In the urinary bladder it is thought to cause relaxation of the bladder and prevention of urination.Due to enzymatic inhibition, fluvoxamine increases the exposure to nebivolol and its active hydroxylated metabolite (4-OH-nebivolol) in healthy volunteers. Vasodilator action
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. Antihypertensive effect
Nebivolol lowers blood pressure (BP) by reducing peripheral vascular resistance, and significantly increases stroke volume with preservation of cardiac output. The net hemodynamic effect of nebivolol is the result of a balance between the depressant effects of beta-blockade and an action that maintains cardiac output. Antihypertensive responses were significantly higher with nebivolol than with placebo in trials enrolling patient groups considered representative of the U.S. hypertensive population, in black people, and in those receiving concurrent treatment with other antihypertensive drugs. Pharmacokinetics
Nebivolol plasma protein binding is approximately 98%, mostly to albumin and its half-life of low doses is 12 hours in extensive CYP2D6 metabolizers and 19 hours in poor metabolizers. Contraindications
Severe bradycardia
Heart block greater than first degree
Patients with cardiogenic shock
Decompensated cardiac failure
Sick sinus syndrome (unless a permanent pacemaker is in place)
Patients with severe hepatic impairment (Child-Pugh class B)
Patients who are hypersensitive to any component of this product. Side effects
Side effects might include headache, tiredness, dizziness, lightheadedness, reduced blood flow to extremities, bradycardia.
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. In 2019, it was the 191st most commonly prescribed medication in the United States, with more than 3 million prescriptions. Medical uses
It is used to treat high blood pressure and heart failure. Nebivolol is used in the treatment of angina, to decrease the heart rate and contractile force. This is relevant in patients who need to decrease the oxygen demand of the heart so that the blood supplied from stenosed or constricted arteries is adequate. ACE inhibitors, angiotensin II receptor antagonists, calcium-channel blockers, and thiazide diuretics are generally preferred over beta blockers for the treatment of primary hypertension in the absence of co-morbidities. Pharmacology and biochemistry
β1-selectivity
Beta blockers help patients with cardiovascular disease by blocking β1 receptors, while many of the side-effects of these medications are caused by their blockade of β2 receptors.