Telmisartan: Difference between revisions

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<!--T:1-->
{{Short description|Angiotensin II receptor antagonist}}
{{Short description|Angiotensin II receptor antagonist}}
{{Drugbox
{{Drugbox
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| alt =  
| alt =  


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<!-- Clinical data -->
<!-- Clinical data -->
| pronounce  = {{IPAc-en|t|ɛ|l|m|ɪ|ˈ|s|ɑr|t|ən}}
| pronounce  = {{IPAc-en|t|ɛ|l|m|ɪ|ˈ|s|ɑr|t|ən}}
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| ATC_suffix = CA07
| ATC_suffix = CA07


<!--T:3-->
| legal_AU = S4
| legal_AU = S4
| legal_CA          = Rx-only
| legal_CA          = Rx-only
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| legal_EU = RX-only
| legal_EU = RX-only


<!--T:4-->
<!-- Pharmacokinetic data -->
<!-- Pharmacokinetic data -->
| bioavailability = 42–100%
| bioavailability = 42–100%
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| excretion = Feces 97%
| excretion = Feces 97%


<!--T:5-->
<!-- Identifiers -->
<!-- Identifiers -->
| CAS_number_Ref = {{cascite|correct|??}}
| CAS_number_Ref = {{cascite|correct|??}}
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| ChEMBL = 1017
| ChEMBL = 1017


<!--T:6-->
<!-- Chemical data -->
<!-- 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
| 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
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}}
}}


<!--T:7-->
<!-- Definition and medical uses -->
<!-- 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]].
'''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]].


<!--T:8-->
<!-- Side effects and mechanisms -->
<!-- Side effects and mechanisms -->
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]].
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]].


<!--T:9-->
<!-- Society and culture -->
<!-- Society and culture -->
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 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==
==Medical uses== <!--T:10-->
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.
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==
==Contraindications== <!--T:11-->
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]].
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== <!--T:12-->
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.
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 ==
== Interactions == <!--T:13-->


<!--T:14-->
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]].
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==
==Pharmacology== <!--T:15-->


===Mechanism of action===
===Mechanism of action=== <!--T:16-->
Telmisartan is an angiotensin II receptor blocker that shows high affinity for the [[angiotensin II receptor type 1]] (AT<sub>1</sub>), with a binding affinity 3000 times greater for AT<sub>1</sub> than [[Angiotensin II receptor type 2|AT<sub>2</sub>]].
Telmisartan is an angiotensin II receptor blocker that shows high affinity for the [[angiotensin II receptor type 1]] (AT<sub>1</sub>), with a binding affinity 3000 times greater for AT<sub>1</sub> than [[Angiotensin II receptor type 2|AT<sub>2</sub>]].


<!--T:17-->
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).
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).


<!--T:18-->
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.
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.


<!--T:19-->
Also, telmisartan has a [[PPAR agonist|PPAR-γ agonist]] activity.
Also, telmisartan has a [[PPAR agonist|PPAR-γ agonist]] activity.


===Pharmacokinetics===
===Pharmacokinetics=== <!--T:20-->
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.
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==
==History== <!--T:21-->
{{see also|Discovery and development of angiotensin receptor blockers}}
{{see also|Discovery and development of angiotensin receptor blockers}}


==Society and culture==
==Society and culture== <!--T:22-->


<!--T:23-->
Telmisartan is available as a [[generic medication]].
Telmisartan is available as a [[generic medication]].


== Further reading ==
== Further reading == <!--T:24-->
* {{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 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 }}
* {{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 }}


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{{Agents acting on the renin–angiotensin system}}
{{Agents acting on the renin–angiotensin system}}
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{{Navboxes
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{{Portal bar | Medicine}}
{{Portal bar | Medicine}}


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{{二次利用|date= 3 March 2024}}
{{二次利用|date= 3 March 2024}}
[[Category:Angiotensin II receptor antagonists]]
[[Category:Angiotensin II receptor antagonists]]
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[[Category:PPAR agonists]]
[[Category:PPAR agonists]]
[[Category:Wikipedia medicine articles ready to translate]]
[[Category:Wikipedia medicine articles ready to translate]]
</translate>

Latest revision as of 16:02, 28 March 2024

Other languages:
Telmisartan
Clinical data
Pronunciation/tɛlmɪˈsɑːrtən/
Trade namesMicardis, Actavis, others
AHFS/Drugs.comMonograph
MedlinePlusa601249
License data
Pregnancy
category
  • AU: D
Routes of
administration		By mouth
Drug classAngiotensin II receptor antagonist
ATC code
Legal status
Legal status
Pharmacokinetic data
Bioavailability42–100%
Protein binding>99.5%
MetabolismMinimal liver (glucuronidation)
Elimination half-life24 hours
ExcretionFeces 97%
Identifiers
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
Chemical and physical data
FormulaC33H30N4O2
Molar mass514.629 g·mol−1
3D model (JSmol)
  (verify)

Telmisartan, sold under the brand name Micardis among others, is a medication used to treat 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 million prescriptions.

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.

Contraindications

Telmisartan is contraindicated during pregnancy. Like other drugs affecting the renin–angiotensin system (RAS), telmisartan can cause birth defects, stillbirths, and neonatal deaths. 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 reactions may also occur.

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.

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.

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-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

  • Yusuf S, Teo KK, Pogue J, Dyal L, Copland I, Schumacher H, et al. (April 2008). "Telmisartan, ramipril, or both in patients at high risk for vascular events". The New England Journal of Medicine. Massachusetts Medical Society. 358 (15): 1547–59. doi:10.1056/nejmoa0801317. hdl:2437/81925. PMID 18378520.
  • Yusuf S, Teo K, Anderson C, Pogue J, Dyal L, Copland I, et al. (September 2008). "Effects of the angiotensin-receptor blocker telmisartan on cardiovascular events in high-risk patients intolerant to angiotensin-converting enzyme inhibitors: a randomised controlled trial". Lancet. 372 (9644): 1174–83. doi:10.1016/S0140-6736(08)61242-8. PMID 18757085. S2CID 5203511. Retrieved 26 November 2019.
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