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Adrenergic Antagonists: Pharmacological Actions of ɑ-Receptor Blockers01:22

Adrenergic Antagonists: Pharmacological Actions of ɑ-Receptor Blockers

α-Adrenergic antagonists, known as α-blockers, exert their effects by inhibiting α-adrenoceptors, leading to specific physiological actions. α1-blockers and α2-blockers have distinct pharmacological actions and therapeutic applications.
α1-blockers: These drugs inhibit α1-adrenoceptors on smooth muscle cells, resulting in vasodilation. This vasodilation lowers blood pressure, making α1-blockers valuable in treating hypertension. Additionally, α1-blockers effectively address urinary obstruction...
Treatment for Pulmonary Arterial Hypertension: Phosphodiesterase Inhibitors01:28

Treatment for Pulmonary Arterial Hypertension: Phosphodiesterase Inhibitors

Phosphodiesterase 5 (PDE5) inhibitors are potent enzymes that function to hydrolyze cyclic nucleotides to their corresponding 5' monophosphates. Their unique biochemical properties have been applied in treating Pulmonary Arterial Hypertension (PAH).
Among the PDE5 inhibitors, sildenafil (Revatio) stands out as a competitive and selective inhibitor. It operates by elevating cellular levels of cGMP and augmenting signaling through the cGMP-PKG pathway, promoting vasodilation. Upon oral...
Adrenergic Antagonists: Chemistry and Classification of ɑ-Receptor Blockers01:17

Adrenergic Antagonists: Chemistry and Classification of ɑ-Receptor Blockers

Adrenergic antagonists, or sympatholytics, inhibit adrenoceptor activation driven by catecholamines or agonists. Based on their adrenoceptor specificity, adrenergic blockers can be categorized into two primary groups: α-adrenergic blockers (α-blockers) and β-adrenergic blockers (β-blockers). α-blockers interact with α1 and α2 subtypes of α-adrenoceptors.
Nonselective α-blockers: Nonselective α-blockers contain haloalkylamine or imidazoline moieties. Phenoxybenzamine, with a haloalkylamine...
Treatment for Pulmonary Arterial Hypertension: Prostacyclin Receptor Agonists01:23

Treatment for Pulmonary Arterial Hypertension: Prostacyclin Receptor Agonists

Prostacyclin receptor agonists are a class of therapeutic agents integral to managing pulmonary arterial hypertension (PAH). These drugs operate by mimicking the action of prostaglandin I2, or PGI2, a naturally occurring compound in the body.
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Treatment for Pulmonary Arterial Hypertension: Receptor Tyrosine Kinase Inhibitors and Calcium Channel Blockers01:26

Treatment for Pulmonary Arterial Hypertension: Receptor Tyrosine Kinase Inhibitors and Calcium Channel Blockers

Receptor tyrosine kinase inhibitors (TKIs) and calcium channel blockers (CCBs) are two critical categories of drugs employed in the treatment of pulmonary artery hypertension (PAH). PAH is a disease that causes high blood pressure in the pulmonary arteries, resulting in chest pain, fatigue, and shortness of breath.
TKIs, such as imatinib (Gleevec), are particularly effective in tackling the growth and mitogenic factors that become upregulated in PAH patients. These factors contribute to the...
Treatment for Pulmonary Arterial Hypertension: Endothelin Receptor Antagonists01:18

Treatment for Pulmonary Arterial Hypertension: Endothelin Receptor Antagonists

Endothelins (ETs) are potent vasoactive peptides critical in the human body's various physiological and pathological processes. One of the most promising therapeutic strategies for treating pulmonary arterial hypertension (PAH) involves counteracting the effects of these endothelins using a class of drugs known as endothelin receptor antagonists.
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A New Technique for Treating Low-risk Prostate Cancer—Super Active Surveillance
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5 Alpha Reductase Inhibitors (5ARIs) Monotherapy and Combinations: Current Role in Benign Prostatic Hyperplasia (BPH)

Christos Roidos1, Petros Sountoulides1, Konstantinos Papathanasiou1

  • 11st Department of Urology, School of Medicine, Faculty of Health Sciences, Aristotle University of Thessaloniki, 541 24 Thessaloniki, Greece.

Medicina (Kaunas, Lithuania)
|May 27, 2026
PubMed
Summary

5α-reductase inhibitors (5-ARIs) effectively manage benign prostatic hyperplasia (BPH) by reducing prostate size and preventing progression. Combination therapy offers superior outcomes, especially for high-risk patients.

Keywords:
5-a reductase inhibitorsBPH progressionbenign prostatic hyperplasiacombination therapydutasteridefinasterideα-blockers

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Ultrasonography of the Adult Male Urinary Tract for Urinary Functional Testing
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Ultrasonography of the Adult Male Urinary Tract for Urinary Functional Testing

Published on: August 14, 2019

Area of Science:

  • Urology
  • Pharmacology

Background:

  • Benign prostatic hyperplasia (BPH) is an androgen-dependent condition driven by dihydrotestosterone (DHT).
  • 5α-reductase inhibitors (5-ARIs) target the DHT pathway, offering disease-modifying effects for BPH management.

Purpose of the Study:

  • To review the efficacy, timing, and safety of 5-ARIs in managing lower urinary tract symptoms (LUTS) due to BPH.
  • To evaluate the benefits of combination therapy with α-blockers.

Main Methods:

  • Narrative review of randomized trials, meta-analyses, and observational studies.
  • Analysis of data on prostate volume reduction, PSA levels, and clinical outcomes.

Main Results:

  • 5-ARIs reduce prostate volume (18-28%) and PSA (~50%) within 6-12 months.
  • Landmark trials show 5-ARIs significantly reduce acute urinary retention and BPH-related surgery (>50% RR reduction).
  • Combination therapy with α-blockers improves symptom control and prevents progression, especially in men with larger prostates or higher PSA levels.

Conclusions:

  • 5-ARIs are crucial for BPH management, providing sustained benefits and preventing disease progression.
  • Optimal outcomes are achieved through appropriate patient selection, early treatment for high-risk individuals, and individualized long-term strategies.
  • Emerging data suggests a possible association between 5-ARIs and depression, alongside mainly sexual adverse events.