Сулопенем

Описание

Sulopenem is a parenteral penem that demonstrates high activity against Gram-positive, Gram-negative, and anaerobic bacteria. Since it is stable in relation to renal dehydropeptidase I, it does not require concomitant administration of an inhibitor of this enzyme.

Использование

Sulopenem is a β-Lactamase inhibitor which is used in treatment of microbial infections. It is an important reagent for many drugs synthesized against bacterial infections.

Механизм действия

Sulopenem is one of the penems and, as such, interacts with penicillin-binding proteins (PBPs). From in vitro studies, sulopenem has shown a high affinity for PBP1a, 1b, 2, and 3 in E. coli.

Фармакокине?тика

When 1 g of CP-65,207 [containing 46.3% of S-isomer (sulopenem) and 53.7% of R-isomer] was administered by 10-minute intravenous infusions, the peak concentration of sulopenem in serum was 36.0 mg/ ml, its half-life was 52.8 minutes, and the area under the serum concentration-versus-time curve (AUC) from 0 to 8 hours was 21.0 mg/ml per hour.