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PubMed1980

Bioavailability and kinetics of maprotiline.

Six male subjects received simultaneously single 50-mg oral doses of a maprotiline hydrochloride tablet and a trideuterated maprotiline hydrochloride aqueous solution. No side effects or other problems were encountered. The blood levels of unlabeled and isotope-labeled maprotiline for each subject were essentially superimposable. Peak levels, averaging about 50 ng/ml, were attained between 8 and 24 hr after drug. The biologic t1/2 (beta-phase) averaged 58 hr for the unlabeled and 60.5 hr for the labeled drug. The total areas under the curves (extended to time infinity) averaged 3,862 and 3,944 ng . hr/ml for maprotiline and trideuterated maprotiline, respectively (differences between the two are not significant). At the 95% degree of confidence the Westlake confidence limits show less than 10% differences between the formulations with respect to area under the curve data (calculated both to 168 hr and extended to time infinity), peak blood levels, and biologic t1/2s. There were no differences between formulations with respect to times of peak concentrations. Estimates were made for apparent volumes of distribution (about 1,000 l), apparent blood clearance (about 14 l/hr), lag times (about 1.42 hr for tablets and 1.31 hr for solution), and absorption rate constants (about 0.34 hr-1 for the tablets and 0.42 hr-1 for the solution).

Adult↗
PubMed1993

Efficacy and safety of moclobemide compared with maprotiline in treatment of major depressive disorder. A double-blind multicenter study with parallel groups.

This report describes the results obtained in a double-blind, six week, prospective, randomized multicenter study. The efficacy, tolerability, and safety of moclobemide (300-600 mg/d) were compared to those of maprotiline (75-150 mg/d) in parallel groups of patients with a Major Depressive Episode (DS-III). In addition, participants were required to have a minimum baseline total score of 17 on the 17-item Hamilton Depression Rating Scale (HAMD) (no run-in), 115 male or female outpatients (aged over 18 years) were randomly allocated to moclobemide t.i.d. (n = 58) or to maprotiline t.i.d. (n = 57). Demographic and illness characteristics were comparable in both treatment groups upon study entry. During the study the patients were not required to avoid tyramine-rich foods but they were advised to take trial medication after meals. Patients were assessed for efficacy and tolerability on days 4, 11, 18, 25, 32, 39, and 46. Efficacy was judged primarily on the HAMD, the investigator's final overall assessment, and on the number of premature terminations associated with insufficient efficacy. No significant difference was observed between both groups. The mean % reduction of the HAMD at the end of treatment was 62.2 in the moclobemide group and 61.2 in the maprotiline group. The percentage of patients in whom efficacy was globally judged as "good" or "very good" was 63.0% in the moclobemide group and 58.5% in the maprotiline group. Seventeen percent moclobemide patients and 21% of maprotiline patients did not complete because of insufficient efficacy.(ABSTRACT TRUNCATED AT 250 WORDS)

Adolescent↗
PubMed1994

Comparison of the efficacy and tolerability of moclobemide and maprotiline in depressed patients treated by general practitioners.

We report the results of a multicenter, double-blind study conducted in a general practice setting, in which the efficacy and tolerability of moclobemide, a new antidepressant drug of the reversible inhibitor of monoamine oxidase type A class, were compared with those of maprotiline, a noradrenaline reuptake inhibitor often prescribed in the general practice setting. Participating general practitioners were required to make differential diagnoses of depressive disorders according to DSM-III criteria and then quantitatively assess the efficacy of treatment using the Hamilton Depression Rating Scale (HDRS) and the Zung self-rating depression scale (Zung SDS). One hundred thirty outpatients (mean age 48 years) with major depression according to DSM-III were randomized to receive either moclobemide 300 mg or maprotiline 75 mg daily for 4 weeks. From day 8, dosages were increased if necessary up to a maximum of 400 mg of moclobemide or 100 mg of maprotiline. The results showed that moclobemide was as effective as maprotiline (HDRS, Zung SDS); moclobemide appeared to have the same antidepressant and anxiolytic activity, but a stronger drive-enhancing effect. Moclobemide was the better-tolerated drug, producing fewer side effects than maprotiline did: in particular, fewer instances of somnolence and dry mouth. The good tolerability of the compound was confirmed by the qualitative assessments of the study physicians.

Antidepressive Agents↗
PubMed1983

Placebo-controlled trial of mianserin and maprotiline in primary depressive illness: a preliminary report.

1 Preliminary results of a double-blind placebo-controlled trial of mianserin and maprotiline carried out in 58 outpatients with primary depressive illness are reported. 2 Patients received six weeks' treatment with 30 to 90 mg mianserin, 75 to 225 mg maprotiline or one to three capsules of placebo, all medication being taken at night. 3 There were statistically significant improvements in each treatment group and a better response to mianserin than to placebo or maprotiline on the Hamilton Rating Scale for Depression, after one week's treatment. 4 Neither mianserin nor maprotiline was superior to placebo after two or four weeks' treatment and relatively few patients completed six weeks' treatment because of a generally unsatisfactory response. 5 Unwanted effects were not particularly troublesome, though mianserin and maprotiline caused more drowsiness and blurred vision than did placebo, while maptrotiline produced more constipation than either of the other two treatments. 6 The importance of placebo-controlled trials of antidepressants is emphasized and the precautions that should be taken when they are carried out in outpatients are described.

Adolescent↗
PubMed1981

Effects of mianserin, desipramine and maprotiline on blood pressure responses evoked by acetylcholine, histamine and 5-hydroxytryptamine in rats.

1 In rats anaesthetized with pentobarbitone, intravenous administration of desipramine (0.1 mg/kg), maprotiline (0.5 mg/kg) or mianserin (0.3-3.0 mg/kg) did not modify the blood pressure lowering effects of acetylcholine (0.25-1.0 micrograms/kg, i.v.) which were significantly reduced by atropine (3.0 micrograms/kg, i.v.). 2 Maprotiline and mianserin, like promethazine (0.1 mg/kg, i.v.), inhibited the vasodepressor responses evoked by histamine (2.5-10.0 micrograms/kg,i.v.). however, desipramine was inactive against histamine. 3 In pithed rats, the pressor effects of intravenous 5-hydroxytryptamine (5-HT: 5.0-20.0 micrograms/kg) were antagonized by mianserin (0.01-0.3 mg/kg, i.v.) and cyproheptadine (0.01 mg/kg) but were unaffected by maprotiline and desipramine. 4 In syrosingopine pretreated rats given mianserin 0.1 mg/kg, intravenously, 5-HT (20.0 micrograms/kg, i.v.) produced a significant fall in blood pressure which could be reduced by a large dose of mianserin (10.0 mg/kg, i.v.). 5 In conclusion, desipramine, maptrotiline and mianserin, in doses previously found to inhibit noradrenaline neuronal reuptake in the rat cardiovascular system, lack muscarinic receptor antagonist properties. Whilst maprotiline and mianserin blocked vascular histamine receptors, only mianserin (10.0 mg/kg, i.v.). 5 In conclusion, desipramine, maptrotiline and mianserin, in doses previously found to inhibit noradrenaline neuronal reuptake in the rat cardiovascular system, lack muscarinic receptor antagonist properties. Whilst maprotiline and mianserin blocked vascular histamine receptors, only mianserin, like cyproheptadine, was a potent antagonist of the 5-HT receptors that mediate increases in blood pressure in rats. Finally, the vasodepressor effects of 5-HT in syrosingopine pretreated rats given a small dose of mianserin were antagonized by a large dose of mianserin, suggesting that 5-HT may activate two distinct types of receptors in the rat.

Acetylcholine↗
PubMed1987

Citalopram versus maprotiline: a controlled, clinical multicentre trial in depressed patients.

In a double-blind trial, comprising 96 depressed patients, citalopram was compared with maprotiline. The trial period was 6 weeks with ratings (MADRS, CGI) and side effects recordings taking place at Weeks 0, 1, 2, 4, and 6. Both drugs were administered as a single evening dose, 40 or 60 mg for citalopram, and 75 or 150 mg for maprotiline. MADRS total scores and CGI scores showed a highly significant reduction in both groups with no significant difference between them, whether the groups were considered as a whole or whether they were subdivided into endogenously/non-endogenously depressed or melancholic/non-melancholic patients. Side effects were not significantly different, but the maprotiline group showed more anticholinergic side effects, whereas the citalopram group showed more nausea, increased sweating and headache. Two patients on maprotiline were withdrawn because of side effects (hypotension and somnolence in the one case; tremor and insomnia in the other). One patient in each group was withdrawn because of increased transaminases, the citalopram-treated patient having increased values, however, already at baseline. Apart from this, no cardiovascular side effects and no pathological laboratory values related to treatment were observed. The authors conclude that citalopram is a safe antidepressant drug and as effective as maprotiline.

Adult↗
PubMed1996

Effects of fluoxetine and maprotiline on functional recovery in poststroke hemiplegic patients undergoing rehabilitation therapy.

BACKGROUND AND PURPOSE: In animals, drugs that increase brain amine concentrations influence the rate and degree of recovery from cortical lesions. It is therefore conceivable that antidepressants may influence outcome after ischemic brain injury in humans. We evaluated the effects of the norepinephrine reuptake blocker maprotiline and the serotonin reuptake blocker fluoxetine on the motor/functional capacities of poststroke patients undergoing physical therapy. METHODS: Fifty-two severely disabled hemiplegic subjects were randomly assigned to three treatment groups; during 3 months of physical therapy, patients were treated with placebo, maprotiline (150 mg/d), or fluoxetine (20 mg/d). Before and at the end of the observation period, we assessed activities of daily living by the Barthel Index, degree of neurological deficit by a neurological scale for hemiplegic subjects, and depressive symptomatology by the Hamilton Depression Rating Scale. RESULTS: The diverse treatments ameliorated walking and activities of daily living capacities to different extents. The greatest improvements were observed in the fluoxetine-treated group and the lowest in the maprotiline-treated group. Furthermore, fluoxetine yielded a significantly larger number of patients with good recovery compared with maprotiline or placebo. These effects of the drugs were not related to their efficacy in treating depressive symptoms. CONCLUSIONS: Fluoxetine may facilitate or, alternatively, maprotiline may hinder recovery in poststroke patients undergoing rehabilitation. The effects of fluoxetine as an adjunct to physical therapy warrant further investigation, since treatment with fluoxetine may result in a better functional outcome from stroke than physical therapy alone.

Activities of Daily Living↗
PubMed2000

[A comparative efficiency of amitriptyline, fluoxetine and maprotiline in prevention of migraine in attack-free period].

To reduce frequency and severity of the attacks, migraine was treated preventively between the attacks. The most effective drugs were beta-blockers and antidepressants. In a single-blind study we estimated comparative efficiency of amitriptiline (inhibitor of noradrenaline and serotonin reuptake and 5-HT2-receptor antagonist) 12.5-25 mg/daily, fluoxetine (a selective serotonin reuptake inhibitor) 10-20 mg/daily, and maprotiline (a selective noradrenaline reuptake inhibitor) 10-25 mg/daily. The duration of the therapy of migraine between the attacks was 12 weeks. Each group included 20 patients. 46 patients completed the whole course of therapy: 14 patients received amitriptyline, 16 patients--fluoxetine, and 16 patients--maprotiline. Positive results of the treatment (a reduction of the frequency of the migraine attacks during a treatment by 50% as compared with the baseline period) were observed in 71% of the patients treated with amitriptyline, in 56% of the patients treated with fluoxetine, and in 38% of the patients treated with maprotiline. All the drugs were able to reduce both intensity and duration of a headache. Index of the Quality of Life in the patients with migraine was increased in the groups treated with either amitriptyline or fluoxetine, but not in a group treated with maprotiline. The results obtained agree with the notion about high efficiency of antidepressants given between migraine attacks. Amitriptyline and fluoxetine were more efficient in preventive therapy than maprotiline. These findings suggested indirectly, that the efficiency of antidepressants in treatment of migraine is explained by inhibition of serotonin reuptake and by 5-HT2-receptor antagonism, while influence on the inhibition of noradrenaline reuptake was not so significant.

Acute Disease↗
PubMed1990

[Maprotiline and the heart rate].

The increased heart rate is a frequent, seldom clinically significant side-effect of antidepressants. There are different opinions about the Maprotiline influence on the heart rate, either about its very existence or the pathophysiological mechanism of its side-effect. The aim of this study was to test the Maprotiline influence on the heart rate of depressed patients and to compare the results with the results of other studies. The study was carried out in a group of 21 patients with a depressive involutional syndrome treated by fixed daily doses of 150 mg of Maprotiline. The heart rate was estimated in a small sample of examinees using the method of paired observations, as a part of the orthostatic cardiovascular tolerance testing by Schellong's method; this was done before the therapy and twice a week during four week of the application of Maprotiline. The increase in the heart rate in the basal reclining position was noticed in 20 patients. The average value was 16 beats per minute. The increase of the heart rate was not noticed immediately after the application of the first doses but after the latency of 8 days on average. While increasing in the basal reclining position, the orthostatic deviation of the heart rate did not significantly change during the therapy. At the end of the study the orthostatic deviation even showed a negative sign. The reclining of the patients at the end of Schellong's test discovered a frequent occurrence of the prolonged blood pressure return from higher to normal values. The results obtained confirm the thesis that the increased heart rate in the therapy with Maprotiline is due to its noradrenergic activity, in other words, to its ability to block the "reuptake" of noradrenalin in the synaptic cleft. The delay of the heart rate increase in the basal reclining position, a more frequent prolonged blood pressure return in the further phase of the study, and the therapeutic response delay in the treatment of depression are explained by the authors by the same mechanism: by the most probable existence of the pathological changes in the synapses.(ABSTRACT TRUNCATED AT 400 WORDS)

Blood Pressure↗
PubMed1985

Trimipramine and maprotiline: antidepressant, anxiolytic, and cardiotoxic comparison.

A 5-week placebo washout comparison of trimipramine 150 mg/day and maprotiline 150 mg/day was carried out in 15 male and 24 female patients with unipolar major affective disorder. There were no significant differences between the two groups in age, sex, weight, height, or vital signs. Both groups showed significant improvement over time, with no difference between the groups on the Severity and Improvement factors of the Clinical Global Impression scale, on the total and factor subscales of the Hamilton Depression Rating Scale, and on the Anxiety Status Inventory. The maprotiline group showed a greater increase in weight over the study period than did the trimipramine group. There was a significant lowering of systolic blood pressure in the trimipramine group only and a significant and linear increase in pulse rate by Week 3 in the maprotiline group. Analysis of ECG showed that the atrial rates were significantly increased in the maprotiline group (p less than .002) but not in the trimipramine group. Trimipramine had significantly fewer anticholinergic, neurologic, and cardiovascular adverse effects than maprotiline.

Adult↗
PubMedDate not supplied

[Blood concentrations of maprotiline in depressive patients].

Blood levels of Maprotiline were analysed and their relationship to the clinical response was examined in 89 depressed inpatients, according DSM III criteria for Major Depressive Episode, given the drug treatment for 3 weeks. Maprotiline produced marked decreases in mean MADRS and COVI scale scores by the end of treatment. On day 21, no correlation between blood levels of Maprotiline and MADRS or COVI scores were found when all patients were considered. Nevertheless, significant correlations were observed on day 14 (r = .22; p less than .05 for MADRS and r = .23; p less than .05 for COVI scale). In addition, a significant correlation between MADRS or COVI scale scores and Maprotiline blood levels were observed on days 14 and 21 in subgroups of young patients, severe depression (high scores to clinical global investigations), during of at least 3 months, treated without other drug than Maprotiline and good responders.

Adult↗
PubMed1977

A comparative study of maprotiline (Ludiomil) and viloxazine in the management of depressed patients in general practice.

A double-blind, comparative, multicentre study comparing the efficacy and tolerability of maprotiline (Ludiomil) and viloxazine as antidepressants in general practice usage is described. Progress was measured at weekly intervals over the 4-week trial duration using a modified Hamilton Rating Scale and patient self-assessment visual analogue scales. A total of 127 patients were randomized into two groups; 63 patients being allocated maprotiline and 64 patients being allocated viloxazine. Of the patients receiving maprotiline, 12 withdrew during the course of the study compared to 9 patients receiving viloxazine. Maprotiline appeared to be superior to viloxazine on the sleep and sadness scales and some evidence to show it to be better also on the tension scale. Whilst the trend favoured maprotiline, the two drugs did not appear to be significantly different on either the doctors' or the patients' assessments. There was little to choose between the drugs in terms of side-effects or ultimate patient tolerability and preference.

Adjustment Disorders↗
PubMedDate not supplied

[Different effects of tricyclic (clomipramine and amitriptyline) and tetracyclic (maprotiline) antidepressors on the release of thyroid stimulating hormone, prolactin and growth hormone to thyrostimulating releasing hormone in patients with psychoaffective disorders (author's transl)].

The hormonal alterations induced by tricyclic and tetracyclic antidepressors (AD) were studied in patients with psychoaffective disorders (PAD) to ascertain the role of certain biogenic amines in the regulation of thyroid stimulating hormone (TSH), prolactin (PRL) and growth hormone (GH). The responsiveness of plasma TSH, PRL and GH to synthetic thyrostimulating release hormone (TRH; 250 microgram i.v.) was determined in 57 patients distributed in 5 groups according to the treatment: 10 non treated patients, 16 tricyclic (clomipramine and amitriptyline) treated patients, 6 patients treated by clomipramine in association with lithium, 6 tetracyclic (maprotiline) treated patients and 19 patients treated by major neuroleptics. Results of untreated patients were compared to those observed in 10 age and sex matched normal subjects. Basal plasma levels of TSH were normal in all the patients. The TSH response to TRH (delta TSH) was blunted in non treated patients. delta TSH was normal in the patients treated by maprotiline or neuroleptics and increased in the group treated by tricyclic AD in association with lithium. Basal plasma levels of PRL and PRL response to TRH (delta PRL) were decreased in the women treated by tricyclic AD, but remained normal under maprotiline. They were markedly increased in the neuroleptic group. No inadequate response of GH to TRH was noted in our series of patients. The different hormonal effects induced by AD--dissociation between delta TSH and delta PRL under tricyclics and normal or increased delta TSH under maprotiline--may be logically explained by the various ways of action of these AD on the brain monoamines. delta TSH decrease and tendency to an increased delta PRL observed with clomipramine argue for a serotoninergic regulation of these two hormones, whereas the normalisation of delta TSH under maprotiline argues for a noradrenergic regulation of this hormone. Effectively, tricyclic AD inhibits mainly the serotonin recaptation and tetracyclic inhibits rather norepinephrine recaptation. The persistent delta TSH increase observed in the group treated by the association clomipramine-lithium demonstrates that the tricyclics do not interact with the hypophyso-thyroid positive feedback.

Adult↗
PubMed1993

[Effect of maprotiline on bronchodilation in patients with bronchospasm].

The bronchodilatory effect of maprotiline (Ludiomil, firm Ciba-Geigy) was investigated in 20 patients with bronchospasm (FEV %below 60%). The effect of a single dose of 75 mg maprotiline was compared with that produced by 500 mg of aminophylline, applied each time in 500 ml normal saline during 90 min, on two different days, in randomized sequence, always at the same day time. Prior to and at 5, 10, 20, 30, 60, 90, 120, 150 and 180 minutes after commencement of the infusion the following parameters of pulmonary ventilation have been determined: VC, FEV1, FEV1%., MEFR and MBC. The stated differences between the efficacy of maprotiline and aminophylline were statistically not significant (p > 0.05). In 18 patients maprotiline caused sedation and even somnolence. The authors conclude that maprotiline is an efficacious bronchodilator in patients with bronchospasm and is well tolerated by the patients.

Adult↗
PubMed1981

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

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 degrees C and 14C-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 alpha 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.

Adolescent↗
PubMed1986

Urinary 3-methoxy, 4-hydroxyphenylethylene glycol and therapeutic response to maprotiline and indalpine in major depression.

The potential value of pretreatment urinary 3-methoxy, 4-hydroxyphenylethyleneglycol (MHPG) levels to predict the therapeutic response to antidepressants was studied by measuring urinary MHPG output in 42 depressed inpatients treated with a selective inhibitor of serotonin (Indalpine) or noradrenaline (Maprotiline) reuptake. Among the 42 depressed inpatients there were 33 cases of major depressive episode. Patients were treated for at least 3 weeks, firstly with intravenous infusions of maprotiline or indalpine which have been administered at random. No difference in pretreatment urinary MHPG levels was found between the responders to indalpine (1.08 +/- 0.48 micrograms/24 h/mg of creatinine) and the responders to maprotiline (1.15 +/- 0.62 micrograms/24 h/mg of creatinine). However, there was a difference in the pretreatment levels of urinary MHPG between the non-responders to indalpine (0.56 +/- 0.28 microgram/24 h/mg of creatinine) and the non-responders to maprotiline (1.37 +/- 0.68 micrograms/24 h/mg of creatinine). No correlation between this biochemical parameter and HDRS score was found. These results indicate that, in this study, there is no obvious relationship between the pretreatment urinary MHPG levels in depressed patients and their therapeutic response to specific inhibitors of noradrenaline or serotonin reuptake. However, there was a positive trend towards a lower pretreatment MHPG level to be associated with lack of response to indalpine.

Adult↗
PubMed2006

Inhibition of cardiac HERG potassium channels by antidepressant maprotiline.

Many drugs block delayed rectifier K+ channels and prolong the cardiac action potential duration. Here we investigate the molecular mechanisms of voltage-dependent block of human ether-a-go-go-related gene (HERG) K+ channels expressed in cells HEK-293 and Xenopus oocytes by maprotiline. The IC50 determined at 0 mV on HERG expressed HEK-293 cell and oocytes was 5.2 and 23.7 microM, respectively. Block of HERG expressed in oocytes by maprotiline was enhanced by progressive membrane depolarization and accompanied by a negative shift in the voltage dependence of channel activation. The potency of maprotiline was reduced 7-fold by point mutation of a key aromatic residue (F656T) and 3-fold for Y652A, both located in the S6 domain. The mutation Y652A inverted the voltage dependence of HERG channel block by maprotiline. Together, these results suggest that voltage-dependent block of HERG results from gating dependent changes in the accessibility of Y652, a critical component of the drug binding site.

Animals↗
PubMedDate not supplied

Behavioural effects in mice of subchronic chlordiazepoxide, maprotiline, and fluvoxamine. I. Social interactions.

The present study compares the effects of subchronic administration (daily. 21 days) of chlordiazepoxide (CD), maprotiline and fluvoxamine on the behavior of male mice during dyadic social interactions. Maprotiline like chlordiazepoxide, stimulated aggression at 4 mg/kg and 2 mg/kg respectively (intermediate dose levels), whereas effects of fluvoxamine (3-8 mg/kg) were mainly sedative. Non-social activity was reduced by CD at 4 and 8 mg/kg and by maprotiline at 0.5 mg/kg. At the highest dose tested (10 mg/kg), maprotiline increased immobility, resembling the effects of fluvoxamine, while at 2 mg/kg, it reduced social investigation. Thus, despite some commonalities, there were several differences in behavioral profile of the compounds tested. Data are discussed in relation to the efficacy of each of these compounds in treating anxiety and depressive disorders.

Adrenergic Uptake Inhibitors↗