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Overview: Buspirone an Anxioselective Neuromodulator

From Innovative Psychopharmacotherapy

Vernon M. Neppe

Buspirone (BuSpar) belongs to a new chemical subgroup, previously called the azaspirodecanediones, now referred to as the azapirones It is the first in the class of pure anxioselective agents. It differs substantially in both clinical and pharmacological properties from the benzodiazepines. Clinically, it does not cause the sedation, hypnosis, anticonvulsant effects and muscle relaxation effects of the benzodiazepines, and it takes several weeks to achieve its maximal therapeutic effects as an anxiety agent. Consequently, target symptoms such as decreased agitation, irritability, improved concentration, and diminished worry should be sought after during its first weeks of administration. Chemically, the exact anxioselective effect probably relates to a post-synaptic partial agonist effects at the serotonin 1A receptor at usual therapeutic doses (30-60 mg per day). At higher supratherapeutic doses it has a partial agonist dopaminergic effect. Its action initially is as a pure agonist at the autoreceptor raphe nucleus level; its post-synaptic effect impacts several strategic areas - limbic system, hippocampus, amygdala, cerebral cortex and even neuroglia. There are no significant neuro-endocrine effects of therapeutic doses, and the drug has no antipsychotic effects. Eleven major research studies, including nine double-blind studies of buspirone versus diazepam or chlorazepate, have shown equal efficacy with less untoward side effects and a marked superiority compared with placebo after four weeks of treatment for generalized anxiety disorder. This bears out the anxiety paradigm studies in experimental animals. The anxiolytic action may be an effect of either the parent drug or its metabolite, 1- 2- pyrimidinyl piperazine (1PP) or both. Studies in both man and animals suggest buspirone should not induce physical or psychological dependence, and drug reactions with other psychotropics are under study. It does not significantly interact with propranolol, but may slightly raise levels of haloperidol. It is possible that it could be effective in the prophylaxis of panic disorder, tardive dyskinesia, in the management of hostility, and of obsessionality. These are all areas for future research.

Keywords

1- (2-pyrimidinyl) piperazine (1-PP), Anxioselectivity, Azaspirodecanedione, Azapirone, Buspirone, Buspirone neuropharmacology (animal, man), Dependence - buspirone, Intrinsic dopaminergic activity, modulation, Non-benzodiazepine anxiolytic, Pharmacokinetics of buspirone, Serotonin-mimetic

 

 


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