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Nephroprotective effect of betamipron on a new carbapenem, DA-1131, in rabbits.

Abstract
The nephroprotective effect of betamipron (200 mg/kg) was evaluated after intravenous administration of a high dose of DA-1131 (200 mg/kg) to rabbits. Extensive tubular necrosis was observed without betamipron but the necrosis was not observed with betamipron at 8 h after intravenous administration of DA-1131 based on kidney microscopy. By treatment with betamipron, the amounts and tissue to plasma (T/P) ratios of DA-1131 in renal cortex and whole kidney decreased significantly (65-91% decrease) at both 30 min and 2 h after intravenous administration of the drug to rabbits. This indicated that the accumulation of DA-1131 in rabbit renal cortex and whole kidney was inhibited by betamipron. This resulted in significantly greater percentages of intravenous DA-1131 excreted in urine as unchanged drug, 60.9 versus 40.1%, and significantly faster renal clearance (Cl(r)) of DA-1131 (6.10 versus 3.22 mL/min/kg) by treatment with betamipron. By treatment with betamipron, the amounts and T/P ratios of DA-1131 in renal cortex and whole kidney decreased significantly from 30 min and the renal function remained intact at 8 h after intravenous administration of DA-1131. The above data suggested that the nephroprotective effect of betamipron was fast and persisted for a long period of time in rabbits.
AuthorsS H Kim, W B Kim, J W Kwon, M G Lee
JournalBiopharmaceutics & drug disposition (Biopharm Drug Dispos) Vol. 20 Issue 3 Pg. 125-9 (Apr 1999) ISSN: 0142-2782 [Print] England
PMID10211864 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
Chemical References
  • Carbapenems
  • DA 1131
  • Protective Agents
  • N-benzoylalanine
  • Alanine
Topics
  • Alanine (analogs & derivatives, therapeutic use)
  • Animals
  • Carbapenems (adverse effects, pharmacokinetics)
  • Drug Interactions
  • Kidney Function Tests
  • Kidney Tubular Necrosis, Acute (chemically induced, prevention & control)
  • Male
  • Protective Agents (therapeutic use)
  • Rabbits

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