Bystolic: Advanced Beta-Blocker Therapy for Hypertension Control
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Synonyms | |||
Bystolic (nebivolol) is a beta-blocker medication specifically designed for the management of hypertension. It represents a modern therapeutic option within its class, offering a unique pharmacological profile that combines beta-1 adrenergic receptor blockade with vasodilatory properties. This dual mechanism of action allows for effective blood pressure reduction while potentially mitigating some of the undesirable effects associated with older generation beta-blockers. Clinicians often consider Bystolic for patients requiring a well-tolerated antihypertensive agent, particularly those who may benefit from its hemodynamic and metabolic profile.
Features
- Active pharmaceutical ingredient: Nebivolol hydrochloride.
- Pharmacological class: Beta-1 selective adrenergic receptor antagonist with additional nitric oxide-mediated vasodilation.
- Available in multiple tablet strengths: 2.5 mg, 5 mg, 10 mg, and 20 mg.
- Typically administered as a once-daily oral medication.
- Metabolized primarily via the cytochrome P450 2D6 (CYP2D6) pathway.
- Exhibits high selectivity for beta-1 adrenergic receptors.
Benefits
- Provides effective and sustained 24-hour blood pressure control with a single daily dose.
- The vasodilatory effect, mediated by endothelial nitric oxide, may contribute to a favorable hemodynamic profile, reducing peripheral resistance.
- High beta-1 selectivity may result in a lower incidence of certain side effects common to non-selective beta-blockers, such as bronchospasm and glucose/lipid metabolism interference.
- Can be used as monotherapy or in combination with other antihypertensive agents for a synergistic effect.
- May improve endothelial function, which is a key factor in cardiovascular health.
- Offers a treatment option for patients who have experienced intolerance to other beta-blocker therapies.
Common use
Bystolic is indicated for the treatment of hypertension, either alone or in combination with other antihypertensive agents. It is used to lower elevated blood pressure, thereby reducing the risk of fatal and nonfatal cardiovascular events, primarily strokes and myocardial infarctions. Its use is based on a thorough clinical assessment of the patient’s overall cardiovascular risk profile. While its primary indication is hypertension, the pharmacological principles of beta-blockade mean its use may be considered off-label for other conditions like stable chronic heart failure (though not a first-line choice) or management of certain cardiac arrhythmias, always under strict specialist supervision.
Dosage and direction
The dosage of Bystolic must be individualized based on patient response and tolerability. The recommended starting dose for most patients is 5 mg once daily, with or without food. Dosage can be increased at 2-week intervals, as needed, to achieve optimal blood pressure control. The full antihypertensive effect is usually seen within 1-2 weeks of dosing. The maximum recommended dose is 40 mg once daily.
- Dosage in special populations:
- Patients with hepatic impairment: Initiate therapy at 2.5 mg once daily; titrate cautiously. Use is not recommended in patients with severe hepatic impairment.
- Patients with renal impairment: Initiate therapy at 2.5 mg once daily in patients with severe renal impairment (CrCl <30 mL/min); titrate cautiously.
- CYP2D6 poor metabolizers: Initiate therapy at 2.5 mg once daily; titrate cautiously as these patients will have higher nebivolol levels.
- Geriatric patients: Consider initiating therapy at 2.5 mg once daily due to the potential for decreased renal or hepatic function.
The tablet should be swallowed whole with a glass of water. It should not be chewed or crushed. It is crucial to adhere to a consistent dosing schedule. Abrupt discontinuation of beta-blocker therapy should be avoided, as it can lead to a rebound hypertensive crisis or exacerbation of angina. Tapering the dose over 1-2 weeks is recommended under medical supervision.
Precautions
Before initiating Bystolic, a comprehensive patient evaluation is necessary.
- Cardiac Conditions: Use with caution in patients with compensated heart failure. Worsening cardiac failure may occur. It is contraindicated in patients with severe heart failure (NYHA Class IV), cardiogenic shock, or sick sinus syndrome (unless a permanent pacemaker is in place).
- Bronchospastic Diseases: Although beta-1 selective, Bystolic should be administered with caution to patients with bronchospastic diseases who do not respond to, or cannot tolerate, other antihypertensive treatment. It is not absolutely contraindicated but requires extreme vigilance.
- Peripheral Vascular Disease: Beta-blockers can precipitate or aggravate symptoms of arterial insufficiency in patients with peripheral vascular disease (e.g., Raynaud’s phenomenon).
- Anesthesia and Major Surgery: The beta-blocking effect of Bystolic may impair the ability of the heart to respond to reflex stimuli. The attending anesthesiologist must be made aware of beta-blocker therapy. Continuation of therapy reduces the risk of ischemia during intubation, but the negative inotropic effects can be problematic.
- Diabetes and Hypoglycemia: Beta-blockers may mask some cardinal signs of hypoglycemia (e.g., tachycardia). They may also potentiate insulin-induced hypoglycemia and delay recovery of blood glucose levels. This is less likely with a beta-1 selective agent like nebivolol but remains a consideration.
- Thyrotoxicosis: Beta-blockers may mask clinical signs of hyperthyroidism. Abrupt withdrawal may precipitate a thyroid storm.
- Psoriasis: Beta-blockers have been reported to exacerbate psoriasis.
- Pheochromocytoma: Bystolic should not be used unless an alpha-blocker has been initiated first, to avoid unopposed alpha-adrenergic activity leading to severe hypertension.
- Prinzmetal’s Angina: Non-selective beta-blockers may exacerbate angina attacks. Caution is advised.
Contraindications
Bystolic is contraindicated in patients with:
- Severe bradycardia.
- Heart block greater than first degree (in the absence of a functioning pacemaker).
- Cardiogenic shock.
- Decompensated cardiac failure (requiring IV inotropic therapy).
- Sick sinus syndrome (if a pacemaker is not present).
- Severe hepatic impairment (Child-Pugh class C).
- Hypersensitivity to nebivolol or any component of the product.
Possible side effects
As with all medications, Bystolic can cause side effects, although not everybody gets them. Most are mild and often diminish with continued therapy.
- Very Common (≥1/10): Headache, fatigue, dizziness.
- Common (≥1/100 to <1/10): Bradycardia, diarrhea, nausea, dyspnea, insomnia, rash, peripheral edema (e.g., swollen ankles).
- Uncommon (≥1/1,000 to <1/100): Heart block, postural hypotension, vomiting, depression, nightmares, blurred vision, impotence (erectile dysfunction).
- Rare (<1/1,000): Syncope, bronchospasm, hallucinations, worsening of psoriasis, hypertriglyceridemia.
This is not an exhaustive list. Patients should report any new, worsening, or unusual symptoms to their healthcare provider promptly.
Drug interaction
Bystolic has the potential to interact with many other medications. A complete review of all concomitant medications, including over-the-counter drugs and supplements, is essential.
- Other Antihypertives: Concomitant use with other blood pressure-lowering agents (e.g., other beta-blockers, calcium channel blockers like verapamil or diltiazem, alpha-blockers) may potentiate the hypotensive and bradycardic effects.
- Antiarrhythmics: Drugs like disopyramide, amiodarone, and propafenone can have additive negative chronotropic and inotropic effects, increasing the risk of bradycardia and heart block.
- CYP2D6 Inhibitors: Medications such as fluoxetine, paroxetine, quinidine, and terbinafine can significantly increase nebivolol plasma concentrations, necessitating a dose reduction of Bystolic.
- Digoxin: Concomitant use can increase the risk of bradycardia.
- Clonidine: Concurrent use can potentiate the rebound hypertension effect if clonidine is abruptly withdrawn. Bystolic should be discontinued several days before the gradual withdrawal of clonidine.
- Insulin and Oral Hypoglycemics: As noted in Precautions, the masking of hypoglycemic symptoms and potential impairment of glucose recovery can occur.
- NSAIDs: Nonsteroidal anti-inflammatory drugs (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. A double dose should not be taken to make up for a missed one. Maintaining a consistent daily routine is key to effective blood pressure management.
Overdose
Overdose with Bystolic is primarily characterized by the exacerbation of its pharmacological effects.
- 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.
- Bradycardia: Administer atropine. If unresponsive, consider isoproterenol, a cardiac pacemaker, or IV glucagon.
- Hypotension: Utilize IV fluids and vasopressors (e.g., epinephrine, norepinephrine, dopamine). Glucagon may be beneficial.
- Heart Failure: Administer diuretics and digitalis glycosides.
- Bronchospasm: Administer a beta2-stimulating agent and/or a theophylline derivative.
- Hypoglycemia: Administer IV glucose. Gastric lavage may be considered if ingestion was recent. Due to the high protein binding of nebivolol, dialysis is unlikely to be of benefit.
Storage
- Store Bystolic tablets at room temperature, between 20°C to 25°C (68°F to 77°F).
- Keep the medication in its original blister pack or bottle to protect it from light and moisture.
- Keep all medications out of the reach of children and pets.
- Do not use medicine beyond the expiration date printed on the packaging.
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 been compiled from various sources believed to be accurate but cannot be guaranteed. The manufacturer’s official prescribing information is the ultimate authority on the safe and effective use of this product.
Reviews
- Clinical Consensus: Bystolic is generally well-regarded in the cardiology community for its efficacy in hypertension and its potentially favorable side effect profile compared to non-vasodilating beta-blockers. Its hemodynamic effects are viewed positively.
- Patient Feedback: Patient reviews on reputable medical websites often highlight effective blood pressure control with fewer side effects like fatigue and sexual dysfunction than experienced with other beta-blockers. However, individual experiences vary significantly, and some patients do report side effects like headache and dizziness, especially upon initiation.
- Research Summary: Numerous clinical trials, such as the SENIORS trial (which studied nebivolol in elderly heart failure patients) and various hypertension studies, have demonstrated the drug’s efficacy and safety. It is considered a valuable option within the antihypertensive arsenal.