Telmisartan 1

Telmisartan
Telmisartan

Systematic (IUPAC) name

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
Identifiers

CAS number [1]

144701-48-4

ATC code [2]

C09 CA07

PubChem [3]
CID 65999

IUPHAR ligand [4]

592

DrugBank [5]
APRD01247

ChemSpider [6]
59391

UNII [7]
U5SYW473RQ  

Chemical data

Formula C33H30N4O2

Mol. mass 514.617 g/mol

SMILES [8] [9]

eMolecules & PubChem

Pharmacokinetic data

Bioavailability 42–100%

Protein binding ≥99.5%

Metabolism Minimal hepatic

Half-life 24 hours

Excretion Faecal 97%

Therapeutic considerations

Pregnancy cat. D (Au), D (U.S.)

Legal status S4 (Au), POM (UK), ℞-only (U.S.)

Routes Oral
[10]
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Telmisartan 2

Telmisartan (INN) (pronounced /tɛlmɪˈsɑrtən/) is an angiotensin II receptor antagonist (ARB) used in the
management of hypertension. It is marketed under the trade names , Micardis (Boehringer Ingelheim), Targit
(Pfizer India Ltd), Temax (Wockhardt Ltd)

Administration
The usually effective dose telmisartan is (20-)40-80 mg once daily. Some patients may already benefit at a daily dose
of 20 mg. In cases where the target blood pressure is not achieved, telmisartan dose can be increased to a maximum
of 80 mg once daily. [11]

Mode of action
Telmisartan is an Angiotensin Receptor Blocker (ARB) that shows high affinity for the angiotensin II type 1 (AT1)
receptors, has a long duration of action, and has the longest half-life of any ARB. [11] [12]
In addition to blocking the Renin-Angiotensin System (RAS), 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). [12]
Telmisartan has binding affinity 3000 times greater for AT1 than AT2 receptors. Telmisartan also has the longest half
life (24 hrs) of all angiotensin II type 1 receptor antagonists. & It has largest volume of distribution

Indication
Telmisartan is indicated in the treatment of essential hypertension. [11]

Key Recent Clinical Trials

ONTARGET
The ONTARGET Trial Programme (The Ongoing Telmisartan Alone and in combination with Ramipril Global
Endpoint Trial) was one of the largest ARB clinical study programmes ever undertaken.[13]
Salim Yusuf, Lead Investigator and Director of the Population Health Research Institute at McMaster University,
Hamilton, Canada, presented the results of the l trial at the 57th Annual Scientific Session of the American College
of Cardiology (ACC) in Chicago, USA. [14] The results were then published in The New England Journal of
Medicine in April 2008.[15]
25,620 patients from 733 centres in 41 countries were randomised for 5.5 years of treatment of either telmisartan, the
ACE inhibitor ramipril or a combination of the two. The study aimed to investigate the role of telmisartan in
Cardiovascular (CV) protection through the primary composite outcome of death from CV causes, myocardial
infarction, stroke or hospilization for heart failure, in high CV risk patients.
The results revealed that telmisartan was as effective as ramipril but with lower rates of cough and angioedema
which led to fewer discontinuations. The combination group experienced similar efficacy but with increased risk of
hypotensive symptoms. Moreover, even in a patient population selected to tolerate ACE inhibitors, telmisartan was
shown to be better tolerated and associated with higher treatment compliance than ramipril. [16]
Telmisartan 3

TRANSCEND
As part of the ONTARGET study, patients who could not tolerate ACE inhibitors were randomly assigned to receive
either telmisartan or placebo as part of the TRANSCEND (Telmisartan Randomized Assessment Study in ACE
Intolerant Subjects with Cardiovascular Disease (CVD)) study. Results from this study were published in the Lancet,
September 2008. An accompanying editorial comments: "Overall, data supporting use of angiotensin-receptor
blockers to prevent vascular events in various cardiovascular groups, other than heart failure, are incomplete.
TRANSCEND's results challenge the non-inferiority shown in ONTARGET and suggest no more than a modest
effect, if any at all." [17]

PROTECTION
The PROTECTION programme (Programme of Research tO show Telmisartan End-organ proteCTION) consisted
of ten trials with 6,875 patients from 32 countries.[18]
The programme examined the efficacy of telmisartan or telmisartan/ hydrochlorothiazide at different stages of the
cardiovascular and renal continuum. The trials were conducted in patients with varying degrees of cardiovascular
risk from around the world
The 10 studies in the programme evaluated the effect of telmisartan on blood pressure control in two general patient
populations: patients at high risk for cardiovascular disease and patients with various renal pathologies. In all the
studies, telmisartan was compared either to placebo or to a gold standard medication such as the ACE inhibitors
ramipril and enalapril or the ARBs losartan and valsartan.
Telmisartan met and sometimes exceeded the gold standards (ACEIs and other ARBs) during the programme. In
at-risk patient populations, telmisartan induced strong and sustained blood pressure lowering throughout the critical
morning period where CV risk is highest ,and renoprotective effects at every stage of the renal continuum. [19] [20]

PRoFESS
PRoFESS - Prevention Regimen For Effectively Avoiding Second Strokes. Therapy with telmisartan initiated soon
after an ischemic stroke and continued for 2.5 years did not significantly lower the rate of recurrent stroke, major
cardiovascular events, or diabetes. (ClinicalTrials.gov number, NCT00153062)[21]

See also
Angiotensin Receptor Blockers: Drug discovery and development

External links
• http://www.pritor.com
• http://www.micardis.com/index.jsp
• http://www.pslgroup.com/dg/e6dce.htm
• http://www.ICMAedu.com
• http://www.emea.europa.eu
Telmisartan 4

References
[1] http:/ / www. nlm. nih. gov/ cgi/ mesh/ 2009/ MB_cgi?term=144701-48-4& rn=1
[2] http:/ / www. whocc. no/ atc_ddd_index/ ?code=C09CA07
[3] http:/ / pubchem. ncbi. nlm. nih. gov/ summary/ summary. cgi?cid=65999
[4] http:/ / www. iuphar-db. org/ DATABASE/ LigandDisplayForward?ligandId=592
[5] http:/ / www. drugbank. ca/ cgi-bin/ show_drug. cgi?CARD=APRD01247
[6] http:/ / www. chemspider. com/ Chemical-Structure. 59391
[7] http:/ / fdasis. nlm. nih. gov/ srs/ srsdirect. jsp?regno=U5SYW473RQ
[8] http:/ / www. emolecules. com/ cgi-bin/ search?t=ex&
q=O%3DC%28O%29c1ccccc1c2ccc%28cc2%29Cn3c4cc%28cc%28c4nc3CCC%29C%29c5nc6ccccc6n5C
[9] http:/ / pubchem. ncbi. nlm. nih. gov/ search/
?smarts=O%3DC%28O%29c1ccccc1c2ccc%28cc2%29Cn3c4cc%28cc%28c4nc3CCC%29C%29c5nc6ccccc6n5C
[10] http:/ / en. wikipedia. org/ w/ index. php?& diff=cur& oldid=395358330
[11] Pritor prescribing information
[12] Benson SC et al. Identification of telmisartan as a unique angiotensin II receptor antagonist with selective PPARgamma-modulating activity.
Hypertension 2004 May; 43(5): 993-1002.
[13] The ONTARGET Investigators. Telmisartan, Ramipril, or Both in Patients at High Risk for Vascular Events N Engl J Med
2008;358:1547-59.
[14] http:/ / www. ICMAedu. com
[15] The ONTARGET Investigators. Telmisartan, Ramipril, or Both in Patients at High Risk for Vascular Events N Engl J Med
2008;358:1547-59.
[16] http:/ / www. ICMAedu. com
[17] The Lancet 2008;372(9644): 1128–1130.
[18] Weber M. The telmisartan Programme of Research tO show Telmisartan End-organ proteCTION (PROTECTION) programme. J Hypertens
2003;21 (Suppl 6):S37–S46.
[19] Weber M. The telmisartan Programme of Research tO show Telmisartan End-organ proteCTION (PROTECTION) programme. J Hypertens
2003;21 (Suppl 6):S37–S46.
[20] http:/ / www. pritor. com
[21] http:/ / clinicaltrials. gov/ show/ NCT00153062
Article Sources and Contributors 5

Article Sources and Contributors

Telmisartan  Source: http://en.wikipedia.org/w/index.php?oldid=395702012  Contributors: A-giau, Agibso02, Aldis90, Arcadian, Bagith, Beetstra, Brim, Chowbok, DGG, Davidruben,
Elinborgus, Fabioli2010, Fahadsadah, Iridescent, Kotroskin, Kwamikagami, Lord spectre, Maazahmed84, Osnimf, Renee Bischoff, Retroneo, RiddlesNRhymes, Rjwilmsi, Rkc singh, Sababu,
Tavilis, Techelf, Triwbe, Uthbrian, Where next Columbus?, Wouterstomp, Zamphuor, ‫طبلا يلع نسح‬, 56 anonymous edits

Image Sources, Licenses and Contributors

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License
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