PMID: 3766146Jul 1, 1986Paper

Felodipine, pharmacodynamics and pharmacokinetics in the isolated rabbit heart

Acta Pharmacologica Et Toxicologica
J Askholt, F Nielsen-Kudsk

Abstract

Myocardial pharmacodynamics of the Ca2+-antagonist felodipine, a structural analogue of nifedipine, were studied in isolated, spontaneously beating and retrogradely perfused rabbit hearts. The concentration of felodipine in the Krebs-Henseleit perfusion liquid was stepwise increased from 0.7 ng/ml to 90.4 ng/ml (1.8 to 235.3 nmol/l). Increasing felodipine concentrations from 0.7 to 3.6 ng/ml produced an increase of up to 115% in coronary flow rate, which then decreased at higher concentrations to 84% of the control value. Oxygen consumption decreased progressively to 28% at concentrations from 3.6 to 90.4 ng/ml. Myocardial contractility measured by amplitude and rate of contraction decreased progressively to 45.7 and 41.5%, respectively, at concentrations from 0.7 to 9.4 ng/ml and further to 4.0 and 3.0%, respectively, at 90.4 ng/ml. Myocardial efficiency expressed as the percentual ratio of contraction amplitude times frequency to oxygen consumption decreased to 11% at the highest concentration of felodipine. Heart beat frequency decreased simultaneously to 45.6%. The electrocardiographic PQ and QRS intervals increased at the highest concentration to 174 and 111%, respectively, whereas the QT interval decreased to 86.6%. Asyst...Continue Reading

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Citations

Aug 1, 1989·British Journal of Pharmacology·S Herzig, H Lüllmann
Mar 1, 1987·British Journal of Pharmacology·H Lüllmann, K Mohr
Sep 1, 1988·Pharmacology & Toxicology·J E Nielsen-Kudsk, J Askholt
Aug 1, 1988·Pharmacology & Toxicology·F Nielsen-KudskP Jakobsen
Mar 1, 1988·Pharmacology & Toxicology·H K Jensen, F Nielsen-Kudsk

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