Abstract
Bacampicillin, a new oral prodrug which in vivo is rapidly transformed to ampicillin, was compared with ampicillin, pivampicillin, and amoxycillin in a randomized cross-over study on 11 healthy volunteers. All drugs were given in oral doses equimolar to 400 mg of bacampicillin (800 μmol). The mean of the individual peak concentrations in serum was 8.3 μg/ml for bacampicillin, 7.1 μg/ml for pivampicillin, 7.7 μg/ml for amoxycillin, and 3.7 μg/ml for ampicillin. Furthermore, bacampicillin had a higher absorption rate than all the other drugs, although there were statistically significant differences only versus ampicillin. The peak serum levels of the individual subjects were more dispersed with ampicillin and amoxycillin, suggesting a more uniform absorption of bacampicillin and pivampicillin. The relative bioavailability of bacampicillin and pivampicillin was comparable, whereas ampicillin was only 2/3 that of the others.
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- Barza M., Weinstein L. Penetration of antibiotics into fibrin loci in vivo. I. Comparison of penetration of ampicillin into fibrin clots, abscesses, and "interstitial fluid". J Infect Dis. 1974 Jan;129(1):59–65. doi: 10.1093/infdis/129.1.59. [DOI] [PubMed] [Google Scholar]
- Barza M., Weinstein L. Pharmacokinetics of the penicillins in man. Clin Pharmacokinet. 1976;1(4):297–308. doi: 10.2165/00003088-197601040-00004. [DOI] [PubMed] [Google Scholar]
- Bodey G. P., Nance J. Amoxicillin: in vitro and pharmacological studies. Antimicrob Agents Chemother. 1972 Apr;1(4):358–362. doi: 10.1128/aac.1.4.358. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Bodin N. O., Ekström B., Forsgren U., Jalar L. P., Magni L., Ramsay C. H., Sjöberg B. Bacampicillin: a new orally well-absorbed derivative of ampicillin. Antimicrob Agents Chemother. 1975 Nov;8(5):518–525. doi: 10.1128/aac.8.5.518. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Clayton J. P., Cole M., Elson S. W., Ferres H. BRL.8988 (talampicillin), a well-absorbed oral form of ampicillin. Antimicrob Agents Chemother. 1974 Jun;5(6):670–671. doi: 10.1128/aac.5.6.670. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Daehne W., Frederiksen E., Gundersen E., Lund F., Morch P., Petersen H. J., Roholt K., Tybring L., Godtfredsen W. O. Acyloxymethyl esters of ampicillin. J Med Chem. 1970 Jul;13(4):607–612. doi: 10.1021/jm00298a005. [DOI] [PubMed] [Google Scholar]
- Hallander H. O., Flodström A., Sjövall J. Pharmacological and clinical study of bacampicillin in acute peritonsillitis--a comparison with ampicillin. Antimicrob Agents Chemother. 1977 Feb;11(2):185–190. doi: 10.1128/aac.11.2.185. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Klastersky J., Daneau D., Swings G., Weerts D. Antibacterial activity in serum and urine as a therapeutic guide in bacterial infections. J Infect Dis. 1974 Feb;129(2):187–193. doi: 10.1093/infdis/129.2.187. [DOI] [PubMed] [Google Scholar]
- Loo J. C., Foltz E. L., Wallick H., Kwan K. C. Pharmacokinetics of pivampicillin and ampicillin in man. Clin Pharmacol Ther. 1974 Jul;16(1):35–43. doi: 10.1002/cpt1974161part135. [DOI] [PubMed] [Google Scholar]
- MacLeod C., Rabin H., Ogilvie R., Ruedy J., Caron M., Zarowny D., Davies R. O. Practical concepts of drug absorption, distribution and loss. Can Med Assoc J. 1974 Aug 17;111(4):341–346. [PMC free article] [PubMed] [Google Scholar]
- Rozencweig M., Staquet M., Klastersky J. Antibacterial activity and pharmacokinetics of bacampicillin and ampicillin. Clin Pharmacol Ther. 1976 May;19(5 Pt 1):592–597. doi: 10.1002/cpt1976195part1592. [DOI] [PubMed] [Google Scholar]
- Shiobara Y., Tachibana A., Sasaki H., Watanabe T., Sado T. Phthalidyl D-alpha-aminobenzylpenicillinate hydrochloride (PC-183), a new orally active ampicillin ester. I. Absorption, excretion and metabolism of PC-183 and ampicillin. J Antibiot (Tokyo) 1974 Sep;27(9):665–673. doi: 10.7164/antibiotics.27.665. [DOI] [PubMed] [Google Scholar]
- WEINSTEIN L., DAIKOS G. K., PERRIN T. S. Studies on the relationship of tissue fluid and blood levels of penicillin. J Lab Clin Med. 1951 Nov;38(5):712–718. [PubMed] [Google Scholar]
- Westlake W. J. Problems associated with analysis of pharmacokinetic models. J Pharm Sci. 1971 Jun;60(6):882–885. doi: 10.1002/jps.2600600616. [DOI] [PubMed] [Google Scholar]
- Williams J. D., Andrews J. Sensitivity of Haemophilus influenzae to antibiotics. Br Med J. 1974 Jan 26;1(5899):134–137. doi: 10.1136/bmj.1.5899.134. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Zarowny D., Ogilvie R., Tamblyn D., MacLeod C., Ruedy J. Pharmacokinetics of amoxicillin. Clin Pharmacol Ther. 1974 Dec;16(6):1045–1051. doi: 10.1002/cpt19741661045. [DOI] [PubMed] [Google Scholar]