Moxonidine

Pharmacological action This product is a central antihypertensive drug. It has a high affinity for imidazoline ⅰreceptor and is a selective agonist of imidazoline ⅰreceptor. By activating imidazoline receptor in medullae oblongata, peripheral sympathetic nerve activity is decreased, blood vessel dilation is decreased, peripheral vascular resistance is decreased, and blood pressure is lowered. The affinity of this product to the α2 receptor is weaker than that of the ⅱimidazoline receptor, so this product does not slow down the heart rate during hypotension, and has no obvious central sedation effect.
The oral absorption of this product is fast, the blood concentration reaches the peak in 0.3 to 1 hour, and the bioavailability is about 88%. This product has no first-pass effect, 58 to 60% of the prototype compound is excreted by the kidney, and less than 2% of the drug is excreted by the stool. Less than 15% of the drug is metabolized in the body, and the main products are 4, 5-deoxymoxonidine and guanidine derivatives, with an oral T1/2 (elimination half-life) of about 2 hours. Food intake did not affect the pharmacokinetics of this product.