Telmisartan

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Image:Telmisartan.png
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	C09 CA07
PubChem	65999
DrugBank	APRD01247
Chemical data
Formula	C₃₃H₃₀N₄O₂
Mol. weight	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 (GSK).

[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.