Telmisartan

Overview

Telmisartan, sold under the brand name Micardis among others, is a medication used to treat high blood pressure and heart failure. It is a reasonable initial treatment for high blood pressure. It is taken by mouth.[1][2] WP

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 blocker and works by blocking the effects of angiotensin II.[2][3] WP

Telmisartan was patented in 1991 and came into medical use in 1999. It is available as a generic medication. In 2023, it was the 184th most commonly prescribed medication in the United States, with more than 2 million prescriptions. It is available in combination with hydrochlorothiazide as telmisartan/hydrochlorothiazide; with cilnidipine as telmisartan/cilnidipine; and with amlodipine as telmisartan/amlodipine.[2][4–10] WP

Drug class

Angiotensin II receptor antagonist WP

From the Wikipedia article's infobox.

Uses, dosage and effects

Medical uses

Telmisartan is used to treat high blood pressure, heart failure, and diabetic kidney disease. It is a reasonable initial treatment for high blood pressure.[2][11] WP

Risks and side effects

Contraindications

Telmisartan is contraindicated during pregnancy. Telmisartan affects the renin–angiotensin system and can cause birth defects, stillbirths, and neonatal deaths. It is not known whether the medication passes into breast milk.[1][2][3] WP

Side effects

Side effects 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 reactions may also occur.[2] WP

Interactions

Interactions

Due to its mechanism of action, telmisartan increases blood potassium levels. Combination with potassium preparations or potassium-sparing diuretics 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.[12] WP

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 AT₂. WP⚠ Wikipedia itself has flagged this text: citation needed.

In addition to blocking the renin–angiotensin system, telmisartan acts as a partial agonist 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). As a partial agonist, it activates the receptor by 25–30%. Clinical trials have shown that telmisartan increases insulin sensitivity, reduces cardiac fibrosis and hypertrophy, and improves endothilial function; all these effects can be attributed to its activity on PPAR-γ. The kidney-protecting activity of telmisartan is attributed to both angiotensin II antagonism and improved endothelial function from PPAR-γ.[11][13][14] WP

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. In mice, this results in effects such as enhanced endurance. However, telmisartan does not improve the walking performance (6-minute walk distance) in people with lower extremity peripheral artery disease.[15–20] WP

Telmisartan activates PPAR-α in vitro. Telmisartan inhibits CYP2J2.[21][22] WP

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.[2][12][13][23][24][25] WP

Research

Research

Telmisartan does not appear effective for slowing the growth of abdominal aortic aneurysm.[26] WP

Telmisartan does not cause rapid cancer growth like the PPAR-δ agonist GW 501516, but whether it causes a change in cancer rates is disputed. Short-term use is not associated with an increased incidence of cancer over other ARB drugs, according to a large 2016 analysis of UK patients. A 2022 meta-analysis finds that a longer duration of taking ARBs (including telmisartan) is associated with an increase in cancer rates. Patients who have taken an ARB for more than 3 years appears 11% more likely to develop cancer. A 2023 large-scale study on Lebanese patients finds that taking ARBs reduces the incidence of cancer, with greater effects on those who have taken the drug for a long time. A 2021 Korean study and a 2012 Japanese study finds similar results.[27][28][29] WP

Legal status

Society and culture

Telmisartan is available as a generic medication.[5] WP

Chemistry

Formula

C33H30N4O2 PC

CAS number

144701-48-4 PC

Molar mass (g/mol)

514.6 PC

IUPAC name (computed by PubChem)

2-[4-[[4-methyl-6-(1-methylbenzimidazol-2-yl)-2-propylbenzimidazol-1-yl]methyl]phenyl]benzoic acid PC

SMILES

CCCC1=NC2=C(N1CC3=CC=C(C=C3)C4=CC=CC=C4C(=O)O)C=C(C=C2C)C5=NC6=CC=CC=C6N5C PC

InChIKey

RMMXLENWKUUMAY-UHFFFAOYSA-N PC

PubChem CID

65999

Harm reduction information

No harm reduction data is on file for this compound yet. That means no dose, timing or combination data from PsychonautWiki or TripSit. Please don't guess a dose from similar compounds. If you have taken it and feel unwell, contact emergency services or a poison control center.

User reports

Pop culture

No references added yet.

Sources

1. Journal / agency Micardis- telmisartan tablet. 19 December 2022
2. Other Telmisartan Monograph for Professionals
3. Other Telmisartan Pregnancy and Breastfeeding Warnings
4. Other Fischer J, Ganellin CR. Analogue-based Drug Discovery. 2006
5. Other British national formulary: BNF 76. 2018
6. Other Top 300 of 2023
7. Other Telmisartan Drug Usage Statistics, United States, 2014 - 2023
8. Journal / agency Micardis HCT- telmisartan and hydrochlorothiazide tablet. 29 June 2023
9. Other Cilacar T
10. Journal / agency Telmisartan and amlodipine tablet. 15 December 2023
11. Other Opie LH, Gersh BJ. Drugs for the heart. 2009
12. Other Austria-Codex. 2015
13. Journal / agency Benson SC, Pershadsingh HA, Ho CI, Chittiboyina A, Desai P, Pravenec M, Qi N, Wang J, Avery MA, Kurtz TW. Identification of telmisartan as a unique angiotensin II receptor antagonist with selective PPARgamma-modulating activity. Hypertension. May 2004. doi:10.1161/01.HYP.0000123072.34629.57 · PMID 15007034
14. Journal / agency Ayza MA, Zewdie KA, Tesfaye BA, Gebrekirstos ST, Berhe DF. Anti-Diabetic Effect of Telmisartan Through its Partial PPARγ-Agonistic Activity. Diabetes, Metabolic Syndrome and Obesity: Targets and Therapy. 2020. doi:10.2147/DMSO.S265399 · PMID 33116714 · PMC7567533
15. Journal / agency Sanchis-Gomar F, Lippi G. Telmisartan as metabolic modulator: a new perspective in sports doping?. Journal of Strength and Conditioning Research. March 2012. doi:10.1519/JSC.0b013e31824301b6 · PMID 22130396
16. Other Cytoplasmic and Nuclear Receptors: Advances in Research and Application: 2011 Edition. 2012
17. Journal / agency Feng X, Luo Z, Ma L, Ma S, Yang D, Zhao Z, Yan Z, He H, Cao T, Liu D, Zhu Z. Angiotensin II receptor blocker telmisartan enhances running endurance of skeletal muscle through activation of the PPAR-δ/AMPK pathway. Journal of Cellular and Molecular Medicine. July 2011. doi:10.1111/j.1582-4934.2010.01085.x · PMID 20477906 · PMC3823201
18. Journal / agency He H, Yang D, Ma L, Luo Z, Ma S, Feng X, Cao T, Yan Z, Liu D, Tepel M, Zhu Z. Telmisartan prevents weight gain and obesity through activation of peroxisome proliferator-activated receptor-delta-dependent pathways. Hypertension. April 2010. doi:10.1161/HYPERTENSIONAHA.109.143958 · PMID 20176998
19. Journal / agency Li L, Luo Z, Yu H, Feng X, Wang P, Chen J, Pu Y, Zhao Y, He H, Zhong J, Liu D, Zhu Z. Telmisartan improves insulin resistance of skeletal muscle through peroxisome proliferator-activated receptor-δ activation. Diabetes. March 2013. doi:10.2337/db12-0570 · PMID 23238297 · PMC3581229
20. Journal / agency McDermott MM, Bazzano L, Peterson CA, Sufit R, Ferrucci L, Domanchuk K, Zhao L, Polonsky TS, Zhang D, Lloyd-Jones D, Leeuwenburgh C, Guralnik JM, Kibbe MR, Kosmac K, Criqui MH, Tian L. Effect of Telmisartan on Walking Performance in Patients With Lower Extremity Peripheral Artery Disease: The TELEX Randomized Clinical Trial. JAMA. October 2022. doi:10.1001/jama.2022.16797 · PMID 36194220 · PMC9533188
21. Journal / agency Yin SN, Liu M, Jing DQ, Mu YM, Lu JM, Pan CY. Telmisartan increases lipoprotein lipase expression via peroxisome proliferator-activated receptor-alpha in HepG2 cells. Endocrine Research. 2014. doi:10.3109/07435800.2013.828741 · PMID 24067162
22. Journal / agency Marco Sisignano, Dieter Steinhilber, Michael J Parnham, Gerd Geisslinger. Exploring CYP2J2: lipid mediators, inhibitors and therapeutic implications. Drug Discovery Today. September 2020. doi:10.1016/j.drudis.2020.07.002 · PMID 32652311
23. Other Pritor prescribing information
24. Journal / agency Stangier J, Su CA, Roth W. Pharmacokinetics of orally and intravenously administered telmisartan in healthy young and elderly volunteers and in hypertensive patients. The Journal of International Medical Research. 2000. doi:10.1177/147323000002800401 · PMID 11014323
25. Journal / agency Gosse P. A review of telmisartan in the treatment of hypertension: blood pressure control in the early morning hours. Vascular Health and Risk Management. September 2006. doi:10.2147/vhrm.2006.2.3.195 · PMID 17326326 · PMC1993985
26. Journal / agency Golledge J, Pinchbeck J, Tomee SM, Rowbotham SE, Singh TP, Moxon JV, Jenkins JS, Lindeman JH, Dalman RL, McDonnell L, Fitridge R, Morris DR. Efficacy of Telmisartan to Slow Growth of Small Abdominal Aortic Aneurysms: A Randomized Clinical Trial. JAMA Cardiology. December 2020. doi:10.1001/jamacardio.2020.3524 · PMID 32845283 · PMC7450408
27. Journal / agency Tascilar K, Azoulay L, Dell'Aniello S, Bartels DB, Suissa S. The Use of Telmisartan and the Incidence of Cancer. American Journal of Hypertension. December 2016. doi:10.1093/ajh/hpw095 · PMID 27557862 · PMC5863774
28. Journal / agency Sipahi I. Risk of cancer with angiotensin-receptor blockers increases with increasing cumulative exposure: Meta-regression analysis of randomized trials. PLOS ONE. 2022. doi:10.1371/journal.pone.0263461 · PMID 35235571 · PMC8890666
29. Journal / agency Dagher YG, El Helou S, Haifa KG, Chalhoub IG, Boulos RT, Atallah B, Nasr F, Kassab I, Chahine MN. The association between angiotensin receptor blockers and lung, bladder, and colon cancer development: A 10-year multicentric retrospective Lebanese study. Medicine. September 2023. doi:10.1097/MD.0000000000034901 · PMID 37682163 · PMC10489396

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