Cefuroxime axetil is the 1-acetoxyethyl ester of cefuroxime. The axetil salt renders the molecule more lipophilic, thus allowing enhanced oral absorption. Once cefuroxime axetil reaches the intestinal mucosa and portal blood flow it rapidly undergoes de-esterification to yield the active parent compound cefuroxime.
Cefuroxime axetil is a broad spectrum betalactam antibiotic. It has many approved indications, however, it is considered a second-line alternative. It is not the drug of choice for any infection, particularly those encountered in the field of obstetrics and gynecology. It is safe to use in pregnancy and has a low adverse effect profile, but due to its excessive acquisition cost and better therapeutic alternatives, it should be reserved for select cases.
Mechanism of action
Cefuroxime axetil is a second-generation cephalosporin that contains the classic [3-1actam ring structure. Bactericidal activity in vivo is resultant of its binding to essential target proteins, termed the penicillin-binding proteins, which are located in the bacterial cell wall. Inhibition of these proteins leads to bacterial cell wall elongation and leakage, thus the bacteria are unable to divide and mature.
– Upper respiratory tract infections for example, ear, nose and throat infections, such as otitis media, sinusitis, tonsillitis and pharyngitis
– Lower respiratory tract infections for example, pneumonia, acute bronchitis, and acute exacerbations of chronic bronchitis
– Genito-urinary tract infections for example, pyelonephritis, cystitis and urethritis
– Skin and soft tissue infections for example, furunculosis, pyoderma and impetigo
– Gonorrhoea, acute uncomplicated gonococcal urethritis, and cervicitis.
– Treatment of early Lyme disease and subsequent prevention of late Lyme disease in adults and children over 12 years old.
Cefuroxime is also available as the sodium salt (Zinacef®) for parenteral administration. This permits the use of sequential therapy with the same antibiotic, when a change from parenteral to oral therapy is clinically indicated.
Where appropriate Cefuroxime (as axetil) (Zinnat®) is effective when used following initial parenteral cefuroxime sodium (Zinacef®) in the treatment of pneumonia and acute exacerbations of chronic bronchitis.
Pregnancy and lactation
There is no experimental evidence of embryopathic or teratogenic effects attributable to cefuroxime axetil but, as with all drugs, it should be administered with caution during the early months of pregnancy.
Cefuroxime is excreted in human milk, and consequently caution should be exercised when cefuroxime axetil is administered to a nursing mother. Available dosage form in the hospital: 750MG TAB, 500MG CAP, 125MG/5ML SUSP, 250MG TAB, 250MG/5ML SUSP. 1.5G VIAL, 750MG VIAL.
Bronchitis, acute (and exacerbations of chronic bronchitis): -Oral: 250-500 mg every 12 hours for 10 days -I.V.: 500-750 mg every 8 hours (complete therapy with oral dosing)
Cellulitis, orbital: I.V.: 1.5 g every 8 hours -Cholecystitis, mild-to-moderate: I.V.: 1.5 g every 8 hours for 4-7 days (provided source controlled)
Gonorrhea: -Disseminated: I.M., I.V.: 750 mg every 8 hours -Uncomplicated: -Oral: 1 g as a single dose -I.M.: 1.5g as single dose (administer in two different sites with probenecid) Intra-abdominal infection, complicated, community-acquired, mild-to-moderate (in combination with metronidazole): I.V.: 1.5 g every 8 hours for 4-7 days (provided source controlled)
Lyme disease (early): Oral: 500 mg twice daily for 20 days
Pharyngitis/tonsillitis and sinusitis: Oral: 250 mg twice daily for 10 days
Skin/skin structure infection, uncomplicated: -Oral: 250-500 mg every 12 hours for 10 days
Side effects and interactions
Cefuroxime axetil is associated with a low incidence of adverse effects and is generally well tolerated. The most frequently reported adverse effects are primarily gastrointestinal in nature, including diarrhea/loose stools (3.7%), nausea (2.6%), and vomiting (2.6%). Of those who discontinued treatment, 85% did so because of gastrointestinal complaints.
Other occasionally reported adverse events associated with cefuroxime axetil include antibiotic associated colitis and liver function abnormalities.
Hypersensitivity reactions including Stevens-Johnson syndrome, erythema multiforme, and toxic epidermal necrolysis have been reported rarely during post-marketing surveillance.
Concurrent use of cefuroxime with probenecid may increase the serum concentration of cefuroxime.
Use with warfarin may increase the hypoprothrombotic effect of the anticoagulant; therefore, closer monitoring of the patient’s international normalized ratio during cefuroxime therapy is recommended.