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Sulbactam/Ampicillin

Published online by Cambridge University Press:  07 February 2022

Francine R. Salamone*
Affiliation:
Division of Pharmacy Services, Memorial Sloan Kettering Cancer Center, New York, New York
*
Infectious Diseases, Division of Pharmacy Services, Memorial Sloan Kettering Cancer Center, 1275 York Ave, New York, NY 10021

Abstract

Sulbactam/ampicillin was recently marketed for use in several infections caused by beta-lactamase-producing organisms. Sulbactam is the second beta-lactamase inhibitor to become available in the United States. Interest in inhibition of beta-lactamases arose in the late 1960s when a combination consisting of an antibacterial agent and an enzyme inhibitor was found effective in the treatment of certain resistant gram-negative infections. It is now well accepted that the addition of a beta-lactamase inhibitor to a beta-lactam antibiotic may expand its usefulness in a variety of infections.

The penicillin derivatives, known as beta-lactam antibiotics, possess a four-membered ring (beta-lactam ring) fused to a second ring (Figure). It is the beta-lactam ring that is essential for the inhibition of bacterial cell wall synthesis and subsequent bactericidal activity of these agents. The development of resistance to beta-lactam antibiotics may occur by a number of mechanisms, although the most important is bacterial production of enzymes (beta-lactamases) that are capable of beta-lactam ring hydrolysis and inactivation.

Sulbactam resembles the penicillin derivatives in structure (Figure) and is able to preserve their activity by its ability to inhibit the action of beta-lactamases, particularly those of the Richmond classes II-V (gram-negative) and the group A beta-lactamases (gram-positive). Sulbactam is referred to as a “suicide inhibitor” because while forming an irreversible complex with the enzyme, it is destroyed in the process. By virtue of its ability to render the beta-lactamases inactive, sulbactam has been combined with ampicillin in an effort to restore its activity against a number of pathogens that have developed resistance by this mechanism.

Type
Special Sections
Copyright
Copyright © The Society for Healthcare Epidemiology of America 1988

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References

1. Sabath, LD, Elder, HA, McCall, CE, et al: Synergistic combinations of penicillin in the treatment of bacteruria. N Engl J Med 1967;277:232238.CrossRefGoogle Scholar
2. Bauernfeind, A: Classification of β-lactamases. Rev Infect Dis 1986;8:S470S481.CrossRefGoogle ScholarPubMed
3. Noguchi, JK, Gill, MA: Sulbactam: A p-lactamase inhibitor. Clin Pharm 1988;7:3751.Google Scholar
4. Labia, R, Morand, A, Lelievre, V et al: Sulbactam: Biochemical factors involved in its synergy with ampicillin. Rev Infect Dis 1986;8(suppl 5):S644S650.CrossRefGoogle ScholarPubMed
5. Retsema, JA, English, AK, Girard, A, et al: Sulbactamiampicillin: In vitro spectrum, potency, and activity in models of acute infection. Rev Infect Dis 1986;8:S528S534.CrossRefGoogle Scholar
6. Wexler, HM, Harris, B, Carter, WT, et al: In vitro efficacy of sulbactam combined with ampicillin against anaerobic bacteria. Antimicrob Agents Chemother 1985;27:876878.CrossRefGoogle ScholarPubMed
7. Campoli-Richards, DM, Brogden, RN: Sulbactam/ampicillin. A review of its antibacterial activity, pharmacokinetic properties, and therapeutic use. Drugs 1987;33:577609.CrossRefGoogle ScholarPubMed
8. Anonymous: Ampicillin/sulbactam (Unasyn). Med Lett Drugs Ther 1987;29:7981.Google Scholar
9. Lewis, GP, Jusko, WJ: Pharmacokinetics of ampicillin in cirrhosis. Clin Pharmacol Ther 1975;18:475484.CrossRefGoogle ScholarPubMed
10. Rogers, HJ, Bradbrook, ID, Morrison, I'], et al: Pharmacokinetics and bioavailability of sultamicillin estimated by high performance liquid chromatography. J Antimicrob Chemother 1983;11:435445.CrossRefGoogle ScholarPubMed
11. Brown, RM, Wise, R, Andrews, JM, et al: Comparative pharmacokinetics and tissue penetration of sulbactam and ampicillin after concurrent intravenous administration. Antimicrob Agents Chemother 1982;21:565567.CrossRefGoogle ScholarPubMed
12. Foulds, G, Stankewich, JP, Marshal, DC: Pharmacokinetics of sulbactam in humans. Antimicrob Agents Chemother 1983;23:692699.CrossRefGoogle ScholarPubMed
13. Foulds, G: Pharmacokinetics of sulbactam/ampicillin in humans: A review. Rev Infect Dis 1986;8:S503-S511CrossRefGoogle ScholarPubMed
14. Gill, M 4, Kern, JW, Cherella, F, et al: Pharmacokinrtics of parenteral sulbactam in patients with appendicitis. Ther Drug Monit 1984;6:428431.CrossRefGoogle ScholarPubMed
15. Sutton, AM, Turner, TL, Cockburn, F, et al: Pharmacokinetic study of sulbactam and ampicillin administered concomitantly by intraarterialor intravenous infusion in the newborn. Rev Infect Dis 1986;8(suppl 5):S5l8S522.CrossRefGoogle ScholarPubMed
16. Caine, VA, Foulds, G, Handsfield, HH: Therapeutic trial and pharmacokinetics of sulbactam for uncomplicated gonorrhea in men. Antimicrob Agents Chemother 1984;26:683685.CrossRefGoogle ScholarPubMed
17. Morris, DL, Ubhi, CS, Robertson, CS, et al: Biliary pharmacokinetics of sulbactam plus ampicillin in humans. Rev Infect Dis 1986;8(suppl 5):S589S592.CrossRefGoogle ScholarPubMed
18. Mehtar, S, Croft, RJ, Hilas, A: A non-comparative study of parenteral ampicillin and sulbactam in intra-thoracic and intra-abdominal infections. J Antimicrob Chemother 1986;17:389396.CrossRefGoogle ScholarPubMed
19. Kager, L, Malmborg, AS, Nord, CE, et al: A randomized trial of ampicillin plus sulbactam v. gentamicin plus clindamycin in the treatment of intraabdominal infections. Rev Infect Dis 1986;5:S583S588.Google Scholar
20. Yellin, AE, Heseltine, PNR, Berne, TV, et al: The role of Pseudomonas species in patients treated with ampicillin and sulbactam for gangrenous and perforated appendicitis. Surg Gynecol Obstet 1985;161:303307.Google ScholarPubMed
21. Senft, HH, Stiglmayer, R, Eibach, HW, et al: Sulbactam/ampicillin versus cefoxitin in the treatment of obstetric and gynecologic infections. Drugs 1986;31:1821.CrossRefGoogle Scholar
22. Bruhat, MA, Pouly, JL, LeBoedec, G, et al: Treatment of acute salpingitis with sulbactam/ampicillin: Comparison with cefoxitin. Drugs 1986;31:710.CrossRefGoogle ScholarPubMed
23. Gunning, J: A comparison of parenteral sulbactam/ampicillin versus clindamycin/gentamicin in the treatment of pelvic inflammatory disease. Drugs 1986;31:(suppl 2):14l7.CrossRefGoogle ScholarPubMed
24. Crombleholme, W, Landers, D, Ohm-Smith, M, et al: Sulbactam/ampicillin versus metronidazole/gentamicin in the treatment of severe pelvic infections. Drugs 1986;31:1113.CrossRefGoogle ScholarPubMed
25. Lees, L, Milson, JA, Knirsch, AK, et al: Sulbactam plus ampicillin: Interim review of efficacy and safety for therapeutic and prophylactic use. Rev Infect Dis 1986;8(suppl 5):S644S650.CrossRefGoogle ScholarPubMed
26. Houang, ET, Reardon, P: Single dose of intramuscular sulbactam and ampicillin in treating acute uncomplicated gonorrhea. Genitourin Med 1985;61:209213.Google Scholar
27. Stromberg, BV, Reines, HD, Hunt, P: Comparative clinical study of sulbactam/ampicillin and clindamycin for the treatment of aerobic and anaerobic/aerobic infections. Rev Infect Dis 1986;8:S569S575.Google Scholar
28. Reinhardt, JF, Johnston, L, Ruane, P, et al: A randomized double-blind comparison of sulbactam and ampicillin and clindamycin and tobramycin of infections of soft tissues. Surg Gynecol Obstet 1986;162:575578.Google Scholar
29. Ball, AP, Fox, C, Ghosh, D: Sultamicillin (CP-49,952): Evaluation of two dosage schedules in urinary infection. J Antimicrob Chemother 1984;14:395401.CrossRefGoogle ScholarPubMed
30. Dorflinger, T, Madsen, PO: Antibiotic prophylaxis in transurethral surgery: A comparison of transurethral surgery: A comparison of sulbactam/ampicillin and cefoxitin. Infection 1985:13:6669.CrossRefGoogle Scholar
31. de la Hunt, HN, Karran, SJ, Chir, M: Sulbactam/ampicillin compared with cefoxitin for chemoprophylaxis in elective colorectal surgery. Dis Colon Rectum 1986;29:157159.CrossRefGoogle ScholarPubMed
32. Foster, MC, Kapila, L, Morris, DL, et al: A randomized comparative study of sulbactam plus ampicillin vs. metronidazole plus cefotaxime in the management of acute appendicitis in children. Rev Infect Dis 1986;8:634638.CrossRefGoogle ScholarPubMed
33. Krohn, KT: Effect of prophylactic administration of sulbactam/ampicillin on the rate of postoperative endometritis after first trimester abortion. Rev Infect Dis 1986;8:S576S578.CrossRefGoogle ScholarPubMed
34. Houang, ET, Watson, C, Howell, R, et al: Ampicillin combined with sulbactam or metronidazole for single dose chemoprophylaxis in major gynecologic surgery. J Antimicrob Chemother 1984;14:529535.CrossRefGoogle ScholarPubMed
35. Jones, S, Yu, VL, Johnson, JT, et al: Pharmacokinetics and therapeutic trial of sultamicillin in acute sinusitis. Antimicrob Agents Chemother 1985;28:832833.CrossRefGoogle ScholarPubMed
36. Heimdahl, A, Kager, L, Nord, CE: Alterations in the human oropharyngeal microflora related to therapy with aztreonam, moxalactam, and ampicillin plus sulbactam. Scand J Infect Dis 1986;18:4952.CrossRefGoogle ScholarPubMed
37. Unasyn, product information. New York, Pfizer Inc, June 1987.Google Scholar
38. Muchinsky, RF, Reynolds, CA, Nicholson, CA, et al: Stability of sulbactam/ampicillin in diluents for parenteral administration. Rev Infect Dis 1986;8:S523S527.Google Scholar