Effect of Ceftizoxime, a New Cephalosporin Antibiotic, on Binding of Bilirubin to Human Serum Albumin

Sakamoto, Hiroshi; Murakawa, Takeo; Hirose, Toshiharu; Nishida, Motohiro

doi:10.1159/000238205

Cited by 8 publications

(3 citation statements)

References 7 publications

(11 reference statements)

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“…These varia tions, proportionally more important for low concentrations of ceftriaxone, may be explained by a higher protein binding at these concentrations [15] and/or by an easier displacement from weakly binding sites of serum albumin. Importance of competition between bilirubin and anti biotics might depend on the large extent of protein binding [11] and our results might be explained by the high binding of ceftri axone (83-96%) [15]. However, this fea ture is not the only one: Stutman et al [16] reported that cefoperazone is bound up to 90% to serum albumin and exhibits a less er bilirubin-displacing effect than moxalactam for which binding is about 60%.…”

Section: Discussionmentioning

confidence: 72%

Displacement Effect of Ceftriaxone on Bilirubin Bound to Human Serum Albumin

Gulian¹,

Dalmasso²,

Pontier³

et al. 1986

Chemotherapy

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The effects of ceftriaxone, a ‘third-generation’ cephalosporin, on bilirubin-serum albumin complexes were investigated. This study was performed on human adult samples at various bilirubin-albumin ratios. Ceftriaxone caused a decrease of unconjugated bilirubin and simultaneously an increase of erythrocyte-bound bilirubin. These variations were proportionally more important for low concentrations of antibiotic, including therapeutic values. It was concluded that ceftriaxone competes with bilirubin and displaces it from albumin-binding sites.

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Section: Discussionmentioning

confidence: 72%

Displacement Effect of Ceftriaxone on Bilirubin Bound to Human Serum Albumin

Gulian¹,

Dalmasso²,

Pontier³

et al. 1986

Chemotherapy

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“…Ceftizoxime is a third-generation broadspectrum parenteral cephalosporin with ac tivity against a wide variety of gram-positive may be an advantage for hyperbilirubinémie infants with sepsis [2], It is excreted essential ly unchanged via the kidney [3], In prelimina ry studies, satisfactory clinical response to ceftizoxime was seen in 86-88% of septic neo nates [4,5], Satisfactory bacteriological re sponse ranged from 86 to 100% depending on the étiologie agent [4,5], This broad-spectrum antibiotic may prove to be an effective single agent for treating neonatal infections without any of the potential adverse effects of an ami noglycoside.…”

Section: Introductionmentioning

confidence: 99%

Population Pharmacokinetics of Ceftizoxime in Premature Newborns

et al. 1993

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The population pharmacokinetic parameters of ceftizoxime were determined in 50 premature newborns less than 1 week of age (birth weight = 1.8 ± 0.6 kg) with a clinical diagnosis of suspected sepsis. Each infant received ceftizoxime 25 mg/kg every 12 h intravenously over 30 min for a total of 6 doses. Serum concentrations of ceftizoxime were assayed by HPLC at 0.5, 1, 2.5 and 11.5 h or at 0.5, 1.5, 4.5 and 11.5 h after the first and the sixth dose. A total of 184 serum concentrations following the first dose and 160 following the sixth dose were fit separately and then collectively to a one-compartment model using NONMEM. The separately estimated parameters were not significantly different between the first and the sixth dose. The final parameter estimates were 27.1 ml/h/kg, 333 ml/kg and 8.5 h for clearance, volume of distribution and halflife, respectively. Other factors including gestational and postnatal age were not associated with alterations in ceftizoxime clearance. That the large variability in clearance was decreased from a coefficient of variation of 80 to 50% warrants dosing premature infants on the basis of body weight. The results of this study suggest that 25 mg/kg ceftizoxime every 12 h appears to be an appropriate dosing regimen for premature neonates.

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“…An increasing unbound bilirubin con centration in blood by the drug-induced displacement from human serum albumin (HSA) causes bilirubin encephalopathy [1][2][3]. Caution must be exercised in admin istering these drugs to neonates having a strong binding capacity for HSA.…”

Section: Introductionmentioning

confidence: 99%

Analytical Studies on β-Lactam Antibiotics

Matsuura

Nagayama²,

Kitagawa³

1988

Chemotherapy

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We established a method for determining the K_D value as a measure of the bilirubin-displacing effect for drugs by using bilirubin oxidase, which is produced by Myrothecium verrucaria MT-1. This method makes it possible to conduct measurements of many β-lactam antibiotics, including those which could not be determined by Bro-dersen’s method. The K_D values of latamoxef reported by many investigators based on Brodersen’s method were higher than the true value owing to interaction of the drug with peroxidase and H₂O₂. Our K_D value under the new enzyme conditions was 2.6 x 10³. Little or no interaction of drug with the enzyme system was tentatively confirmed. Flomoxef, a newly developed drug, and 7432-S, under development in our company, had K_D values of 0.4 x 10³ and 2.8 x 10³, respectively.

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Effect of Ceftizoxime, a New Cephalosporin Antibiotic, on Binding of Bilirubin to Human Serum Albumin

Cited by 8 publications

References 7 publications

Displacement Effect of Ceftriaxone on Bilirubin Bound to Human Serum Albumin

Displacement Effect of Ceftriaxone on Bilirubin Bound to Human Serum Albumin

Population Pharmacokinetics of Ceftizoxime in Premature Newborns

Analytical Studies on β-Lactam Antibiotics

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