The value added by measuring myocardial contractility 'in vivo' in safety pharmacological profiling of drug candidates

J Pharmacol Toxicol Methods. 2007 Sep-Oct;56(2):203-11. doi: 10.1016/j.vascn.2007.03.004. Epub 2007 May 24.

Abstract

Introduction: The objective of this study was to define the normal LVdP/dt (an index of myocardial contractility)-heart rate relationship in telemetered conscious dogs, primates and mini-pigs in our laboratory and to use these data as the basis for an additional parameter useful in drug safety evaluation.

Methods: Trained dogs, Rhesus monkeys, Cynomolgus monkeys and mini-pigs (Goettinger) were equipped with radiotelemetry transmitters (ITS). Aortic pressure (AP), left ventricular pressure (LVP), a lead II ECG and body temperature could be continuously monitored. The contractility index LVdP/dtmax was derived from the LVP signal. Notocord HEM 4.1 software was used for data acquisition. For each species an LVdP/dt-heart rate relationship was evaluated using spontaneous heart rates (HR) throughout the observation period. A validation compound with positive inotropic effects (pimobendan) was then used to investigate the LVdP/dt-heart rate relationship.

Results: There was a clear LVdP/dt-HR relationship in the animals tested. The inotropic agent pimobendan demonstrated the expected shift in this relationship.

Discussion: Contractility of the myocardium is regulated by autonomic input activating primarily myocardial beta1-adrenoceptors, but it is also affected by the "force-frequency" relationship. Compounds can therefore either directly or indirectly affect the contractility of the heart. The chronotropic effects are routinely measured in preclinical studies; however, the inotropic effects are not routinely analysed in cardiovascular safety studies. Our experience strongly recommends including this evaluation for drug candidate selection. The evaluation of LVdP/dtmax, as an index of myocardial contractile state must, however, take into account its HR-dependency.

MeSH terms

  • Administration, Oral
  • Animals
  • Blood Pressure / drug effects*
  • Cardiotonic Agents / administration & dosage
  • Cardiotonic Agents / pharmacology
  • Dogs
  • Drug Evaluation, Preclinical / instrumentation
  • Drug Evaluation, Preclinical / methods
  • Electrocardiography / drug effects
  • Female
  • Heart Rate / drug effects*
  • Humans
  • Macaca fascicularis
  • Male
  • Myocardial Contraction / drug effects*
  • Pyridazines / administration & dosage
  • Pyridazines / pharmacology
  • Reproducibility of Results
  • Signal Processing, Computer-Assisted
  • Species Specificity
  • Swine
  • Swine, Miniature
  • Telemetry / instrumentation
  • Telemetry / methods*
  • Ventricular Function, Left / drug effects

Substances

  • Cardiotonic Agents
  • Pyridazines
  • pimobendan