From the Guidelines
The best angiotensin receptor blocker (ARB) with the longest half-life is telmisartan, with a half-life of approximately 24 hours, allowing for once-daily dosing. According to the 2017 ACC/AHA/AAPA/ABC/ACPM/AGS/APhA/ASH/ASPC/NMA/PCNA guideline for the prevention, detection, evaluation, and management of high blood pressure in adults 1, telmisartan has a daily frequency of 1, indicating its suitability for once-daily administration. The usual dose range for telmisartan is 20-80 mg/d, and it is essential to note that it should be avoided in pregnancy.
Some key points to consider when prescribing telmisartan include:
- It is an ARB, which works by blocking the action of angiotensin II, a potent vasoconstrictor, thereby reducing blood pressure and decreasing the risk of cardiovascular events.
- Telmisartan has been shown to be effective in reducing the risk of cardiovascular morbidity and mortality in patients with hypertension, as demonstrated in various clinical trials, including the ONTARGET study 1.
- The half-life of telmisartan allows for once-daily dosing, which can improve patient compliance and adherence to treatment.
- As with all ARBs, telmisartan should not be used in combination with ACE inhibitors or direct renin inhibitors, and caution should be exercised in patients with severe bilateral renal artery stenosis or those with a history of angioedema.
In terms of comparison with other ARBs, the ESC guidelines for the diagnosis and treatment of acute and chronic heart failure 2012 1 highlight the benefits of ARBs, such as valsartan and candesartan, in reducing the risk of heart failure hospitalization and improving symptoms and quality of life. However, telmisartan's longer half-life and once-daily dosing regimen make it a more convenient option for patients.
Overall, telmisartan is a suitable choice for patients requiring an ARB, due to its long half-life, once-daily dosing, and efficacy in reducing cardiovascular risk.
From the Research
Angiotensin Receptor Blockers (ARBs) with the Longest Half-Life
- Telmisartan has been identified as the ARB with the longest plasma half-life, highest lipophilicity, highest receptor binding affinity, and slowest dissociation of any ARB, making it suitable for sustained 24-hour blood pressure control 2, 3, 4.
- Studies have shown that telmisartan provides 24-hour blood pressure control superior to that of other ARBs, such as losartan and valsartan, as well as other antihypertensive agents like amlodipine and ramipril 2, 4, 5.
- The long half-life of telmisartan offers more sustained blood pressure control, especially at the end of the dosing period, and provides sustained efficacy in poorly compliant patients in the event of a missed dose, with statistical superiority compared to valsartan 5.
Comparison with Other ARBs
- Telmisartan has a unique profile among ARBs, with a high affinity for the angiotensin II type 1 receptor, a long duration of receptor binding, a high lipophilicity, and a long plasma half-life, which distinguishes it from other members of the ARB class 3, 4.
- The ONgoing Telmisartan Alone and in combination with Ramipril Global Endpoint Trial (ONTARGET) study demonstrated that telmisartan has similar cardiovascular protective effects to ramipril in a large, high-risk patient population, but was better tolerated 3, 4.
Clinical Implications
- Telmisartan may be a preferred option for patients with hypertension due to its powerful and sustained blood pressure control, cardiovascular protection, and tolerability 4.
- The use of telmisartan in combination with other antihypertensive agents, such as amlodipine, may provide effective blood pressure control while minimizing side effects and reducing exposure to high doses of individual medications 6.