Absorption, tissue disposition, and excretion of fasudil hydrochloride, a RHO kinase inhibitor, in rats and dogs

Liu, Wenjun; Gao, Jing; Yi, Xin; Li, Yazhuo; Zeng, Yong

doi:10.1002/bdd.2231

Cited by 6 publications

(1 citation statement)

References 24 publications

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“…Butylphthalide, as a new synthetic drug, has been proved to improve vascular function and can be used in the treatment of SAH complicated with CVS. 4 Fasudil can dilate blood vessels and improve spasticity, 5 showing an inhibitory effect on the condition of CVS. However, few studies have been carried out on butylphthalide combined with fasudil in the treatment of SAH complicated with CVS.…”

Section: Introductionmentioning

confidence: 99%

Effects of Butylphthalide Combined with Fasudil on Inflammatory Factors, Cognitive Function and Vascular Endothelial Function in Patients with Subarachnoid Hemorrhage Complicated with Cerebral Vasospasm

Tian,

Gan,

Song

et al. 2023

Pak J Med Sci

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Objective: To investigate the effect of butylphthalide combined with fasudil in the treatment of subarachnoid hemorrhage (SAH) with cerebral vasospasm (CVS) on inflammatory factors, cognitive function and vascular endothelial function. Methods: It is a retrospective study in which a total of 104 patients with SAH with CVS admitted to Baoding First Central Hospital from July 2020 to February 2022 were selected and randomly divided into two groups by drawing lots. Patients in the control group were treated with basic symptomatic treatment, while those in the observation group were treated with butylphthalide soft capsule combined with fasudil hydrochloride injection on the basis of the control group. Before and after treatment, serum neuron specific enolase (NSE), tumor necrosis factor-α(TNF-α), interleukin-8(IL-8), hypersensitive C-reactive protein (CRP), Birmingham Cognitive Screen test (BCoS) score, serum soluble intercellular adhesion molecule-1(ICAM-1), serum endothelin-1(ET-1), vascular endothelial growth factor (VEGF) levels, and endothelium-dependent vasodilation function (FMD) in the two groups were compared. Results: After treatment, the expression levels of NSE, TNF-α, IL-8 and CRP in the two groups were significantly decreased, and the expression levels of all indicators in the observation group were lower than that in the control group (p<0.05). After treatment, the scores of orientations, attention, memory, language, practice and action in the two groups were significantly increased, and the scores of all dimensions in the observation group were higher than those in the control group (p<0.05). After treatment, S-ICAM-1, ET-1, VEGF, FMD decreased in both groups, and all indicators of the observation group were lower than those of the control group, with statistically significant differences (p<0.05). Conclusion: Butylphthalide combined with fasudil therapy was found as effective in reducing inflammatory factors, ameliorating cognitive function and vascular endothelial function in patients with subarachnoid hemorrhage complicated with cerebral vasospasm. doi: https://doi.org/10.12669/pjms.39.6.6768 How to cite this: Tian N, Gan N, Song C, Su F, Xie J, Zhang Y. Effects of Butylphthalide Combined with Fasudil on Inflammatory Factors, Cognitive Function and Vascular Endothelial Function in Patients with Subarachnoid Hemorrhage Complicated with Cerebral Vasospasm. Pak J Med Sci. 2023;39(6):---------. doi: https://doi.org/10.12669/pjms.39.6.6768 This is an Open Access article distributed under the terms of the Creative Commons Attribution License (http://creativecommons.org/licenses/by/3.0), which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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Section: Introductionmentioning

confidence: 99%

Effects of Butylphthalide Combined with Fasudil on Inflammatory Factors, Cognitive Function and Vascular Endothelial Function in Patients with Subarachnoid Hemorrhage Complicated with Cerebral Vasospasm

Tian,

Gan,

Song

et al. 2023

Pak J Med Sci

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Pharmaceuticals targeting signaling pathways of endometriosis as potential new medical treatment: A review

Hung

Zhang

Tan

et al. 2021

Medicinal Research Reviews

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Endometriosis (EM) is defined as endometrial tissues found outside the uterus. Growth and development of endometriotic cells in ectopic sites can be promoted via multiple pathways, including MAPK/MEK/ERK, PI3K/Akt/mTOR, NF‐κB, Rho/ROCK, reactive oxidative stress, tumor necrosis factor, transforming growth factor‐β, Wnt/β‐catenin, vascular endothelial growth factor, estrogen, and cytokines. The underlying pathophysiological mechanisms include proliferation, apoptosis, autophagy, migration, invasion, fibrosis, angiogenesis, oxidative stress, inflammation, and immune escape. Current medical treatments for EM are mainly hormonal and symptomatic, and thus the development of new, effective, and safe pharmaceuticals targeting specific molecular and signaling pathways is needed. Here, we systematically reviewed the literature focused on pharmaceuticals that specifically target the molecular and signaling pathways involved in the pathophysiology of EM. Potential drug targets, their upstream and downstream molecules with key aberrant signaling, and the regulatory mechanisms promoting the growth and development of endometriotic cells and tissues were discussed. Hormonal pharmaceuticals, including melatonin, exerts proapoptotic via regulating matrix metallopeptidase activity while nonhormonal pharmaceutical sorafenib exerts antiproliferative effect via MAPK/ERK pathway and antiangiogenesis activity via VEGF/VEGFR pathway. N‐acetyl cysteine, curcumin, and ginsenoside exert antioxidant and anti‐inflammatory effects via radical scavenging activity. Natural products have high efficacy with minimal side effects; for example, resveratrol and epigallocatechin gallate have multiple targets and provide synergistic efficacy to resolve the complexity of the pathophysiology of EM, showing promising efficacy in treating EM. Although new medical treatments are currently being developed, more detailed pharmacological studies and large sample size clinical trials are needed to confirm the efficacy and safety of these treatments in the near future.

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Beyond nimodipine: advanced neuroprotection strategies for aneurysmal subarachnoid hemorrhage vasospasm and delayed cerebral ischemia

Luzzi,

Bektaşoğlu,

Doğruel

et al. 2024

Neurosurg Rev

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The clinical management of aneurysmal subarachnoid hemorrhage (SAH)-associated vasospasm remains a challenge in neurosurgical practice, with its prevention and treatment having a major impact on neurological outcome. While considered a mainstay, nimodipine is burdened by some non-negligible limitations that make it still a suboptimal candidate of pharmacotherapy for SAH. This narrative review aims to provide an update on the pharmacodynamics, pharmacokinetics, overall evidence, and strength of recommendation of nimodipine alternative drugs for aneurysmal SAH-associated vasospasm and delayed cerebral ischemia. A PRISMA literature search was performed in the PubMed/Medline, Web of Science, ClinicalTrials.gov, and PubChem databases using a combination of the MeSH terms “medical therapy,” “management,” “cerebral vasospasm,” “subarachnoid hemorrhage,” and “delayed cerebral ischemia.” Collected articles were reviewed for typology and relevance prior to final inclusion. A total of 346 articles were initially collected. The identification, screening, eligibility, and inclusion process resulted in the selection of 59 studies. Nicardipine and cilostazol, which have longer half-lives than nimodipine, had robust evidence of efficacy and safety. Eicosapentaenoic acid, dapsone and clazosentan showed a good balance between effectiveness and favorable pharmacokinetics. Combinations between different drug classes have been studied to a very limited extent. Nicardipine, cilostazol, Rho-kinase inhibitors, and clazosentan proved their better pharmacokinetic profiles compared with nimodipine without prejudice with effective and safe neuroprotective role. However, the number of trials conducted is significantly lower than for nimodipine. Aneurysmal SAH-associated vasospasm remains an area of ongoing preclinical and clinical research where the search for new drugs or associations is critical.

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Absorption, tissue disposition, and excretion of fasudil hydrochloride, a RHO kinase inhibitor, in rats and dogs

Cited by 6 publications

References 24 publications

Effects of Butylphthalide Combined with Fasudil on Inflammatory Factors, Cognitive Function and Vascular Endothelial Function in Patients with Subarachnoid Hemorrhage Complicated with Cerebral Vasospasm

Effects of Butylphthalide Combined with Fasudil on Inflammatory Factors, Cognitive Function and Vascular Endothelial Function in Patients with Subarachnoid Hemorrhage Complicated with Cerebral Vasospasm

Pharmaceuticals targeting signaling pathways of endometriosis as potential new medical treatment: A review

Beyond nimodipine: advanced neuroprotection strategies for aneurysmal subarachnoid hemorrhage vasospasm and delayed cerebral ischemia

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