Telmisartan

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Telmisartan
Systematic (IUPAC) name
2-[4-[[4-methyl-6-(1-methylbenzoimidazol-2-yl)-
2-propyl-benzoimidazol-1-yl]methyl]phenyl]
benzoic acid
Identifiers
CAS number 144701-48-4
ATC code C09CA07
PubChem 65999
DrugBank APRD01247
Chemical data
Formula C33H30N4O2 
Mol. mass 514.617 g/mol
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

Telmisartan (INN) (IPA: [tɛlmɪˈsatən]) is an angiotensin II receptor antagonist (ARB) used in the management of hypertension. It is marketed under the trade names Micardis (Boehringer Ingelheim) and Pritor (Bayer Schering Pharma).

[edit] Pharmacology

Generally, angiotensin II receptor blockers (ARBs) such as telmisartan bind to the angiotensin II type 1 (AT1) receptors with high affinity, causing inhibition of the action of angiotensin II on vascular smooth muscle, ultimately leading to a reduction in arterial blood pressure.

New studies suggest that telmisartan may also have PPARγ agonistic properties that could potentially confer beneficial metabolic effects. This observation is currently being explored in clinical trials.

[edit] Clinical use


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