Second-Generation Cephalosporin (true 2nd generation cephalosporin)
Staphylococcus aureus (methicillin susceptible), Coagulase negative Staphylococci, Streptococcus pneumoniae (penicillin susceptible), Streptococcus spp. Haemophilus influenzae, Moraxella catarrhalis, Neisseria meningitides, Neisseria gonorrhoeae, E. coli
Cephalosporins exert bactericidal activity by interfering with bacterial cell wall synthesis and inhibiting cross-linking of the peptidoglycan. The cephalosporins are also thought to play a role in the activation of bacterical cell autolysins which may contribute to bacterial cell lysis.
Cephalosporins exhibit time-dependent killing (T > MIC)
Dose of 1g: Cmax: 139 mcg/L; Protein binding: 70%; Half-life: 0.8 hours; Table 10
Hypersensitivity: Maculopapular rash, Urticaria, Pruritis, Anaphylaxis/angioedema, eosinophilia
Hematologic: Neutropenia, Leukopenia, Thrombocytopenia
GI: Diarrhea, C. difficile disease
Renal: Interstitial nephritis
IV/IM: Powder for reconstitution: 1g, 2g, 10g
Dosing in adults:
Bone/joint infection: 500mg-1g IV/IM q4-8h
Skin and/or subcutaneous tissue infection: 500mg IV/IM q6h
Peritonitis: 500mg-1g IV/IM q4-8h
Uncomplicated UTI: 500mg IV/IM q8h
Dosing in pediatrics:
50-150mg/kg/day IV q4-8h
Disease state based dosing:
Renal failure: CrCl > 80mL/min Standard dose
CrCl 50-80mL/min 1.5g q4h OR 2g q6h
CrCl 25-50mL/min 1.5g q6h OR 2g q8h
CrCl 10-25mL/min 1g q6h OR 1.25g q8h
CrCl 2-10mL/min 1g q12h
Hepatic failure: No dosing changes recommended at this time.
Precautions: hypersensitivity to penicillins, history of gastrointestinal disease, particularly colitis, renal impairment
Heparin - increased risk of bleeding
Live Typhoid Vaccine - decreased immunological response to the typhoid vaccine
Warfarin – increased risk of bleeding
Category B: No evidence of risk in humans but studies inadequate.
Therapeutic: Culture and sensitivities, serum levels, signs and symptoms of infection, white blood cell count
Toxic: Urinalysis, BUN, SCr, AST and ALT, skin rash, Neutropenia and leukopenia, Prothrombin time in patients with renal or hepatic impairment or poor nutritional state, as well as patients receiving a protracted course of antimicrobial therapy, and patients previously stabilized on anticoagulant therapy.
Mandol̉/Eli Lilly