Celiprolol is a beta-blocker for the management of hypertension and angina pectoris. It is simultaneously a selective β1 receptor antagonist, a β2 receptor partial agonist and a weak α2 receptor antagonist. The beta-2 agonist activity is thought to account for its mild vasodilating properties. It lowers blood pressure in hypertensive patients at rest and on exercise. The effects on heart rate and cardiac output are dependent on the pre-existing background level of sympathetic tone. Under conditions of stress such as exercise, celiprolol attenuates chronotropic and inotropic responses to sympathetic stimulation. However, at rest minimal impairment of cardiac function is seen. By blocking the beta-1 receptors the G signalling cascade is blocked, leading to decreased levels of intracellular calcium and muscle relaxation, therefore altering the heart rate. Celiprolol is administered as an oral capsule. Possible side effects of using celiprolol may include headache, hot flushes, dizziness, and fatigue.

Celiprolol B1-Adrenergic Cardiac Muscle Relaxation Pathway References