Beta-blockers are heterogeneous pharmacological drug group which are used in treatment of hypertension, angina and acute coronary syndrome, supraventricular and ventricular arrhythmias and congestive heart failure. Classification, pharmacodynamics, and pharmacokinetics of beta-blockers are summarized in this review. Advantages and deficiencies of the full and partial antagonists, selective and nonselective, lipophilic and hydrophilic, as well as peripheral vasodilator actions of beta-blocker -blockers are discussed. The underlying sub cellular mechanisms of beta-blockers leading to the vasodilatation are presented.