Mechanism of action<unk>  is cardioprotective because it selectively and competitively blocks catecholamine (adrenaline) stimulation of β1 adrenergic receptors (adrenoreceptors), which are mainly found in the heart muscle cells and heart conduction tissue (cardiospecific), but also found in juxtaglomerular cells in the kidney. Normally, adrenaline and noradrenaline stimulation of the β1 adrenoreceptor activates a signalling cascade (Gs protein and cAMP) which ultimately leads to increased contractility and increased heart rate of the heart muscle and heart pacemaker, respectively.<unk>  competitively blocks the activation of this cascade, so decreases the adrenergic tone/stimulation of the heart muscle and pacemaker cells. Decreased adrenergic tone shows less contractility of heart muscle and lowered heart rate of pacemakers. β1-selectivity Selectivity of various β-blockers<unk>  β1-selectivity is especially important in comparison to other nonselective beta blockers. The effects of the drug are limited to areas containing β1 adrenoreceptors, which is mainly the heart and part of the kidney.<unk>  minimizes the side effects that might occur from administration of a nonspecific beta blocker where blockage of the other adrenoreceptors (β2, β3, α1, α2) occurs. The other receptors elicit a variety of responses in the body, and their blockage could cause a wide range of reactions, but β1 adrenoreceptors are cardiospecific for the most part, making<unk>  ideal for treatment of cardiac events.<unk>  has a higher degree of β1-selectivity compared to other β1-selective beta blockers such as atenolol, metoprolol, and betaxolol. However nebivolol is approximately 3.5 times more β1-selective. Renin-angiotensin system<unk>  inhibits renin secretion by about 65% and tachycardia by about 30%. Pharmacokinetics<unk>  has both lipid- and water-soluble properties. It has an approximate half-life of 10–12 hours, and when ingested has high bioavailability (approx. 90%). When being eliminated, the body evenly distributes it (50–50) between kidney excretion and liver biotransformation (then excreted).
Bisoprolol
Metoprolol
Sotalol
Digoxin
Carvedilol
Digitoxin
Amiodarone
Diltiazem