Usage
- Bisoprolol + Telmisartan is prescribed for the treatment of hypertension (high blood pressure). It is also used to reduce cardiovascular risk in patients who are unable to take ACE inhibitors and in patients with stable chronic heart failure with reduced systolic left ventricular function.
- Pharmacological classification: This combination drug includes two classifications:
- Bisoprolol: Beta-blocker (specifically, a cardioselective beta-1 adrenergic receptor blocker)
- Telmisartan: Angiotensin II receptor blocker (ARB)
- Mechanism of action: Bisoprolol works by blocking the action of certain natural substances, such as adrenaline, on the beta-1 receptors in the heart. This slows the heart rate and reduces the force of contraction, ultimately lowering blood pressure. Telmisartan blocks the effects of angiotensin II, a hormone that constricts blood vessels. This causes the blood vessels to relax, lowering blood pressure and improving blood flow.
Alternate Names
- This fixed-dose combination (FDC) is often referred to simply as the bisoprolol-telmisartan combination.
- Brand names: Telmistrum Biso 40-2.5
How It Works
- Pharmacodynamics: Bisoprolol reduces heart rate, myocardial contractility, and cardiac output, resulting in a decrease in blood pressure. Telmisartan blocks the binding of angiotensin II to its receptor, leading to vasodilation and reduced blood pressure.
- Pharmacokinetics:
- Bisoprolol: Well absorbed orally. Peak plasma concentration is reached in 2-4 hours. Metabolized in the liver, primarily by CYP2D6, and excreted via both renal and hepatic routes.
- Telmisartan: Incompletely absorbed orally, but has high bioavailability due to extensive enterohepatic recirculation. Peak plasma concentration in 0.5-1.5 hours. Excreted primarily in feces via biliary excretion.
- Mode of action: Bisoprolol competitively binds to beta-1 adrenergic receptors in the heart, inhibiting the sympathetic nervous system’s effects on the heart. Telmisartan selectively blocks the angiotensin II type 1 (AT1) receptor, preventing angiotensin II-mediated vasoconstriction and aldosterone release.
- Receptor binding/Enzyme inhibition: Bisoprolol binds to beta-1 receptors. Telmisartan blocks AT1 receptors.
- Elimination pathways: Bisoprolol undergoes hepatic metabolism and is excreted renally and in bile. Telmisartan is excreted primarily in feces via biliary excretion.
Dosage
Standard Dosage
Adults:
- Hypertension: Initial dose is typically Bisoprolol 2.5 mg + Telmisartan 40 mg once daily, taken in the morning with or without food. The dose may be increased up to a maximum of Bisoprolol 20mg + Telmisartan 80 mg daily based on blood pressure response.
- Heart Failure: Initial dose is Bisoprolol 1.25 mg once daily. This can be titrated up gradually, as tolerated, to a maximum of 10 mg once daily.
Children:
- The safety and efficacy of Bisoprolol + Telmisartan have not been established in children under 18 years of age. Its use is not recommended in this population.
Special Cases:
- Elderly Patients: Start with the lowest dose and titrate slowly, monitoring closely.
- Patients with Renal Impairment: For severe renal impairment (creatinine clearance <20 mL/min), the maximum dose of Bisoprolol should not exceed 10 mg once daily. No dosage adjustment is typically necessary for Telmisartan, but close monitoring is advised.
- Patients with Hepatic Dysfunction: For severe liver impairment, the maximum dose of Bisoprolol should not exceed 10 mg once daily. Telmisartan dose should be reduced in severe hepatic impairment.
- Patients with Comorbid Conditions: Use with caution in patients with diabetes, asthma, or chronic obstructive pulmonary disease (COPD), as bisoprolol can mask symptoms of hypoglycemia and exacerbate respiratory issues.
Clinical Use Cases
- The specific dosages for clinical use cases like intubation, surgical procedures, mechanical ventilation, ICU use, or emergency situations are not directly related to Bisoprolol + Telmisartan’s primary indication of hypertension management. Dosage adjustments in these settings would be based on the individual patient’s condition and any concomitant medications.
Dosage Adjustments
- Dosage adjustments are based on blood pressure response, tolerability, and renal/hepatic function. Slow titration is crucial, especially in patients with renal or hepatic impairment.
Side Effects
Common Side Effects
- Dizziness, lightheadedness, fatigue, tiredness, nausea, slow heart rate (bradycardia), headache, back pain, diarrhea, congestion, and swollen ankles.
Rare but Serious Side Effects
- Shortness of breath or wheezing, severe hypotension (low blood pressure), kidney problems, signs of a serious allergic reaction (e.g., difficulty breathing, swelling of the face, hives).
Long-Term Effects
- May include worsening of pre-existing kidney or heart conditions if not adequately monitored and managed.
Adverse Drug Reactions (ADR)
- Angioedema, severe hypotension, bronchospasm (especially in patients with asthma or COPD).
Contraindications
- Hypersensitivity to bisoprolol, telmisartan, or any component of the formulation.
- Severe bradycardia, second or third-degree heart block (without a pacemaker), sick sinus syndrome, severe hypotension, cardiogenic shock, severe asthma or COPD, severe peripheral arterial occlusive disease, metabolic acidosis, untreated phaeochromocytoma.
Drug Interactions
- Other antihypertensive medications (e.g., aliskiren, amiloride, enalapril, diltiazem), asthma medications (theophylline, aminophylline), potassium-rich supplements, NSAIDs (ibuprofen), certain antidepressants, digoxin, rifampin, medications for irregular heartbeat (e.g. amiodarone, verapamil), diabetes medications (e.g. insulin).
- Grapefruit and protein-rich foods may interact with this combination.
- Pre-existing conditions like diabetes, asthma, coronary heart disease, low blood pressure, and liver/kidney disease require careful consideration when prescribing this combination.
Pregnancy and Breastfeeding
- Pregnancy Safety Category: D (Bisoprolol) and D (Telmisartan).
- This medication is generally not recommended during pregnancy, especially in the second and third trimesters. It can affect fetal development, cause fetal growth restriction, and potentially harm the unborn baby.
- Bisoprolol may pass into breast milk. While breastfeeding may be possible, it’s essential to consult with a doctor to weigh the benefits and risks. Alternatives might be considered. Close monitoring of the infant for potential side effects is crucial if breastfeeding continues.
Drug Profile Summary
- Mechanism of Action: Bisoprolol blocks beta-1 receptors reducing heart rate and blood pressure, while telmisartan blocks AT1 receptors promoting vasodilation.
- Side Effects: Dizziness, fatigue, slow heart rate, hypotension, headache. Serious side effects include shortness of breath, severe hypotension, kidney problems, and allergic reactions.
- Contraindications: Severe bradycardia, heart block, hypotension, cardiogenic shock, severe asthma/COPD, severe peripheral arterial disease, untreated phaeochromocytoma.
- Drug Interactions: Other antihypertensives, asthma medications, potassium supplements, NSAIDs, digoxin, rifampin.
- Pregnancy & Breastfeeding: Not recommended during pregnancy. Consult a physician before using during breastfeeding.
- Dosage: Initial: Bisoprolol 2.5mg + Telmisartan 40mg once daily, titrated up as needed. Max: Bisoprolol 20mg + Telmisartan 80mg.
- Monitoring Parameters: Blood pressure, heart rate, kidney function tests, liver function tests, electrolytes (especially potassium), signs of heart failure exacerbation, blood glucose levels in diabetics.
Popular Combinations
- Bisoprolol + Telmisartan is itself a popular combination. Sometimes, hydrochlorothiazide (a diuretic) is added to this combination for enhanced blood pressure control.
Precautions
- Pre-screening for allergies, pre-existing medical conditions like diabetes, asthma, COPD, kidney or liver problems is necessary.
- Close monitoring during pregnancy and breastfeeding is important if use is deemed absolutely necessary.
- Start with the lowest dose in children and elderly patients. Monitor for adverse effects.
- Advise patients about potential side effects affecting driving and operating machinery.
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for Bisoprolol + Telmisartan?
A: The initial dose is typically Bisoprolol 2.5mg + Telmisartan 40mg once daily. This can be increased to a maximum of Bisoprolol 20mg + Telmisartan 80mg daily based on blood pressure response and tolerability.
Q2: What are the common side effects of Bisoprolol + Telmisartan?
A: Common side effects include dizziness, fatigue, headache, slow heart rate, and gastrointestinal upset.
Q3: Is Bisoprolol + Telmisartan safe during pregnancy?
A: No. It’s generally contraindicated, especially during the second and third trimesters. It carries a risk of fetal harm.
Q4: How does Bisoprolol + Telmisartan affect patients with diabetes?
A: Bisoprolol may mask symptoms of hypoglycemia, making it more difficult to recognize. Careful blood glucose monitoring is crucial in diabetic patients taking this medication.
Q5: Can Bisoprolol + Telmisartan be used in patients with renal impairment?
A: It can be used, but with caution and potential dose adjustment, especially in severe renal impairment (creatinine clearance <20 mL/min), where the maximum bisoprolol dose should not exceed 10mg.
Q6: What are the major drug interactions with Bisoprolol + Telmisartan?
A: Significant interactions can occur with other antihypertensives, certain calcium channel blockers (e.g., verapamil, diltiazem), digoxin, rifampin, and some antidepressants.
Q7: When should I avoid prescribing Bisoprolol + Telmisartan?
A: Avoid in patients with severe bradycardia, second or third degree heart block, sick sinus syndrome, severe hypotension, cardiogenic shock, uncontrolled heart failure, severe asthma/COPD.
Q8: How should treatment with Bisoprolol + Telmisartan be discontinued?
A: Treatment should not be stopped abruptly. The dosage should be reduced gradually to prevent rebound hypertension or worsening of heart failure.
Q9: What are the key monitoring parameters for patients on Bisoprolol + Telmisartan?
A: Monitor blood pressure, heart rate, renal function, liver function, electrolytes (potassium), and signs of heart failure exacerbation. In diabetic patients, close blood glucose monitoring is crucial.
