The nephrotoxic adverse effect of cyclosporine in renal transplantation may be counteracted by calcium antagonists. The effect of a single oral dose of 10 mg of the calcium antagonist felodipine or placebo was studied in ten cyclosporine-treated renal transplant recipients before, during, and after an acute intravenous infusion of cyclosporine in a randomized, single-blind crossover study. Glomerular filtration rate, and renal plasma flow, and tubular function evaluated by the lithium clearance technique were determined. Both glomerular filtration rate, renal plasma flow, urinary sodium excretion, fractional excretion of sodium, and lithium clearance increased after felodipine, whereas proximal and distal fractional reabsorption and blood pressure were reduced. Intravenous infusion of cyclosporine per se did not influence any of the parameters. It is concluded that a single dose of felodipine in cyclosporine-treated renal transplant recipients has beneficial effects on renal hemodynamics, tubular function and blood pressure. It is suggested that these effects result from a direct vasodilatation and an effect on tubular function, and that felodipine given intravenously seems to antagonize at least some of the nephrotoxic effects of cyclosporine.