Pharmacokinetic profile of cefoperazone in healthy volunteers

Warns, C. M.; Lode, H.; Belmega, G.; Jendroschek, T.

doi:10.1007/bf01641032

Cited by 4 publications

(1 citation statement)

References 1 publication

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Accordingly, it may be more sensitive to changes in the liver function and/or plasma protein binding than other cephalosporins, which are not primarily cleared by the liver. [11][12][13] In order to study the influence of chronic lobular hepatitis on the pharmacokinetics of cefoperazone, a dose of l g of cefoperazone was administered to 11 normal, healthy volunteers and 16 patients with chronic lobular hepatitis. In each volunteer or patient, a novel galactose single-point (GSP) method, recently developed by our laboratory,I4 the galactose elimination capacity (GEC)" test, and the modified galactose elimination capacity (MGEC) test14 were also performed as a measure of residual liver function.…”

Section: Introductionmentioning

confidence: 99%

The influence of chronic lobular hepatitis on pharmacokinetics of cefoperazone—a novel galactose single‐point method as a measure of residual liver function

Hu¹,

Tang

Chang³

1994

Biopharm & Drug Disp

View full text Add to dashboard Cite

Cefoperazone is a semisynthetic cephalosporin antibiotic containing a piperazine side chain, which results in antipseudomonal activity. Unlike the other cephalosporins, it is mainly cleared by the liver (60-80%) and it may be more sensitive to changes in the liver function and/or plasma protein binding than other cephalosporins, which are not primarily cleared by the liver. In order to study the influence of chronic lobular hepatitis on the pharmacokinetics of cefoperazone, a dose of 1 g of cefoperazone was administered to 11 normal, healthy volunteers and 16 subjects with chronic lobular hepatitis. In each volunteer or patient, a novel galactose single-point (GSP) method, the galactose elimination capacity (GEC) test, and the modified galactose elimination capacity (MGEC) test were also performed as a measure of residual liver function. Cefoperazone was administered intravenously over a period of 3-5 min. Blood and urine samples were collected at appropriate intervals after drug administration and stored at -30 degrees C until high-pressure liquid chromatographic (HPLC) analysis. The cefoperazone hepatic clearance, mean residence time, and renal clearance in hepatitis patients were significantly different from those of normal healthy volunteers, whereas the plasma protein binding was unaltered between the two groups. Urinary excretion of cefoperazone showed a highly significant increase in patients, 23.95 +/- 5.06% and 37.54 +/- 13.61% for normal men and hepatitis patients respectively. Hepatic clearance and fraction excreted in urine significantly correlated with values of GSP and MGEC respectively (p < 0.05). These results suggest (i) cefoperazone kinetics was significantly altered in patients with chronic lobular hepatitis; (ii) GSP, a novel simple, clinically useful quantitative liver function test, can predict the cefoperazone hepatic clearance in patients with liver dysfunction.

show abstract

Section: Introductionmentioning

confidence: 99%

The influence of chronic lobular hepatitis on pharmacokinetics of cefoperazone—a novel galactose single‐point method as a measure of residual liver function

Hu¹,

Tang

Chang³

1994

Biopharm & Drug Disp

View full text Add to dashboard Cite

show abstract

Novel Galactose Single Point Method as a Measure of Residual Liver Function: Example of Cefoperazone Kinetics in Patients with Liver Cirrhosis

Hu¹,

Tang²,

Chang³

1995

The Journal of Clinical Pharma

View full text Add to dashboard Cite

A novel, simple, clinically useful quantitative liver function test, called the galactose single point (GSP) method, was developed to assess residual liver function by measuring galactose blood concentration 1 hour after galactose was administered (0.5 g/kg). This method was applied to the study of cefoperazone kinetics in patients with hepatic cirrhosis. To study the influence of hepatic cirrhosis on the residual liver function and the correlation between the residual liver function and the pharmacokinetics of cefoperazone, a dose of 1 g of cefoperazone was administered to 11 healthy volunteers and 12 patients with liver cirrhosis. The GSP method, the galactose elimination capacity (GEC) test, and the modified galactose elimination capacity (MGEC) test were done for each volunteer and patient to measure residual liver function. The galactose concentrations were determined enzymatically. Cefoperazone was administered intravenously, and blood and urine samples were collected at appropriate intervals after drug administration. All blood and urine samples were stored at -30 degrees C until high-performance liquid chromatography analysis. Cefoperazone plasma concentrations were much higher in cirrhosis patients than in normal subjects at all times. The elimination half-life, hepatic clearance, mean residence time, and renal clearance of cirrhosis patients differed significantly from those of healthy volunteers. The plasma protein binding was unaltered in both groups. Urinary excretion of cefoperazone was significantly increased in cirrhosis patients (23.95 +/- 5.06% for normal men and 51.09 +/- 11.50% in cirrhosis patients). Hepatic clearance, fraction excreted in urine, and total clearance significantly correlated with GSP, GEC, and MGEC (P < .001).(ABSTRACT TRUNCATED AT 250 WORDS)

show abstract

Cefoperazone Sodium in the Treatment of Serious Bacterial Infections in 2,100 Adults and Children: Multicentered Trials in Europe, Latin America, and Australasia

Gordon¹,

Phyfferoen²

1983

Clinical Infectious Diseases

View full text Add to dashboard Cite

Pharmacokinetic profile of cefoperazone in healthy volunteers

Cited by 4 publications

References 1 publication

The influence of chronic lobular hepatitis on pharmacokinetics of cefoperazone—a novel galactose single‐point method as a measure of residual liver function

The influence of chronic lobular hepatitis on pharmacokinetics of cefoperazone—a novel galactose single‐point method as a measure of residual liver function

Novel Galactose Single Point Method as a Measure of Residual Liver Function: Example of Cefoperazone Kinetics in Patients with Liver Cirrhosis

Cefoperazone Sodium in the Treatment of Serious Bacterial Infections in 2,100 Adults and Children: Multicentered Trials in Europe, Latin America, and Australasia

Contact Info

Product

Resources

About