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Therapeutic monitoring of amikacin and gentamicin in critically and noncritically ill patients. 阿米卡星和庆大霉素在危重症和非危重症患者中的治疗监测。
Pub Date : 2016-06-01 DOI: 10.4103/0976-0105.183260
Tijana Kovačević, Sanja Avram, Dragana Milaković, Nikolina Špirić, Pedja Kovačević

Objective: Therapeutic drug monitoring (TDM) enables individualization in the treatment to optimize clinical benefit and minimize drugs' side effects. Critically ill septic patients represent a challenge for antimicrobial treatment because of pathophysiological impact of sepsis on pharmacokinetics of drugs. The aim of this study was to assess the appropriateness of gentamicin and amikacin dosing in critically and noncritically ill patients, as well as to estimate the need for its regular therapeutic monitoring.

Subjects and methods: It was a prospective study which included 31 patients on gentamicin and 16 patients on amikacin from four different units who met the inclusion criteria. Trough concentrations of drugs were measured in serum just before third or fourth dose of antibiotic, whereas peak concentrations were measured in serum 1 h after the completion of drug administration (steady state). Relevant data on patients' clinical course of disease, comorbidities, and concomitant medication were collected from medical charts in order to identify their possible influence on drugs' concentrations.

Results: Peak concentrations of amikacin were in reference range in 81.8% critically ill and in 80% of noncritically ill patients (P = 0.931). Peak concentrations of gentamicin were in reference range in 88.9% critically ill and in 77.3% of noncritically ill patients (P = 0.457).

Conclusion: Serum concentrations of aminoglycosides (amikacin and gentamicin) were in reference range in most of the patients in our study, suggesting that dosing of these drugs in the University Hospital Clinical Center, Banja Luka, was adequate. In patients without kidney or liver disease, regular TDM of aminoglycosides is not necessary.

目的:治疗性药物监测(TDM)可实现个体化治疗,优化临床疗效,减少药物副作用。由于脓毒症对药物药代动力学的病理生理影响,重症脓毒症患者对抗菌治疗提出了挑战。本研究的目的是评估庆大霉素和阿米卡星在危重症和非危重症患者中剂量的适宜性,并评估其定期治疗监测的必要性。对象和方法:这是一项前瞻性研究,包括来自4个不同单位的31例庆大霉素患者和16例阿米卡星患者,符合纳入标准。在第三次或第四次给药前测量血清中药物的低谷浓度,而在给药完成后1小时(稳定状态)测量血清中药物的峰值浓度。从病历中收集患者的临床病程、合并症和伴随用药的相关数据,以确定其对药物浓度的可能影响。结果:81.8%的危重病人和80%的非危重病人阿米卡星浓度在参考值范围内(P = 0.931)。88.9%的危重病人和77.3%的非危重病人庆大霉素的峰值浓度在参考值范围内(P = 0.457)。结论:本研究中大多数患者血清氨基糖苷类药物(阿米卡星和庆大霉素)浓度均在参考范围内,提示巴尼亚卢卡大学医院临床中心的氨基糖苷类药物的剂量是足够的。对于没有肾脏或肝脏疾病的患者,不需要常规的氨基糖苷类TDM。
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引用次数: 22
Monitoring of adverse drug reactions in psychiatry outpatient department of a Secondary Care Hospital of Ras Al Khaimah, UAE. 阿拉伯联合酋长国Ras Al Khaimah二级医院精神科门诊药物不良反应监测
Pub Date : 2016-06-01 DOI: 10.4103/0976-0105.183263
Sathvik Belagodu Sridhar, Sura Saad Faris Al-Thamer, Riadh Jabbar

Background: Adverse drug reactions (ADRs) are a significant cause of morbidity and mortality, resulting in increased healthcare cost. Association of psychotropic medications with ADRs is common. Pharmacovigilance can play a vital role in alerting the healthcare providers from the possible ADRs and thus protecting the patients receiving psychotropic medications.

Aim: To monitor and report the incidence and nature of ADRs in psychiatry outpatient department (OPD).

Materials and methods: A prospective observational study was carried out in the psychiatry OPD. All the patients attending psychiatry outpatient and satisfying the inclusion criteria were monitored for ADRs. The causality, severity and preventability assessment of documented ADRs was done. Chi-square test was done to identify the association between ADRs and sociodemographic, disease and treatment-related variables. Paired Student's t-test was carried out to compare the significance difference in the weight of the patients who reported weight gain to psychotropic medications.

Results: The incidence rate of ADR was found to be 10.2%. A total of 112 ADRs were documented. Weight gain 18 (16.07%) followed by somnolence 8 (7.14%) was the most commonly reported ADR. Atypical antipsychotics 37 (33.0%) were the most common class of psychotropic drugs implicated in ADRs. Escitalopram 16 (14.28%) followed by quetiapine 14 (12.5%) were associated with a maximum number of ADRs. No significant association (P > 0.05) documented between demographic and treatment-related variables with number of ADRs.

Conclusion: Study revealed a moderate incidence of ADRs in patients attending the psychiatry OPD. Majority of the ADRs reported during the study were mild in nature and not preventable type.

背景:药物不良反应(adr)是发病率和死亡率的重要原因,导致医疗成本增加。精神药物与不良反应的关联是常见的。药物警戒在提醒医疗服务提供者可能出现不良反应,从而保护接受精神药物治疗的患者方面发挥着至关重要的作用。目的:监测和报告精神科门诊不良反应的发生率和性质。材料和方法:在精神科门诊进行了一项前瞻性观察性研究。所有参加精神科门诊并符合纳入标准的患者均进行不良反应监测。对记录在案的不良反应进行因果关系、严重程度和可预防性评估。采用卡方检验确定不良反应与社会人口学、疾病和治疗相关变量之间的关系。采用配对学生t检验比较精神药物治疗后体重增加患者体重的显著性差异。结果:药品不良反应发生率为10.2%。总共记录了112例adr。最常见的不良反应是体重增加18(16.07%),其次是嗜睡8(7.14%)。非典型抗精神病药物37(33.0%)是最常见的一类与不良反应有关的精神药物。艾司西酞普兰16(14.28%)和喹硫平14(12.5%)与最大不良反应次数相关。人口统计学和治疗相关变量与不良反应数量无显著相关性(P > 0.05)。结论:研究显示,在精神科门诊就诊的患者中,不良反应发生率中等。研究中报告的大多数不良反应是轻微的,不是可预防的。
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引用次数: 35
Prevalence and assessment of biochemical parameters of attention-deficit hyperactivity disorder children in Bangladesh. 孟加拉国儿童注意缺陷多动障碍的患病率及生化参数评估。
Pub Date : 2016-06-01 DOI: 10.4103/0976-0105.183261
Chowdhury Mohammad Monirul Hasan, Mohammad Monirul Islam, Muhammad Mamunur Rashid Mahib, Mahmud Ahmed Chowdhury Arju

Background and objectives: This study aimed to evaluate some new biochemical parameters that help ensuring the early and precise diagnosis of attention-deficit hyperactivity disorder (ADHD) in blood plasma.

Design and settings: A prospective study conducted with patients scheduled for some new biochemical parameters that help ensuring the early and precise diagnosis of ADHD in blood plasma in a Child Development Center of the Chittagong, Bangladesh.

Materials and methods: The study was carried out at two levels. The first level was questionnaire on personal data and disease history while the second was on biochemical examination of the plasma ammonia and lactate status. A total of 100 children (age range 2 years 4 months to 12 years 6 months, mean age 7 years 5 months) were investigated in this study among 75 were male and 25 were female. This study was conducted in Chittagong Maa-O-Shishu General Hospital, Bangladesh.

Results: We observed that the level of plasma ammonia and lactate were higher in ADHD children (36-60 μmol/L; P < 0.05 and 22-30 μmol/L; P < 0.05, respectively) compare to a reference value. The prevalence of ADHD is higher in male (75%) than in female (25%) with a ratio of 3:1. Consanguinity increases the risk of having ADHD in the next generation.

Conclusion: This study concludes that there might be a correlation between ADHD and increased level of plasma ammonia and lactate level, and those might be an important parameter in the diagnosis of ADHD patients.

背景与目的:本研究旨在评估一些新的血浆生化参数,以确保早期准确诊断注意缺陷多动障碍(ADHD)。设计和设置:在孟加拉国吉大港的儿童发展中心,对患者进行了一项前瞻性研究,安排了一些新的生化参数,以帮助确保血浆中ADHD的早期和精确诊断。材料与方法:本研究分为两个层次。第一阶段为个人资料和病史问卷调查,第二阶段为血浆氨、乳酸生化检查。本研究共调查了100例儿童(年龄范围2岁4个月至12岁6个月,平均年龄7岁5个月),其中男性75例,女性25例。本研究在孟加拉国吉大港Maa-O-Shishu总医院进行。结果:ADHD患儿血浆氨、乳酸水平较高(36 ~ 60 μmol/L;P < 0.05, 22 ~ 30 μmol/L;P < 0.05),与参考值比较。ADHD的患病率男性(75%)高于女性(25%),比例为3:1。近亲关系会增加下一代患多动症的风险。结论:本研究认为ADHD与血浆氨、乳酸水平升高可能存在相关性,这可能是ADHD患者诊断的重要参数。
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引用次数: 4
A simple practice guide for dose conversion between animals and human 动物和人之间剂量转换的简单实践指南
Pub Date : 2016-03-01 DOI: 10.4103/0976-0105.177703
Anroop B Nair, Shery Jacob
Understanding the concept of extrapolation of dose between species is important for pharmaceutical researchers when initiating new animal or human experiments. Interspecies allometric scaling for dose conversion from animal to human studies is one of the most controversial areas in clinical pharmacology. Allometric approach considers the differences in body surface area, which is associated with animal weight while extrapolating the doses of therapeutic agents among the species. This review provides basic information about translation of doses between species and estimation of starting dose for clinical trials using allometric scaling. The method of calculation of injection volume for parenteral formulation based on human equivalent dose is also briefed.
在开展新的动物或人体实验时,了解物种间剂量外推的概念对药物研究人员很重要。从动物到人的剂量转换的种间异速缩放是临床药理学中最具争议的领域之一。异速测量法在推断不同物种间治疗剂的剂量时,考虑了与动物体重有关的体表面积的差异。这篇综述提供了物种间剂量转换的基本信息,以及使用异速缩放法估计临床试验的起始剂量。并简要介绍了基于人体等效剂量的注射量计算方法。
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引用次数: 3272
Antiurolithiatic activity of Abelmoschus moschatus seed extracts against zinc disc implantation-induced urolithiasis in rats 沙鼠种子提取物对锌片植入所致大鼠尿石症的抗尿石作用
Pub Date : 2016-03-01 DOI: 10.4103/0976-0105.177704
A. Pawar, N. Vyawahare
Background: The commonly used techniques for removing renal calculi are associated with the risk of acute renal injury and increase in stone recurrence which indicates an urgent need for alternate therapy.Objectives: The aim was to evaluate the antiurolithiatic activity of Abelmoschus moschatus seed extracts in rats.Materials and Methods: Urolithiasis was induced by surgical implantations of zinc disc in the urinary bladders of rats. Upon postsurgical recovery, different doses of chloroform (CAM) and methanolic (MAM) extracts of A. moschatus seeds (viz., 100, 200 and 400 mg/kg body weight) were administered to disc implanted rats for the period of 7 days by the oral route. Antiurolithiatic activity was evaluated by measuring various dimensions of stones and estimating levels of various biomarkers in serum and urine samples.Results: A significant decrease in urinary output was observed in disc implanted animals, which was prevented by the treatment with extracts. Supplementation with extracts caused significant improvement in glomerular filtration rate and urinary total protein excretion. The elevated levels of serum creatinine, uric acid, and blood urea nitrogen were also prevented by the extracts. The extracts significantly reduced deposition of calculi deposition around the implanted disc. This antiurolithiatic potential is observed at all doses (100, 200, and 400 mg/kg) of MAM, whereas only higher dose (400 mg/kg) of CAM showed significant antiurolithiatic potential.Conclusion: The extracts of A. moschatus seeds possessed significant antiurolithiatic activity. The possible mechanism underlying this effect is mediated collectively through diuretic, antioxidant, and free-radical scavenging effects of the plant.
背景:常用的肾结石清除技术与急性肾损伤的风险和结石复发的增加有关,这表明迫切需要替代治疗。目的:评价沙鼠种子提取物对大鼠的抗尿石作用。材料与方法:采用大鼠膀胱植入锌片诱导尿石症。术后恢复后,采用不同剂量的沙棘种子氯仿(CAM)和甲醇(MAM)提取物(分别为100、200和400 mg/kg体重)口服给药,为期7天。通过测量结石的各种尺寸和估计血清和尿液样本中各种生物标志物的水平来评估抗尿石活性。结果:椎间盘植入术大鼠尿量明显减少,但经提取物处理后,尿量明显减少。补充提取物可显著改善肾小球滤过率和尿总蛋白排泄。血清肌酐、尿酸和血尿素氮的升高也被提取物所预防。提取物可显著减少植入椎间盘周围的结石沉积。在所有剂量(100mg /kg、200mg /kg和400mg /kg)的MAM中都观察到这种抗尿石潜能,而只有较高剂量(400mg /kg)的CAM显示出显著的抗尿石潜能。结论:沙棘种子提取物具有明显的抗尿石活性。这种作用的可能机制是通过植物的利尿、抗氧化和自由基清除作用共同介导的。
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引用次数: 18
Quality of life, clinical effectiveness, and satisfaction in patients with beta thalassemia major and sickle cell anemia receiving deferasirox chelation therapy 重度地中海贫血和镰状细胞性贫血患者接受去铁铁螯合治疗的生活质量、临床疗效和满意度
Pub Date : 2016-03-01 DOI: 10.4103/0976-0105.177706
S. P. Senol, E. Tiftik, S. Unal, A. Akdeniz, B. Taşdelen, B. Tunctan
Objectives: There is a need to remove excess iron with iron chelation therapy (ICT) to avoid the serious clinical sequelae associated with iron overload in patients with beta thalassemia major (BTM) and sickle cell anemia (SCA). Due to the effects of the diseases and their treatments, ICT is still a major reason for unsatisfactory compliance. The aim of this single-center observational study was to evaluate the quality of life, clinical effectiveness, and satisfaction in pediatric and adult patients with BTM and SCA receiving deferasirox (DFX) chelation therapy. Methods: In this study, 37 pediatric and 35 adult patients with BTM or SCA receiving DFX for at least 6 months participated. Upon receipt of Informed Consent Form, Case Report Form, Demographic Data Collection Form, Child Health Questionnaire-Parent Form, Life Quality Survey Short Form-36, and ICT Satisfaction Survey were used to obtain data for the effectiveness of ICT and parameters that may affect compliance to treatment and life quality of the participants. Results: As a main index for the effectiveness of DFX chelation therapy, serum ferritin levels were higher than the normal values in the patients receiving DFX. The increased ferritin levels were also associated with hematological and biochemical abnormalities. Our findings regarding quality of life and satisfaction with DFX chelation therapy indicated that the patients with BTM or SCA had lower scores. Overall, problems with treatment regimen and side effects appeared to be common causes of poor compliance to DFX chelation therapy. Conclusions: Our findings suggest that health care providers should be aware of the importance of monitoring iron load with timely initiation of DFX chelation therapy and ongoing adjustments to chelation regimens and/or transfusion methods to decrease hospitalizations and improve compliance to ICT of the patients with BTM and SCA.
目的:有必要通过铁螯合疗法(ICT)去除过量的铁,以避免β -地中海贫血(BTM)和镰状细胞性贫血(SCA)患者铁超载相关的严重临床后遗症。由于疾病及其治疗的影响,信息通信技术仍然是依从性不理想的主要原因。本单中心观察性研究的目的是评估接受去铁酸铁(DFX)螯合治疗的BTM和SCA儿童和成人患者的生活质量、临床疗效和满意度。方法:在本研究中,37名儿童和35名接受DFX治疗至少6个月的BTM或SCA患者参与了研究。在收到知情同意书、病例报告表、人口统计数据收集表、儿童健康问卷-家长表、生活质量调查短表-36和ICT满意度调查后,获取ICT有效性和可能影响参与者依从性和生活质量的参数的数据。结果:作为DFX螯合治疗有效性的主要指标,接受DFX治疗的患者血清铁蛋白水平高于正常值。铁蛋白水平升高还与血液学和生化异常有关。我们关于DFX螯合治疗的生活质量和满意度的研究结果表明,BTM或SCA患者的得分较低。总的来说,治疗方案的问题和副作用似乎是DFX螯合治疗依从性差的常见原因。结论:我们的研究结果表明,卫生保健提供者应该意识到监测铁负荷的重要性,及时开始DFX螯合治疗,不断调整螯合方案和/或输血方法,以减少住院率,提高BTM和SCA患者对ICT的依从性。
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引用次数: 22
Fabrication, characterization, and evaluation of microsponge delivery system for facilitated fungal therapy 促进真菌治疗的微海绵输送系统的制造、表征和评价
Pub Date : 2016-03-01 DOI: 10.4103/0976-0105.177705
A. Moin, T. Deb, R. Osmani, Rohit R. Bhosale, U. Hani
Objective: The rationale behind present research vocation was to develop and investigate a novel microsponge based gel as a topical carrier for the prolonged release and cutaneous drug deposition of fluconazole (FLZ); destined for facilitated fungal therapy. Materials and Methods: Microsponges were prepared using quasi-emulsion solvent diffusion method using Eudragit S-100. In the direction of optimization, the effect of formulation variables (drug-polymer ratio and amount of emulsifier) and diverse factors affecting physical characteristics of microsponge were investigated as well. Fabricated microsponges were characterized by differential scanning calorimetry, Fourier transform-infrared, scanning electron microscopy (SEM), particle size analysis, and also evaluated for drug content, encapsulation efficiency, in vitro drug release and in vitro antifungal activity. Results: Compatibility studies results reflected no sign of any chemical interaction between the drug and polymers used. Whereas, varied drug-polymer ratios and emulsifier concentration indicated significant effect on production yield, drug content, encapsulation efficiency, particle size and drug release. Spherical microsponges with a porous surface and 29.327 ± 0.31 μm mean particle size were evident from SEM micrographs. In vitro release outcomes, from microsponge loaded gels depicted that F1 formulation was more efficient to give extended drug release of 85.38% at the end of 8 h, while conventional formulation by releasing 83.17% of drug got exhausted incredibly earlier at the end of 4 h merely. Moreover, microsponge gels demonstrated substantial spreadability and extrudability along with promising antifungal activity. Conclusions: Fabricated microsponges would be impending pharmaceutical topical carriers of FLZ and a leading alternative to conventional therapy for efficient, safe and facilitated eradication of fungal infections.
目的:研制一种新型微海绵凝胶作为氟康唑缓释和皮肤药物沉积的外用载体;用于促进真菌治疗。材料与方法:采用准乳状溶剂扩散法制备微海绵。在优化方向上,考察了配方变量(药聚合物比、乳化剂用量)和各种因素对微海绵物理特性的影响。采用差示扫描量热法、傅里叶变换红外、扫描电镜(SEM)、粒度分析等方法对制备的微海绵进行了表征,并对其药物含量、包封效率、体外释药和体外抗真菌活性进行了评价。结果:相容性研究结果反映没有任何迹象表明药物和聚合物之间的化学相互作用。而不同的药聚合物比和乳化剂浓度对产率、药物含量、包封效率、颗粒大小和药物释放度均有显著影响。微海绵呈球形,表面多孔,平均粒径为29.327±0.31 μm。体外释药结果显示,F1配方在8 h时释药率达到85.38%,而常规配方仅在4 h时释药率就达到了83.17%。此外,微海绵凝胶具有良好的铺展性和挤压性,并具有良好的抗真菌活性。结论:制备的微海绵是一种潜在的药物外用FLZ载体,是一种有效、安全、易于根除真菌感染的替代方法。
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引用次数: 50
Rapid transformation of chronic lymphocytic leukemia to acute lymphoblastic leukemia: A rare case report 慢性淋巴细胞白血病迅速转化为急性淋巴细胞白血病:罕见病例报告
Pub Date : 2016-03-01 DOI: 10.4103/0976-0105.177702
Manmeet Kaur, Sarita Nibhoria, K. Tiwana, A. Bajaj, S. Chhabra
Chronic lymphocytic leukemia (CLL) is characterized by the accumulation of mature-appearing lymphocytes in blood, bone marrow, lymph nodes, and spleen with a median lymphocyte count of 20–30 × 109/L at the time of diagnosis. In half of the patients, the lymphocyte count doubles over a period of 1-year and cyclic rise up to 50 × 109/L can occur in untreated patients while in others the count may remain stable for years. Based on the cytogenetic and molecular studies, it has been demonstrated that multiple clones may occur in CLL and clonal evolution is a frequent occurrence. The transformation of CLL to a high-grade non-Hodgkin's lymphoma such as diffuse large B cell lymphoma, Hodgkin lymphoma, and prolymphocytic leukemia is well documented. Whereas the transformation of CLL to acute leukemia occurs in <1% cases and this contrasts the almost invariable progression in patients with chronic myeloid leukemia. Here, we report a rare case of a 55-year-old lady, a diagnosed case of CLL transforming into B-cell acute lymphocytic leukemia over a very short interval of 1 week period.
慢性淋巴细胞白血病(Chronic lymphocytic leukemia, CLL)以血液、骨髓、淋巴结和脾脏中出现成熟淋巴细胞积累为特征,诊断时淋巴细胞中位数为20 ~ 30 × 109/L。在一半的患者中,淋巴细胞计数在1年内翻倍,未经治疗的患者循环上升至50 × 109/L,而在其他患者中,计数可能保持稳定数年。基于细胞遗传学和分子生物学的研究表明,CLL可能存在多个克隆,克隆进化是一个频繁发生的过程。CLL向高级别非霍奇金淋巴瘤(如弥漫性大B细胞淋巴瘤、霍奇金淋巴瘤和前淋巴细胞白血病)的转变有充分的文献记载。然而,CLL向急性白血病的转化发生在<1%的病例中,这与慢性髓性白血病患者几乎不变的进展形成对比。在此,我们报告一个罕见的病例,一位55岁的女性,诊断为CLL转化为b细胞急性淋巴细胞白血病,时间间隔很短,只有1周。
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引用次数: 5
Knowledge regarding prescription of drugs among dental students: A descriptive study 牙科学生对药物处方知识的描述性研究
Pub Date : 2015-12-01 DOI: 10.4103/0976-0105.170584
Ankita Jain, Devanand Gupta, D. Singh, Y. Garg, Antima Saxena, Himani J. Chaudhary, Alpana Singh, R. Gupta
Introduction: The act of indicating one or more drugs to be taken by the patient, its dosage, and the interval of the treatment is known as prescribing. It is a dynamic and individualized clinical process. Cultural, social, economic and promotional factors can influence the pattern of prescription. Thus the present study was conducted to evaluate the drug prescription knowledge in third year and final year dental students at Teerthanker Mahaveer Dental College and Research Centre, Moradabad, Uttar Pradesh, India. Methodology: A questionnaire consisting of 10 open-ended questions was used in a study which was conducted among 170 male and female, third year and final year dental students of Teerthanker Mahaveer Dental College and Research Centre. Tables and graphs were used to represent data. Results: Pain was found to be the most important reason for prescribing medication. Diclofenac was found to be the most commonly prescribed NSAID. While amoxicillin was found to be the most widely prescribed antibiotic. Lack of knowledge about drug posology was the basic reason for error done by students. Maximum number of students gets their information for prescribing drugs from their professors. Maximum number of students was unacquainted about the WHO Guide to Good Prescribing. Conclusion: The knowledge of prescribing drugs is of utmost need for good dental practice and hence, it is essential to expand the knowledge related to pharmacological therapy and to know about the proper therapeutic guidelines. With the help of WHO Guide to Good Prescribing, and some educational programs students will develop better prescribing skills.
导言:指示病人服用一种或多种药物、其剂量和治疗间隔的行为称为开处方。这是一个动态的、个性化的临床过程。文化、社会、经济和促进因素可以影响处方模式。因此,本研究旨在评估印度北方邦莫拉达巴德市Teerthanker Mahaveer牙科学院和研究中心三年级和大四牙科学生的药物处方知识。方法:采用10个开放式问题的调查问卷,对170名来自Teerthanker Mahaveer牙科学院和研究中心的三年级和大四学生进行调查。用表格和图表来表示数据。结果:疼痛是患者开具处方的最主要原因。双氯芬酸是最常用的非甾体抗炎药。而阿莫西林被发现是最广泛使用的抗生素。对药物生理学知识的缺乏是导致学生用药错误的根本原因。最大数量的学生从他们的教授那里获得处方药物的信息。大多数学生不了解世卫组织《良好处方指南》。结论:提高处方知识是良好口腔卫生的基本要求,扩大药理治疗知识,掌握正确的治疗指南是十分必要的。在《世卫组织良好处方指南》和一些教育规划的帮助下,学生将发展更好的处方技能。
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引用次数: 33
Phytochemicals of Aristolochia tagala and Curcuma caesia exert anticancer effect by tumor necrosis factor-α-mediated decrease in nuclear factor kappaB binding activity 马兜铃和姜黄的植物化学物质通过肿瘤坏死因子-α-介导的核因子κ b结合活性降低发挥抗癌作用
Pub Date : 2015-12-01 DOI: 10.4103/0976-0105.170585
K. L. H. Hadem, R. Sharan, L. Kma
Rationale: The active compounds or metabolites of herbal plants exert a definite physiological action on the human body and thus are widely used in human therapy for various diseases including cancer. Previous studies by our group have reported the anticarcinogenic properties of the two herbal plants extracts (HPE) of Aristolochia tagala (AT) Cham. and Curcuma caesia (CC) Roxb. in diethylnitrosamine-induced mouse liver cancer in vivo. The anticarcinogenic properties of these extracts may be due to the active compounds present in them. Objectives: Our objective was to analyze the phytochemical constituents present in AT and CC, to assay their antioxidant properties and to determine their role in a possible intervention on tumor progression. Materials and Methods: Qualitative and quantitative analysis of constituent with anticancer properties present in the crude methanol extract of the two plants CC and AT was carried out following standard methods. Separation of the phytochemical compounds was done by open column chromatography. The extracts were eluted out with gradients of chloroform-methanol solvents. Ultraviolet-visible spectra of individual fractions were recorded, and the fractions were combined based on their λmax. The free radical scavenging activity of crude extracts and fractions obtained was also determined; the radical scavenging activity was expressed as IC50. High-performance thin layer chromatography (HPTLC) analysis of fractionated compounds was carried out to identify partially the phytochemical compounds. The anti-inflammatory and anticancer activity of AT and CC extracts was studied in DEN induced BALB/c mice by analyzing the tumor necrosis factor-α (TNF-α) levels in serum and the nuclear factor kappaB (NF-κB) binding activity in nuclear extracts of the liver. Results: It was observed that both AT and CC contained compounds such as phenolics, tannins, flavonoids, terpenoids, etc., and both extracts exhibited antioxidant capacity. HPTLC analysis revealed the presence of phenolic compounds in CC and indicated the presence of anthocynidin 3-glycosides, 6-hydroxylated flavonols, some flavones and chalcone glycosides in AT and also confirmed the presence of compounds such as terpenes, phenols, steroids, and other organic compounds in CC and presence of flavonoids in AT. In vivo studies carried out in BALB/c mice showed that exposure to DEN caused an increase in TNF-α and NF-κB binding activity. The HPE (CC or AT) was seen to revert this effect. Conclusions: The current paper documents the antioxidant, anti-inflammatory, and anticancer activity of the two extracts probably through TNF-α-mediated decrease in NF-κB binding activity. The active components of AT and CC may act as the potential anticancer agents in hepatocellular carcinoma and warrants further investigation.
理由:草本植物的活性化合物或代谢物对人体有一定的生理作用,广泛应用于人体治疗包括癌症在内的各种疾病。本课题组前期研究报道了马兜铃(Aristolochia tagala, AT) Cham的两种草本植物提取物(HPE)的抗癌作用。姜黄(Curcuma caesia, CC);二乙基亚硝胺诱导小鼠肝癌的体内实验研究。这些提取物的抗癌特性可能是由于其中存在的活性化合物。目的:我们的目的是分析AT和CC中存在的植物化学成分,测定它们的抗氧化特性,并确定它们在可能干预肿瘤进展中的作用。材料与方法:采用标准方法对CC和AT两种植物粗甲醇提取物中具有抗癌作用的成分进行定性和定量分析。采用开柱色谱法分离植物化合物。提取液用氯仿-甲醇溶剂梯度洗脱。记录各组分的紫外可见光谱,并根据其λmax值进行组合。测定了粗提物和馏分的自由基清除活性;自由基清除活性用IC50表示。对分离化合物进行高效薄层色谱(HPTLC)分析,鉴定部分植物化学成分。通过对DEN诱导的BALB/c小鼠血清中肿瘤坏死因子-α (TNF-α)水平和肝脏核提取物中核因子κ b (NF-κB)结合活性的测定,研究AT和CC提取物的抗炎和抗癌活性。结果:两种提取物均含有酚类、单宁类、黄酮类、萜类等化合物,均具有抗氧化能力。HPTLC分析结果表明,白藜芦醇中存在酚类化合物,白藜芦醇中存在花青素3-苷类、6-羟基黄酮醇类、部分黄酮类和查尔酮类苷类化合物,白藜芦醇中存在萜类、酚类、甾体等有机化合物,白藜芦醇中存在黄酮类化合物。在BALB/c小鼠体内进行的研究表明,暴露于DEN可引起TNF-α和NF-κB结合活性的增加。HPE (CC或AT)可以恢复这种效果。结论:两种提取物的抗氧化、抗炎、抗癌作用可能是通过TNF-α-介导的NF-κB结合活性的降低来实现的。AT和CC的活性成分可能在肝细胞癌中具有潜在的抗癌作用,值得进一步研究。
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引用次数: 17
期刊
Journal of Basic and Clinical Pharmacy
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