Dr. Holmberg is a freelance clinical writer based in Phoenix, Arizona.
Often called the "silent killer," hypertension usually presents without symptoms, and patients may not be diagnosed until damage has occurred to the heart, brain, eyes, or kidneys.2 Of the 72 million Americans who are affected by hypertension, about 65% of those diagnosed have not reached optimal blood pressure control.1,2
Bystolic is a b-adrenergic receptor blocker. At doses less than 10 mg and in patients who are extensive metabolizers (most of the population), Bystolic displays b1 selective activity. In patients who are poor metabolizers and in doses greater than 10 mg, Bystolic has been shown to inhibit both b1 and b2 receptors. Bystolic does not affect the a1 adrenergic receptors when administered at clinically appropriate doses.3
The recommended starting dose for Bystolic is 5 mg once a day, with dose increases at 2-week intervals as appropriate to obtain optimal blood pressure control. The maximum daily dose is 40 mg.3
Three randomized, double-blind, multicenter, placebo-controlled trials have evaluated the effectiveness of Bystolic's antihypertensive effects when administered as monotherapy. A total of 2016 patients (1811 given Bystolic; 205 given placebo) were given doses ranging from 1.25 mg daily to 40 mg daily and were followed for 12 weeks.3
A fourth placebo-controlled trial of 669 patients evaluated Bystolic in combination with up to 2 other antihypertensive agents from the following classes: angiotensin-converting enzyme inhibitors, angiotensin II receptor antagonists, or thiazide diuretics. Bystolic doses ranged from 5 to 20 mg daily.3 An increasing response was noted in most studies at doses above 5 mg. Statistically significant reductions in both diastolic and systolic blood pressure were noticed in all groups at doses of 20 mg daily and higher.3
Bystolic is contraindicated in patients with the following conditions: severe bradycardia, heart block greater than first degree, cardiogenic shock, decompensated cardiac failure, sick sinus syndrome without a permanent pacemaker in place, severe hepatic impairment, and hypersensitivity to any of its components.3
Bystolic should be used cautiously in patients with peripheral vascular disease, thyrotoxicosis, severe renal impairment, hepatic impairment of any extent, and in patients undergoing major surgery.
Concomitant treatment of Bystolic and nondihydropyridine calcium channel blockers should be avoided or used cautiously if necessary; in these cases, electrocardiogram and blood pressure should be monitored closely.
Patients with diabetes should be aware that treatment with beta-blockers may mask some of the signs and symptoms of hypoglycemia, such as tachycardia. Patients with bronchospastic disease should not receive beta-blockers.1
Drugs known to inhibit CYP2D6 may increase plasma levels of Bystolic; patients using these agents together should be monitored as appropriate.3
Prior to discontinuing treatment with Bystolic, the dose should be gradually reduced over 1 to 2 weeks. Sudden discontinuation of therapy has been associated with severe angina exacerbations, myocardial infarction, and ventricular arrhythmia.1
Bystolic is available in over 50 countries outside of North America.1 Bystolic is a pregnancy category C. Its use is not recommended in patients who are breast-feeding. Bystolic has not been studied in children younger than 18 years of age.3
The most commonly reported side effects from treatment with Bystolic included headache, fatigue, dizziness, diarrhea, nausea, insomnia, chest pain, bradycardia, dyspnea, rash, and peripheral edema.1