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A major metabolite of buspirone, 1-(2-pyrimidinyl)piperazine (1-PP), occurs at higher circulating levels than buspirone itself and is known to act as a potent α 2-adrenergic receptor antagonist. [ 44 ] [ 46 ] [ 47 ] This metabolite may be responsible for the increased noradrenergic and dopaminergic activity observed with buspirone in animals.
A common metabolite of several azapirones including buspirone, gepirone, ipsapirone, revospirone, and tandospirone is 1-(2-pyrimidinyl)piperazine (1-PP). [ 47 ] [ 48 ] [ 49 ] 1-PP possesses 5-HT 1A partial agonist and α 2 -adrenergic antagonist actions and likely contributes overall mostly to side effects.
They showed that "In terms of efficacy, all antidepressants were more effective than placebo, with odds ratios (ORs) ranging between 2.13 (95% credible interval [CrI] 1.89–2.41) for amitriptyline and 1.37 (1.16–1.63) for reboxetine." [16] The odds ratios were specifically in terms of response rates (≥50% reduction in observer-rated ...
The TCAs are used primarily in the clinical treatment of mood disorders such as major depressive disorder (MDD), dysthymia, and treatment-resistant variants. They are also used in the treatment of a number of other medical disorders, including cyclic vomiting syndrome (CVS) and anxiety disorders such as generalized anxiety disorder (GAD), social phobia (SP) also known as social anxiety ...
A serotonin reuptake inhibitor (SRI) is a type of drug which acts as a reuptake inhibitor of the neurotransmitter serotonin (5-hydroxytryptamine, or 5-HT) by blocking the action of the serotonin transporter (SERT). This in turn leads to increased extracellular concentrations of serotonin and, therefore, an increase in serotonergic ...
The consensus is to reduce dosage gradually over several weeks, e.g. 4 or more weeks for diazepam doses over 30 mg/day, [1] with the rate determined by the person's ability to tolerate symptoms. [120] The recommended reduction rates range from 50% of the initial dose every week or so, [121] to 10–25% of the daily dose every 2 weeks. [120]