BRAND NAMES
 MECHANISM OF ACTION
Nebivolol is a β1 selective adrenergic antagonist; It competes with sympathomimetic neurotransmitters such as catecholamines for binding at β1 adrenergic receptors.
β1 receptors are predominantly located in the heart. The blockade of these receptors reduces the ability of the sympathetic nervous system to increase the myocardial contractile force and rate and the result is a decrease in heart rate and blood pressure.
β1 receptors are also located in the juxtaglomerular apparatus of the kidney. The blockade of these receptors inhibits the release of renin from the kidney. Decreased circulating plasma renin leads to a decrease in angiotensin II and aldosterone production, causing a decrease in vasoconstriction and a decrease in water retention.
Nebivolol also increases nitric oxide release for vasodilation
In poor CYP2D6 metabolizers and at higher doses, nebivolol inhibits both β1 and β2 adrenergic receptors.
- Treatment of hypertension, to lower blood pressure. Lowering blood pressure reduces the risk of fatal and nonfatal cardiovascular events, primarily strokes and myocardial infarctions.
- Hypertension: Individualize to the needs of the patient. Most patients start at 5 mg once daily. Dose can be increased at 2-week intervals up to 40 mg. Nebivolol can be taken with and without food. Individualize to the
- Sinus bradycardia (resting heart rate of 60 beats per minute or less)
- Second- or third-degree AV block
- Patients in cardiogenic shock or decompensated heart failure.
- Sick sinus syndrome (unless a permanent pacemaker is in place)
- Patients with severe hepatic impairment (Child-Pugh >B)
- History of hypersensitivity to Nebivolol
 WARNINGS AND PRECAUTIONS
- Acute exacerbation of coronary artery disease upon cessation of therapy: Severe exacerbation of angina and the occurrence of myocardial infarction and ventricular arrhythmias have been reported in angina patients following the abrupt discontinuation of therapy with beta blockers. Do not abruptly discontinue.
- Bronchospastic Diseases: In general, patients with bronchospastic diseases should not receive β-blockers
- Diabetes and Hypoglycemia: Beta-blockers may mask some of the manifestations of hypoglycemia, particularly tachycardia. Nonselective beta blockers may potentiate insulin-induced hypoglycemia and delay recovery of serum glucose levels. It is not known whether nebivolol has these effects. Patients subject to spontaneous hypoglycemia, or diabetic patients receiving insulin or oral hypoglycemic agents, should be cautioned about these possibilities and Nebivolol should be used with caution
- Concomitant Use of Verapamil or Diltiazem type calcium channel blockers: Bradycardia and heart block can occur. Use with care.
- Use with CYP2D6 Inhibitors (quinidine, propafenone, fluoxetine, paroxetine, etc.): Nebivolol exposure increases with inhibition of CYP2D6. The dose of Nebivolol may need to be reduced.
- Hypotensive agents (e.g., reserpine, MAO inhibitors, clonidine) may increase the risk of hypotension and/or severe bradycardia.
- Both digitalis glycosides and beta blockers slow atrioventricular conduction and decrease heart rate. Concomitant use can increase the risk of bradycardia.
 PREGNANCY AND LACTATION
- Pregnancy Category C (US)
- Nursing Mothers: Studies in rats have shown that nebivolol or its metabolites cross the placental barrier and are excreted in breast milk. It is not known whether this drug is excreted in human milk. Because of the potential for β-blockers to produce serious adverse reactions in nursing infants, especially bradycardia, nebivolol is not recommended during nursing.
 SIDE EFFECTS
Most common adverse reactions are Headache and fatigue
 RELATED LINKS
|ACE inhibitors||Benazepril (Lotensin) • Captopril (Capoten) • Cilazapril • Delapril • Enalapril (Renitec, Vasotec) • Fosinopril (Monopril) • Lisinopril (Prinivil, Zestril) • Moexipril (Univasc) • Perindopril (Aceon) • Quinapril (Accupril) • Ramipril (Altace, Triatec) • Trandolapril (Mavik) • Zofenopril (Bifril, Zopranol)|
|Angiotensin II receptor antagonist||Azilsartan (Edarbi) • Candesartan (Atacand) • Eprosartan (Teveten) • Irbesartan (Aprovel, Avapro, Karvea) • Losartan (Cozaar) • Olmesartan (Benicar, Olmetec) • Telmisartan (Micadis) • Valsartan (Diovan, Tareg)|
|Renin inhibitors||Aliskiren (Rasilez, Tekturna)|
|Alpha-1 blockers||Doxazosin (Cardura) • Prazosin (Minipress) • Terazosin (Hytrin)|
|Alpha-2 agonists (centrally acting)||Clonidine (Oral route) • Clonidine (Transdermal) (Catapresan) • Guanfacine (Tenex) • Methyldopa (Aldomet)|
|Calcium channel blockers||Dihydropyridines||Amlodipine (Norvasc) • Barnidipine (Vasexten) • Felodipine (Plendil) • Isradipine (Dynacirc) • Lacidipine (Lacipil, Motens) • Lercanidipine (Zanidip) • Manidipine • Nicardipine • Nifedipine (Adalat) • Nisoldipine • Nitrendipine|
|Benzothiazepine||Diltiazem (Cardizem, Taztia XT, Tiazac, Tildiem)|
|Phenylalkylamine||Gallopamil • Verapamil (Calan)|
|Beta blockers||Beta1 selective (cardioselective)||Acebutolol (Sectral) • Atenolol (Tenormin) • Betaxolol (Kerlon) • Bisoprolol (Concor) • Celiprolol (Cordiax) • Metoprolol (Betaloc, Lopressor, Toprol-XL) • Nebivolol (Bystolic, Lobivon, Nebilox)|
|Nonselective (Beta1 and Beta2 blockers)||Oxprenolol (Trasitensin) • Propranolol (Inderal) • Timolol (Blocadren)|
|Nonselective (Beta1, Beta2 and Alpha1 blockers)||Carvedilol (Dilatrend) • Labetalol (Trandate)|
|Beta blocker with intrinsic sympathomimetic activity (ISA)||Acebutolol (Sectral) • Celiprolol (Cordiax)|
|Lipophilic Beta blockers||Propranolol (Inderal) • Metoprolol (Betaloc, Lopressor, Toprol-XL) • Oxprenolol (Trasitensin)|
|Diuretics||Carbonic anhydrase inhibitors||Acetazolamide (Diamox)|
|Loop diuretics||Bumetanide • Etacrynic acid • Furosemide (Lasix) • Piretanide • Torasemide (Demadex)|
|Thiazide diuretics||Chlorothiazide (Diuril) • Hydrochlorothiazide (Esidrex)|
|Thiazide-like diuretics||Chlortalidone (Hygroton) • Indapamide (Lozol, Lozide) • Metolazone|
|Potassium-sparing diuretics|| Epithelial sodium channel blockers: Amiloride (Midamor) • Triamterene (Dyrenium) |
Aldosterone receptor antagonists: Potassium canrenoate • Eplerenone (Inspra) • Spironolactone (Aldactone)
|Combination therapy||Amiloride/Hydrochlorothiazide (Moduretic) • Spironolactone/Hydrochlorothiazide (Aldactazide)|