Cilnidipine Light Yellow Powder Chemical Intermediate API CAS 132203-70-4

More Info

Cilnidipine is unique because it blocks both L-type and N-type calcium channels, unlike other calcium channel blockers that primarily affect L-type channels. This dual action is thought to provide additional benefits in managing hypertension and potentially other conditions.

Pharmacodynamics

Cilnidipine is a third-generation dihydropyridine calcium channel blocker with strong blocking effect on both L-type and N-type Ca2+ channels. Animal experiments show that it can effectively reduce blood pressure in spontaneous hypertension, acute cold stimulation-induced elevated blood pressure response, and stroke-prone spontaneous hypertension in rats, and can prevent the occurrence of heart, brain, kidney and other organs complications; it also has a significant blood pressure-lowering effect on renal hypertension in dogs, and there is no rebound phenomenon when stopping the drug. Human studies have shown that the antihypertensive effect on essential hypertension is exact, the effect on myocardial contractility is very weak, can inhibit cardiac sympathetic hyperactivity, does not increase plasma renin activity, can inhibit norepinephrine and dopamine generation. Compared with other dihydropyridine calcium channel blockers, this product has the following characteristics: in addition to acting on L-type calcium channels as most calcium channel blockers, this product can also act on the N-type calcium channels in the sympathetic nerve endings, inhibiting sympathetic activation, which produces unique clinical characteristics, such as not increasing the heart rate of patients with essential hypertension, and also significantly reduce the patient's cardiothoracic ratio (the ratio of the transverse diameter of the heart to the transverse diameter of the thorax). It can also significantly reduce the cardiothoracic ratio (the ratio of the transverse diameter of the heart to the transverse diameter of the thorax) of patients, which is expected to be used in the prevention of high-risk heart attacks induced by sympathetic reflex activation.

It has good antihypertensive efficacy and anti-atherosclerotic effect. Although the antihypertensive activity of this product is similar to that of nifedipine and nicardipine, it has a slow onset of action, a long duration of maintenance of action, needs to be taken only once a day, does not increase the heart rate, has a weaker inhibition of the myocardium, and also has a stronger effect of dilating the coronary artery. These combined antihypertensive effects are superior to traditional dihydropyridine calcium channel blockers such as nifedipine. Clinical studies have also shown that this product, while lowering blood pressure, also has an anti-atherosclerotic effect, which is manifested in the ability to reduce the concentration of lipid peroxidase and atherosclerotic index (LDL/HDL cholesterol), and significantly increase the activity of superoxide dismutase, scavenging oxygen free radicals.

Applications

Cilnidipine is widely used to lower blood pressure.

Side Effects

The incidence of adverse reactions is low, mainly including headache, dizziness, flushing, palpitations, stomach discomfort, nausea, rash, itching, and elevated transaminase (GOT, GPT) levels.

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