Telmisartan: Difference between revisions

{{Short description|Angiotensin II receptor antagonist}}

{{Drugbox

| alt =  

<!-- Clinical data -->

| pronounce  = {{IPAc-en|t|ɛ|l|m|ɪ|ˈ|s|ɑr|t|ən}}

| ATC_suffix = CA07

| legal_AU = S4

| legal_CA          = Rx-only

| legal_EU = RX-only

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| bioavailability = 42–100%

| excretion = Feces 97%

<!-- Identifiers -->

| CAS_number_Ref = {{cascite|correct|??}}

| ChEMBL = 1017

<!-- Chemical data -->

| IUPAC_name = 2-(4-<nowiki/>{[4-Methyl-6-(1-methyl-1''H''-1,3-benzodiazol-2-yl)-2-propyl-1''H''-1,3-benzodiazol-1-yl]methyl}phenyl)benzoic acid

}}

<!-- Definition and medical uses -->

'''Telmisartan''', sold under the brand name '''Micardis''' among others, is a [[medication]] used to treat [[hypertension|high blood pressure]], [[heart failure]], and [[diabetic kidney disease]]. It is a reasonable initial treatment for high blood pressure. It is taken by mouth.  Versions are available as the combination [[telmisartan/hydrochlorothiazide]], telmisartan/cilnidipine and telmisartan/[[amlodipine]].

<!-- Side effects and mechanisms -->

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Telmisartan was patented in 1991 and came into medical use in 1999. It is available as a [[generic medication]]. In 2021, it was the 217th most commonly prescribed medication in the United States, with more than 1{{nbsp}}million prescriptions.

Telmisartan is contraindicated during [[pregnancy]]. Like other drugs affecting the [[renin–angiotensin system]] (RAS), telmisartan can cause [[birth defect]]s, [[stillbirth]]s, and [[neonatal death]]s. It is not known whether the drug passes into the breast milk. Also it is contraindicated in bilateral [[renal artery stenosis]] in which it can cause [[kidney failure]].

Side effects are similar to other angiotensin II receptor antagonists and    include [[tachycardia]] and [[bradycardia]] (fast or slow heartbeat), [[hypotension]] (low blood pressure) and [[edema]] (swelling of arms, legs, lips, tongue, or throat, the latter leading to breathing problems). [[Allergic reaction]]s may also occur.

Due to its mechanism of action, telmisartan increases blood [[potassium]] levels. Combination with potassium preparations or [[potassium-sparing diuretic]]s could cause [[hyperkalaemia]] (excessive potassium levels). Combination with [[NSAIDs]], especially in patients with impaired kidney function, has a risk of causing (usually reversible) [[kidney failure]].

Telmisartan is an angiotensin II receptor blocker that shows high affinity for the [[angiotensin II receptor type 1]] (AT₁), with a binding affinity 3000 times greater for AT₁ than [[Angiotensin II receptor type 2|AT₂]].

Telmisartan's activity at the [[peroxisome proliferator-activated receptor delta]] (PPAR-δ) receptor has prompted speculation around its potential as a sport doping agent as an alternative to [[GW 501516]]. Telmisartan activates PPAR-δ receptors in several tissues.

Also, telmisartan has a [[PPAR agonist|PPAR-γ agonist]] activity.

The substance is quickly but to varying degrees absorbed from the gut. The average [[bioavailability]] is about 50% (42–100%). Food intake has no clinically relevant influence on the kinetics of telmisartan. [[Plasma protein binding]] is over 99.5%, mainly to [[albumin]] and [[alpha-1-acid glycoprotein]]. It has the longest half-life of any [[angiotensin II receptor blocker]] (ARB) (24 hours) and the largest [[volume of distribution]] among ARBs (500 liters). Less than 3% of telmisartan is inactivated by [[glucuronidation]] in the liver, and over 97% is eliminated in unchanged form via [[bile]] and faeces.

{{see also|Discovery and development of angiotensin receptor blockers}}

* {{cite journal | vauthors = Yusuf S, Teo KK, Pogue J, Dyal L, Copland I, Schumacher H, Dagenais G, Sleight P, Anderson C | display-authors = 6 | title = Telmisartan, ramipril, or both in patients at high risk for vascular events | journal = The New England Journal of Medicine | volume = 358 | issue = 15 | pages = 1547–59 | date = April 2008 | pmid = 18378520 | doi = 10.1056/nejmoa0801317 | publisher = Massachusetts Medical Society | hdl = 2437/81925 | hdl-access = free }}

* {{cite journal | vauthors = Yusuf S, Teo K, Anderson C, Pogue J, Dyal L, Copland I, Schumacher H, Dagenais G, Sleight P | display-authors = 6 | title = Effects of the angiotensin-receptor blocker telmisartan on cardiovascular events in high-risk patients intolerant to angiotensin-converting enzyme inhibitors: a randomised controlled trial | journal = Lancet | volume = 372 | issue = 9644 | pages = 1174–83 | date = September 2008 | pmid = 18757085 | doi = 10.1016/S0140-6736(08)61242-8 | s2cid = 5203511 | url = https://www.thelancet.com/journals/lancet/article/PIIS0140-6736(08)61242-8/abstract | access-date = 26 November 2019 }}

{{Agents acting on the renin–angiotensin system}}

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{{二次利用|date= 3 March 2024}}

[[Category:Angiotensin II receptor antagonists]]

[[Category:PPAR agonists]]

[[Category:Wikipedia medicine articles ready to translate]]