Buspirone: An Anti-Anxiety Drug

Buspirone is a different type of anti-anxiety drug with few adverse effects. Although it's mainly used to treat generalized anxiety disorder (GAD), it also has other interesting uses.
Buspirone: An Anti-Anxiety Drug

Last update: 05 December, 2020

Buspirone is an anti-anxiety drug. It was first synthesized in 1968 and initially developed as an antipsychotic drug. However, it was soon recognized that its anti-anxiety effects were more useful. The U.S. Food and Drug Administration (FDA) approved buspirone in 1986.

Buspirone is an orally active drug. It belongs to the group of azapirones and it differs from other anti-anxiety drugs, both pharmacologically and structurally. Because of this, it has fewer side effects than barbiturates and benzodiazepines. However, it’s slow-acting and it takes between two to four weeks to work. Therefore, if you have an acute anxiety disorder, it isn’t suitable. However, it’s increased in popularity over recent years.

Uses of buspirone

Buspirone is a drug to treat anxiety. It mainly treats generalized anxiety disorder (GAD). According to some studies, it doesn’t differ much in its efficacy from benzodiazepine treatments. It can be used as a second-line anti-depressant when selective serotonin uptake receptors (SSRIs) don’t work or aren’t tolerated, or as an adjuvant to them. Buspirone can also help relieve the sexual side effects of SSRIs.

A handful of tablets.

Some studies suggest buspirone might be helpful in treating social anxiety phobia and attention-deficit/hyperactivity disorder (ADHD). It can also be used to manage agitation and aggression in patients with dementia. Recent evidence suggests that buspirone might have immunosuppressive properties. Therefore, tests are being conducted to see how effective it is in treating atopic dermatitis. Furthermore, investigations are being conducted to see if it can be used in combination with melatonin to promote neurogenesis. This would help in treating depression and cognitive disorders.

Buspirone: how the anti-anxiety drug works

Buspirone operates in a different way to other benzodiazepines and barbiturates. Unlike these anti-anxiety drugs, buspirone doesn’t affect the GABA neurotransmitter. This lack of activity in the GABA receptors has two important consequences for users of buspirone:

Buspirone doesn’t work in treating withdrawal symptoms. For example, when a patient is quitting alcohol, benzodiazepines, or barbiturates.

You can’t become dependent upon it.  And you won’t suffer any withdrawal symptoms when you stop taking it.

Buspirone acts primarily as a partial agonist of the 5-HT1A serotonin receptors. In addition, it has some affinity for 5-HT2 receptors. And it also acts as a weak antagonist of the D2 dopamine receptors.

The specific way in which buspirone works isn’t exactly clear. It’s assumed that increased serotonin activity in different regions of the brain causes the anti-anxiety effect.

At the same time, it’s believed that buspirone exerts modifications on the 5-HT1 receptors, which is why it takes longer to work. It may also indirectly affect other neurotransmitters in the brain.

Buspirone: side effects of the anti-anxiety drug

Compared to other anti-anxiety medications, buspirone has few adverse effects. Its advantages over barbiturates and benzodiazepines include:

  • It doesn’t make you sleepy. It doesn’t have any hypnotic effects.
  • You stay awake and alert.
  • You won’t become dependent upon it. And you won’t suffer withdrawal effects when you stop taking it.
  • You won’t experience any muscle-relaxing effects.
  • You won’t suffer any anticonvulsant episodes.

However, like any drug, it does have some side effects. The most common are:

  • Dizziness.
  • Drowsiness.
  • Headache.
  • Nausea and vomiting.
  • Restlessness syndrome with nervousness and arousal.
A woman looking stressed.

These side effects usually decrease after the first few days of treatment. If they don’t, you should consult your doctor. And, of course, you should also consult your doctor if you suffer more severe symptoms.

You shouldn’t use this drug if you’re taking monoamine oxidase inhibitors (MAOIs). This is due to the risk of hypertension or serotonin syndrome.

In addition, you shouldn’t use this drug if you have severe liver or kidney problems. And furthermore, it can interact with other drugs. You must always ask your doctor for their advice.

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  • Wilson TK, Tripp J. Buspirone. [Updated 2019 Feb 14]. In: StatPearls [Internet]. Treasure Island (FL): StatPearls Publishing; 2019 Jan-. Available from: https://www.ncbi.nlm.nih.gov/books/NBK531477/
  • Howland, R. H. (2015). Buspirone: back to the future. Journal of psychosocial nursing and mental health services, 53(11), 21-24.
  • Fava, M., Targum, S. D., Nierenberg, A. A., Bleicher, L. S., Carter, T. A., Wedel, P. C., … & Barlow, C. (2012). An exploratory study of combination buspirone and melatonin SR in major depressive disorder (MDD): a possible role for neurogenesis in drug discovery. Journal of psychiatric research, 46(12), 1553-1563.