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PMID: 3038500 Published · ppublish English Journal Article Review

Sulbactam/ampicillin. A review of its antibacterial activity, pharmacokinetic properties, and therapeutic use.

Drugs ·Vol. 33 ·No. 6 ·1987-06-00 ·Pages 577-609

Campoli-Richards DM, Brogden RN

Abstract

Sulbactam is a semisynthetic beta-lactamase inhibitor which when combined with certain beta-lactam antibacterials extends their activity against bacteria that are normally resistant to the antibiotic due to production of beta-lactamases. In combination with ampicillin it extends the antibacterial activity of ampicillin to include beta-lactamase-producing strains which are otherwise resistant, including Bacteroides fragilis, and increases the susceptibility of many sensitive strains. Sulbactam is poorly absorbed after oral administration and sulbactam/ampicillin is therefore administered parenterally, although another linked sulbactam-ampicillin compound, sultamicillin, has been developed which is well absorbed after oral administration. The basic pharmacokinetic characteristics of sulbactam after parenteral administration are similar to those of ampicillin. Multiple-dose therapy with sulbactam/ampicillin is clinically and bacteriologically effective in infections of the urinary tract, skin and soft tissue, bones and joints, respiratory tract, ears, nose and throat, as well as intra-abdominal and obstetric and gynaecological infections and septicaemia. In addition, single intramuscular doses of sulbactam/ampicillin administered with oral probenecid are therapeutically effective in gonorrhoea, including infections due to penicillinase-producing and/or ampicillin-resistant Neisseria gonorrhoeae. In the prophylaxis of infectious complications of surgery sulbactam/ampicillin is superior to placebo and appears to be similar in efficacy to several alternative antibacterial regimens. Further studies involving larger numbers of patients are needed to clarify the comparative therapeutic and prophylactic efficacy of sulbactam/ampicillin and alternative antibacterial drugs. Nonetheless, sulbactam/ampicillin improves the therapeutic and prophylactic efficacy of an antibacterial of familiar safety, and must be seen as a worthwhile advance.

MeSH Terms
Ampicillin/metabolism,pharmacology,therapeutic use Bacteria/drug effects Bacterial Infections/drug therapy Humans Kinetics Penicillanic Acid/metabolism,pharmacology,therapeutic use Sulbactam beta-Lactamase Inhibitors
Chemicals
beta-Lactamase Inhibitors Ampicillin Penicillanic Acid Sulbactam
Authors & Affiliations
2 authors, click to expand affiliations / ORCID
Campoli-Richards D M
Brogden R N
References (82)
82 references, click to expand
  1. 6-beta-bromo- and 6-beta-iodo penicillanic acid, two novel beta-lactamase inhibitors.
    J Antimicrob Chemother. 1981 May;7(5):531-6 PMID: 6267005
  2. Cefoxitin, N-formimidoyl thienamycin, clavulanic acid, and penicillanic acid sulfone as suicide inhibitors for different types of beta-lactamases produced by gram-negative bacteria.
    J Antibiot (Tokyo). 1982 Nov;35(11):1594-602 PMID: 6298169
  3. An open, comparative study of sulbactam plus ampicillin vs. cefotaxime as initial therapy for serious soft tissue and bone and joint infections.
    Rev Infect Dis. 1986 Nov-Dec;8 Suppl 5:S593-8 PMID: 3026009
  4. Characterization of cephalosporinases from Bacteroides fragilis, Bacteroides thetaiotaomicron and Bacteroides vulgatus.
    J Antibiot (Tokyo). 1983 Jan;36(1):76-85 PMID: 6332105
  5. Pharmacokinetic study of sulbactam and ampicillin administered concomitantly by intraarterial or intravenous infusion in the newborn.
    Rev Infect Dis. 1986 Nov-Dec;8 Suppl 5:S518-22 PMID: 3025999
  6. Single-dose pharmacokinetics of intravenous sulbactam in pediatric patients.
    Rev Infect Dis. 1986 Nov-Dec;8 Suppl 5:S512-7 PMID: 3025998
  7. A randomized, double-blind comparison of sulbactam/ampicillin and clindamycin for the treatment of aerobic and aerobic-anaerobic infections.
    Rev Infect Dis. 1986 Nov-Dec;8 Suppl 5:S569-75 PMID: 3026005
  8. In vitro bactericidal activity of sulbactam plus ampicillin against methicillin-resistant Staphylococcus aureus.
    Rev Infect Dis. 1986 Nov-Dec;8 Suppl 5:S549-54 PMID: 3026003
  9. Antibacterial activity and kill kinetics of ampicillin/sulbactam (CP-45899) combinations against Escherichia coli and Klebsiella aerogenes.
    Infection. 1984 Jan-Feb;12(1):46-50 PMID: 6323321
  10. Correlation of the effect of beta-lactamase inhibitors on the beta-lactamase in growing cultures of gram-negative bacteria with their effect on the isolated beta-lactamase.
    Antimicrob Agents Chemother. 1984 Sep;26(3):358-63 PMID: 6095753
  11. Therapeutic trial and pharmacokinetics of sulbactam for uncomplicated gonorrhea in men.
    Antimicrob Agents Chemother. 1984 Nov;26(5):683-5 PMID: 6097173
  12. Sulbactam/ampicillin versus cefoxitin in the treatment of obstetric and gynaecological infections.
    Drugs. 1986;31 Suppl 2:18-21 PMID: 3013568
  13. A randomized comparative study of sulbactam plus ampicillin vs. metronidazole plus cefotaxime in the management of acute appendicitis in children.
    Rev Infect Dis. 1986 Nov-Dec;8 Suppl 5:S634-8 PMID: 3026017
  14. Assays of sulbactam in the presence of ampicillin.
    Ther Drug Monit. 1986;8(2):223-7 PMID: 3014686
  15. Pharmacokinetics of sulbactam/ampicillin in humans: a review.
    Rev Infect Dis. 1986 Nov-Dec;8 Suppl 5:S503-11 PMID: 3025997
  16. Comparative pharmacokinetics and tissue penetration of sulbactam and ampicillin after concurrent intravenous administration.
    Antimicrob Agents Chemother. 1982 Apr;21(4):565-7 PMID: 6282211
  17. Alterations in the human oropharyngeal microflora related to therapy with aztreonam, moxalactam and ampicillin plus sulbactam.
    Scand J Infect Dis. 1986;18(1):49-52 PMID: 3008310
  18. Sulbactam/ampicillin: effects on glucose metabolism in diabetics with soft tissue infection.
    J Antimicrob Chemother. 1985 Nov;16(5):643-7 PMID: 3001015
  19. The beta-lactamases of gram-negative bacteria and their role in resistance to beta-lactam antibiotics.
    J Antimicrob Chemother. 1976 Jun;2(2):115-57 PMID: 783110
  20. Sulbactam plus ampicillin: interim review of efficacy and safety for therapeutic and prophylactic use.
    Rev Infect Dis. 1986 Nov-Dec;8 Suppl 5:S644-50 PMID: 3026019
  21. Comparative inhibition beta-lactamases by novel beta-lactam compounds.
    Antimicrob Agents Chemother. 1979 Feb;15(2):171-6 PMID: 311616
  22. A randomized controlled trial of ampicillin plus sulbactam vs. gentamicin plus clindamycin in the treatment of intraabdominal infections: a preliminary report. Study Group of Intraabdominal Infections.
    Rev Infect Dis. 1986 Nov-Dec;8 Suppl 5:S583-8 PMID: 2879345
  23. Susceptibility of Haemophilus ducreyi to ampicillin and sulbactam in vitro.
    Antimicrob Agents Chemother. 1986 Jun;29(6):1110-2 PMID: 3015016
  24. Sulbactam/ampicillin vs. chloramphenicol/ampicillin for the treatment of meningitis in infants and children.
    Rev Infect Dis. 1986 Nov-Dec;8 Suppl 5:S620-9 PMID: 3026015
  25. Concentrations of ampicillin plus sulbactam in serum and intestinal mucosa and effects on the colonic microflora in patients undergoing colorectal surgery.
    Eur J Clin Microbiol. 1983 Dec;2(6):559-63 PMID: 6321166
  26. Inactivation of the RTEM beta-lactamase from Escherichia coli. Interaction of penam sulfones with enzyme.
    Biochemistry. 1981 May 12;20(10):2726-31 PMID: 7018564
  27. Treatment of acute salpingitis with sulbactam/ampicillin. Comparison with cefoxitin.
    Drugs. 1986;31 Suppl 2:7-10 PMID: 3013571
  28. Penetration of sulbactam into the cerebrospinal fluid of patients with bacterial meningitis receiving ampicillin therapy.
    Rev Infect Dis. 1986 Nov-Dec;8 Suppl 5:S612-6 PMID: 3026013
  29. Efficacy and safety of sequential treatment with parenteral sulbactam/ampicillin and oral sultamicillin for skeletal infections in children.
    Rev Infect Dis. 1986 Nov-Dec;8 Suppl 5:S639-43 PMID: 3026018
  30. Penetration of sulbactam and ampicillin into peritoneal fluid.
    Antimicrob Agents Chemother. 1983 Aug;24(2):290-2 PMID: 6314889
  31. Penetration of sulbactam-ampicillin and clavulanic acid-amoxicillin into the pelvic peritoneum.
    Antimicrob Agents Chemother. 1985 Jul;28(1):165-6 PMID: 2994556
  32. CP-45,899 in combination with penicillin or ampicillin against penicillin-resistant Staphylococcus, Haemophilus influenzae, and Bacteroides.
    Antimicrob Agents Chemother. 1980 Apr;17(4):615-22 PMID: 6249192
  33. Pharmacokinetics of sulbactam in humans.
    Antimicrob Agents Chemother. 1983 May;23(5):692-9 PMID: 6307133
  34. Sulbactam: alkaline degradation and determination by high-performance liquid chromatography.
    Chem Pharm Bull (Tokyo). 1984 Jul;32(7):2752-8 PMID: 6094028
  35. Sulbactam/ampicillin compared with cefoxitin for chemoprophylaxis in elective colorectal surgery.
    Dis Colon Rectum. 1986 Mar;29(3):157-9 PMID: 3002735
  36. Excess of ampicillin rashes associated with allopurinol or hyperuricemia. A report from the Boston Collaborative Drug Surveillance Program, Boston University Medical Center.
    N Engl J Med. 1972 Mar 9;286(10):505-7 PMID: 4258181
  37. Sulbactam/ampicillin in the treatment of acute epiglottitis in children.
    Rev Infect Dis. 1986 Nov-Dec;8 Suppl 5:S617-9 PMID: 3026014
  38. Treatment of infections caused by ampicillin-resistant pathogens with a combination of ampicillin and CP-45,899.
    Antimicrob Agents Chemother. 1982 Mar;21(3):519-20 PMID: 6285812
  39. In vitro efficacy of sulbactam combined with ampicillin against anaerobic bacteria.
    Antimicrob Agents Chemother. 1985 May;27(5):876-8 PMID: 2990330
  40. Biliary pharmacokinetics of sulbactam plus ampicillin in humans.
    Rev Infect Dis. 1986 Nov-Dec;8 Suppl 5:S589-92 PMID: 3026008
  41. Single dose intramuscular sulbactam and ampicillin in treating acute uncomplicated gonorrhoea.
    Genitourin Med. 1985 Jun;61(3):209 PMID: 2989156
  42. The effect of inhibitors of beta-lactamases on beta-lactamase extracts and on intact cells.
    J Antimicrob Chemother. 1982 Apr;9(4):287-96 PMID: 6282800
  43. Sulbactam/ampicillin versus metronidazole/gentamicin in the treatment of severe pelvic infections.
    Drugs. 1986;31 Suppl 2:11-3 PMID: 3013566
  44. A sulfone beta-lactam compound which acts as a beta-lactamase inhibitor.
    J Antibiot (Tokyo). 1978 Dec;31(12):1238-44 PMID: 310815
  45. Antibiotic prophylaxis in transurethral surgery: a comparison of sulbactam-ampicillin and cefoxitin.
    Infection. 1985 Mar-Apr;13(2):66-9 PMID: 2987133
  46. Comparative clinical study of Sulbactam and ampicillin and clindamycin and tobramycin in infections of soft tissues.
    Surg Gynecol Obstet. 1986 Jun;162(6):575-8 PMID: 3012808
  47. High-pressure liquid chromatographic assay of sulbactam in plasma, urine, and tissue.
    Antimicrob Agents Chemother. 1986 Aug;30(2):231-3 PMID: 3021050
  48. Treatment of infections due to multiresistant Neisseria gonorrhoeae with sulbactam/ampicillin.
    Rev Infect Dis. 1986 Nov-Dec;8 Suppl 5:S599-603 PMID: 3026010
  49. Sultamicillin--a new antibiotic in the treatment of persistent lower respiratory tract infections caused by Haemophilus influenzae.
    J Antimicrob Chemother. 1986 Apr;17(4):529-33 PMID: 3011725
  50. Sequence of the Citrobacter freundii OS60 chromosomal ampC beta-lactamase gene.
    Eur J Biochem. 1986 May 2;156(3):441-5 PMID: 3486121
  51. Effect of prophylactic administration of sulbactam/ampicillin on the rate of postoperative endometritis after first-trimester abortion.
    Rev Infect Dis. 1986 Nov-Dec;8 Suppl 5:S576-8 PMID: 3026006
  52. Pharmacokinetics and bioavailability of sultamicillin estimated by high performance liquid chromatography.
    J Antimicrob Chemother. 1983 May;11(5):435-45 PMID: 6307964
  53. 6-Acetylmethylenepenicillanic acid (Ro 15-1903), a potent beta-lactamase inhibitor. I. Inhibition of chromosomally and R-factor-mediated beta-lactamases.
    J Antibiot (Tokyo). 1982 Nov;35(11):1578-83 PMID: 6298167
  54. Clinical efficacy of sulbactam/ampicillin in pediatric infections caused by ampicillin-resistant or penicillin-resistant organisms.
    Rev Infect Dis. 1986 Nov-Dec;8 Suppl 5:S630-3 PMID: 3026016
  55. Concentration of sulbactam and ampicillin in serum and the myometrium.
    Drugs. 1986;31 Suppl 2:26-8 PMID: 3013570
  56. Efficacy of ampicillin plus a beta-lactamase inhibitor (CP-45,899) in experimental endocarditis due to Staphylococcus aureus.
    J Infect Dis. 1981 Sep;144(3):237-43 PMID: 6268715
  57. Variation in the potentiation of beta-lactam antibiotic activity by clavulanic acid and sulbactam against multiply antibiotic-resistant bacteria.
    J Antimicrob Chemother. 1986 Apr;17(4):463-9 PMID: 3011724
  58. Effects of ampicillin plus sulbactam on bowel flora in patients undergoing colorectal surgery.
    Antimicrob Agents Chemother. 1982 Aug;22(2):208-12 PMID: 6100422
  59. Penetration of sulbactam into cerebrospinal fluid of patients with viral meningitis or without meningitis.
    Rev Infect Dis. 1986 Nov-Dec;8 Suppl 5:S609-11 PMID: 3026012
  60. The elimination of sulbactam alone and combined with ampicillin in patients with renal dysfunction.
    J Antimicrob Chemother. 1983 Jun;11(6):583-7 PMID: 6309731
  61. Beta-lactamases.
    Br Med Bull. 1984 Jan;40(1):18-27 PMID: 6100076
  62. Pharmacokinetics of parenteral sulbactam in patients with appendicitis.
    Ther Drug Monit. 1984;6(4):428-31 PMID: 6096991
  63. In-vitro evaluation of sulbactam, a penicillanic acid sulphone with beta-lactamase inhibitory properties.
    J Antimicrob Chemother. 1982 Aug;10(2):117-23 PMID: 6288651
  64. Inhibition kinetics of three R-factor-mediated beta-lactamases by a new beta-lactam sulfone (CP 45899).
    Biochim Biophys Acta. 1980 Feb 14;611(2):351-7 PMID: 6243991
  65. Clavulanic acid and CP-45,899: a comparison of their in vitro activity in combination with penicillins.
    J Antimicrob Chemother. 1980 Mar;6(2):197-206 PMID: 6247316
  66. Inconsistency of synergy between the beta-lactamase inhibitor CP-45,899 and beta-lactam antibiotics against multiply drug-resistant Enterobacteriaceae and pseudomonas species.
    Antimicrob Agents Chemother. 1981 Feb;19(2):361-3 PMID: 6289732
  67. Treatment of ampicillin-resistant acute otitis media in the chinchilla.
    Arch Otolaryngol. 1983 Aug;109(8):533-5 PMID: 6307238
  68. The beta-lactamases of gram-negative bacteria and their possible physiological role.
    Adv Microb Physiol. 1973;9:31-88 PMID: 4581138
  69. CP-45,899, a beta-lactamase inhibitor that extends the antibacterial spectrum of beta-lactams: initial bacteriological characterization.
    Antimicrob Agents Chemother. 1978 Sep;14(3):414-9 PMID: 309306
  70. Penicillanic acid sulfone: interaction with RTEM beta-lactamase from Escherichia coli at different pH values.
    Biochemistry. 1981 Jun 23;20(13):3688-95 PMID: 6268141
  71. The parenteral kinetics of ampicillin/sulbactam in man.
    Int J Clin Pharmacol Res. 1985;5(2):79-86 PMID: 2991150
  72. A non-comparative study of parenteral ampicillin and sulbactam in intra-thoracic and intra-abdominal infections.
    J Antimicrob Chemother. 1986 Mar;17(3):389-96 PMID: 3009384
  73. Comparative activities of the beta-lactamase inhibitors YTR 830, clavulanate, and sulbactam combined with ampicillin and broad-spectrum penicillins against defined beta-lactamase-producing aerobic gram-negative bacilli.
    Antimicrob Agents Chemother. 1986 Jun;29(6):980-5 PMID: 3015017
  74. Clinical efficacy and safety of sulbactam/ampicillin in patients suffering from chronic liver disease.
    J Antimicrob Chemother. 1987 Apr;19(4):527-32 PMID: 3034850
  75. Induction/inhibition of chromosomal beta-lactamases by beta-lactamase inhibitors.
    Rev Infect Dis. 1986 Nov-Dec;8 Suppl 5:S562-8 PMID: 3026004
  76. Intestinal beta-lactamase activity in ampicillin-induced, Clostridium difficile-associated ileocecitis.
    J Infect Dis. 1983 Feb;147(2):227-35 PMID: 6600772
  77. High-performance liquid chromatographic assay of sulbactam using pre-column reaction with 1,2,4-triazole.
    J Chromatogr. 1985 May 31;341(1):115-22 PMID: 2991310
  78. The role of Pseudomonas species in patients treated with ampicillin and Sulbactam for gangrenous and perforated appendicitis.
    Surg Gynecol Obstet. 1985 Oct;161(4):303-7 PMID: 2996161
  79. A comparison of parenteral sulbactam/ampicillin versus clindamycin/gentamicin in the treatment of pelvic inflammatory disease.
    Drugs. 1986;31 Suppl 2:14-7 PMID: 3013567
  80. Ampicillin combined with sulbactam or metronidazole for single-dose chemoprophylaxis in major gynaecological surgery.
    J Antimicrob Chemother. 1984 Nov;14(5):529-35 PMID: 6096349
  81. Sulbactam kinetics and excretion into breast milk in postpartum women.
    Clin Pharmacol Ther. 1985 Dec;38(6):692-6 PMID: 2998677
  82. Pharmacokinetics and bactericidal activity of sultamicillin in infants and children.
    J Antimicrob Chemother. 1985 Mar;15(3):345-51 PMID: 2987174
Article Info
Journal
Drugs
Abbr.
Drugs
ISSN
0012-6667
Published
1987-06-00
Pages
577-609
Language
English
Region
New Zealand
NLM ID
7600076
Subset
IM
Corrections
ErratumIn
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