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Generic Nebivolol ( Nebivolol )
Nebivolol is a beta-adrenergic receptor blocker with selectivity for beta-1 receptors and additional nitric oxide-mediated vasodilatory properties. It is indicated for the treatment of mild to moderate essential hypertension. Nebivolol lowers blood pressure by reducing heart rate, myocardial contractility, and cardiac output through beta-1 blockade, while the vasodilating effect is thought to result from enhanced endothelial nitric oxide release, which reduces peripheral vascular resistance. It is also used off-label for chronic heart failure in some jurisdictions under specialist supervision. Nebivolol is available only by prescription in Canada.
Usual adult dose: The recommended starting dose is 5 mg taken orally once daily, with or without food. For patients who require a lower starting dose (e.g., elderly patients or those with mild hepatic or renal impairment), 2.5 mg once daily may be used. If blood pressure control is inadequate after 2 to 4 weeks, the dose may be increased to 10 mg once daily. The maximum recommended dose is 10 mg per day. The tablets should be swallowed whole with water and taken at the same time each day. No dose adjustment is required in mild to moderate renal impairment, but the dose should not exceed 10 mg in severe renal impairment; in moderate hepatic impairment, a starting dose of 2.5 mg once daily is recommended with cautious titration. If a dose is missed, it should be taken as soon as remembered, but two doses should not be taken on the same day. Abrupt discontinuation should be avoided because of the risk of rebound hypertension or worsening angina; the dose should be tapered over 1 to 2 weeks under medical supervision.
Dosage form: Oral tablets: 2.5 mg (small, round, scored), 5 mg (round, scored), and 10 mg (round, scored). The 2.5 mg tablet is used for dose titration and for patients requiring lower initial doses; the 5 mg and 10 mg strengths are used for standard and higher-dose maintenance therapy. Available in blister packs or bottles of 30 or 100 tablets.
Onset of action: The antihypertensive effect begins within 1 to 2 weeks of starting therapy, with peak blood pressure reduction typically achieved after 2 to 4 weeks of continuous once-daily dosing. Heart rate reduction may be observed within the first few days.
Duration of action: The elimination half-life of nebivolol is approximately 10 hours, but the pharmacodynamic effect persists for 24 hours, supporting once-daily dosing. The blood-pressure-lowering effect is maintained throughout the day with regular daily administration.
Alcohol recommendation: Alcohol should be used with caution during nebivolol therapy. Alcohol can potentiate the blood-pressure-lowering and central nervous system depressant effects, increasing the risk of dizziness, fainting, and impaired coordination. Patients should limit alcohol intake, especially when first starting therapy or when the dose is increased.
Most common side effects: Fatigue, headache, dizziness, bradycardia, cold extremities, nausea, and diarrhea. These effects are generally mild to moderate and may diminish with continued use. Nebivolol can mask the symptoms of hypoglycemia (except sweating) in diabetic patients, so glucose monitoring should be intensified. It is contraindicated in patients with severe bradycardia, second- or third-degree heart block, cardiogenic shock, decompensated heart failure, sick sinus syndrome (unless a pacemaker is present), and severe hepatic impairment. Caution is required in patients with asthma or chronic obstructive pulmonary disease because of beta-blockade; although nebivolol is beta-1 selective, higher doses may cause bronchospasm. Patients with peripheral vascular disease or Raynaud's phenomenon should be monitored. If a dose is missed, it should be taken as soon as remembered, but two doses should not be taken at the same time. Nebivolol is available only by prescription in Canada and must be initiated and monitored by a healthcare professional.
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