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Pharmacodynamics and pharmacokinetics of oral nitrendipine solution in hypertensive patients with advanced renal failure

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Summary

Nitrendipine solution 5 mg·ml−1 in the dose of 5 mg was given orally to 20 patients with chronic renal failure and elevated diastolic blood pressure (≥110 mmHg), of whom 10 were on maintenance haemodialysis (endogenous creatinine clearance <5 ml·min−1) and 10 were at the predialysis stage (endogenous creatinine clearance 5–20 ml·min−1).

The aim of the study was to investigate the influence of kidney function and/or dialysis treatment on the pharmacokinetic and pharmacodynamic profile of a solution of nitrendipine and to assess its antihypertensive efficacy.

After 10 min there was a significant reduction in blood pressure from 188/113 to 173/100 (patients not dependent on dialysis) and from 197/112 to 161/94 mmHg (patients dependent on dialysis). The maximum fall in blood pressure (approximately 30%) was attained after 90 min in the dialysis patients and after 120 min in the non-dialysis group. Blood pressure increased again about 3 h after the administration of nitrendipine but it was still below baseline after 12 h. The terminal elimination half-life (4.1 h in the dialysis patients and 3.6 h in non-dialysis patients) was similar to that observed in patients with normal renal function. The pharmacokinetics of nitrendipine did not differ between the dialysis and non-dialysis groups. There was a correlation between plasma concentration and the blood pressure reduction. The maximum plasma concentration of nitrendipine was reached after 0.5 h (median) and did not differ between the two groups. The mean maximum plasma concentration was 14.8 μg·1−1 in the study population as a whole, with comparable means in the dialysis (17.3 μg·1−1) and non-dialysis (12.4 μg·1−1) groups.

The nitrendipine solution proved to be effective in lowering acutely elevated blood pressure in patients with advanced renal failure and renal hypertension, and was well tolerated. The pharmacokinetics was not affected by renal impairment or by dialysis.

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Authors and Affiliations

  1. Department of Internal Medicine II, Technical University, Aachen, Germany

    H. Kierdorf, A. Müller, B. Heintz & J. Kindler

  2. Bayropharm GmbH, Clinical Development, Leverkusen, Germany

    P. M. Blanke

  3. Medical Department, Bayer AG, Wuppertal, Germany

    J. Gellert, K. D. Rämsch & M. Wargenau

Authors
  1. H. Kierdorf
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  2. A. Müller
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  3. P. M. Blanke
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  4. J. Gellert
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  5. B. Heintz
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  6. K. D. Rämsch
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  7. M. Wargenau
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  8. J. Kindler
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Kierdorf, H., Müller, A., Blanke, P.M. et al. Pharmacodynamics and pharmacokinetics of oral nitrendipine solution in hypertensive patients with advanced renal failure. Eur J Clin Pharmacol 45, 129–134 (1993). https://doi.org/10.1007/BF00315493

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  • DOI: https://doi.org/10.1007/BF00315493

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