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  • Title: Aminopenicillins - clinical pharmacology and use in disease states.
    Author: Neu HC.
    Journal: Int J Clin Pharmacol Biopharm; 1975 Mar; 11(2):132-44. PubMed ID: 1095502.
    Abstract:
    Ampicillin introduced in 1961 has been administered in the treatment of diverse infections by both oral and parenteral means. Oral infections of the upper airways such as otitis media, bronchitis, and pneumonia have responded with high success rates since the microorganisms involved have remained sensitive to ampicillin. Similarly, out-patient urinary tract infections caused by Escherichia coli, Proteus mirabilis, and enterococci are cured. Typhoid fever may yet be treated with ampicillin, but shigellosis has become refractory with the development of resistant strains. Ampicillin has assumed a prominent role in the treatment of gonorrhoea. Parenteral ampicillin is still a mainstay of the treatment of Hemophilus meningitis, but the recent appearance of ampicillin resistant strains may become a serious problem. A number of derivatives and analogues of ampicillin have been developed. Among the compounds, hetacillin, metampicillin and pivampicillin which hydrolyze in the body to yield ampicillin, only pivampicillin appears to offer advantage over the parent compound. Blood levels are twice those of a comparable dose of ampicillin. However, more comparisons with ampicillin in clinical situations are needed. The other analogues of ampicillin are epicillin, cyclacillin and amoxicillin. Epicillin has no superiority to ampicillin, and the cyclacillin data do not show clear superiority over ampicillin in spite of initially high blood levels, since the compound is less active and so rapidly cleared from the body. Amoxicillin, on the other hand, has been shown to have it vitro activity equal to ampicillin and to produce higher blood levels for a longer period of time. Clinical studies have substantiated efficacy in treatment of otitis media, pharyngitis, bronchitis, pneumonitis, and urinary tract infections at doses half those of ampicillin. It has been effective in gonorrhoea and typhoid, but not in shigellosis. It would seem that to date only pivampicillin and amoxicillin, particularly the later, should be considered as replacements of ampicillin in oral therapy.
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