The pharmacodynamics and pharmacokinetics of a new calcium antagonist nisoldipine in normotensive and hypertensive subjects
The pharmacodynamic and pharmacokinetic profiles of nifedipine and nisoldipine were compared in a double blind, placebo-controlled study. Nisoldipine, 10 mg significantly reduced systolic blood pressure but nifedipine 20 mg retard did not, although both drugs had significant pharmacodynamic effects as evidenced by increased heart rates. The terminal elimination half-life in plasma was similar for both drugs with a mean of 2 h. The pharmacodynamics of nisoldipine were studied in 8 hypertensives following both acute and chronic administration. Antihypertensive efficacy was demonstrated after acute dosing and was maintained over 4 weeks of twice daily treatment as monotherapy.
Key wordsnisoldipine nifedipine pharmacokinetics pharmacodynamics calcium channel blocking drugs hypertension side-effects
Unable to display preview. Download preview PDF.
- 1.Kazda S, Garthoff B, Meyer H, Schlobmonn K, Stoepel K, Towart R, Vater W, Welringer E (1980) Pharmacology of a new calcium antagonistic compound. Isobutyl methyl 1,4-dihydro-2-6-dimethyl-4-(2-nitrophenyl)-3,5-pyridinedecarboxylate (Nisoldipine, Bay K5552). Arzneimittelforsch Drug Res 30 (II), : 2144–2162Google Scholar
- 2.Maxwell GM, Crompton S, Rencis V (1982) Effect of nisoldipine upon the general and coronary haemodynamics of the anaesthetized dog. J Cardiovasc Pharmacol 43: 393–397Google Scholar
- 3.Warltier DC, Meils CM, Garrett JG, Brooks HL (1981) Blood flow in normal and acutely ischaemic myocardium after verapamil, diltiamem and nisoldipine (Bay K 5552), a new dihydropyridine calcium antagonist. J Pharmacol Exp Ther 218 : 296–302Google Scholar
- 4.Hamann SR, McAllister RG (1983) Measurement of Nifedipine in plasma by gas-liquid chromatography and electron capture detection. Clin Chem 29 : 158–160Google Scholar
- 5.Millar JA, McLean KA, Sumner DJ, Reid JL (1983) The effect of the calcium antagonist nifedipine on pressor and aldosterone responses to angiotensin II in normal man. Eur J Clin Pharmacol 24: 315–321Google Scholar
- 6.MacGregor GA, Rotellar C, Markandu ND, Smith SJ, Sagnella AG (1982) Contrasting effects of nifedipine, captopril and propranalol in normotensive and hypertensive subjects. J Cardiovasc Pharmacol 4: S358–362Google Scholar
- 7.Littler WA, Watson RDS, Stallard TJ, McLeary RAB (1983) The effect of nifedipine on arterial pressure and reflex cardiac control. Postgrad Med J 59 [Suppl 2]: 109–112Google Scholar
- 8.Young MA, Watson RDS, Littler WA (1984) Baroreflex setting and sensitivity after acute and chronic nicardipine therapy. Clin Sci 66: 233–235Google Scholar
- 9.Pasanisi F, Reid JL (1983) Plasma nifedipine levels and fall in blood pressure in a 53 year old woman. Eur J Clin Pharmacol 25: 143–144Google Scholar