Nebivolol 5mg Tablets
It is used to treat high blood pressure.It may be given to you for other reasons. Talk with the doctor.
Drug Class
Antihypertensive
Pharmacologic Class
Beta-1 Selective Adrenergic Blocker with Vasodilating Properties
Pregnancy Category
Category C
FDA Approved
Dec 2007
DEA Schedule
Not Controlled
Overview
What is this medicine?
Nebivolol is a medication used to treat high blood pressure. It works by relaxing blood vessels and slowing down your heart rate, which helps your heart pump blood more easily throughout your body. This can lower your blood pressure and reduce the strain on your heart.
How to Use This Medicine
Taking Your Medication
To use this medication correctly, follow your doctor's instructions and read all the information provided. Take your medication as directed, with or without food. Continue taking it even if you feel well, unless your doctor or healthcare provider advises you to stop.
Storing and Disposing of Your Medication
Store your medication at room temperature, away from light and moisture. Keep it in a dry place, avoiding storage in a bathroom. Ensure all medications are kept in a safe location, out of reach of children and pets. When disposing of unused or expired medication, do not flush it down the toilet or pour it down the drain unless instructed to do so. Instead, check with your pharmacist for guidance on proper disposal or explore local drug take-back programs.
Missing a Dose
If you miss a dose, take it as soon as you remember. However, if it's close to the time for your next scheduled dose, skip the missed dose and resume your regular dosing schedule. Avoid taking two doses at the same time or taking extra doses.
To use this medication correctly, follow your doctor's instructions and read all the information provided. Take your medication as directed, with or without food. Continue taking it even if you feel well, unless your doctor or healthcare provider advises you to stop.
Storing and Disposing of Your Medication
Store your medication at room temperature, away from light and moisture. Keep it in a dry place, avoiding storage in a bathroom. Ensure all medications are kept in a safe location, out of reach of children and pets. When disposing of unused or expired medication, do not flush it down the toilet or pour it down the drain unless instructed to do so. Instead, check with your pharmacist for guidance on proper disposal or explore local drug take-back programs.
Missing a Dose
If you miss a dose, take it as soon as you remember. However, if it's close to the time for your next scheduled dose, skip the missed dose and resume your regular dosing schedule. Avoid taking two doses at the same time or taking extra doses.
Lifestyle & Tips
- Take nebivolol exactly as prescribed by your doctor, usually once a day, with or without food.
- Do not stop taking this medication suddenly, as it can worsen your condition, especially if you have heart disease. Your doctor will tell you how to gradually reduce the dose if needed.
- Continue to follow a heart-healthy diet (low in salt, saturated fat, and cholesterol).
- Engage in regular physical activity as recommended by your doctor.
- Limit alcohol intake, as it can further lower blood pressure.
- Avoid activities requiring mental alertness, such as driving or operating machinery, until you know how this medication affects you, as it may cause dizziness or fatigue.
- Monitor your blood pressure and heart rate regularly at home if advised by your doctor.
Available Forms & Alternatives
Available Strengths:
Dosing & Administration
Adult Dosing
Standard Dose:
5 mg orally once daily
Dose Range:
2.5 - 40 mg
Condition-Specific Dosing:
hypertension:
Initial 5 mg orally once daily; may be increased at 2-week intervals to a maximum of 40 mg once daily. Doses above 5 mg should be individualized based on patient response and tolerability.
heart_failure:
Not FDA approved for heart failure in the US, but used off-label in some regions. Dosing typically starts at 1.25 mg once daily and titrated slowly.
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established
Child:
Not established
Adolescent:
Not established
Dose Adjustments
Renal Impairment:
Mild:
No dosage adjustment required (CrCl > 50 mL/min)
Moderate:
Initial dose 2.5 mg orally once daily (CrCl 30-50 mL/min). Titrate cautiously.
Severe:
Initial dose 2.5 mg orally once daily (CrCl < 30 mL/min). Titrate cautiously. Limited clinical experience.
Dialysis:
Not studied in patients on dialysis. Use with caution and monitor closely.
Hepatic Impairment:
Mild:
No dosage adjustment required (Child-Pugh A)
Moderate:
Initial dose 2.5 mg orally once daily (Child-Pugh B). Titrate cautiously.
Severe:
Not recommended (Child-Pugh C). Not studied in patients with severe hepatic impairment.
Pharmacology
Mechanism of Action
Nebivolol is a beta-1 selective adrenergic receptor blocker. It competitively and selectively blocks beta-1 adrenergic receptors, leading to decreased heart rate, myocardial contractility, and cardiac output, thus lowering blood pressure. Additionally, nebivolol causes vasodilation, which is mediated by nitric oxide release from endothelial cells, contributing to its antihypertensive effect.
Pharmacokinetics
Absorption:
Bioavailability:
12% (extensive metabolizers), 96% (poor metabolizers) due to CYP2D6 polymorphism
Tmax:
1.5-4 hours (nebivolol), 3-6 hours (active hydroxyl metabolites)
FoodEffect:
Food increases absorption slightly but does not significantly affect overall exposure.
Distribution:
Vd:
Approximately 6.3 L/kg
ProteinBinding:
Approximately 98% (primarily to albumin)
CnssPenetration:
Limited
Elimination:
HalfLife:
10-12 hours (extensive metabolizers), 20-24 hours (poor metabolizers) for nebivolol; 24-30 hours for active metabolites
Clearance:
Not available (highly variable due to metabolism)
ExcretionRoute:
Approximately 38% in urine and 48% in feces (as metabolites and unchanged drug)
Unchanged:
Less than 0.5% in urine
Pharmacodynamics
OnsetOfAction:
Within 1-2 hours
PeakEffect:
Within 2-4 weeks of consistent dosing for full antihypertensive effect
DurationOfAction:
24 hours (allows once-daily dosing)
Confidence:
Medium
Safety & Warnings
BLACK BOX WARNING
Abrupt Cessation of Therapy: Do not abruptly discontinue nebivolol therapy, especially in patients with ischemic heart disease. Severe exacerbation of angina, myocardial infarction, and ventricular arrhythmias have been reported following abrupt discontinuation of beta-blocker therapy. When discontinuing chronically administered nebivolol, particularly in patients with ischemic heart disease, the dosage should be gradually reduced over 1 to 2 weeks and the patient should be carefully monitored. If angina worsens or acute coronary insufficiency develops, nebivolol administration should be reinstituted promptly, at least temporarily, and other measures appropriate for the management of angina pectoris should be taken. Patients should be warned against interruption or discontinuation of therapy without the physician's advice.
Side Effects
Urgent Side Effects: Seek Medical Help Right Away
While rare, some people may experience severe and potentially life-threatening side effects when taking this medication. If you notice any of the following symptoms, contact your doctor or seek immediate medical attention:
Signs of an allergic reaction, such as:
+ Rash
+ Hives
+ Itching
+ Red, swollen, blistered, or peeling skin with or without fever
+ Wheezing
+ Tightness in the chest or throat
+ Trouble breathing, swallowing, or talking
+ Unusual hoarseness
+ Swelling of the mouth, face, lips, tongue, or throat
Signs of low blood sugar, including:
+ Dizziness
+ Headache
+ Feeling sleepy
+ Feeling weak
+ Shaking
+ Fast heartbeat
+ Confusion
+ Hunger
+ Sweating
Dizziness or fainting
Shortness of breath
Sudden weight gain or swelling in the arms or legs
Slow heartbeat
Other Possible Side Effects
Like all medications, this drug can cause side effects. However, many people do not experience any side effects or only have mild ones. If you are bothered by any of the following side effects or if they do not go away, contact your doctor:
Headache
Feeling tired or weak
Reporting Side Effects
This is not a complete list of possible side effects. If you have questions or concerns about side effects, contact your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
While rare, some people may experience severe and potentially life-threatening side effects when taking this medication. If you notice any of the following symptoms, contact your doctor or seek immediate medical attention:
Signs of an allergic reaction, such as:
+ Rash
+ Hives
+ Itching
+ Red, swollen, blistered, or peeling skin with or without fever
+ Wheezing
+ Tightness in the chest or throat
+ Trouble breathing, swallowing, or talking
+ Unusual hoarseness
+ Swelling of the mouth, face, lips, tongue, or throat
Signs of low blood sugar, including:
+ Dizziness
+ Headache
+ Feeling sleepy
+ Feeling weak
+ Shaking
+ Fast heartbeat
+ Confusion
+ Hunger
+ Sweating
Dizziness or fainting
Shortness of breath
Sudden weight gain or swelling in the arms or legs
Slow heartbeat
Other Possible Side Effects
Like all medications, this drug can cause side effects. However, many people do not experience any side effects or only have mild ones. If you are bothered by any of the following side effects or if they do not go away, contact your doctor:
Headache
Feeling tired or weak
Reporting Side Effects
This is not a complete list of possible side effects. If you have questions or concerns about side effects, contact your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
Seek Immediate Medical Attention If You Experience:
- Severe dizziness or fainting
- Very slow heart rate (less than 50 beats per minute)
- Shortness of breath, especially with exertion or at rest
- Swelling in your ankles or feet
- Unusual weight gain
- Chest pain or discomfort that worsens
- Coldness or numbness in your hands or feet
- Symptoms of depression (e.g., persistent sadness, loss of interest)
Before Using This Medicine
Before Taking This Medication: Important Information to Share with Your Doctor
It is essential to inform your doctor about the following:
Any allergies you have, including allergies to this medication, its components, or other substances, such as foods or drugs. Describe the allergic reaction you experienced, including the symptoms that occurred.
Certain health conditions, including:
+ Asthma or other lung or breathing problems that cause shortness of breath or wheezing
+ Heart failure (weak heart)
+ Abnormal heartbeats, such as heart block or sick sinus syndrome
+ A slow heartbeat
Liver disease
Use of another medication similar to this one. If you are unsure, consult your doctor or pharmacist for clarification.
* Breast-feeding. It is recommended that you do not breast-feed while taking this medication.
This list is not exhaustive, and it is crucial to discuss all your medications (prescription, over-the-counter, natural products, and vitamins) and health problems with your doctor and pharmacist. They will help determine whether it is safe to take this medication with your existing health conditions and other medications. Never start, stop, or change the dose of any medication without first consulting your doctor.
It is essential to inform your doctor about the following:
Any allergies you have, including allergies to this medication, its components, or other substances, such as foods or drugs. Describe the allergic reaction you experienced, including the symptoms that occurred.
Certain health conditions, including:
+ Asthma or other lung or breathing problems that cause shortness of breath or wheezing
+ Heart failure (weak heart)
+ Abnormal heartbeats, such as heart block or sick sinus syndrome
+ A slow heartbeat
Liver disease
Use of another medication similar to this one. If you are unsure, consult your doctor or pharmacist for clarification.
* Breast-feeding. It is recommended that you do not breast-feed while taking this medication.
This list is not exhaustive, and it is crucial to discuss all your medications (prescription, over-the-counter, natural products, and vitamins) and health problems with your doctor and pharmacist. They will help determine whether it is safe to take this medication with your existing health conditions and other medications. Never start, stop, or change the dose of any medication without first consulting your doctor.
Precautions & Cautions
Important Warnings and Precautions
It is essential to inform all your healthcare providers, including doctors, nurses, pharmacists, and dentists, that you are taking this medication.
Caution with Daily Activities
Until you know how this medication affects you, avoid driving and other tasks that require alertness. To minimize the risk of dizziness or fainting, rise slowly from a sitting or lying down position, and be cautious when climbing stairs.
Monitoring Your Condition
Follow your doctor's instructions for checking your blood pressure and heart rate. Additionally, have your blood work checked as directed by your doctor, and discuss any concerns with them.
Interference with Lab Tests
This medication may affect certain laboratory tests. Be sure to inform all your healthcare providers and lab personnel that you are taking this medication.
Alcohol Consumption
Before consuming alcohol, consult with your doctor. This medication may mask symptoms of low blood sugar, such as rapid heartbeat, which can increase the risk of severe or prolonged hypoglycemia, especially in individuals with diabetes, children, and those who are fasting or undergoing surgery.
Diabetes Management
If you have high blood sugar (diabetes), it is crucial to closely monitor your blood sugar levels while taking this medication.
Over-the-Counter Medications
Before using over-the-counter products that may increase blood pressure, such as cough or cold medications, diet pills, stimulants, non-steroidal anti-inflammatory drugs (NSAIDs) like ibuprofen or naproxen, or certain natural products, consult with your doctor.
Stopping the Medication
Do not stop taking this medication abruptly, as this may lead to worsening chest pain or even a heart attack, especially in individuals with certain types of heart disease. To avoid side effects, your doctor will instruct you on how to gradually stop taking this medication. If you experience new or worsening chest pain or other heart problems, contact your doctor immediately.
Allergic Reactions
If you have a history of severe allergic reactions, discuss this with your doctor, as you may be at risk of an even more severe reaction. If you use epinephrine to treat severe allergic reactions, inform your doctor, as this medication may reduce the effectiveness of epinephrine.
Thyroid Conditions
This medication may make it more challenging to recognize symptoms of an overactive thyroid, such as rapid heartbeat. If you have an overactive thyroid and stop taking this medication suddenly, your condition may worsen and become life-threatening. Consult with your doctor for guidance.
Pregnancy
If you are pregnant or plan to become pregnant, discuss the benefits and risks of taking this medication with your doctor.
It is essential to inform all your healthcare providers, including doctors, nurses, pharmacists, and dentists, that you are taking this medication.
Caution with Daily Activities
Until you know how this medication affects you, avoid driving and other tasks that require alertness. To minimize the risk of dizziness or fainting, rise slowly from a sitting or lying down position, and be cautious when climbing stairs.
Monitoring Your Condition
Follow your doctor's instructions for checking your blood pressure and heart rate. Additionally, have your blood work checked as directed by your doctor, and discuss any concerns with them.
Interference with Lab Tests
This medication may affect certain laboratory tests. Be sure to inform all your healthcare providers and lab personnel that you are taking this medication.
Alcohol Consumption
Before consuming alcohol, consult with your doctor. This medication may mask symptoms of low blood sugar, such as rapid heartbeat, which can increase the risk of severe or prolonged hypoglycemia, especially in individuals with diabetes, children, and those who are fasting or undergoing surgery.
Diabetes Management
If you have high blood sugar (diabetes), it is crucial to closely monitor your blood sugar levels while taking this medication.
Over-the-Counter Medications
Before using over-the-counter products that may increase blood pressure, such as cough or cold medications, diet pills, stimulants, non-steroidal anti-inflammatory drugs (NSAIDs) like ibuprofen or naproxen, or certain natural products, consult with your doctor.
Stopping the Medication
Do not stop taking this medication abruptly, as this may lead to worsening chest pain or even a heart attack, especially in individuals with certain types of heart disease. To avoid side effects, your doctor will instruct you on how to gradually stop taking this medication. If you experience new or worsening chest pain or other heart problems, contact your doctor immediately.
Allergic Reactions
If you have a history of severe allergic reactions, discuss this with your doctor, as you may be at risk of an even more severe reaction. If you use epinephrine to treat severe allergic reactions, inform your doctor, as this medication may reduce the effectiveness of epinephrine.
Thyroid Conditions
This medication may make it more challenging to recognize symptoms of an overactive thyroid, such as rapid heartbeat. If you have an overactive thyroid and stop taking this medication suddenly, your condition may worsen and become life-threatening. Consult with your doctor for guidance.
Pregnancy
If you are pregnant or plan to become pregnant, discuss the benefits and risks of taking this medication with your doctor.
Overdose Information
Overdose Symptoms:
- Severe bradycardia (very slow heart rate)
- Hypotension (very low blood pressure)
- Acute cardiac failure
- Cardiogenic shock
- Bronchospasm
- Vomiting
- Impaired consciousness
- Generalized seizures
What to Do:
Seek immediate medical attention. Call 911 or your local emergency number. For poison control, call 1-800-222-1222. Treatment is supportive and symptomatic, and may include atropine for bradycardia, vasopressors for hypotension, glucagon, and/or intravenous fluids.
Drug Interactions
Major Interactions
- CYP2D6 inhibitors (e.g., fluoxetine, paroxetine, quinidine, propafenone, thioridazine): May significantly increase nebivolol plasma concentrations, leading to increased beta-blocking effects (e.g., bradycardia, hypotension).
- Other beta-blockers (e.g., atenolol, metoprolol): Additive effects on heart rate and blood pressure.
- Calcium channel blockers (e.g., verapamil, diltiazem): Increased risk of bradycardia, AV block, and heart failure.
- Clonidine: Potentiation of rebound hypertension upon clonidine withdrawal.
Moderate Interactions
- Digoxin: Increased risk of bradycardia.
- Antiarrhythmics (e.g., amiodarone, disopyramide): Increased risk of bradycardia and AV block.
- NSAIDs (e.g., ibuprofen, naproxen): May attenuate the antihypertensive effect of nebivolol.
- Insulin and oral hypoglycemics: Beta-blockers may mask symptoms of hypoglycemia (e.g., tachycardia) and prolong hypoglycemic episodes.
- Sympathomimetics (e.g., epinephrine, norepinephrine): May antagonize the effects of nebivolol and increase risk of hypertension and bradycardia.
Minor Interactions
- Alcohol: May enhance hypotensive effects.
Monitoring
Baseline Monitoring
Blood Pressure (BP)
Rationale: To establish baseline and guide initial dosing.
Timing: Prior to initiation
Heart Rate (HR)
Rationale: To establish baseline and assess for bradycardia.
Timing: Prior to initiation
Renal Function (SCr, eGFR)
Rationale: To assess kidney function and guide dose adjustment in renal impairment.
Timing: Prior to initiation
Hepatic Function (ALT, AST, Bilirubin)
Rationale: To assess liver function and guide dose adjustment in hepatic impairment.
Timing: Prior to initiation
Routine Monitoring
Blood Pressure (BP)
Frequency: Regularly, especially after dose adjustments and during maintenance therapy (e.g., weekly initially, then monthly or quarterly)
Target: <130/80 mmHg (individualized based on guidelines and patient comorbidities)
Action Threshold: If BP remains uncontrolled or drops excessively low (e.g., <90/60 mmHg).
Heart Rate (HR)
Frequency: Regularly, especially after dose adjustments and during maintenance therapy
Target: 50-70 bpm (avoiding symptomatic bradycardia)
Action Threshold: If HR < 50 bpm or symptomatic bradycardia occurs.
Symptoms of Hypotension/Bradycardia
Frequency: Ongoing patient assessment
Target: N/A
Action Threshold: Dizziness, lightheadedness, fatigue, syncope.
Symptom Monitoring
- Dizziness
- Lightheadedness
- Fatigue
- Bradycardia (slow heart rate)
- Hypotension (low blood pressure)
- Shortness of breath (especially in patients with underlying respiratory conditions)
- Peripheral edema
- Cold extremities
- Insomnia
- Depression
Special Patient Groups
Pregnancy
Nebivolol is classified as Pregnancy Category C. There are no adequate and well-controlled studies in pregnant women. Use during pregnancy only if the potential benefit justifies the potential risk to the fetus. Beta-blockers can cause fetal bradycardia, hypotension, and hypoglycemia. Neonates exposed to beta-blockers in utero may be at risk for these effects for several days after birth.
Trimester-Specific Risks:
First Trimester:
Limited data, but generally avoided unless clearly needed.
Second Trimester:
Potential for fetal growth restriction, bradycardia, and hypoglycemia.
Third Trimester:
Increased risk of neonatal bradycardia, hypoglycemia, and respiratory depression. Monitor neonate for several days post-delivery.
Lactation
Nebivolol is excreted in human milk. Due to the potential for serious adverse reactions in breastfed infants (e.g., bradycardia, hypotension), a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother.
Infant Risk:
L3 (Moderately Safe) - Monitor infant for signs of beta-blockade (bradycardia, hypotension, lethargy, poor feeding). Consider alternative agents or lowest effective dose.
Pediatric Use
Safety and effectiveness in pediatric patients have not been established. Not recommended for use in children.
Geriatric Use
No overall differences in safety or effectiveness were observed between elderly and younger patients, but greater sensitivity of some older individuals cannot be ruled out. Start with the lowest effective dose (e.g., 2.5 mg) and titrate slowly, monitoring for adverse effects.
Clinical Information
Clinical Pearls
- Nebivolol is a highly selective beta-1 blocker with an additional vasodilatory effect mediated by nitric oxide, which may lead to a more favorable hemodynamic profile compared to other beta-blockers.
- Due to CYP2D6 polymorphism, there is significant inter-individual variability in nebivolol exposure. Poor metabolizers will have higher plasma concentrations and may require lower doses.
- Always warn patients about the black box warning regarding abrupt discontinuation, especially if they have underlying ischemic heart disease.
- Nebivolol is generally considered to have less impact on lipid profiles and glucose metabolism compared to non-selective beta-blockers, but caution is still advised in diabetic patients as it can mask hypoglycemic symptoms.
- Monitor for signs of heart failure exacerbation, especially in patients with pre-existing cardiac conditions, as beta-blockers can worsen heart failure in some cases.
Alternative Therapies
- Other Beta-blockers (e.g., Metoprolol, Atenolol, Bisoprolol, Carvedilol)
- ACE Inhibitors (e.g., Lisinopril, Enalapril)
- Angiotensin Receptor Blockers (ARBs) (e.g., Valsartan, Losartan)
- Calcium Channel Blockers (e.g., Amlodipine, Nifedipine, Diltiazem, Verapamil)
- Thiazide Diuretics (e.g., Hydrochlorothiazide, Chlorthalidone)
Cost & Coverage
Average Cost:
$15 - $100+ per 30 tablets (5mg)
Generic Available:
Yes
Insurance Coverage:
Tier 1 or Tier 2 (for generic)
General Drug Facts
If your symptoms or health issues persist or worsen, it is essential to contact your doctor promptly. To ensure safe and effective treatment, never share your medication with others or take someone else's medication. Some medications may come with an additional patient information leaflet, so it is a good idea to check with your pharmacist for more information. If you have any questions or concerns about your medication, do not hesitate to discuss them with your doctor, nurse, pharmacist, or other healthcare provider. In the event of a suspected overdose, immediately call your local poison control center or seek emergency medical attention. When seeking help, be prepared to provide details about the medication taken, the amount, and the time it happened.