Antimicrobial activity
A semisynthetic acylureidopenicillin supplied as the sodium salt for parenteral administration.
Ampicillin-susceptible strains of H. influenzae and Neisseria spp. are very susceptible, but β-lactamase-producing organisms are usually resistant. It is less active than azlocillin and piperacillin against Ps. aeruginosa and has variable activity against B. fragilis, independent of β-lactamase production. It exhibits typical β-lactam synergy with aminoglycosides against Ps. aeruginosa and enterobacteria.
It attains peak concentrations of 250 mg/L after a 2 g intravenous infusion, with a plasma half-life of 55 min. Protein binding is 20–30%. It distributes into multiple tissues and human body fluids at therapeutically useful concentrations. Up to 60% of the dose is recoverable unchanged from the urine, with up to 2.5% excreted in the bile.
Toxicity and side effects are similar to those associated with carboxypenicillins. Its clinical use is for serious infections with susceptible organisms, including lower respiratory tract, intra-abdominal, urinary tract and gynecological infections. Commercial availability is quite limited.