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Medical Disclaimer: This information is for educational purposes only and is not a substitute for professional medical advice.
Brand Name
Nebivolol
Generic Name
Nebivolol
Active Ingredient
NebivololCategory
beta-Adrenergic Blocker [EPC]
Salt Form
Hydrochloride
Variants
77
Different strengths and dosage forms
| Strength | Form | Route | NDC |
|---|---|---|---|
| 5 mg/1 | TABLET | ORAL | 62559-276 |
| 2.5 mg/1 | TABLET | ORAL | 72162-2415 |
| 5 mg/1 | TABLET | ORAL | 72162-2417 |
This page is for informational purposes only and does not replace medical advice. Before using any prescription or over-the-counter medication for Nebivolol, you must consult a qualified healthcare professional.
| 20 mg/1 | TABLET | ORAL | 72189-592 |
| 10 mg/1 | TABLET | ORAL | 0904-7499 |
| 5 mg/1 | TABLET | ORAL | 31722-586 |
| 10 mg/1 | TABLET | ORAL | 51407-485 |
| 5 mg/1 | TABLET | ORAL | 63629-9589 |
| 10 mg/1 | TABLET | ORAL | 67877-391 |
| 5 mg/1 | TABLET | ORAL | 70518-3527 |
| 5 mg/1 | TABLET | ORAL | 72241-033 |
| 2.5 mg/1 | TABLET | ORAL | 0904-7497 |
+ 38 more variants
Detailed information about Nebivolol
Nebivolol is a third-generation, highly selective beta-1 adrenergic blocker with unique vasodilatory properties mediated through the nitric oxide pathway, primarily used to treat hypertension.
For the management of hypertension, the dosing of Nebivolol must be individualized according to the patient's blood pressure response and heart rate.
The safety and effectiveness of Nebivolol in pediatric patients (under the age of 18) have not been established. Therefore, Nebivolol is not currently approved for pediatric use. Clinical trials in children are lacking, and the potential impact on growth and development remains unknown.
In patients with severe renal (kidney) impairment (Creatinine Clearance or CrCl less than 30 mL/min), the body may not clear the drug effectively. For these patients, the recommended starting dose is 2.5 mg once daily. Up-titration should be performed with extreme caution and close medical supervision.
For patients with moderate hepatic (liver) impairment, the starting dose should be 2.5 mg once daily. Nebivolol is contraindicated (should not be used) in patients with severe hepatic impairment (Child-Pugh Class C), as the liver is the primary site of metabolism for this medication.
In general, dose selection for an elderly patient should be cautious, usually starting at the low end of the dosing range (2.5 mg to 5 mg). While clinical studies did not show overall differences in safety between older and younger patients, the elderly are more likely to have decreased hepatic, renal, or cardiac function and may be taking other medications that interact with Nebivolol.
If you miss a dose of Nebivolol, take it as soon as you remember. However, if it is almost time for your next scheduled dose, skip the missed dose and resume your regular dosing schedule. Do not take two doses at once to make up for a missed one, as this increases the risk of severe side effects like a dangerously low heart rate or fainting.
An overdose of Nebivolol can be life-threatening. Symptoms of overdose include:
If an overdose is suspected, seek emergency medical attention immediately or contact a poison control center. Treatment usually involves supportive care, including intravenous fluids and medications like atropine or glucagon to increase the heart rate and improve cardiac function.
> Important: Follow your healthcare provider's dosing instructions exactly. Do not adjust your dose or stop taking this medication without medical guidance, as sudden discontinuation can cause serious heart problems.
Nebivolol is generally better tolerated than older beta-blockers, but side effects can still occur. The most frequently reported adverse reactions include:
Nebivolol is a potent cardiovascular medication that requires careful management. It is essential to understand that while it controls high blood pressure, it does not 'cure' it. Most patients will need to take antihypertensive medication indefinitely. You should never share this medication with others, even if they have similar symptoms.
According to the FDA-approved labeling for beta-blockers, including Nebivolol, patients with coronary artery disease who abruptly stop therapy may experience an exacerbation of angina pectoris (chest pain), myocardial infarction (heart attack), and ventricular arrhythmias. Even in patients without overt coronary artery disease, it is advised to taper the dose over 1 to 2 weeks. If angina occurs or acute coronary insufficiency develops, Nebivolol should be promptly reinstituted, at least temporarily.
There are certain medications that should never be combined with Nebivolol due to the risk of severe, life-threatening reactions:
Nebivolol must NEVER be used in patients with the following conditions, as the risks of life-threatening complications far outweigh any potential benefit:
Nebivolol is classified as Pregnancy Category C (under the older FDA system). There are no adequate and well-controlled studies in pregnant women. Animal studies have shown that Nebivolol can cause fetal harm, including decreased birth weight and increased fetal resorption.
Nebivolol should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.
It is not known whether Nebivolol is excreted in human milk. However, because many drugs are excreted in human milk and because of the potential for serious adverse reactions in nursing infants (such as bradycardia),
Nebivolol is a unique, long-acting, highly selective beta-1 adrenergic receptor antagonist. At the molecular level, it competes with catecholamines (like adrenaline) for binding sites on the beta-1 receptors in the heart.
What sets Nebivolol apart is its action on the endothelial nitric oxide synthase (eNOS) enzyme. It acts as a partial agonist at beta-3 adrenergic receptors in the blood vessels, which triggers the release of nitric oxide (NO). Nitric oxide then diffuses into the smooth muscle cells of the arteries, causing them to relax. This dual action—beta-1 blockade (reducing heart effort) and NO-mediated vasodilation (reducing vessel resistance)—lowers blood pressure more comprehensively than older beta-blockers.
Common questions about Nebivolol
Nebivolol is primarily used to treat hypertension, also known as high blood pressure. By lowering blood pressure, it helps prevent serious health problems such as strokes, heart attacks, and kidney issues. It works by slowing the heart rate and relaxing the blood vessels, making it easier for the heart to pump blood throughout the body. While its main FDA-approved use is for hypertension, some doctors may prescribe it off-label for other heart-related conditions like heart failure or chest pain. Always take this medication exactly as prescribed by your healthcare provider for your specific condition.
The most common side effects reported by patients taking Nebivolol include headaches, fatigue, and dizziness. Some people may also experience a tingling sensation in their hands or feet, known as paresthesia, or mild stomach issues like nausea or diarrhea. Because Nebivolol slows the heart rate, a slow pulse (bradycardia) is also a frequent occurrence. Most of these side effects are mild and tend to go away as your body gets used to the medication. However, if these symptoms persist or become bothersome, you should contact your doctor to discuss a possible dose adjustment.
It is generally recommended to limit or avoid alcohol while taking Nebivolol. Alcohol can increase the blood pressure-lowering effects of the medication, which may lead to excessive dizziness, lightheadedness, or even fainting, especially when you stand up from a sitting or lying position. Additionally, both alcohol and beta-blockers can have a depressant effect on the central nervous system, which might increase feelings of fatigue or sluggishness. If you choose to drink, do so in moderation and only after you know how Nebivolol affects you. Always consult your healthcare provider regarding your alcohol consumption habits.
Nebivolol is generally not recommended during pregnancy unless the potential benefits clearly outweigh the risks to the fetus. It is classified as Pregnancy Category C, meaning animal studies have shown potential harm, but there isn't enough data in humans. Taking beta-blockers during pregnancy can reduce blood flow to the placenta, which might lead to low birth weight or premature delivery. Babies born to mothers using Nebivolol may also experience low blood sugar or a slow heart rate at birth. If you are pregnant or planning to become pregnant, discuss alternative blood pressure treatments with your doctor immediately.
While Nebivolol begins to lower your heart rate and blood pressure within a few hours of the first dose, the full therapeutic effect on your blood pressure may not be reached for several weeks. Most doctors will wait about two weeks before deciding if your dose needs to be increased. It is important to continue taking the medication every day, even if you feel fine, as high blood pressure often has no symptoms. Do not stop taking the drug if you don't see an immediate change; consistent use is key to its effectiveness. Your doctor will monitor your progress through regular blood pressure checks.
No, you should never stop taking Nebivolol suddenly. Doing so can cause a 'rebound' effect, leading to a sudden and dangerous increase in blood pressure, chest pain (angina), or even a heart attack. This is because your heart becomes more sensitive to adrenaline while on the medication. If you need to stop taking Nebivolol, your doctor will provide a schedule to gradually reduce your dose over one to two weeks. This tapering process allows your heart to safely adjust to the change. Always seek medical advice before making any changes to how you take your heart medication.
If you miss a dose of Nebivolol, you should take it as soon as you remember. However, if it is almost time for your next scheduled dose (for example, within 8 hours), you should skip the missed dose and simply take the next one at your regular time. Never take two doses at once to 'catch up,' as this can cause your heart rate or blood pressure to drop to dangerously low levels. To help you remember your dose, try taking it at the same time every day, such as with breakfast. If you frequently miss doses, consider using a pill organizer or a reminder app.
Weight gain is not a common side effect of Nebivolol, especially when compared to older beta-blockers like Propranolol or Atenolol. Because Nebivolol has a unique effect on nitric oxide and is more selective for the heart, it generally does not interfere with metabolism or cause the significant fluid retention seen with older drugs in this class. However, if you notice a sudden, rapid weight gain (such as 3 pounds in a day or 5 pounds in a week), this could be a sign of worsening heart failure rather than a direct side effect of the drug. In such cases, you should contact your doctor immediately.
Nebivolol can interact with several other medications, so it is vital to share your full medication list with your doctor. It can have serious interactions with certain calcium channel blockers like Verapamil or Diltiazem, which can dangerously slow the heart. Other interactions include certain antidepressants like Fluoxetine (Prozac), which can increase the levels of Nebivolol in your blood. Even over-the-counter medicines like Ibuprofen or cold remedies containing stimulants can interfere with how well Nebivolol lowers your blood pressure. Your doctor will help you manage these combinations safely through dose adjustments or close monitoring.
Yes, Nebivolol is available as a generic medication. The brand-name version, Bystolic, was the primary form for many years, but several manufacturers now produce generic Nebivolol hydrochloride tablets in the same strengths (2.5mg, 5mg, 10mg, and 20mg). Generic versions are required by the FDA to have the same active ingredient, strength, and effectiveness as the brand-name drug, but they are typically much more affordable. If you are concerned about the cost of your medication, ask your pharmacist or doctor if the generic version of Nebivolol is an appropriate option for you.
Other drugs with the same active ingredient (Nebivolol)
> Warning: Stop taking Nebivolol and call your doctor immediately or seek emergency care if you experience any of the following:
With prolonged use, Nebivolol is generally considered 'metabolically neutral.' Unlike older beta-blockers, it typically does not cause significant increases in blood glucose or negatively impact cholesterol levels (triglycerides). However, long-term use requires monitoring of heart rate and kidney function. Some patients may develop a tolerance to the side effects over time, while others may find that fatigue persists. There is no evidence that Nebivolol causes long-term organ damage when used as directed.
Abrupt Cessation of Therapy: While Nebivolol does not have a unique 'boxed warning' separate from the class, all beta-blockers carry a critical warning regarding sudden discontinuation. If you stop taking Nebivolol abruptly, it can lead to a 'rebound' effect, characterized by severe hypertension, heart attacks, or ventricular arrhythmias (dangerous heart rhythms). If the drug must be stopped, it must be tapered gradually over 1 to 2 weeks under a doctor's supervision.
Report any unusual symptoms or persistent side effects to your healthcare provider immediately. They may adjust your dose or switch you to an alternative medication.
Regular follow-up appointments are necessary to ensure the medication is working correctly. Your doctor will likely monitor:
Nebivolol may cause dizziness or fatigue, especially during the first few weeks of treatment or after a dose increase. Do not drive, operate heavy machinery, or engage in dangerous activities until you know how this medication affects you.
Alcohol can enhance the blood pressure-lowering effect of Nebivolol, which may lead to excessive dizziness, lightheadedness, or fainting. It is generally advised to limit alcohol consumption while taking this medication.
As noted in the black box warning, never stop taking Nebivolol suddenly. If you need to stop the medication due to side effects or a change in treatment, your doctor will provide a tapering schedule. This usually involves cutting the dose in half every few days over a period of 14 days.
> Important: Discuss all your medical conditions, especially asthma, heart rhythm problems, or diabetes, with your healthcare provider before starting Nebivolol.
Nebivolol does not typically interfere with most common laboratory tests. However, it may affect the results of an Exercise Stress Test or a Glucagon Stimulation Test. Always inform the laboratory staff and your doctor of all medications you are taking before undergoing medical testing.
Most interactions with Nebivolol occur through two mechanisms:
> Important: Tell your doctor about ALL medications, supplements, and herbal products you are taking, including over-the-counter cold medicines which often contain stimulants.
In these cases, a doctor must perform a careful risk-benefit analysis:
Patients who have had a severe allergic reaction to other beta-blockers (such as Metoprolol, Atenolol, or Carvedilol) may be at an increased risk of a reaction to Nebivolol. While they are chemically different, the underlying pharmacological class is the same. Always report previous drug allergies to your provider.
> Important: Your healthcare provider will evaluate your complete medical history, including your heart rhythm and lung function, before prescribing Nebivolol.
Nebivolol is not approved for use in children. Its safety and effectiveness in the pediatric population have not been established. There is no data on how the drug affects growth, pubertal development, or long-term cardiovascular health in children.
In clinical trials, approximately 28% of patients were 65 years or older. No overall differences in efficacy or safety were observed between these patients and younger patients. However:
For patients with a Creatinine Clearance (CrCl) less than 30 mL/min, the clearance of Nebivolol is significantly reduced. These patients should start at a dose of 2.5 mg once daily. The dose should be increased very slowly. Nebivolol is not significantly removed by hemodialysis.
Nebivolol is extensively metabolized by the liver.
Failure to adjust the dose in patients with liver disease can lead to dangerously high levels of the drug in the system.
> Important: Special populations require individualized medical assessment and more frequent monitoring by a healthcare professional.
| Parameter | Value |
|---|---|
| Bioavailability | 12% (Extensive Metabolizers) to 96% (Poor Metabolizers) |
| Protein Binding | ~98% (primarily to Albumin) |
| Half-life | 12 hours (Extensive) to 19 hours (Poor) |
| Tmax (Time to peak) | 1.5 to 4 hours |
| Metabolism | Liver (CYP2D6 pathway) |
| Excretion | Urine (38%), Feces (44%) |
Nebivolol belongs to the therapeutic class of Antihypertensives and the pharmacological class of Beta-Adrenergic Blockers. Specifically, it is a 'Third-Generation Beta-Blocker,' a group that also includes Carvedilol and Labetalol, though Nebivolol is the only one in this group that is highly beta-1 selective.