Hypertension is a leading age‑related disease in our society and if left untreated, leads to fatal
cardiovascular complications. The prevalence of hypertension has increased and becomes a
significant global health economic burden, particularly in lower‑income societies. Many loci associated
with blood pressure and hypertension have been reported by genome‑wide association studies that
provided potential targets for pharmacotherapy. Pharmacogenetic research had shown interindividual
variations in drug efficacy, safety, and tolerability. This could be due to genetic polymorphisms in
the pharmacokinetics (genes involved in a transporter, plasma protein binding, and metabolism)
or pharmacodynamic pathway (receptors, ion channels, enzymes). Pharmacogenetics promises
great hope toward targeted therapy, but challenges remain in implementing pharmacogenetic aided
antihypertensive therapy in clinical practice. Using various databases, we analyzed the underlying
mechanisms between the candidate gene polymorphisms and antihypertensive drug interactions and
the challenges of implementing precision medicine. We review the emergence of pharmacogenetics
and its relevance to clinical pharmacological practice.