Usage
- Amlodipine + Nebivolol is prescribed for the treatment of mild to moderate essential hypertension (high blood pressure). It is also indicated for chronic stable angina.
- Pharmacological classification: This is a combination drug containing a beta-blocker (Nebivolol) and a calcium channel blocker (Amlodipine).
- Mechanism of action: Nebivolol is a third-generation, cardioselective beta-1 receptor blocker. It decreases heart rate and myocardial contractility, thus reducing cardiac output and blood pressure. It also vasodilates blood vessels through nitric oxide release. Amlodipine is a dihydropyridine calcium channel blocker. It inhibits calcium ion influx into vascular smooth muscle and cardiac muscle, leading to vasodilation and reduced peripheral vascular resistance, which lowers blood pressure.
Alternate Names
- Nebilong-AM is a common alternate name. Other names exist depending on the manufacturer and region.
- Brand names: Numerous brand names exist internationally depending on the manufacturer and country.
How It Works
- Pharmacodynamics: Amlodipine causes vasodilation, reducing peripheral vascular resistance and lowering blood pressure. It also dilates coronary arteries, improving myocardial oxygen supply. Nebivolol lowers heart rate, decreases myocardial contractility, and causes vasodilation, reducing cardiac output and blood pressure.
- Pharmacokinetics: Both drugs are orally administered. Amlodipine is well absorbed, highly protein-bound, and extensively metabolized by the liver, with a half-life of about 30-50 hours. Nebivolol is rapidly absorbed and undergoes extensive hepatic metabolism, particularly by CYP2D6. However, dose adjustments are not required for poor metabolizers of CYP2D6. The elimination half-life of nebivolol is approximately 10 hours. Both drugs are primarily excreted in urine and feces.
- Mode of action: Amlodipine blocks L-type calcium channels in vascular smooth muscle and cardiac muscle, preventing calcium entry and leading to vasodilation. Nebivolol selectively blocks beta-1 adrenergic receptors in the heart, decreasing heart rate and contractility. It also promotes nitric oxide release, contributing to vasodilation.
Dosage
Standard Dosage
Adults:
- Initial dose: One tablet containing 5 mg amlodipine and 5 mg nebivolol once daily.
- Maximum dose: One tablet containing 5 mg amlodipine and 10 mg nebivolol or as directed by a physician once daily.
Children: Use in children and adolescents is not recommended due to the lack of clinical studies.
Special Cases:
- Elderly Patients: Initial dose is usually half a tablet (2.5 mg nebivolol/ 5mg amlodipine), which can be increased to the standard adult dose if needed.
- Patients with Renal Impairment: No dose adjustment is generally required in patients with mild to moderate renal impairment. For severe renal impairment, the starting dose should be lowered (2.5 mg nebivolol/ 5 mg amlodipine), with careful titration.
- Patients with Hepatic Dysfunction: For moderate hepatic impairment, the starting dose is typically halved, and titration should proceed with caution. The combination is not recommended for severe hepatic impairment.
- Patients with Comorbid Conditions: Caution is advised in patients with certain conditions like diabetes, heart failure, and peripheral vascular disease. Individualized dose adjustments may be necessary.
Clinical Use Cases There is no specific dosing for intubation, surgical procedures, mechanical ventilation, ICU use, or emergency situations.
Dosage Adjustments:
Dose adjustments may be necessary based on individual patient characteristics, including renal or hepatic impairment, other comorbid conditions, and response to therapy.
Side Effects
Common Side Effects:
Headache, dizziness, edema (especially of the ankles and feet), fatigue, nausea, flushing.
Rare but Serious Side Effects:
Bradycardia (slow heart rate), hypotension (low blood pressure), worsening heart failure, severe allergic reactions.
Long-Term Effects: May include worsening of pre-existing conditions like heart failure or peripheral vascular disease if not managed properly.
Contraindications
- Severe bradycardia, second or third-degree heart block (unless a pacemaker is present), cardiogenic shock, decompensated heart failure, severe hepatic impairment, sick sinus syndrome, severe hypotension, history of bronchospasm or bronchial asthma, untreated pheochromocytoma, hypersensitivity to amlodipine or nebivolol.
Drug Interactions
- Other antihypertensive medications (additive hypotensive effects).
- Beta-blockers and calcium channel blockers (increased risk of bradycardia and hypotension).
- CYP2D6 inhibitors (may increase nebivolol levels).
- CYP3A4 inhibitors (may increase amlodipine levels).
- Grapefruit juice (may increase amlodipine levels).
Pregnancy and Breastfeeding
- Pregnancy: Nebivolol is generally contraindicated during pregnancy due to potential risks to the fetus. Amlodipine’s safety during pregnancy hasn’t been fully established, and its use should be carefully considered.
- Breastfeeding: Both nebivolol and amlodipine can pass into breast milk. Breastfeeding is generally not recommended while taking this medication.
Drug Profile Summary
- Mechanism of Action: Nebivolol blocks beta-1 receptors and increases nitric oxide; amlodipine blocks calcium channels, both leading to vasodilation and lower blood pressure.
- Side Effects: Headache, dizziness, edema, fatigue, nausea. Serious effects include bradycardia, hypotension, and worsening heart failure.
- Contraindications: Severe bradycardia, heart block, heart failure, hepatic impairment, asthma, hypersensitivity.
- Drug Interactions: Other antihypertensives, beta-blockers, calcium channel blockers, CYP inhibitors, grapefruit juice.
- Pregnancy & Breastfeeding: Generally contraindicated.
- Dosage: Adults: 5mg/5mg once daily, max 5mg/10mg. Adjustments needed for elderly and those with hepatic or renal impairment.
- Monitoring Parameters: Blood pressure, heart rate, signs of edema, and symptoms of heart failure. Monitor serum glucose in diabetic patients.
Popular Combinations
Sometimes combined with other antihypertensives like valsartan or hydrochlorothiazide for enhanced blood pressure control in some patients.
Precautions
- Monitor for hypotension and bradycardia, especially at the start of treatment or with dose increases.
- Caution in patients with heart failure, hepatic or renal impairment, diabetes, or peripheral vascular disease.
- Avoid abrupt discontinuation.
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for Amlodipine + Nebivolol?
A: The standard initial adult dose is 5mg Amlodipine + 5 mg Nebivolol once daily.
Q2: Can this medication be used in children?
A: No, the safety and efficacy in children have not been established.
Q3: How should I take this medication?
A: Take it orally, once daily, with or without food.
Q4: What are the common side effects?
A: Common side effects include headache, dizziness, edema, fatigue, and nausea.
Q5: What should I do if I miss a dose?
A: Take the missed dose as soon as you remember, unless it’s almost time for your next dose. Do not double the dose.
Q6: Can I drink alcohol while taking this medication?
A: Alcohol can exacerbate the hypotensive effects, so consult your doctor before consuming alcohol.
Q7: Are there any drug interactions I should be aware of?
A: Yes, this combination can interact with other antihypertensives, certain heart medications, and some other drugs. Inform your physician about all the medications you are taking.
Q8: Can I stop taking this medication abruptly?
A: No, abrupt discontinuation can cause rebound hypertension and other adverse events. Consult your doctor for guidance on how to gradually discontinue the medication.
Q9: What should I do if I experience severe side effects?
A: If you experience severe or persistent side effects, such as severe dizziness, slow heart rate, difficulty breathing, or swelling, seek immediate medical attention.
