Telmisartan 144701-48-4

Non-peptide angiotensin Ⅱ receptor antagonists can selectively and irreversibly block ATI receptors, but have no effect on other receptor systems. For mild to moderate hypertension. Telmisartan is a new antihypertensive drug. It is a specific angiotensin Ⅱ receptor (ATⅠ) antagonist for the treatment of essential hypertension. The alternative angiotensin Ⅱ receptor binds with high affinity to ATⅠ receptor subtype (known angiotensin Ⅱ action site). Telmisartan does not have any agonist effect at the ATⅠ receptor site. It selectively binds to ATⅠ receptor, and the binding effect is long-lasting. It has no affinity for other receptors, including ATII and AT receptors with less characteristics. The function of the other receptors mentioned above is unknown, and the possible receptor over stimulation effect is unknown due to the increase of angiotensin II level caused by Telmisartan. Telmisartan does not inhibit human plasma renin and does not block ion channels. Without inhibiting angiotensin converting enzyme II, the enzyme can also degrade the adverse reactions caused by the enhanced action of bradykinin. Administration of 80 mg telmisartan in human body can almost completely inhibit the increase of blood pressure caused by angiotensin II. The inhibitory effect lasted for 24 hours and could still be measured at 48 hours. The hypotensive effect was gradually obvious within 3 hours after the first dose. The maximum antihypertensive effect can be obtained 4 weeks after the start of treatment and can be maintained in long-term treatment. If the treatment is suddenly interrupted, the blood pressure will gradually return to the pre-treatment level after a few days without rebound hypertension. In the clinical trial of directly comparing the two hypertension drugs, the incidence of dry cough in the treatment group was significantly lower than that in the angiotensin converting enzyme inhibitor treatment group.