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Buspirone has also been found to bind with much higher affinity to the dopamine D 3 and D 4 receptors, where it is similarly an antagonist. [45] 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.
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. [47] [48] [50]
Fluvoxamine, sold under the brand name Luvox among others, is an antidepressant of the selective serotonin reuptake inhibitor (SSRI) class. [8] It is primarily used to treat major depressive disorder and, perhaps more-especially, obsessive–compulsive disorder (OCD), [9] but is also used to treat anxiety disorders [10] such as panic disorder, social anxiety disorder, and post-traumatic stress ...
A box of Lorazepam Orion (Lorazepam) tablets. Lorazepam, sold under the brand name Ativan among others, is a benzodiazepine medication. [14] It is used to treat anxiety (including anxiety disorders), trouble sleeping, severe agitation, active seizures including status epilepticus, alcohol withdrawal, and chemotherapy-induced nausea and vomiting. [14]
The authors also warned of the similarities in pharmacology and mechanism of action of the newer nonbenzodiazepine Z drugs. [ 136 ] The elimination half-life of diazepam and chlordiazepoxide , as well as other long half-life benzodiazepines, is twice as long in the elderly compared to younger individuals.
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 ...
Unlike its relative buspirone, however, gepirone has greater efficacy in activating the 5-HT 1A and has negligible affinity for the D 2 receptor (30- to 50-fold lower in comparison to buspirone). [10] However, similarly to buspirone, gepirone metabolizes into 1-(2-pyrimidinyl)piperazine (1-PP), which is known to act as a potent antagonist of ...
Fluphenazine, sold under the brand name Prolixin among others, is a high-potency typical antipsychotic medication. [2] It is used in the treatment of chronic psychoses such as schizophrenia, [2] [3] and appears to be about equal in effectiveness to low-potency antipsychotics like chlorpromazine. [4]