Buspirone: an anxiolytic without many side effects

Buspirone is an anxiolytic drug. It was first synthesized in 1968. It was initially developed as an antipsychotic, but its anxiolytic effects were soon seen to be more useful. It was approved by the United States Drug Agency -FDA- in 1986.

It is active orally. It belongs to the azapirone group and is different from other anxiolytic drugs, both pharmacologically and structurally. Because of this, Has fewer adverse effects than barbiturates and benzodiazepines.

However, it is slow acting. Its anxiolytic effect takes two to four weeks to establish itself. Therefore, it is not suitable for an acute anxiety situation. Still, its popularity is growing in recent years.

What is buspirone used for?

Buspirone is used as an anxiolytic mainly in the treatment of generalized anxiety disorder (GAD).. According to some studies, its effectiveness does not differ much from that of benzodiazepine treatments.

It can be used as a second-line antidepressant when Selective Serotonin Reuptake Inhibitors (SSRIs) do not work or are not tolerated; or also as an adjuvant to them. Buspirone is sometimes used to relieve the sexual side effects of SSRIs..

Some studies suggest that could be useful in the treatment of social phobia and attention deficit hyperactivity disorder (ADHD). Also in the management of disorders with agitation and aggression in people with dementia.

It has recently been discovered that buspirone may also have immunosuppressive properties. That is why its effectiveness is being studied in atopic dermatitis, for example. Another possibility that being investigated is its use in combination with melatonin to promote neurogenesis. This could be effective in treating depression and cognitive disorders.

Mechanism of action

The mechanism of action of buspirone also differs from that of benzodiazepines or barbiturates. Unlike these anxiolytics, Buspirone has no activity on GABA neurotransmitter (NT) receptors..

This lack of activity at GABA receptors has two important consequences for buspirone:

Not effective in the treatment of withdrawal syndrome due to the withdrawal of benzodiazepines, barbiturates or alcohol.There is no risk of generating dependency nor withdrawal syndrome.

Buspirone acts primarily as a partial agonist of serotonin 5HT1a receptors.. In addition, it has a certain affinity for 5HT2 receptors and acts as a weak antagonist of dopamine D2 receptors.

The specific mechanism by which buspirone acts is not entirely clear. Be supposed to the increase in serotonin activity in different regions of the brain is what causes the anxiolytic effect.

Likewise, buspirone is believed to exert modifications on 5HT1a receptors. That is why its effect would take longer to manifest. It may also have indirect effects on other NTs in the brain..

Side effects

Compared to other anxiolytics, it is a drug with few adverse effects. Some advantages over barbiturates and benzodiazepines are:

It does not have sedative or hypnotic effects.It maintains alertness and alertness. It does not cause dependence or generate withdrawal syndrome.It lacks a muscle relaxing effect.It lacks anticonvulsant properties.

Despite this, like any drug, it is not free of some side effects. The most frequent adverse effects in treatment with buspirone are:

Dizziness.Drowsiness.Headache.Nausea and vomiting.Restlessness syndrome with nervousness and excitement.

Usually, These adverse effects usually decrease after the first days of treatment.. If this is not the case, you should consult your doctor, just as if other more serious symptoms appear.

The use of buspirone is contraindicated in patients being treated with monoamine oxidase inhibitor antidepressants (MAOIs).. This is due to the risk of suffering from hypertension or serotonin syndrome.

Its use is also contraindicated in people with serious liver or kidney problems. Additionally, it may interact with other drugs. The doctor is always the one who has to evaluate each case.

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