Nebivolol

Nebivolol is a beta blocker used to treat high blood pressure and heart failure. As with other β-blockers, it is generally a less preferred treatment for high blood pressure. It may be used by itself or with other blood pressure medication. It is taken by mouth. Nebivolol is a beta blocker used to treat high blood pressure and heart failure. As with other β-blockers, it is generally a less preferred treatment for high blood pressure. It may be used by itself or with other blood pressure medication. It is taken by mouth. Common side effects include dizziness, feeling tired, nausea, and headaches. Serious side effects may include heart failure and bronchospasm. Its use in pregnancy and breastfeeding is not recommended. It works by blocking β1-adrenergic receptors in the heart and dilating blood vessels. Nebivolol was patented in 1983 and came into medical use in 1997. It is available as a generic medication in the United Kingdom. A month supply in the United Kingdom costs the NHS about 0.89 £ as of 2019. In the United States the wholesale cost of this amount is about US$128.00. In 2016 it was the 126th most prescribed medication in the United States with more than 5 million prescriptions. It is used to treat high blood pressure and heart failure. ACE inhibitors, angiotensin II receptor antagonists, calcium-channel blockers, and thiazide diuretics are generally preferred over beta blockers for the treatment of high blood pressure. Beta blockers help patients with cardiovascular disease by blocking β receptors, while many of the side-effects of these medications are caused by their blockade of β2 receptors. For this reason, beta blockers that selectively block β1 adrenergic receptors (termed cardioselective or β1-selective beta blockers) produce fewer adverse effects (for instance, bronchoconstriction) than those drugs that non-selectively block both β1 and β2 receptors. In a laboratory experiment conducted on biopsied heart tissue, nebivolol proved to be the most β1-selective of the β-blockers tested, being approximately 3.5 times more β1-selective than bisoprolol. However, the drug's receptor selectivity in humans is more complex and depends on the drug dose and the genetic profile of the patient taking the medication. The drug is highly cardioselective at 5 mg. In addition, at doses above 10 mg, nebivolol loses its cardioselectivity and blocks both β1 and β2 receptors. (While the recommended starting dose of nebivolol is 5 mg, sufficient control of blood pressure may require doses up to 40 mg). Furthermore, nebivolol is also not cardioselective when taken by patients with a genetic makeup that makes them 'poor metabolizers' of nebivolol (and other drugs) or with CYP2D6 inhibitors. As many as 1 in 10 whites and even more blacks are poor CYP2D6 metabolizers and therefore might benefit less from nebivolol's cardioselectivity although currently there are no directly comparable studies. Due to enzymatic inhibition, fluvoxamine increases the exposure to nebivolol and its active hydroxylated metabolite (4-OH-nebivolol) in healthy volunteers. Nebivolol is unique as a beta-blocker. Unlike carvedilol, it has a nitric oxide (NO)-potentiating, vasodilatory effect via stimulation of β3 receptors. Along with labetalol, celiprolol and carvedilol, it is one of four beta blockers to cause dilation of blood vessels in addition to effects on the heart.