The "All-Round" Guardian of Hypertension Treatment: A Comprehensive Understanding of the Characteristics and Cough Management of ACEI Drugs (Priligy)

Angiotensin-Converting Enzyme Inhibitors (ACEIs)

What are Angiotensin-Converting Enzyme Inhibitors (ACEIs)?

What are their characteristics?

The advent of angiotensin-converting enzyme inhibitors (ACEIs) is a major advancement in the treatment of hypertension. They work by inhibiting the activity of angiotensin-converting enzyme (ACE), preventing the conversion of angiotensin I (ANGI) into angiotensin II (ANGII), which has a strong vasoconstrictive effect, thus causing dilation of systemic arterioles; reducing sympathetic nerve excitability; increasing parasympathetic nerve activity; reducing aldosterone secretion, facilitating sodium excretion; inhibiting kininase; increasing prostaglandin synthesis; further reducing peripheral resistance; thereby reducing and alleviating cardiac afterload, reversing left ventricular hypertrophy, and improving cardiac function. Therefore, this product is not only suitable for treating various types of hypertension but is also a good drug for treating congestive heart failure. This product can also specifically dilate the efferent artery of the glomerulus, reducing intraglomerular pressure, increasing renal blood flow, and improving renal function. In recent years, studies have also found that this product can improve insulin sensitivity, reduce plasma insulin levels, improve insulin resistance, and reduce sympathetic nerve excitability. Compared with β-blockers and diuretics, this class of drugs also has the advantages of improving blood lipid and glucose metabolism and increasing uric acid excretion.

What are some commonly used angiotensin-converting enzyme inhibitors (ACEIs)? How are they taken? Drugs ending in "pril" belong to this class. Commonly used drugs in this class include the following:

① Captopril: Also known as methylcaptopril, captopril, and captopril. It has a mild to moderate antihypertensive effect. It is rapidly absorbed orally, with an absorption rate of about 70%. The antihypertensive effect appears 15 minutes after administration and lasts for 6–12 hours. Its half-life is 2–3 hours, making it a short-acting drug, mainly used for various types of hypertension, especially myocardial infarction and diabetes mellitus with hypertension. Oral administration: Adults take 6.25–12.5 mg each time, 2–3 times daily; if necessary, the dose can be increased to 25–50 mg twice daily after 2–4 weeks.

② Enalapril: Also known as Enalapril or Enalapril. It has a strong and long-lasting antihypertensive effect, approximately 10 times stronger than captopril. In addition, it can increase cardiac output and slow heart rate, thereby improving cardiac function in congestive heart failure. The initial dose is 5 mg once daily; for severe hypertension, the dose can be increased to 40 mg daily, divided into two oral doses.

③ Lisinopril: Also known as Zestriil. Oral absorption is slightly slower than enalapril, and the antihypertensive effect can last for about 24 hours. The starting dose is 5 mg once daily.

④ Benazepril: Also known as Benazepril or Benazepril. It is rapidly absorbed orally, with maximum effect occurring in 2-4 hours and lasting for at least 24 hours. The dosage is 10 mg once daily, with a maximum dose of 20-40 mg daily, divided into two doses. For patients with renal insufficiency, the initial dose is 5 mg daily.

⑤ Perindopril: Also known as Jasida. It has a rapid onset of action, with effects occurring 1 hour after administration. Maximum effect occurs in 4-8 hours, and the effect lasts for 24 hours. Its potency is 3-11 times stronger than cilazapril and enalapril, and its antihypertensive efficacy is superior to captopril, verapamil, metoprolol, atenolol, and nifedipine. The initial dose is 2 mg, and the maintenance dose is 4 mg once daily.

⑥ Fosinopril: Also known as Monopril. This product features equal excretion through two pathways, making it suitable not only for general hypertension patients and elderly hypertension patients, but also for patients with hepatic or renal insufficiency. It can significantly improve symptoms and signs in patients with chronic heart failure, such as dyspnea, fatigue, paroxysmal nocturnal dyspnea, and edema. For oral administration, the initial adult dose is 10 mg daily. The usual maintenance dose is 10–40 mg daily.

⑦ Cilapril: Also known as Cilapril. It is 10 times more potent than captopril, taking effect 1 hour after administration, with maximum effect 3–7 hours after administration, and its effect lasts for 24 hours. The initial adult dose is 1 mg daily; a few patients may start with 0.25 mg or 0.5 mg.

Why are ACEIs recommended as first-line antihypertensive drugs?

Angiotensin-converting enzyme inhibitors are recommended as first-line antihypertensive drugs mainly for the following reasons.

① The long-term effect of angiotensin-converting enzyme inhibitors (ACEIs) on the renin-angiotensin-aldosterone (RAAS) system in tissues is a key mechanism for the long-term effectiveness of hypertension treatment.

② Changes in vascular structure and function (i.e., remodeling) during the pathogenesis of hypertension are one of the reasons for the maintenance or aggravation of hypertension. While some antihypertensive drugs can lower blood pressure, they cannot inhibit or reverse myocardial remodeling. ACEIs not only lower blood pressure but also reverse myocardial remodeling, reducing myocardial weight, improving cardiac function, improving and restoring myocardial geometry, and reversing existing fibrosis and thickening of the coronary artery wall within the myocardial layer, thus improving vascular compliance.
③ Hypertension is often complicated by hyperlipidemia, impaired glucose tolerance, and hyperinsulinemia, all of which are risk factors for cardiovascular disease. Therefore, when choosing antihypertensive drugs, those beneficial to lipid and glucose metabolism should be selected. ACEIs have no effect on lipid and glucose metabolism and may even be beneficial.

In summary, ACEIs have a significant antihypertensive effect on patients with primary and renal hypertension, and they are effective in lowering blood pressure in patients with different renin levels. Their antihypertensive effect is characterized by: rapid onset, strong effect, high efficacy, no increase in heart rate, no vacuum hypotension, improvement of myocardial function and renal blood flow, no water and sodium retention, no adverse effects on blood lipids and blood glucose, reversal of myocardial hypertrophy, and improved insulin sensitivity. Therefore, ACEIs can be used alone or in combination with other drugs for various types of mild to moderate hypertension in clinical practice.