Early diagnosis and effective pharmacotherapy of arterial hypertension are urgent problems, a significant contribution to the solution of which can be made by metabolomics. The etiology of hypertension remains unknown for the majority of patients with high blood pressure; the diagnosis for 90% is defined as essential (primary) hypertension. This population is characterized by disturbance of the metabolic pathways of lipids, glucose, biogenic amines and amino acids, which may manifest with hyperlipidemia, hyperglycemia, and insulin resistance with the possible subsequent development of type II diabetes mellitus. The study of the metabolomic signature can provide a clue to the identification of biomarkers of hypertension and contribute to the effective development of preclinical diagnosis and identification of risk groups, as well as a more complete understanding of the etiological and pathogenetic mechanisms of increased blood pressure. Published studies indicate the existence of metabolome characteristic of hypertensive patients, distinguishing them from normotensive subjects. The most typical are changes involving amino acids, polyunsaturated fatty acids, carnitines, phosphatidylcholines, and acylglycerols. The variability of the response to antihypertensive therapy does not allow achieving effective control of blood pressure in a significant proportion of patients. The peculiarities of changes in the metabolome under the use of various pharmacological groups can be used to identify metabolite markers of the response to the main classes of antihypertensive drugs, as well as markers of the development of side effects of drug therapy. Thus, individualization of the pharmacotherapeutic approach based on pharmacometabolomics can significantly increase the efficacy and safety of antihypertensive therapy. This review aims to study the main groups of metabolites identified in published trials as predictors of the development of hypertension, as well as metabolite markers of response to antihypertensive therapy. © 2021, Remedium Group Ltd. All rights reserved.