Ceftiolene

General

  • Type: 3rd generation Cephalosporin
  • Dosage Forms: powder for injection
  • Dosage Strengths: 500mg, 1g
  • Routes of Administration: IV, IM
  • Common Trade Names: Lanocef (Investigational/International)

Adult Dosing

General

  • Standard: 1g IM/IV q12h
  • Severe: 2g IM/IV q8-12h
  • Max: 4-6g/day

Pneumonia / Lower Respiratory Tract Infection

  • 1g IM/IV q12h

UTI, Complicated and Uncomplicated

  • 0.5-1g IM/IV q12h

Sepsis

  • 2g IV q8h

Pediatric Dosing

General

  • Safety and efficacy in children have not been fully established.
  • Based on class: 50–100 mg/kg/day IM/IV divided q12h
  • Max: 2g/day

Special Populations

  • Pregnancy: Category B (Presumed based on class; specific data limited)
  • Lactation: Excreted in breast milk; use with caution
  • Renal
    • Adult
      • CrCl 30-50: 1g q12h
      • CrCl 10-29: 0.5-1g q24h
      • CrCl <10: 0.5g q24h
      • Hemodialysis: Administer dose after dialysis
    • Pediatric
      • Not defined; adjust based on adult GFR principles
  • Hepatic
    • No adjustment necessary

Contraindications

  • Allergy to class/drug (Cephalosporins)
  • History of anaphylaxis to Penicillin

Adverse Reactions

Serious

Common

Pharmacology

  • Half-life: 1.3 - 1.5h
  • Metabolism: Minimally metabolized
  • Excretion: Urine (high recovery rates) & Bile
  • Mechanism of Action: Bactericidal; inhibits cell wall mucopeptide synthesis.
  • Spectrum: Broad gram-negative coverage characteristic of 3rd generation; weaker gram-positive coverage than 1st generation.

Antibiotic Sensitivities[1]

Group Organism Sensitivity
Gram Positive Strep. Group A, B, C, G S
Strep. Pneumoniae S
Viridans strep S
Strep. anginosus gp X1
Enterococcus faecalis R
Enterococcus faecium R
MSSA S
MRSA R
CA-MRSA R
Staph. Epidermidis I
C. jeikeium R
L. monocytogenes R
Gram Negatives N. gonorrhoeae S
N. meningitidis S
Moraxella catarrhalis S
H. influenzae S
E. coli S
Klebsiella sp S
E. coli/Klebsiella ESBL+ R
E coli/Klebsiella KPC+ R
Enterobacter sp, AmpC neg I
Enterobacter sp, AmpC pos R
Serratia sp I
Serratia marcescens I
Salmonella sp S
Shigella sp S
Proteus mirabilis S
Proteus vulgaris S
Providencia sp. S
Morganella sp. S
Citrobacter freundii I
Citrobacter diversus S
Citrobacter sp. I
Aeromonas sp S
Acinetobacter sp. R
Pseudomonas aeruginosa R
Burkholderia cepacia R
Stenotrophomonas maltophilia R
Yersinia enterocolitica S
Francisella tularensis X1
Brucella sp. X1
Legionella sp. R
Pasteurella multocida S
Haemophilus ducreyi X1
Vibrio vulnificus X1
Misc Chlamydophila sp R
Mycoplasm pneumoniae R
Rickettsia sp X1
Mycobacterium avium X1
Anaerobes Actinomyces X1
Bacteroides fragilis R
Prevotella melaninogenica I
Clostridium difficile X1
Clostridium (not difficile) I
Fusobacterium necrophorum S
Peptostreptococcus sp. S

Key

  • S susceptible/sensitive (usually)
  • I intermediate (variably susceptible/resistant)
  • R resistant (or not effective clinically)
  • S+ synergistic with cell wall antibiotics
  • U sensitive for UTI only (non systemic infection)
  • X1 no data
  • X2 active in vitro, but not used clinically
  • X3 active in vitro, but not clinically effective for Group A strep pharyngitis or infections due to E. faecalis
  • X4 active in vitro, but not clinically effective for strep pneumonia

See Also

References

  1. Antimicrob Agents Chemother 1983; 23(1):9-14