefuroxime Axetil is a second-generation cephalosporin antibiotic. It is the acetoxyethyl ester of cefuroxime. It can inhibit several Gram-positive and Gram-negative organisms. It is suitable for the treatment of infections caused by sensitive strains.

1. Respiratory tract infection: acute pharyngitis or tonsillitis, maxillary sinusitis, acute exacerbation of chronic bronchitis, acute bronchitis.

2. Otolaryngology infections: acute otitis media, acute pharyngitis, tonsillitis.

3. Urinary tract infection: simple urinary tract infection, uncomplicated Neisseria gonorrhoea urethritis.

4. Skin and soft tissue infections.

5. Other infections: cervicitis, impetigo.

Packing

20Kg per drum

Storage：

Preserve in tight containers in a dry place.

Shelf Life :

36 months from date of production when stored in good condition.

Minimum Order

One package

Cefuroxime Axetil Introduction

Item	Details
Generic Name	Cefuroxime Axetil
Trade Names	Ceftin (西力欣), Zinnat 等
Classification	Second – generation cephalosporin antibiotic
Chemical Structure	The chemical name is (6R,7R)-7-(2 – furyl(methoxyimino)acetamido)-3 – aminocarbonyloxymethyl – 8 – oxo – 5 – thia – 1 – azabicyclo(4.2.0)oct – 2 – ene – 2 – carboxylic acid, (1RS)-1 – acetoxyethyl ester. Its molecular formula is C₂₀H₂₂N₄O₁₀S, with a molecular weight of 510. It contains a beta – lactam ring as the core structure for antibacterial activity, and the axetil moiety improves its oral absorption.
Pharmacological Action	Cefuroxime axetil is a prodrug of cefuroxime. After oral administration, it is hydrolyzed by esterases in the intestinal mucosa and blood to release cefuroxime, which then exerts antibacterial effects. Cefuroxime binds to penicillin – binding proteins (PBPs) in bacteria, inhibiting the cross – linking of peptidoglycan chains in the cell wall. This leads to weakened cell walls, causing bacteria to be more susceptible to osmotic pressure and ultimately resulting in cell lysis and death. It has a broad antibacterial spectrum, being effective against both Gram – positive and Gram – negative bacteria, and shows good stability against some β – lactamases.
Clinical Applications	1. Respiratory Tract Infections: – Pharyngitis and tonsillitis caused by Streptococcus pyogenes. – Acute otitis media due to Streptococcus pneumoniae (penicillin – sensitive strains), Haemophilus influenzae (including β – lactamase – producing strains), and Moraxella catarrhalis (including β – lactamase – producing strains). – Acute bacterial sinusitis caused by Streptococcus pneumoniae and Haemophilus influenzae (non – β – lactamase – producing strains). – Community – acquired pneumonia caused by Streptococcus pneumoniae (penicillin – sensitive strains) and Haemophilus influenzae (including β – lactamase – producing strains). – Acute bacterial exacerbation of chronic bronchitis due to Streptococcus pneumoniae (penicillin – sensitive strains), Haemophilus influenzae (including β – lactamase – producing strains), and Haemophilus parainfluenzae (including β – lactamase – producing strains). 2. Skin and Soft Tissue Infections: Such as those caused by methicillin – sensitive Staphylococcus aureus and Streptococcus pyogenes. 3. Urinary Tract Infections: Acute simple cystitis caused by Escherichia coli or Klebsiella pneumoniae. 4. Gonorrhea: Acute simple gonococcal urethritis, cervicitis, and anorectal infections caused by Neisseria gonorrhoeae (both penicillin – producing and non – penicillin – producing strains).
Dosage and Administration	Adults: – Routine oral dose: 250 mg twice daily. – For lower respiratory tract infections: 500 mg twice daily. – For simple lower urinary tract infections: 125 mg twice daily. – For simple gonorrhea and Neisseria gonorrhoeae urethritis: a single oral dose of 1000 mg. Children: – Routine use (children under 5 years old are not suitable for taking tablets and should use the suspension): – 3 months – 2 years old: 10 mg/kg per dose (maximum 250 mg), twice daily. – 2 – 12 years old: 15 mg/kg per dose (maximum 250 mg), twice daily. – 12 – 18 years old: 250 mg twice daily. – For acute pharyngitis or acute tonsillitis in 3 months – 12 – year – old children: 10 mg/kg per dose, twice daily (maximum 500 mg per day). – For acute otitis media and impetigo: 15 mg/kg per dose, twice daily (maximum not exceeding 1000 mg per day). – For severe lower respiratory tract infections: 500 mg twice daily. – The dose for lower urinary tract infections is halved, 125 mg twice daily. It is usually taken orally. Food can promote its absorption, and it can be taken with or without food.
Adverse Reactions	1. Gastrointestinal Effects: Nausea, vomiting, diarrhea, and loose stools are relatively common, with an incidence of 3.0% – 3.7%. 2. Allergic Reactions: Similar to other cephalosporins, it may cause allergic reactions such as polymorphic erythema, Stevens – Johnson syndrome, toxic epidermal necrolysis, and severe anaphylactoid reactions, although these are rare. 3. Reproductive System: Vaginitis may occur, with an incidence of 0.1% – 5.4%. 4. Digestive System: Pseudomembranous colitis may occur occasionally. 5. Hematological Effects: Eosinophilia may occur in 1.1% of patients. 6. Hepatic and Biliary System: Transient elevation of serum aminotransferases may occur in 1.0% – 1.6% of patients. 7. Others: Drinking alcohol after using cefuroxime axetil can lead to a disulfiram – like reaction. In rare cases, frequent premature ventricular contractions may occur.
Drug Interactions	1. With Probenecid: Co – administration with probenecid can increase the AUC of cefuroxime axetil by about 50%. 2. With Antacids: Concurrent use with antacids can reduce its absorption. 3. With Loop Diuretics: Patients taking loop diuretics simultaneously with cefuroxime axetil should monitor renal function. 4. With Oral Contraceptives: Similar to other antibiotics, it may affect the intestinal flora, reducing the reabsorption of estrogen and thus reducing the efficacy of combined oral contraceptives. 5. Blood Cross – matching: Cefuroxime axetil may interfere with blood cross – matching tests. 6. With Chloramphenicol: When using cefuroxime axetil and chloramphenicol together, the possibility of antagonism should be considered. 7. Compatibility: It has compatibility issues with drugs such as amikacin sulfate, gentamicin, kanamycin, tobramycin, neomycin, chlortetracycline hydrochloride, tetracycline hydrochloride, oxytetracycline hydrochloride, colistimethate sodium, polymyxin sulfate, erythromycin gluconate, erythromycin lactate, lincomycin, sulfisoxazole, aminophylline, soluble barbiturates, calcium chloride, calcium gluconate, diphenhydramine hydrochloride, and other anti – histamines, lidocaine, norepinephrine, metaraminol, methylphenidate, and succinylcholine. It may also have compatibility issues with penicillin, methicillin, hydrocortisone succinate, phenytoin sodium, prochlorperazine, vitamins B and C, and hydrolyzed proteins.
Special Population Considerations	1. Children: Administration in children under 3 months old is not recommended. Children under 5 years old are more suitable to use the suspension. 2. Pregnant Women: Should be used with caution. According to the US FDA pregnancy drug safety classification, it is category B for oral and injection use. 3. Breastfeeding Women: Should be used with caution. If used, breastfeeding should be stopped. 4. Patients with Liver or Kidney Impairment: Should be used with caution. 5. Patients with Gastrointestinal Diseases: Especially patients with colitis should use this drug with caution.
History and Development	Developed by GlaxoSmithKline, it was first launched in the UK in 1987 and then approved by the US FDA in 1988. Due to its effectiveness, convenient use, broad antibacterial spectrum, low renal toxicity, strong permeability, and high stability against β – lactamases, it is widely used clinically to treat various infections caused by sensitive bacteria. It has been included in the list of 289 generic drugs in China that need to complete the evaluation of quality and efficacy consistency by the end of 2018.

 

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