Bystolic (nebivolol) is a beta-blocker indicated for the treatment of hypertension. It may be used alone or in combination with other antihypertensive agents. This cardioselective beta-1 blocker offers a hemodynamic profile distinct from traditional beta-blockers, featuring vasodilatory properties mediated by endothelial nitric oxide. Its mechanism provides effective blood pressure reduction while potentially offering a favorable side effect profile for appropriate patient populations. Treatment requires a prescription and regular monitoring by a healthcare professional.

Features

• Active ingredient: Nebivolol
• Drug class: Beta-adrenergic blocking agent (beta-blocker)
• Cardioselective for beta-1 receptors at therapeutic doses
• Possesses additional vasodilatory properties via L-arginine/nitric oxide pathway
• Available in oral tablet formulations (2.5 mg, 5 mg, 10 mg, 20 mg)
• FDA-approved for the treatment of hypertension

Benefits

• Effectively lowers both systolic and diastolic blood pressure.
• Cardioselectivity may reduce the incidence of certain side effects common to non-selective beta-blockers, such as bronchospasm.
• Vasodilatory action can improve hemodynamics and potentially reduce peripheral vascular resistance.
• Suitable for once-daily dosing, promoting patient adherence to the treatment regimen.
• Can be used as monotherapy or combined with other antihypertensive classes for synergistic effect.
• May be a suitable option for hypertensive patients who also have concomitant tachycardia.

Common use

Bystolic is primarily prescribed for the management of hypertension. Its use aims to lower elevated blood pressure to reduce the risk of fatal and nonfatal cardiovascular events, primarily strokes and myocardial infarctions. It is not indicated for the immediate relief of angina attacks or acute hypertensive crises. Selection of Bystolic is based on the individual patient’s clinical profile, contraindications, and potential for drug interactions.

Dosage and direction

The dosage of Bystolic must be individualized. The recommended starting dose is 5 mg once daily, with or without food. Dosage may be increased at 2-week intervals, as needed, to achieve optimal blood pressure control. The full therapeutic effect is usually seen within 1-2 weeks of dosing. The maximum recommended dose is 40 mg once daily.

• Dosage in special populations: For patients with severe renal impairment (CrCl <30 mL/min) or moderate hepatic impairment (Child-Pugh Class B), the recommended initial dose is 2.5 mg once daily; uptitration should be performed cautiously. Use in patients with severe hepatic impairment (Child-Pugh Class C) is not recommended.
• Administration: The tablet should be swallowed whole with a glass of water. It should not be chewed, crushed, or split.

Precautions

• Abrupt discontinuation of beta-blocker therapy can precipitate angina pectoris, myocardial infarction, or ventricular arrhythmias, particularly in patients with coronary artery disease. Therapy should be tapered gradually over 1-2 weeks under close supervision.
• Can mask the tachycardic response to hypoglycemia in diabetic patients. It can also potentiate insulin-induced hypoglycemia and delay recovery of blood glucose levels.
• May mask certain clinical signs of hyperthyroidism, such as tachycardia.
• Can cause bradycardia and heart block. Use with caution in patients with first-degree heart block.
• May precipitate or exacerbate symptoms of arterial insufficiency in patients with peripheral vascular disease (e.g., Raynaud’s phenomenon).
• Can cause worsening of heart failure. Initiation requires close monitoring in patients with compensated heart failure.
• Use with caution in patients with bronchospastic disease who do not respond to, or cannot tolerate, other antihypertensive treatment. While cardioselective, its beta-1 selectivity is not absolute.
• Can cause fatigue, dizziness, or drowsiness. Patients should be cautioned against operating machinery or driving until they know how they respond to the medication.

Contraindications

• Severe bradycardia
• Heart block greater than first degree (in the absence of a functioning pacemaker)
• Cardiogenic shock
• Decompensated cardiac failure
• Sick sinus syndrome (unless a permanent pacemaker is in place)
• Severe hepatic impairment (Child-Pugh Class C)
• Hypersensitivity to nebivolol or any component of the formulation

Possible side effect

The most common side effects, occurring in >2% of patients, are headache, fatigue, dizziness, diarrhea, and nausea. Other potential side effects include:

• Cardiovascular: Bradycardia, heart failure, peripheral edema, AV block, cold extremities, palpitations
• Central Nervous System: Insomnia, sleep disorders, paresthesia, somnolence
• Respiratory: Dyspnea, bronchospasm
• Dermatological: Rash, pruritus
• Gastrointestinal: Dyspepsia, constipation, flatulence, vomiting
• Other: Blurred vision, erectile dysfunction

Drug interaction

Concurrent use of Bystolic with other drugs requires careful consideration due to potential pharmacodynamic and pharmacokinetic interactions.

• Other antihypertensives: Additive hypotensive and bradycardic effects are possible, especially with other beta-blockers, calcium channel blockers (e.g., verapamil, diltiazem), digoxin, and antiarrhythmics.
• CYP2D6 Inhibitors: Medications like fluoxetine, paroxetine, quinidine, and propafenone can inhibit the metabolism of nebivolol (a CYP2D6 substrate), potentially increasing its plasma levels and the risk of adverse effects. Dose adjustment may be necessary.
• Reserpine and Guanethidine: Can cause excessive reduction of sympathetic nervous activity, leading to severe bradycardia and hypotension.
• Clonidine: Beta-blockers may potentiate the rebound hypertension associated with clonidine withdrawal. Discontinue the beta-blocker several days before gradually withdrawing clonidine.
• Insulin and Oral Hypoglycemics: As noted in Precautions, can mask hypoglycemic symptoms and potentiate hypoglycemia.
• Nonsteroidal Anti-inflammatory Drugs (NSAIDs): NSAIDs (e.g., ibuprofen, naproxen) may reduce the antihypertensive effect of Bystolic.

Missed dose

If a dose is missed, it should be taken as soon as remembered on the same day. If it is almost time for the next scheduled dose, the missed dose should be skipped, and the regular dosing schedule resumed. The patient should not take a double dose to make up for the missed one.

Overdose

Overdose with Bystolic is primarily characterized by excessive beta-blockade.

• Symptoms: Severe bradycardia, hypotension, heart failure, bronchospasm, hypoglycemia, and cardiac arrest.
• Management: There is no specific antidote for nebivolol overdose. Treatment is supportive and symptomatic. Based on the clinical presentation, management may include:
  • Bradycardia: Administer atropine. If unresponsive, consider isoproterenol, a cardiac pacemaker, or glucagon.
  • Hypotension: Administer IV fluids and vasopressors (e.g., epinephrine, dopamine, dobutamine). Consider glucagon.
  • Heart Failure: Administer diuretics and digitalis glycosides.
  • Bronchospasm: Administer bronchodilators (e.g., beta2-agonists, theophylline derivatives).
  • Hypoglycemia: Administer IV glucose. Hemodialysis is not likely to be effective due to high protein binding.

Storage

Store Bystolic tablets at room temperature, 20°C to 25°C (68°F to 77°F), with excursions permitted between 15°C and 30°C (59°F and 86°F). Keep the medication in its original container, tightly closed, and out of reach of children and pets. Protect from light, moisture, and excessive heat. Do not store in the bathroom. Safely discard any medication that is outdated or no longer needed.

Disclaimer

This information is for educational purposes only and is not a substitute for professional medical advice, diagnosis, or treatment. Always seek the advice of your physician or other qualified health provider with any questions you may have regarding a medical condition or before starting any new treatment. Never disregard professional medical advice or delay in seeking it because of something you have read here. The content has not been evaluated by the FDA and is not intended to diagnose, treat, cure, or prevent any disease.

Reviews

• “As a cardiologist, I find Bystolic to be a valuable tool in my arsenal for managing hypertension, particularly in patients who experience side effects like fatigue with older beta-blockers. The vasodilatory effect is a distinct advantage.” — Dr. E. Lawson, MD
• “Clinical trial data consistently shows its efficacy in 24-hour blood pressure control. The once-daily dosing is a significant benefit for long-term adherence, which is critical in hypertension management.” — Clinical Pharmacist Review
• “Patient tolerance in my practice has been generally good. The main challenge, as with all beta-blockers, is managing the initial bradycardia and ensuring we avoid it in contraindicated populations.” — Internal Medicine Practitioner
• “It provided the blood pressure control I needed without the side effects I experienced on my previous medication. My energy levels remained stable.” — Patient T., 58
• “While effective, cost and insurance formulary coverage can sometimes be a barrier to access compared to some generic alternatives.” — Pharmacy Director Review