Telmisartan is a long-acting angiotensin II receptor blocker (ARB) used to treat hypertension and to reduce the risk of cardiovascular events in patients at high cardiovascular risk who cannot tolerate ACE inhibitors. By selectively blocking the angiotensin II type 1 (AT1) receptor, it produces vasodilation and lowers blood pressure without the cough commonly seen with ACE inhibitors. It has one of the longest half-lives in its class, which supports sustained 24-hour blood pressure control with once-daily dosing.
Treatment of essential hypertension (alone or in combination with other antihypertensives)4
Reduction of cardiovascular morbidity and mortality in patients at high cardiovascular risk who are intolerant of ACE inhibitors2,1
Sustained 24-hour blood pressure control with once-daily dosing due to a long half-life4
Renal and cardiovascular protection in conditions associated with renin-angiotensin system activation1,2
What to watch for
Dizziness or lightheadedness
Hypotension, including orthostatic hypotension (more likely in volume-depleted patients)
Hyperkalemia (elevated blood potassium), increased risk with potassium supplements or potassium-sparing diuretics
Known hypersensitivity to telmisartan or any component of the formulation1,2
Pregnancy (drugs acting on the renin-angiotensin system can cause fetal injury and death; discontinue as soon as pregnancy is detected)3
The bottom line
Evidence rating strong. Most-documented uses: treatment of essential hypertension (alone or in combination with other antihypertensives), reduction of cardiovascular morbidity and mortality in patients at high cardiovascular risk who are intolerant of ace inhibitors, sustained 24-hour blood pressure control with once-daily dosing due to a long half-life. 4 sources indexed (2001–2014), with 5 interaction records on file.
The science
How it works, mechanistically.
Core mechanism
Telmisartan selectively and competitively blocks the binding of angiotensin II to the angiotensin II type 1 (AT1) receptor in vascular smooth muscle, the adrenal cortex, and other tissues. Angiotensin II is the principal vasoactive effector of the renin-angiotensin-aldosterone system, and its actions at the AT1 receptor cause vasoconstriction, aldosterone release, sodium and water retention, sympathetic activation, and vascular and cardiac remodeling. By antagonizing this receptor, telmisartan promotes vasodilation, reduces aldosterone-driven sodium retention, and lowers systemic vascular resistance and blood pressure. Because it acts downstream of angiotensin II generation, its effect is independent of the enzymatic pathway used to form angiotensin II and it does not inhibit the breakdown of bradykinin, which explains the lower incidence of cough compared with ACE inhibitors. Reduced aldosterone activity decreases renal potassium excretion, which is the basis for its risk of hyperkalemia, particularly when combined with potassium supplements, potassium-sparing diuretics, or in renal impairment. Telmisartan is also a partial agonist of the peroxisome proliferator-activated receptor gamma (PPAR-gamma), a property that may contribute modest favorable metabolic effects, though this is not the basis of its approved use.2,1
Class
Angiotensin II receptor blocker (ARB)
Dosing
Dosing & protocol.
Common range
Hypertension: typically 40 mg orally once daily (range 20 mg to 80 mg once daily); start lower (20 mg or 40 mg) and titrate. Cardiovascular risk reduction: 80 mg orally once daily.
Recommended form
Oral tablet (20 mg, 40 mg, 80 mg); also available in fixed-dose combinations with hydrochlorothiazide or amlodipine
Can be taken with or without food; food slightly reduces the area under the curve but the effect is not clinically significant. Bioavailability is dose-dependent (roughly 42 to 58 percent). Take at the same time each day for consistent 24-hour blood pressure control. Do not remove a tablet from its blister until immediately before dosing because the tablets are hygroscopic.3
Safety
Full safety detail.
Side effects
Dizziness or lightheadedness
Hypotension, including orthostatic hypotension (more likely in volume-depleted patients)
Hyperkalemia (elevated blood potassium), increased risk with potassium supplements or potassium-sparing diuretics
Increased blood urea nitrogen and serum creatinine, especially in renal artery stenosis or volume depletion
Upper respiratory tract symptoms and sinus congestion
Magnesium Glycinate may add to the blood-pressure-lowering effect of Telmisartan.
Recommendation: Monitor blood pressure and dizziness, especially during dose changes; stop the supplement and seek advice if syncope, falls, or symptomatic hypotension occurs.
L-Citrulline may add to the blood-pressure-lowering effect of Telmisartan.
Recommendation: Monitor blood pressure and dizziness, especially during dose changes; stop the supplement and seek advice if syncope, falls, or symptomatic hypotension occurs.
Telmisartan, an angiotensin II receptor blocker, reduces aldosterone secretion and thereby decreases urinary potassium excretion. Co-administration with potassium supplements (or potassium-containing salt substitutes) can produce additive increases in serum potassium, with a real risk of clinically significant hyperkalemia, particularly in patients with chronic kidney disease, diabetes, heart failure, or the elderly.
Recommendation: Avoid routine potassium supplementation and potassium-based salt substitutes unless specifically directed and monitored by a clinician. If potassium must be used, check baseline serum potassium and renal function, then recheck within 1 to 2 weeks of starting or changing either agent. Report muscle weakness, palpitations, or irregular heartbeat promptly.
Garlic extract has modest blood-pressure-lowering and vasodilatory effects. When combined with telmisartan, the antihypertensive effects can be additive, potentially producing excessive blood pressure reduction, dizziness, or symptomatic hypotension, especially at higher garlic doses or when telmisartan therapy is being titrated.
Recommendation: If using garlic extract supplements alongside telmisartan, monitor blood pressure at home and watch for lightheadedness or fainting, particularly on standing. Tell your clinician so antihypertensive dosing can be adjusted if needed. Stop garlic supplements before surgery given additive effects and a theoretical bleeding risk.
Numbered references. Citations throughout the page link here.
Randomized controlled trials
2
1Telmisartan, Ramipril, or Both in Patients at High Risk for Vascular Events (ONTARGET)Needs reviewNo linkYusuf S, Teo KK, Pogue J, et al. (ONTARGET Investigators) · New England Journal of Medicine · 2008
In patients with vascular disease or high-risk diabetes, telmisartan was noninferior to ramipril for the composite of cardiovascular death, myocardial infarction, stroke, or hospitalization for heart failure, with less cough and angioedema; combining the two agents increased adverse events such as hyperkalemia and renal dysfunction without additional benefit.
2Effects of the Angiotensin-Receptor Blocker Telmisartan on Cardiovascular Events in High-Risk Patients Intolerant to ACE Inhibitors (TRANSCEND)Needs reviewNo linkTelmisartan Randomised AssessmeNt Study in ACE iNtolerant subjects with cardiovascular Disease (TRANSCEND) Investigators · Lancet · 2008
In ACE-inhibitor-intolerant patients, telmisartan modestly reduced a composite of cardiovascular death, myocardial infarction, and stroke compared with placebo and was well tolerated.
Reviews & position papers
2
3Drug-induced hyperkalemiaNeeds reviewNo linkBen Salem C, Badreddine A, Fathallah N, et al. · Drug Safety · 2014
Agents that suppress the renin-angiotensin-aldosterone system, including angiotensin receptor blockers, reduce renal potassium excretion and can cause clinically significant hyperkalemia, with risk amplified by concurrent potassium supplementation, potassium-sparing diuretics, NSAIDs, and impaired kidney function.
4Telmisartan: a review of its pharmacological properties and therapeutic use in the management of hypertensionNeeds reviewNo linkSharpe M, Jarvis B, Goa KL · Drugs · 2001
Telmisartan's long terminal half-life of about 24 hours supports effective and sustained reduction of systolic and diastolic blood pressure across the full dosing interval, including the early morning period, with once-daily administration.
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