Although exercise remains the preferred method of cardiac stress testing, pharmacological stress plays an important role in nuclear cardiology. The globally ageing population will see an expansion of the application of pharmacological stress testing, and with this, comes the need to understand the pharmacological basis, mechanisms of action, potential interactions and adverse effects to inform usage in less-than-ideal circumstances. This study aims to enhance the decision-making process in day-to-day clinical nuclear cardiology practice through a better understanding of nuances relevant to the pharmacological agents used for cardiac stress testing.