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Urapidil, a dual-acting antihypertensive agent: Current usage considerations
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Insights
Many patients with hypertension struggle to reach target blood pressure (BP) levels. Alpha-blockers, like urapidil, are effective add-on therapies and offer additional benefits beyond BP control.
Area of Science:
- Pharmacology and Therapeutics
- Cardiovascular Medicine
- Nephrology
Background:
- A significant number of patients with hypertension do not achieve target blood pressure (BP) levels despite various treatments.
- Combination therapy with multiple antihypertensive agents is often necessary for effective BP management.
- Alpha-1-adrenoreceptor antagonists (alpha-blockers) are a class of antihypertensive drugs with BP-lowering effects comparable to other classes.
Purpose of the Study:
- To review the role of alpha-blockers in hypertension management.
- To highlight the specific properties and clinical applications of urapidil as an antihypertensive agent.
- To discuss urapidil's efficacy as second-line therapy and its potential benefits beyond BP reduction.
Main Methods:
- Review of existing studies on alpha-blockers in hypertension.
- Focus on urapidil's pharmacological profile, including its dual mechanism of action (alpha-blocking and central sympatholytic effects).
- Evaluation of clinical evidence for oral and intravenous urapidil in various settings.
Main Results:
- Alpha-blockers are effective as add-on therapy for inadequately controlled hypertension.
- Urapidil demonstrates efficacy and tolerability as a second-line treatment for hypertension.
- Urapidil may improve glucose and lipid metabolism and has applications in hypertensive crises, perioperative hypertension, pre-eclampsia, and potentially acute stroke.
Conclusions:
- Alpha-blockers, particularly urapidil, are valuable in managing hypertension, especially when BP targets are not met.
- Urapidil offers additional metabolic benefits and has a broad range of clinical uses, including emergency situations.
- The review underscores the importance of considering urapidil in diverse clinical scenarios for effective hypertension management.
Abstract:
Despite the availability of a wide range of effective blood pressure (BP)-lowering agents, a substantial proportion of patients with hypertension fail to achieve target BP levels. The majority of patients with hypertension need a combination of two or more drugs to achieve BP targets and choice of second-line or subsequent-line therapy is an important consideration in hypertension management. Alpha-1-adrenoreceptor antagonists (alpha-blockers) have a BP-lowering effect broadly similar to the other antihypertensive drug classes and are effective as add-on therapy in patients with inadequately controlled hypertension. Alpha-blockers may also have therapeutic benefits that go beyond BP control, including improvements in lipid profile and glucose metabolism, as well as reducing the symptoms of benign prostatic hyperplasia. Urapidil has an alpha-blocking effect but, unlike other alpha-blockers, also has a central sympatholytic effect mediated via stimulation of serotonin 5HT(1A) receptors in the central nervous system. Several studies have suggested that oral urapidil is effective and well tolerated when used as second-line therapy in patients with BP inadequately controlled with other agents. Urapidil has also been shown to improve glucose and lipid metabolism in hypertensive patients with concomitant diabetes and/or hyperlipidemia. Intravenous urapidil is effective in the treatment of hypertensive crises, perioperative hypertension, and pre-eclampsia and may have a potential role in the management of acute stroke. In this review, the use of alpha-blockers in hypertension is discussed, with particular focus on urapidil for the lowering of BP in a variety of clinical settings.
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