Ceftobiprole

General

• Type: 5th generation Cephalosporin
• Dosage Forms: powder for reconstitution
• Dosage Strengths: 500mg (equivalent to 666.6mg ceftobiprole medocaril sodium)
• Routes of Administration: IV
• Common Trade Names: Zevtera, Mabelio

Adult Dosing

General

• Administer as a 2-hour prolonged intravenous infusion
• Standard: 500mg IV q8h
• Max: 1500mg/day

Staphylococcus aureus Bacteremia (SAB)

• 500mg IV q8h x 14-42 days (depending on source/complications)

Acute Bacterial Skin and Skin Structure Infections (ABSSSI)

• 500mg IV q8h x 5-14 days

Community Acquired Pneumonia (CABP)

• 500mg IV q8h x 5-14 days

Hospital Acquired Pneumonia (HAP)

• 500mg IV q8h x 7-14 days (Excluding VAP)

Pediatric Dosing

General (3 months to <18 years)

• Administer as a 2-hour prolonged intravenous infusion
• Adolescents (12 to <18 years): 500mg IV q8h
• Children (6 to <12 years): 15mg/kg IV q8h
• Infants/Children (3 months to <6 years): 20mg/kg IV q8h
• Max: 500mg/dose

Special Populations

• Pregnancy: Safety not established; studies in animals showed no harm. Use if benefit outweighs risk.
• Lactation: Unknown excretion; use with caution.
• Renal
  • Adult
    • CrCl 30-50: 500mg q12h
    • CrCl 15-29: 250mg q12h
    • CrCl <15 (ESRD) or intermittent hemodialysis: 250mg q24h
    • NOTE: Dosing for patients receiving hemodialysis should be administered after the dialysis session.
  • Pediatric
    • Renal impairment requires adjustment based on adult principles but specific pediatric nomograms should be consulted.
• Hepatic
  • No adjustment necessary

Contraindications

• Severe hypersensitivity to Ceftobiprole or other Cephalosporins
• History of severe anaphylaxis to other Beta-lactams

Adverse Reactions

Serious

• Anaphylaxis
• Clostridium difficile associated diarrhea
• Seizures (risk increases in renal impairment without adjustment)
• Hyponatremia

Common

• Dysgeusia (Metallic taste)
• Nausea and Vomiting
• Diarrhea
• Headache
• Infusion site reactions
• Hepatic enzyme elevation

Pharmacology

• Half-life: 3h
• Metabolism: Converted rapidly from prodrug (ceftobiprole medocaril) to active drug in plasma by type A esterases; minimal hepatic metabolism.
• Excretion: Urine (89% unchanged)
• Mechanism of Action: Bactericidal; inhibits cell wall mucopeptide synthesis.
  • High affinity for PBP2a (confers activity against MRSA).
  • High affinity for PBP2x (confers activity against Penicillin-Resistant Strep. Pneumoniae).

Antibiotic Sensitivities

Group	Organism	Sensitivity
Gram Positive	Strep. Group A, B, C, G	S
	Strep. Pneumoniae	S
	Viridans strep	S
	Strep. anginosus gp	S
	Enterococcus faecalis	S
	Enterococcus faecium	R
	MSSA	S
	MRSA	S
	CA-MRSA	S
	Staph. Epidermidis	S (Including MRSE)
	C. jeikeium	I
	L. monocytogenes	I
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	S
	Enterobacter sp, AmpC pos	S
	Serratia sp	S
	Serratia marcescens	S
	Salmonella sp	S
	Shigella sp	S
	Proteus mirabilis	S
	Proteus vulgaris	S
	Providencia sp.	S
	Morganella sp.	S
	Citrobacter freundii	S
	Citrobacter diversus	S
	Citrobacter sp.	S
	Aeromonas sp	S
	Acinetobacter sp.	I
	Pseudomonas aeruginosa	S
	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	R
	Mycobacterium avium	R
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

• Antibiotics (Main)