A regular exercising activity is a fundamental non-pharmacological approach to the treatment of patients with cardiovascular diseases including hypertension. Despite a positive influence of regular sport on blood pressure decrease, very often we cannot avoid using drugs – antihypertensives. Pharmacological treatment of hypertension in population of physically active individuals and sportsmen require a specific approach in use of appropriate medication, i.e. treatment tailored for a given patient. Selection of suitable antihypertensives comes from general recommended procedures for the treatment of high blood pressure. The most frequent groups of drugs are ACEI, sartans, calcium channel blockers, thiazide diuretics and betablockers. When using them it is necessary to take into consideration the risk of unfavourable effects. Mainly diuretics and betablockers are medicaments which may unfavourably influence highly intensive physical activity. What is more, both groups are in the list of forbidden supportive remedies (doping) and its use is controlled by certain rules in top sportsmen. Their most frequent use is in combined approach in resistant hypertension or in specific situations – typically beta1 selective blockers in ischaemic heart disease or both mentioned groups in chronic heart failure. Contrary, an interesting choice from betablockers in the treatment of hypertension might be representatives of a subgroup of drugs with intrinsic sympathomimetic activity (so-called ISA) or direct vasodilating effect. Other groups of antihypertensives as central blockers of the sympathetic nervous system, aldosterone blockers or alphalytic agents are used in combined treatment in resistant hypertension or in special situations (secondary hypertension).