Enalapril intermediate (ECPPA) 82717-96-2

ECPPA is a metabolite of Enalapril,Enalapril is used in the treatment of hypertension, diabetic nephropathy, and some types of chronic heart failure. It has been proven to protect the function of the kidneys in hypertension, heart failure, and diabetes, and may be used in the absence of hypertension for its kidney protective effects. It is widely used in chronic kidney failure.

Like captopril, enalapril selectively suppresses the rennin–angiotensin–aldosterone system, inhibits angiotensin-converting enzyme, and prevents conversion of angiotensin I into angiotensin II.

Angiotensin converting enzyme inhibitor (ACE-I) is the second ACE-I in the world to be launched after captopril. The effect of treating hypertension is similar to that of captopril, but stronger, with a slow and long-lasting effect. Like captopril, when combined with the diuretic dihydrochlorothiazide to form a compound, the therapeutic effect can generally be improved by 15% -30%. Used for primary, renal hypertension, renal vascular hypertension, malignant hypertension, etc., it is also suitable for congestive heart failure, especially for hypertensive patients with high renin and high blood calcium that require long-term medication, and patients with congestive heart failure who have ineffective treatment with digitalis and diuretics. It can also be used for patients who cannot tolerate captopril.

After oral administration, the absorption of this product is about 60%, and it is not affected by food in the gastrointestinal tract. After absorption, the dicarboxylic acid enalapril generated by hydrolysis in the liver has a stronger inhibitory effect on angiotensin converting enzyme than this product, but oral enalapril absorption is extremely poor. After oral administration of this product, the blood drug concentration reaches its peak about 1 hour, while the peak blood drug concentration of enalapril is between 3-4 hours. The effective half-life of enalapril after most doses of this product is 11 hours. After taking one dose of this product orally, the antihypertensive effect begins at 1 hour and reaches its peak at 4-6 hours. The recommended dosage is used, and the antihypertensive effect can be maintained for more than 24 hours. Through renal excretion, about 94% of the oral dose is present in urine and feces as this product or enalapril, with no other metabolites. When the glomerular filtration rate decreases to below 30ml per minute, the peak and steady-state times are delayed. Enalapril can be cleared by dialysis at a rate of 62ml per minute. This product is not easily able to pass through the blood-brain barrier, and enalapril does not enter the brain.

This product is an angiotensin-converting enzyme inhibitor, which works by hydrolyzing it into enalapril in the liver after oral administration. The inhibitory effect of the latter on angiotensin-converting enzyme is more than 8 times that of captopril. The mechanism of antihypertensive action is the same as that of captopril, but the duration of action is long-lasting. This product can reduce blood pressure while maintaining myocardial contractility, without affecting cardiac output. In patients with congestive heart failure, peripheral vascular resistance and pulmonary capillary wedge pressure can be reduced, thereby reducing the pre - and post cardiac load and improving cardiac function. This product can increase renal blood flow and has no significant effect on blood glucose, uric acid, and cholesterol metabolism.