Advertisement

Clinical Pharmacology of Nisoldipine Coat Core

Conference paper
  • 31 Downloads

Abstract

Nisoldipine is a second-generation dihydropyridine calcium antagonist structurally related to nifedipine and used in the treatment of stable angina and arterial hypertension. It is also under investigation for the treatment of left ventricular dysfunction. It was first developed as an immediate release tablet, but this formulation was not considered optimal for once-daily administration because of the variable results obtained at peak and trough in clinical studies. Consequently, nisoldipine coat core (CC) was developed with the aim of optimizing the drug’s time-effect profile over the 24-h dosing interval. The in vitro release pattern classifies this tablet as an “extended release” formulation according to European Community guidelines. The present article outlines the pharmacokinetic and pharmacodynamic profiles of nisoldipine CC, as obtained from recent clinical studies. (Am J Cardiol 1995; 75:41 E-45E)

Keywords

Cold Pressure Test Release Tablet Dihydropyridine Calcium Antagonist Supine Diastolic Blood Pressure Nisoldipine Coat Core 
These keywords were added by machine and not by the authors. This process is experimental and the keywords may be updated as the learning algorithm improves.

Preview

Unable to display preview. Download preview PDF.

Unable to display preview. Download preview PDF.

References

  1. 1.
    Lasseter KC, Shamblen EC, Lettieri J, Kml G, Taylor RJ, Fein SH (1987) Dose-proportional pharmacokinetics of nisoldipine in healthy volunteers. Clin Pharmacol Ther 41: 234Google Scholar
  2. 2.
    Edgar B, Bailey D, Bergstrand R, Johnsson G, Regardh CG (1992) Acute effects of drinking grapefruit juice on the pharmacokinetics and dynamics of felodipineand its potential clinical relevance. Eur J Pharmacol 42: 313–317Google Scholar
  3. 3.
    Bolaert J, Valcke Y, Dammekens H, Devries G, Schurgers M, Daneels R, Bogaert MG (1988) Pharmacokinetics of nisoldipine in renal dysfunction. Eur J Clin Pharmacol 34: 207–209CrossRefGoogle Scholar
  4. 4.
    Breimer DD, Lodewijks MTM, Van Brummelen P, Van Harten J, Wilson JPH (1986) Pharmacokinetics and haemodynanic effects of nisoldipine in patients with liver cirrhosis. BrJ Pharmacol 89 (Suppl): 482Google Scholar
  5. 5.
    Joeres R, Ahr G, Hofstetter G, Klinker H, Richter E (1987) Steady state pharmacokinetics of nisoldipine in patients with liver disease. In: Hugenholtz PG, Meyer J, eds. Nisoldipine 1987. Berlin-Heidelberg: Springer-Verlag 80–84Google Scholar
  6. 6.
    Van Harten J, Van Brummelen P, Van Wilson JHP, Lodewijks MTM, Breimer DD (1988) Nisoldipine: kinetics and effects on blood pressure and heart rate in patients with liver cirrhosis after intravenous and oral administration. Eur J Clin Pharmacol 34: 387–394PubMedCrossRefGoogle Scholar
  7. 7.
    Elliott HL, Meredith PA, McNally C, Reid JL (1991) The interactions between nisoldipine and two ß-adrenoceptor antagonists, atenolol and propranolol. Br J Clin Pharmacol 32: 279–385Google Scholar
  8. 8.
    Levine MAH, Ogilive RI, Leenen FHH (1988) Pharmacokinetic and pharmacodynamic interactions between nisoldipine and propranolol. Clin Pharmacol 7her 43: 39–48CrossRefGoogle Scholar
  9. 9.
    Shaw-Stiffel TA, Browning FM, Holliwell DL, Ogilvie RI, Leenen FHH (1989) Pharmacokinetic and pharmacodynamic interaction between nisoldipine and propranolol during chronic dosing. Clin Invest Med 12 (Suppl 4): 314Google Scholar
  10. 10.
    Kirch W, Stenzel J, Dylewicz P, Hutt HJ, Santos SR, Ohenhaus EE (1986) Influence of nisoldipine on haemodynamic effects and plasma levels of digoxine. Br J Clin Pharmacol 22: 155–159PubMedGoogle Scholar
  11. 11.
    Kuhlmann J, Ziegler R, Wingender W, Ramsch KD, Ahr G (1986) Beeinflussen Nisoldipine, Nitrendipie and Nimodipin die Pharmakokinetik and Wirksamkeit von Herzglykosiden? Z Kardiol 75 (Suppl 4): 78Google Scholar
  12. 12.
    Van Harten J, Van Brummelen P, Danhof M, Lodewijks MTM, Breimer DD (1986) Pharmacokinetics and haemodynamic effects of nisoldipine and its interaction with cimetidine in healthy volunteers. Acta Pharmacol Toxicol 59 (Suppl 5): 314Google Scholar
  13. 13.
    Van Harten J, Van Brummelen P, Danhof M, Lodewijks MTM, Breimer DD (1988) Pharmacokinetics and haemodynamic effects of nisoldipine and its interaction with cimetidine. Clin Pharmacol Ther 43: 332–341PubMedCrossRefGoogle Scholar
  14. 14.
    Godfraind T, Egleme C, Finet M, Jaumin P (1987) The action of nifedipine and nisoldipine on the contractile activity of human coronary arteries and human cardiac tissue in vitro. Pharm Toxicol 61: 79–84CrossRefGoogle Scholar
  15. 15.
    Godfraind T (1994) Cardioselectivity of calcium antagonists Cardiovasc Drugs Ther 8: 353–364PubMedCrossRefGoogle Scholar
  16. 16.
    Friedel HA, Sorkin EM (1988) Nisoldipine–a preliminary review of its pharmacodynamic and pharmacokinetic properties and therapeutic efficiency in the treatment of anginal pectoris, hypertension and related cardiovascular disorders. Drug 36: 682–731CrossRefGoogle Scholar
  17. 17.
    The Defiant Research Group (1992) Improved diastolic function with the calcium antagonist nisoldipine (coat-core) in patients with post myocardial infarction: results of the DEFIANT Study. Eur Heart J 13: 1496–1505Google Scholar
  18. 18.
    Pouleur H, Van Eyll C, Gurne O, Rousseau MF (1992) Analysis of the mechanisms underlying the changes in left ventricular filling dynamics during oral nisoldipine therapy in patients with anterior myocardial infarction. Eur Heart J 13: 952–959PubMedGoogle Scholar
  19. 19.
    Dymond DS, Caplin JL, O’Keefe JC, Banim S (1987) Effects of nisoldipine on left ventricular function during exercise or cold pressor stress. Eur Heart J 8 (Suppl K): 27–33PubMedGoogle Scholar
  20. 20.
    Mindejahn KP, Hanrath P, Thier W, Bleifeld W (1983) Hemodynamic effect of nisoldipine in chronic congestive heart failure. (Abstr.) Eur Heart J 4 (Suppl E): 26Google Scholar
  21. 21.
    Barjon JN, Rouleau JL, Bichet D, Juneau C, De Champlain J (1987) Chronic renal and neurohumoral effects of the calcium entry blocker nisoldipine in patients with congestive heart failure. J Am Coll Cardiol 9: 622–630PubMedCrossRefGoogle Scholar
  22. 22.
    Rousseau MF, Vincent MF, Van Hoof F, Van Den Berghe G, Charlier AA, Pouleur H (1984) Effects of nicardipine and nisoldipine on myocardial metabolism, coronary blood flow and oxygen supply in angina pectoris. Am J Cardiol 54: 1189–1194PubMedCrossRefGoogle Scholar
  23. 23.
    Lewis BS, Schefer A, Merdier A, Flugelman M, Hardoff R, Halon DA (1987) Acute effects of intravenous nisoldipine on hemodynamics and left ventricular function in cardiac failure. In: Hugenholtz PG, Meyer J, eds. Nisoldipine 1987. Berlin-Heidelberg. Springer-Verlag, 315–323CrossRefGoogle Scholar
  24. 24.
    Serruys PW, Suryapranata H, Planellas J, Wijns W, Vanhaleweyk GLJ, Soward A, Jaski BE, Hugenholtz PG (1985) Acute effects of intravenous nisoldipine on left ventricular function and coronary hemodynamics. Am J Cardiol 56: 140–146PubMedCrossRefGoogle Scholar
  25. 25.
    Meredith PA, Pasanisi F, Elliott HL, Reid JL (1985) The effect of nisoldipine on apparent liver blood flow and effective renal plasma flow. Br J Clin Pharmacol 20: 235–237PubMedGoogle Scholar

Copyright information

© Springer-Verlag Berlin Heidelberg 1999

Authors and Affiliations

There are no affiliations available

Personalised recommendations