Trade Names:Bystolic- Tablets 2.5 mg- Tablets 5 mg- Tablets 10 mg- Tablets 20 mg
Blocks beta receptors, which may decrease heart rate and myocardial contractility, diminish tonic sympathetic outflow to the periphery from cerebral vasomotor centers, suppress renin activity, and decrease peripheral vascular resistance. Lacks intrisic sympathomimetic activity at therapeutically relevant doses.
Mean C max is approximately 1.5 to 4 h postdosing.
Protein binding is 98%, primarily to albumin.
Predominantly metabolized via direct glucuronidation and to a lesser extent via N-dealkylation and oxidation by CYP2D6. Stereospecific metabolites contribute to the pharmacologic activity.
In extensive metabolizers, elimination is 38% in urine and 44% in feces, while, in poor metabolizers, elimination is 67% in urine and 13% in feces.
C max increases 3-fold, AUC increases 10-fold, and apparent Cl decreases 86% in patients with moderate hepatic function impairment.
Treatment of hypertension.
Severe bradycardia, heart block more than first degree, cardiogenic shock, decompensated cardiac failure, sick sinus syndrome (unless a permanent pacemaker is in place), severe hepatic function impairment, hypersensitivity to any component of the product.
PO Recommended starting dose is 5 mg/day. The dose can be increased at 2-week intervals up to 40 mg/day.Renal Function ImpairmentAdults
PO Start with 2.5 mg/day and cautiously titrate dose upward if needed. Studies have not been conducted in patients receiving dialysis.Hepatic Function ImpairmentAdults
PO Start with 2.5 mg/day and cautiously titrate dose upward if needed. Studies have not been conducted in patients with severe hepatic function impairment.
Store at 68° to 77°F. Protect form light.
Risk of bradycardia may be increased.Cimetidine
Nebivolol plasma concentrations may be increased.Clonidine
In patients receiving clonidine and nebivolol concurrently, discontinue nebivolol several days before gradually tapering clonidine dose.Guanethidine, other beta-blockers, reserpine
Excessive sympathetic activity may occur.Inhibitors of CYP2D6 (eg, amiodarone, fluoxetine, propafenone, quinidine)
Nebivolol plasma concentrations may be elevated, increasing pharmacologic effects and adverse reactions.Sildenafil
Sildenafil and nebivolol plasma concentrations may be reduced slightly with coadministration.
None well documented.
Bradycardia, chest pain (1%); MI, peripheral ischemia/claudication, second- and third-degree AV block, syncope (postmarketing).
Headache (9%); fatigue (5%); dizziness (4%); asthenia, paresthesia (at least 1%); insomnia (1%); somnolence, vertigo (postmarketing).
Rash (1%); pruritus, psoriasis (postmarketing).
Diarrhea, nausea (3%); abdominal pain (at least 1%); vomiting (postmarketing).
Acute renal failure, erectile dysfunction (postmarketing).
Abnormal hepatic function, including increased ALT, AST, and bilirubin (postmarketing).
Decreased HDL cholesterol and platelet count, increased BUN, triglycerides, and uric acids (at least 1%).
Hypercholesterolemia, hyperuricemia (at least 1%).
Dyspnea (1%); acute pulmonary edema, bronchospasm (postmarketing).
Peripheral edema (1%); hypersensitivity (including urticaria, allergic vasculitis, and angioedema), Raynaud phenomenon (postmarketing).
Closely monitor patients receiving anesthetic agents that depress myocardial function.
Category C .
Safety and efficacy not established.
No overall difference in efficacy or adverse reactions between older and younger patients.
Use with caution and adjust dose in severe renal function impairment.
Use with caution and reduce dose in patients with moderate hepatic function impairment.
Ventricular arrhythmias and MI have occurred in patients with coronary artery disease following abrupt discontinuation of therapy.
Patients receiving beta-blockers and who have a history of severe anaphylactic reactions to a variety of allergens may be more reactive to repeated challenge. Such patients may be unresponsive to the usual dose of epinephrine used to treat allergic reactions.
If nebivolol use is continued perioperatively, closely monitor when anesthetic agents that depress myocardial function (eg, ether) are used.
Severe cardiac failure may be precipitated because of depression of myocardial contractility.
Use with caution because beta-blockers may mask symptoms of hypoglycemia (eg, tachycardia) and nonselective beta-blockers may potentiate insulin-induced hypoglycemia and delay recovery of serum glucose levels.
Use with caution in patients with peripheral vascular disease because symptoms of arterial insufficiency may be precipitated.
May mask signs of hyperthyroidism (eg, tachycardia); abrupt withdrawal may exacerbate symptoms of hyperthyroidism or potentiate thyroid storm.
Bradycardia, bronchospasm, cardiac failure, dizziness, fatigue, heart block, hypoglycemia, hypotension, vomiting.
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