Usage
- Medical Conditions: This fixed-dose combination (FDC) medication is primarily prescribed for the management of hypertension (high blood pressure) in patients, especially those with associated coronary artery disease (CAD) or heart failure. It may also be used in patients inadequately controlled on dual therapy.
- Pharmacological Classification: This FDC comprises two drug classes:
- Metoprolol: Beta-adrenergic blocker (specifically, a cardioselective beta-1 blocker).
- Telmisartan: Angiotensin II receptor blocker (ARB).
- Mechanism of Action: This combination works by two distinct mechanisms:
- Metoprolol blocks the effects of adrenaline on the heart, reducing heart rate and the force of contractions, thereby lowering blood pressure. Its cardioselectivity helps minimize effects on the lungs.
- Telmisartan blocks the action of angiotensin II, a hormone that narrows blood vessels. This vasodilation helps lower blood pressure and reduce the workload on the heart.
Alternate Names
- While the generic name “Metoprolol Succinate + Telmisartan” is widely recognized, there is no universally accepted alternate generic name. Variations may exist based on the manufacturer.
- Brand Names: This combination is marketed under various brand names, including Xstan-Beta (25mg/40mg and 50mg/40mg), depending on the region.
How It Works
- Pharmacodynamics: Metoprolol decreases heart rate, cardiac output, and myocardial oxygen demand. Telmisartan lowers blood pressure by blocking the vasoconstrictor and aldosterone-secreting effects of angiotensin II.
- Pharmacokinetics:
- Absorption: Both drugs are orally absorbed. Metoprolol succinate is an extended-release formulation, providing gradual release for once-daily dosing. Telmisartan is also well-absorbed, though food may slightly delay its absorption without affecting overall bioavailability.
- Metabolism: Metoprolol is primarily metabolized by the liver, specifically CYP2D6 enzymes. Telmisartan undergoes minimal hepatic metabolism, primarily via glucuronidation. This makes it less susceptible to drug interactions involving CYP enzymes.
- Elimination: Metoprolol is primarily excreted in the urine, while telmisartan is eliminated primarily in feces via biliary excretion, with a small amount in the urine.
- Mode of Action: Metoprolol acts by selectively binding to beta-1 adrenergic receptors in the heart, inhibiting the effects of catecholamines. Telmisartan selectively binds to the angiotensin II type 1 (AT1) receptor, blocking the effects of angiotensin II.
Dosage
Standard Dosage
Adults:
- The starting dose is typically one tablet of Telmisartan 40mg/Metoprolol Succinate 25mg once daily. This can be increased to Telmisartan 40mg/Metoprolol Succinate 50mg once daily after 2-4 weeks if blood pressure remains uncontrolled. The maximum recommended dose for Metoprolol Succinate is 200mg. For Telmisartan, doses above 80mg haven’t demonstrated additional benefit.
Children:
- The combination is not typically recommended for children.
Special Cases:
- Elderly Patients: Start with a low dose and titrate cautiously. Closely monitor renal function.
- Patients with Renal Impairment: Dosage adjustments of metoprolol succinate may be necessary in patients with severe renal impairment (creatinine clearance < 30 mL/min). No dosage adjustment for telmisartan is typically needed unless severe renal disease is present.
- Patients with Hepatic Dysfunction: Use with caution in mild to moderate hepatic impairment and avoid in severe hepatic impairment for Metoprolol. Telmisartan can generally be used without adjustment in mild to moderate hepatic impairment but is contraindicated in severe hepatic impairment.
- Patients with Comorbid Conditions: Dosage adjustments may be needed based on coexisting conditions such as diabetes, heart failure, or other cardiovascular diseases.
Clinical Use Cases
The use of this specific FDC in clinical settings like intubation, surgical procedures, mechanical ventilation, ICU use, or emergency situations is not standard practice. Metoprolol tartrate (IV formulation) may be used in acute settings such as myocardial infarction.
Dosage Adjustments
Dosage adjustments are made based on individual patient response and tolerability, renal function, hepatic function, and drug interactions.
Side Effects
Common Side Effects
- Dizziness, lightheadedness
- Fatigue
- Headache
- Nausea
- Slowed heart rate (bradycardia)
Rare but Serious Side Effects
- Worsening heart failure
- Severe allergic reactions (angioedema, anaphylaxis)
- Liver dysfunction
- Kidney problems
Long-Term Effects
- Potential for worsening pre-existing heart block
Adverse Drug Reactions (ADR)
- Severe hypotension
- Bronchospasm (in susceptible individuals)
Contraindications
- Hypersensitivity to either drug
- Second or third-degree heart block (without a pacemaker)
- Severe bradycardia
- Cardiogenic shock
- Decompensated heart failure
- Sick sinus syndrome (unless a permanent pacemaker is in place)
- Severe hepatic impairment or biliary obstructive disorders
- Pregnancy and breastfeeding
- Concomitant use of telmisartan with aliskiren in patients with diabetes or renal impairment
Drug Interactions
- Other blood pressure lowering medications
- Calcium channel blockers (especially verapamil and diltiazem)
- Digoxin
- Insulin or oral hypoglycemic agents
- Rifampin
- CYP2D6 inhibitors (fluoxetine, paroxetine)
- Alcohol
Pregnancy and Breastfeeding
- Pregnancy Safety Category: D (Metoprolol), D (Telmisartan)
- Contraindicated during pregnancy due to potential for fetal harm.
- Not recommended during breastfeeding.
Drug Profile Summary
- Mechanism of Action: Metoprolol: Beta-1 adrenergic blocker; Telmisartan: Angiotensin II receptor blocker.
- Side Effects: Dizziness, fatigue, headache, nausea, bradycardia.
- Contraindications: Hypersensitivity, heart block, severe bradycardia, decompensated heart failure, pregnancy.
- Drug Interactions: Other antihypertensives, digoxin, CYP2D6 inhibitors.
- Pregnancy & Breastfeeding: Contraindicated.
- Dosage: Start with Telmisartan 40mg/Metoprolol 25mg once daily; may increase to 50mg of Metoprolol if needed.
- Monitoring Parameters: Blood pressure, heart rate, renal function, electrolytes.
Popular Combinations
While this FDC contains Metoprolol + Telmisartan, other combinations may be used concurrently, such as the addition of hydrochlorothiazide (a diuretic) for patients who don’t achieve adequate blood pressure control. However, this is determined by the physician based on patient needs.
Precautions
- General Precautions: Monitor blood pressure and heart rate regularly. Assess renal and hepatic function.
- Specific Populations: Use with caution in elderly patients, those with renal/hepatic impairment, and patients with diabetes.
- Lifestyle Considerations: Encourage lifestyle modifications such as diet, exercise, and smoking cessation.
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for Metoprolol Succinate + Telmisartan?
A: The usual starting dose is one tablet of Telmisartan 40mg/Metoprolol Succinate 25mg once daily. This can be increased to Telmisartan 40mg/Metoprolol Succinate 50mg after 2-4 weeks if blood pressure goals are not met.
Q2: How should I take Metoprolol Succinate + Telmisartan?
A: Take one tablet once daily, preferably at the same time each day, with or without food. Swallow the tablet whole with water; do not crush or chew.
Q3: What are the common side effects?
A: Common side effects include dizziness, fatigue, headache, nausea, and slowed heart rate.
Q4: What are the serious side effects I should watch for?
A: Watch for signs of worsening heart failure, allergic reactions (swelling of face, lips, or tongue), liver problems (yellowing of skin or eyes), or kidney problems (changes in urination). Seek immediate medical attention if these occur.
Q5: Can I take this medication if I am pregnant or breastfeeding?
A: No, this medication is contraindicated during pregnancy and breastfeeding.
Q6: What should I do if I miss a dose?
A: If you miss a dose, take it as soon as you remember, unless it is almost time for your next dose. Do not double up on doses.
Q7: Does this medication interact with other drugs?
A: Yes, it can interact with other medications, including other blood pressure medications, calcium channel blockers, digoxin, and some antidepressants. Inform your doctor about all other medications you are taking.
Q8: What are the contraindications for this medication?
A: This medication is contraindicated in patients with hypersensitivity to either drug, severe bradycardia, second or third-degree heart block, cardiogenic shock, decompensated heart failure, severe liver impairment and biliary obstructive disorders, and concomitant use with aliskiren in certain patient populations. It is also contraindicated during pregnancy and breastfeeding.
Q9: What are the long-term effects of this medication?
A: Prolonged use might worsen pre-existing heart block. Regular monitoring of cardiac function is recommended.
Q10: How does this combination differ from taking Metoprolol and Telmisartan individually?
A: The FDC provides convenience of a single tablet. Individual components allow for dose titration of each medicine separately, which may be required for some patients.
