盐酸多塞平乳膏人体透皮吸收试验

目的 :比较进口与国产5 %盐酸多塞平乳膏的人体透皮吸收效果。方法 :采用高效液相色谱法测定血药浓度 ,8位健康男性受试者按交叉试验设计 ,以进口的5 %盐酸多塞平乳膏为对照品 ,对比研究国产5 %盐酸多塞平乳膏的人体透皮吸收效果。结果 :连续8d于受试者前臂皮肤涂抹相同剂量的盐酸多塞平乳膏试验品和对照品后进行测定 ,两组血药浓度均较低 ,无显著性差异。结论 :国产5 %盐酸多塞平乳膏的人体透皮吸收效果可达国外同类品种水平 ,且安全、有效     

Low-dose doxepin for the treatment of insomnia: emerging data

Background: Doxepin is a tricyclic compound that has been used extensively for the treatment of depressive and anxiety disorders for approximately thirty years. It was noted early to have sedative effects and assist with the improvement of disrupted sleep patterns, but in higher antidepressant doses it was also noted to have significant anticholinergic and antinoradrenergic properties. These properties led to significant dose-limiting side effects, which at times precluded its effective use. Recently, doxepin has seen renewed interest in low doses as an H1 specific antagonist in sleep disorders. Objective: The review seeks systematically to examine currently published data on the use of doxepin for the treatment of insomnia, and its pharmacological basis. Methods: Medline articles showing from a search of ‘doxepin and insomnia’ were included in the review. Results/conclusion: Currently available data support the use of low-dose doxepin as preferential H1 antagonist for the treatment of primary insomnia. There are likely preferential effects upon sleep maintenance insomnia compared with sleep initiation given the role of histamine in the sleep–wake cycle.     

In vitro genotoxic and cytotoxic effects of doxepin and escitalopram on human peripheral lymphocytes

Antidepressants are drugs used for the treatment of many psychiatric conditions including depression. There are findings suggesting that these drugs might have genotoxic, carcinogenic, and/or mutagenic effects. Therefore, the present in vitro study is intended to investigate potential genotoxic and cytotoxic effects of the antidepressants escitalopram (selective serotonin reuptake inhibitor) and doxepin (Tricyclic antidepressant) on human peripheral lymphocytes cytokinesis-block micronucleus (CBMN), sister chromatid exchange (SCE), and single cell gel electrophoresis (alkaline comet assay) were used for the purpose of the study. In the study, four different concentrations of both drugs (1, 2.5, 5, and 10?µg/mL) were administered to human peripheral lymphocytes for 24?h. The tested concentrations of both drugs were found to exhibit no cytotoxic and mitotic inhibitory effects. SCE increase caused by 5 and 10?µg/mL of escitalopram was found statistically significant, while no statistically significant increase was observed in DNA damage and micronucleus (MN) formation. Moreover, the increase caused by doxepin in MN formation was not found statistically significant. Besides, 10?µg/mL of doxepin was demonstrated to significantly increase arbitrary unit and SCE formation. These findings suggest that the investigated concentrations of escitalopram and doxepin were non-cytotoxic but potentially genotoxic at higher concentrations.     

盐酸多塞平异构体的非水毛细管电泳分离

目的　用非水毛细管电泳法分离盐酸多塞平异构体。方法　采用未涂层石英毛细管柱 (50 μm× 47cm ,有效分离长度为 40cm) ,以用 2 0 0mmol·L- 1 醋酸铵的甲醇 乙腈 (95∶5)溶液 (含 3 .0 %冰醋酸 )为运行缓冲液 ,压力进样 ,时间 4s,运行电压为 2 5kV ,检测波长为 2 54nm。结果　方法分离效率高 ,精密度和回收率较好 ,所选浓度范围内线性关系良好 ,r值为 0 .9998。结论　方法简单可靠 ,分析时间短 ,可有效分离盐酸多塞平异构体     

Maprotiline and doxepin in the treatment of depression. A double-glind multicentre comparison.

Maprotiline (Ludiomil) and doxepin were compared in the treatment of depression in a double-blind multicentre trial. Four centres and 95 in- and out-patients took part in the trial. The severity of depression was evaluated with the aid of a visual analogue scale and nine target symptoms. Both maprotiline and doxepin diminished neurotic as well as psychotic depression significantly. The mean time of onset of action was 7.0 days in the maprotiline group and 7.7 days in the doxepin group. No statistically significant differences in antidepressive effect were found between the treatments. Two patients in the maprotiline group and four patients in the doxepin group discontinued the treatment because of unwanted effects, one patient in each group because of lack of efficacy and nine patients due to reasons not related to the treatment.     

Radioimmunoassay for Doxepin and Desmethyldoxepin

Abstract: A simple and sensitive radioimmunoassay (RIA) for the determination of doxepin and desmethyldoxepin in plasma or serum has been developed using a previously reported antiserum to the tricyclic anti-depressants. Before assay, doxepin is separated from desmethyldoxepin with selective extraction at different pH values enabling each to be measured specifically. ³H-imipramine is used as tracer. By using the extraction procedure doxepin and desmethyldoxepin concentrations can be measured down to 9 nmol/l from a 0.1 ml sample. If necessary, sensitivity can be doubled by taking a 0.2 ml sample to the extraction. Recoveries of doxepin and desmethyldoxepin were quantitative when the drugs were added at different concentrations to normal, pooled human plasma and the inter- and intra-assay coefficients of variation did not exceed 9%. The concentrations obtained from patient samples by the present RIA correlated well with those by high-pressure liquid chromatography. The RIA was also shown to be useful in pharmacokinetic single dose studies with doxepin.     

脐部给药的多塞平栓研制及应用

目的：研制透皮制剂多塞平栓,考察其治疗各型急、慢性荨麻疹的临床疗效。方法：多塞平以甘油明胶为质,氮酮为促透剂,制成栓剂,经脐部给药,观察５０个病例,与口服多塞平片作对照,观察临床疗效。结果：多塞平栓治疗各型急、慢性荨麻疹,总有效率为９４．０％,经统计学分析,Ｐ〈０．０５,差异具显著性。结论：本品制备工艺可行,疗效确切,用药剂量小,无副作用,具有进一步研究、开发的价值。     

西沙必利、比沙可啶、多塞平联合治疗功能性便秘

目的 :比较西沙必利、比沙可啶、多塞平联合治疗与单用西沙必利对功能性便秘的疗效。方法 :6 0例临床诊断功能性便秘病人 ,随机分 2组 ,西沙必利组 (对照组 ) ,d 1～ 90单用西沙必利 10mg ,tid ;西沙必利、比沙可啶、多塞平组 (治疗组 )d 1～ 2 :西沙必利 10mg ,tid、比沙可啶 10mgqd ;d 3～ 30 :西沙必利 10mg ,tid ,多塞平 12 .5mg ,tid ;d 31～90 :西沙必利 10mgtid。结果 :对照组与治疗组治疗后 1wk ,1,2 ,3mo 2组便秘缓解率分别为 2 3%与 5 0 % ,33%与 6 0 % ,5 0 %与 80 % ,5 7%与 90% ,(P <0 .0 5 )。 2组病人治疗后均无不良反应。结论 :西沙必利、比沙可啶、多塞平联合治疗功能性便秘比单用西沙必利疗效好     

国产西酞普兰联用多塞平治疗广泛性焦虑障碍的开放性研究

目的：通过国产西酞普兰和多塞平低剂量联用的开放性治疗,探讨其对广泛性焦虑障碍（GAD）的效果及安全性。方法：以西酞普兰20mg/d[原服有选择性5-羟色胺（5-HT）再回收抑制剂者药物及剂量保持不变]加用多塞平（75-125mg/d）,并与同期志愿接受文拉法辛治疗者对照比较。选择Hamilton焦虑量表（HAMA）评定治疗前,治疗后1、2、4、6周分值变化,以基线减分率评定6周治疗效果,副反应量表（TESS）评定治疗过程中的不良反应发生率。结果：两组完成6周治疗者50例和30例,脱落率分别为10.7%和9.1%,P=0.70,6周基线减分率差异均无统计学意义;有效率分别为92.0%、93.3%,P=0.83,两法效果差异经Ridit值比较也无统计学意义。HA-MA评定中,精神性焦虑因子减分差值在4-6周时有重要统计学意义。靶症状结合因子减分差值分析中,联用组的失眠、记忆/注意障碍和呼吸系统症状在4-6周时较文拉法辛组改善更为明显（P〈0.05-0.01）。不良反应中按SS集分析,联用组有较高的口干、便秘及体重增加现象。结论：西酞普兰等选择性5-HT再回收抑制类药物与抑制NE再摄取作用的多塞平联用对GAD显示出与SNRIS相同的效果,且安全性较高。因治疗成本不足文拉法辛的1/3,对低收入病员群体是一种更为实际的治疗方法。     

红霉素、盐酸多虑平联合治疗糖尿病胃轻瘫疗效观察

目的:探讨红霉素、盐酸多虑平联合治疗糖尿病胃轻瘫的疗效及安全性。方法:102 例糖尿病胃轻瘫患者,随机分为两组。治疗组52例,给予注射用红霉素1.0 g加入5%葡萄糖液500 ml中,同时内加短效胰岛素6~12 U,静脉滴注,1次/d;多虑平片12.5 mg,3次/d,口服。对照组50例,给予多潘立酮片10 mg,3次/d,口服。疗程均为半个月,治疗前后进行血、尿常规,肝、肾功能及心电图检查,详细记录症状的变化及不良反应,随访3 个月。结果:两组总有效率,治疗组高于对照组,差异具有显著性(P<0.05),复发率治疗组低于对照组,但差异无显著性(P>0.05)。结论:糖尿病胃轻瘫的发病往往与情绪因素有关,用红霉素联合多虑平进行治疗安全有效,且不良反应少。