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1.
Summary

The analgesic potency of nefopam was compared to that of morphine, pentazocine and pethidine, double-blind in 200 patients with post-operative pain. Each drug was given as a single intramuscular injecton on the first post-operative day. Pain relief was measured both with a 0 to 3 graded pain scale and a 0 to 10 visual analogue scale and expressed as pain intensity, pain intensity difference and sum of pain intensity difference. The degree and time course of pain relief was similar for all four treatments with maximum analgesia 90 minutes after injection. Side-effects were reported by 58% of patients on nefopam compared to 68% on morphine, 82% on pentazocine and 74% on pethidine, the commonest side-effect being sleepiness. These results suggest that nefopam is a sufficiently potent analgesic agent to control post-operative pain, with a relatively low incidence of side-effects.  相似文献   
2.
HPLC法同时测定盐酸奈福泮萘普生胶囊中2种成分的含量   总被引:1,自引:0,他引:1  
程洪兵 《中国药事》2012,26(7):740-742,746
目的 建立同时测定盐酸奈福泮萘普生胶囊中盐酸奈福泮和萘普生含量的高效液相色谱方法.方法 采用Apollo C18色谱柱,以庚烷磺酸钠溶液-乙腈(53:47)为流动相,流速为1.0 mL·min-1,检测波长为215 nm.结果 盐酸奈福泮浓度在15.8~47.5 μg·mL-1范围内与峰面积线性关系良好(r=0.9997),平均回收率为99.43%,RSD为1.31%(n=3);萘普生在54.7~164.2 μg·mL-1范围内线性关系良好(r=0.9999),平均回收率为99.72%,RSD为0.80%(n=3).结论 该方法操作简便,结果准确,精密度高,可用于控制盐酸奈福泮萘普生胶囊的质量.  相似文献   
3.
目的 评估盐酸奈福泮静脉或鞘内注射的镇痛效果及脊髓多巴胺能神经传递在其中的作用。方法 复制大鼠甲醛炎性痛模型,然后进行微透析研究,检测盐酸奈福泮注射后大鼠脊髓背角细胞外多巴胺浓度变 化。通过预先注射舒必利,多巴胺D2 受体拮抗剂,观察多巴胺水平变化与盐酸奈福泮镇痛的关系。结果 静 脉注射盐酸奈福泮,可抑制甲醛诱导的Ⅰ期退缩反应,但对Ⅱ期退缩反应无影响。鞘内注射盐酸奈福泮可减 少Ⅰ和Ⅱ期退缩反应,并呈剂量依赖性。微透析研究发现,鞘内注射盐酸奈福泮引起大鼠脊髓多巴胺水平增加。 预处理舒必利不影响静脉或鞘内注射盐酸奈福泮的镇痛作用。结论 无论是静脉和鞘内注射盐酸奈福泮均有 效缓解大鼠炎性痛。盐酸奈福泮镇痛机制可能不涉及脊髓水平多巴胺能神经传递。  相似文献   
4.
目的:制备平痛新缓释片并建立其质量控制方法。方法:以亲水性高分子材料羟丙基甲基纤维素为主要辅料制备平痛新缓释片;采用紫外分光光度法测定其主药含量及体外释放度。结果:平痛新检测浓度线性范围为10.0~300.0μg.mL-1(r=0.9996),平均回收率为99.97%(RSD=0.49%,n=9)。结论:所制制剂工艺简单,缓释效果理想,稳定性好,质量可控。  相似文献   
5.
Nefopam, a non-opioid, centrally acting benzoxazocine analgesic, proved to be as efficient in treatment of postanaesthetic thermoregulatory shivering as clonidine or meperidine. However, its exact mechanism of action is still unclear. Potent anti-shivering activity was also demonstrated for physostigmine primarily based on cholinergic but probably also different additional mechanisms of action. Hypothesizing an involvement of α2-adrenoceptors we studied their role in nefopam- and physostigmine-mediated thermoregulation in a mouse model of nonshivering thermogenesis. To differentiate possible α2-adrenoceptor subtype-specific interactions, we analysed wildtype mice and mice with deletion of the α2A-, α2B- or α2C-adrenoceptor (knock out).Ten mice of each genotype (n = 40) were administered saline, saline plus atipamezole, 1 mg/kg nefopam, 25 mg/kg nefopam, 25 mg/kg nefopam plus atipamezole, physostigmine and physostigmine plus atipamezole intraperitoneally. Each mouse was randomly subjected to each of the seven different treatments. Afterwards, the mice were positioned into a plexiglas chamber where rectal temperature and mixed expired carbon dioxide were measured during following whole body cooling. Thermoregulatory threshold temperature of nonshivering thermogenesis and maximum response intensity were analysed.Nefopam decreased the thermoregulatory threshold temperature in wildtype, α2B- and α2C-adrenoceptor mice. This effect was partially abolished by additional administration of the α2-adrenoceptor antagonist atipamezole. In α2A-adrenoceptor knock out mice, nefopam did not affect the thermoregulatory threshold. In contrast, physostigmine decreased the thermoregulatory threshold in wildtype and all α2-adrenoceptor knock out mice independently from additional atipamezole administration.Our results indicate an important role of the α2A-adrenoceptor in the thermoregulatory response induced by nefopam but not by physostigmine in mice.  相似文献   
6.
A comparative assay of nefopam,morphine and d-amphetamine   总被引:3,自引:0,他引:3  
Nefopam is a non-opioid analgesic reported to have some stimulant properties. The subjective, behavioral and physiological effects of nefopam, morphine and d-amphetamine were compared in seven non-dependent substance abusers to assess the abuse potential of nefopam. Morphine and d-amphetamine had significant effects on a number of measures generally consistent with the effects of drugs of the opioid and psychomotor stimulant drug classes. Subjects correctly discriminated between morphine and d-amphetamine. Nefopam was most frequently identified by subjects as being amphetamine-like, though several measures indicated that nefopam produced some sedation. Little or no liking of the effects of nefopam was reported by subjects. Overall, nefopam was one fifth as potent as morphine and one quarter as potent as d-amphetamine in producing subjective and physiological effects. The results indicate that nefopam is neither entirely morphine-like nor d-amphetamine-like. In our opinion, nefopam has a lesser potential to be abused than morphine or d-amphetamine. Offprint requests to: Librarian, NIDA Addiction Research Center, P.O. Box 5180, Baltimore, MD 21224, USA  相似文献   
7.
Zusammenfassung In der Arbeit werden analytische Daten zum Nachweis von Nefopam (Ajan®) und einigen Metaboliten (Nor-Nefopam, Nefopam-N-Oxid) beschrieben. Nähere Einzelheiten s. auch Schlüsselwörter.Hersteller: Fa. Kettelhack Riker Pharma GmbH, 4280 Borken  相似文献   
8.
吗啡盐酸奈福泮静脉平衡镇痛用于开胸病人的临床研究   总被引:2,自引:0,他引:2  
目的探讨开胸手术后吗啡与盐酸奈福泮静脉平衡镇痛与单独应用吗啡效果比较研究。方法ASAⅠ、Ⅱ级60例择期开胸手术病人,随机分为吗啡(A)组(n=30)和吗啡+盐酸奈福泮(B)组(n=30),A组:吗啡60.0mg+恩丹西酮4.0mg,B组:吗啡40.0mg+盐酸奈福泮30.0mg+恩丹西酮4.0mg。均以生理盐水稀释至100mL,给予吗啡2.5mg+恩丹西酮4mg作为负荷量后连接PCIA泵进行自控镇痛。术后第1、2、3天静息及咳嗽时行VAS评分,监测用药量及不良反应发生情况。结果两组VAS评分无明显差异,用药量、不良反应A组明显高于B组。结论吗啡与盐酸奈福泮联合应用于开胸手术后镇痛与吗啡单独应用效果相当,但吗啡用量及不良反应发生率明显降低,是一种更安全、有效的镇痛方法。  相似文献   
9.
目的 比较剖宫产术后两种硬膜外自控镇痛效果及恶心呕吐、嗜睡、尿潴留发生率.方法 60例剖宫产患者随机分成两组,每组各30例,术毕分别接硬膜外自控镇痛泵.I组:0.15%盐酸布比卡因加曲马多;Ⅱ组:0.179%甲磺酸罗哌卡因加盐酸奈福泮,观察并记录术后48 h内各时点的视觉模拟评分(VAS)和对应时点下肢运动阻滞程度(Bromage评分)及术后恶心呕吐、嗜睡、尿潴留等不良反应发生率.结果 两组术后6、12、24、36 h VAS比较差异无统计学意义(P>0.05);Bro-Inage评分Ⅰ组各时点分别为(2.75±0.49)分、(1.51±0.42)分、(0.92±1.08)分、(0.89±0.12)分,Ⅱ组分别为(1.31±0.57)分、(0.35±0.31)分、(0.08±0.30)分、(0.06±0.28)分,两组比较差异有统计学意作者单位:252601 山东临清,聊城市第二人民医院麻醉科义(P<0.05);恶心呕吐、嗜睡、尿潴留发生率Ⅰ组分别为16.7%、13.3%、50.0%,Ⅱ组分别为6.7%、3.3%、10.0%,两组比较差异有统计学意义(P<0.01).结论 甲磺酸罗哌卡因复合盐酸奈福泮行硬膜外自控镇痛效果确切,在运动功能恢复,降低恶心呕吐、嗜睡、尿潴留发生率方面显示明显优越性.  相似文献   
10.
A specific and sensitive liquid chromatography–tandem mass spectrometric (LC–MS–MS) method using an ion trap spectrometer was developed for quantitation of nefopam and desmethyl-nefopam in human plasma. Nefopam, desmethyl-nefopam and the internal standard (ethyl loflazepate) were extracted in a single step with diethyl ether from 1 mL of alkalinized plasma. The mobile phase consisted of acetonitrile with 0.1% formic acid (50:50, v:v). It was delivered at a flow-rate of 0.3 mL/min. The effluent was monitored by MS–MS in positive-ion mode. Ionisation was performed using an electrospray ion source operating at 200 °C. Nefopam and desmethyl-nefopam were identified and quantified in full scan MS–MS mode using a homemade MS–MS library. Calibration curves were linear over the concentration range of 0.78–100 ng/mL with determination coefficients >0.996. This method was fast (total run time < 6 min), accurate (bias < 12.5%), and reproducible (intra- and inter-assay precision < 17.5%) with a quantitation limit of 0.78 ng/mL. The high specificity and sensitivity achieved by this method allowed the determination of nefopam and desmethyl-nefopam plasma levels in patients following either intermittent or continuous intravenous administration of nefopam.  相似文献   
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