Abstract
Studies on pivampicillin hydrochloride and ampicillin trihydrate, administered in capsules to healthy volunteers, indicated that pivampicillin was absorbed more efficiently from the gastrointestinal tract than ampicillin. Average peak concentrations of ampicillin in the serum after doses equimolar to 250 mg of ampicillin were 6.8 μg/ml at 56 min with pivampicillin and 1.96 μg/ml at 1 h 24 min with ampicillin. The maximal concentration after pivampicillin treatment was also higher than that recorded when twice the equimolar dose of ampicillin, which averaged 3.2 μg/ml at 1 h 42 min, was used. The urinary excretion of ampicillin, expressed as a percentage of the administered dose, averaged 67 to 73 and 25 to 29% after administration of pivampicillin and ampicillin, respectively. The bioavailability of ampicillin, taken as the area under the serum curve, obtained with pivampicillin at a 250-mg ampicillin dose level was superior to that obtained with a 500-mg dose of ampicillin. Comparison of a suspension intended for children, containing the pivampicillin free base with a suspension of ampicillin trihydrate, emphasized the difference recorded for the capsule preparations. Administration of pivampicillin with a meal rich in fat and protein had no depressant effect on the absorption. Concurrent administration of probenecid caused higher and prolonged concentrations of ampicillin in the serum.
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Selected References
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- ANDERSON K. N., KENNEDY R. P., PLORDE J. J., SHULMAN J. A., PETERSDORF R. G. EFFECTIVENESS OF AMPICILLIN AGAINST GRAM-NEGATIVE BACTERIA. IN VITRO AND IN VIVO STUDIES OF A NEW ANTIBIOTIC. JAMA. 1964 Feb 22;187:555–561. [PubMed] [Google Scholar]
- Brumfitt W., Franklin I., Hayek L., Pursell R. Treatment of urinary tract infection with pivampicillin. A new ampicillin derivative. Scand J Infect Dis. 1973;5(1):59–65. doi: 10.3109/inf.1973.5.issue-1.11. [DOI] [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]
- Engberg-Pedersen H. Empirical equation for pharmacokinetic analysis of drug serum levels after oral application. Antimicrob Agents Chemother. 1974 Nov;6(5):554–562. doi: 10.1128/aac.6.5.554. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Frederiksen E., Godtfredsen W. O., Nielsen B., Roholt K. Pivampicillinkloid--et nyt bredspektret antibiotikum til oral anvendelse. Nord Med. 1971 Nov 25;86(47):1376–1380. [PubMed] [Google Scholar]
- Hultberg E. R., Backelin B. Studies on the absorption of pivampicillin and ampicillin. Scand J Infect Dis. 1972;4(2):149–153. doi: 10.3109/inf.1972.4.issue-2.16. [DOI] [PubMed] [Google Scholar]
- KLEIN J. O., FINLAND M. Ampicillin activity in vitro and absorption and excretion in normal young men. Am J Med Sci. 1963 May;245:544–555. [PubMed] [Google Scholar]
- KNUDSEN E. T., ROLINSON G. N., STEVENS S. Absorption and excretion of "Penbritin". Br Med J. 1961 Jul 22;2(5246):198–200. doi: 10.1136/bmj.2.5246.198. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Kirby W. M., Kind A. C. Clinical pharmacology of ampicillin and hetacillin. Ann N Y Acad Sci. 1967 Sep 27;145(2):291–297. doi: 10.1111/j.1749-6632.1967.tb50226.x. [DOI] [PubMed] [Google Scholar]
- Marget W., Daschner F., Unertl K. Investigations on pivampicillin treatment in newborns and infants. Infection. 1973;1(1):41–45. doi: 10.1007/BF01638255. [DOI] [PubMed] [Google Scholar]
- ROLINSON G. N., STEVENS S. Microbiological studies on a new broad-spectrum penicilin, "Penbritin". Br Med J. 1961 Jul 22;2(5246):191–196. doi: 10.1136/bmj.2.5246.191. [DOI] [PMC free article] [PubMed] [Google Scholar]
- SUTHERLAND R., ROLINSON G. N. ACTIVITY OF AMPICILLIN IN VITRO COMPARED WITH OTHER ANTIBIOTICS. J Clin Pathol. 1964 Jul;17:461–465. doi: 10.1136/jcp.17.4.461. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Simon C., Nehls R., Malerczyk V., Toeller W., Zierott G., Lehmann K. Pivampicillin, ein neues Ampicillin-Derivat. Dtsch Med Wochenschr. 1974 Jan 25;99(4):137–141. doi: 10.1055/s-0028-1107725. [DOI] [PubMed] [Google Scholar]
- Stewart G. T., Coles H. M., Nixon H. H., Holt R. J. "Penbritin": An Oral Penicillin with Broad-spectrum Activity. Br Med J. 1961 Jul 22;2(5246):200–206. doi: 10.1136/bmj.2.5246.200. [DOI] [PMC free article] [PubMed] [Google Scholar]
