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Opinions of pharmacists in Turkiye on drug shortages and effects on treatment 土耳其药剂师对药品短缺及其对治疗影响的看法
Q4 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2024-02-06 DOI: 10.52794/hujpharm.1306922
Muammer Çalikuşu, Gülbin Özçelikay
Abstract Drug shortage is defined as a lack of supply of a medicinal product that affects the patient's ability to access the necessary treatment when they need it. The origins of this deficiency are complex and varied, and both supply and demand can cause the problem. Drug shortages affect every stakeholder of the health system, and collaborative efforts are needed to manage and reduce deficiencies. This study determined the reasons for the drug shortages, their incidence, the most affected drug groups, the precautions taken, and their effects on treatment. The research is in a survey model and quantitative type. A questionnaire form prepared by the researchers was used as a data collection tool in the study. The questionnaire form was sent to community and hospital pharmacists via the Internet. Volunteers were asked to participate. 107 people, including 90 community pharmacists and 17 hospital pharmacists, participated in the research. In our study, the participants listed the essential causes of drug shortage as problems in the supply of raw materials (78.5%), production problems (53.3%), and increased demand for some drugs (29%). Early warning systems should be developed and integrated into relevant processes, ensuring a consistent supply of drugs to prevent drug shortages. Ensuring this structure requires the cooperation of all professionals, institutions, and organizations involved in the national and international health system.
摘要 药品短缺是指药品供应不足,影响了患者在需要时获得必要治疗的能力。造成药品短缺的原因复杂多样,供需双方都有可能造成这一问题。药品短缺会影响到医疗系统中的每一个利益相关者,因此需要共同努力来管理和减少药品短缺。本研究确定了药物短缺的原因、发生率、受影响最大的药物类别、采取的预防措施及其对治疗的影响。研究采用调查模式和定量类型。研究人员准备了一份调查问卷作为数据收集工具。问卷通过互联网发送给社区和医院药剂师。要求志愿者参与。共有 107 人参与了研究,其中包括 90 名社区药剂师和 17 名医院药剂师。在我们的研究中,参与者列出了药品短缺的主要原因,包括原材料供应问题(78.5%)、生产问题(53.3%)和部分药品需求增加(29%)。应开发预警系统,并将其纳入相关流程,确保持续供应药品,防止药品短缺。确保这一结构需要国家和国际卫生系统的所有专业人员、机构和组织的合作。
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引用次数: 0
THE INVESTIGATION OF THE RELATIONSHIP BETWEEN PHARMACEUTICAL CONSUMPTION AND HEALTH STATUS 药品消费与健康状况关系的调查
Q4 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2023-11-14 DOI: 10.52794/hujpharm.1243959
Gökçen ÖZLER, İsmail AĞIRBAŞ
It is thought that it is important to reveal the contribution of pharmaceutical consumption to health outcomes because the share of pharmaceutical expenditures in health expenditures is quite high and the debate about controlling healthcare costs. The study aims to examine the relationship between pharmaceutical consumption and the health status of EFPIA member countries with canonical correlation analysis. It was found that the health status of the EFPIA member countries and their pharmaceutical consumption were strongly correlated (rc=75.9). According to canonical cross loadings, the variable of life expectancy at birth (0.846), which has the strongest relationship with its own set, also establishes the strongest relationship with pharmaceutical consumption (0.642). The pharmaceutical consumption dataset remarkably correlates with antidepressant use and lipid use, respectively. According to canonical cross loadings, antidepressant use, which had the strongest association with its own set, had the strongest association with the health status dataset (0.592). This research provides evidence that pharmaceutical consumption and the health status of EFPIA member countries are positive associated. It is thought that the potential of pharmaceutical-related interventions can be exploited as a way to improve the health status.
由于医药支出在卫生支出中所占的份额相当高,以及关于控制卫生保健费用的争论,人们认为揭示药品消费对卫生结果的贡献是很重要的。本研究旨在运用典型相关分析的方法,探讨EFPIA成员国药品消费与健康状况之间的关系。结果发现,EFPIA成员国的健康状况与其药品消费呈强相关(rc=75.9)。根据典型交叉加载,出生时预期寿命变量(0.846)与自身集的关系最强,与药品消费的关系也最强(0.642)。药物消费数据集分别与抗抑郁药使用和脂质使用显著相关。根据规范交叉加载,抗抑郁药的使用与其自身的数据集有最强的关联,与健康状态数据集有最强的关联(0.592)。本研究提供了证据,证明药品消费与EFPIA成员国的健康状况呈正相关。人们认为,与药物有关的干预措施的潜力可以作为改善健康状况的一种方式加以利用。
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引用次数: 0
Netrin-1 ve Reseptörlerinin Çeşitli Kanserlerdeki Rolü Netrin-1 及其受体在各种癌症中的作用
Q4 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2023-11-13 DOI: 10.52794/hujpharm.1327025
Aymelek GÖNENÇ, Hülya KARA
ABSTRACT Netrin-1 is a laminin-like protein that is secreted. It plays a role in the development of the nervous system and is also involved in processes such as cell migration, proliferation, angiogenesis, differentiation, apoptosis, metastasis, and invasion. DCC, neogenin, and UNC5 receptor families form the main receptors of netrin-1. These receptors have a dual role depending on the presence or absence of netrin-1. Netrin-1 influences carcinogenesis through signaling pathways such as PI3K/AKT, ERK/MAPK, Notch, and NF-kB. Netrin-1 receptor interactions are effective in cancer cell viability and carcinogenesis mechanisms. Overall, overexpression of netrin-1 and loss of its receptors promote carcinogenesis. Netrin-1 is involved in apoptosis through different receptors. Changes in the expression of DCC and UNC5H receptors affect cancer cell growth and metastasis. Loss of expression in dependent receptors is observed in advanced stages of various tumors. Neogenin is associated with migration and metastasis in tumors. Studies have shown that netrin-1 influences tumor development in various cancers such as gastric cancer, pancreatic ductal adenocarcinoma, colorectal cancer, and glioblastoma. Overexpression of netrin-1 is associated with poor prognosis and decreased overall survival. Netrin-1 levels are reported to be higher in patient groups compared to healthy control groups and decrease with chemotherapy. The mechanism of netrin-1 and its receptors in tumor development is not clear due to their different effects. This article summarizes research findings presenting the role and position of netrin-1 in various cancers.
摘要# x0D;Netrin-1是一种分泌的层粘连蛋白样蛋白。它在神经系统发育中起重要作用,并参与细胞迁移、增殖、血管生成、分化、凋亡、转移和侵袭等过程。DCC、neogenin和UNC5受体家族是netrin-1的主要受体。这些受体具有双重作用,取决于netrin-1的存在与否。Netrin-1通过PI3K/AKT、ERK/MAPK、Notch和NF-kB等信号通路影响癌变。Netrin-1受体相互作用在癌细胞生存和癌变机制中是有效的。总的来说,netrin-1的过度表达和其受体的缺失促进了癌变。Netrin-1通过不同的受体参与细胞凋亡。DCC和UNC5H受体的表达变化影响癌细胞的生长和转移。依赖性受体的表达缺失在各种肿瘤的晚期都可以观察到。Neogenin与肿瘤的迁移和转移有关。研究表明,netrin-1影响各种癌症的肿瘤发展,如胃癌、胰腺导管腺癌、结直肠癌和胶质母细胞瘤。netrin-1过表达与预后不良和总生存率降低有关。据报道,患者组的Netrin-1水平高于健康对照组,并随化疗而降低。netrin-1及其受体在肿瘤发生中的作用机制不同,目前尚不清楚。本文综述了netrin-1在各种癌症中的作用和地位的研究成果。
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 Netrin-1 is a laminin-like protein that is secreted. It plays a role in the development of the nervous system and is also involved in processes such as cell migration, proliferation, angiogenesis, differentiation, apoptosis, metastasis, and invasion. DCC, neogenin, and UNC5 receptor families form the main receptors of netrin-1. These receptors have a dual role depending on the presence or absence of netrin-1. Netrin-1 influences carcinogenesis through signaling pathways such as PI3K/AKT, ERK/MAPK, Notch, and NF-kB. Netrin-1 receptor interactions are effective in cancer cell viability and carcinogenesis mechanisms. Overall, overexpression of netrin-1 and loss of its receptors promote carcinogenesis. Netrin-1 is involved in apoptosis through different receptors. Changes in the expression of DCC and UNC5H receptors affect cancer cell growth and metastasis. Loss of expression in dependent receptors is observed in advanced stages of various tumors. Neogenin is associated with migration and metastasis in tumors. Studies have shown that netrin-1 influences tumor development in various cancers such as gastric cancer, pancreatic ductal adenocarcinoma, colorectal cancer, and glioblastoma. Overexpression of netrin-1 is associated with poor prognosis and decreased overall survival. Netrin-1 levels are reported to be higher in patient groups compared to healthy control groups and decrease with chemotherapy. The mechanism of netrin-1 and its receptors in tumor development is not clear due to their different effects. This article summarizes research findings presenting the role and position of netrin-1 in various cancers.","PeriodicalId":39138,"journal":{"name":"Hacettepe University Journal of the Faculty of Pharmacy","volume":"68 7","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-11-13","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"136281851","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Development and evaluation of buspirone hyrdochloride loaded transdermal patch using natural polymers 天然聚合物负载盐酸丁螺环酮透皮贴剂的研制与评价
Q4 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2023-11-07 DOI: 10.52794/hujpharm.1214109
Meshva PATEL, Mehul PATEL, Komal PARMAR, Tejal SONİ, Dr. Bhanubhai SUHAGİA
The purpose of this present study was to design and develop a Buspirone hydrochloride loaded matrix type transdermal drug delivery system (TDDS) with four natural gum polymers such as Guar gum, Gellan gum, Xanthan gum, Karaya gum. A total of twelve batch of matrix patches were formulated with above stated polymers and other excipient like Glycerin, Propylene glycol (PG), Polyethylene glycol (PEG) as plasticizer. These all batches were characterized by evaluation parameters which including drug content, flatness, thickness, uniformity of weight, folding endurance, moisture content, moisture uptake and to determine the amount of Buspirone hydrochloride present in the matrix of patches in vitro dissolution study of all twelve formulations were performed. Fourier transform infrared (FTIR) technique and Differential Scanning Colorimetry (DSC) carried out to determine interaction between Buspirone HCl and excipients which are present in patch. Permeation study of patch of Buspirone HCl was performed in Franz's diffusion cell to evaluate In-vitro skin permeation and it was found that batch G3 shows 98.89% permeability. After evaluating all batches and based on results which are obtained characterization and In-Vitro dissolution it was concluded that patches containing natural polymers are not showing any interaction and better release study.
以瓜尔胶、结冷胶、黄原胶、卡拉亚胶等4种天然胶为原料,设计并制备了一种载药基质型盐酸丁螺环酮透皮给药系统。以上述聚合物和其它赋形剂如甘油、丙二醇(PG)、聚乙二醇(PEG)作为增塑剂,共配制了12批基质贴剂。采用药物含量、平整度、厚度、重量均匀性、折叠耐力、水分含量、吸湿率等评价参数对12个剂型进行表征,并测定膜片基质中盐酸丁螺环酮的体外溶出度。采用傅里叶变换红外(FTIR)技术和差示扫描比色法(DSC)测定了盐酸丁螺环酮与贴剂中辅料的相互作用。采用Franz扩散池对盐酸丁螺环酮贴剂进行透性研究,评价其体外皮肤透性,发现G3批次的透性为98.89%。在评估了所有批次并根据获得的表征和体外溶出度的结果得出结论,含有天然聚合物的贴剂没有表现出任何相互作用和更好的释放研究。
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引用次数: 0
Synthesis and Investigation of Cytotoxicity in Different Cell Lines of Novel Hydroxypyranones 新型羟基吡喃酮的合成及其对不同细胞系细胞毒性的研究
Q4 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2023-11-02 DOI: 10.52794/hujpharm.1374319
Pelin Nur ÜÇKAN, Gülşah KARAKAYA, Beyza DÜZLEYEN, Canan SEVİMLİ GÜR, Mutlu AYTEMİR
Mannich bases synthesized from kojic acid have been determined in extensive studies conducted by our study group that they have a wide variety of biological activities. In this study, new anticancer-active compounds were synthesized from compounds with high anticancer activity. The compounds' structures were identified through the utilization of spectroscopic methods and elemental analyses. The cytotoxicity screening of the compounds were done by MTT assay on different human cancer cell lines. Compound 1 bearing iodomethyl moiety, showed remarkable cytotoxicity with IC50 values in the range of 8.11 and 21.24 µg/mL. The IC50 value on Vero (African green monkey kidney epithelial) is over 100 µg/mL which means low cytotoxicity against healthy cells. Compared to this, SK-MEL cells have 12 times less IC50 value, with a therapeutic index over 12. The closest cytotoxic effectivity to KOJI MG84 which is previously reported as a cytotoxic agent, is observed on the SK-MEL cell line in compound 1, with 4 times less cytotoxic activity.
由曲酸合成的曼尼希碱在我们研究组进行的广泛研究中已经确定它们具有广泛的生物活性。& # x0D;本研究从具有高抗癌活性的化合物中合成了新的抗癌活性化合物。利用光谱学方法和元素分析鉴定了化合物的结构。用MTT法对不同的人癌细胞进行了细胞毒性筛选。 化合物1具有显著的细胞毒性,IC50值在8.11 ~ 21.24µg/mL之间。对Vero(非洲绿猴肾上皮)的IC50值大于100µg/mL,这意味着对健康细胞的细胞毒性低。与此相比,SK-MEL细胞的IC50值降低了12倍,治疗指数超过12。在SK-MEL细胞系上,化合物1的细胞毒活性比先前报道的细胞毒剂KOJI MG84的细胞毒活性低4倍,与KOJI MG84最接近。
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 In this study, new anticancer-active compounds were synthesized from compounds with high anticancer activity. The compounds' structures were identified through the utilization of spectroscopic methods and elemental analyses. The cytotoxicity screening of the compounds were done by MTT assay on different human cancer cell lines.
 Compound 1 bearing iodomethyl moiety, showed remarkable cytotoxicity with IC50 values in the range of 8.11 and 21.24 µg/mL. The IC50 value on Vero (African green monkey kidney epithelial) is over 100 µg/mL which means low cytotoxicity against healthy cells. Compared to this, SK-MEL cells have 12 times less IC50 value, with a therapeutic index over 12. The closest cytotoxic effectivity to KOJI MG84 which is previously reported as a cytotoxic agent, is observed on the SK-MEL cell line in compound 1, with 4 times less cytotoxic activity.","PeriodicalId":39138,"journal":{"name":"Hacettepe University Journal of the Faculty of Pharmacy","volume":"41 9","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-11-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135934606","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
GSK-3β inhibitörleri için in siliko ilaç yeniden konumlandırma 针对 GSK-3β 抑制剂的硅学药物重新定位
Q4 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2023-11-01 DOI: 10.52794/hujpharm.1361472
Elif DENİZ, Fuat KARAKUŞ, Burak KUZU
Tau, a protein associated with microtubules, is widely distributed throughout the central nervous system and promotes the polymerization, assembly, and stability of microtubules. Hyperphosphorylation of tau proteins leads to intracellular neurofibrillary tangles, which are the pathological hallmark of numerous neurodegenerative diseases (e.g., Alzheimer's disease) and are collectively referred to as "tauopathies". The most notable kinase identified in tau phosphorylation is glycogen synthase kinase 3 (GSK3). Among the GSK-3 isoforms, GSK-3β has been linked to the pathophysiology of neurodegenerative diseases. Pharmacological inhibition of GSK-3β has been suggested as a potential therapeutic target for these diseases. In this study, the literature and databases (e.g., HIT 2.0, PubChem, and ChEMBL) were searched for potential inhibitory drugs against GSK-3β and found 58 drugs. The drugs were filtered according to physicochemical-pharmacological properties and toxicity profiles via SwissADME, pkCSM, and ProTox-II, free web tools. After pre-filtration, molecular docking was performed against GSK-3β (PDB ID: 5K5N) with the remaining seven drugs (Nabumeton, Loxoprofen, Ketoprofen, Oxytetracycline, Benzoyl Peroxide, Naproxen, and Epinephrine Hydrochloride). According to the results, nabumetone had the best binding energy (-7.39 kcal/mol) and inhibition ability at the lowest concentration (3.8 µM) against GSK-3β among the seven drugs [compared to PF-04802367 (PDB ID: 6QH), a highly selective brain-penetrant kinase inhibitor]. Nabumetone is an NSAID used to treat some arthritis, postoperative pains, and dysmenorrhea. Our results suggest that nabumetone may be a potential inhibitor of GSK-3β.
Tau是一种与微管相关的蛋白质,广泛分布于整个中枢神经系统,并促进微管的聚合、组装和稳定性。tau蛋白的过度磷酸化导致细胞内神经原纤维缠结,这是许多神经退行性疾病(例如阿尔茨海默病)的病理标志,统称为“tau病”。在tau磷酸化中发现的最显著的激酶是糖原合成酶激酶3 (GSK3)。在GSK-3亚型中,GSK-3β与神经退行性疾病的病理生理有关。GSK-3β的药理抑制已被认为是这些疾病的潜在治疗靶点。本研究通过检索HIT 2.0、PubChem、ChEMBL等文献和数据库寻找GSK-3β潜在抑制药物,共发现58种药物。通过免费网络工具SwissADME、pkCSM和ProTox-II根据药物的理化药理学性质和毒性特征进行筛选。预过滤后,GSK-3β (PDB ID: 5K5N)与其余7种药物(那布美顿、洛索洛芬、酮洛芬、土霉素、过氧化苯甲酰、萘普生、盐酸肾上腺素)进行分子对接。结果表明,与高选择性脑渗透激酶抑制剂PF-04802367 (PDB ID: 6QH)相比,纳布美酮对GSK-3β的结合能最高(-7.39 kcal/mol),抑制能力最低(3.8µM)。那布美酮是一种非甾体抗炎药,用于治疗一些关节炎、术后疼痛和痛经。我们的结果表明纳布美酮可能是GSK-3β的潜在抑制剂。
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引用次数: 0
Effects of the Aronia Melanocarpa extract action on the activity of mitochondrial creatine kinase under immobilization stress in old rats 在老龄大鼠的固定应激状态下,Aronia Melanocarpa 提取物对线粒体肌酸激酶活性的影响
Q4 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2023-10-10 DOI: 10.52794/hujpharm.1269999
Volodymyr Shvets, Hanna Maslak, V. Davydov, Halyna Berest, Inna Nosulenko, O. Voskoboinik, Liudmyla Omeli̇anchyk, Oleksandr Brazhko
The effects of the Aronia melanocarpa extract on mitochondrial creatine kinase isoenzyme of the old rats heart under stress were studied. The research was performed on 30 male rats of the Wistar line. For expiriment were used old (22–25 months) animals. It was established, that the injection of the extract (Aronia melanocarpa) at a dose of 0.2 g/kg 60 minutes before the immobilization has limited sensitivity of the heart muscle’s CPK-MT to damaging stress factors (reduced medium pH, increased medium tonicity, increased concentration of calcium, activated free radical processes), and helps the normalization of its kinetic properties, has an influence on the myocardium’s kinetic supply. Thus, the extract of Aronia melanocarpa increases the myocardial resistance to the injury effect of stress.
研究了 Aronia melanocarpa 提取物对压力下老龄大鼠心脏线粒体肌酸激酶同工酶的影响。研究对象是 30 只 Wistar 系雄性大鼠。实验使用的是老龄(22-25 个月)动物。结果表明,在固定前 60 分钟注射 0.2 克/千克剂量的提取物(Aronia melanocarpa)可限制心肌 CPK-MT 对破坏性应激因素(介质 pH 值降低、介质强直性增加、钙浓度增加、自由基激活过程)的敏感性,并有助于其动力学特性的正常化,对心肌的动力学供应产生影响。因此,Aronia melanocarpa 提取物能增强心肌对应激损伤效应的抵抗力。
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引用次数: 0
Comparative acute toxicity study of Syringodium isoetifolium on aquatic and rodent experimental animals 异叶丁香对水生动物和啮齿动物急性毒性比较研究
Q4 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2023-08-25 DOI: 10.52794/hujpharm.1140865
D. Kavitha, R. Padmini, V. Alekhya, C. Gopi, M. Dhanaraju
This study was intended to assess the acute toxicity of hydroalcoholic leaf exact of Syringodium isoetifolium seagrass on brine shrimp, zebrafish and Wistar albino rats. The extract of different concentrations were used for brine shrimp (0.01-5 mg/ml in propylene glycerol/Tween 80/ water (4:1:4), zebrafish (12.5, 25, 50, 100, 200, 400 mg/ml), and female albino Wistar rat (500, 1000, 2000, 2500 and 5000 mg/kg) study. The control group received distilled water and the studies were carried out as per the OECD guidelines. The experimental subjects were observed individually for the first 24 hours, with special attention given during the first four hours, thereafter for a prescribed duration. The results of brine shrimp exhibited increased mortality with increasing concentration of the extract. Maximum mortality occurred at 1000 µg/ml and the least mortalities happened at 1 µg/ml concentration. Whereas no mortality and physical damage were identified in the zebrafish and Wistar albino rats irrespective of the concentration. The study revealed that the extract was found to be a toxic effect on brine shrimp due to the poor elimination of cytotoxic substances from the body at high concentrations and elimination freely at low concentrations. No toxicity was exerted on other study subjects.
本研究旨在评价紫花海草水酒精叶精对盐水对虾、斑马鱼和Wistar白化大鼠的急性毒性。不同浓度的提取物分别用于卤虾(0.01 ~ 5 mg/ml丙三醇/吐温80/水(4:1:4))、斑马鱼(12.5、25、50、100、200、400 mg/ml)和雌性白化Wistar大鼠(500、1000、2000、2500和5000 mg/kg)的研究。对照组接受蒸馏水,研究按照经合组织的指导方针进行。实验对象在前24小时进行单独观察,在前4小时给予特别注意,随后进行规定时间的观察。结果表明,随着提取物浓度的增加,盐水虾的死亡率增加。浓度为1000µg/ml时死亡率最高,浓度为1µg/ml时死亡率最低。然而,无论浓度如何,斑马鱼和Wistar白化大鼠均未发现死亡和身体损伤。研究发现,该提取物对盐水虾具有毒性作用,因为高浓度时细胞毒性物质难以从体内清除,低浓度时可自由清除。对其他研究对象无毒性作用。
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引用次数: 0
Antiepileptics pharmacotherapy or antidiabetics may hold potential in ‎treatment of ‎‎epileptic ‎patients with diabetes mellitus: A narrative review 抗癫痫药物治疗或抗糖尿病药物治疗可能在治疗伴有糖尿病的癫痫患者中具有潜力
Q4 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2023-08-22 DOI: 10.52794/hujpharm.1198613
Marwan S. Al-Nimer, Saeed A. S. AL-ZUHAIRY
Several studies have reported the association of diabetes mellitus with epilepsy. With respect to ‎the management of diabetes–epilepsy patients, these studies pointed out the beneficial effects of ‎the ketogenic diet. Ketogenic diets may have antiepileptic properties as the utilization of ketone ‎bodies in the brain instead of glucose delays or inhibits the degradation of γ-aminobutyric acid ‎‎(GABA) transaminase, and thereby enhances the concentration of GABA. By restoring normal ‎intracerebral GABA levels and reducing the cerebral inflammation linked to epilepsy, metformin ‎is useful in preventing seizures. Sitagliptin is one of the dipeptidyl dipeptidase-4 inhibitors, ‎which have a positive impact on epilepsy in experimental animal models with pentylenetetrazole-‎induced seizures, by reducing reactive oxygen species, (antioxidant effect), normalization of ‎GABA level, suppression of neuroinflammation (autophagy) and reduced neuronal damage ‎‎(antiapoptotic effect). Weight gain is a well-known side effect of anti-seizure medications. ‎Sodium valproate can cause dyslipidemia and inhibit glucose transporter-1 in the brain, putting ‎patients with epilepsy and diabetes at risk of developing atherosclerosis. It's worth looking at ‎how ferroptosis and autophagy contribute to the etiology of diabetes and epilepsy, as well as ‎how antiepileptics and antidiabetics alter these pathological processes. Therefore, it was worth ‎performing a narrative-review on the effects of antiepileptics on diabetes, the effect of ‎antidiabetics on epilepsy, as well the net results of antiepileptic–antidiabetic interactions in those ‎patients.‎
一些研究报道了糖尿病与癫痫的关系。关于糖尿病癫痫患者的管理,这些研究指出了生酮饮食的有益作用。生酮饮食可能具有抗癫痫作用,因为利用脑内酮体代替葡萄糖延缓或抑制γ-氨基丁酸(GABA)转氨酶的降解,从而提高GABA的浓度。通过恢复正常的脑内GABA水平和减少与癫痫有关的脑炎症,二甲双胍在预防癫痫发作方面是有用的。西格列汀是二肽基二肽酶-4抑制剂之一,通过降低活性氧(抗氧化作用)、使GABA水平正常化、抑制神经炎症(自噬)和减少神经元损伤(抗凋亡作用),对戊四唑诱发癫痫的实验动物模型有积极影响。体重增加是抗癫痫药物的一个众所周知的副作用。丙戊酸钠会导致血脂异常,抑制大脑中的葡萄糖转运蛋白-1,使癫痫和糖尿病患者有发展为动脉粥样硬化的风险。值得关注的是,铁下垂和自噬如何导致糖尿病和癫痫的病因,以及抗癫痫药和抗糖尿病药如何改变这些病理过程。因此,有必要对抗癫痫药物对糖尿病的影响、抗糖尿病药物对癫痫的影响以及这些患者抗癫痫-抗糖尿病相互作用的净结果进行叙述性回顾
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引用次数: 0
Opioid Peptides: Pharmaceutical Significance and Formulation Approaches 阿片肽:药学意义和处方方法
Q4 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2023-08-21 DOI: 10.52794/hujpharm.1109147
Demet Engi̇n, S. Timur, Stela Muçaj, R. N. Gürsoy
Opioidler, kendi reseptörlerine bağlanarak gösterdikleri ağrı kesici etkisi nedeniyle, binlerce yıldır ağrı tedavisinde kullanılmaktadır. Günümüzde kullanımları daha kontrollü olarak hala devam etmektedir. Ancak yan etkileri ve bağımlılık potansiyelleri nedeniyle hastaların izlenmesi gerekmektedir. Araştırmacılar tarafından, insan vücudunda doğal olarak sentezlenen ve opioid benzeri etkilere yol açan endojen opioid peptidleri bulunmuştur. Bu peptidlerin sentetik analogları da sentezlenmektedir. Bu bileşikler kimyasal yapılarından dolayı hidrofiliktir, yük taşırlar ve oral olarak uygulanmaları kısıtlıdır. Bu nedenle formülasyon için farklı yaklaşımlar geliştirilmiştir. Peptid tabanlı hidrojel sentezlenmesi ve bileşiğin hidrojele konjuge edilmesi, peptidin kumarinik asit temelli siklik bir ön ilaca dönüştürülmesi yaklaşımları stabil olmayan opioid peptidleri enzimatik parçalanmadan korur. Peptidin bir nanopartiküle yüklenmesi ve lipozomal nanotaşıyıcıların kullanılmasında nanoteknolojiden yararlanılmıştır. Multiveziküler lipozomlar (DepoFoam) kullanılarak cerrahi sonrası ağrı yönetiminde peptid temelli ilaç uygulanması mümkündür. Opioid peptidler, tedavide faydalanılabilecek birçok endikasyona sahiptir. Peptidlerin formülasyonunda çok çeşitli teknolojiler kullanılmaktadır ve bu çalışmalardan umut verici sonuçlar elde edilmiştir.
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引用次数: 0
期刊
Hacettepe University Journal of the Faculty of Pharmacy
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