Clavulanic acid and CP-45, 899: a comparison of their <i>in vitro</i> activity in combination with penicillins

Wise, R.; Andrews, J. M.; Bedford, K. A.

doi:10.1093/jac/6.2.197

Cited by 76 publications

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“…The pharmacokinetic data presented here and the data on the 13-lactamase inhibitory activity of sulbactam in vitro [1,2] indicate that a dosage of 12.5-25 mg/kg given iv over 3 min every 6-8 hr should be adequate for the study of sulbactam as an adjunct to iv 13-lactamtherapy for various bacterial infections in children. At present, ampicillin appears to be the most attractive parenteral partner for sulbactam in pediatric patients.…”

Section: Schaad Guenin and Straehlmentioning

confidence: 96%

“…arthritis, osteomyelitis), urinary tract infections, and meningitis in children are susceptible to sulbactam plus ampicillin. This group of pathogens includes the 13-lactamase-producing strains of Haemophi/us influenzae, Staphylococcus aureus, and Escherichia coli [1,2].In the present study we evaluated the pharmacoInformed consent for these studies was obtained from the parents of the study patients. The guidelines of the local Institutional Committee on Human Investigations were followed in the conduct of this research.…”

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confidence: 99%

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confidence: 99%

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Single-Dose Pharmacokinetics of Intravenous Sulbactam in Pediatric Patients

Schaad¹,

Guenin²,

Straehl³

1986

Clinical Infectious Diseases

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The pharmacokinetics of intravenously administered sulbactam were studied in 17 pediatric patients two to 14 years of age. Single doses of 12.5 or 25 mg/kg were infused over 3 min, and in previously healthy children, mean peak plasma concentrations 5 min after dosing were 71 and 163 ug/ml, respectively. Noncompartmental and compartmental calculations resulted in similar pharmacokinetic parameters. Linear pharmacokinetics were found in the concentration range studied. The mean terminal-phase half-life was 1.75hr, the mean total plasma clearance was 180 ml/min per 1.73 m-, and the mean apparent volume of distribution was 340 ml/kg. Approximately 70Ofo-80Ofo of an intravenous dose was excreted unchanged in the urine. In children with cystic fibrosis, both total plasma clearance and apparent volume of distribution were significantly increased. The data support the intravenous administration of 12.5-25 mg of sulbactam/kg every 6 to 8 hr for assessing the adequacy of this drug as an adjunct to 13-lactam therapy for various bacterial infections in children.An increasing number of gram-positive and gramnegative organisms that cause infections in children have become resistant to penicillin or cephalosporin compounds through the production of 13-lactamases, enzymes that destroy these antibiotics. One way of restoring the susceptibility of resistant strains of bacteria to these agents is by co-administering an inhibitor of 13-lactamases. Sulbactam is a potent and relatively stable 13-lactamase inhibitor that shows promise as an adjunct to 13-lactam therapy.The majority of the bacterial agents that cause respiratory tract infections (e.g., pneumonia, bronchitis, sinusitis, otitis), cellulitis, skeletal infections (e.g. arthritis, osteomyelitis), urinary tract infections, and meningitis in children are susceptible to sulbactam plus ampicillin. This group of pathogens includes the 13-lactamase-producing strains of Haemophi/us influenzae, Staphylococcus aureus, and Escherichia coli [1,2].In the present study we evaluated the pharmacoInformed consent for these studies was obtained from the parents of the study patients. The guidelines of the local Institutional Committee on Human Investigations were followed in the conduct of this research.

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Section: Schaad Guenin and Straehlmentioning

confidence: 96%

mentioning

confidence: 99%

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Single-Dose Pharmacokinetics of Intravenous Sulbactam in Pediatric Patients

Schaad¹,

Guenin²,

Straehl³

1986

Clinical Infectious Diseases

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“…Doses should be given every 24 h for those undergoing maintenance hemodialysis. On hemodialysis days, doses should be given after hemodialysis.Ampicillin-sulbactam is a broad-spectrum, bactericidal, P-lactamase-resistant antimicrobial combination with potent activity against Haemophilus influenzae, Branhamella catarrhalis, Neisseria species, and most gram-positive and anaerobic pathogens (3,9,10,13). Coadministration of sulbactam appears to have very little effect on the pharmacokinetics of ampicillin, suggesting that coadministration of the sulbactam will not affect the usual dosing regimens for ampicillin (5).…”

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confidence: 99%

Pharmacokinetics of ampicillin (2.0 grams) and sulbactam (1.0 gram) coadministered to subjects with normal and abnormal renal function and with end-stage renal disease on hemodialysis

Blum

Kohli

Harrison

et al. 1989

Antimicrob Agents Chemother

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The single-dose pharmacokinetics of intravenously administered ampicillin (2.0 g) and sulbactam (1.0 g) were studied in normal subjects and in patients with various degrees of creatinine clearance (CLCR). Six normal subjects (CLCR, >60 ml/min), six patients with mild renal failure (CLCR, 31 to 60 ml/min), four patients with severe renal failure (CLCR, 7 to 30 ml/min), and four patients requiring maintenance hemodialysis (CLCR, <7 ml/min) were studied. The terminal half-lives for ampicillin and sulbactam more than doubled in patients with severe renal failure compared with subjects with normal renal function and mild renal insufficiency. CLCR significantly correlated with ampicillin (r = 0.88) and sulbactam (r = 0.54) total body clearance. Mean steady-state volume of distribution and nonrenal clearance for ampicillin and sulbactam were not affected by renal function. Hemodialysis approximately doubled the ampicillin and sulbactam total body clearance. Mean totals of 34.8 4.0% of the ampicillin dose and 44.7 + 3.2% of the sulbactam dose were removed during a 4-h hemodialysis treatment. A slight rebound in concentrations in serum after hemodialysis was observed for both drugs in all four subjects. In hemodialysis patients, the ampicillin half-life was 17.4 8.0 h and the sulbactam half-life was 13.4 + 7.4 h. The ampicillin and sulbactam half-lives were appreciably altered during the hemodialysis period (means of 2.2 and 2.3 h, respectively). The nearly parallel decrease in total body clearance, with volume of distribution and nonrenal clearance remaining relatively constant, suggests that the same ratio of ampicillin to sulbactam is appropriate regardless of renal function. An adjustment of the ampicillin (2.0 g) and sulbactam (1.0 g) dose to twice daily would be appropriate in patients with a CLCR between 7 and 30 ml/min. Doses should be given every 24 h for those undergoing maintenance hemodialysis. On hemodialysis days, doses should be given after hemodialysis.Ampicillin-sulbactam is a broad-spectrum, bactericidal, P-lactamase-resistant antimicrobial combination with potent activity against Haemophilus influenzae, Branhamella catarrhalis, Neisseria species, and most gram-positive and anaerobic pathogens (3,9,10,13). Coadministration of sulbactam appears to have very little effect on the pharmacokinetics of ampicillin, suggesting that coadministration of the sulbactam will not affect the usual dosing regimens for ampicillin (5). The pharmacokinetics of sulbactam are very similar to those of ampicillin in subjects with normal renal function (2,4,5,11,14). The purposes of this study were to evaluate the pharmacokinetics of ampicillin-sulbactam in subjects with various degrees of renal function to evolve dosage guidelines and to determine the effect of hemodialysis on the clearances of ampicillin and sulbactam.

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“…Sulbactam has higher stability in the solution compared to its counterpart clavulanate. (Wise et al, 1980). Keeping in the view clinical significance of fixed dose combination of meropenem and sulbactam, we planned to study the antimicrobial activity of the combination and its safety profile.…”

Section: Introductionmentioning

confidence: 99%

Synergistically Active and Safe Fixed Dose Combination of Meropenem and Sulbactam

Beniwal

Parmjit

2013

iioablett

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Meropenem is a third generation broad spectrum antibiotic. Emergence of meropenem resistance has been reported due to development of mutant plasmid mediated metallo-β-lactamases (IMP-6) and AmpC β-lactamases. Sulbactam, a stable β-lactamase inhibitor, increase antimicrobial activity of meropenem by inhibiting the enzyme β-lactamase. Fixed dose combination of Meropenem-sulbactam in the proportion of 1:1, 1:2, 1:3, 2:1 and 3:1 were evaluated for the antimicrobial activity. Combination of meropenem and sulbactam in the ratio of 2:1 exhibited the synergistic activity. This combination was checked for the subchronic toxicity on wistar rats and no change in biochemical and physiological parameters was observed.

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Clavulanic acid and CP-45, 899: a comparison of their in vitro activity in combination with penicillins

Cited by 76 publications

References 0 publications

Single-Dose Pharmacokinetics of Intravenous Sulbactam in Pediatric Patients

Single-Dose Pharmacokinetics of Intravenous Sulbactam in Pediatric Patients

Pharmacokinetics of ampicillin (2.0 grams) and sulbactam (1.0 gram) coadministered to subjects with normal and abnormal renal function and with end-stage renal disease on hemodialysis

Synergistically Active and Safe Fixed Dose Combination of Meropenem and Sulbactam

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