丁螺环酮与阿米替林治疗抑郁症60例

应用丁螺环酮治疗抑郁症患者30例，并与应用阿米替林的患者进行比较。两组疗效比较相似，丁螺环酮显效时间晚于阿米替林，但副作用较阿米替林少。提示丁螺环酮治疗抑郁症有效且副作用小，安全性较好。     

丁螺环酮与阿米替林治疗抑郁症60例

应用丁螺环酮治疗抑郁症患者30例,并与应用阿米替林的患者进行比较。两组疗效比较相似,丁螺环酮显效时间晚于阿米替林,但副作用较阿米替林少。提示丁螺环酮治疗抑郁症有效且副作用小,安全性较好。     

丁螺环酮与阿米替林治疗伴焦虑症状的抑郁症对照研究

目的 评价丁螺环酮和阿米替林治疗伴焦虑症状抑郁症的临床疗效及副反应。方法按投币法随机将58例伴焦虑症状抑郁症患者分为丁螺环酮组和阿米替林组,其中脱落8例,资料完整者50例。丁螺环酮组(甲组)25例,其中男11例,女14例,年龄18～59a,平均29.5±9.77a;阿米替林组(乙组)25例,男10例,女15例,年龄18～54a,平均29.8±11.54a。两组患者的一般情况用t检验。甲组患者服用丁螺环酮,初始剂量10mg·d～1,视病情及躯体情况渐增加剂量,最高剂量80mg·d～1。乙组患者服用阿米替林,初始剂量50mg·d～1,视病情及躯体情况渐增加剂量,最高剂量250mg·d-1。疗程均为6w。疗效观察指标:(1)治疗前后分别进行汉密顿焦虑量表(HAMA)、汉密顿抑郁量表(HAMD)、副反应量表(TESS)评定,各量表均由两名高年资精神科医师共同评定,总体疗效按痊愈、显进、进步和无效或恶化4级评定(其中痊愈加显进为显效,显进加进步为有效)。评定标准为量表减分率>75％为显效,50～75％为进步,<25％为无效,在治疗前及治疗后各进行血常规、尿常规、肝功能、心电图、肾功能检查。结果丁螺环酮治疗抑郁症状的疗效与阿米替林相似,治疗焦虑症状的疗效优于阿米替林,且副作用小。结论对于伴有焦虑症状的抑郁症患者,丁螺环酮可作为首选药物。     

丁螺环酮与劳拉西泮治疗焦虑症的临床分析

目的比较丁螺环酮与劳拉西泮治疗焦虑症的疗效。方法将符合条件的患者33例，随机分为两组：丁螺环酮组18例（男性11例，女性7例，予以丁螺环酮15mg，口服，3次／d，4周为一个疗程），劳拉西泮组15例（男性9例，女性6例，予以劳拉西泮2mg，口服，3次／d，4周为一个疗程），两组对比疗效。结果丁螺环酮组有效16例，显效1例，总有效率88．8％；劳拉西泮组有效14例，无效1例，总有效率91％。两组间疗效差异无显著性（P〉0．05）。丁螺环酮组未见严重不良反应。劳拉西泮组有6例嗜睡，1例眩晕。结论丁螺环酮与劳拉西泮疗效相同，均无严重的不良反应，但劳拉西泮的镇静、嗜睡作用较丁螺环酮明显。而上药在抗焦虑作用方面相同。丁螺环酮更适合用于非住院患者的治疗，有利于提高患者对治疗的依从性，从而达到更好的治疗效果。     

丁螺环酮与盐酸马普替林治疗抑郁症对照研究

目的评价丁螺环酮与盐酸马普替林治疗抑郁症的临床疗效和不良反应。方法对56例抑郁症患者随机分成2组,分别用丁螺环酮联合盐酸马普替林治疗和单用盐酸马普替林治疗,疗程6周。采用汉密顿抑郁量表（HAMD）、汉密顿焦虑量表（HAMA）评定疗效,用不良反应量表（TESS）评定不良反应。结果治疗6周后联合用药组HAMD和HAMA评分显著低于单用药组;在第2、6周末联合用药组的治疗有效递增显著高于单用药组。2组不良反应相仿。结论丁螺环酮联合盐酸马普替林治疗抑郁症有良好的疗效。     

九味镇心颗粒联合丁螺环酮治疗精神分裂症患者药源性焦虑的疗效观察

目的探讨九味镇心颗粒联合丁螺环酮治疗精神分裂症患者药源性焦虑的疗效。方法精神分裂症伴药源性焦虑患者90例,随机分为丁螺环酮组(n=30),九味镇心颗粒组(n=30),九味镇心颗粒联合丁螺环酮组(n=30),采用汉密尔顿焦虑量表(HAMA)评定疗效,副反应量表(TESS)评定安全性。结果治疗第2周,九味镇心颗粒联合丁螺环酮组HAMA评分低于丁螺环酮组比较,差异有统计学意义(P<0.05),治疗第4、6周,九味镇心颗粒联合丁螺环酮组HAMA评分低于丁螺环酮组(P<0.05),九味镇心颗粒联合丁螺环酮组有效率(97.0%)高于丁螺环酮组(80.0%),差异有统计学意义(P<0.05)。结论九味镇心颗粒联合丁螺环酮治疗精神分裂症患者药源性焦虑有明确的治疗效果,耐受性较好。     

丁螺环酮改善脑卒中后共济失调症状的临床研究

目的观察丁螺环酮对改善脑卒中后共济失调症状的临床疗效。方法选取有共济失调症状的脑卒中患者30例口服丁螺环酮治疗，治疗前后分别用共济失调量表进行评定，与未服丁螺环酮的对照组30例进行比较。结果治疗组在平衡性和协调性方面与对照组比较有明显改善（P〈0．01）。结论丁螺环酮短期内可有效改善脑卒中后共济失调症状。     

丁螺环酮与地西泮治疗焦虑症的双盲对照

目的:比较丁螺环酮与地西泮治疗焦虑症的疗效及不良反应。方法:采用随机双盲对照观察的方法,分为丁螺环酮组23例(男11例,女12例,年龄38±13α),丁螺环酮片15mg tid po;4Wk,为一个疗程。地西泮组22例(男9例,女13例,年龄40±11α),地西泮7.5mg tid,po;4wk为一个疗程。治疗结果:丁螺环酮组有效率86%,地西泮组90%,Ridit分析P>0.05。药物不良反应发生率地西泮组高于丁螺环酮组,但反应轻微不影响治疗。结论:丁螺环酮与地西泮比较疗效相同,不良反应少。     

丁螺环酮和阿普唑仑治疗焦虑症的对照研究

目的：评价丁螺环酮治疗焦虑症的临床疗效和不良反应。方法：对60例焦虑症患者，分别应用丁螺环酮和阿普唑仑进行对照治疗，疗程4周采用Hamihon焦虑量表（HAMA）和副反应量表（TESS）评定疗效和不良反应。结果：丁螺环酮与阿普唑仑对焦虑症的疗效差异无显著性。两药不良反应相仿。结论：丁螺环酮治疗焦虑症有效，不良反应轻。     

氯丙咪嗪合用丁螺环酮治疗强迫症40例

目的:探讨氯丙咪嗪合用丁螺环酮治疗强迫症的疗效。方法:将40例强迫症患者分为氯丙咪嗪合并丁螺环酮组和单用氯丙咪嗪组,治疗8周。采用强迫量表(Y-BOCS)、汉密顿焦虑量表(HAMA)、汉密顿抑郁量表(HAMD)评定疗效。结果:治疗结束时两组Y-BOCS、HAMA、HAMD的评分均显著下降,尤其合用丁螺环酮为明显。结论:氯丙咪嗪合用丁螺环酮治疗强迫症可以增强疗效。     

Gas-chromatographic analysis for therapeutic concentrations of amitriptyline and nortriptyline in plasma, with use of a nitrogen detector.

We describe a gas-chromatographic procedure for the simultaneous determination of amitriptyline and its active metabolite, nortriptyline, in therapeutic concentrations in human plasma, with use of a nitrogen detector. Both drugs are extracted at pH 10.5 into hexane/isoamyl alcohol, back-extracted into dilute HCl, and re-extracted into hexane/isoamyl alcohol after alkalinization of the HCl. The solvent is evaporated and the residue gas-chromatographed. Protriptyline is used as the internal standard. As little as 5 mug of amitriptyline or nortriptyline can be detected per liter of plasma. The coefficients of variation, for a concentration of 200 mug/liter, are 4.6% and 4.3% within-day and 8.6% and 3.4% day-to-day for amitriptyline and nortriptyline, respectively. The procedure was applied to patients receiving therapeutic doses of both drugs and also to patients who had taken overdoses of amitriptyline.     

Prophylaxis of Migraine and Mixed Headache. A Randomized Controlled Study

SYNOPSIS
The three most commonly used modalities in the prophylactic treatment of headache, namely propranolol, amitriptyline and biofeedback training, were compared individually and in combination. Three hundred forty patients with migraine end 375 patients with mixed headache were randomly allotted to 8 therapeutic categories. The total duration of the study was 312 years and the therapeutic groups were evaluated for a period of 7 months including I month of pretreatment observation. Improvement was assessed by percentage of change in the average headache index during the last three months of evaluation from the pretreatment headache index. In the migraine group 273 patients completed the study. Improvement was significantly higher in patients receiving prophylactic treatment compared to control patients who were on abortive Ergotamine treatment. Propranolol plus biofeedback yielded the best results in the migraine group and addition of amitriptyline did not significantly change the percentage of improvement. Propranolol alone (62%) was significantly superior to amitriptyline (42%) (p < 0.01). The differences between propranolol alone and propranolol plus amitriptyline was not statistically significant.
In the mixed headache group 281 patients completed the study. The most effective treatment was combination of amitriptyline, propranolol and biofeedback training. Amitriptyline alone was superior to propranolol alone in the treatment of mixed headache (p<0.01). A combination of propranolol and amitriptyline was superior to either of those alone. Biofeedback, though by itself, did not appear to be the treatment of choice, significantly contributed to better results as an adjunct when it is combined with pharmacological agents. Concomitant use of propranolol and amitriptyline did not result in any adverse reactions or clinical incompatibility.     

Therapeutic plasma exchange in amitriptyline intoxication: Case report and review of the literature

Severe amitriptyline poisoning results in cardiac and neurological toxicity and continues to be a leading cause of significant morbidity and mortality both in children and adults. We present a case of severe amitriptyline poisoning successfully treated with plasma exchange. Due to high plasma protein binding property of amitriptyline, plasma exchange therapy should be considered in cases of severe amitriptyline intoxication as a life saving therapeutic modality.     

State-dependent block of voltage-gated Na+ channels by amitriptyline via the local anesthetic receptor and its implication for neuropathic pain

Amitriptyline is a tricyclic antidepressant, which also alleviates various pain syndromes at its therapeutic plasma concentration (0.36-0.90 microM). Accumulated evidence suggests that such efficacy may be due to block of voltage-gated Na(+) channels. The Na(+) channel alpha-subunit protein consists of four homologous domains (D1-D4), each with six transmembrane segments (S1-S6). The aims of this study were to locate the amitriptyline receptor in the Na(+) channel alpha-subunit and to compare the amitriptyline affinity in open, inactivated, and resting states of the Na(+) channel. Wild-type and mutant rat skeletal muscle alpha-subunit Na(+) channels were expressed in human embryonic kidney cells and assayed under whole-cell voltage clamp conditions. Our results indicate that the amitriptyline receptor overlaps with the local anesthetic receptor to a great extent in Na(+) channels. Residues N434 (at D1-S6), L1280 (D3-S6), and F1579 (D4-S6) may jointly form parts of the amitriptyline/local anesthetic receptor, with residue L1280 being most critical for amitriptyline binding. Open-channel block by amitriptyline was assessed in inactivation-deficient Na(+) channels and compared with the resting- and inactivated-channel block in wild-type channels. The open-channel block by amitriptyline has the highest affinity, with a 50% inhibitory concentration (IC(50)) of 0.26 microM. The inactivated-channel block by amitriptyline had a weaker affinity (0.51 microM), whereas the resting-channel displayed the weakest affinity (33 microM). We hypothesize that selective block of both persistent late openings and the inactivated state of neuronal Na(+) channel isoforms by amitriptyline also occurs at its therapeutic concentration and likely contributes to its efficacy in pain syndromes.     

中药汽雾透皮疗法治疗原发性纤维肌痛综合征前瞻性临床初步研究

目的 评价中药汽雾透皮疗法治疗纤维肌痛综合征（FMS）的临床疗效和安全性。方法 将132例患者随机分为对照组、汽疗组和联合组,三组均以心理干预为基础治疗,同时对照组服阿米替林治疗,汽疗组采用中药汽雾透皮疗法治疗,联合组采用中药汽雾透皮疗法和阿米替林联合治疗,三组在治疗4周、12周时以简化麦吉尔疼痛问卷（SFMPQ）、汉密尔顿抑郁量表（HAMD）、纤维肌痛影响问卷（FIQ）和压痛点计数评估疗效,同时观察记录不良反应。结果 三组治疗后SFMPQ中的所有分项得分、HAMD评分、FIQ总分较治疗前均有不同程度的改善（P＜0.01）,且联合组和汽疗组较对照组改善明显,差异有统计学意义（P＜0.05,P＜0.01）;汽疗组和联合组压痛点计数较治疗前显著减少（P＜0.01）,而对照组无变化（P＞0.05）;同组治疗12周与4周时比较,SFMPQ中的所有分项得分、HAMD评分、FIQ总分及压痛点计数差异均无统计学意义（P＞0.05）。不良反应发生率汽疗组小于对照组 （P＜0.01）,联合组与对照组比较差异无统计学意义（P＞0.05）。结论 中药汽雾透皮疗法可以有效治疗FMS,疗效与安全性优于阿米替林,二者联合可以显著提高疗效。     

Block of human heart hH1 sodium channels by amitriptyline

Amitriptyline is a tricyclic antidepressant used to treat major depression and various neuropathic pain syndromes. This drug also causes cardiac toxicity in patients with overdose. We characterized the tonic and use-dependent amitriptyline block of human cardiac (hH1) Na(+) channels expressed in human embryonic kidney cells under voltage-clamp conditions. Our results show that, near the therapeutic plasma concentration of 1 microM, amitriptyline is an effective use-dependent blocker of hH1 Na(+) channels during repetitive pulses (approximately 55% block at 5 Hz). The tonic block for resting and for inactivated hH1 channels by amitriptyline (0.1-100 microM) yielded IC(50) values (50% inhibitory concentration) of 24.8 +/- 2.0 (n = 9) and 0.58 +/- 0.03 microM (n = 7), respectively. Substitution of phenylalanine with lysine at the hH1-F1760 position, a putative binding site for local anesthetics, eliminates the use-dependent block by amitriptyline at 1 microM. The time constants of recovery from the inactivated-state amitriptyline block in hH1 wild-type and hH1-F1760K mutant channels are 8.0 +/- 0. 5 (n = 6) and 0.45 +/- 0.07 s (n = 6), respectively. A substitution at either hH1-F1760K or hH1-Y1767K significantly increases the IC(50) values for resting and inactivated states of amitriptyline, but the increase is much more pronounced with the hH1-F1760K mutation. Because these two residues were proposed to form a part of the local anesthetic binding site, we conclude that amitriptyline and local anesthetics interact with a common binding site. Furthermore, at therapeutic concentrations, the ability of amitriptyline to act as a potent use-dependent blocker of Na(+) channels may, in part, explain its analgesic actions.     

Pharmacokinetic-pharmacodynamic modeling of buspirone and its metabolite 1-(2-pyrimidinyl)-piperazine in rats

The objective of this investigation was to compare the in vivo potency and intrinsic activity of buspirone and its metabolite 1-(2-pyrimidinyl)-piperazine (1-PP) in rats by pharmacokinetic-pharmacodynamic modeling. Following intravenous administration of buspirone (5 or 15 mg/kg in 15 min) or 1-PP (10 mg/kg in 15 min), the time course of the concentrations in blood were determined in conjunction with the effect on body temperature. The pharmacokinetics of buspirone and 1-PP were analyzed based on a two-compartment model with metabolite formation. Differences in the pharmacokinetics of buspirone and 1-PP were observed with values for clearance of 13.1 and 8.2 ml/min and for terminal elimination half-life of 25 and 79 min, respectively. At least 26% of the administered dose of buspirone was converted into 1-PP. Complex hypothermic effects versus time profiles were observed, which were successfully analyzed on the basis of a physiological indirect response model with set-point control. Both buspirone and 1-PP behaved as partial agonists relative to R-(+)-8-hydroxy-2-(di-n-propylamino)tetralin (R-8-OH-DPAT) with values of the intrinsic activity of 0.465 and 0.312, respectively. Differences in the potency were observed with values of 17.6 and 304 ng/ml for buspirone and 1-PP, respectively. The results of this analysis show that buspirone and 1-PP behave as partial 5-hydroxytryptamine(1A) agonists in vivo and that following intravenous administration the amount of 1-PP formed is too small to contribute to the hypothermic effect.     

氟西汀治疗老年抑郁症的疗效观察

目的:探讨氟西汀治疗老年抑郁症的疗效及安全性。方法:56例老年抑郁症患者随机分为两组:A组和B组,每组各28例。A组采用氟西汀治疗,B组采用阿米替林治疗,两组疗程均为6周。两组疗效评定采用汉密顿抑郁量表(HAMD),两组副反应评定采用副反应量表(TESS)。结果:A组治疗后第2、4、6周末HAMD评分与B组比较,无显著性差异(P>0.05),A组治疗后第2、4、6周末TESS评分明显低于B组(P<0.05)。A组总有效率为78.57%,B组总有效率为71.43%,两组比较,无显著性差异(P>0.05)。结论:氟西汀可作为治疗老年抑郁症的首选药物。