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{{Short description|Angiotensin II receptor antagonist}}
{{Drugbox
| Watchedfields = changed
| verifiedrevid = 477861448
| image = Telmisartan.svg
| width = 220
| alt =


| pronounce = {{IPAc-en|t|ɛ|l|m|ɪ|ˈ|s|ɑr|t|ən}}
| tradename = Micardis, Actavis, others
| Drugs.com = {{drugs.com|monograph|telmisartan}}
| MedlinePlus = a601249
| DailyMedID = Telmisartan
| pregnancy_AU = D
| routes_of_administration = [[Oral administration|By mouth]]
| class = [[Angiotensin II receptor antagonist]]
| ATC_prefix = C09
| ATC_suffix = CA07

| legal_AU = S4
| legal_CA = Rx-only
| legal_CA_comment =
| legal_UK = POM
| legal_US = RX-only
| legal_EU = RX-only


| bioavailability = 42–100%
| protein_bound = >99.5%
| metabolism = Minimal liver ([[glucuronidation]])
| elimination_half-life = 24 hours
| excretion = Feces 97%


| CAS_number_Ref = {{cascite|correct|??}}
| CAS_number = 144701-48-4
| PubChem = 65999
| IUPHAR_ligand = 592
| DrugBank_Ref = {{drugbankcite|correct|drugbank}}
| DrugBank = DB00966
| ChemSpiderID_Ref = {{chemspidercite|correct|chemspider}}
| ChemSpiderID = 59391
| UNII_Ref = {{fdacite|correct|FDA}}
| UNII = U5SYW473RQ
| KEGG_Ref = {{keggcite|correct|kegg}}
| KEGG = D00627
| ChEBI_Ref = {{ebicite|correct|EBI}}
| ChEBI = 9434
| ChEMBL_Ref = {{ebicite|correct|EBI}}
| ChEMBL = 1017


| 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
| C=33 | H=30 | N=4 | O=2
| smiles = O=C(O)c1ccccc1c2ccc(cc2)Cn3c4cc(cc(c4nc3CCC)C)c5nc6ccccc6n5C
| StdInChI_Ref = {{stdinchicite|correct|chemspider}}
| StdInChI = 1S/C33H30N4O2/c1-4-9-30-35-31-21(2)18-24(32-34-27-12-7-8-13-28(27)36(32)3)19-29(31)37(30)20-22-14-16-23(17-15-22)25-10-5-6-11-26(25)33(38)39/h5-8,10-19H,4,9,20H2,1-3H3,(H,38,39)
| StdInChIKey_Ref = {{stdinchicite|correct|chemspider}}
| StdInChIKey = RMMXLENWKUUMAY-UHFFFAOYSA-N
}}


'''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]].


Common side effects include [[upper respiratory tract infections]], diarrhea, and back pain. Serious side effects may include [[kidney problems]], [[low blood pressure]], and [[angioedema]]. Use in [[pregnancy]] may harm the baby and use when [[breastfeeding]] is not recommended. It is an [[angiotensin II receptor antagonist]] and works by blocking the effects of [[angiotensin II]].


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.

==Medical uses==
Telmisartan is used to treat [[hypertension|high blood pressure]], [[heart failure]], and [[diabetic kidney disease]]. It is a reasonable initial treatment for high blood pressure.

==Contraindications==
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==
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.

== Interactions ==

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]].

==Pharmacology==

===Mechanism of action===
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]].

In addition to blocking the [[renin–angiotensin system]], telmisartan acts as a selective modulator of [[peroxisome proliferator-activated receptor gamma]] (PPAR-γ), a central regulator of [[insulin]] and [[glucose]] metabolism. It is believed that telmisartan's dual mode of action may provide protective benefits against the vascular and renal damage caused by [[diabetes]] and [[cardiovascular disease]] (CVD).

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.

===Pharmacokinetics===
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.

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

==Society and culture==

Telmisartan is available as a [[generic medication]].

== Further reading ==
* {{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}}
{{Navboxes
| title = [[Pharmacodynamics]]
| titlestyle = background:#ccccff
| list1 =
{{Angiotensin receptor modulators}}
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{{二次利用|date= 3 March 2024}}
[[Category:Angiotensin II receptor antagonists]]
[[Category:Benzimidazoles]]
[[Category:Benzoic acids]]
[[Category:Biphenyls]]
[[Category:Drugs developed by Boehringer Ingelheim]]
[[Category:PPAR agonists]]
[[Category:Wikipedia medicine articles ready to translate]]

Telmisartan/en - Revision history

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