Neurochemical and autonomic pharmacological profiles of the 6-aza-analogue of mianserin, org 3770 and its enantiomers

Th, de Boer; Maura, Guido; Raiteri, Maurizio; Cj, de Vos; Wieringa, Joop H.; Rm, Pinder

doi:10.1016/0028-3908(88)90149-9

Cited by 176 publications

(95 citation statements)

References 33 publications

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“…In such a pharmacologic condition, 5-HT terminals would release more 5-HT because there would no longer be any direct negative feedback action (Figure 1). This possibility does not, however, appear consistent with recent reports of the beneficial action of mirtazapine in SSRI-resistant patients, despite this drug's having an affinity for alpha 2-adrenoceptors 10 times lower than its 5-HT 2A property (113)(114)(115). It remains to be determined, however, whether mirtazapine's apparent benefit is a true anti-OCD effect or a nonspecific anxiolytic action.…”

Section: Ssri Effects On Postsynaptic 5-ht Receptors In Brain Regionsmentioning

confidence: 59%

Pharmacotherapies in the Management of Obsessive—Compulsive Disorder

2006

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T he first reports of the potential for medications to exert an antiobsessional effect in patients without major depression were published about 35 years ago (1-4). The tricyclic antidepressant G-34586, or CMI, was used successfully in these first attempts. The serendipitous finding of its beneficial effect on obsessions in depression patients motivated its use in that disorder. Several case series in the following decade seemed to confirm the usefulness of this medication in treating OCD, then denoted obsessive-compulsive neurosis. The first controlled trials demonstrating a therapeutic action of CMI in OCD were published in 1980 (5,6). These were followed by many positive studies (see 7 for a review). Clinical Implications· OCD is a chronic disorder amenable to pharmacotherapy using a single class of medications: the potent SRIs. · With a good knowledge of the properties of these drugs, optimal response and patient safety and comfort can be achieved. · It is possible to augment the anti-OCD response with various augmentation strategies. · The response to various pharmacotherapies is generally partial, and their administration must be prolonged to avoid the resurgence of symptoms. Limitations· SRIs exert class side effects that are sometimes difficult to minimize. · Few augmentation strategies are supported by double-blind studies.Few medications are effective in treating obsessive-compulsive disorder (OCD). As monotherapy, only potent serotonin (5-HT) reuptake inhibitors (SRIs) consistently exert an intrinsic therapeutic action in OCD. Their use in OCD, however, differs from their use in depression. This paper first reviews the evidence supporting the key role of 5-HT as a pivotal neurotransmitter in the anti-OCD response. Then, we describe the practicalities of SRI use, followed by the steps that can be taken when these medications do not produce an adequate clinical response. We provide specifics for the treatment of children and adolescents with OCD. We include a brief description of the brain circuitry involved in OCD and the mechanisms of action of the pharmacologic agents reported to be effective in this disorder, as well as those that are useful in depression but not in OCD. We present this information to promote better understanding of the research endeavours needed to develop new pharmacotherapeutic approaches. Information on funding and support and author affiliations appears at the end of the article.

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Section: Ssri Effects On Postsynaptic 5-ht Receptors In Brain Regionsmentioning

confidence: 59%

Pharmacotherapies in the Management of Obsessive—Compulsive Disorder

2006

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“…83) (Stimmel et al, 1997). Mirtazepine acts by antagonizing the a 2 -adrenergic receptor, which results in downstream effects on serotonin and norepinephrine release (de Boer et al, 1988). It also binds to some serotonin receptors and the H 1 receptor.…”

Section: Drugs With Metabolites That Possess Target Potency But Comentioning

confidence: 99%

Pharmacologically Active Drug Metabolites: Impact on Drug Discovery and Pharmacotherapy

Obach

2013

Pharmacol Rev

137

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“…Mirtazapine is an antidepressant that acts as an ␣-2-receptor antagonist and selective blocker of postsynaptic 5HT2 and 5HT3 receptors. 46 One class II study evaluated the safety and tolerability of mirtazapine in 17 patients with ET and found no significant improvement with mirtazapine use. 47 Nifedipine (Adalat, Procardia).…”

Section: F Pharmacologic Agents With Recommendations Against Use (Lmentioning

confidence: 99%

Practice Parameter: Therapies for essential tremor [RETIRED]

et al. 2005

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Abstract-Background: Essential tremor (ET) is one of the most common tremor disorders in adults and is characterized by kinetic and postural tremor. To develop this practice parameter, the authors reviewed available evidence regarding initiation of pharmacologic and surgical therapies, duration of their effect, their relative benefits and risks, and the strength of evidence supporting their use. Methods: A literature review using MEDLINE, EMBASE, Science Citation Index, and CINAHL was performed to identify clinical trials in patients with ET published between 1966 and August 2004. Articles were classified according to a four-tiered level of evidence scheme and recommendations were based on the level of evidence. Results and Conclusions: Propranolol and primidone reduce limb tremor (Level A). Alprazolam, atenolol, gabapentin (monotherapy), sotalol, and topiramate are probably effective in reducing limb tremor (Level B). Limited studies suggest that propranolol reduces head tremor (Level B). Clonazepam, clozapine, nadolol, and nimodipine possibly reduce limb tremor (Level C). Botulinum toxin A may reduce hand tremor but is associated with dose-dependent hand weakness (Level C). Botulinum toxin A may reduce head tremor (Level C) and voice tremor (Level C), but breathiness, hoarseness, and swallowing difficulties may occur in the treatment of voice tremor. Chronic deep brain stimulation (DBS) (Level C) and thalamotomy (Level C) are highly efficacious in reducing tremor. Each procedure carries a small risk of major complications. Some adverse events from DBS may resolve with time or with adjustment of stimulator settings. There is insufficient evidence regarding the surgical treatment of head and voice tremor and the use of gamma knife thalamotomy (Level U). Additional prospective, double-blind, placebo-controlled trials are needed to better determine the efficacy and side effects of pharmacologic and surgical treatments of ET.

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Neurochemical and autonomic pharmacological profiles of the 6-aza-analogue of mianserin, org 3770 and its enantiomers

Cited by 176 publications

References 33 publications

Pharmacotherapies in the Management of Obsessive—Compulsive Disorder

Pharmacotherapies in the Management of Obsessive—Compulsive Disorder

Pharmacologically Active Drug Metabolites: Impact on Drug Discovery and Pharmacotherapy

Practice Parameter: Therapies for essential tremor [RETIRED]

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