Hostname: page-component-76fb5796d-r6qrq Total loading time: 0 Render date: 2024-04-26T09:17:28.769Z Has data issue: false hasContentIssue false

Sulbactam/Ampicillin

Published online by Cambridge University Press:  02 January 2015

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

Access options

Get access to the full version of this content by using one of the access options below. (Log in options will check for institutional or personal access. Content may require purchase if you do not have access.)

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, Vet 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 ScholarPubMed
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 ScholarPubMed
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