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ANTIINFECTIVES FOR SYSTEMIC USE › ANTIBACTERIALS FOR SYSTEMIC USE › OTHER BETA-LACTAM ANTIBACTERIALS › Third-generation cephalosporins
cefotaxime and beta-lactamase inhibitor
J01DD51
Forms & Strengths
- Powder for injection: 1 g cefotaxime with 0.5 g beta-lactamase inhibitor (e.g., clavulanic acid or sulbactam)
- Powder for injection: 2 g cefotaxime with 1 g beta-lactamase inhibitor
- Intravenous and intramuscular preparation
Adult Dosing
- Severe infections: 1 g to 2 g of cefotaxime component every 8 hours IV or IM
- Life-threatening infections: Up to 2 g every 4 to 6 hours IV
- Maximum daily dose: Up to 12 g of the cefotaxime component per day in divided doses
- Renal impairment adjustment: Reduce dose by 50% or extend dosing interval if creatinine clearance is < 20 mL/min
Pediatric Dosing
- Neonates (0-7 days): 50 mg/kg (cefotaxime component) every 12 hours IV
- Neonates (8-28 days): 50 mg/kg (cefotaxime component) every 8 hours IV
- Infants and children (1 month to 12 years): 100 to 200 mg/kg/day divided every 6 to 8 hours IV or IM
- Maximum pediatric dose: 12 g per day
Indications
- Empiric treatment of severe polymicrobial intra-abdominal infections
- Complicated urinary tract infections and pyelonephritis caused by beta-lactamase producing strains
- Lower respiratory tract infections including hospital-acquired and community-acquired pneumonia
- Skin and soft tissue infections
- Septicemia and bacteremia
Mechanism of Action
- Cefotaxime is a third-generation cephalosporin that inhibits bacterial cell wall synthesis by binding to penicillin-binding proteins (PBPs)
- Beta-lactamase inhibitor component irreversibly binds to and inactivates plasmid- and chromosomally-mediated beta-lactamases
- Combination protects cefotaxime from degradation and expands spectrum of activity against resistant Gram-negative and anaerobic pathogens
Contraindications
- Known hypersensitivity to cefotaxime, other cephalosporins, or beta-lactamase inhibitors
- History of severe immediate hypersensitivity reaction (e.g., anaphylaxis) to penicillins or other beta-lactam antibiotics
Adverse Reactions
- Injection site reactions: Pain, inflammation, phlebitis at the IV/IM site
- Gastrointestinal: Diarrhea, pseudomembranous colitis, nausea, vomiting
- Hypersensitivity: Rash, pruritus, urticaria, fever, drug fever, rare cases of anaphylaxis and Stevens-Johnson syndrome
- Hematologic: Transient leukopenia, neutropenia, thrombocytopenia, eosinophilia, positive direct Coombs test
- Hepatic: Transient elevations in AST, ALT, and alkaline phosphatase
- Renal: Interstitial nephritis, transient increases in BUN and serum creatinine
Drug Interactions
- Probenecid: Competitively inhibits renal tubular secretion of cefotaxime, leading to higher and more prolonged serum concentrations
- Aminoglycosides: Co-administration may increase the risk of nephrotoxicity
- Loop diuretics: May increase the risk of nephrotoxicity when given concurrently with cephalosporins
- Anticoagulants: May enhance the anticoagulant effect of vitamin K antagonists (e.g., warfarin) by altering gut flora and reducing vitamin K synthesis
Curated Content: Needs Vetting Before Put to Clinical Use