莫索尼定

概览

Moxonidine is an imidazoline/α-2 receptor agonist used to treat hypertension, especially in cases where ACE inhibitors, β-blockers, calcium channel blockers, and thiazides are not appropriate or provide inadequate blood pressure control.

作用机制

Stimulation of central alpha 2-adrenergic receptors is associated with sympathoadrenal suppression and subsequent reduction of blood pressure. As this class was further explored it was discovered that sympathoadrenal activity can also be suppressed by a second pathway with a newly discovered drug target specific to imidazolines . Specifically, moxonidine binds the imidazoline receptor subtype 1 (I1) and to a lesser extent αlpha-2-adrenoreceptors in the RSV causing a reduction of sympathetic activity, reducing systemic vascular resistance and thus arterial blood pressure. Moreover, since alpha-2-adrenergic receptors are considered the primary molecular target that facilitates the most common side effects of sedation and dry mouth that are elicited by most centrally acting antihypertensives, moxonidine differs from these other centrally acting antihypertensives by demonstrating only low affinity for central alpha-2-adrenoceptors compared to the aforementioned I1-imidazoline receptors .

适应症

For the treatment of mild to moderate essential or primary hypertension . Effective as most first-line antihypertensives when used as monotherapy .

• Hypertension