Role of α1‐blockers in the current management of hypertension

Abstract

There is emerging evidence that α1‐blockers can be safely used in the treatment of hypertension. These drugs can be used in almost all hypertensive patients for blood pressure control. However, there are several special indications. Benign prostatic hyperplasia is a compelling indication of α1‐blockers, because of the dual treatment effect on both high blood pressure and lower urinary tract symptoms. Many patients with resistant hypertension would require α1‐blockers as add‐on therapy. Primary aldosteronism screen is a rapidly increasing clinical demand in the management of hypertension, where α1‐blockers are useful for blood pressure control in the preparation for the measurement of plasma aldosterone and renin. Nonetheless, α1‐blockers have to be used under several considerations. Among the currently available agents, only long‐acting α1‐blockers, such as doxazosin gastrointestinal therapeutic system 4–8 mg daily and terazosin 2–4 mg daily, should be chosen. Orthostatic hypotension is a concern with the use of α1‐blockers especially in the elderly, and requires careful initial bedtime dosing and avoiding overdosing. Fluid retention is potentially also a concern, which may be overcome by combining an α1‐blocker with a diuretic.

2023 ESH Guidelines for the management of arterial hypertension The Task Force for the management of arterial hypertension of the European Society of Hypertension

“…treatment of benign prostatic hyperplasia). Orthostatic hypotension and fluid retention may be a concern with the use of alpha-1 blockers, especially in the older patients [601]. In a real-life study on older patients, administration of alpha-1 blockers in newly treated old hypertensive patients was followed by a significant increase of hospitalization for hip fracture over the following month, presumably as a result of orthostatic BP reductions and injurious falls [602].…”

Aerosolized ⍺1adrenoreceptor antagonism does not affect experimentally induced lung fibrosis in animal models

“…Terazosin is a specific ⍺ 1 -AR antagonist [50] that has been approved for use for decades in the treatment of benign prostatic hyperplasia and hypertension, and has a well-established safety profile [51, 52]. Its long half-life makes it well suited for once daily administration [53].…”

“…In contrast, systemic administration of terazosin is more likely to achieve therapeutic levels for ⍺1-AR antagonism in fibrotic foci. Created with BioRender.com Terazosin is a specific ⍺1-AR antagonist [50] that has been approved for use for decades in the treatment of benign prostatic hyperplasia and hypertension, and has a well-established safety profile [51,52]. Its long half-life makes it well suited for once daily administration [53].…”

Trends in exercise for hypertension: a bibliometric analysis

“…Adrenergic blockade is one of the most important drug treatments for hypertension and heart disease. It can inhibit the effects of adrenaline on the body via β-blockers or α -blockers, which slow the heart rate, dilate blood vessels, and lower blood pressure ( 39 , 40 ). Combined with exercise, adrenergic blocking drugs can synergistically control hypertension.…”