Advantages of ACEI antihypertensive drugs: Blood pressure management that protects the heart, brain, and kidneys

What are the advantages and adverse reactions of angiotensin-converting enzyme inhibitors (ACEIs)?

(1) Advantages of ACEIs and their effects beyond lowering blood pressure: Angiotensin-converting enzyme inhibitors (ACEIs) are relatively new antihypertensive drugs, first synthesized artificially in 1977. Their antihypertensive mechanism targets the renin-angiotensin-aldosterone system, with a clear antihypertensive effect. In addition to lowering blood pressure, they have effects beyond lowering blood pressure, such as reversing vascular wall and myocardial hypertrophy, reducing the incidence of new-onset diabetes, slowing diabetic nephropathy, and improving insulin sensitivity. They have no adverse effects on glucose and lipid metabolism. Therefore, new varieties are constantly emerging, with more than 20 varieties available to date. Nearly 10 varieties are also marketed in my country. They are widely recognized as first-line drugs for hypertension treatment. In addition to their antihypertensive effects, these drugs have many other applications:

① In patients at high risk of coronary heart disease, heart failure, abnormal left ventricular systolic function, or myocardial infarction, they can significantly improve prognosis and reduce mortality;

② In patients with diabetes or diabetic nephropathy and other chronic kidney diseases and renal impairment, they can delay renal function deterioration;

③ In patients with hypertension and stroke, they can prevent and reduce stroke recurrence.

Evidence-based medicine studies have demonstrated that ACEIs have excellent protective effects on the heart, brain, and kidneys. As mentioned earlier, when used alone, their effects on lowering blood pressure, preventing cardiovascular events, preventing stroke, and preventing heart failure are slightly less than those of diuretics and calcium channel blockers. However, their unique advantage lies in not affecting glucose and lipid metabolism and their kidney-protective effect. Therefore, this drug should be the first choice for patients with hypertension accompanied by diabetes, coronary heart disease, heart failure, and renal impairment.

(2) Major adverse reactions of ACEIs: ACEIs work by blocking the renin-angiotensin-aldosterone pathway, leading to a decrease in angiotensin II and bradykinin degradation, thereby dilating blood vessels and lowering blood pressure. Bradykinin is the main cause of the common adverse reaction, cough.

① Cough: Literature reports an incidence rate ranging from 10% to 30%. Fosinopril and imidapril have lower incidence rates.

② Hyperkalemia: More likely to occur in patients with renal insufficiency. Renal function should be rechecked one week after starting medication; thereafter, occasional checks are sufficient.

③ Elevated serum creatinine: A slight increase in serum creatinine (< 30%) may occur in the initial stages of ACEI use; this is a normal reaction and does not require discontinuation. If the increase is significant (>30%~50%), medication should be discontinued.

④ Hypotension: Hypotension may occur in the first few days of treatment or when increasing the dose; it is more likely to occur in patients with low sodium levels. Therefore, when taking ACEIs for the first time, start with a small dose or reduce the dosage of diuretics.

⑤ Other adverse reactions: rash, altered taste, and occasionally leukopenia and angioedema.

(3) Contraindications for ACEIs: Because ACEIs reduce renal blood flow, they should not be used by women with bilateral renal artery stenosis, hyperkalemia, or gestational hypertension.

What are the differences between different ACEI drugs?

Among these drugs, except for captopril which directly inhibits angiotensin-converting enzyme (ACE) after absorption into the bloodstream, the others are metabolized by the liver or kidneys into active substances that inhibit ACE. These active substances bind more tightly to ACE, resulting in a longer duration of action and a more sustained antihypertensive effect. Except for captopril, most only require once-daily administration.

ACEIs have a higher affinity for tissues with carboxyl groups and a lower affinity with sulfhydryl and phosphate groups. The affinity with the organization is in the following order: benazepril > quinapril > remipril > perindopril > lisinopril > enalapril > fosinopril > captopril.