2.5 mg, 5 mg, 10 mg, 20 mg (base equivalent)
For the treatment of hypertension: The recommended starting dose is 5 mg once daily. The dose can be increased at 2-week intervals up to a maximum of 40 mg once daily. May be used as monotherapy or in combination with other agents.
Dosage in renal or hepatic impairment: The recommended starting dose is 2.5 mg once daily in patients with severe renal (ClCr <30 mL/min) or moderate hepatic impairment.
Pharmacology/Pharmacokinetics:
Nebivolol is primarily a beta-1 adrenergic blocker. In poor metabolizers and at higher doses, nebivolol is both a beta-1 and a beta-2 adrenergic blocker. At therapeutic doses, it does not show intrinsic sympathomimetic or membrane-stabilizing activity. It does not block alpha-adrenergic receptors. Beta-blockade by nebivolol causes decreased heart rate, decreased myocardial contractibility, vasodilation and decreased peripheral resistance, suppression of renin activity, and diminution of tonic sympathetic outflow to the periphery from cerebral vasomotor centers. Metabolism occurs in the liver primarily via CYP2D6. Peak plasma levels are reached in 1.5-4 hours following an oral dose. Its half-life is 12 hours in extensive metabolizers (most patients) and about 19 hours in poor metabolizers. Excretion of metabolites occurs in the urine and feces.
Drug Interactions:
Drug which inhibits CYP2D6 (paroxetine, fluoxetine, propafenone, quinidine) may increase plasma levels. Drugs which induce CYP2D6 may decrease plasma levels. Use with digitalis glycosides and non-dihydropyridine calcium channel blockers (verapamil, diltiazem) may cause excessive bradycardia.
Contraindications/Precautions:
Contraindicated in patients with any of the following conditions: severe bradycardia; heart block greater than first degree; patients with cardiogenic shock; decompensated cardiac failure; sick sinus syndrome (without a pacemaker); severe hepatic impairment; hypersensitivity to any component. Abruptly discontinuing therapy may exacerbate angina, myocardial infarction, and ventricular arrhythmias. Use with caution in patients with bronchospastic diseases. May mask the symptoms of hypoglycemia in diabetes. Pregnancy Category C.
Adverse Effects:
The most common adverse effects are headache, nausea, fatigue, and dizziness.
Store in a cool, dry place away from sunlight and children.
If a dose is missed, take it as soon as possible. If it is closer to the time of your next dose than the dose you missed, skip the missed dose and return to your dosing schedule. Do not double doses.
Do not discontinue therapy without first consulting physician.
May cause drowsiness. Use caution while operating machinery or when mental alertness is required.
Patients with diabetes need to be aware that this agent can cause masking of hypoglycemic symptoms.
Avoid nonprescription cough, cold, and allergy medications unless otherwise directed.
