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PubMed1995

[Ca(2+)-channel blockers and binding of tricyclic antidepressive agents].

The interactions between Ca(2+)-channel blockers (verapamil and gallopamil) and synaptic plasma membranes (SPM) from bovine brain or human lymphocyte and platelet plasma membranes were studied. Changes in binding parameters of [3H]imipramine, [3H]desmethylimipramine and [3H]gallopamil were determined after addition of unlabelled verapamil or imipramine and after addition of phosphatidylserine (PS) (PS-stimulation). Specific binding of [3H]imipramine to SPM was decreased and [3H]desmethylimipramine binding was increased by 1 microM verapamil. [3H]gallopamil binds specifically to SPM as well as to platelet and lymphocyte membranes. [3H]gallopamil binding to SPM or lymphocyte plasma membranes was PS-stimulated in contrast to platelet plasma membranes without PS effect on binding. Imipramine inhibited both [3H]gallopamil binding and PS-stimulated [3H]gallopamil binding to SPM or lymphocyte plasma membranes. Mutual effects of tricyclic antidepressants and Ca(2+)-channel blockers on their binding sites require relatively high drug concentrations. Mechanism of Ca(2+)-channel blockers action in the treatment of depression may be connected rather with changes in signal transduction through serotonin and catecholamine receptor systems than with direct interaction of drugs with binding sites for tricyclic antidepressants.

Animals↗

PubMed1977

[Manic-depressive psychoses. Chronic treatment with tricyclic antidepressive agents].

Long-course Tricyclic anti-depressing treatment affonds clinical healing--i.e. abolition of the recurrences--in melancolic unipolary periodic depressions. This treatment--T.A.T.C.--allows a good prevention of melancolic recurrences in bipolar periodic patterns of psychosis. For the authors Lithium and/or Dipropylacétamide are not sufficient protection for melancolic or maniac recurrences in this patterns. It seems to be three patterns in fact: pure melancolic, pure maniac, and maniaco-depressive. Therapeutic and psychopathologic considerations.

Adult↗

PubMed1995

[The effect of an antidepressive agent on premature ejaculation].

Premature ejaculation is a common male sexual dysfunction. Many kinds of medication have been used without great success. The start-stop technique is usually preferred. However, some patients and couples do not want to learn this kind of sexual therapy. One common adverse effect of the new selective serotonin re-uptake inhibitors is delayed ejaculation. This article discusses a patient with a premature ejaculation problem combined with minor depression and anxiety, who was successfully treated with paroxetine.

Adult↗

PubMed1985

[Long-term administration of antidepressive agents: maintenance therapy and phase prevention].

Long-term regimen of psychotropic drugs in depression is particularly indicated in those patients who benefit most from the drugs, namely patients of the "endogenous" or "endogenomorphic" type. Medication over months or even years is indicated for two frequently concurrent reasons: firstly for "maintenance therapy", i.e., medication should be continued after remission of the depressive syndrome because of not yet identifiable "vulnerability" to relapse in many patients and, secondly, for "prophylactic therapy", i.e. medication can be given during apparent psychological health and in the absence of any imminent risk in order to prevent a possible new episode of depression. Long-term regimen of both types of medication is different, though not decisively so. Neither can cure a patient of depression; however, recurrence of the psychopathological syndrome can be successfully prevented. This paper presents a practical and updated discussion of various questions related to long-term regimen with psychotropic drugs used in depression: tricyclic antidepressants, lithium, carbamazepine and others.

Antidepressive Agents, Tricyclic↗

PubMed1986

Effect of dihydroergosine (DHESN) on the serotoninergic system and behaviour: is DHESN a new antidepressive agent?

Acute (50.0 mg/kg) and repeated (0.1-10.0 mg/kg) administration of dihydroergosine (DHESN) to rats over 5 days lowered the concentration of 5-HIAA in the brain. DHESN given acutely increased the brain 5-HT in p-CPA-treated animals and diminished the probenecid-induced increase in brain 5-HIAA. In pargyline-treated rats DHESN enhanced the 5-HT/5-HIAA ratio. DHESN administered to rats repeatedly over 5 days decreased the level of 5-HT in blood platelets, and in vitro at concentrations of 10(-4) M and 10(-3) M inhibited the uptake of [14C]-5-HT in platelets. DHESN (10.0-100.0 mg/kg) potentiated the 5-HT syndrome produced in rats by pargyline and 5-HTP. This potentiation was blocked with cyproheptadine but not with haloperidol. DHESN (1.0 and 10.0 mg/kg) lowered the locomotor activity of rats and 10.0 mg/kg DHESN also reduced the duration of immobility in rats forced to swim in a restricted space. The results indicate that DHESN, like antidepressants, decreases the turnover of serotonin in the brain and potentiates the 5-HT-mediated behaviour. This might suggest that the drug should be further investigated for its potential antidepressive properties.

Animals↗

PubMed1991

[Contribution of electrophysiology to the study of tianeptine and other antidepressive agents].

Intravenous perfusion of tianeptine reduces the frequency of coeruleus locus neural discharge. It does not affect the rate of neural discharge in the dorsal raphe, increase the rate of neural discharge in the ventral tegument air and the rate of discharge in the pyramidal cells of the hippocampus (CA1). In comparison, intravenous perfusion of clomipramine decreases the rate of neural discharge in the coeruleus locus, the dorsal raphe, the ventral tegument air (temporarily) and the pyramidal cells of the hippocampus. Iontophoretic application of tianeptine does not affect the response of pyramidal cells in the hippocampus to application of serotonin or gamma amino-butyric acid (GABA), but lowers recovery time after iontophoretic administration of serotonin or GABA. Iontophoretic application of clomipramine increases pyramidal cell response to serotonin but not to GABA and lengthens the recovery time after serotonin and GABA. The results are in agreement with the fact that tianeptine, unlike clomipramine, increases serotonin capture. Tianeptine leads to an original electrophysiologic pattern distinct from classic antidepressants and clomipramine.

Animals↗

PubMed1973

Interactions between sympathomimetic amines and antidepressant agents in man.

Intravenous infusions of phenylephrine, noradrenaline, adrenaline, and isoprenaline were given to healthy human volunteers after five to seven days on phenelzine, tranylcypromine, or imipramine, and cardiovascular responses were compared with those observed under control conditions. With monoamine oxidase inhibitors there was a 2-2(1/2) fold potentiation of the pressor effect of phenylephrine, but no clinically significant potentiation of cardiovascular effects of noradrenaline, adrenaline, or isoprenaline. With imipramine there was potentiation of the pressor effects of phenylephrine (2-3 fold), noradrenaline (4-8 fold), and adrenaline (2-4 fold); there were dysrhythmias during adrenaline infusions, but no noticeable or consistent changes in response to isoprenaline.Noradrenaline and adrenaline in amounts contained in local anaesthetics used in dentistry are not likely to be significantly potentiated in otherwise healthy patients receiving monoamine oxidase inhibitors. Hazardous potentiation of their cardiovascular effects might occur in patients receiving tricyclic antidepressants.Our observations do not indicate that the hazards associated with isoprenaline inhalation by bronchial asthmatics would be increased by coincident therapy with a monoamine oxidase inhibitor or tricyclic antidepressant.

Adult↗

PubMed2002

Overcoming the effects of stress on synaptic plasticity in the intact hippocampus: rapid actions of serotonergic and antidepressant agents.

Acute inescapable stress dramatically affects the inducibility of plasticity at glutamatergic synapses in the intact hippocampus. The present study examined the involvement of serotonergic mechanisms in mediating and modulating the block of long-term potentiation (LTP) in the CA1 area of anesthetized rats after exposure to an elevated platform stress. Fluoxetine and fenfluramine, agents that raise hippocampal extracellular 5-HT concentration, blocked the induction of LTP in nonstressed animals, thus mimicking the effect of stress. In contrast, (+/-)-tianeptine, a drug that decreases 5-HT levels, had no effect on LTP induction in nonstressed animals. Remarkably, (+/-) administration of tianeptine after the stress rapidly overcame the block of LTP induction without affecting baseline excitatory transmission. Consistent with a reduction of 5-HT levels being responsible for this effect of tianeptine, the (-) enantiomer, which is associated with the 5-HT uptake enhancing action of (+/-)-tianeptine, also caused a recovery of the induction of LTP in previously stressed animals, whereas the relatively inactive (+) enantiomer had no effect. Furthermore, fluoxetine prevented the effect of tianeptine in stressed animals. These findings show that antidepressants have rapid and powerful interactions with the mechanisms controlling the persistence of the block of LTP by inescapable stress.

Animals↗

PubMed1983

[Classification and determination of the pharmacodynamics of a new tetracyclic antidepressive agent, pirlindol, using pharmaco-EEG and psychometry].

In a double-blind placebo-controlled study the encephalotropic and psychotropic properties of a new tetracyclic pyrazino-indole derivative were studied in 10 normal volunteers. They received, randomized at weekly intervals, single oral doses of placebo, 75 mg, 150 mg and 225 mg pirlindol, as well as 75 mg imipramine, 20 mg tranylcypromine and 150 mg nomifensine as reference drugs. Pharmaco-EEG, psychometric and physiological data were obtained at the hours 0, 1, 2, 4, 6 and 8 after oral administration. Digital computer period analysis of the EEG demonstrated moderate CNS effects with pirlindol as compared with placebo. Its pharmaco-EEG profile, especially after higher dosage (150 and 225 mg), was characterized by a decrease in delta and theta activity, an increase in alpha activity and a delta and theta activity, an increase in alpha activity and a decrease in beta activity, as well as by an attenuation of the average frequency and frequency deviation and a trend towards an augmentation of the amplitude and amplitude variability. This profile is typical for antidepressants of the desipramine type and was also observed in our present study after 150 mg nomifensine and (although less markedly) and 20 mg tranylcypromine. 75 mg pirlindol induced, however, changes characterized by a concomitant increase in slow and superimposed fast activities and by a decrease in alpha activity. These alterations were described previously as typical for antidepressants of the imipramine type, and were also noted after 75 mg imipramine in the present study. Time-efficacy calculations showed the maximal pharmacodynamic effect of pirlindol in the 4th to 6th hour, of 75 mg imipramine in the 2nd hour, of 20 mg tranylcypromine in the 4th hour and of 150 mg nomifensine in the 6th hour. Dose/treatment-efficacy calculations identified in the 1st and 2nd hour post drug 75 mg imipramine as the most CNS-effective drug, in the 4th and 6th hour 150 mg pirlindol and in the 8th hour 225 mg pirlindol. Psychometric investigations showed only slight changes after pirlindol, reaching only rarely the level of statistical significance (improvement in attention after 225 mg pirlindol, decrease in tapping after 75 and 150 mg pirlindol, as well as attenuation of the complex reaction after all 3 doses of pirlindol). Concentration, attention-variability, psychomotor activity, CFF, after effect (Archimedean spiral), reaction time, mood and affectivity were not significantly altered as compared with placebo. Pulse, systolic and diastolic blood pressure did not show any clinical relevant changes either.(ABSTRACT TRUNCATED AT 400 WORDS)

Adult↗

PubMedDate not supplied

The metabolism of EGYT-475, a new antidepressant agent, in rats.

The metabolites of EGYT-475 excreted by the kidney were studied in rats using radioactive analogues of the compound tested. 40% of the total radioactivity was found in rat urine which was collected over 48 h, pooled, centrifuged, membrane-filtered, and from which the metabolites were separated by combined chromatographic procedures or extracted after acidic hydrolysis. Gas chromatographic and GC/MS studies showed that 31.1% of the radioactivity found in urine proved to be picolinyl-piperazine, 3.7% was N-benzyl-piperazine and 28.5% of it was picolinic acid. Hippuric acid accounted for 53.2% of the radioactivity of the acid hydrolyzed urine.

Animals↗

PubMed1995

Preclinical pharmacological actions of (+/-)-(1'R,3R)-3-phenyl-1- [1',2',3',4'-tetrahydro-5',6'-methylene-dioxy-1'-naphthalenyl) methyl] pyrrolidine methanesulfonate (ABT-200), a potential antidepressant agent that antagonizes alpha-2 adrenergic receptors and inhibits the neuronal uptake of norepinephrine.

(+/-)-(1'R*,3R*)-3-phenyl-1-[(1',2',3',4'-tetrahydro-5',6'-methylene- dioxy-1'-naphthalenyl) methyl] pyrrolidine methanesulfonate (ABT-200) was evaluated in a number of biological tests to establish its pharmacological profile of activity. ABT-200 antagonized the uptake of [3H]-norepinephrine into synaptosomes of rat hypothalamus (IC50 = 841 nM) and blocked 4,alpha-dimethyl-m-tyramine- induced hypermotility in rats. In addition, ABT-200 potently inhibited binding of [3H]-rauwolscine to alpha-2 adrenergic receptors with a Ki value in radioligand binding assays of approximately 1 nM in the rat cortex and was much less potent at other receptor binding sites. ABT-200 antagonized alpha-2 receptors in vitro in the rat vas deferens and dog saphenous vein, where pA2 values of 7.7 and 8.2, respectively, were obtained. ABT-200 also antagonized clonidine-induced mydriasis and increased the overflow of [3H]-norepinephrine in guinea pig hippocampal slices, manifestations of blockade of alpha-2 adrenoceptors in the central nervous system. ABT-200 was active in antagonizing nocturnal hyperactivity in olfactory bulbectomized rats, a test for putative antidepressant activity. In cardiovascular studies, ABT-200 exhibited negligible activity in affecting hemodynamic parameters and was free of postural hypotensive activity. In both in vitro and in vivo, ABT-200 was devoid of antihistaminic or anticholinergic activity. This profile of activity of moderate inhibition of norepinephrine uptake with blockade of alpha-2 adrenoceptors suggests potential dual-action effects for ABT-200, which may represent a putative antidepressant with minimal cardiovascular side-effect liability.

Adrenergic Uptake Inhibitors↗

PubMed1975

Clinical pharmacology of SQ 10,996, a potential antidepressive agent.

Single oral doses of SQ 10,996 ranging from 500 to 1000 mg (0.34 to 15.3 mg/kg), given once daily for 3 consecutive days to groups of healthy volunteers, were well tolerated. One of three subjects given 1250 mg (17.1 mg/kg) and two of three subjects given 1500 mg (15.6 and 21.4 mg/kg) became drowsy on the second and third days; this symptom disappeared within 24 hrs after cessation of dosage. A short-term, multiple-dose tolerance study was carried out with a formulation of SQ 10,996, the bioavailability of which was comparable to that of the formulation used earlier in the ascending-dose tolerance study. When 200-mg doses were administered every 12, 8, or 6 hrs over a 6-day period, mean steady-state serum concentrations of approximately 4, 7, and 8 mug/ml were attained within 48 hrs; unexpectedly, no subject showed any sign of drowsiness. The half-life for SQ 10,996 in serum, estimated from concentrations in serum after the last dose, was approximately 13 hrs, significantly shorter than the half-life found previously after the administration of single 10-mg doses. These clinical pharmacology studies in healthy volunteers have shown SQ 10,996 to be biologically available and well tolerated. Future studies will test its antidepressive potential in patients.

Adult↗

PubMed1987

Quantitative structure-activity relationship of antidepressant agents. Derivatives of cis- and trans-1-amino-4-aryltetralin.

The quantitative structure-activity relationship (QSAR) was studied for monoamine uptake inhibition of cis- and trans-1-amino-4-aryltetralins. The physicochemical parameters, electronic (sigma), hydrophobic (pi), and molar refraction (MR) were found to be significantly correlated with 5-hydroxytryptamine (5-HT) uptake inhibition activity in corpus striatum of rat brain in both series of compounds. The norepinephrine (NE) uptake inhibition activity in hypothalamus and dopamine (DA) uptake inhibition activity in corpus striatum, however, yielded poor correlations in either set of compounds. However, the selectivity ratios, - log [IC50 (DA)/IC50 (5-HT)] and - log [IC50 (NE)/IC50 (5-HT)] described statistically sound correlations with properly chosen physicochemical parameters in cis- and trans-1-amino-4-aryltetralins.

Animals↗

PubMed1982

Determination of the antidepressant agent citalopram and metabolites in plasma by liquid chromatography with fluorescence detection.

A high-performance liquid chromatographic method is described for the determination of citalopram [1-(3-(dimethylaminopropyl)-1-(4-fluorophenyl)-5-phthalancarbonitrile] and its two main metabolites (the methylamino and amino derivatives). The compounds were extracted from alkaline plasma with diethyl ether. The combined ether layers were evaporated after addition of 50 microliter of 0.1 N HCl. The residual extracts were purified with diethyl ether and 20 microliter were injected into a Spherisorb ODS 5-micrometer column with acetonitrile--0.6% phosphate buffer pH 3 (55:45, v/v) as the mobile phase. Using a fluorescence detector the detection limits are 1 ng/ml of plasma for citalopram and the methylamino metabolite and 0.5 ng/ml for the amino metabolite.

Antidepressive Agents↗

PubMedDate not supplied

Pharmacokinetic aspects of the mode of action of EGYT-475, a new antidepressant agent.

EGYT-475 (N-benzyl-piperazine-picolinyl fumarate; Trelibet) metabolism was compared in rats, dogs and man. In the rat 7 urinary metabolites of EGYT-475 were found, and 4 were identified as: N-picolinyl-piperazine (EGYT-1354) (30%), picolinic acid (28.5%), hippuric acid (53%) and N-benzylpiperazine (EGYPT-2760) (3.7%). The results show that debenzylation is the main route of EGYT-475 metabolism in the rat. By this route EGYT-2760, the active EGYT-475 metabolite, is further metabolized. In the dog the main metabolic pathway is hydrolysis, and because of that the formed EGYT-2760 is not metabolized further and its urinary content exceeds 50%. In man, similarly as in the rat, debenzylation is the preferred route of EGYT-475 metabolism. These results explain much higher toxicity of EGYT-475 in dogs than in rats and man.

Animals↗

PubMed2001

[Sibutramine--antidepressive agent tested against obesity].

Eight European centers recruited 605 obese patients (BMI 30-45 kg/m2) for a six month period of weight loss with sibutramine (10 mg/d) combined with an individualized 600 kcal/d deficit. 467 (77%) patients with > 5% weight loss were then randomized to sibutramine (10 mg/day) and placebo groups over a further 18 months. Initially weight loss progressed to a total of -11.3 +/- 5.5 kg. After randomization the placebo group regained weight to -4.7 +/- 7.2 kg from baseline at 2 years; the sibutramine group only showed slight weight regain to -10.2 kg +/- 9.3 kg (mean group difference 5.5 kg, 95% C.I. 2.9, 8.1, p < 0.001). VLDL fell and HDL increased more than expected by weight loss. Twenty (3%) patients were withdrawn because of increases in blood pressure. This individualized management program achieves metabolically significant and sustained weight loss in 77% of obese patients.

Antidepressive Agents, Second-Generation↗

PubMed1976

Psychometric assessment of the therapeutic efficiency of antidepressant agents.

A clinical trial of four weeks duration was conducted involving a total of thirty depressed patients, of both sexes, aged between twenty and thirty-four years. The total number of patients was divided into three groups of ten patients each. One group received amitriptyline, the second group was administered noxiptyline and the third group was given dibenzepine. All drugs were administered orally. Patients were submitted to psychometric testing before and after drug administration. The tests used included the 'Hamilton Rating Scale for depression', the 'Hildreth Feeling Scale' and the 'D Scale' and the 'Trail Making Test' for the evaluation of psychomotor retardation. It was concluded that the Hamilton Rating Scale was the most relatively sensitive test utilized in assessing the depressive state and its improvement. Amitriptyline was found to be mostly anxiolytic; noxiptyline controlled both depression and anxiety to approximately the same extent; and dibenzepine was found to be a mood-elevating drug with an energizing action.

Adult↗

PubMed1985

Tricyclic antidepressants in obsessive-compulsive disorder: antiobsessional or antidepressant agents? II.

The authors explored the relationship between the antiobsessional and antidepressant effects of tricyclic drugs in primary obsessive-compulsive disorders. Study 1 consisted of a controlled 12-week trial with clomipramine (N = 7) and placebo (N = 5); study 2 analyzed the pooled data from 15 patients uniformly selected and treated with either clomipramine or imipramine. Although the antiobsessional and antidepressant effects of the drugs covaried, their antidepressant action was not a prerequisite for their antiobsessional effect. The findings suggest that clomipramine and probably imipramine possess specific antiobsessive effects that are at least partially independent of their antidepressant effects.

Adult↗