PLASMA TURNOVER OF METHYLDOPA IN ADVANCED RENAL FAILURE

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Abstract
Methyldopa is one of the most useful drugs for treatment of hypertension in patients with reduced renal function. Few data are available on the metabolism of this drug in renal failure, therefore the plasma turnover rate has been determined in 8 patients with advanced renal failure and 11 cases with essential hypertension with no or only slightly reduced renal function. In both groups of patients a biphasic plasma elimination first was obtained after i.v. injection of the drug. The first, and quantitatively most important, part of the curve showed a half‐life of 3.6 hours in advanced renal failure compared to 1.7 in essential hypertension. A fairly good correlation was demonstrated between the half‐life of the drug in plasma according to the initial disappearance rate and the endogenous creatinine clearance. In patients with renal failure only 50–60% of the drug injected was eliminated during the initial phase, the remainder disappeared even more slowly. The slow, second phase of the elimination curve was also exponential with a slope corresponding to a T/2 of 7–16 hours. In patients with a drug was nearly normal renal function about 95% of the drug was eliminated during the rapid, initial phase. Our findings are in good agreement with the drug accumulation occurring in renal failure.

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