Widespread in clinical practice, comorbid conditions and diseases, among which is the high prevalence of metabolic syndrome (MS), determine the need for selection of the optimal pharmacotherapy. The presence of certain liver diseases, including nonalcoholic fatty liver disease (NAFLD), may interfere with the processes of transformation of drugs, the metabolism of which occurs in the liver, which has been proved by experimental investigations. The article deals with the rational choice of antihypertensive drugs as a whole, and angiotensin-converting enzyme (ACE) in particular in patients with metabolic syndrome and NAFLD. Particular attention is paid to the possibilities of certain ACE inhibitors and their pharmacological properties.