Effects of a selective adenosine A1 receptor antagonist on the development of cyclosporin nephrotoxicity

Br J Pharmacol. 1996 Mar;117(5):879-84. doi: 10.1111/j.1476-5381.1996.tb15275.x.

Abstract

1. The clinical application of cyclosporin as an immunosuppressive agent is limited by its nephrotoxicity. 2. The effect of FK453, a selective A1-receptor antagonist, administered twice daily to rats at a dose of 100 mg kg-1 was assessed on the development of nephrotoxicity induced by cyclosporin (10 mg kg-1 i.p. daily) administered for 14 days. The effects of nifedipine administered twice daily (0.3 mg kg-1 s.c.) for 14 days, on cyclosporin nephrotoxicity were also studied. 3. Cyclosporin induced a 46.58% and 35.78% decline in glomerular filtration rate (GFR) and effective renal plasma flow (ERPF) respectively and a reduction of 16.69% in filtration fraction (FF). Co-administration of FK453 resulted in falls of 30.5%, 18.59% and 14.7% in GFR, ERPF and FF respectively, the former two significantly less than the falls seen with cyclosporin (CyA) alone (P < 0.05 vs CyA, ANOVA). 4. Nifedipine appeared to have a more pronounced protective effect resulting in a decline of only 20.91% in GFR, with no significant change in ERPF (increase of 0.93%) when co-administered with CyA. 5. These observations indicate adenosine plays a minor role in the pathophysiology of CyA nephrotoxicity.

Publication types

  • Comparative Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Blood Pressure / drug effects
  • Cyclosporine / toxicity*
  • Drug Interactions
  • Glomerular Filtration Rate / drug effects
  • Immunosuppressive Agents / toxicity*
  • Kidney Diseases / chemically induced
  • Kidney Diseases / prevention & control*
  • Male
  • Nifedipine / pharmacology
  • Purinergic Antagonists*
  • Pyrazoles / pharmacology*
  • Pyridines / pharmacology*
  • Rats
  • Rats, Sprague-Dawley
  • Renal Plasma Flow, Effective / drug effects
  • Vasodilator Agents / pharmacology

Substances

  • Immunosuppressive Agents
  • Purinergic Antagonists
  • Pyrazoles
  • Pyridines
  • Vasodilator Agents
  • FK 453
  • Cyclosporine
  • Nifedipine