Receptors and ion channels are key targets for commonly used drugs in anaesthesia and intensive care medicine, with drugs interacting with targets as agonists, antagonists or inverse agonists to exert their physiological effects. This article introduces the basic concepts of drug affinity, efficacy and potency and how these principals relate to the mechanism of action of select drugs. Drug–receptor interaction is described for intracellular receptors, nuclear receptors and G-protein-coupled receptors (GPCRs), including a discussion of receptor structure and examples of intracellular signaling pathways that control cellular function. The article also explores voltage-gated and ligand-gated ion channels, with discussion of how the activity of these ion channels is governed by changes in the membrane potential. Voltage-gated sodium, potassium and calcium ion channels are discussed, in addition to major excitatory (e.g. N-methyl-D-aspartate (NMDA) receptors) and inhibitory (e.g. γ-aminobutyric acid A (GABAA) receptors) ligand-gated ion channels that constitute targets for a variety of drugs including examples used in anaesthesia and intensive care medicine.
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