Usage
- Medical Conditions: Nebivolol + Valsartan is prescribed for the treatment of hypertension (high blood pressure). It is used when treatment with either nebivolol or valsartan alone does not adequately control blood pressure.
- Pharmacological Classification: Antihypertensive, combining a beta-blocker (nebivolol) and an angiotensin II receptor blocker (ARB) (valsartan).
- Mechanism of Action: Nebivolol reduces heart rate and blood pressure by blocking beta-adrenergic receptors in the heart and blood vessels. Valsartan blocks the action of angiotensin II, a hormone that causes vasoconstriction (narrowing of blood vessels), leading to vasodilation and a decrease in blood pressure. The combination of these two mechanisms provides a synergistic effect in lowering blood pressure.
Alternate Names
- No widely used alternate generic names.
- Brand Names: Byvalson (discontinued in some regions).
How It Works
- Pharmacodynamics: Nebivolol decreases heart rate, myocardial contractility, and peripheral vascular resistance. Valsartan blocks the binding of angiotensin II to its receptors, resulting in vasodilation.
- Pharmacokinetics: Nebivolol is well-absorbed orally and extensively metabolized by the liver, primarily by CYP2D6. Valsartan is also well-absorbed and has high bioavailability. It is minimally metabolized and primarily excreted unchanged in the bile. Both drugs reach peak plasma concentrations within a few hours.
- Mode of Action: Nebivolol is a highly selective beta-1 adrenergic receptor blocker with some vasodilating properties. It may also increase nitric oxide production, which contributes to vasodilation. Valsartan selectively blocks the AT1 subtype of angiotensin II receptors, preventing angiotensin II-mediated vasoconstriction and aldosterone secretion.
- Receptor Binding/Enzyme Inhibition: Nebivolol binds to beta-1 adrenergic receptors. Valsartan blocks AT1 angiotensin II receptors.
- Elimination Pathways: Nebivolol is primarily eliminated by hepatic metabolism followed by renal excretion. Valsartan is mainly eliminated by biliary excretion with a small amount excreted renally.
Dosage
Standard Dosage
Adults:
- Initial dose: One tablet of 5 mg nebivolol/80 mg valsartan once daily.
- Maximum dose: One tablet of 5 mg nebivolol/80 mg valsartan once daily. Higher doses do not significantly improve blood pressure control.
Children:
- Not recommended for use in children under 18 years of age. Safety and efficacy have not been established.
Special Cases:
- Elderly Patients: No specific dosage adjustment is typically required, but caution is advised due to potential age-related decline in organ function.
- Patients with Renal Impairment: No dosage adjustment is generally required for mild to moderate renal impairment. Not recommended as initial therapy for severe renal impairment (creatinine clearance < 30 mL/min).
- Patients with Hepatic Dysfunction: No dosage adjustment is required for mild hepatic impairment. Not recommended as initial therapy for moderate hepatic impairment. Contraindicated in severe hepatic impairment.
- Patients with Comorbid Conditions: Caution is advised in patients with diabetes, as nebivolol may mask symptoms of hypoglycemia. Monitor blood glucose levels closely in these patients.
Clinical Use Cases
- Not typically used in clinical settings such as intubation, surgical procedures, mechanical ventilation, or emergency situations. Its primary indication is chronic hypertension management.
Dosage Adjustments
- Adjust dose based on patient response and tolerability.
- Consider renal/hepatic function, comorbidities, and concurrent medications.
Side Effects
Common Side Effects
- Dizziness
- Headache
- Fatigue
- Slow heart rate (bradycardia)
- Low blood pressure (hypotension)
Rare but Serious Side Effects
- Angioedema (swelling of the face, lips, tongue, or throat)
- Worsening heart failure
- Kidney problems
- Hyperkalemia (high potassium levels)
- Allergic reactions
Long-Term Effects
- Long-term effects primarily relate to the underlying condition of hypertension, which the medication aims to control.
Adverse Drug Reactions (ADR)
- Angioedema, severe hypotension, hyperkalemia, and allergic reactions require immediate intervention.
Contraindications
- Severe bradycardia
- Second or third-degree heart block (unless a pacemaker is present)
- Cardiogenic shock
- Decompensated heart failure
- Sick sinus syndrome (unless a pacemaker is present)
- Severe hepatic impairment (Child-Pugh > B)
- Hypersensitivity to nebivolol or valsartan
- Co-administration with aliskiren in patients with diabetes
Drug Interactions
- CYP2D6 inhibitors (e.g., fluoxetine, paroxetine, quinidine) can increase nebivolol levels.
- Other antihypertensive medications may have additive effects and increase the risk of hypotension.
- Potassium-sparing diuretics or potassium supplements can increase the risk of hyperkalemia.
- NSAIDs may reduce the antihypertensive effect and increase the risk of renal impairment.
- Alcohol may increase the risk of hypotension.
Pregnancy and Breastfeeding
- Pregnancy Safety Category: D (contraindicated)
- Fetal Risks: Can cause fetal harm, including injury or death, especially during the second and third trimesters.
- Breastfeeding: Not recommended. It is unknown if nebivolol or valsartan pass into breast milk.
Drug Profile Summary
- Mechanism of Action: Beta-blocker (nebivolol) and angiotensin II receptor blocker (valsartan) combination for synergistic blood pressure reduction.
- Side Effects: Dizziness, headache, fatigue, bradycardia, hypotension.
- Contraindications: Severe bradycardia, heart block, heart failure, severe hepatic impairment, pregnancy.
- Drug Interactions: CYP2D6 inhibitors, other antihypertensives, potassium-sparing diuretics, NSAIDs.
- Pregnancy & Breastfeeding: Contraindicated in pregnancy, not recommended during breastfeeding.
- Dosage: 5 mg nebivolol/80 mg valsartan once daily.
- Monitoring Parameters: Blood pressure, heart rate, renal function, potassium levels (especially in susceptible individuals).
Popular Combinations
- Not typically combined with other antihypertensives in a single pill. However, it may be used in combination with other antihypertensive medications if blood pressure control is inadequate with nebivolol/valsartan alone. This may include thiazide diuretics, calcium channel blockers, or other agents.
Precautions
- General Precautions: Monitor blood pressure, heart rate, renal function, and potassium levels, especially in patients with comorbidities.
- Specific Populations:
- Pregnant Women: Contraindicated.
- Breastfeeding Mothers: Not recommended.
- Children & Elderly: Not recommended for children. Use with caution in elderly patients.
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for Nebivolol + Valsartan?
A: The standard recommended dosage is one tablet of 5 mg nebivolol/80 mg valsartan taken orally once daily.
Q2: Can Nebivolol + Valsartan be used in patients with diabetes?
A: It can be used with caution. Nebivolol may mask the symptoms of hypoglycemia. Closely monitor blood glucose levels. Co-administration with aliskiren is contraindicated in patients with diabetes.
Q3: What are the most common side effects?
A: Common side effects include dizziness, headache, fatigue, slow heart rate (bradycardia), and low blood pressure (hypotension).
Q4: Is Nebivolol + Valsartan safe during pregnancy?
A: No. It is contraindicated during pregnancy, especially during the second and third trimesters, due to the risk of fetal harm.
Q5: How does Nebivolol + Valsartan differ from taking nebivolol or valsartan alone?
A: The combination provides a synergistic effect in lowering blood pressure, achieving better control than either drug alone in some patients.
Q6: Can Nebivolol + Valsartan be crushed or chewed?
A: It is generally recommended to swallow the tablet whole. Consult the specific product labeling or a pharmacist for confirmation.
Q7: What should I do if I miss a dose?
A: Take the missed dose as soon as you remember. If it is almost time for your next dose, skip the missed dose and continue your regular dosing schedule. Do not double the dose.
Q8: Can I drink alcohol while taking Nebivolol + Valsartan?
A: Alcohol can further lower blood pressure and increase the risk of side effects. It is best to avoid or limit alcohol consumption.
Q9: Are there any specific dietary restrictions while taking this medication?
A: No specific dietary restrictions, but a healthy diet low in sodium is generally recommended for managing hypertension. Avoid potassium supplements or salt substitutes unless specifically advised by your doctor.
A: Seek immediate medical attention if you experience symptoms such as angioedema (swelling of face, lips, tongue, or throat), severe dizziness or lightheadedness, chest pain, or difficulty breathing.
