可溶性关酸环酶激活剂用于治疗良性前列腺增生和相关的LUTS
A J Kanai1, K-E Andersson2, L A Birder1
1University of Pittsburgh, Department of Medicine, Renal-Electrolyte Division, USA.
Continence (Amsterdam, Netherlands)
|June 30, 2023
概括
溶性甘酸环酶 (sGC) 激活剂在治疗良性前列腺增生症 (BPH) 中表现有前途. 奇纳西瓜特可以通过即使在氧化应激下也发挥作用来克服塔达拉菲尔的折射性,从而有可能改善下泌尿道症状.
科学领域:
- 泌尿器科 泌尿器科 泌尿器科 泌尿器科
- 药理学 药理学是指药理学的学科.
- 细胞信号传输 细胞信号传输
背景情况:
- 良性前列腺增生 (BPH) 影响大约75%的男性在80岁时,导致膀外流阻塞 (BOO) 和下泌尿道症状 (LUTS).
- 目前的治疗方法包括α阻断剂,5α减小酶抑制剂和tadalafil (一种PDE5抑制剂).
- 塔达拉菲尔的疗效表明氧化 (NO) 激活可溶性酸环酶 (sGC) 产生循环氨酸单酸盐 (cGMP),这使光滑肌肉放松,并具有抗纤维作用.
研究的目的:
- 审查使用sGC激活剂用于BPH,阻塞和纤维化的机制概念和临床影响.
- 讨论超越BPH现有治疗方法的新型治疗策略.
- 探索sGC激活剂在克服治疗折射性方面的潜力.
主要方法:
- 来自国际节制协会 (ICS) 2021年研讨会的演讲摘要.
- 在BPH的背景下讨论氧化-sGC-cGMP通路.
- 将PDE5抑制剂与新型sGC激活剂进行比较.
主要成果:
- 患者对塔达拉菲尔的折射性可能源于氧化应激失活sGC.
- 辛纳西瓜特是一种sGC激活剂,即使sGC被氧化时也能起作用,这表明它比PDE5抑制剂优越.
- 与减少活性氧物种的药物进行联合治疗的潜力.
结论:
- sGC激活剂代表了BPH和相关疾病的有希望的治疗途径.
- 奇纳西瓜特比PDE5抑制剂具有潜在的优势,特别是在氧化应激的情况下.
- 对组合疗法的进一步研究可能会提高BPH的治疗疗效.
相关概念视频
01:23Treatment for Pulmonary Arterial Hypertension: Prostacyclin Receptor Agonists
218
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.
These agonists bind to the IPR receptor situated on the plasma membrane of the pulmonary artery smooth muscle cells. This binding triggers a cascade of reactions known as the GS-AC-cAMP-PKA pathway. This pathway results in the relaxation of smooth muscle...
These agonists bind to the IPR receptor situated on the plasma membrane of the pulmonary artery smooth muscle cells. This binding triggers a cascade of reactions known as the GS-AC-cAMP-PKA pathway. This pathway results in the relaxation of smooth muscle...
218
01:27Transducer Mechanism: Enzyme-Linked Receptors
2.5K
Enzyme-linked receptors are cell-surface receptors acting as an enzyme or associating with an enzyme intracellularly. They make excellent drug targets. Drugs can bind to the extracellular ligand-binding domain or directly affect their enzymatic domain and alter their activity.
Major types that are helpful drug targets include:
Major types that are helpful drug targets include:
2.5K
01:28Treatment for Pulmonary Arterial Hypertension: Phosphodiesterase Inhibitors
194
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...
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...
194
01:23Antihypertensive Drugs: Vasodilators
576
Vasodilators, primarily affecting the smooth muscles within arterial and venous walls, are commonly used for hypertension treatment. Medications such as minoxidil and hydralazine primarily target arteries and arterioles, while sodium nitroprusside acts on arterioles and venules. Minoxidil, functioning as a prodrug, is metabolized by hepatic sulfotransferase into its active form, minoxidil sulfate, after oral administration. This metabolite binds to the sulfonylurea receptor (SUR) component of...
576
01:18Treatment for Pulmonary Arterial Hypertension: Endothelin Receptor Antagonists
202
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.
ETs are synthesized through a complex sequence of enzymatic steps, primarily involving an enzyme referred to as endothelin-converting enzyme...
ETs are synthesized through a complex sequence of enzymatic steps, primarily involving an enzyme referred to as endothelin-converting enzyme...
202
01:19Antiasthma Drugs: Leukotriene Modifiers
369
Leukotriene modifiers, or cysteinyl leukotriene receptor antagonists, are medications used to manage chronic asthma. These agents target specific inflammatory mediators produced during arachidonic acid metabolism, an essential process in generating inflammation in the body.
Leukotriene modifiers work through two distinct mechanisms:
Leukotriene modifiers work through two distinct mechanisms:
369