Pharmacological action

Antihypertensive drug.

Pharmacodynamics

Telmisartan is a specific antagonist of angiotensin II receptors. Has a high affinity for the AT1 receptor subtype of angiotensin II, through which the action of angiotensin II is realized. Telmisartan displaces angiotensin II from its binding to the receptor, without the action of an agonist for this receptor. It only binds to the AT1 receptor subtype of angiotensin II. Binding is long-lasting. Telmisartan does not have an affinity for other receptors (including AT2 receptors) and other less studied angiotensin receptors. The functional significance of these receptors, as well as the effect of their possible excessive stimulation with angiotensin II, whose concentration increases with the appointment of telmisartan, have not been studied. Reduces the concentration of aldosterone in the blood, does not inhibit renin in the blood plasma and does not block the ion channels. It does not inhibit ACE (kininase II), an enzyme that also breaks down bradykinin, so the increase in side effects caused by bradykinin is not expected.

Telmisartan at a dose of 80 mg completely blocks the hypertensive effect of angiotensin II. The onset of hypotensive action is noted within 3 hours after the first administration of telmisartan. The effect of the drug persists for 24 hours and remains significant until 48 hours. The pronounced antihypertensive effect usually develops after 4-8 weeks of regular administration.

In patients with arterial hypertension telmisartan reduces systolic and diastolic blood pressure, without affecting the heart rate.

In the case of a sharp withdrawal of telmisartan, blood pressure gradually returns to the baseline without the development of withdrawal syndrome.

Indications

- arterial hypertension;

- Reduction of cardiovascular morbidity and mortality in patients aged 55 years and older with a high risk of cardiovascular disease.