Drug information of Nebivolol
Mechanism of effect
Nebivolol is a selective β1-receptor antagonist. Activation of β1-receptors by epinephrine increases the heart rate and the blood pressure, and the heart consumes more oxygen. Nebivolol blocks these receptors which reverses the effects of epinephrine, lowering the heart rate and blood pressure. In addition, beta blockers prevent the release of renin, which is a hormone produced by the kidneys which leads to constriction of blood vessels. At high enough concentrations, this drug may also bind beta 2 receptors.
Nebivolol is a competitive and highly selective beta-1 receptor antagonist with mild vasodilating properties, possibly due to an interaction with the L-arginine/nitric oxide pathway. In preclinical studies, nebivolol has been shown to induce endothelium-dependent arterial relaxation in a dose dependent manner, by stimulation of the release of endothelial nitric oxide. Nitric oxide acts to relax vascular smooth muscle cells and inhibits platelet aggregation and adhesion.
Bioavailability: Extensive metabolizers, 12%; poor metabolizers, 96%
Peak plasma time: 1.5-4 hr
Protein bound: 98%
Vd: 8-12 L/kg
Metabolism: Metabolized by CYP2D6 via alicyclic and aromatic hydroxylation, N-dealkylation, glucuronidation
Half-life: Extensive metabolizers, 10-12 hr; poor metabolizers, 19-32 hr
Excretion: Urine (38-67%), feces (13-44%)
Drug indicationsHigh Blood Pressure
5 mg/day PO; may be increased every 2 weeks; not to exceed 40 mg/day
Safety and efficacy not established
Drug contraindicationsovert cardiac failure , Sick sinus syndrome , Hypersensitivity
Side effectsInsomnia , Diarrhea , Headache , nausea , vertigo , asthenia , Peripheral edema , hypertriglyceridemia , tiredness
InteractionsDrospirenone , Doxazosin , Dolasetron , lipiodol , Atenolol , Betaxolol , Paroxetine , Timolol , Digoxin , Diltiazem , lofexidine , lumefantrine , Celiprolol , Penbutolol , Lumefantrine / artemether , Esmolol , Nadolol , Dacomitinib , Carvedilol , Clonidine , Bisoprolol , Quinidine , Acebutolol , Pindolol , Rivastigmine , Sotalol , Fluoxetine , Labetalol , Metoprolol , Verapamil , ProHance , Treprostinil , Naltrexone and Bupropion , Oxtriphylline , lasmiditan
Anesthetics that cause myocardial depression, bradycardia, 1° heart block, ischemic heart disease, Prinzmetal angina, untreated congestive heart failure (CHF)
Patients with bronchospastic disease should not receive beta-blockers; patients with bronchospastic disease who do not respond to other therapies, initial low doses may be employed and used cautiously; monitor closely; patient should have immediate access to beta2-agonist
May mask hyperthyroidism, including tachycardia; abrupt withdrawal may exacerbate symptoms of hyperthyroidism or precipitate thyroid storm; if thyrotoxicosis suspected, carefully manage and treat
Severe renal impairment decreases clearance; adjust dose in severe renal failure
Moderate hepatic impairment decreases metabolism ; adjust dose in moderate hepatic impairment (Child-Pugh class B); contraindicated in severe hepatic impairment (Child-Pugh class C)
May potentiate hypoglycemia in patients with hypoglycemia and/or mask signs and symptoms
Sudden discontinuance can exacerbate angina and lead to MI; to discontinue therapy, taper gradually over 1-2 weeks to avoid acute tachycardia, ischemia, and/or hypertension; temporary but prompt resumption of beta-blocker therapy may be necessary if angina symptoms or acute coronary insufficiency symptoms worsen
Can precipitate or worsen symptoms of arterial insufficiency in patients with peripheral and Raynaud disease (intermittent claudication); use caution; monitor for progression of arterial obstruction
Renal disease, cerebrovascular insufficiency, use in pheochromocytoma (alpha blocker should be started before beta blocker)
Increased risk of stroke after surgery; routine withdrawal of chronic beta-blocker therapy not recommended prior to major surgery
Use with caution in patients with myasthenia gravis
Use with caution in patients taking calcium-channel blockers or cardiac glycosides or using inhaled anesthetics
Drug loses receptor selectivity in poor metabolizers and in high doses (blocks both beta1 and beta2)
Excerbation or induction of psoriasis associated with psoriasis; use caution
Not shown to reduce morbidity or mortality in heart failure population; use caution in patients with compensated heart failure and monitor for worsening of condition; temporarily discontinue or reduce dose if condition worsens; stabilize patients on heart failure regimen before initiating beta-blocker therapy; initiate therapy at very low doses; may require adjustment of other medications, including ACE inhibitors and/or diuretics
May cause or exacerbate CNS depression; use caution in patient with psychiatric disorder
Points of recommendation
Use the medicine exactly as directed.
You may take nebivolol with or without food.
Your blood pressure will need to be checked often.
If you need surgery, tell the surgeon ahead of time that you are using nebivolol.
You should not skip doses or stop using nebivolol suddenly. Stopping suddenly may make your condition worse or cause serious heart problems, including heart attack. Follow your doctor's instructions about tapering your dose.
Keep using nebivolol as directed, even if you feel well. High blood pressure often has no symptoms. You may need to use blood pressure medicine for the rest of your life.
Store at room temperature away from moisture and heat.
Take the medicine as soon as you can, but skip the missed dose if it is almost time for your next dose. Do not take two doses at one time.
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