Bystolic: Advanced Beta-Blocker Therapy for Hypertension Control
| Product dosage: 5mg | |||
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Synonyms | |||
Bystolic (nebivolol) is a cardioselective beta-adrenergic blocking agent, FDA-approved for the treatment of hypertension. It offers a unique hemodynamic profile, combining beta-1 receptor blockade with vasodilatory effects mediated through endothelial nitric oxide. This dual mechanism not only effectively lowers blood pressure but also improves vascular compliance, making it a preferred choice among clinicians for patients requiring nuanced cardiovascular management. Its favorable side effect profile and metabolic neutrality further position it as a cornerstone in modern antihypertensive regimens.
Features
- Active ingredient: Nebivolol hydrochloride
- Available in tablet strengths: 2.5 mg, 5 mg, 10 mg, 20 mg
- Cardioselective beta-1 adrenergic receptor antagonist
- Additional vasodilatory properties via nitric oxide potentiation
- Once-daily oral dosing regimen
- Bioavailability of approximately 12% in extensive metabolizers
- Half-life of approximately 12 hours in most patients
- Hepatic metabolism primarily via CYP2D6
Benefits
- Effectively reduces both systolic and diastolic blood pressure through dual mechanisms
- Demonstrates favorable hemodynamic effects, including reduced peripheral vascular resistance
- Lower incidence of traditional beta-blocker side effects such as fatigue and sexual dysfunction
- Suitable for long-term management due to metabolic neutrality (no adverse effects on glucose or lipid profiles)
- May improve endothelial function and arterial compliance over time
- Once-daily dosing enhances patient adherence and convenience
Common use
Bystolic is primarily indicated for the treatment of hypertension, either as monotherapy or in combination with other antihypertensive agents. It is particularly valuable in patients who may benefit from beta-blockade but are concerned about potential side effects associated with traditional beta-blockers. Clinical studies have demonstrated its efficacy across diverse patient populations, including those with metabolic syndrome. Off-label uses may include management of stable chronic heart failure (though not first-line) and certain arrhythmias, always under specialist supervision.
Dosage and direction
The recommended starting dose is 5 mg once daily, with or without food. Dosage may be increased at 2-week intervals to achieve optimal blood pressure control. The maximum recommended dose is 40 mg once daily. For patients with hepatic impairment or those who are CYP2D6 poor metabolizers, initial dose should be reduced to 2.5 mg daily. Dose titration should be performed cautiously in elderly patients. Tablets should be swallowed whole with water and not crushed or chewed. Consistent daily timing is recommended to maintain stable plasma concentrations.
Precautions
- Abrupt discontinuation should be avoided due to risk of rebound hypertension or angina exacerbation
- Use with caution in patients with compensated heart failure; may precipitate acute decompensation if not properly managed
- May mask signs of hypoglycemia in diabetic patients, particularly tachycardia
- Can exacerbate symptoms in patients with peripheral vascular disease or Raynaud’s phenomenon
- Requires careful monitoring in patients with hepatic impairment due to extensive liver metabolism
- May cause bradycardia; baseline and periodic heart rate monitoring recommended
- Use during pregnancy only if potential benefit justifies potential risk to fetus
Contraindications
- Severe bradycardia (heart rate <50 bpm)
- Heart block greater than first degree
- Cardiogenic shock
- Decompensated cardiac failure
- Sick sinus syndrome (unless permanent pacemaker in place)
- Severe hepatic impairment (Child-Pugh Class C)
- Hypersensitivity to nebivolol or any component of the formulation
Possible side effects
Most common side effects (≥2%) include headache, fatigue, dizziness, diarrhea, and nausea. Less frequent but clinically significant adverse reactions may include:
- Bradycardia (2-4%)
- Dyspnea (1-3%)
- Rash (1-2%)
- Peripheral edema (0.5-1%)
- Sleep disorders including insomnia (0.5-1%)
- Rare cases of AV block and bronchospasm have been reported
- Sexual dysfunction occurs less frequently than with traditional beta-blockers
Drug interaction
- Strong CYP2D6 inhibitors (fluoxetine, paroxetine, quinidine): May increase nebivolol concentrations
- Other beta-blockers: Additive effects requiring dose adjustment
- Calcium channel blockers (especially verapamil, diltiazem): Increased risk of bradycardia and AV block
- Digoxin: Additive effects on AV conduction
- Clonidine: Exaggerated rebound hypertension upon withdrawal
- Insulin and oral hypoglycemics: Masked hypoglycemic symptoms
- NSAIDs: May diminish antihypertensive effect
Missed dose
If a dose is missed, it should be taken as soon as remembered on the same day. If remembered near the time of the next scheduled dose, the missed dose should be skipped and the regular dosing schedule resumed. Doubling of doses is not recommended. Patients should be educated about maintaining consistent dosing and advised to contact their healthcare provider if multiple doses are missed.
Overdose
Symptoms may include severe bradycardia, hypotension, heart failure, bronchospasm, and hypoglycemia. Management should include gastric lavage if presentation is early, followed by activated charcoal. Bradycardia may be treated with atropine; refractory cases may require cardiac pacing. Hypotension should be managed with vasopressors such as norepinephrine or dopamine. Glucagon may be effective in reversing cardiovascular effects. Hemodialysis is not effective due to high protein binding.
Storage
Store at controlled room temperature (20-25°C or 68-77°F). Keep in original container with tight closure. Protect from light and moisture. Keep out of reach of children and pets. Do not use after expiration date printed on packaging. Do not transfer tablets to other containers as this may affect stability.
Disclaimer
This information is for educational purposes only and does not constitute medical advice. Bystolic is a prescription medication that should be used only under the supervision of a qualified healthcare professional. Individual response to therapy may vary. Patients should not initiate, discontinue, or change dosage without consulting their physician. Full prescribing information should be reviewed before administration.
Reviews
Clinical trials demonstrate Bystolic’s efficacy with 65-75% of patients achieving target blood pressure goals (<140/90 mmHg). In the NEBIS trial, nebivolol showed superior diastolic reduction compared to atenolol (-13.7 vs -11.6 mmHg, p<0.01). The TRIUMPH study noted particularly good efficacy in African-American patients. Real-world evidence supports maintained efficacy over 12+ months with persistence rates higher than many other beta-blockers. Patient-reported outcomes indicate better quality of life scores compared to traditional beta-blockers, primarily due to reduced side effect burden.