Buspirone: An Update on a Unique Anxiolytic Agent

doi:10.1002/j.1875-9114.1988.tb03543.x

Paper

Buspirone: An Update on a Unique Anxiolytic Agent

Published Mar 4, 1988 · M. Jann

Pharmacotherapy: The Journal of Human Pharmacology and Drug Therapy

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70

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0

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Abstract

Buspirone (Buspar) is a azaspirodecanedione anxiolytic agent. Its mechanism of action is extremely complex, but current investigations indicate that its main neuropharmacologic effects are mediated by the 5‐HT1A receptors. Other neuroreceptor systems could be involved, as buspirone displays some affinity for DA2 autoreceptors and 5‐HT2 receptors. It has been proposed that inhibition of synthesis and release of serotonin result through the combined interactions of neuroreceptors and secondary messenger systems. This action leads to inhibition of the firing rate of 5‐HT‐containing neurons in the dorsal raphe. From this novel profile, that differs from that of the benzodiazepines, buspirone lacks anticonvulsant and muscle‐relaxant properties, and causes only mimimal sedation. The drug is rapidly absorbed after oral administration, with a mean bioavailability of 3.9%. After a single oral dose, the mean elimination half‐life is 2.1 hours. Buspirone is mainly bound to albumin and oxacid glycoprotein. It is metabolized to an active metabolite 1‐(2‐pyrimidinyl) piperazine (1‐PP). The mean elimination half‐life of 1‐PP is 6.1 hours. Buspirone is indicated in the treatment of generalized anxiety disorders. Its efficacy is comparable to the benzodiazepines. Its use in depression and panic disorders requires further investigation. When combined with alcohol or given alone, psychomotor impairment was not detected. Abuse, dependence, and withdrawal symptoms have not been reported. The frequency of adverse effects is low, and the most common effects are headaches, dizziness, nervousness, and lightheadness. Buspirone should be added to drug formularies and could represent a significant addition in psychopharmacology.

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Study Snapshot

Buspirone is a promising anxiolytic agent for treating generalized anxiety disorders, with comparable efficacy to benzodiazepines and low frequency of adverse effects.

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

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Paper

Buspirone: An Update on a Unique Anxiolytic Agent

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References

Buspirone in the long-term treatment of generalized anxiety disorder.

Buspirone effectively reduces anxiety in long-term generalized anxiety disorder patients, with well-tolerated side effects and low discontinuation rates after the third month.

A comparison of buspirone, diazepam, and placebo in patients with chronic anxiety states.

Buspirone is ineffective in treating chronic anxiety in patients with previous long-term benzodiazepine therapy, suggesting its potential for use in chronic anxiety patients not cross-tolerant to benzodiazepines.

A second look at the second messenger hypothesis.

The second messenger hypothesis suggests that signal specificity may be encoded in the primary structure of receptors, potentially addressing the paradox of information-transfer within cells through few intermediates.

Assessing the potential for buspirone dependence or abuse and effects of its withdrawal.

Buspirone, a new antianxiety agent, does not lead to drug dependence or withdrawal symptoms, as assessed in animal and clinical studies.

Lack of Interaction Between Cimetidine and Buspirone

Within normal therapeutic dosage ranges, cimetidine and buspirone show no clinically significant interaction.

A Comparison of Buspirone and Placebo in Relieving Benzodiazepine Withdrawal Symptoms

Buspirone does not help benzodiazepine withdrawal and does not suppress benzodiazepine withdrawal symptoms.

Differential effects of the anxiolytic drugs, diazepam and buspirone, on memory function.

Diazepam has a selective impairment in noun recall after a 20-minute delay, while buspirone shows no significant effect on delayed recall of word lists in generalized anxiety disorder patients.

Failure of buspirone to manage benzodiazepine withdrawal.

Buspirone does not significantly reduce the intensity of benzodiazepine withdrawal, as it has no clinically significant benzodiazepine receptor activity.

Citations

Spiro-Heterocycles: Recent Advances in Biological Applications and Synthetic Strategies

Spiro-heterocycles have diverse biological applications and are versatile building blocks for synthesizing biologically useful and structurally complex motifs.

Longitudinal cytokine and multi-modal health data of an extremely severe ME/CFS patient with HSD reveals insights into immunopathology, and disease severity

Longitudinal multi-omics data and AI techniques can help better understand ME/CFS and its comorbidities, potentially guiding personalized medicine strategies.

Buspirone Enhances Cell Survival and Preserves Structural Integrity during Oxidative Injury to the Retinal Pigment Epithelium

Buspirone, an anxiety medication, can protect retinal pigment epithelium from oxidative stress-induced damage, potentially aiding in treating or preventing dry age-related macular degeneration.

Pharmacological management of neurocognitive impairment in schizophrenia: A narrative review

Pharmacological options for treating cognitive deficits in schizophrenia have not shown significant benefits, but cognitive abilities play a crucial role in independent living, employment, and overall well-being.

Synthesis of 2‐amino‐4‐aryl‐6‐styrylpyrimidines through aza‐Michael addition/nucleophilic addition/dehydrogenation cascade reactions

This efficient method for synthesizing 2amino-4-aryl-6-styrylpyrimidines using distyryl ketones and guanidine hydrochloride offers easy-to-obtain substrates, transition-metal-free system, mild reaction conditions, high

Worsening psychosis associated with administrations of buspirone and concerns for intranasal administration: A case report

Buspirone may worsen psychosis when administered through intranasal administration, potentially due to increased dopaminergic metabolites and faster drug absorption.

Buspirone Ameliorates Colon Inflammation in TNBS-Induced Rat Acute Colitis: The Involvement of TLR4/NF-kB Pathway.

Buspirone effectively reduces colon inflammation in a TNBS-induced rat model of acute colitis by lowering the TLR4/NF-B signaling pathway's activity.

Further disentangling the motivational processes underlying benzodiazepine hyperphagia

Benzodiazepines selectively enhance the hedonic acceptance of gustatory orosensory stimuli, independent of general anxiolytic or oromotor coordination effects, or physiological states like thirst.

Recurrent Suicidal Ideation With Topiramate in Tourette Syndrome

Buspirone may have abuse potential, particularly in individuals with a history of substance abuse or incarceration, and prescribers should exercise caution in prescribing patterns.