Unii-p9vxv1408y

Definition

ChEBI: Ceftaroline fosamil acetate monohydrate is a hydrate that is the monohydrate form of ceftaroline fosamil acetate. A prodrug for ceftaroline, used for the treatment of adults with acute bacterial skin and skin structure infections. It has a role as an antimicrobial agent, an antibacterial drug and a prodrug. It contains a ceftaroline fosamil acetate.

Antimicrobial activity

A semisynthetic cephalosporin formulated as the water-soluble fosamil acetate prodrug for intravenous administration. Its properties are similar to those of ceftobiprole, with which it shares an enhanced affinity for penicillin-binding protein 2′ (2a) of methicillin-resistant Staph. aureus. It is hydrolyzed by extended-spectrum β-lactamases and is not active against Amp-C derepressed strains of Gram-negative bacilli.

Pharmacokinetics

C_{max 600 mg intravenous (1-h infusion): 19 mg/L end infusion
Plasma half-life: 2.6 h
Volume of distribution: 0.37 L/kg
Plasma protein binding :<20%
Like ceftobiprole, ceftaroline fosamil is rapidly hydrolyzed in plasma after intravenous infusion and excreted principally in urine. In preliminary clinical studies it appears to be well tolerated.}