Nebivolol 2.5mg 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; Vasodilator
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 (hypertension). It works by relaxing blood vessels and slowing down the heart rate, which helps the heart pump blood more easily throughout the body.
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, protected from light and moisture. Keep it in a dry place, away from bathrooms. Ensure all medications are stored 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 participate in a drug take-back program in your area.
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. Do not take two doses at the same time or take extra doses to make up for a missed one.
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, protected from light and moisture. Keep it in a dry place, away from bathrooms. Ensure all medications are stored 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 participate in a drug take-back program in your area.
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. Do not take two doses at the same time or take extra doses to make up for a missed one.
Lifestyle & Tips
- Continue to follow a healthy diet (e.g., low sodium, low fat).
- Engage in regular physical activity as advised by your doctor.
- Limit alcohol intake.
- Quit smoking.
- Manage stress effectively.
- Monitor your blood pressure and heart rate regularly at home as instructed.
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 10 mg, 20 mg, and 40 mg once daily based on response.
Hypertension (Elderly):
Initial: 2.5 mg orally once daily; may be increased to 5 mg once daily if needed.
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established
Child:
Not established
Adolescent:
Not established
Dose Adjustments
Renal Impairment:
Mild:
No adjustment needed (CrCl > 50 mL/min)
Moderate:
Initial: 2.5 mg orally once daily (CrCl 30-50 mL/min)
Severe:
Initial: 2.5 mg orally once daily (CrCl < 30 mL/min); titrate cautiously.
Dialysis:
Not significantly removed by dialysis; initial 2.5 mg once daily, titrate cautiously.
Hepatic Impairment:
Mild:
No adjustment needed
Moderate:
Initial: 2.5 mg orally once daily; titrate cautiously.
Severe:
Not recommended (Child-Pugh > B)
Pharmacology
Mechanism of Action
Nebivolol is a highly selective beta-1 adrenergic receptor blocker. It also produces vasodilation through an endothelium-derived nitric oxide (NO) dependent mechanism. This dual mechanism contributes to its antihypertensive effects by reducing heart rate, myocardial contractility, and systemic vascular resistance.
Pharmacokinetics
Absorption:
Bioavailability:
12% (extensive metabolizers), 96% (poor metabolizers)
Tmax:
1.5-4 hours
FoodEffect:
Food increases absorption (AUC and Cmax increased by 21% and 23% respectively, but not clinically significant for dosing).
Distribution:
Vd:
6.3 L/kg (extensive metabolizers), 20.2 L/kg (poor metabolizers)
ProteinBinding:
Approximately 98% (primarily to albumin)
CnssPenetration:
Limited
Elimination:
HalfLife:
10-12 hours (extensive metabolizers), 20-50 hours (poor metabolizers)
Clearance:
Not available
ExcretionRoute:
Approximately 38% renal, 48% fecal (as metabolites and unchanged drug)
Unchanged:
Less than 0.5% in urine
Pharmacodynamics
OnsetOfAction:
Within hours (for blood pressure reduction)
PeakEffect:
1-2 weeks (for full antihypertensive effect)
DurationOfAction:
24 hours
Safety & Warnings
Side Effects
Urgent Side Effects: Seek Medical Help Right Away
Although rare, this medication can cause severe and potentially life-threatening side effects. If you experience any of the following symptoms, contact your doctor or seek medical attention immediately:
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, significant weight gain, or swelling in the arms or legs
Slow heartbeat
Other Possible Side Effects
Like all medications, this drug can cause side effects. While many people may not experience any side effects or only minor ones, it's essential to discuss any concerns with your doctor. If you experience any of the following side effects or any other unusual symptoms that bother you or do not go away, contact your doctor:
Headache
* Feeling tired or weak
Reporting Side Effects
This list is not exhaustive, and you may experience other side effects. If you have questions or concerns, 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.
Although rare, this medication can cause severe and potentially life-threatening side effects. If you experience any of the following symptoms, contact your doctor or seek medical attention immediately:
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, significant weight gain, or swelling in the arms or legs
Slow heartbeat
Other Possible Side Effects
Like all medications, this drug can cause side effects. While many people may not experience any side effects or only minor ones, it's essential to discuss any concerns with your doctor. If you experience any of the following side effects or any other unusual symptoms that bother you or do not go away, contact your doctor:
Headache
* Feeling tired or weak
Reporting Side Effects
This list is not exhaustive, and you may experience other side effects. If you have questions or concerns, 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 (e.g., less than 50 beats per minute)
- Difficulty breathing or worsening shortness of breath
- Swelling in your hands, ankles, or feet
- Unusual weight gain
- Chest pain or discomfort
- 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 if it is safe to take this medication with your other medications and health conditions. Do not initiate, discontinue, or modify 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 if it is safe to take this medication with your other medications and health conditions. Do not initiate, discontinue, or modify the dose of any medication without first consulting your doctor.
Precautions & Cautions
Important Warnings and Cautions
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
Avoid driving and performing tasks that require alertness until you understand how this medication affects you. To minimize the risk of dizziness or fainting, rise slowly from a sitting or lying 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 blood work done as directed by your doctor, and discuss the results with them.
Interference with Lab Tests
This medication may affect certain laboratory tests. Inform all your healthcare providers and lab personnel that you are taking this medication.
Alcohol Consumption
Discuss alcohol consumption with your doctor before drinking, as this medication may mask symptoms of low blood sugar, such as a rapid heartbeat, which can increase the risk of severe or prolonged low blood sugar. This is particularly important for individuals with diabetes, children, and those who are fasting, undergoing surgery, or experiencing nausea and vomiting.
Diabetes Management
If you have high blood sugar (diabetes), closely monitor your blood sugar levels while taking this medication.
Over-the-Counter (OTC) Products
Before using OTC 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.
Discontinuing the Medication
Do not stop taking this medication abruptly, as this may lead to worsened chest pain or even a heart attack, particularly in individuals with certain types of heart disease. To avoid side effects, your doctor will instruct you on how to gradually discontinue the 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 a 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 before discontinuing the medication.
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
Avoid driving and performing tasks that require alertness until you understand how this medication affects you. To minimize the risk of dizziness or fainting, rise slowly from a sitting or lying 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 blood work done as directed by your doctor, and discuss the results with them.
Interference with Lab Tests
This medication may affect certain laboratory tests. Inform all your healthcare providers and lab personnel that you are taking this medication.
Alcohol Consumption
Discuss alcohol consumption with your doctor before drinking, as this medication may mask symptoms of low blood sugar, such as a rapid heartbeat, which can increase the risk of severe or prolonged low blood sugar. This is particularly important for individuals with diabetes, children, and those who are fasting, undergoing surgery, or experiencing nausea and vomiting.
Diabetes Management
If you have high blood sugar (diabetes), closely monitor your blood sugar levels while taking this medication.
Over-the-Counter (OTC) Products
Before using OTC 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.
Discontinuing the Medication
Do not stop taking this medication abruptly, as this may lead to worsened chest pain or even a heart attack, particularly in individuals with certain types of heart disease. To avoid side effects, your doctor will instruct you on how to gradually discontinue the 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 a 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 before discontinuing the medication.
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 insufficiency
- Cardiogenic shock
- Bronchospasm
- Vomiting
- Impaired consciousness
- Generalized convulsions
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, including atropine for bradycardia, vasopressors for hypotension, glucagon, and possibly intravenous fluids.
Drug Interactions
Contraindicated Interactions
- Not applicable (no absolute drug-drug contraindications listed, but contraindications for use include severe bradycardia, heart block greater than first degree, cardiogenic shock, decompensated cardiac failure, sick sinus syndrome, severe hepatic impairment, and hypersensitivity).
Major Interactions
- CYP2D6 inhibitors (e.g., fluoxetine, paroxetine, quinidine, propafenone, thioridazine): May significantly increase nebivolol plasma concentrations, leading to increased beta-blocking effects (bradycardia, hypotension). Dose reduction of nebivolol may be necessary.
- Other antihypertensives (e.g., ACE inhibitors, ARBs, diuretics, calcium channel blockers): Additive hypotensive effects.
- Antiarrhythmics (e.g., amiodarone, disopyramide, quinidine): Increased risk of bradycardia and AV block.
- Digoxin: Increased risk of bradycardia.
- Clonidine: Potentiation of rebound hypertension upon clonidine withdrawal; discontinue nebivolol several days before gradual withdrawal of clonidine.
Moderate Interactions
- 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 beta-blockers and lead to severe hypertension and bradycardia.
Minor Interactions
- Not available
Monitoring
Baseline Monitoring
Blood Pressure (BP)
Rationale: To establish baseline and guide initial dosing.
Timing: Prior to initiation of therapy.
Heart Rate (HR)
Rationale: To establish baseline and assess for bradycardia.
Timing: Prior to initiation of therapy.
Renal Function (SCr, eGFR)
Rationale: To assess kidney function and guide dose adjustments in renal impairment.
Timing: Prior to initiation of therapy.
Hepatic Function (ALT, AST, Bilirubin)
Rationale: To assess liver function and guide dose adjustments in hepatic impairment.
Timing: Prior to initiation of therapy.
Routine Monitoring
Blood Pressure (BP)
Frequency: Regularly, especially after dose adjustments and during maintenance therapy.
Target: <130/80 mmHg (individualized based on guidelines and patient comorbidities)
Action Threshold: Persistent BP above target or symptomatic hypotension.
Heart Rate (HR)
Frequency: Regularly, especially after dose adjustments.
Target: 50-90 bpm (avoid symptomatic bradycardia <50 bpm)
Action Threshold: HR <50 bpm or symptomatic bradycardia.
Symptoms of Heart Failure
Frequency: Regularly, especially in patients with pre-existing heart failure.
Target: Absence of worsening symptoms (e.g., dyspnea, edema, weight gain)
Action Threshold: Worsening heart failure symptoms.
Blood Glucose (for diabetics)
Frequency: Regularly
Target: Individualized
Action Threshold: Unexplained hypoglycemia or hyperglycemia.
Symptom Monitoring
- Dizziness
- Lightheadedness
- Fatigue
- Bradycardia (slow heart rate)
- Shortness of breath
- Swelling in ankles/feet
- Cold extremities
- Depression
- Insomnia
Special Patient Groups
Pregnancy
Nebivolol is classified as Pregnancy Category C. It should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. Beta-blockers can cause adverse effects in the fetus/neonate, including bradycardia, hypoglycemia, and respiratory depression.
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, respiratory depression, and prolonged labor. Monitor neonates for signs of beta-blockade for several days after birth.
Lactation
Nebivolol and its active metabolites are excreted in human milk. Due to the potential for serious adverse reactions in breastfed infants (e.g., bradycardia, hypotension, hypoglycemia), 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:
Low to moderate risk. Monitor infant for signs of beta-blockade (e.g., bradycardia, lethargy, poor feeding).
Pediatric Use
Safety and effectiveness in pediatric patients have not been established. Use is generally not recommended.
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 a lower dose (2.5 mg once daily) and titrate cautiously due to potential for increased sensitivity and decreased renal/hepatic function.
Clinical Information
Clinical Pearls
- Nebivolol is unique among beta-blockers due to its additional vasodilatory effect mediated by nitric oxide, which may contribute to better tolerability and potentially less impact on lipid profiles and glucose metabolism compared to older beta-blockers.
- Due to its metabolism by CYP2D6, patients who are poor metabolizers of CYP2D6 will have significantly higher plasma concentrations of nebivolol and its active metabolites, requiring lower doses.
- Abrupt discontinuation of beta-blockers, including nebivolol, can exacerbate angina, myocardial infarction, and ventricular arrhythmias, particularly in patients with coronary artery disease. Taper dose gradually over 1-2 weeks.
- Nebivolol is highly beta-1 selective, but selectivity is dose-dependent and may decrease at higher doses, potentially affecting patients with asthma or COPD.
- Monitor for signs of worsening heart failure, especially when initiating or increasing the dose in patients with compensated heart failure.
Alternative Therapies
- Other Beta-blockers (e.g., metoprolol, carvedilol, atenolol, bisoprolol)
- ACE Inhibitors (e.g., lisinopril, enalapril)
- Angiotensin Receptor Blockers (ARBs) (e.g., losartan, valsartan)
- Calcium Channel Blockers (e.g., amlodipine, diltiazem, verapamil)
- Thiazide Diuretics (e.g., hydrochlorothiazide, chlorthalidone)
Cost & Coverage
Average Cost:
$10 - $50 (generic) per 30 tablets
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's a good idea to check with your pharmacist for more information. If you have any questions or concerns about your medication, don't hesitate to reach out to 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.