Piperacillin distribution into bile, gallbladder wall, abdominal skeletal muscle, and adipose tissue in surgical patients

Russo, John; Thompson, M I; Russo, Mary E.; Saxon, B A; Matsen, John M.; Moody, Frank G.; Rikkers, Layton F.

doi:10.1128/aac.22.3.488

Cited by 13 publications

(6 citation statements)

References 6 publications

(3 reference statements)

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“…The reason that declining renal function has such a small effect on piperacillin kinetics has not been explained by previous studies or by the present results; however, piperacillin is known to concentrate in bile (5,10), and this may provide an alternate route of elimination in uremia.…”

Section: Discussionmentioning

confidence: 54%

Pharmacokinetics of piperacillin in subjects with various degrees of renal function

Welling¹,

Craig²,

Bundtzen³

et al. 1983

Antimicrob Agents Chemother

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The pharmacokinetics of piperacillin were examined after single intravenous doses to three groups of male patients with creatinine clearances.of -60 (group I), .20 but <60 (group II), and <20 (group III) ml/min per 1.73 M2. Each of 32 patients received either 1 or 4 g of piperacillin as a bolus injection. Three patients received both doses. After a rapid 0.5-to 1-h distribution phase, antibiotic levels in serum declined monoexponentially. After the 1-g dose, mean peak piperacillin levels in serum were 60, 103, and 67 ,g/ml and the P phase elimination half-lives were 1.0, 1.6, and 3.9 h in groups I, II, and III, respectively. After the 4-g dose, the respective mean peak piperacillin levels in serum were 329, 232, and 262 ,ug/ml and P phase half-lives were 1.4, 2.3, and 2.6 h in the three groups. There was no clear evidence of significant dose-dependent effects on any pharmacokinetic parameters in any of the groups. Piperacillin levels in urine were far higher than those in serum, generally exceeding the minimal inhibitory concentrations for susceptible organisms during the 24 h after both the 1-and the 4-g dose. Piperacillin dosage modification is required only in patients with severe renal impairment.

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Section: Discussionmentioning

confidence: 54%

Pharmacokinetics of piperacillin in subjects with various degrees of renal function

Welling¹,

Craig²,

Bundtzen³

et al. 1983

Antimicrob Agents Chemother

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“…Piperacillin is a semisynthetic penicillin of the acylureidopenicillin group with broad‐spectrum activity that has been proven to afford enhanced protection against biliary tract pathogens 1–3 . Like other newer penicillins, piperacillin is excreted by both renal and biliary mechanisms.…”

Section: Introductionmentioning

confidence: 99%

“…Piperacillin is a semisynthetic penicillin of the acylureidopenicillin group with broad-spectrum activity that has been proven to afford enhanced protection against biliary tract pathogens. [1][2][3] Like other newer penicillins, piperacillin is excreted by both renal and biliary mechanisms. The primary route of elimination is by glomerular filtration, which results in a high urinary concentration of the unchanged compound, but the levels in the bile greatly exceed simultaneous serum concentrations.…”

Section: Introductionmentioning

confidence: 99%

Choleresis and inhibition of biliary lipid secretion induced by piperacillin in the rat

González

Mauriz

Jiménez

et al. 2002

Clin Exp Pharma Physio

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1. The effects of the administration piperacillin on bile flow and biliary lipid secretion were studied in male Wistar rats. 2. Intravenous injection of piperacillin at doses ranging from 0.3 to 3.0 mmol/kg bodyweight led to an increase in its biliary concentration and excretion rate. Maximal biliary excretion was reached at a dose of 2.0 mmol/kg piperacillin. 3. Excretion of the antibiotic into bile was associated with a marked choleresis. A linear relationship was observed between bile flow and piperacillin excretion, 5.7 micro L bile being produced per micro mol piperacillin excreted into the bile. 4. Continuous i.v. infusion of piperacillin at 2.0 mmol/100 g per min did not result in significant changes in bile acid or cholesterol secretion, but biliary phospholipid secretion was markedly reduced. The inhibitory effect on phospholipid secretion was also present when biliary lipid output had been previously increased by an infusion of taurocholate (200 nmol/100 g per min). Addition of taurocholate did not reverse the impairment of phospholipid secretion induced by piperacillin. 5. These results indicate that acute administration of piperacillin in the rat induces a marked choleresis by stimulating bile acid-independent bile flow. The significant impairment in phospholipid secretion suggests a specific effect on intracellular supply and/or translocation across the canalicular membrane.

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“…This is a unique property that has not been reported for any other antibiotic. Both ciprofloxacin and piperacillin are actively excreted in unobstructed bile ducts and reach bile-to-serum ratios of 25 to Ͼ50 (4,6,19,21). Piperacillin excretion in obstructed bile ducts, however, is greatly diminished (3,17).…”

mentioning

confidence: 99%

Biliary excretion of ciprofloxacin and piperacillin in the obstructed biliary tract

Hazel

Vries

Speelman

et al. 1996

Antimicrob Agents Chemother

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Biliary excretion of ciprofloxacin and piperacillin was determined in cholestatic patients who had undergone endoscopic cholangiography. The median concentration of ciprofloxacin (n = 9) was 2.36 micrograms/ml (range, 0.29 to 19.8 micrograms/ml) in bile compared with 1.66 micrograms/ml (range, 0.73 to 2.69 micrograms/ml) in serum. The median concentration of piperacillin (n = 7) was < 5 micrograms/ml (range, < 5 to 26) in bile compared with 14.3 micrograms/ml (range, 5.3 to 80) in serum. Ciprofloxacin, but not piperacillin, can be actively excreted into bile in the presence of a biliary tract obstruction.

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Piperacillin distribution into bile, gallbladder wall, abdominal skeletal muscle, and adipose tissue in surgical patients

Cited by 13 publications

References 6 publications

Pharmacokinetics of piperacillin in subjects with various degrees of renal function

Pharmacokinetics of piperacillin in subjects with various degrees of renal function

Choleresis and inhibition of biliary lipid secretion induced by piperacillin in the rat

Biliary excretion of ciprofloxacin and piperacillin in the obstructed biliary tract

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