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Antiepileptic geissoschizine methyl ether is an inhibitor of multiple neuronal channels 认领
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作者 Zhu-qing Xie Xiao-ting Tian +5 位作者 Yue-ming Zheng Li Zhan Xue-qin Chen Xiao-ming Xin Cheng-gang Huang Zhao-bing Gao 《中国药理学报:英文版》 SCIE CAS CSCD 2020年第5期629-637,共9页
Geissoschizine methyl ether(GM)is an indole alkaloid isolated from Uncaria rhynchophyll(UR)that has been used for the treatment of epilepsy in traditional Chinese medicine.An early study in a glutamate-induced mouse s... Geissoschizine methyl ether(GM)is an indole alkaloid isolated from Uncaria rhynchophyll(UR)that has been used for the treatment of epilepsy in traditional Chinese medicine.An early study in a glutamate-induced mouse seizure model demonstrated that GM was one of the active ingredients of UR.In this study,electrophysiological technique was used to explore the mechanism underlying the antiepileptic activity of GM.We first showed that GM(1−30μmol/L)dose-dependently suppressed the spontaneous firing and prolonged the action potential duration in cultured mouse and rat hippocampal neurons.Given the pivotal roles of ion channels in regulating neuronal excitability,we then examined the effects of GM on both voltage-gated and ligand-gated channels in rat hippocampal neurons.We found that GM is an inhibitor of multiple neuronal channels:GM potently inhibited the voltage-gated sodium(NaV),calcium(CaV),and delayed rectifier potassium(IK)currents,and the ligand-gated nicotinic acetylcholine(nACh)currents with IC50 values in the range of 1.3−13.3μmol/L.In contrast,GM had little effect on the voltage-gated transient outward potassium currents(IA)and four types of ligand-gated channels(γ-amino butyric acid(GABA),N-methyl-D-aspartate(NMDA),α-amino-3-hydroxy-5-methylisoxazole-4-propionate/kainite(AMPA/KA receptors)).The in vivo antiepileptic activity of GM was validated in two electricity-induced seizure models.In the maximal electroshock(MES)-induced mouse seizure model,oral administration of GM(50−100 mg/kg)dose-dependently suppressed generalized tonic-clonic seizures.In 6-Hz-induced mouse seizure model,oral administration of GM(100 mg/kg)reduced treatment-resistant seizures.Thus,we conclude that GM is a promising antiepileptic candidate that inhibits multiple neuronal channels. 展开更多
关键词 geissoschizine methyl ether Uncaria rhynchophyll antiepileptic drug hippocampal neurons action potential nicotinic acetylcholine receptors voltage-gated ion channels mouse seizure model
Renal transplant recipient seizure practical management 认领
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作者 Harpreet Sawhney Simon S Gill 《世界肾病学杂志:英文版》 2020年第1期1-8,共8页
Seizures are not uncommon in renal transplant patients.The common aetiologies are metabolic disturbance associated with renal failure,immunosuppression and associated complications and infections.Their management can ... Seizures are not uncommon in renal transplant patients.The common aetiologies are metabolic disturbance associated with renal failure,immunosuppression and associated complications and infections.Their management can be challenging because of altered pharmacokinetics of antiepileptic drugs(AEDs)and their removal by dialysis.A practical approach to the management of seizure in renal transplant patients is discussed.This review highlights the guidelines for use of various AEDs in renal transplants. 展开更多
关键词 Seizures Renal transplant HAEMODIALYSIS URAEMIA Antiepileptic drugs
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Extended Antiepileptic Drug Prophylaxis and Late Onset Seizures in Aneurysmal Subarachnoid Hemorrhage 认领
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作者 Wen Hao Low Qing Yuan Goh Miqi Mavis Teo 《现代神经外科学进展(英文)》 2019年第4期401-409,共9页
Background: The indication and optimal duration of antiepileptic drug (AED) prophylaxis after aneurysmal subarachnoid hemorrhage (SAH) remains controversial. Our institution practices routine seizure prophylaxis for v... Background: The indication and optimal duration of antiepileptic drug (AED) prophylaxis after aneurysmal subarachnoid hemorrhage (SAH) remains controversial. Our institution practices routine seizure prophylaxis for variable durations at the discretion of the neurosurgeon and neuro-intensivist. Given the propensity of late onset seizures to progress to chronic epilepsy, we sought to investigate the efficacy of extended AED prophylaxis in reducing the risk of late seizures. Methods: This retrospective study analyzed 36 patients who were admitted to our neurosurgical intensive care unit (NICU) over a 2-year period (1st November 2015 to 31st October 2017). All hospital admissions records, electronic medication records as well as outpatient visits up to 1 year were reviewed. Late onset seizures were defined as seizures occurring more than 7 days post-intervention (or presentation if no intervention was performed) up to 1 year of follow-up. Results: Majority of the patients received Levetiracetam (94%) as seizure prophylaxis and late onset seizures occurred in 6 (17%) of the patients. Those patients who received a greater proportion of in-patient stay with AED prophylaxis had a statistically significant lower risk of developing late seizures (OR = 0.964, 95%, p = 0.02). Although the value tended towards benefit (OR = 0.382) for AED > 21 days in-hospital, the result was not statistically significant (p = 0.307). Conclusion: An extended duration of AED prophylaxis, in particular Levetiracetam, may confer some benefit in reducing risk of developing late seizures. However, the optimal duration of therapy is yet to be determined and further large multi-centered randomized studies are necessary. 展开更多
关键词 ANTIEPILEPTIC SEIZURE PROPHYLAXIS Aneursymal SUBARACHNOID HEMORRHAGE
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A pharmacodynamic model of respiratory rate and end-tidal carbon dioxide values during anesthesia in children 认领
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作者 Ji-Hyun Lee Pyo-Yoon Kang +3 位作者 Young-Eun Jang Eun-Hee Kim Jin-Tae Kim Hee-Soo Kim 《中国药理学报:英文版》 SCIE CAS CSCD 2019年第5期642-647,共6页
It is essential to monitor the end-tidal carbon dioxide (ETCO2) during general anesthesia and adjust the tidal volume and respiratory rate (RR). For the purpose of this study, we used a population pharmacodynamic mode... It is essential to monitor the end-tidal carbon dioxide (ETCO2) during general anesthesia and adjust the tidal volume and respiratory rate (RR). For the purpose of this study, we used a population pharmacodynamic modeling approach to establish the relationship between RR versus ETCO2 data during general anesthesia in children, and to identify the clinical variables affecting this relationship. A prospective observational study was designed to include 51 patients (aged≤12 years), including users of antiepileptic drugs (levetiracetam, valproic, or phenobarbital (n=21)) and non-users (n=30), scheduled to receive general anesthesia during elective surgery. When the ETCO2 was at 40mmHg, the RR was adjusted 1 breath per every 2?min until the ETCO2 was 30 mmHg and recovered to 40 mmHg. Pharmacodynamic analysis using a sigmoid Emax model was performed to assess the RR-ETCO2 relationship. As RR varied from 3 to 37 breaths per minute, the ETCO2 changed from 40 to 30mmHg. Hysteresis between the RR and ETCO2 was observed and accounted for when the model was developed. The Ce50 (RR to achieve 50% of maximum decrease in ETCO2;i.e. 35mmHg) was 20.5 in non-users of antiepileptic drugs and 14.9 in those on antiepileptic drug medication. The values of γ(the steepness of the concentration-response relation curve) and keo (the first-order rate constant determining the equilibration between the RR and ETCO2) were 7.53 and 0.467?min-1, respectively. The Ce50 and ETCO2 data fit to a sigmoid Emax model. In conclusion, the RR required to get the target ETCO2 was much lower in children patients taking antiepileptic drugs than that of non-user children patients during the general anesthesia. 展开更多
关键词 PEDIATRIC ANESTHESIA end-tidal carbon dioxide RESPIRATORY rate population PHARMACODYNAMIC modeling ANTIEPILEPTIC drugs
Low-velocity simultaneous bilateral femoral neck fracture following long-term antiepileptic therapy:A case report 认领
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作者 Mohammed Sadiq Vikrant Kulkarni +2 位作者 Syed Azher Hussain Mohammed Ismail Mayur Nayak 《世界骨科杂志(英文版)》 2019年第10期371-377,共7页
BACKGROUND Simultaneous bilateral femoral neck fractures are relatively rare injuries.They are usually associated with underlying metabolic bone disorders or systemic diseases.Long-term use of narcotics and bisphospho... BACKGROUND Simultaneous bilateral femoral neck fractures are relatively rare injuries.They are usually associated with underlying metabolic bone disorders or systemic diseases.Long-term use of narcotics and bisphosphonates can also result in similar fracture patterns;however,association of this fracture type with longterm use of antiepileptic drugs is not very common.Only one such case has been reported in the literature.This article describes the second.CASE REPORT We report a case of simultaneous displaced bilateral femoral neck fractures in a 50-year-old epileptic patient,who had taken phenytoin for the past 3 years.The fractures were a result of low-velocity injury following a fall from the bed.The fractures were managed with a bilateral hemi-replacement arthroplasty.Oral bisphosphonates were given to improve the bone quality in the post-operative period.The patient had a good post-operative outcome,that was sustained throughout the entire follow-up period of 1 year.CONCLUSION Antiepileptic drugs should be supplemented with bisphosphonates and vitamin D to improve bone quality and prevent fractures in epileptic patients. 展开更多
关键词 Case report BILATERAL FEMORAL neck fracture ANTIEPILEPTIC drug THERAPY Druginduced OSTEOPENIA BISPHOSPHONATES Vitamin D
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基于混合式学习理念的教学设计研究与实践——以护理专业药物学基础课程中抗癫痫药为例 认领
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作者 覃梦岚 黎芳 +1 位作者 李和珍 朱浩荣 《科教导刊》 2019年第3期48-49,54共3页
随着信息技术的飞速发展,以信息化为基础的教师教育教学改革也在不断创新,能够统筹线上、线下学习优势的混合式学习受到越来越多的关注,在教学中的应用与日俱增。中职护理专业的“药物学基础课程”理论性强,学生学习兴趣较低、学习要点... 随着信息技术的飞速发展,以信息化为基础的教师教育教学改革也在不断创新,能够统筹线上、线下学习优势的混合式学习受到越来越多的关注,在教学中的应用与日俱增。中职护理专业的“药物学基础课程”理论性强,学生学习兴趣较低、学习要点掌握不牢。本文基于混合式学习理念来进行教学设计,将教学资源平台、问卷星答题、微课教学等线上方式与面对面教学等线下方式相结合并实际运用于教学中,有效实现真正以学习者为中心的教学活动的开展,使“药物学基础”课程教学的各个环节成为有机联系的整体,收到良好的教学效果。 展开更多
关键词 混合式学习 教学设计 护理专业 抗癫痫药
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Oxcarbazepine oral suspension in young pediatric patients with partial seizures and/or generalized tonic-clonic seizures in routine clinical practice in China: a prospective observational study 认领
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作者 Jiong Qin Yi Wang +9 位作者 Xin-Fang Huang Yu-Qin Zhang Fang Fang Yin-Bo Chen Zhong-Dong Lin Yan-Chun Deng Fei Yin Li Jiang Ye Wu Xiang-Shu Hu 《世界儿科杂志(英文版)》 SCIE 2018年第3期280-289,共10页
Background This study aimed to assess efficacy and safety of oxcarbazepine (OXC) oral suspension in pediatric patients aged 2-5 years with partial seizures (PS) and/or generalized tonic-clonic seizures (GTCS) in real-... Background This study aimed to assess efficacy and safety of oxcarbazepine (OXC) oral suspension in pediatric patients aged 2-5 years with partial seizures (PS) and/or generalized tonic-clonic seizures (GTCS) in real-world clinical practice in China. Methods This 26-week, prospective, single-arm, multicenter, observational study recruited pediatric patients aged 2-5 years with PS or GTCS suitable for OXC oral suspension treatment based on physicians' judgments from 11 medical centers in China. Enrolled subjects started OXC oral suspension treatment as monotherapy or in combination with other antiepileptic drugs. Primary efficacy outcome was the percentage of pediatric subjects achieving ≥ 50% seizure frequency reduction at the end of the 26-week treatment. Secondary efficacy-related parameters and safety parameters such as adverse events (AEs) and serious AEs (SAEs) were also monitored during the 26-week treatment period. Results Six hundred and six pediatric patients were enrolled and 531 (87.6%) completed the study. After 26 weeks of treat-ment, 93.3% subjects achieved ≥ 50% seizure frequency reduction, and 81.8% achieved 100% seizure frequency reduction compared to baseline. Among diff erent seizure types, OXC was eff ective in all subjects with simple PS and in > 90% of subject with other type of seizure present in the study. AEs were observed in 49 (8.1%) subjects. Only three subjects expe-rienced SAE. Rash (n = 18, 2.97%) was the most common AE. Only 17 subjects discontinued due to AEs. Conclusion This study, reporting the real-world data, further confi rms the efficacy and good safety profi le of OXC oral suspension in Chinese pediatric patients aged 2-5 years with PS and/or GTCS. 展开更多
关键词 ANTIEPILEPTIC drugs Generalized tonic-clonic seizures OXCARBAZEPINE oral SUSPENSION Partial seizures PEDIATRIC patients
Use of antiepileptic drugs in children with brain tumors: A review for acute management 认领
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作者 Jennifer Herrera-Bejarano Amit Agrawal +5 位作者 Claudia Marcela Navas Valbuena Guru Dutta Satyarthee Chandramouli Balasubramanian Andrei F.Joaquim George Chater Cure Luis Rafael Moscote-Salazar 《急性病杂志(英文版)》 2018年第5期181-185,共5页
Patients with primary or secondary tumors in the central nervous system may have seizures resulting from direct tissue damage,metabolic abnormalities,infection,or toxic side effects of medications.In pediatric patient... Patients with primary or secondary tumors in the central nervous system may have seizures resulting from direct tissue damage,metabolic abnormalities,infection,or toxic side effects of medications.In pediatric patients,it is more frequent to use drugs to control secondary epilepsy.In this article,we discuss the main nuances of antiepileptic drugs for the proper management of children with central nervous system tumors. 展开更多
关键词 ANTIEPILEPTIC DRUGS BRAIN TUMORS NEURO ONCOLOGY Seizures
Antiepileptic Drug-Induced Apoptosis Was Prevented by L-Type Calcium Channel Activator in Cultured Rat Cortical Cells 认领
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作者 Tsuneo Takadera Masashi Aoki Naruto Nakanishi 《细胞凋亡(英文)》 2017年第2期17-27,共11页
Experimental data have shown that antiepileptic drugs cause neurodegeneration in developing rats. Valproate (VPA) is the drug of choice in primary generalized epilepsies, and carbamazepine (CBZ) is one of the most pre... Experimental data have shown that antiepileptic drugs cause neurodegeneration in developing rats. Valproate (VPA) is the drug of choice in primary generalized epilepsies, and carbamazepine (CBZ) is one of the most prescribed drugs in partial seizures. These drugs block sodium channels, thereby reducing sustained repetitive neuronal firing. The intracellular mechanisms whereby AEDs induce neuronal cell death are unclear. We examined whether AEDs induce apoptotic cell death in cultured cortical cells and whether calcium ions are involved in the AED-induced cell death. VPA and CBZ increased apoptotic cell death and induced morphological changes that were characterized by cell shrinkage and nuclear condensation or fragmentation. Incubation of cortical cultures with VPA or CBZ decreased phospho-Akt levels. CBZ decreased the intracellular calcium levels. On the other hand, FPL64176, an L-type calcium channel activator, increased the intracellular calcium levels and prevented the AED-induced apoptosis. Glycogen synthase kinase-3 inhibitors, such as alsterpaullone and azakenpaullone, prevented the AED-induced apoptosis. These results suggest that intracellular calcium level changes are associated with AEDs and apoptosis and that the activation of glycogen synthase kinase-3 is involved in the death of rat cortical neurons. 展开更多
关键词 ANTIEPILEPTIC Drug Valproate CARBAMAZEPINE L-TYPE Calcium Channel GLYCOGEN SYNTHASE Kinase-3 Apoptosis
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新诊断癫痫患儿首次单药治疗疗效影响因素分析 认领 被引量:1
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作者 江志 杨理明 +3 位作者 张洁 陈波 宁泽淑 郭峰 《中南药学》 CAS 2017年第11期1637-1642,共6页
目的探讨新诊断癫痫患儿首次使用单药治疗疗效的影响因素。方法前瞻性、开放性收集新诊断癫痫患儿,根据发作类型予以规范化抗癫痫治疗,定期随访及复诊,评估疗效。收集患儿治疗前头颅MRI、发作间期脑电图等资料,根据疗效分为控制、... 目的探讨新诊断癫痫患儿首次使用单药治疗疗效的影响因素。方法前瞻性、开放性收集新诊断癫痫患儿,根据发作类型予以规范化抗癫痫治疗,定期随访及复诊,评估疗效。收集患儿治疗前头颅MRI、发作间期脑电图等资料,根据疗效分为控制、显效、有效及无效4组;使用有序多分变量Logistic回归探讨治疗前的头颅MRJ等因素对疗效的影响情况。结果一共有260例患儿完成本研究。1年后癫痫控制140例,显效55例,有效40例,无效25例。各组开始用药年龄(X^2=6.122,P=0.106),发作类型(Z=6.228,P=0.398),抗癫痫药物浓度[丙戊酸钠(VPA):F值=1.797,P=0.152;拉莫三嗪(LTG):F值:0.377,P=0.7711、剂量[VPA:F值=0.659,P=0.579;左乙拉西坦(LEV):F值=1.584,P=0.200;奥卡西平(OXC):F值=1.735,P:0.172;LTG:F值=0.432,P=0.7331等比较,差异无统计学意义(P〉0.05)。头颅MRI异常率(X^2=10.392,P=0.012),智能障碍(Z=8.592,P=0.035),出生窒息(X^2=12.356,P=0.006)等比较,差异有统计学意义(P〈0.05,P〈0.01)。有序多分变量Logistic回归分析发现首发年龄[首发年龄=0时,参数估计-0.994,95%CI(ConfidenceInterval,可信区间)一0.174~1.815,P=0.018;首发年龄=1时,参数估计-0.578,95%CI-0.009~1.156,P=0.037,首发年龄=2时,参数估计0.453,95%CI-0.306~1.212,P=0.2421,出生窒息(参数估计0.603,95%C10.021~1.942,P=0.041),头颅MRI异常(参数估计0.617,95%a0.039~1.196,P=0.036),智能障碍(参数估计1.470,95%C10.506~2.433,P=0.003),发作间歇期脑电图异常(参数估计0.868,95%C10.25l~1.496,P=0.006)为治疗不同转归的风险因素(P〈0.05)。结论新诊断癫痫患儿首次单药治疗疗效影响因素有首发年龄、出 展开更多
关键词 抗癫痫 癫痫 疗效 有序多分变量Logistic回归 影响因素
Comparison of efficacy of folic acid and silymann in the management of antiepileptic drug induced liver injury: a randomized clinical trial 认领
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作者 Masoumeh Asgarshirazi Mamak Shariat Mahdi Sheikh 《国际肝胆胰疾病杂志:英文版》 SCIE CAS CSCD 2017年第3期296-302,共7页
BACKGROUND: Liver injury associated with antiepileptic drugs accounts for a large proportion of drug-induced liver injuries(DILI) in children. Although withdrawal of the causative agent is the only proved treatment fo... BACKGROUND: Liver injury associated with antiepileptic drugs accounts for a large proportion of drug-induced liver injuries(DILI) in children. Although withdrawal of the causative agent is the only proved treatment for DILI, in some clinical situations it is not possible. Recent studies have reported promising results of using hepatoprotective drugs with antioxidant actions for the management of DILI. This study aimed to evaluate the efficacy of folic acid versus silymarin treatment in relation to decreasing liver enzymes in patients with DILI due to antiepileptic therapy.METHODS: This randomized, open-label, clinical trial evaluated 55 children with epilepsy who were on antiepileptic treatment and experienced DILI. The children were randomized to receive either silymarin(5 mg/kg per day) or folic acid(1 mg per day) for one month and were followed up for three months.RESULTS: Liver enzymes significantly decreased in both groups. The decrease trend in alanine aminotransferase(ALT) and aspartate aminotransferase(AST) were stronger in the folic acid group compared to silymarin group(P=0.04 and P=0.007, respectively). At the end of the study patients in the folic acid group had significantly lower ALT(P=0.04), AST(P=0.02), and gamma-glutamyl transferase(GGT)(P<0.001) levels and also higher percentage of normal ALT(30.7% vs 3.4%, P=0.009) and AST(42.3% vs 0%, P<0.001), and GGT(23.1% vs 0%, P=0.008) values compared to the patients in the silymarin group. No rebound elevations in ALT, AST and GGT levels or adverse reactions were noted in neither of the study groups.CONCLUSION: Although both treatments were safe and effective in decreasing liver enzymes, folic acid seems to be superior to silymarin in the management of DILI. 展开更多
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Emergency treatment of proximal femural fracture within 48h: The Umbria Region experience 认领
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作者 Pellegrino Ferrara Luca Khalil El Jaouni +1 位作者 Giuseppe Rocco Talesa Serena Parmeggiani 《急性病杂志(英文版)》 2017年第5期210-213,共4页
Objective: To study the main aspects of osteoporotic emergency fracture of the hip in the Umbria Region in the years 2006-2011. Methods: The study was conducted from January 1 of 2006 to December 31 of 2011, and inclu... Objective: To study the main aspects of osteoporotic emergency fracture of the hip in the Umbria Region in the years 2006-2011. Methods: The study was conducted from January 1 of 2006 to December 31 of 2011, and included only patients over 49 years of age. Patients who did not habitually reside in the region were excluded. They were collected in each based on the following data: age, sex, place of residence (urban or rural), time of the year, fractured side, type of trauma, history of fracture contralateral and perioperative mortality. Results: From 2006 to 2011, a progressive increase in the number of femoral fracture admissions in regional hospitals was observed, equal to 4.73% per annum. The incidence went from 6.8 to 8.1 for 1.000 ultra-65th residents. The most affected age groups are those between 75-84 years and 85-94 years. Conclusions: The epidemiology of osteoporotic hip fracture in the Umbria Region follows a pattern similar to that of other Italian regions. The in-hospital mortality of these patients is partly determined by age and number of complications they suffer during admission. The impact of economic resources on patients who break the osteoporotic hip justifies the implementation of programs for the prevention of osteoporosis and fractures. 展开更多
关键词 Eslicarbazepine ACETATE Partial-onset seizures EPILEPSY ANTIEPILEPTIC DRUGS Drug INTERACTIONS
Topiramate induced peripheral neuropathy:A case report and review of literature 认领
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作者 Sherifa Ahmed Hamed 《世界临床病例杂志》 2017年第12期446-452,共7页
Drug-induced peripheral neuropathy had been rarely reported as an adverse effect of some antiepileptic drugs(AEDs)at high cumulative doses or even within the therapeutic drug doses or levels.We describe clinical and d... Drug-induced peripheral neuropathy had been rarely reported as an adverse effect of some antiepileptic drugs(AEDs)at high cumulative doses or even within the therapeutic drug doses or levels.We describe clinical and diagnostic features of a patient with peripheral neuropathy as an adverse effect of chronic topiramate(TPM)therapy.A 37-year-old woman was presented for the control of active epilepsy(2010).She was resistant to some AEDs as mono-or combined therapies(carbamazepine,sodium valproate,levetiracetam,oxcarbazepine and lamotrigine).She has the diagnosis of frontal lobe epilepsy with secondary generalization and has a brother,sister and son with active epilepsies.She became seizure free on TPM(2013-2017)but is complaining of persistent distal lower extremities paresthesia in a stocking distribution.Neurological examination revealed presence of diminished Achilles tendon reflexes,stocking hypesthesia and delayed distal latencies,reduced conduction velocities and amplitudes of action potentials of posterior tibial and sural nerves,indicating demyelinating and axonal peripheral neuropathy of the lower extremities.After exclusion of the possible causes of peripheral neuropathy,chronic TPM therapy is suggested as the most probable cause of patient’s neuropathy.This is the first case report of topiramate induced peripheral neuropathy in the literature. 展开更多
关键词 TOPIRAMATE PERIPHERAL NEUROPATHY Sodium channel BLOCKADE ANTIEPILEPTIC DRUGS
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Eslicarbazepine acetate:A therapeutic agent of paramount importance in acute anticonvulsant therapy 认领
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作者 Farah Iram Shah Alam Khan +2 位作者 Aftab Ahmad Anees A.Siddiqui Asif Husain 《急性病杂志(英文版)》 2017年第6期245-254,253共11页
Eslicarbazepine acetate (ESL) is a new, once daily, orally administered, third generation antiepileptic drug which is indicated in the treatment of partial-onset seizures. ESL is known to exert it's anticonvulsant... Eslicarbazepine acetate (ESL) is a new, once daily, orally administered, third generation antiepileptic drug which is indicated in the treatment of partial-onset seizures. ESL is known to exert it's anticonvulsant effect by blocking the voltage-gated sodium channels. Several clinical trials and pharmacological studies have revealed that seizure control was better with ESL monotherapy (1 200 or 1 600 mg once daily) following a switch from other antiepileptic drugs in comparison with pseudo-placebo patients. The studies have indicated the ESL to be well tolerated and produced only mild to moderate emergent adverse events with the therapy. Being a dibenzazepine family member, structure and chemistry of ESL resembles more or less to carbamazepine and oxcarbazepine. ESL differs structurally from carbamazepine and oxcarbazepine at the 10, 11 position of dibenazepine nucleus. This molecular variation results in differences in metabolism and thus helps to prevent the formation of toxic epoxide metabolites. ESL following oral administration is rapidly metabolised to active metabolite namely S-licarbazepine which is responsible for its pharmacological activity. ESL exhibits acceptable pharmacokinetic profile and shows insignificant drug-drug interactions. In phase III clinical program, ESL was found to be efficacious and well tolerated in adult patients with partial onset seizures previously not controlled with treatment with one or two other antiepileptic drugs. 展开更多
关键词 Eslicarbazepine ACETATE Partial-onset seizures EPILEPSY ANTIEPILEPTIC drugs Drug interactions
Mono-Therapy versus Poly-Therapy: Ten Years Indian Experience on Various Seizure Disorders 认领
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作者 Deepak Goel Manish Mittal 《神经科学国际期刊(英文)》 2015年第5期350-357,共8页
Objectives: To find out prescription patterns and seizure freedom with different mono-, duo- and poly-therapies used in various seizure disorders in Indian setting. Material and Methods: Subjects with seizures, not re... Objectives: To find out prescription patterns and seizure freedom with different mono-, duo- and poly-therapies used in various seizure disorders in Indian setting. Material and Methods: Subjects with seizures, not responding to first antiepileptic drug, were evaluated prospectively for a period of 6 months. Patients on various dual antiepileptic drugs (AEDs) prescriptions were prospectively analyzed for 1) the pattern and frequency of different duo-therapies;2) etiological profile of patients in duo-therapy prescription;and 3) frequency of seizure freedom on various duo-therapy groups. Results: Among 2542 patients, 293 (11.5%) lost in follow-up and thus, 2249 (88.5%) were followed. 1324 (58.9%) had seizure freedom on mono-therapy, 532 (23.7%) required duo-therapy and only 45 (2%) were better controlled on poly-therapy. Among the subjects, who were on mono-therapy, Carbamazepine/Oxcarbazepine was the most commonly prescribed in 1285 (50.55%) patients as first drug followed by Valproate compound and Phenytoin. The most common duo-therapy used was combination of Valproate with Lamotregine, followed by Phenytoin and Phenobarbitone. Other mono-therapy and combinations are given in this paper. Conclusions: Duo-therapy was required and found to be effective in 23.7% of Indian patients with epilepsy. Selection of appropriate two drug combination is based on individual approach and overall clinical profile of patient. 展开更多
关键词 ANTIEPILEPTIC Drugs Refractory EPILEPSY RATIONALE Poly-Therapy
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Brain Tumours and Prophylactic Antiepileptic Drug Prescribing Patterns by Neurosurgeons Practising in Australasia 认领
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作者 Chrisovalantis A. Tsimiklis Marguerite A. Harding 《神经系统科学与医药(英文)》 2015年第1期13-19,共7页
Prescribing patterns amongst practising Australasian neurosurgeons regarding the use of prophylactic antiepileptic drugs (AEDs) in patients with newly diagnosed intrinsic brain tumours are not well established. This s... Prescribing patterns amongst practising Australasian neurosurgeons regarding the use of prophylactic antiepileptic drugs (AEDs) in patients with newly diagnosed intrinsic brain tumours are not well established. This study aimed to determine the rate of prophylactic AED prescribing in this clinical context and to determine if there were some particular factors that influenced prescribers in their decision. A survey was conducted, and of the 91 respondents, 23 (25.3%) prescribed prophylactic AEDs. No neurosurgeons practising in New Zealand prescribed, whereas within Australian states/territories, prescribing was most common in Western Australia (3/4, 75.0%) and Queensland (8/18, 44.4%) and less common in the Australian Capital Territory (0/2, 0.0%) and South Australia (1/7, 14.3%). The most commonly prescribed first-line AED was phenytoin (n = 15, 68.2%) followed by levetiracetam (n = 5, 22.7%). The duration of prescription varied from 1 week to 6 months, with 6 weeks chosen by most prescribers (n = 7, 35%). Important factors that influence the decision to prescribe include tumour location and a history of previous seizure/s, whereas the presence of oedema or haemorrhage and patients’ age do not seem to be major influences amongst prescribers. 展开更多
关键词 Brain Tumours ANTIEPILEPTIC Drugs SEIZURE PROPHYLAXIS Medication PRESCRIBING
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207例抗癫痫药物血药质量浓度测定结果分析 认领 被引量:3
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作者 赵萌 郑南波 杨红莲 《西北药学杂志》 CAS 2015年第5期640-642,共3页
目的探讨抗癫痫药物血药质量浓度监测对抗癫痫药物合理应用的意义。方法建立我院抗癫痫药Access数据库,回顾性分析我院所监测的207例样品。结果 207例样品的患者控制有效率为76.32%。结论监测癫痫患者服药后的血药质量浓度,对临床及时... 目的探讨抗癫痫药物血药质量浓度监测对抗癫痫药物合理应用的意义。方法建立我院抗癫痫药Access数据库,回顾性分析我院所监测的207例样品。结果 207例样品的患者控制有效率为76.32%。结论监测癫痫患者服药后的血药质量浓度,对临床及时调整给药方案、降低癫痫的发作率、减少癫痫药物的不良反应具有重要的意义。 展开更多
关键词 丙戊酸钠 卡马西平 抗癫痫药物 血药质量浓度监测
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丙戊酸钠的合成 认领
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作者 吴长增 李公春 +2 位作者 牛亮峰 何琴 王伟 《化学工程师》 CAS 2015年第8期10-12,共3页
钠与绝对乙醇作用生成乙醇钠,然后与丙二酸二乙酯反应,再用1-溴丙烷进行烷基化,碱性条件下水解,HCl酸化,加热脱羧,与NaOH成盐,合成了丙戊酸钠,总收率为45.1%。该合成方法操作简单,适合工业化生产。
关键词 丙戊酸钠 丙二酸二乙酯 抗癫痫 合成
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西坦类药物研究进展 认领 被引量:5
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作者 宋艳玲 孙欢 李柏娜 《中国药业》 CAS 2015年第1期4-7,共4页
西坦类药物有防治认知功能障碍、抗癫痫和镇痛等作用,具有作用机制独特、疗效显著、不良反应发生率低等优点,目前已成为临床的常用药物。通过对西坦类药物进行总结,并从作用机制、临床应用等方面对其研究进展进行归纳,将有助于西坦类药... 西坦类药物有防治认知功能障碍、抗癫痫和镇痛等作用,具有作用机制独特、疗效显著、不良反应发生率低等优点,目前已成为临床的常用药物。通过对西坦类药物进行总结,并从作用机制、临床应用等方面对其研究进展进行归纳,将有助于西坦类药物的进一步发展。 展开更多
关键词 西坦类药物 认知功能障碍 抗癫痫 镇痛 研究进展
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HPLC法同时测定5种抗癫痫药的血清药物浓度 认领 被引量:4
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作者 周晶 王漪檬 +4 位作者 赵宁民 段虹飞 马爱玲 赵红卫 郭玉忠 《中国医药科学》 2015年第5期39-41,共3页
目的:建立同时测定拉莫三嗪、苯巴比妥、苯妥英、卡马西平和氯硝西泮血清浓度的HPLC法。方法血清样品经甲醇沉淀蛋白后直接进样分析,色谱柱为Waters C18(5μm,4.6×250mm)柱,流动相为甲醇-水(55∶45),检测波长235nm。结果... 目的:建立同时测定拉莫三嗪、苯巴比妥、苯妥英、卡马西平和氯硝西泮血清浓度的HPLC法。方法血清样品经甲醇沉淀蛋白后直接进样分析,色谱柱为Waters C18(5μm,4.6×250mm)柱,流动相为甲醇-水(55∶45),检测波长235nm。结果在一定浓度范围内(拉莫三嗪:1.3~50.0μg/mL;苯巴比妥:2.5~100.0μg/mL;苯妥英:2.2~70.0μg/mL;卡马西平:1.8~35.0μg/mL;氯硝西泮:2.5~80.0μg/mL),各药物的峰面积与浓度呈良好的线性关系。低、中、高浓度的质控样品回收率均高于95%,相对标准差(RSD)均小于10%。结论本方法操作简便,结果稳定可靠,适用于临床进行血药浓度监测。 展开更多
关键词 抗癫痫药 血药浓度 高效液相色谱法 治疗药物监测
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