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.     

A double-blind comparison of mianserin and maprotiline in depressed medically ill elderly people

A double-blind, randomized 4-week mianserin vs maprotiline trial was conducted in 48 depressed geriatric medical inpatients. The drug dosages were up to 90 mg of mianserin and up to 150 mg of maprotiline per day. Efficacy was measured by the Geriatric Depression Scale, the Hopkins Symptom Check List depression subscale and the Clinical Global Impression Scale. The overall dropout figure was 27% of the sample. Side effects were relatively similar in the two treatment groups and suggested a safety profile somewhat better than that of the first-generation antidepressants. Mianserin showed some advantages in efficacy over maprotiline, particularly by the 4th week of the trial, but the overall figures of treatment responders were rather small (Geriatric Depression Scale: mianserin 48%, maprotiline 30%). Clinical trials vs placebo are needed to clarify the role of antidepressant pharmacotherapy in depressed geriatric medical inpatients.     

Long-term-effects of two principally different antidepressant drugs on saliva secretion and composition

Abstract – In a double-blind, controlled, cross-over trial on 10 healthy volunteers, the effects of daily doses of maprotiline (75 mg) and zimelidine (100 mg) over a 14-day period were tested on saliva secretion rate and saliva composition. Based on current knowledge of salivary gland physiology and the difference in specificity between the two drugs, differences in salivary gland response could be expected. Since both drugs have anticholinergic effects which influence saliva secretion rate, the measured component concentrations had to be recalculated with regard to dependencies of secretion rate. Maprotiline, but not zimelidine, caused strong inhibition of secretion rate and accommodation ability. Maprotiline consistently caused around 50% increases in concentrations of the following saliva components: protein, amylase, fucose, hexose, sialic acid and potassium. The effects of zimelidine were less pronounced and resulted in initial increases of most organic components. 14 and 18 h after the intake of the drug these increases had disappeared and some of the components instead showed decreased concentrations. The results are consistent with current theories about facilitated serotoninergic and noradrenergic transmissions during treatment with antidepressants.     

Serum Levels of Maprotiline and Its Adverse Effects on Depressed Patients

Abstract: The relationships between the side effects of maprotiline (MPT) andthe serum concentration of MPT and desmethylmaprotiline (DMPT) were investigated with 27 blood samplings in 15 depressed inpatients. There were significant correlations between the side effects and serum levels of MPT and DMPT. Mild side effects frequently occurred at levels of more than 130 ng/ml of MPT and 70 ng/ml of DMPT. At more than 220 ng/ml of the MPT levels and 110 ng/ml of DMPT levels, severe side effects occurred. Nearly sigmoidalserum level/side effect response curves occurred with both compounds.     

Simultaneous Measurement of Various Antidepressants in the Plasma of Depressed Patients by High Performance Liquid Chromatography

Abstract: A simultaneous analytical method was reported for measuring the plasma levels of amitriptyline, imipramine, clomipramine, maprotiline, nor-triptyline, desipramine, desmethylclomipramine, desmethylmaprotiline and amoxapine by high performance liquid chromatography (HPLC). The total plasma levels of each parent drug plus its desmethyl metabolite were monitored in 29 depressed patients administered with amitriptyline, maprotiline or amoxapine using the present analytical method. There were significant linear correlations between the dose per kg body weight and the total plasma levels with amitriptyline and maprotiline, but no such correlation was found with amoxapine. The ratios of total plasma levels to dose per kg body weight of these three drugs were lower in outpatients than in inpatients. These results indicate that the monitoring of plasma levels of antidepressants is useful in treating depression.     

Comparison between a serotonin and a noradrenaline reuptake blocker in the treatment of depressed outpatients. Biochemical aspects

Seventy-five outpatients with major depressive disorder (RDC) were randomly referred to treatment with a dominant 5-HT reuptake blocker (zimeldine, 100 mg b.i.d.) or a dominant NA reuptake blocker (maprotiline 75 mg b.i.d.). Pretreatment biochemical, pharmacodynamic and pharmacokinetic variables were studied and related to the treatment outcome with the two drugs. Female responders to the dominant 5-HT reuptake blocker were characterized by low pretreatment accumulation of 14C-5-HT in rat synaptosomes, when incubated in patient plasma. Among zimeldine responders there was a relationship between antidepressive effect and steady-state concentrations of zimeldine and norzimeldine. These findings support the hypothesis of a subgroup of depression characterized by serotonin disturbance.     

Comparison of the serum protein binding of maprotiline and phenytoin in uraemic patients on haemodialysis

Summary The serum protein binding of maprotiline and phenytoin has been compared in a group of 22 uraemic patients receiving haemodialysis. Determination of protein binding was carried out in vitro using equilibrium dialysis at 37°C and¹⁴C-labelled drug. The mean percentage unbound maprotiline found in patients (10.0%, SD 2.5) was not significantly different from that obtained in healthy volunteers (mean 10.5%, SD 1.0). However, there was a significantly increased variability in binding in patients compared with healthy subjects. The mean percentage unbound phenytoin in the same patients (22.2%, SD 3.3) was significantly greater than that obtained in healthy control subjects (12.5%, SD 0.6). Although there was no correlation between maprotiline and phenytoin binding and serum concentrations of ₁-acid glycoprotein, there was a significant correlation between percentage unbound maprotiline and serum albumin concentrations. The findings indicate that the binding of this tricyclic antidepressant is essentially normal in uraemia, although there may be increased interindividual variability in the free fraction of drug.     

小剂量马普替林对更年期女性高血压患者的辅助治疗

目的 研究小剂量抗抑郁药马普替林25mg对更年期女性的高血压患者协同降压的疗效.方法 对更年期女性高血压患者98例随机分为实验组(常规降压+马普替林)和对照组(常规降压+安慰剂)各49例,进行SCL-90评分并随访15d,比较两组血压的下降幅度、降压显效率、降压药物的数量以及治疗前后SCL-90评分的差异.结果 ①实验组在治疗10d后至结束时,血压的下降幅度[实验组:(130.6±13.5)/(80.7±10.3)mm Hg比对照组:(150.0±14.5)/(94.5±12.6)mm Hg,P＜0.011和降压显效率(86.8 vs 59.4%,P＜0.01)较对照组明显提高.②治疗第5周后,对照组联合使用的高血压药物的数量明显较实验组明显增多(3.5±0.6 vs1.8±0.6,P＜0.01).③实验组治疗后的SCL-90的焦虑、抑郁、躯体化症状因子评分较治疗前明显下降,对照组有轻度下降但仍明显高于常模.结论 小剂量抗抑郁药马普替林协同治疗更年期女性高血压患者的疗效显著,可以明显提高降压的有效率和提前显效时间、减少降血压药物的数量,同时显著降低高血压患者的焦虑、抑郁和躯体化症状的水平.     

中药解郁丸与麦普替林治疗抑郁症的疗效对照观察

目的 观察中药解郁丸治疗抑郁症的临床疗效、不良反应及安全性。方法 通过随机对照试验,共纳入中药组(解郁丸)28列,对照组(麦普替林)29例,于用药前及用药后14、28、42天分别采用Hamilton抑郁量表(HAMD)、抑郁自评量表(SDS)、焦虑自评量表(SAS)和临床总体印象量表(CGI)评定药物疗效,用Asberg副反应量表评定不良反应,结果 解郁丸对抑郁症治疗有效,愈显率为78．6％,与麦普替林(82．8％)相当(P>0．05);解郁丸与麦普替林治疗后HAMD、SDS和SAS分数均明显低于治疗前(P<0．01),两组间比较差异无显著性(P>0．05)。治疗后解郁丸的Asberg副反应量表分数明显低于麦普替林(P<0．01),中药解郁丸疗效指数显著高于麦普替林(P<0．01)。结论 解郁丸治疗抑郁症疗效与麦普替林相当,不良反应明显少于麦普替林。