Cefuroxime

Cefuroxime
ATC Code J01DC02, S01AA27
Formula C16H16N4O8S
Molar Mass (g·mol−1) 424,39
Physical State solid
Melting Point (°C) 218-225
PKS Value 2,5
CAS Number C16H16N4O8S
PUB Number 5479529
Drugbank ID DB01112
Solubility moderate in water / poor in ethanol

Basics

Cefuroxime is a bactericidal antibiotic from the group of β-lactams. Within this group, it belongs to the 2nd generation cephalosporins. It is effective against Gram-positive and Gram-negative bacteria and is characterised by its cerebrospinal fluid (CSF) penetrability. It is therefore used in the treatment of meningitis and in the treatment of infections of the kidneys, respiratory tract and skin. It is used either as an infusion or as a tablet. Cefuroxime is available only on prescription.

Pharmacology

Pharmacodynamics

Cefuroxime is a beta-lactam antibiotic. Its action is based on the inhibition of cell wall synthesis of bacteria. By binding to specific penicillin-binding proteins (PBPs) located within the bacterial cell wall, the third and final stage of bacterial cell wall synthesis is inhibited. As a result, cross-links important for stability can no longer be formed and the pathogen's cell wall disintegrates. Cell lysis is then mediated by autolytic enzymes of the bacterial cell wall such as autolysins; It is possible that cefuroxime interferes with an autolysin inhibitor.

Pharmacokinetics

Cefuroxime is absorbed from the gastrointestinal tract. Absorption is greater when cefuroxime is taken after meals (absolute bioavailability increases from 37% to 52%). Protein binding is 50%. Half-life is approximately 80 minutes after intramuscular or intravenous injection.

Drug Interactions

  • Medications used to reduce gastric acidity may affect the bioavailability of cefuroxime. The beneficial effect of a meal on absorption of the drug may also be reversed.
  • Cefuroxime affects the intestinal flora. Therefore, other drugs such as estrogens may be less readily absorbed and oral contraceptives may have a decreased effect. Similarly, there may be an increase in the International Normalized Ratio (INR) if oral blood thinners (anticoagulants) are given concomitantly with the antibiotic.
  • When the agent is co-prescribed with probenecid, the maximum concentration of cefuroxime may increase significantly and the elimination half-life may be prolonged. Therefore, concomitant medication with the two agents is not recommended. The drug should also not be combined with other antibiotics such as tetracyclines, erythromycin, chloramphenicol, or sulfonamides because antagonistic and synergistic effects may occur with aminoglycosides.
  • Since cefuroxime is excreted almost unchanged by the kidneys, renal function should be regularly checked and monitored if patients are taking parallel loop diuretics such as furosemide or etacrynic acid or potentially kidney-damaging drugs such as aminoglycoside antibiotics, polymyxin B and colistin are combined with the active substance. This also applies to elderly patients with impaired renal function.

Toxicity

Side effects

  • Promoted growth of Candida
  • Eosinophilia
  • Headache
  • Dizziness
  • diarrhea, nausea, abdominal pain
  • transient increase in liver enzymes.
Markus Falkenstätter

Markus Falkenstätter
Author

Markus Falkenstätter ist Autor zu pharmazeutischen Themen in der Medizin-Redaktion von Medikamio. Er befindet sich im letzten Semester seines Pharmaziestudiums an der Universität Wien und liebt das wissenschaftliche Arbeiten im Bereich der Naturwissenschaften.

Mag. pharm Stefanie Lehenauer

Mag. pharm Stefanie Lehenauer
Lector

Stefanie Lehenauer ist seit 2020 freie Autorin bei Medikamio und studierte Pharmazie an der Universität Wien. Sie arbeitet als Apothekerin in Wien und ihre Leidenschaft sind pflanzliche Arzneimittel und deren Wirkung.

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