Effect of caffeine on ceftriaxone disposition and plasma protein binding in the rat

Kwon K.I. and Bourne D.W.A. (1986) Effect of caffeine on ceftriaxone disposition and plasma protein binding in the rat. Journal of Pharmacokinetics and Biopharmaceutics, 14 4: 397-408. doi:10.1007/BF01059199

Author Kwon K.I.
Bourne D.W.A.
Title Effect of caffeine on ceftriaxone disposition and plasma protein binding in the rat
Journal name Journal of Pharmacokinetics and Biopharmaceutics   Check publisher's open access policy
ISSN 0090-466X
Publication date 1986-01-01
Sub-type Article (original research)
DOI 10.1007/BF01059199
Volume 14
Issue 4
Start page 397
End page 408
Total pages 12
Publisher Kluwer Academic Publishers-Plenum Publishers
Subject 3000 Pharmacology, Toxicology and Pharmaceutics
2736 Pharmacology (medical)
Abstract Previous studies have shown that caffeine can affect drug kinetics by altering drug binding to plasma protein, drug absorption, or drug distribution. In this study, the effect of caffeine on the in vivo protein binding and the disposition of ceftriaxone (a highly protein-bound cephalosporin) were investigated in the rat. Ceftriaxone 100mg/kg and caffeine 20mg/kg were i.v. injected via the tail vein and ceftriaxone in plasma, plasma filtrate, urine, feces, and tissues (brain, heart, kidney, liver, gut, lung, and muscle) was assayed by HPLC with UV detection. The fraction of free ceftriaxone in plasma ranged from 5.6 to 32.8% of total ceftriaxone (3-347 μg/ml) without caffeine and showed no alteration by caffeine. The total amount of ceftriaxone excreted in urine and feces was increased significantly (p<0.05)from 13.1±1.8mg (mean±SD, 54.6% of total) to 15.3 ±1.1 mg (63.8% of total) by caffeine coadministration. The terminal half-life of ceftriaxone in plasma was shortened from 59 to 47 min, and the area under the plasma drug concentration-time curve (AUC)was reduced from 612 to 516 μg hr/ml Although the peak drug concentrations and the times of peak concentration of ceftriaxone in tissues were not altered by caffeine administration, the elimination of ceftriaxone was increased, as indicated by generally shorter half-lives (decreases ranged from 17.5% in liver to 34.2% in brain) and lower AUC values (from 9.0% in heart to 54.5% in brain). These results suggest that caffeine does not alter the protein binding of ceftriaxone, but enhances the elimination of ceftriaxone in the rat.
Keyword caffeine
compartment model
protein binding
Q-Index Code C1
Q-Index Status Provisional Code
Institutional Status Unknown

Document type: Journal Article
Sub-type: Article (original research)
Collection: Scopus Import
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Citation counts: TR Web of Science Citation Count  Cited 6 times in Thomson Reuters Web of Science Article | Citations
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