Duration of angiotensin-converting enzyme inhibition: implications for tolerability

N H Murray1

  • 1Medical Research Department, ICI Pharmaceuticals, Macclesfield, UK.

Cardiology
|January 1, 1991
PubMed

Insights

Lisinopril, enalapril, and captopril show similar safety profiles in hypertension treatment. These angiotensin-converting enzyme inhibitors do not increase side-effect risks, even in long-term use.

Area of Science:

  • Pharmacology
  • Clinical Trials
  • Cardiovascular Medicine

Background:

  • Hypertension management often involves angiotensin-converting enzyme (ACE) inhibitors.
  • Comparative safety data for ACE inhibitors like lisinopril, enalapril, and captopril are crucial for clinical decision-making.

Purpose of the Study:

  • To compare the incidence of adverse events and withdrawals among lisinopril, enalapril, and captopril in patients with hypertension.
  • To assess the safety profiles of these ACE inhibitors across different patient demographics, including age.

Main Methods:

  • A multinational clinical-trial program involving patients with hypertension.
  • Comparative analysis of adverse events and treatment withdrawals between lisinopril and enalapril groups (n=318 vs. n=321).
  • Comparative analysis of adverse events and treatment withdrawals between lisinopril and captopril groups (n=230 vs. n=235).

Main Results:

  • The incidence of adverse events was similar for lisinopril versus enalapril (10.4% vs. 8.7%) and lisinopril versus captopril (11.7% vs. 11.9%).
  • Withdrawal rates were comparable across all three drug groups, with no significant differences observed.
  • The safety profiles were consistent across different age groups, and adverse events reflected known class-specific effects of ACE inhibitors.

Conclusions:

  • Lisinopril, enalapril, and captopril demonstrate comparable safety profiles in the management of hypertension.
  • Long-acting ACE inhibitors do not appear to confer additional side-effect risks.
  • The study supports the use of these ACE inhibitors with similar safety expectations.

Related Concept Videos

Time Course of Drug Effect01:14

Time Course of Drug Effect

The progression of a drug's impact can be analyzed by examining both the concentration-time course and the effect-time course. The concentration-time course is determined by the drug's half-life and is influenced by factors such as its pharmacokinetics, including absorption, distribution, metabolism, and elimination. The effect of the drug is often related to its concentration in the plasma and is calculated using the maximum drug effect and the plasma concentration that generates 50 percent of...
Antihypertensive Drugs: Angiotensin-Converting Enzyme Inhibitors01:30

Antihypertensive Drugs: Angiotensin-Converting Enzyme Inhibitors

Angiotensin-converting enzyme (ACE), a vital component of the renin-angiotensin-aldosterone system, is abundant in lung endothelial cells. ACE converts the inactive decapeptide, angiotensin I, into the active octapeptide, angiotensin II. This potent vasoconstrictor narrows blood vessels, increasing resistance to blood flow and elevating blood pressure. Angiotensin II also stimulates aldosterone production, encouraging kidney cells to reabsorb more sodium and water from urine, thereby increasing...
Antihypertensive Drugs: Angiotensin II Receptor Blockers01:30

Antihypertensive Drugs: Angiotensin II Receptor Blockers

In the renin-angiotensin-aldosterone system, a hormone called angiotensin II plays a crucial role. It binds to the AT1 receptors in vascular smooth muscles coupled with Gq proteins. The activation of these receptors activates an enzyme called phospholipase C, which releases two molecules: inositol trisphosphate and diacylglycerol. These molecules cause a chain reaction that leads to the phosphorylation of myosin light chains and promotes interaction between actin and myosin, leading to smooth...
Antihypertensive Drugs: Direct Renin Inhibitors01:25

Antihypertensive Drugs: Direct Renin Inhibitors

The renin-angiotensin-aldosterone system (RAAS) is an intricate physiological pathway involving numerous enzymes and hormones, including renin, angiotensin-converting enzyme (ACE), angiotensin I and II, and aldosterone. Imbalances within this system increase the production of angiotensin II and aldosterone. Increased angiotensin II levels promote vasoconstriction and blood pressure elevation. Concurrently, higher aldosterone levels stimulate sodium and water reabsorption in the kidneys,...
Heart Failure Drugs: Inhibitors of Renin-Angiotensin System01:26

Heart Failure Drugs: Inhibitors of Renin-Angiotensin System

The activation of the sympathetic nervous system and the renin-angiotensin-aldosterone system (RAAS) contributes to cardiac remodeling, and inhibiting the RAAS is a pharmacological target in heart failure management. As a result, neurohumoral modulation is a crucial treatment principle for managing heart failure. This approach involves using medications like ACE inhibitors (ACEIs), angiotensin receptor blockers (ARBs), β-blockers, mineralocorticoid receptor antagonists (MRAs), and neutral...
Pharmacokinetic–Pharmacodynamic Relationship: Influence of Elimination Half-Life on Effect Duration01:23

Pharmacokinetic–Pharmacodynamic Relationship: Influence of Elimination Half-Life on Effect Duration

Drug elimination from the body primarily occurs through metabolic and excretion pathways. Hepatic metabolism transforms lipophilic drugs into hydrophilic forms for excretion, typically via enzymatic processes classified as phase I (modification) and phase II (conjugation). Renal excretion eliminates drugs and metabolites through filtration and secretion in the kidneys. Impairment in liver or kidney function can hinder these processes, delaying drug clearance and extending the drug’s half-life.