Telmisartan

Product name: Telmisartan

CAS No.: 144701-48-4

Molecular formula: C33H30N4O2

Molecular weight: 514.62

Melting point: 261-263°C

Introduction

Telmisartan is an angiotensin II receptor antagonist (angiotensin receptor blocker) used in the treatment of hypertension. Telmisartan has the longest efficacy among similar drugs; clinical studies have shown that it can reduce blood pressure 24 hours a day, including at the highest risk of cardiovascular disease in the early morning. Telmisartan is also the only angiotensin receptor blocker at present. Clinical studies have shown that besides lowering blood pressure in patients with high cardiovascular risk and diabetes mellitus, Telmisartan can provide additional cardiovascular protection and reduce their chances of death, myocardial infarction or stroke due to cardiovascular disease.

Function

Telmisartan is a non-peptide angiotensin II receptor antagonist, selectively and irreversibly blocking ATI receptor, but has no effect on other receptor systems. For mild to moderate hypertension. Telmisartan is a new type of antihypertensive drug, a specific angiotensin II receptor (ATI) antagonist, used in the treatment of essential hypertension. Replacement of angiotensin II receptor binds to ATI receptor subtype (known site of action of angiotensin II) with high affinity.

Application

Telmisartan has no agonist effect at ATI receptor site. It selectively binds to ATI receptor and the binding effect lasts for a long time. There was no affinity for other receptors, including AT2 and other AT receptors with fewer characteristics. The function of the other receptors mentioned above is unknown. Because telmisartan increases the level of angiotensin II, it is also unknown that telmisartan may cause receptor overstimulation. Telmisartan does not inhibit renin in human plasma, nor does it block ion channels. It does not inhibit angiotensin converting enzyme II, which can also degrade the adverse reactions caused by increased bradykinin action. 80 mg telmisartan can almost completely inhibit the elevation of blood pressure induced by angiotensin II in human body. The inhibitory effect lasted 24 hours and was still detectable in 48 hours.