Cefpirome clinical pharmacokinetics

L. C. Strenkoski, David E. Nix

Research output: Contribution to journalArticle

20 Citations (Scopus)

Abstract

Cefpirome is a new cephalosporin that exhibits similar in vitro potency to ceftazidime against Gram-negative organisms but has significantly greater in vitro potency against Gram-positive organisms. Cefpirome differs from cefotaxime in that a 3'-pyridinium moiety replaces the acetoxy moiety of cefotaxime. This structural change imparts greater β-lactamase stability, increases the ability to penetrate the outer membrane of Gram-negative bacteria, and enhances activity against Gram-positive organisms. The pharmacokinetic properties of cefpirome are typical of cephalosporins. The drug can be administered by intravenous or intramuscular injection, but is not well absorbed after oral administration. Bioavailability following intramuscular injection exceeds 90%. Cefpirome exhibits low protein binding (≃10%) and has a volume of distribution similar to extracellular fluid volume. Cefpirome penetrates the prostate gland, lung, blister fluid, cerebrospinal fluid and peritoneal fluid, reaching concentrations that are similar to those achieved by other later generation cephalosporins. Approximately 80% of an intravenous dose is eliminated unchanged in the urine. No active metabolites of cefpirome have been identified. The elimination half-life of cefpirome is approximately 2 hours. Elimination appears to be primarily by glomerular filtration since the total clearance of cefpirome is approximately equal to creatinine clearance. The time during which drug concentrations exceed the minimum inhibitory concentration (MIC) represents the most clinically important pharmacodynamic parameter for β-lactam agents. When cefpirome is administered at a dosage of 2g every 12 hours to patients without renal insufficiency [creatinine clearance 70 ml/min (4.2 L/h)], drug concentrations continuously remain above the MIC for pathogens with MIC values of ≤2 μg/ml. With this dosage regimen, drug concentrations will be above the MIC for a pathogen with an MIC of 4 μg/ml for 80% of the dosage interval. The time above MIC for pathogens with an MIC of 8 μg/ml is only 60% of the dosage interval.

Original languageEnglish (US)
Pages (from-to)263-273
Number of pages11
JournalClinical Pharmacokinetics
Volume25
Issue number4
StatePublished - 1993
Externally publishedYes

Fingerprint

cefpirome
Microbial Sensitivity Tests
Pharmacokinetics
Cephalosporins
Cefotaxime
Intramuscular Injections
Pharmaceutical Preparations
Creatinine
Lactams
Ceftazidime
Ascitic Fluid
Extracellular Fluid

ASJC Scopus subject areas

  • Pharmacology (medical)
  • Pharmacology, Toxicology and Pharmaceutics(all)

Cite this

Cefpirome clinical pharmacokinetics. / Strenkoski, L. C.; Nix, David E.

In: Clinical Pharmacokinetics, Vol. 25, No. 4, 1993, p. 263-273.

Research output: Contribution to journalArticle

Strenkoski, LC & Nix, DE 1993, 'Cefpirome clinical pharmacokinetics', Clinical Pharmacokinetics, vol. 25, no. 4, pp. 263-273.
Strenkoski, L. C. ; Nix, David E. / Cefpirome clinical pharmacokinetics. In: Clinical Pharmacokinetics. 1993 ; Vol. 25, No. 4. pp. 263-273.
@article{860d63af7a15426f9dbf4913fdda32d8,
title = "Cefpirome clinical pharmacokinetics",
abstract = "Cefpirome is a new cephalosporin that exhibits similar in vitro potency to ceftazidime against Gram-negative organisms but has significantly greater in vitro potency against Gram-positive organisms. Cefpirome differs from cefotaxime in that a 3'-pyridinium moiety replaces the acetoxy moiety of cefotaxime. This structural change imparts greater β-lactamase stability, increases the ability to penetrate the outer membrane of Gram-negative bacteria, and enhances activity against Gram-positive organisms. The pharmacokinetic properties of cefpirome are typical of cephalosporins. The drug can be administered by intravenous or intramuscular injection, but is not well absorbed after oral administration. Bioavailability following intramuscular injection exceeds 90{\%}. Cefpirome exhibits low protein binding (≃10{\%}) and has a volume of distribution similar to extracellular fluid volume. Cefpirome penetrates the prostate gland, lung, blister fluid, cerebrospinal fluid and peritoneal fluid, reaching concentrations that are similar to those achieved by other later generation cephalosporins. Approximately 80{\%} of an intravenous dose is eliminated unchanged in the urine. No active metabolites of cefpirome have been identified. The elimination half-life of cefpirome is approximately 2 hours. Elimination appears to be primarily by glomerular filtration since the total clearance of cefpirome is approximately equal to creatinine clearance. The time during which drug concentrations exceed the minimum inhibitory concentration (MIC) represents the most clinically important pharmacodynamic parameter for β-lactam agents. When cefpirome is administered at a dosage of 2g every 12 hours to patients without renal insufficiency [creatinine clearance 70 ml/min (4.2 L/h)], drug concentrations continuously remain above the MIC for pathogens with MIC values of ≤2 μg/ml. With this dosage regimen, drug concentrations will be above the MIC for a pathogen with an MIC of 4 μg/ml for 80{\%} of the dosage interval. The time above MIC for pathogens with an MIC of 8 μg/ml is only 60{\%} of the dosage interval.",
author = "Strenkoski, {L. C.} and Nix, {David E.}",
year = "1993",
language = "English (US)",
volume = "25",
pages = "263--273",
journal = "Clinical Pharmacokinetics",
issn = "0312-5963",
publisher = "Adis International Ltd",
number = "4",

}

TY - JOUR

T1 - Cefpirome clinical pharmacokinetics

AU - Strenkoski, L. C.

AU - Nix, David E.

PY - 1993

Y1 - 1993

N2 - Cefpirome is a new cephalosporin that exhibits similar in vitro potency to ceftazidime against Gram-negative organisms but has significantly greater in vitro potency against Gram-positive organisms. Cefpirome differs from cefotaxime in that a 3'-pyridinium moiety replaces the acetoxy moiety of cefotaxime. This structural change imparts greater β-lactamase stability, increases the ability to penetrate the outer membrane of Gram-negative bacteria, and enhances activity against Gram-positive organisms. The pharmacokinetic properties of cefpirome are typical of cephalosporins. The drug can be administered by intravenous or intramuscular injection, but is not well absorbed after oral administration. Bioavailability following intramuscular injection exceeds 90%. Cefpirome exhibits low protein binding (≃10%) and has a volume of distribution similar to extracellular fluid volume. Cefpirome penetrates the prostate gland, lung, blister fluid, cerebrospinal fluid and peritoneal fluid, reaching concentrations that are similar to those achieved by other later generation cephalosporins. Approximately 80% of an intravenous dose is eliminated unchanged in the urine. No active metabolites of cefpirome have been identified. The elimination half-life of cefpirome is approximately 2 hours. Elimination appears to be primarily by glomerular filtration since the total clearance of cefpirome is approximately equal to creatinine clearance. The time during which drug concentrations exceed the minimum inhibitory concentration (MIC) represents the most clinically important pharmacodynamic parameter for β-lactam agents. When cefpirome is administered at a dosage of 2g every 12 hours to patients without renal insufficiency [creatinine clearance 70 ml/min (4.2 L/h)], drug concentrations continuously remain above the MIC for pathogens with MIC values of ≤2 μg/ml. With this dosage regimen, drug concentrations will be above the MIC for a pathogen with an MIC of 4 μg/ml for 80% of the dosage interval. The time above MIC for pathogens with an MIC of 8 μg/ml is only 60% of the dosage interval.

AB - Cefpirome is a new cephalosporin that exhibits similar in vitro potency to ceftazidime against Gram-negative organisms but has significantly greater in vitro potency against Gram-positive organisms. Cefpirome differs from cefotaxime in that a 3'-pyridinium moiety replaces the acetoxy moiety of cefotaxime. This structural change imparts greater β-lactamase stability, increases the ability to penetrate the outer membrane of Gram-negative bacteria, and enhances activity against Gram-positive organisms. The pharmacokinetic properties of cefpirome are typical of cephalosporins. The drug can be administered by intravenous or intramuscular injection, but is not well absorbed after oral administration. Bioavailability following intramuscular injection exceeds 90%. Cefpirome exhibits low protein binding (≃10%) and has a volume of distribution similar to extracellular fluid volume. Cefpirome penetrates the prostate gland, lung, blister fluid, cerebrospinal fluid and peritoneal fluid, reaching concentrations that are similar to those achieved by other later generation cephalosporins. Approximately 80% of an intravenous dose is eliminated unchanged in the urine. No active metabolites of cefpirome have been identified. The elimination half-life of cefpirome is approximately 2 hours. Elimination appears to be primarily by glomerular filtration since the total clearance of cefpirome is approximately equal to creatinine clearance. The time during which drug concentrations exceed the minimum inhibitory concentration (MIC) represents the most clinically important pharmacodynamic parameter for β-lactam agents. When cefpirome is administered at a dosage of 2g every 12 hours to patients without renal insufficiency [creatinine clearance 70 ml/min (4.2 L/h)], drug concentrations continuously remain above the MIC for pathogens with MIC values of ≤2 μg/ml. With this dosage regimen, drug concentrations will be above the MIC for a pathogen with an MIC of 4 μg/ml for 80% of the dosage interval. The time above MIC for pathogens with an MIC of 8 μg/ml is only 60% of the dosage interval.

UR - http://www.scopus.com/inward/record.url?scp=0027435460&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=0027435460&partnerID=8YFLogxK

M3 - Article

VL - 25

SP - 263

EP - 273

JO - Clinical Pharmacokinetics

JF - Clinical Pharmacokinetics

SN - 0312-5963

IS - 4

ER -