In vitro and in vivo evaluation of benzamidomethyl-benzylpenicillinate (FI7303). A new 'repository' form.
A new type of hydrolyzable ester of penicillin G, benzamidomethyl benzylpenicillinate (FI 7303), was studied for the antibacterial activity and kinetics of absorption in comparison with DBED-penicillin G. FI 7303 resulted to be a good repository form of penicillin G, slowly eliminated in mouse, dog and man. It exerted a remarkable therapeutic activity in mice infected with Staphylococcus aureus even when administered 26 h before infection. The protective effect in mice was more prolonged than that of DBED-penicillin G, in agreement with the longer persistence of significant blood levels.
D000042:Absorption; D000818:Animals; D001419:Bacteria / Q000187:drug effects*; D004285:Dogs; D004353:Drug Evaluation, Preclinical; D006801:Humans; D051379:Mice; D010400:Penicillin G / Q000031:analogs & derivatives* / Q000378:metabolism / Q000494:pharmacology / Q000627:therapeutic use; D010401:Penicillin G Benzathine / Q000378:metabolism / Q000494:pharmacology / Q000627:therapeutic use; D010403:Penicillin Resistance; D013203:Staphylococcal Infections / Q000188:drug therapy*; D013211:Staphylococcus aureus
C017804:benzamidomethyl benzylpenicillinate; D010400:Penicillin G; D010401:Penicillin G Benzathine