What is Lisinopril (Angiotensin-Converting Enzyme (ACE) inhibitor) and its mechanism of action?

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From the Guidelines

Lisinopril is a medication that belongs to a class of drugs called angiotensin-converting enzyme (ACE) inhibitors, commonly prescribed to treat high blood pressure (hypertension), heart failure, and to improve survival after heart attacks, as recommended by the 2017 ACC/AHA/HFSA focused update 1.

How Lisinopril Works

Lisinopril works by blocking the action of an enzyme in your body that causes blood vessels to tighten. By inhibiting this enzyme, lisinopril allows blood vessels to relax and widen, which lowers blood pressure and increases blood and oxygen supply to the heart. This mechanism is supported by studies such as the Assessment of Treatment With Lisinopril and Survival (ATLAS) trial, which showed that mortality was significantly lower in patients with heart failure who received a high dose of lisinopril compared to those treated with a low dose 1.

Dosage and Administration

The typical starting dose for hypertension is 10 mg once daily, which may be adjusted based on blood pressure response, with a usual maintenance dose of 20-40 mg daily. For heart failure, treatment usually begins with 5 mg daily, potentially increasing to 40 mg daily. Lisinopril should be taken at the same time each day, with or without food.

Side Effects and Precautions

Common side effects include dizziness, headache, dry cough, and increased potassium levels. It's essential to know that ACE inhibitors like lisinopril can cause serious swelling of the face, lips, tongue, and throat, which requires immediate medical attention. Additionally, pregnant women should not take lisinopril as it can harm the developing fetus, particularly in the second and third trimesters.

Benefits and Recommendations

The use of ACE inhibitors, including lisinopril, is beneficial for patients with prior or current symptoms of chronic heart failure with reduced ejection fraction (HFrEF) to reduce morbidity and mortality, as recommended by the 2017 ACC/AHA/HFSA focused update 1. Lisinopril has been shown to reduce morbidity and mortality in patients with HFrEF, and its use is strongly advised for all classes of HFrEF, especially in patients who are intolerant to angiotensin receptor-neprilysin inhibitors (ARNI) or angiotensin receptor blockers (ARB).

From the FDA Drug Label

CLINICAL PHARMACOLOGY 12. 1 Mechanism of Action Lisinopril inhibits angiotensin-converting enzyme (ACE) in human subjects and animals. ACE is a peptidyl dipeptidase that catalyzes the conversion of angiotensin I to the vasoconstrictor substance, angiotensin II. The beneficial effects of lisinopril in hypertension and heart failure appear to result primarily from suppression of the renin-angiotensin-aldosterone system.

Lisinopril is an angiotensin-converting enzyme (ACE) inhibitor. It works by:

  • Inhibiting the conversion of angiotensin I to angiotensin II, a potent vasoconstrictor
  • Suppressing the renin-angiotensin-aldosterone system, which leads to decreased vasopressor activity and aldosterone secretion
  • Resulting in a decrease in blood pressure, with effects seen as early as 1 hour after administration and peak effects at 6 hours 2 2

From the Research

What is Lisinopril

  • Lisinopril is an orally active angiotensin-converting enzyme (ACE) inhibitor 3, 4, 5, 6
  • It is used to lower blood pressure in patients with essential hypertension and to treat congestive heart failure 3, 4, 5, 6

How Does Lisinopril Work

  • Lisinopril inhibits ACE activity, reducing plasma angiotensin II and aldosterone, and increasing plasma renin activity 5
  • It produces a smooth, gradual blood pressure reduction in hypertensive patients without affecting heart rate or cardiovascular reflexes 5
  • The antihypertensive effect of lisinopril begins within 2 hours, peaks around 6 hours, and lasts for at least 24 hours 5

Efficacy and Safety of Lisinopril

  • Lisinopril is effective in lowering blood pressure in patients with essential hypertension, with a comparable efficacy to other antihypertensive agents such as hydrochlorothiazide, nifedipine, and beta-blocking agents 3, 4, 5, 6
  • It is also effective in treating congestive heart failure, with hemodynamic effects comparable to those of captopril 3, 4, 6
  • Lisinopril is generally well-tolerated, with common side effects including cough, dizziness, and rash 4, 6
  • However, recent studies suggest that angiotensin receptor blockers (ARBs) may be associated with fewer adverse events and similar efficacy to ACE inhibitors, including lisinopril, in the treatment of hypertension 7

Professional Medical Disclaimer

This information is intended for healthcare professionals. Any medical decision-making should rely on clinical judgment and independently verified information. The content provided herein does not replace professional discretion and should be considered supplementary to established clinical guidelines. Healthcare providers should verify all information against primary literature and current practice standards before application in patient care. Dr.Oracle assumes no liability for clinical decisions based on this content.

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