Usage
- Medical Conditions: This fixed-dose combination medication is primarily prescribed for the management of hypertension (high blood pressure) in patients whose blood pressure is not adequately controlled by monotherapy with either drug alone.
- Pharmacological Classification: Antihypertensive (a combination of a beta-blocker and an angiotensin II receptor blocker).
- Mechanism of Action: Nebivolol, a beta-1 receptor blocker, reduces heart rate and cardiac output, leading to a decrease in blood pressure. Telmisartan, an angiotensin II receptor blocker (ARB), blocks the action of angiotensin II, a hormone that causes vasoconstriction. By blocking angiotensin II, telmisartan causes vasodilation, lowering blood pressure.
Alternate Names
- No widely recognized alternate names exist for the combination itself. The individual components are sometimes referred to as nebivolol hydrochloride and telmisartan.
- Brand Names: Several brands are available, such as Nebi T, Telma NB, Nebilyst T, and Telmistrum Nebi 40-5 (depending on region).
How It Works
- Pharmacodynamics: Nebivolol decreases heart rate, myocardial contractility, and cardiac output. It also possesses vasodilatory properties, possibly through nitric oxide pathways. Telmisartan blocks the binding of angiotensin II to its receptor, preventing vasoconstriction and promoting vasodilation. The combination results in synergistic blood pressure reduction by addressing both cardiac output and peripheral vascular resistance.
- Pharmacokinetics: Nebivolol is absorbed orally with peak plasma concentrations reached in 1-4 hours. It is extensively metabolized by the liver, primarily by CYP2D6. Telmisartan is also absorbed orally, reaching peak plasma concentrations in 0.5-1.5 hours. It undergoes glucuronidation in the liver but is not extensively metabolized. Both drugs are primarily eliminated through biliary excretion.
- Mode of Action: Nebivolol acts on beta-1 adrenergic receptors in the heart, inhibiting the effects of sympathetic stimulation, leading to reduced heart rate and contractility. Telmisartan selectively blocks the AT1 subtype of angiotensin II receptors, preventing the vasoconstrictor and aldosterone-secreting effects of angiotensin II.
- Receptor Binding/Enzyme Inhibition: Nebivolol binds to beta-1 adrenergic receptors. Telmisartan binds to AT1 receptors. Neither drug significantly inhibits CYP enzymes, though nebivolol metabolism is influenced by CYP2D6 polymorphism.
- Elimination Pathways: Both drugs are primarily eliminated via biliary/fecal excretion with a minor component of renal excretion.
Dosage
Standard Dosage
Adults:
- Initial dose: One tablet containing Nebivolol 5 mg + Telmisartan 40/80 mg once daily.
- Dosage adjustment: Titration may be done at intervals of 2 weeks or more, based on blood pressure response, up to a maximum nebivolol dose of 40 mg.
Children:
- Not recommended for use in children under 18 years of age.
Special Cases:
- Elderly Patients: Initial dose of Nebivolol 2.5 mg + Telmisartan 40 mg is often recommended. Titrate cautiously. Close monitoring for hypotension and bradycardia is advised.
- Patients with Renal Impairment: For severe renal impairment (CrCl < 30 mL/min): Initial Nebivolol dose 2.5 mg + Telmisartan 40mg. Titrate slowly as needed. Not studied in patients undergoing dialysis.
- Patients with Hepatic Dysfunction: For moderate hepatic impairment, the initial nebivolol dose is 2.5 mg. Titrate slowly. Contraindicated in severe hepatic impairment.
- Patients with Comorbid Conditions: Caution should be exercised in patients with diabetes, chronic obstructive pulmonary disease (COPD), asthma, peripheral vascular disease, and heart failure. Close monitoring is necessary.
Clinical Use Cases
- The combination is not specifically indicated for intubation, surgical procedures, mechanical ventilation, ICU use, or emergency situations. Blood pressure management in these settings would typically involve other agents.
Dosage Adjustments
- Dose modifications are based on patient factors like renal/hepatic dysfunction, age, and response to therapy. Titration should be gradual, typically at intervals of 2 weeks or more.
Side Effects
Common Side Effects
- Dizziness
- Headache
- Fatigue
- Nausea
- Diarrhea
- Slow heart rate (bradycardia)
- Low blood pressure (hypotension)
Rare but Serious Side Effects
- Angioedema (swelling of face, lips, tongue, or throat)
- Worsening heart failure
- Severe allergic reactions
Long-Term Effects
- Long-term effects are primarily related to uncontrolled hypertension if the medication is not effective or adhered to.
Adverse Drug Reactions (ADR)
- Angioedema
- Severe hypotension
- Bradycardia
Contraindications
- Hypersensitivity to nebivolol or telmisartan
- Severe bradycardia
- Second- or third-degree heart block
- Cardiogenic shock
- Decompensated heart failure
- Severe hepatic impairment
Drug Interactions
- Other antihypertensive medications (additive hypotensive effects)
- Digoxin (increased risk of bradycardia)
- Rifampin (decreased nebivolol levels)
- CYP2D6 inhibitors (increased nebivolol levels)
- Potassium supplements or potassium-sparing diuretics (risk of hyperkalemia)
Pregnancy and Breastfeeding
- Pregnancy Safety Category: D (Telmisartan); C (Nebivolol)
- Fetal risks include renal and cardiovascular effects. Avoid use during pregnancy.
- Limited information is available on breastfeeding. The manufacturers recommend avoiding use while breastfeeding.
Drug Profile Summary
- Mechanism of Action: Nebivolol: Beta-1 blocker, reduces heart rate and cardiac output, vasodilatory. Telmisartan: Angiotensin II receptor blocker, vasodilatory.
- Side Effects: Dizziness, headache, fatigue, nausea, bradycardia, hypotension.
- Contraindications: Hypersensitivity, severe bradycardia, heart block, cardiogenic shock, decompensated heart failure, severe hepatic impairment.
- Drug Interactions: Other antihypertensives, digoxin, rifampin, CYP2D6 inhibitors, potassium supplements.
- Pregnancy & Breastfeeding: Contraindicated in pregnancy. Avoid use during breastfeeding.
- Dosage: Adult: Nebivolol 5 mg + Telmisartan 40/80 mg once daily. Titrate as needed. Elderly/Renal impairment: Start with lower Nebivolol dose (2.5 mg).
- Monitoring Parameters: Blood pressure, heart rate, potassium levels, renal function, signs of heart failure.
Popular Combinations
- This medication itself is a popular combination. Adding hydrochlorothiazide (a diuretic) may be considered if blood pressure control is inadequate.
Precautions
- General Precautions: Assess renal and hepatic function before starting therapy. Monitor blood pressure and heart rate regularly.
- Specific Populations: Avoid use during pregnancy and breastfeeding. Caution in elderly patients and those with renal impairment.
- Lifestyle Considerations: Advise patients on lifestyle modifications, including diet, exercise, and limiting alcohol intake.
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for Nebivolol + Telmisartan?
A: The standard starting dose is Nebivolol 5 mg + Telmisartan 40/80 mg once daily for adults. Elderly patients and those with renal impairment may start with a lower nebivolol dose (2.5 mg). Dosage adjustments are made at intervals of 2 weeks or more.
Q2: Can this combination be used in patients with diabetes?
A: Yes, but with caution. Monitor blood glucose levels closely, as nebivolol may mask symptoms of hypoglycemia.
Q3: What are the common side effects?
A: Common side effects include dizziness, headache, fatigue, nausea, bradycardia, and hypotension.
Q4: Are there any serious side effects I should be aware of?
A: Yes. Angioedema, worsening heart failure, and severe allergic reactions are rare but serious side effects that require immediate attention.
Q5: Can this medication be used during pregnancy or breastfeeding?
A: No, it’s contraindicated during pregnancy due to potential fetal harm. Avoid use during breastfeeding.
Q6: What if a patient misses a dose?
A: The patient should take the missed dose as soon as remembered, unless it is close to the time for the next dose. Do not double the dose.
Q7: What other medications should be avoided while taking this combination?
A: Avoid other antihypertensive medications unless prescribed by a physician due to the risk of additive hypotensive effects. Caution should be exercised with drugs like digoxin, rifampin, CYP2D6 inhibitors, and potassium supplements.
Q8: Can this medication be stopped abruptly?
A: No. Abrupt discontinuation of beta-blockers can lead to rebound hypertension or worsen angina. The dose should be tapered gradually under medical supervision.
Q9: How long does it take for this medication to become effective?
A: The maximum antihypertensive effect is usually observed within 2-4 weeks of starting therapy.
Q10: What should I monitor in patients taking this combination?
A: Monitor blood pressure, heart rate, potassium levels, renal function, and look for signs of heart failure, especially in at-risk patients.
