Telmisartan

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Telmisartan
Clinical data
Pronunciation/tɛlmɪˈsɑːrtən/
Trade namesMicardis, Actavis, others
AHFS/Drugs.comMonograph
MedlinePlusa601249
License data
Pregnancy
category
  • AU: D
Angiotensin 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
  • 2-(4-{[4-Methyl-6-(1-methyl-1H-1,3-benzodiazol-2-yl)-2-propyl-1H-1,3-benzodiazol-1-yl]methyl}phenyl)benzoic acid
JSmol)
  • O=C(O)c1ccccc1c2ccc(cc2)Cn3c4cc(cc(c4nc3CCC)C)c5nc6ccccc6n5C
  • InChI=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) checkY
  • Key:RMMXLENWKUUMAY-UHFFFAOYSA-N checkY
  (verify)

Telmisartan, sold under the brand name Micardis among others, is a

diabetic kidney disease.[2] It is a reasonable initial treatment for high blood pressure.[2] It is taken by mouth.[2] Versions are available as the combination[3] telmisartan/hydrochlorothiazide, telmisartan/cilnidipine[4] and telmisartan/amlodipine.[2]

Common side effects include

angiotensin II.[2]

Telmisartan was patented in 1991 and came into medical use in 1999.

generic medication.[7] In 2021, it was the 217th most commonly prescribed medication in the United States, with more than 1 million prescriptions.[8][9]

Medical uses

Telmisartan is used to treat

diabetic kidney disease.[2] It is a reasonable initial treatment for high blood pressure.[2][10]
: 146 

Contraindications

Telmisartan is contraindicated during

neonatal deaths. It is not known whether the drug passes into the breast milk.[11] 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

Allergic reactions may also occur.[11]

Interactions

Due to its mechanism of action, telmisartan increases blood

NSAIDs, especially in patients with impaired kidney function, has a risk of causing (usually reversible) kidney failure.[12]

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).[13]

Telmisartan's activity at the

GW 501516.[14] Telmisartan activates PPAR-δ receptors in several tissues.[15][16][17][18]

Also, telmisartan has a PPAR-γ agonist activity.[10]: 171 

Pharmacokinetics

The substance is quickly but to varying degrees absorbed from the gut. The average

alpha-1-acid glycoprotein.[12] It has the longest half-life of any angiotensin II receptor blocker (ARB) (24 hours)[19][13] and the largest volume of distribution among ARBs (500 liters).[20][21] 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]

History

See also: Discovery and development of angiotensin receptor blockers

Society and culture

Telmisartan is available as a

generic medication.[7]

References

  1. FDA
    . Retrieved 22 October 2023.
  2. ^ a b c d e f g h i j "Telmisartan Monograph for Professionals". Drugs.com. American Society of Health-System Pharmacists. Retrieved 3 March 2019.
  3. ^ Golwala D. "Formulation and Evaluation of Mouth Dissolving Tablets of Telmisartan". Inventi Journals. Retrieved 18 July 2020.[permanent dead link]
  4. ^ "Cilacar T". Medical Dialogues. Retrieved 23 February 2021.
  5. ^ "Telmisartan Pregnancy and Breastfeeding Warnings". Drugs.com. Retrieved 3 March 2019.
  6. ISBN 9783527607495
    .
  7. ^
    ISBN 9780857113382
    .
  8. ^ "The Top 300 of 2021". ClinCalc. Archived from the original on 15 January 2024. Retrieved 14 January 2024.
  9. ^ "Telmisartan - Drug Usage Statistics". ClinCalc. Retrieved 14 January 2024.
  10. ^
    ISBN 978-1-4160-6158-8
    .
  11. ^ a b Drugs.com: Micardis
  12. ^ a b c Haberfeld, H, ed. (2015). Austria-Codex (in German). Vienna: Österreichischer Apothekerverlag.
  13. ^
    PMID 15007034
    .
  14. PMID 22130396
    .
  15. ISBN 978-1-464-93110-9
    . Retrieved 2 April 2013.
  16. PMID 20477906
    .
  17. PMID 20176998
    .
  18. PMID 23238297
    .
  19. ^ Pritor prescribing information
  20. S2CID 33299699
    .
  21. PMID 17326326
    .

Further reading