奥施康定治疗中重度癌痛临床疗效观察

目的观察奥施康定(盐酸羟考酮控释片)治疗中重度癌痛的疗效及不良反应。方法对72例中重度癌痛患者给予奥施康定,起始剂量为10 mg/12 h,根据疼痛缓解程度调整剂量,评价镇痛效果、KPS评分及不良反应。结果平均镇痛起效时间为45 min,平均镇痛时间12.3 h。全组病例总有效率为96.5%,完全缓解率为65.2%,部分缓解率为30.6%,不良反应轻微。结论奥施康定治疗中重度癌痛时,起效快,镇痛效果满意,毒副反应轻,服用安全。     

美施康定与奥施康定直肠给药治疗癌痛的对比研究

目的：观察比较吗啡控释片（美施康定）与羟考酮控释片（奥施康定）直肠给药治疗癌痛的效果。方法将136例晚期癌痛患者随机分为2组：吗啡组（66例）和羟考酮组（70例）。2组间临床资料差异无显著性（ P＞0.05）。2组分别给予吗啡控释片及羟考酮控释片直肠给药治疗癌痛,观察2组直肠给药起效时间及副反应。结果2组癌痛治疗药物起效时间长短差异有显著性（ P＜0．05）。2组癌痛治疗药物不良反应发生率：头晕、恶心呕吐、便秘,差异均有统计学意义（ P＜0．05）。结论盐酸羟考酮控释片直肠给药起效时间更短,而硫酸吗啡控释片直肠给药副反应更小。     

美施康定治疗重度癌痛临床观察

目的 观察美施康定对重度癌痛的治疗效果及其副作用。方法 对310例重度癌痛患美施康定初始剂量为：30mg,q12h。若口服2d镇痛效果不满意,美施康定改为：60mg,q12h,剂量每次递增60mg。结果 310例患中240例得到明显或完全缓解。65例需同时加用非吗啡类镇痛药物才达到明显缓解。3例抿绝继续增加美施康定剂量,未取得明显缓解,2例因副反应和经济原因停用美施康定,毒副作用。主要为消化道反应,表现为恶心、呕吐、便秘。嗜睡常见,未见有呼吸抑制发生,无肝、肾功能损害。结论 美施康定能有效控制重度癌痛,且无严重毒副反应。当为重度癌痛的首选药物。     

奥施康定治疗癌痛疗效观察

目的:观察奥施康定治疗中重度癌痛的疗效。方法:采用开放试验方法,对100例中重度癌痛患者进行治疗。奥施康定初始剂量10mg.12h-1,并根据疼痛缓解程度调整剂量。结果:100例中重度癌痛患者使用的奥施康定最小剂量10mg.12h-1,最大剂量40mg.12h-1;治疗效果:轻度缓解3例(3.0%),中度缓解12例(12.0%),明显缓解65例(65.0%),完全缓解20例(20.0%),中度以上疼痛缓解率97.0%。不良反应有:便秘12例,胃部不适、恶心8例,嗜睡5例,眩晕1例。结论:奥施康定治疗中重度癌痛疗效确切,有效率高,不良反应轻,现已应用于临床。     

奥施康定治疗中重度癌痛临床疗效观察

目的观察奥施康定（盐酸羟考酮控释片）治疗中重度癌痛的疗效及不良反应。方法采用开放试验方法,对95例中重度癌痛患者进行治疗。奥施康定起始剂量1Omg／12h,根据疼痛缓解程度调整剂量,评价镇痛效果和不良反应。结果95例中重度癌痛患者,总有效率85．3％,中度疼痛组有效率90．9％,重度疼痛组有效率83．6％。不良反应主要为便秘31例（32．6％）。结论奥施康定治疗中重度癌痛疗效确切,不良反应轻,服用安全。     

奥施康定治疗118例中重度癌痛临床体会

目的观察奥施康定治疗中重度癌痛疗效、毒副反应,总结应用体会。方法应用奥施康定治疗中重度癌痛患者,回顾性总结有疼痛评分记录及疗效、毒副反应记录的门诊或住院用药患者的临床用药体会。结果有118例本人经管的患者进入本文分析、总结。奥施康定使用剂量5mg q12h至200mg q12h,1例患者用80mgq8h方能持续有效止痛,疼痛控制总有效率为90.7%。应用奥施康定配合速效吗啡片达到良好滴定效果;毒副反应主要为便秘、头晕、恶心、呕吐,尿储留,有出现皮疹、瘙痒,过度镇静,呼吸抑制各两例;预防性用药及用药前与患者充分沟通能减少或减轻不良反应;随着用药时间延长,即使药物剂量加大,不良反应发生率逐渐降低。结论奥施康定是中重度癌痛患者良好选择,应用过程中要注意具体细节,尽量减少不良反应,特别是严重不良反应的发生。     

奥施康定治疗200例中重度癌痛临床体会

目的:观察奥施康定治疗中重度癌痛疗效、毒副反应,总结临床体会。方法:应用奥施康定治疗中重度癌痛患者,回顾性总结有疼痛评分记录及疗效、毒副反应记录的门诊或住院用药患者的临床用药体会。结果:有200例患者纳入本研究。奥施康定使用剂量为5mg q12h至240mg q12h,1例患者用80mg q8h方能持续有效止痛,疼痛控制总有效率为90.0%。应用奥施康定配合速效吗啡片达到良好滴定效果;毒副反应主要为便秘、头晕、恶心、呕吐、尿储留,也有出现皮疹、瘙痒,过度镇静、呼吸抑制各2例;预防性用药及用药前与患者充分沟通能减少或减轻不良反应;尽早、适当应用辅助药可以增加止痛疗效,减少阿片类药物用量;随着用药时间延长,即使药物剂量加大,不良反应发生率逐渐降低。结论:奥施康定是中重度癌痛患者良好选择,应用过程中要注意具体细节,恰当配合止痛辅助药,尽量减少不良反应,特别是严重不良反应的发生。     

奥施康定治疗中重度癌性疼痛的疗效观察

目的观察奥施康定治疗中重度癌性疼痛的疗效与不良反应。方法对96例中重度癌痛患者进行治疗,奥施康定起始剂量10mg／12h,根据疼痛缓解程度调整剂量,评价镇痛效果及不良反应。结果96例中重度癌痛患者,平均镇痛时间12．8h,总有效率95．8％。中度疼痛组有效率100％,重度疼痛组有效率92．6％。不良反应主要为便秘20例（20．8％）。结论奥施康定治疗中重度癌性疼痛疗效确切,不良反应轻微,服用安全。     

奥施康定治疗中重度癌痛的临床观察

目的观察奥施康定治疗中重度癌痛的疗效及不良反应、生活质量。方法对30例癌性中重度疼痛患者进行治疗,其中男19例,女11例。疼痛类型：头痛、胸痛、骨痛、腹痛等。奥施康定剂型为5mg,由患者主诉疼痛明显时给药,且均为首次服用奥施康定。初始剂量10mg.12h-1,服用24h如疼痛评分下降不到3分,则第二天加量至20mg.12h-1,以此类推,最多至50mg.12h-1。在用药过程中根据疼痛缓解程度调整剂量,所有患者均连续用药3周。结果 30例慢性癌性中重度疼痛患者使用的奥施康定最小剂量10mg.12h-1,最大剂量50mg.12h-1。治疗效果：完全缓解11例,部分缓解16例,轻度缓解3例。其中中度疼痛患者的显效率为100.0%,重度疼痛患者的显效率为88%,全部患者总的显效率为90.0%。不良反应有便秘、恶心呕吐、腹胀、厌食、嗜睡、头晕等。患者的生活质量评分用药后与用药前相比有所提高。结论奥施康定治疗慢性癌性中重度疼痛疗效确切,有效率高,不良反应轻,服用安全。     

硫酸吗啡控释片对中晚期癌症患者镇痛效果的临床研究

目的观察硫酸吗啡控释片对中晚期癌症患者疼痛的临床疗效。方法 56例中晚期癌症患者按量定时给药,每次30～180mg口服,(12～24)h∕次。结果 CR19例(33.9%),PR35例(62.5%),MR2例(3.6%),总有效CR+PR54例(96.4%)。结论硫酸吗啡控释片(美施康定)效果良好,服用方便,副作用小,可作为治疗癌痛的首选药物。     

Theoretical π-π* absorption and circular dichroic spectra of cyclic dipeptides

The dipole interaction model, treated by the partially dispersive normal mode method, is used to calculate circular dichroic spectra of cyclo(Gly-Gly), cyclo (Ala-Gly), cyclo(Ala-Ala), cyclo(Pro-Gly), cyclo(Pro-Ala), cyclo(Pro-Val), cyclo (Pro-D-Val), and cyclo(Pro-Pro) in the amide π-π* absorption band near 190 nm. Assuming a standard backbone geometry, spectra which are in fair to good agreement wth experiment are obtained for these molecules. The spectra are predicted to be sensitive to conformations of Pro and Val side chains. The effects of dipeptide ring folding on calculated CD spectra are mostly consistent with those found by other workers, except that it is found that a planar ring conformation of cyclo (Ala-Ala) and cyclo (Ala-Gly) gives predicted spectra comparable to experiment. The same model gives theoretical absorption spectra consistent with available experimental data.     

Effects of Nitro-L-Arginine on Blood Pressure and Cardiac Index in Anesthetized Rats: A Pharmacokinetic-Pharmacodynamic Analysis

Purpose. Nitric oxide synthase (NOS) inhibitors such as Nitro-L-arginine (L-NA) are being considered for the management of hypotension observed in septic shock. However, little information is available regarding the pharmacokinetic and pharmacodynamic properties of these agents. Our objective was to examine the relationships between L-NA plasma concentration and various hemodynamic effects such as cardiac index (CI), mean arterial pressure (MAP), and heart rate (HR) elicited by L-NA administration in rats. Methods. L-NA was infused at doses between 2.5 – 20 mg/kg/hr in anesthetized rats over one hour. Hemodynamic effects and plasma L-NA levels were determined. Results. Infusion of L-NA resulted in dose-dependent increases in MAP and systemic vascular resistance (SVR), decreases in CI, and minimal change in HR. The relationships between the hemodynamic effects and plasma L-NA levels were not monotonic, and hysteresis was observed. Using nonparametric analysis, the equilibration half-time (t_1/2,keo) between plasma L-NA and the hypothetical effect site was determined to be 51.5 ± 6.6 min, 42.4 ± 10.1 min, 43.4 ± 9.0 min for MAP, CI, and SVR, respectively (n = 14). The E_max and EC₅₀ values obtained were + 32.5 ± 8.4 and 2.6 ± 1.3 g/ml for MAP and –52.9 ± 15.6 and 3.7 ± 1.8 g/ml for CI, respectively. Conclusions. Although L-NA can bring about beneficial elevation of MAP, such effect is always accompanied by a stronger effect on CI depression. Dose escalation of L-NA may bring about detrimental negative inotropic effect and loss of therapeutic efficacy.     

HPLC法测定丝裂霉素C聚氰基丙烯酸正丁酯纳米粒中丝裂霉素C的含量

目的:建立高效液相色谱法测定丝裂霉素 C 聚氰基丙烯酸正丁酯纳米粒(MMC-PBCA-NP)中药物含量。方法:采用C_(18)柱(4.6 mm×150 mm,5 μm),以混合磷酸盐缓冲液-乙腈(85:15)为流动相,流速为1 mL·min~(-1),紫外检测器,检测波长为365 nm。结果:丝裂霉素 C(MMC)浓度在5～250 μg·mL~(-1)范围内与峰面积呈良好的线性关系,r=0.9998;平均回收率(n=6)为98.15%。结论:本法专属性强,操作简便,结果准确。适用于 MMC-PBCA-NP 的质量控制。     

洛美沙星体内外抗菌活性研究

洛美沙星对革兰氏阴性菌具有强的抑菌活力。对克氏肺炎杆菌的抗菌活性最强,MIC_(50)为0.12mg/L;对痢疾杆菌、产气杆菌、粘质沙雷氏菌、不动杆菌和枸椽酸杆菌的MIC_(50)分别为1和4mg/L。洛美沙星对肠细菌科细菌的活力比诺氟沙星和依诺沙星强2～16倍,明显地比丁胺卡那霉素、庆大霉素强。对金葡球菌MIC_(50)为1mg/L, MRSA对洛美沙星同样敏感。洛美沙星对表葡球菌、链球菌、粪链球菌及肺炎双球菌等的抗菌活性与地氟沙星相似,比诺氟沙星、依诺沙星、丁胺卡那霉素、庆大霉素和头孢三嗪分别强2～4倍。 洛美沙星对小鼠全身感染的疗效优于诺氟沙星。对大肠杆菌、克氏肺炎杆菌和绿脓杆菌感染小鼠iv的ED_(50)分别是0.74、0.13和3.45mg/kg, po的ED_(50)分别是0.94、1.46和6.20mg/kg。     

The pathogenesis of,and pharmacological treatment for,Canavan disease

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乙酰吉他霉素临床前药理学研究

乙酰吉他霉素对临床分离的革兰氏阳性球菌有较好的抑菌活力，其对金葡球菌、β－溶血性链球菌、表葡球菌的ＭＩＣ_（５０）分别为１、０．２２和４ｍｇ／Ｌ，对耐红霉素、青霉素的金葡球菌、表葡球菌半数以上较敏感，与吉他霉素相似，但其对革兰氏阴性菌无明显作用。乙酰吉他霉素对小鼠实验性细菌感染有明显保护作用。对金葡球菌、肺炎双球菌感染小鼠口服用药的ＥＤ_（５０）分别为７９．６和２５．１ｍｇ／ｋｇ。其疗效与吉他霉素、麦白霉素、乙酰螺旋霉素相似。乙酰吉他霉素小鼠１次口服的ＬＤ_（５０）＞１５ｇ／ｋｇ，与吉他霉素相比毒性无差异。     

大鼠溃疡性结肠炎模型的实验研究

目的对不同剂量的三硝基苯磺酸（ＴＮＢＳ）引起的大鼠溃疡性结肠炎（ＵＣ）模型进行观察和评价。方法采用一次性直肠注入大鼠ＴＮＢＳ（２５～１５０ｍｇ·ｋｇ－１）的３０％乙醇溶液，引起慢性炎症性肠疾病（ＩＢＤ），３ｗｋ后外死动物对各剂量下动物结肠的重量、髓过氧化物酶（ＭＰＯ）活性及组织形态学变化进行观察和评价。结果ＴＮＢＳ在１００～１５０ｍｇ·ｋｇ－１剂量下引起的ＵＣ肠壁明显增厚，炎症和溃疡至少维持７ｗｋ时间，ＭＰＯ活性值显著性升高，组织学检查发现粘膜及粘膜下层有大量中性粒细胞及淋巴细胞、巨噬细胞、纤维细胞浸润，肉芽组织及隐窝脓肿形成，５０ｍｇ·ｋｇ－１剂量时有一较轻度的损伤。２５ｍｇ·ｋｇ－１时对结肠的重量、ＭＰＯ活性及损伤指数都没有显著性改变（Ｐ＞０．０５）。结论用ＴＮＢＳ引起大鼠实验性ＵＣ，其溃疡和炎症维持一较长时间，这一病理特征为炎症性疾病防治药物的研究提供了条件；本模型的最佳剂量为１００ｍｇ·ｋｇ－１左右     

Protective role of exogenous α-lipoic acid (ALA) on hippocampal antioxidant status and memory function in rat pups exposed to sodium arsenite during the early post-natal period

The present work focussed on the effect of exogenous α-lipoic acid (ALA) administration on retention memory and oxidative stress markers in the hippocampus subsequent to early post-natal exposure of rat pups to sodium arsenite (NaAsO₂). Wistar rat pups were divided into the control groups receiving either no treatment (Ia) or distilled water by intraperitoneal route (i.p.) (Ib) and the experimental groups receiving either NaAsO₂ alone (1.5 and 2.0?mg/kg body wt.) (IIa, IIb) or NaAsO₂ (1.5 and 2.0?mg/kg body wt.) followed by ALA (70?mg/kg body wt.) (IIIa, IIIb) (i.p.) from post-natal day (PND) 4–15. The initial and retention transfer latency (ITL and RTL) was determined on PND 14 and 15 using elevated plus maze. The animals were sacrificed by cervical decapitation (PND 16) and the brains were obtained. The dissected out hippocampus was processed for estimation of oxidative stress markers, glutathione (GSH), and superoxide dismutase (SOD). NaAsO₂ exposure resulted in longer RTL in animal groups IIa and IIb, thereby suggestive of arsenic-induced impairment in retention memory. RTL was significantly shorter in animal groups (IIIa, IIIb) receiving ALA following NaAsO₂, thereby suggestive of improvement in retention memory. GSH and SOD levels were significantly decreased in animals receiving NaAsO₂ alone as against group Ib and administration of ALA following NaAsO₂ increased the levels of hippocampal GSH and SOD. These observations are suggestive of the role of exogenous ALA in ameliorating the adverse effects induced by NaAsO₂ exposure of rat pups on retention memory and oxidative stress markers.     

Dinoflagellate polyether within the yessotoxin, pectenotoxin and okadaic acid toxin groups: Characterization, analysis and human health implications

Diarrhetic Shellfish Poisoning (DSP) is a specific type of food poisoning, characterized by severe gastrointestinal illness due to the ingestion of filter feeding bivalves contaminated with a specific suite of toxins. It is known that the problem is worldwide and three chemically different groups of toxins have been historically associated with DSP syndrome: okadaic acid (OA) and dinophysistoxins (DTXs), pectenotoxins (PTXs) and yessotoxins (YTXs). PTXs and YTXs have been considered as DSP toxins because they can be detected with the bioassays used for the toxins of the okadaic acid group, but diarrhegenic effects have only been proven for OA and DTXs. Whereas, some PTXs causes liver necrosis and YTXs damages cardiac muscle after intraperitoneal injection into mice. On the other hand, azaspiracids (AZAs) have never been included in the DSP group, but they cause diarrhoea in humans. This review summarizes the origin, characterization, structure, activity, mechanism of action, clinical symptoms, method for analysis, potential risk, regulation and perspectives of DSP and associated toxins produced by marine dinoflagellates.     

Latent role of in vitro Pb exposure in blocking Aβ clearance and triggering epigenetic modifications

Both β-amyloid (Aβ) catabolism and epigenetic regulation play critical roles in the onset of neurodegeneration. The latter also contribute to Pb neurotoxicity. The present study explored the role of epigenetic modifiers and Aβ degradation enzymes in Pb-induced latent effects on Aβ overproduction in vitro. Our results indicated that in SH-SY5Y cells exposed to Pb, the expression of NEP and IDE remained declined during the recovery period, accompanied with abnormal increase of Aβ_1-42 and amyloid oligomer. A disruption of selective global post-translational histone modifiers including the decrease of H3K9ac and H4K12ac and the induction of H3K9me2 and H3K27me2 dose dependently was also showed in recovery cells. Moreover, histone deacetylase inhibitor VPA could attenuate latent Aβ accumulation and HDAC activity induced by Pb, which might be by regulating the expression of NEP and IDE epigenetically. Overall, our results suggest sustained reduction of NEP and IDE expression in response to Pb sensitizes recovery SH-SY5Y cells to Aβ accumulation; however, administration of VPA is demonstrated to be beneficial in modulating Aβ clearance.