Cardiovascular diseases are the leading cause of mortality, and the medications used in their therapy are among the most widely used drugs in the world. They play a crucial role in controlling symptoms, treating the disease, slowing its progression, and reducing the risk of serious complications. These medications can be categorized into several groups based on therapeutic goals and mechanisms of action: antihypertensives (angiotensin-converting enzyme inhibitors (ACE inhibitors), angiotensin II receptor blockers (ARBs), adrenergic receptor blockers, calcium channel blockers), antithrombotics (anticoagulants, platelet aggregation inhibitors), antiarrhythmics, hypolipidemics, and diuretics. The aim of this thesis was to present the metabolism of these groups of drugs used in the treatment of cardiovascular diseases, with a focus on biotransformation reactions, properties of metabolites, and enzymes involved in biotransformation. Factors that may influence variability in therapeutic response, such as genetic polymorphisms of enzymes and drug-drug interactions, were also described. The literature review results emphasize the importance of understanding drug metabolism and the individualized approach to therapy in accordance with existing comorbidities and patient-specific characteristics.