What are the advantages of Telmisartan (Angiotensin II Receptor Blocker) compared to other Angiotensin-Converting Enzyme inhibitors (ACE inhibitors)/Angiotensin II Receptor Blockers (ARBs)?

From the Guidelines

Telmisartan is a preferred choice over other Angiotensin-Converting Enzyme inhibitors (ACE inhibitors) and Angiotensin II Receptor Blockers (ARBs) due to its unique molecular structure, long half-life, and high lipophilicity, which enable better tissue penetration and potentially greater organ protection, as well as its excellent tolerability profile and demonstrated cardiovascular protection in high-risk patients 1. Key advantages of telmisartan include:

• Long half-life (24 hours), allowing for once-daily dosing and consistent 24-hour blood pressure control
• High lipophilicity, enabling better tissue penetration and potentially greater organ protection
• Partial PPARγ agonist activity, which may provide additional metabolic benefits like improved insulin sensitivity and lipid profile
• Excellent tolerability profile with fewer side effects like cough (compared to ACE inhibitors) or edema (compared to some other ARBs)
• Demonstrated cardiovascular protection in high-risk patients, even beyond blood pressure lowering effects Typical dosing is 20-80 mg once daily, with 40 mg being the most common starting dose. Telmisartan can be used alone or in combination with other antihypertensives like hydrochlorothiazide or amlodipine. When switching from another ACE inhibitor or ARB, it's generally safe to start telmisartan at the equivalent dose. However, monitor blood pressure closely during the transition, especially in elderly patients or those with renal impairment, as recommended by the 2017 ACC/AHA/HFSA focused update of the 2013 ACCF/AHA guideline for the management of heart failure 1. The unique molecular structure of telmisartan contributes to its long duration of action and tissue penetration, explaining its sustained efficacy and potential for organ protection beyond blood pressure control. It is also important to note that the combination of ACE inhibitors and ARBs should not be routinely used, as it may increase the risk of hyperkalemia and AKI without reducing benefit in any CKD subgroup, as shown in the ONTARGET and VA NEPHRON-D studies 1. In patients with heart failure with reduced ejection fraction (HFrEF), the use of ACE inhibitors or ARBs, including telmisartan, is recommended to reduce morbidity and mortality, as stated in the 2016 ACC/AHA/HFSA focused update on new pharmacological therapy for heart failure 1.

From the FDA Drug Label

Telmisartan tablets, USP are an angiotensin II receptor blocker (ARB) indicated for: Treatment of hypertension, to lower blood pressure. Lowering blood pressure reduces the risk of fatal and nonfatal cardiovascular events, primarily strokes and myocardial infarctions. ( 1.1) Cardiovascular (CV) risk reduction in patients unable to take ACE inhibitors ( 1.2)

The advantages of Telmisartan compared to other Angiotensin-Converting Enzyme inhibitors (ACE inhibitors)/Angiotensin II Receptor Blockers (ARBs) include:

• Cardiovascular risk reduction in patients unable to take ACE inhibitors 2
• Treatment of hypertension to lower blood pressure, reducing the risk of fatal and nonfatal cardiovascular events, primarily strokes and myocardial infarctions 2
• Telmisartan does not inhibit ACE (kininase II), and therefore does not affect the response to bradykinin 2 Key points about Telmisartan are:
• Angiotensin II receptor blocker (ARB)
• Indicated for hypertension and cardiovascular risk reduction
• Does not inhibit ACE However, the FDA label does not provide a direct comparison of the advantages of Telmisartan over other ACE inhibitors or ARBs.

From the Research

Advantages of Telmisartan

The advantages of Telmisartan, an Angiotensin II Receptor Blocker, compared to other Angiotensin-Converting Enzyme inhibitors (ACE inhibitors)/Angiotensin II Receptor Blockers (ARBs) include:

• Superior efficacy in controlling blood pressure, especially towards the end of the dosing interval, compared to other antihypertensive drugs such as losartan, valsartan, ramipril, atenolol, and perindopril 3, 4
• A longer half-life than other ARBs, resulting in higher and persistent antihypertensive activity 3
• A partial PPARγ-agonistic effect, which can help improve insulin resistance and metabolic syndrome components, without the safety concerns of full PPARγ agonists 3, 5
• Agonist activity on PPARα and PPARδ receptors, which can help modulate adipokine levels and improve metabolic syndrome components 3
• Better tolerability profile compared to ACE inhibitors, with a lower incidence of persistent, dry cough and angioedema 4, 6

Comparison to Other ARBs

Telmisartan has been shown to be superior to other ARBs in improving insulin resistance, reducing fasting blood glucose and insulin levels, and decreasing diastolic blood pressure 5

• A meta-analysis of 21 randomized controlled trials found that telmisartan was superior to other ARBs in improving homeostasis model assessment of insulin resistance and reducing fasting blood glucose and insulin levels 5

Cardiovascular Disease Prevention

Telmisartan has been shown to be effective in preventing cardiovascular events in patients at high cardiovascular risk, with a similar efficacy to ramipril, but with better tolerability 6, 7

• The ONTARGET trial found that telmisartan was non-inferior to ramipril in reducing the composite primary endpoint of cardiovascular mortality, non-fatal myocardial infarction, non-fatal stroke, and hospitalization for heart failure in patients at high cardiovascular risk 6, 7