Bystolic, indicated for the treatment of hypertension, is a once-daily medication that can be used alone or in combination with other antihypertensive agents.

The antihypertensive effectiveness of Bystolic as monotherapy has been demonstrated in three randomized, double-blind, multi-center, placebo-controlled trials at doses ranging from 1.25 to 40 mg for 12 weeks (Studies 1, 2, and 3). A fourth placebo-controlled trial demonstrated additional antihypertensive effects of Bystolic at doses ranging from 5 to 20 mg when administered concomitantly with up to two other antihypertensive agents (ACE inhibitors, angiotensin II receptor antagonists, and thiazide diuretics) in patients with inadequate blood pressure control.

The three monotherapy trials included a total of 2,016 patients (1,811 Bystolic, 205 placebo) with mild to moderate hypertension who had baseline diastolic blood pressure (DBP) of 95 to 109 mmHg. Patients received either Bystolic or placebo once daily for twelve weeks. Two of these monotherapy trials (Studies 1 and 2) studied 1,716 patients in the general hypertensive population with a mean age of 54 years, 55% males, 26% non-Caucasians, 7% diabetics and 6% genotyped as PMs. The third monotherapy trial (Study 3) studied 300 Black patients with a mean age of 51 years, 45% males, 14% diabetics, and 3% as PMs.

The studies also found that Bystolic was well tolerated, with a low incidence of side effects. Bystolic has a unique mechanism of action that includes cardioselective beta blockade and vasodilation.*

Important Safety Information

Patients being treated with Bystolic should be advised against abrupt discontinuation of therapy. Severe exacerbation of angina and the occurrence of myocardial infarction and ventricular arrhythmias have been reported following the abrupt cessation of therapy with beta blockers. When discontinuation is planned, the dosage should be reduced gradually over a 1- to 2-week period and the patient carefully monitored.

Bystolic is contraindicated in severe bradycardia, heart block greater than first degree, cardiogenic shock, decompensated cardiac failure, sick sinus syndrome (unless a permanent pacemaker is in place), severe hepatic impairment (Child-Pugh >B), and in patients who are hypersensitive to any component of this product.

Bystolic should be used with caution in patients with peripheral vascular disease, thyrotoxicosis, in patients treated concomitantly with beta blockers and calcium channel blockers of the verapamil and diltiazem type (ECG and blood pressure should be monitored), severe renal impairment, and any degree of hepatic impairment or in patients undergoing major surgery. Caution should also be used in diabetic patients as beta blockers may mask some of the manifestations of hypoglycemia, particularly tachycardia.

In general, patients with bronchospastic disease should not receive beta blockers.

Bystolic should not be combined with other beta blockers.

The most common adverse events with Bystolic versus placebo (approximately ≥1% and greater than placebo) were headache, fatigue, dizziness, diarrhea, nausea, insomnia, chest pain, bradycardia, dyspnea, rash, and peripheral edema.

*In extensive metabolizers (most of the population) and at doses
≤ 10 mg, Bystolic is preferentially ß₁ selective. The mechanism of action of the antihypertensive response has not been completely established. Possible factors that may be involved include:
(1) decreased heart rate, (2) decreased myocardial contractility,
(3) diminution of tonic sympathetic outflow to the periphery from cerebral vasomotor centers (4) suppression of renin activity, and
(5) vasodilation and decreased peripheral vascular resistance.