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Fentanyl - A Potent Opioid Analgesic: A Review 芬太尼——一种有效的阿片类镇痛药:综述
Pub Date : 2016-10-14 DOI: 10.4172/2329-6631.1000162
A. Sharma, Maniratna Nareda, Sanaa Aziz, Deepak Sharma, S. Garg
Fentanyl is a potent analgesic that is almost a hundred times accented than morphine, the use of fentanyl is pain allayer and anesthetic was adopted in the medical primed. Fentanyl was first introduced by Dr. Jansen in 1959. Many type of fentanyl derivatives have been developed by adding respective substituents to the canonic molecule inorder to alter the potency, some of the ensunting molecules may exist as isomers. (The isomers of 3-methylfentanyl), which have different types of analgesic potencies depends on which is used. Bever reported that the 3rd position of a methyl group (-CH3) into the piperidine ring, increases analgesic potency. The Trans isomer was slightly more active agent than fentanyl, but its respective cis form was eight folds more active. They found that activity of the cis (+) 3-methylfentanyl more potent than fentanyl, whereas the cis negative form was less potent.
芬太尼是一种强效镇痛药,药效几乎是吗啡的100倍,芬太尼作为止痛剂和麻醉剂的使用在医学上被广泛采用。芬太尼于1959年由詹森博士首次引入。许多类型的芬太尼衍生物都是通过在正分子上加入相应的取代基来改变其效价而被开发出来的,一些相关分子可能以异构体的形式存在。(3-甲基芬太尼的异构体),根据使用的不同,它们具有不同类型的镇痛效力。Bever报道了一个甲基(-CH3)进入哌啶环的第3位,增加了镇痛效力。反式异构体的活性略高于芬太尼,但其各自的顺式形式的活性高8倍。他们发现顺式(+)3-甲基芬太尼的活性比芬太尼更强,而顺式阴性形式的活性则更弱。
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引用次数: 7
Synergistic Effects of Plant Extracts and Antifungal Drugs on C. albicans 植物提取物与抗真菌药物对白色念珠菌的协同作用
Pub Date : 2016-08-31 DOI: 10.4172/2329-6631.1000165
K. A. Salih
Background: Fungi have surrounded us and have affected our life, when changed or getting out from control it should be treated and when change to multi drug resistant it is difficult to treat by antibiotics so we can use plant extracts to produce valuable protection against infection. Objective: In this study, we used agar well diffusion method to investigate the effect of antifungal drug of plant extracts on Candida albicans. Methods: Candida albicans was isolated from oral cavity of Sulaimani Emergency hospital patients. The isolates consisted C. albicans (n=15). The microorganisms were divided into four groups in a factorial design: control, FGE with blackseed, FGE without black seed, black seed without FGE and antibiotic (Fluconazole). The minimum inhibitory concentration of FGE was calculated by using a gradient of concentrations and observing their inhibitory effects on C. albicans. Results: Fresh garlic extract (FGE extract) displayed evident inhibition against Candida albicans by producing more inhibition zone (p<0.05), Black seed extract (BL extract) showed no inhibitory effect on C. albicans at 10% concentration. However, synergism of BI with FGE have shown significant effects on it (P<0.05) and fluconazole had little effect on Candida albicans. Conclusion: The result suggests that FGE can improve the antibiotic sensitivity and BI don’t effect on C. albicans.
背景:真菌围绕在我们身边,影响着我们的生活,当真菌发生变化或失去控制时,需要进行治疗,当真菌发生多重耐药时,抗生素难以治疗,因此我们可以使用植物提取物来产生有价值的抗感染保护。目的:采用琼脂孔扩散法研究植物提取物抗真菌药物对白色念珠菌的作用。方法:从苏莱曼尼急诊医院患者口腔中分离出白色念珠菌。其中白色念珠菌15株。采用因子设计将微生物分为4组:对照组、FGE加黑籽组、FGE不加黑籽组、黑籽不加FGE组和抗生素组(氟康唑)。采用浓度梯度法计算FGE的最低抑菌浓度,并观察其对白色念珠菌的抑菌效果。结果:鲜大蒜提取物(FGE提取物)对白色念珠菌有明显的抑制作用,产生更多的抑制带(p<0.05),黑籽提取物(BL提取物)在10%浓度下对白色念珠菌无抑制作用。而BI与FGE的协同作用对白色念珠菌有显著的影响(P<0.05),氟康唑对白色念珠菌的影响较小。结论:FGE能改善白念珠菌的抗生素敏感性,BI对白念珠菌无影响。
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引用次数: 7
Brand Loyalty as a Strategy for the Competition with Generic Drugs:Physicians Perspective 品牌忠诚作为与仿制药竞争的策略:医师视角
Pub Date : 2016-08-30 DOI: 10.4172/2329-6631.1000159
Ç. Macit, N. Taner, G. Mercanoğlu, F. Mercanoğlu
Like in other industries, the competition among companies in the pharma industry is high. Therefore pharmaceutical companies have to design their strategies in order to achieve competitive advantage. Brand loyalty is a powerful tool in the development of pharmaceutical brands. Physicians play major role in the selection of drugs to consume and can also be considered as the consumer. This descriptive study examines the factors that influence physicians’ choices of medication for their patients. Data was collected using a survey administered to specialists and trainees from Cardiology Department. Total 18 physicians participated in the study. Most of the respondents (85%) declared the scientific literature regarding the drug as their first priority in prescribing. Almost half of the respondents (46%) declared the published clinical trial results as a primary source of information about the launch of new drug. With respect to the inclusion of a newly launched drug in the daily prescribing routine, 85% of the respondents tended to prescribe a new drug after the publication of clinical trials. A vast majority of the participants indicated the patients’ source of payment as a major factor for their preferences; meanwhile 92% of them also emphasized the therapeutic equivalency of the drug for their preferences. More than half of the participants (>70%) tended to prescribe original drugs to patients having chronic disease/comorbidity and special insurance coverage and/or self-payment. Regarding the physicians’ familiarity to the original proprietary names, more than half of the respondents correctly predicted the original proprietary names. This study reflects the physician’s perspective for the establishment of brand loyalty. From the physicians’ standpoint belief in brand is crucial for the creation of brand loyalty and the key for building up trust is the scientific data regarding the effectiveness and safety of the drug obtained from large-scale clinical trials.
与其他行业一样,制药行业公司之间的竞争也很激烈。因此,制药公司必须设计自己的战略,以获得竞争优势。品牌忠诚度是医药品牌发展的有力工具。医生在选择消费药物方面起着主要作用,也可以被视为消费者。本描述性研究探讨了影响医生为病人选择药物的因素。数据是通过对心脏病科专家和受训人员的调查收集的。共有18名医生参与了这项研究。大多数受访者(85%)表示,他们在开处方时首先考虑的是有关药物的科学文献。几乎一半的应答者(46%)宣称已发表的临床试验结果是新药上市信息的主要来源。关于将新上市药物纳入日常处方程序,85%的受访者倾向于在临床试验发表后开新药。绝大多数参与者表示,患者的支付来源是影响他们选择的主要因素;同时,92%的人也强调了药物的治疗等效性。超过一半的参与者(>70%)倾向于给患有慢性病/合并症和特殊保险和/或自费的患者开原药。关于医师对原专利名称的熟悉程度,超过一半的被调查者正确预测了原专利名称。本研究反映了医师对品牌忠诚建立的看法。从医生的角度来看,对品牌的信任对于建立品牌忠诚度至关重要,而建立信任的关键是通过大规模临床试验获得的关于药物有效性和安全性的科学数据。
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引用次数: 5
Computational Sensitive Quantitative Predictions of MHC Binding Peptides from Dracunculus medinensis 麦地那龙MHC结合肽的计算敏感性定量预测
Pub Date : 2016-08-26 DOI: 10.4172/2329-6631.1000160
Sonu K. Mishra, V. Gomase, K. Kale
“Dracunculus medinensis” the Guinea Worm Disease (GWD) causing agent belong to the member of ‘Dracunculidae’ family. The infectious female nematode which is up to 800 mm (31 in) in length is the causative agent of the Guinea worm disease in the humans. Cyclops are the intermediate host of this infectious parasite. The healthy individual drinks or consume the contaminated water with Cyclops, which carries the infectious larvae of the Guinea Worm Disease. For the selection of the nonamers, the antigenic peptide the fragments of specific protein can be used, which can be further utilizing for the rational vaccine design and to increase the understanding the immune system response against the disease. The encouraging outcomes of the MHCII (Major Histocompatibility Complex II) analysis shows that the antigenic peptide of the Guinea Worm Disease are important determinant for the protection of the host from parasitic infection. In this study, the Position Specific Scoring Matrices (PSSM) and Support Vector Machine (SVM)-algorithms has been use for antigenic design and prediction of the binding affinity of the antigen having the 88 amino acids long residue, which shows 80 nonamers. The binding ability of the antigen to the major histocompatibility complex (MHC) class I and II molecules prediction will be helpful in the near future for specific targeted drug designing for the Guinea Worm Disease.
麦地那龙线虫是麦地那龙线虫病的病原,属麦地那龙线虫科。长度可达800毫米(31英寸)的传染性雌性线虫是人类麦地那龙线虫病的病原体。独眼虫是这种传染性寄生虫的中间宿主。健康人饮用或饮用带有携带麦地那龙线虫病传染性幼虫的独眼虫污染的水。对于命名物的选择,可以使用抗原肽或特异性蛋白片段,进一步用于合理的疫苗设计,增加对免疫系统对疾病反应的了解。MHCII(主要组织相容性复合体II)分析的令人鼓舞的结果表明,麦地那龙线虫病的抗原肽是保护宿主免受寄生虫感染的重要决定因素。在本研究中,使用位置特异性评分矩阵(PSSM)和支持向量机(SVM)算法进行抗原设计和预测抗原的结合亲和力,抗原具有88个氨基酸长残基,其中包含80个非命名体。预测抗原与主要组织相容性复合体(MHC) I类和II类分子的结合能力将有助于在不久的将来设计针对麦地那龙线虫病的特异性靶向药物。
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引用次数: 0
Controversial in Menopausal Hormone Replacement Therapy 绝经期激素替代疗法存在争议
Pub Date : 2016-07-11 DOI: 10.4172/2329-6631.1000158
M. Stoicescu
Introduction: The main objective of this presentation is to attract the attention about a hot topic regarding menopausal hormone therapy replacement. It is a good option for a woman to follow or no this hormonal therapy replacement during menopause period, taking into account the benefits and also the risks? This is a modern phenomenon in this moment in the medicine field, but is it really safe for a woman to follow this therapy? Much more research has to be done regarding this therapy to not expose many females to unnecessary side effects. Can we force the natural evolution of the mechanisms of the body in this direction? Materials and methods: Further on it will be presented two cases of medical practice, with two major side effects of this therapy, not insignificant, which should give food for thought. The first case develops occurrence of breast malignancy and the second with endometrial cancer after the therapy. Results and discussion: The idea of menopausal hormone replacement therapy appeared with the all best intentions for this difficult period in a woman’s life in menopause, but the reality is that dangerous side effects can occur like mentioned before. Conclusion: The most important conclusion of this presentation is that hormone replacement therapy at menopause is not safe and more research is needed in the future for the best decision.
本次演讲的主要目的是引起人们对绝经期激素替代疗法的关注。这是一个很好的选择对于女性来说在绝经期是否使用激素替代疗法,考虑到益处和风险?这是当今医学领域的一个现代现象,但女性接受这种疗法真的安全吗?关于这种疗法,还需要做更多的研究,以避免让许多女性遭受不必要的副作用。我们能强迫身体的机制朝着这个方向自然进化吗?材料和方法:接下来将介绍两个医疗实践案例,该疗法的两个主要副作用,不容忽视,应该引起人们的思考。1例经治疗后发生乳腺恶性肿瘤,2例经治疗后发生子宫内膜癌。结果和讨论:绝经期激素替代疗法的想法是出于对绝经期妇女生活中这一困难时期的所有最好的意图,但现实是危险的副作用可能发生,就像前面提到的那样。结论:本报告最重要的结论是,更年期激素替代疗法并不安全,未来需要更多的研究来做出最佳决定。
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引用次数: 1
Fabrication and Evaluation of Fast Disintegrating Oral Hybrid Films of Propranolol Hydrochloride by Using Pectin and Synthetic Polymers 用果胶和合成聚合物制备盐酸心得安口服复合快速崩解膜及评价
Pub Date : 2016-06-27 DOI: 10.4172/2329-6631.1000157
Newton Amj, R. Sm, K. Sukhjinder
The main aim of this investigation is to develop fast disintegrating oral films of Propranolol hydrochloride by using Pectin and synthetic polymers. The Propranolol HCl oro-dispersible films were formulated by using HPMC E15LV, HPMC regular, pectin, Carbopol, and PVA, as film forming polymers. The selected polymers were natural and synthetic water soluble polymers. Generally solvent casting method was used in the manufacture of the mouth dissolving films. The formula which incorporates pectin HPMC E15 LV 4:2 and pectin: Carbopol 3:2 ratios and also other varying ratio were used in the formulation of Oro-dispersible films. The quantity and type of plasticizer affected the formulation of films; Propranolol HCl has bitter taste so taste masking agents were used. Citric acid was used as a salivary stimulating agent. The prepared films were subjected to the analysis of various evaluation tests such as weight variation, tensile strength, thickness, surface pH, and drug content. The significant parameters such as disintegration and dissolution profiles also studied in detail since the product was prepared for fast dissolving in the oral cavity.
本研究的主要目的是利用果胶和合成聚合物制备快速崩解的盐酸心得安口服薄膜。以HPMC E15LV、HPMC regular、果胶、Carbopol和PVA为成膜聚合物,制备了盐酸心得安(Propranolol HCl)或分散膜。所选聚合物为天然和合成水溶性聚合物。口腔溶膜的制造一般采用溶剂铸造法。采用果胶HPMC E15 LV 4:2和果胶:卡波波尔3:2的配比及其他不同配比的配方制备oro分散膜。增塑剂的数量和种类影响薄膜的配方;盐酸心得安有苦味,故使用掩味剂。柠檬酸被用作唾液刺激剂。对制备的膜进行了各种评价试验分析,如重量变化、拉伸强度、厚度、表面pH和药物含量。由于该制剂为口腔快速溶出制剂,因此对其崩解、溶出等重要参数进行了详细的研究。
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引用次数: 9
Heat Shock Protein as Emerging Oncologic Drug Targets 热休克蛋白作为新的肿瘤药物靶点
Pub Date : 2016-06-24 DOI: 10.4172/2329-6631.1000155
L. Tutar, K. A. Coskun, Yusuf Tutar
Lutfi Tutar1, Kübra Açıkalın Coskun2 and Yusuf Tutar2* 1Department of Biology, Graduate School of Natural and Applied Sciences, Kahramanmaraş Sütçü İmam University, Kahramanmaraş, Turkey 2Division of Biochemistry, Department of Basic Sciences, Faculty of Pharmacy, Sivas Cumhuriyet University, Turkey *Corresponding author: Yusuf Tutar, Division of Biochemistry, Department of Basic Sciences, Faculty of Pharmacy, Sivas Cumhuriyet University, Turkey, Tel: +90 3462191010; E-mail: ytutar@yahoo.com
Lutfi Tutar1, k bra Açıkalın Coskun2和Yusuf Tutar2* 1土耳其kahramanmarura大学自然与应用科学研究生院生物学系Sütçü İmam土耳其kahramanmarura大学药学院基础科学系生物化学系*通讯作者:土耳其Sivas Cumhuriyet大学药学院基础科学系生物化学系Yusuf Tutar,电话:+90 3462191010;电子邮件:ytutar@yahoo.com
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引用次数: 4
Edoxaban for the Prevention of Stroke in Patients with Atrial Fibrillation 艾多沙班预防房颤患者脑卒中
Pub Date : 2016-06-23 DOI: 10.4172/2329-6631.1000E148
Amy Wang
Atrial fibrillation (AF) is a devastating disease in the United States and affects almost 12% of patients who are between the ages of 75 to 84. Having AF almost increases the risk of stroke by 5-fold, and therefore, anticoagulation therapy is essential for the prevention of stroke in patients with AF [1]. Warfarin has been the sole oral anticoagulation available for decades. From 2010 to 2012, 3 additional novel oral anticoagulation (NOAC) came onto the market, which includes dabigatran, rivaroxaban, and apixaban and offered viable alternatives to warfarin for the management of AF [2-4]. In January 2015, the FDA approved edoxaban, a factor Xa inhibitor, to come onto the market for the prevention of stroke in AF patients. Edoxaban is the third factor Xa inhibitor currently available, in addition to rivaroxaban and apixaban [5,6].
心房颤动(AF)在美国是一种毁灭性的疾病,影响了近12%的75至84岁之间的患者。房颤患者发生卒中的风险几乎增加了5倍,因此,抗凝治疗对于房颤患者卒中的预防至关重要。几十年来,华法林一直是唯一可用的口服抗凝剂。2010年至2012年,又有3种新型口服抗凝剂(NOAC)上市,包括达比加群、利伐沙班和阿哌沙班,为治疗房颤提供了可行的替代方案[2-4]。2015年1月,FDA批准依多沙班(Xa因子抑制剂)上市,用于预防房颤患者中风。依多沙班是目前除利伐沙班和阿哌沙班外可用的第三种Xa因子抑制剂[5,6]。
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引用次数: 4
Anti-Inflammatory Activity of Methanolic Leaf Extract of Kigelia Africana (Lam.) Benth and Stem Bark Extract of Acacia Hockii De Wild in Mice 非洲木叶甲醇提取物的抗炎活性研究野生金合欢底、茎皮提取物对小鼠的影响
Pub Date : 2016-06-13 DOI: 10.4172/2329-6631.1000156
J. Kamau, Nthiga Pm, Mwonjoria Jk, Ngeranwa Jjn, Ngugi Mp
Inflammation causes discomfort, suffering and lower productivity of the victims. Synthetic anti-inflammatory drugs are not readily available and have adverse side effects. Alternative herbal medicines possess bioactive compounds that are safer and efficient in the management of various diseases and disorders. The present study evaluated for the anti-inflammatory activity of methanolic extracts of Kigelia africana and Acacia hockii in mice to scientifically validate their traditional use among the Embu and Mbeere communities in Kenya. The plant samples were collected with the help of local herbalists in Embu County, Kenya and transported to Kenyatta University biochemistry and biotechnology laboratories for cleaning, air drying, milling, and extraction. Swiss albino mice of either sex were randomly divided into six groups of 5 animals each; normal control, negative control, positive control and three experimental groups. The anti-inflammatory activity was tested using carrageenan-induced hind paw edema method. The anti-inflammatory activity of the extracts was compared to reference drug diclofenac. The leaf extract of K. africana reduced inflamed hind paw diameter of mice by between 0.21%- 4.98% while the stem bark extract of A. hockii reduced inflamed hind paw diameter by between 0.6%-5.38%. The diclofenac reduced inflamed hind paw diameter by between 1.11%-4.9%. The qualitative phytochemical screening indicated the presence of saponins, flavonoid, alkaloids, terpenoids, phenolics, and cardiac glycosides. The present study demonstrated potent antiinflammatory activities of methanolic extracts of K. africana and A. hockii in a dose-dependent manner, which supports their traditional use. The present study, therefore, recommends the ethnomedicinal use of K. africana and A. hockii in the management of inflammation.
炎症会导致患者不适、痛苦和生产力下降。合成抗炎药不易获得,而且有不良副作用。替代草药具有生物活性化合物,在管理各种疾病和失调方面更安全、更有效。本研究评估了非洲木和霍奇尼合欢的甲醇提取物对小鼠的抗炎活性,以科学地验证它们在肯尼亚Embu和Mbeere社区的传统使用。植物样本是在肯尼亚恩布县当地草药医师的帮助下采集的,并运送到肯雅塔大学生物化学和生物技术实验室进行清洗、风干、碾磨和提取。将瑞士白化小鼠随机分为6组,每组5只;正常对照组、阴性对照组、阳性对照组及三个实验组。采用角叉菜胶诱导后足水肿法检测其抗炎活性。并与对照药双氯芬酸进行抗炎活性比较。非洲栎叶提取物对小鼠炎症后爪直径的抑制作用在0.21% ~ 4.98%之间,而胡氏栎茎皮提取物对小鼠炎症后爪直径的抑制作用在0.6% ~ 5.38%之间。双氯芬酸可使发炎后爪直径减少1.11% ~ 4.9%。定性植物化学筛选表明,其含有皂苷、类黄酮、生物碱、萜类、酚类和心苷。本研究表明,非洲蓟和霍奇氏蓟的甲醇提取物具有剂量依赖性的抗炎活性,这支持了它们的传统用途。因此,本研究建议使用非洲支原体和霍奇氏单胞菌治疗炎症。
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引用次数: 21
Visions but Not False Promises Should Be Funded 应该为愿景而不是虚假的承诺提供资金
Pub Date : 2016-06-10 DOI: 10.4172/2329-6631.1000154
K. Petrak
Efforts to develop cell-specific drug-delivery systems have been under way for decades but have not as yet generated effective and reliable therapeutic products. The effect of repeatedly unfulfilled promises is starting to cause a decrease in funding support for research and development in this area. In this commentary, principle flaws in the current approaches are listed and discussed. Further, the manner in which approaches and paradigms for further development should change is suggested.
开发细胞特异性药物输送系统的努力已经进行了几十年,但尚未产生有效和可靠的治疗产品。一再未能兑现的承诺的影响开始导致对这一领域研究和发展的资金支持减少。在这篇评论中,列出并讨论了当前方法的主要缺陷。此外,还建议改变进一步发展的方法和范例的方式。
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引用次数: 0
期刊
Journal of Developing Drugs
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