9ĭespite its clinical effectiveness in generalized anxiety, buspirone demonstrated limited clinical effectiveness on panic disorders, severe anxiety, phobias, and obsessive compulsive disorders. 1, 10 Buspirone also does not exhibit any anticonvulsant or muscle-relaxing properties, 5 but may interfere with arousal reactions due to its inhibitory action on the aactivity of noradrenergic locus coerulus neurons. This is due to the lack of effects on GABA receptors. 1 Unlike benzodiazepines and barbiturates used in anxiety disorders, buspirone is not associated with a risk for developing physical dependence or withdrawal, or any significant interaction with central nervous system depressants such as ethanol.
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10 Buspirone was not shown to alter the psychomotor or cognitive function in healthy volunteers, and the risk of developing sedation is relatively low compared to other anxiolytics, such as benzodiazepines. 10 The delayed onset of action of buspirone suggests that the therapeutic effectiveness in generalized anxiety may involved more than its molecular mechanism of action at the 5-HT 1A receptors, 9 or buspirone may induce adaptations of 5-HT 1A receptors. The clinical effect of buspirone in alleviating the symptoms of generalized anxiety disorders typically takes 2 to 4 weeks to achieve. 4 Type Small Molecule Groups Approved, Investigational Structure 10 The potential use of buspirone in combination with melatonin in depression and cognitive impairment via promoting neurogenesis has also been investigated. It has also been used as a second-line therapy for unipolar depression when the use of selective serotonin reuptake inhibitors (SSRIs) is deemed clinically inadequate or inappropriate. Buspirone was first approved in 1986 by the FDA 4 and has been used to treat anxiety disorders, such as generalized anxiety disorder (GAD), and relieve symptoms of anxiety. 1 First synthesized in 1968 then patented in 1975, 10 it is commonly marketed under the brand name Buspar®.
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Due to these characteristics, buspirone been termed 'anxioselective'. 13 Unlike many drugs used to treat anxiety, buspirone does not exhibit anticonvulsant, sedative, hypnotic, and muscle-relaxant properties. Belonging to the azaspirodecanedione drug class, 2 buspirone is a serotonin 5-HT 1A receptor agonist that is not chemically or pharmacologically related to benzodiazepines, barbiturates, and other sedative/anxiolytic drugs. Buspar Generic Name Buspirone DrugBank Accession Number DB00490 Backgroundīuspirone is a novel anxiolytic agent with a unique structure and a pharmacological profile.