Carfecillin: Antibacterial Activity in vitro and in vivo
| Autor: | K.R. Comber, G.H. Valler, R. Sutherland, M.J. Basker |
|---|---|
| Rok vydání: | 1977 |
| Předmět: |
Pharmacology
Serial dilution Chemistry General Medicine biochemical phenomena metabolism and nutrition Carbenicillin In vitro carbohydrates (lipids) Hydrolysis Infectious Diseases Oncology Biochemistry In vivo Oral administration Carfecillin Drug Discovery polycyclic compounds medicine bacteria heterocyclic compounds Pharmacology (medical) Antibacterial activity medicine.drug |
| Zdroj: | Chemotherapy. 23:424-435 |
| ISSN: | 1421-9794 0009-3157 |
| DOI: | 10.1159/000222012 |
| Popis: | Carfecillin, the α-phenyl ester of carbenicillin, hydrolyses rapidly in the presence of serum or body tissues to liberate carbenicillin but hydrolysis is less rapid in aqueous solution. The activity of carfecillin in antibacterial tests in vitro depends upon the extent of hydrolysis to carbenicillin, and in conventional serial dilution tests carfecillin shows an antibacterial spectrum generally similar to that of carbenicillin due to extensive hydrolysis. However, in tests in which the extent of hydrolysis is reduced, carfecillin displays lesser activity than carbenicillin against gram-negative bacilli and greater activity against gram-positive cocci. In the presence of serum carfecillin is hydrolysed rapidly to carbenicillin and the activity shown is solely that of carbenicillin. Unlike carbenicillin, carfecillin is well absorbed in mice after oral administration, producing significant carbenicillin blood concentrations and the compound is as effective by the oral route in the treatment of various experimental mouse infections as is parenteral carbenicillin. |
| Databáze: | OpenAIRE |
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