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  • 1
    Electronic Resource
    Electronic Resource
    Roxindole, a dopamine autoreceptor agonist, in the treatment of major depression (1993)
    Springer
    Psychopharmacology 111 (1993), S. 123-126 
    Details
    ISSN: 1432-2072
    Keywords: Roxindole ; Dopamine autoreceptor agonist ; Dopamine ; Depression ; Prolactin
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract Roxindole is a potent autoreceptor-“selective” dopamine agonist originally developed for the treatment of schizophrenic syndromes. The drug also inhibits 5-HT uptake and has 5-HT1A agonistic actions. In this open clinical trial 12 in-patients suffering from a major depressive episode (DSM-III-R) were treated with roxindole for 28 days in a fixed dosage of 15 mg per day. A reduction of at least 50% in HAMD-17 total scores was observed in 8 out of 12 patients after 4 weeks (mean HAMD-17 reduction of 56% in all patients), while 4 patients did not respond to roxindole treatment. Half of the patients showed a complete psychopathological remission (HAMD-17 〈8). Roxindole's onset of antidepressant action was remarkably rapid. Seven out of eight responders improved within the first 2 weeks of treatment (at least 50% decrease in HAMD-17 total score), and four patients were nearly asymptomatic within 1 week. Our results indicate that roxindole may possess potent antidepressant properties and that its efficacy should be further evaluated by double-blind controlled studies against reference drugs.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF02257418
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    Paper (German National Licenses)
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  • 2
    Electronic Resource
    Electronic Resource
    The neuroendocrinological profile of roxindole, a dopamine autoreceptor agonist, in schizophrenic patients (1995)
    Springer
    Psychopharmacology 117 (1995), S. 472-478 
    Details
    ISSN: 1432-2072
    Keywords: Roxindole Dopamine autoreceptor agonism 5-HT reuptake inhibition ; 5-HT1A agonism Prolactin ; TSH ; GH ; TRH stimulation
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract Roxindole is a potent autoreceptor-selective dopamine agonist with additional properties as a serotonin reuptake inhibitor and 5-HT1A agonist. In order to get more insight into its mode of action in various psychiatric populations, we evaluated the effects of subchronic roxindole treatment on pituitary and adrenal hormone secretion, i.e. release of prolactin, thyroid stimulating hormone (TSH), growth hormone (GH), luteinizing hormone (LH), and cortisol. Fifteen schizophrenic patients with positive and negative symptomatology, respectively, were treated with roxindole for 28 days. Both basal and thyrotropin releasing hormone (TRH) -induced prolactin secretion diminished significantly to 26.4% and 22.8% of baseline levels, respectively, under roxindole. Basal GH secretion was insignificantly elevated by 89%, whereas GH levels increased nearly 3-fold after stimulation by TRH. TSH levels decreased insignificantly to 57.5% of baseline levels, while TRH-induced TSH release was not affected by subchronic roxindole. Roxindole treatment influenced neither LH secretion nor cortisol release. Our results indicate that roxindole's dopaminergic actions might prevail over its serotonergic effects, at least as far as the regulation of anterior pituitary hormone secretion is concerned.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF02246221
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    Paper (German National Licenses)
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  • 3
    Electronic Resource
    Electronic Resource
    Amisulpride versus flupentixol in schizophrenia with predominantly positive symptomatology – a double-blind controlled study comparing a selective D2-like antagonist to a mixed D1-/D2-like antagonist (1998)
    Springer
    Psychopharmacology 137 (1998), S. 223-232 
    Details
    ISSN: 1432-2072
    Keywords: Key words Amisulpride ; Flupentixol ; Schizophrenia ; Antipsychotic efficacy ; Extrapyramidal tolerability ; Atypical neuroleptic ; Dopamine ; Selective D2-like antagonism ; Mixed D1-/D2-like antagonism
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract The benzamide amisulpride (ASP) is a selective D2-like dopamine antagonist, while flupentixol (FPX), a thioxanthene, blocks D2-like, D1-like and 5-HT2 receptors. To evaluate efficacy and safety of ASP and to investigate the importance of an additional D1-like antagonism for antipsychotic effects and extrapyramidal tolerability, a randomized double-blind multi-center study versus FPX as reference drug was performed for 6 weeks in 132 patients suffering from acute schizophrenia (DSM-III-R) with predominant positive symptomatology. Doses were initially fixed (ASP: 1000 mg/day; FPX: 25 mg/day) but could be reduced by 40% in case of side effects (mean daily doses: ASP: 956 mg; FPX: 22.6 mg). Intention-to-treat evaluation demonstrated significant improvement under both medications. The difference between the mean BPRS decreases of both treatment groups was 5.6 points (95% CI: 0.55; 10.65) in favour of ASP. According to CGI, 62% of patients in either drug group were treatment responders. ANCOVA analysis showed that reductions of BPRS (ASP: −42%; FPX: −32%) and SAPS (ASP: −78%; FPX: −65%) were more pronounced under ASP. Due to adverse events, significantly fewer ASP patients (6%) were withdrawn from the study (FPX: 18%). Extrapyramidal tolerability was better in the ASP group, as demonstrated by smaller increases in the Simpson-Angus Scale, the AIMS, and the Barnes Akathisia Scale in ANCOVA analyses with dosage as covariate. ASP appears to be as effective as FPX with regard to antipsychotic effects on positive schizophrenic symptomatology, while extrapyramidal tolerability is better. These conclusions have to be drawn cautiously, as dosage effects on outcome parameters cannot be entirely ruled out. The present results question the notion that additional blockade of D1-like receptors may be necessary to achieve sufficient antipsychotic effects or to improve extrapyramidal tolerability.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/s002130050614
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  • 4
    Electronic Resource
    Electronic Resource
    Occupancy of striatal D2-like dopamine receptors after treatment with the sigma ligand EMD 57445, a putative atypical antipsychotic (1999)
    Springer
    Psychopharmacology 146 (1999), S. 81-86 
    Details
    ISSN: 1432-2072
    Keywords: Key words EMD 57445 ; Sigma receptor ; Antipsychotic ; Dopamine receptor ; Iodobenzamide ; Single photon emission computed tomography
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract  Rationale: EMD 57445 (panamesine) is a high affinity sigma ligand with the profile of an atypical antipsychotic in animal studies. It has been reported recently to have antipsychotic activity in schizophrenia. However, its metabolite, EMD 59983, binds also to D2 and D3 dopamine (DA) receptors. Objectives: The aim of this study was to test, using single photon emission computed tomography (SPECT) and [123I]iodobenzamide (IBZM) as the radiotracer, whether EMD 59983 would pass the blood-brain barrier and to what extent it would contribute to the effects of EMD 57445 in schizophrenia. Methods: Two IBZM SPECT-scans were performed in five neuroleptic-free schizophrenic patients (DSM IV), one before and one after treatment with 60 mg panamesine daily for a treatment duration of 12–26 days. Results: A high occupancy of striatal D2-like DA receptors similar to that induced by typical neuroleptics was observed in all patients treated with EMD 57445. Conclusions: Our results suggest that a possible antipsychotic activity of EMD 57445 in schizophrenia is not necessarily attributable to its affinity for sigma receptors, but could be simply due to the potent antidopaminergic effects of EMD 59983, its main metabolite.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/s002130051091
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    Paper (German National Licenses)
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