Adrenoceptors (ARs) consist of nine subtypes (alpha(1A)-, alpha(1B)-, alpha(1D)-, beta(1)-, beta(2)-, beta(3)-, alpha(2A)-, alpha(2B)- and alpha(2C)-AR), which are involved in a wide spectrum of physiological functions and are the site of action for a considerable percentage of currently prescribed therapeutics. With the exception of alpha(1D), all AR subtypes are polymorphic with genetic variations in the coding and non-coding regions. This review discusses the biochemical consequences of these genetic variations and their impact in receptor function, disease pathophysiology, and drug response. Pharmacogenomic principles that have been discovered are also discussed.