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H.-j. Möller - One of the best experts on this subject based on the ideXlab platform.
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Brofaromine versus imipramine in in-patients with major depression--a controlled trial.
Journal of affective disorders, 1997Co-Authors: H.-p. Volz, C. H. Gleiter, H.-j. MöllerAbstract:Brofaromine is a selective and reversible inhibitor of monoamine oxidase A. The efficacy and safety of this compound as compared with tricyclic antidepressants, classical monoamine oxidase inhibitors and placebo has been demonstrated in several clinical trials. The present 6-week, double-blind, randomized trial compared Brofaromine with imipramine in in-patients with major depression. Brofaromine was as effective as imipramine in the treatment of major depression, but exhibited a different side-effect profile, in particular lacking the anticholinergic and certain cardiovascular side-effects of the tricyclic imipramine, but more likely to induce sleep disturbances. In this study, in-patients were examined, since the majority of controlled clinical trials on depressed patients conducted so far have focused on the evaluation of out-patients. If one assumes that a different degree of severity of depression exists between these two patient groups, then the results of those trials conducted on out-patients cannot readily be transferred to in-patients.
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Brofaromine--a review of its pharmacological properties and therapeutic use.
Journal of neural transmission (Vienna Austria : 1996), 1996Co-Authors: H.-p. Volz, P.c. Waldmeier, C. H. Gleiter, M Struck, H.-j. MöllerAbstract:The antidepressant activity of monoamine oxidase inhibitors has been well established for 30 years. Nevertheless, this group of compounds was handled with great care, mainly because of the interaction potential with tyramine-containing foodstuff. With the discovery of reversible and selective inhibitors of monoamine oxidase type A a renaissance of these compounds has begun. In this paper one of these new substances--Brofaromine--will be described in detail. Biochemical and pharmacological aspects will be reviewed, showing that Brofaromine is a selective and reversible inhibitor of monoamine oxidase type A with additional serotonin reuptake inhibiting properties. Both mechanisms of action may synergize in the antidepressant effect of the compound. The main results of clinical trials in depression and other indication areas will also be covered. Special attention will be put on the side effect profile.
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Are There Any Differences in the Safety and Efficacy of Brofaromine and Imipramine between Non-Elderly and Elderly Patients with Major Depression?
Neuropsychobiology, 1995Co-Authors: H.-p. Volz, Horst G. Müller, H.-j. MöllerAbstract:There is a rather limited database of controlled clinical trials on the comparative effects of antidepressants in elderly and non-elderly depressed patients. A common finding is reduced efficacy and an increased incidence of side effects. To further examine the question of efficacy and safety of antidepressant drugs in elderly versus non-elderly patients, the differential effects of a new selective type A monoamine oxidase inhibitor Brofaromine, and the classical tricyclic imipramine were investigated using the data of two recently published trials. We found no major difference between non-elderly and elderly depressed patients as concerns efficacy, total incidence of adverse findings or safety parameters such as laboratory values and heart rate. These results are discussed in the light of some methodological questions and previous reports.
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Brofaromine in treatment resistant depressed patients a comparative trial versus tranylcypromine
Journal of Affective Disorders, 1994Co-Authors: H.-p. Volz, F. Faltus, I. Magyar, H.-j. MöllerAbstract:Abstract In a controlled clinical inpatient trial ( n = 93) comparing the efficacy and safety of Brofaromine versus tranylcypromine for 6 weeks in treatment-resistant major depressed patients, the two drugs were found to be of comparable afficacy and tolerability. The response rate (a 50% reduction) on the Hamilton Scale for Depression (HAMD) in both groups was about 73%. The most common side effects in the Brofaromine group were sleep disorders, hypotension, tremor and dryness of mouth; and in the tranylcypromine group sleep disorders, fatique, hypotension, tremor and vertigo. Methodological and practical clinical implications of the results are discussed.
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Brofaromine in treatment-resistant depressed patients — a comparative trial versus tranylcypromine
Journal of affective disorders, 1994Co-Authors: H.-p. Volz, F. Faltus, I. Magyar, H.-j. MöllerAbstract:Abstract In a controlled clinical inpatient trial ( n = 93) comparing the efficacy and safety of Brofaromine versus tranylcypromine for 6 weeks in treatment-resistant major depressed patients, the two drugs were found to be of comparable afficacy and tolerability. The response rate (a 50% reduction) on the Hamilton Scale for Depression (HAMD) in both groups was about 73%. The most common side effects in the Brofaromine group were sleep disorders, hypotension, tremor and dryness of mouth; and in the tranylcypromine group sleep disorders, fatique, hypotension, tremor and vertigo. Methodological and practical clinical implications of the results are discussed.
H.-p. Volz - One of the best experts on this subject based on the ideXlab platform.
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Brofaromine versus imipramine in in-patients with major depression--a controlled trial.
Journal of affective disorders, 1997Co-Authors: H.-p. Volz, C. H. Gleiter, H.-j. MöllerAbstract:Brofaromine is a selective and reversible inhibitor of monoamine oxidase A. The efficacy and safety of this compound as compared with tricyclic antidepressants, classical monoamine oxidase inhibitors and placebo has been demonstrated in several clinical trials. The present 6-week, double-blind, randomized trial compared Brofaromine with imipramine in in-patients with major depression. Brofaromine was as effective as imipramine in the treatment of major depression, but exhibited a different side-effect profile, in particular lacking the anticholinergic and certain cardiovascular side-effects of the tricyclic imipramine, but more likely to induce sleep disturbances. In this study, in-patients were examined, since the majority of controlled clinical trials on depressed patients conducted so far have focused on the evaluation of out-patients. If one assumes that a different degree of severity of depression exists between these two patient groups, then the results of those trials conducted on out-patients cannot readily be transferred to in-patients.
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Brofaromine--a review of its pharmacological properties and therapeutic use.
Journal of neural transmission (Vienna Austria : 1996), 1996Co-Authors: H.-p. Volz, P.c. Waldmeier, C. H. Gleiter, M Struck, H.-j. MöllerAbstract:The antidepressant activity of monoamine oxidase inhibitors has been well established for 30 years. Nevertheless, this group of compounds was handled with great care, mainly because of the interaction potential with tyramine-containing foodstuff. With the discovery of reversible and selective inhibitors of monoamine oxidase type A a renaissance of these compounds has begun. In this paper one of these new substances--Brofaromine--will be described in detail. Biochemical and pharmacological aspects will be reviewed, showing that Brofaromine is a selective and reversible inhibitor of monoamine oxidase type A with additional serotonin reuptake inhibiting properties. Both mechanisms of action may synergize in the antidepressant effect of the compound. The main results of clinical trials in depression and other indication areas will also be covered. Special attention will be put on the side effect profile.
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Are There Any Differences in the Safety and Efficacy of Brofaromine and Imipramine between Non-Elderly and Elderly Patients with Major Depression?
Neuropsychobiology, 1995Co-Authors: H.-p. Volz, Horst G. Müller, H.-j. MöllerAbstract:There is a rather limited database of controlled clinical trials on the comparative effects of antidepressants in elderly and non-elderly depressed patients. A common finding is reduced efficacy and an increased incidence of side effects. To further examine the question of efficacy and safety of antidepressant drugs in elderly versus non-elderly patients, the differential effects of a new selective type A monoamine oxidase inhibitor Brofaromine, and the classical tricyclic imipramine were investigated using the data of two recently published trials. We found no major difference between non-elderly and elderly depressed patients as concerns efficacy, total incidence of adverse findings or safety parameters such as laboratory values and heart rate. These results are discussed in the light of some methodological questions and previous reports.
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Brofaromine in treatment resistant depressed patients a comparative trial versus tranylcypromine
Journal of Affective Disorders, 1994Co-Authors: H.-p. Volz, F. Faltus, I. Magyar, H.-j. MöllerAbstract:Abstract In a controlled clinical inpatient trial ( n = 93) comparing the efficacy and safety of Brofaromine versus tranylcypromine for 6 weeks in treatment-resistant major depressed patients, the two drugs were found to be of comparable afficacy and tolerability. The response rate (a 50% reduction) on the Hamilton Scale for Depression (HAMD) in both groups was about 73%. The most common side effects in the Brofaromine group were sleep disorders, hypotension, tremor and dryness of mouth; and in the tranylcypromine group sleep disorders, fatique, hypotension, tremor and vertigo. Methodological and practical clinical implications of the results are discussed.
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Brofaromine in treatment-resistant depressed patients — a comparative trial versus tranylcypromine
Journal of affective disorders, 1994Co-Authors: H.-p. Volz, F. Faltus, I. Magyar, H.-j. MöllerAbstract:Abstract In a controlled clinical inpatient trial ( n = 93) comparing the efficacy and safety of Brofaromine versus tranylcypromine for 6 weeks in treatment-resistant major depressed patients, the two drugs were found to be of comparable afficacy and tolerability. The response rate (a 50% reduction) on the Hamilton Scale for Depression (HAMD) in both groups was about 73%. The most common side effects in the Brofaromine group were sleep disorders, hypotension, tremor and dryness of mouth; and in the tranylcypromine group sleep disorders, fatique, hypotension, tremor and vertigo. Methodological and practical clinical implications of the results are discussed.
Herman G.m. Westenberg - One of the best experts on this subject based on the ideXlab platform.
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Responders and non-responders to drug treatment in social phobia: differences at baseline and prediction of response
Journal of affective disorders, 1996Co-Authors: B.r. Slaap, Irene M. Van Vliet, Herman G.m. Westenberg, Johan A. Den BoerAbstract:Differences between responders and non-responders to drug therapy were investigated in social phobia. Two previously published studies were pooled to obtain data of 30 patients who were treated for 12 weeks with Brofaromine or fluvoxamine. Four criterion variables were used to divide patients in responders and non-responders. Depending on the criterion variable up to 72% of the patients were regarded as responders. Non-responders differed from responders in that they had a higher heart rate and a higher blood pressure. They were also characterised by higher scores on several psychometric scales, indicative of illness severity.
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Phobic symptoms as predictors of nonresponse to drug therapy in panic disorder patients (a preliminary report).
Journal of affective disorders, 1995Co-Authors: B.r. Slaap, Irene M. Van Vliet, Herman G.m. Westenberg, Johan A. Den BoerAbstract:Factors that predict nonresponse to drug therapy (Brofaromine or fluvoxamine) were investigated in a sample of 44 panic disorder patients. We used a strict definition of nonresponse to find patients who did not respond at all after 12 weeks of treatment. Using this definition, 15 patients (32.6%) were considered nonresponders. Nonresponders had a higher score on the Blood-Injury subscore of the Fear Questionnaire (FQ) and more often had high scores on several FQ subscores, indicative of comorbid phobic symptoms. These variables were subsequently used to predict nonresponse.
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MAO inhibitors in panic disorder: clinical effects of treatment with Brofaromine. A double blind placebo controlled study.
Psychopharmacology, 1993Co-Authors: Irene M. Van Vliet, Herman G.m. Westenberg, Johan A. Den BoerAbstract:There is considerable evidence that antidepressants, particularly serotonin uptake inhibitors, are effective in the treatment of panic disorder (PD). Monoamine oxidase inhibitors (MAOI) may also have beneficial effects in PD. In this study 30 patients with PD with or without agoraphobia (DSM-III-R) were treated with the selective and reversible MAO-A inhibitor Brofaromine (150 mg daily) in a 12-week double-blind placebo controlled design. A clinical relevant improvement was found in more than 70% of the patients treated with Brofaromine, whereas no significant improvement was observed on placebo. After an increase in anxiety in the first week, a clinically relevant improvement in anxiety symptoms was found, followed by a subsequent reduction in agoraphobic avoidance in patients treated with Brofaromine. A similar improvement was observed on distress scores related to panic attacks, although there was no significant reduction in the number of panic attacks. The most prominent side-effects were middle sleep disturbance and nausea. No increase in blood pressure was observed. During a follow-up period of another 12 weeks a further improvement was found in patients treated with Brofaromine.
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Pharmacological treatment of social phobia; recent developments
European Neuropsychopharmacology, 1993Co-Authors: J.a. Den Boer, I.m. Van Vliet, Herman G.m. WestenbergAbstract:Abstract During the last decades the treatments of choice for patients suffering from social phobia have been either psychotherapy, beta blockers or nonselective MAOIs. In the present study we report two studies in social phobia. (1) A double-blind placebo-controlled study using the selective and reversible MAO-A inhibitor Brofaromine. This new compound was found to be effective in reducing both social anxiety and social avoidance. (2) The selective 5-HT uptake inhibitor fluvoxamine was investigated in a double-blind placebo-controlled design. The results show that social anxiety responds to treatment with fluvoxamine, whereas the effects on social avoidance are less impressive.
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psychopharmacological treatment of social phobia clinical and biochemical effects of Brofaromine a selective mao a inhibitor
European Neuropsychopharmacology, 1992Co-Authors: Irene M. Van Vliet, Johan Den A Boer, Herman G.m. WestenbergAbstract:Abstract There is circumstantial evidence that antidepressants, particularly monoamine oxidase inhibitors (MAOIs) and β-blockers, may have some beneficial effects in social phobia. In this study 30 patients with social phobia (DSM-IIIR) were treated with the selective and reversible MAO-A inhibitor Brofaromine, using a 12-week double-blind placebo controlled design. A clinical relevant improvement was seen in 80% of the patients treated with Brofaromine (150 mg daily). A significant improvement was found on measures of social anxiety, phobic avoidance, general (or anticipatory) anxiety and interpersonal sensitivity in patients on Brofaromine, but not placebo. Biochemical measurements revealed a decrease in turnover of noradrenaline, serotonin and dopamine as assessed by the plasma metabolite levels, and an increase in nocturnal release of melatonin. Most prominent side-effect was middle sleep disturbance. No changes in blood pressure were observed. During a follow-up period of 12 weeks a further improvement was found in patients treated with Brofaromine.
C. H. Gleiter - One of the best experts on this subject based on the ideXlab platform.
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Brofaromine versus imipramine in in-patients with major depression--a controlled trial.
Journal of affective disorders, 1997Co-Authors: H.-p. Volz, C. H. Gleiter, H.-j. MöllerAbstract:Brofaromine is a selective and reversible inhibitor of monoamine oxidase A. The efficacy and safety of this compound as compared with tricyclic antidepressants, classical monoamine oxidase inhibitors and placebo has been demonstrated in several clinical trials. The present 6-week, double-blind, randomized trial compared Brofaromine with imipramine in in-patients with major depression. Brofaromine was as effective as imipramine in the treatment of major depression, but exhibited a different side-effect profile, in particular lacking the anticholinergic and certain cardiovascular side-effects of the tricyclic imipramine, but more likely to induce sleep disturbances. In this study, in-patients were examined, since the majority of controlled clinical trials on depressed patients conducted so far have focused on the evaluation of out-patients. If one assumes that a different degree of severity of depression exists between these two patient groups, then the results of those trials conducted on out-patients cannot readily be transferred to in-patients.
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Brofaromine--a review of its pharmacological properties and therapeutic use.
Journal of neural transmission (Vienna Austria : 1996), 1996Co-Authors: H.-p. Volz, P.c. Waldmeier, C. H. Gleiter, M Struck, H.-j. MöllerAbstract:The antidepressant activity of monoamine oxidase inhibitors has been well established for 30 years. Nevertheless, this group of compounds was handled with great care, mainly because of the interaction potential with tyramine-containing foodstuff. With the discovery of reversible and selective inhibitors of monoamine oxidase type A a renaissance of these compounds has begun. In this paper one of these new substances--Brofaromine--will be described in detail. Biochemical and pharmacological aspects will be reviewed, showing that Brofaromine is a selective and reversible inhibitor of monoamine oxidase type A with additional serotonin reuptake inhibiting properties. Both mechanisms of action may synergize in the antidepressant effect of the compound. The main results of clinical trials in depression and other indication areas will also be covered. Special attention will be put on the side effect profile.
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Monoamine oxidase inhibition by the MAO-A inhibitors Brofaromine and clorgyline in healthy volunteers.
Journal of neural transmission. General section, 1994Co-Authors: C. H. Gleiter, K. H. Antonin, Rainer Schulz, B. Mühlbauer, E. Nilsson, P. R. BieckAbstract:The present study compared the extent and duration of MAO inhibition by the selective and reversible MAO-A inhibitor Brofaromine with the selective and irreversible MAO-A inhibitor clorgyline using amine pressor tests and excretion of urinary amine metabolites (MHPG, tryptamine). The pharmacological characterization of clorgyline as an irreversible and Brofaromine as a reversible MAO-A inhibitor in clinically effective doses was confirmed in humans.
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Role of cytochrome P4502D6 in the metabolism of Brofaromine. A new selective MAO-A inhibitor.
European journal of clinical pharmacology, 1993Co-Authors: N. Feifel, P. R. Bieck, K. H. Antonin, K. Kucher, L. Fuchs, M. Jedrychowski, E. K. Schmidt, C. H. GleiterAbstract:The metabolic fate of Brofaromine (CGP 11 305 A), a new, reversible, selective MAO-A inhibitor, has been assessed in poor (PM) and extensive (EM) metabolizers of debrisoquine. Compared to EM, PM had significantly longer t1/2 (136%) and larger AUC(0−∞) (110%) of the parent compound Brofaromine and a lower Cmax (69%) and AUC (0–72 h) (40%) of its O-desmethyl metabolite. The mean metabolite/substrate ratio (based on urine excretion) was about 6-times greater in EM than in PM. Treatment with quinidine converted all EM into phenocopies of PM. All pharmacokinetic parameters of Brofaromine and O-desmethyl-Brofaromine in EM treated with quinidine were similar to those of untreated PM, including the metabolite/substrate ratio. Quinidine treatment of PM did not alter the pharmacokinetics of Brofaromine or of its metabolite, nor the metabolite/substrate ratio. The results indicate a role for the debrisoquine type of oxidation polymorphism in the O-demethylation and pharmacokinetics of Brofaromine.
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Administration of Sympathomimetic Drugs with the Selective MAO-A Inhibitor Brofaromine
Drug Investigation, 1992Co-Authors: C. H. Gleiter, K. H. Antonin, B. Mühlbauer, G. Gradin-frimmer, P. R. BieckAbstract:The interaction between the sympathomimetic agents phenylephrine and phenylpropanol-amine (as used in cold remedies or anorexiants) and the new selective and reversible MAO-A inhibitor Brofaromine (Consonar®) 75mg administered twice daily for 10 days was assessed in 6 volunteers, with particular attention to the occurrence of hypertensive episodes. The recommended maximal intranasal dose of phenylephrine (2.5mg; Neo-Synephrine®) caused no clinically relevant increase in blood pressure before or during Brofaromine treatment. Immediate release phenylpropanolamine (in gelatine capsules) caused a 3.3-fold increase in pressor sensitivity during Brofaromine treatment. Two to 3 days after discontinuation of Brofaromine treatment pressor sensitivity to immediate release phenylephrine was increased only 1.4-fold. The pressor effect of slow release phenylpropanolamine 75mg (Acutrim Late Day®) was monitored continuously for 8 hours. There was no clinically relevant increase in systolic blood pressure during combined treatment with Brofaromine and slow release phenylpropanolamine. Diastolic pressure remained unchanged. The results obtained in this study in healthy young adults show that rapid release formulations of phenylpropanolamine should be avoided during treatment with Brofaromine. The combined administration of Brofaromine and clinically used doses of nasal phenylephrine or phenylpropanolamine in slow release formulations appears to be safe with regard to hypertensive episodes. However, caution may be necessary in hypertensive patients. The rapid reduction in pressor sensitivity after the discontinuation of Brofaromine treatment provides evidence of the reversibility of MAO inhibition.
P.c. Waldmeier - One of the best experts on this subject based on the ideXlab platform.
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Brofaromine--a review of its pharmacological properties and therapeutic use.
Journal of neural transmission (Vienna Austria : 1996), 1996Co-Authors: H.-p. Volz, P.c. Waldmeier, C. H. Gleiter, M Struck, H.-j. MöllerAbstract:The antidepressant activity of monoamine oxidase inhibitors has been well established for 30 years. Nevertheless, this group of compounds was handled with great care, mainly because of the interaction potential with tyramine-containing foodstuff. With the discovery of reversible and selective inhibitors of monoamine oxidase type A a renaissance of these compounds has begun. In this paper one of these new substances--Brofaromine--will be described in detail. Biochemical and pharmacological aspects will be reviewed, showing that Brofaromine is a selective and reversible inhibitor of monoamine oxidase type A with additional serotonin reuptake inhibiting properties. Both mechanisms of action may synergize in the antidepressant effect of the compound. The main results of clinical trials in depression and other indication areas will also be covered. Special attention will be put on the side effect profile.
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Radiosynthesis of [11C]Brofaromine, a potential tracer for imaging monoamine oxidase A.
Nuclear medicine and biology, 1996Co-Authors: Simon M. Ametamey, P.c. Waldmeier, H.-f. Beer, Ilonka Guenther, Angelo Antonini, Klaus L. Leenders, Pius A. SchubigerAbstract:Abstract Brofaromine(4–5(-methoxy-7-bromobenzofuranyl)-2-piperidine-HCl) is a potent and selective inhibitor of monoamine oxidase (MAO) A. Two methods for its synthesis and a preliminary positron emission tomography (PET) evaluation in monkey brain are described. The first method, at low carrier concentration of CO 2 , consisted of direct O-methylation of (4-(5-hydroxy-7-bromobenzofuranyl)-2-piperidine). The total radiochemical yield achieved ranged from 30 to 50% (from end of bombardment [EOB] and decay corrected) with an overall synthesis time of 45 min. The second approach, with high carrier amounts of CO 2 arising from inherent target problems, was accomplished in a three-step route involving protection of secondary amino functionality, O-methylation and deprotection. The total radiochemical yield was 10% (from EOB and decay corrected) with a total synthesis time of 70 min. For both methods methylation was achieved using the classical methylating agent [ 11 C]CH 3 I, and radiochemical purity was higher than 98%. PET evaluation of the radioligand in a Rhesus monkey showed a high uptake of radioactivity in the brain. Using the irreversible MAO-A inhibitor clorgyline and reversible MAO-A inhibitors moclobemide and Brofaromine, three blockade experiments were designed to determine the extent of specific binding of [ 11 C]Brofaromine to MAO-A. No apparent decrease in accumulation of radioactivity in the monkey brain was observed when compared to a baseline scan.
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Serotonin uptake inhibition by the monoamine oxidase inhibitor Brofaromine
Biological psychiatry, 1993Co-Authors: P.c. Waldmeier, T. Graf, M. Germer, J.j. Feldtrauer, H. HowaldAbstract:Abstract The selective, reversible monoamine oxidase (MAO) A inhibitor Brofaromine inhibits serotonin (5-HT) uptake in animal models in vitro and in vivo. We investigated whether such an effect can be demonstrated at clinical doses in humans by treating three groups of six volunteers with either placebo, 15 mg phenelzine three times a day, or 75 mg Brofaromine twice a day in a 2-week experiment. As an indurect, although relevant parameter, binding of 3 H-paroxetine to the 5-HT uptake sites on blood platelets was assessed. Moreover, wholeblood 5-HT as a measure of platelet 5-HT, and serum homovanillic acid (HVA) to tentatively estimate MAO inhibition, were determined. Brofaromine reduced 3 H-paroxetine binding to platelets compared with placebo by 20%–25% throughout the treatment period, significance being reached on the last treatment day. In contrast, phenelzine tended to increase 3 H-paroxetine binding. Both drugs increased whole-blood 5-HT to approximately 140%–150%. Brofaromine moderately and on some days significantly decreased serum HVA, whereas phenelzine only tended to do so. Our results suggest that Brofaromine at the clinically used dosage of 150 mg/day does indeed inhibit 5-HT uptake, as evidenced by measurements of 3 H-paroxetine binding to platelets.
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Brofaromine: a monoamine oxidase-A and serotonin uptake inhibitor.
Clinical Neuropharmacology, 1993Co-Authors: P.c. Waldmeier, A. Glatt, J. Jaekel, H. BittigerAbstract:Brofaromine is a tight-binding, reversible inhibitor of monoamine oxidase-A (MAO-A), with concomitant serotonin (5-HT) uptake-inhibiting properties. In psychopharmacologic investigations, the compound shows the properties expected of an MAO inhibitor, antagonizing the effects of reserpine, tetrabenazine, and 5-hydroxytryptophan in rats and mice, and suppressing rapid eye movement sleep in cats. Brofaromine showed antidepressant-like activity in a rat social conflict test. In radioligand binding assays, Brofaromine exhibited weak or no interaction with alpha 1- and alpha 2-noradrenergic, 5-HT1, 5-HT2, 5-HT3, cholinergic, histamine H1 and H2, mu-opiate, GABAA, benzodiazepine, adenosine, neurotensin, and substance P receptors. Comparison of in vitro and in vivo potencies to inhibit 5-HT uptake with those of reference drugs, and direct evidence in patients and volunteers suggest that 5-HT uptake inhibition plays a role in the clinical profile of Brofaromine.
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Displacement of in vivo binding of [3H]Brofaromine to rat intestinal monoamine oxidase A by orally administered tyramine.
European journal of pharmacology, 1992Co-Authors: P.c. Waldmeier, K. StöcklinAbstract:Abstract The reversibility of the interaction of inhibitors with monoamine oxidase (MAO) is thought to provide a safety valve with respect to tyramine potentiation. We sought experimental evidence for this concept by studying the binding of orally administered [ 3 H]Brofaromine to the A-form of MAO in the rat ileum. Specific binding, defined by pretreatment with 10 mg/kg clorgyline p.o., amounted to 70–90% of total binding between 30 min and 6 h after administration of the radioligand. Brofaromine and clorgyline dose dependently displaced [ 3 H]Brofaromine with ED 50 values of about 0.2 mg/kg when administered orally after the radioligand; so did orally administered tyramine in doses relevant for tyramine potentiation in the rat. It was also found that tyramine was relatively more effective in partially MAO-inhibited rats. The data suggest that the concept of reversibility functioning as a safety valve with respect to the potentially hazardous effects of tyramine ingestion is realistic.
