Buspirone is a prescription medication indicated primarily for anxiety, but can also be used for other disorders such as depression, attention deficient disorder (ADD) and may be useful for treating substance abuse. Buspirone has very mild side effects, is not addictive, and does not act as a sedative. Read on to learn more.

DisclaimerBy writing this post, we are not recommending this drug. Some of our readers who were already taking the drug requested that we commission a post on it and we are simply providing information that is available in the scientific and clinical literature. Please discuss your medications with your doctor.

What is Buspirone?

Buspirone is an anti-anxiety medication (anxiolytic) that is sold under the brand name Buspar. It is chemically and pharmacologically distinct from other anti-anxiety drugs such as benzodiazepines and offers reduced anxiety without physical dependence or withdrawal symptoms [1, 2].

Buspirone is most commonly used for generalized anxiety disorder but is also prescribed occasionally for anxiety related to other brain-related disorders such as depression, attention deficit disorder, social phobia, Parkinson’s disease and Alzheimer’s [3, 4].

Mechanism of Action

The mechanism of action of buspirone is not fully understood. It is known that buspirone binds to serotonin (5-HT1A) receptors and partially mimics the action of serotonin. Serotonin is a chemical in the brain that promotes feelings of well-being and happiness [3, 5].

Buspirone is also able to partially block the action of some dopamine receptors (DRD2) [3, 5].

When buspirone is broken down by the body, one of the major byproducts called 1-PP becomes quite concentrated in the blood. 1-PP can block the activity of a receptor that epinephrine/adrenaline activates (α2-adrenergic), which could account for some of the anti-depressant effects of buspirone [6, 7, 8, 5].

When taken by mouth (20 mg) it is rapidly absorbed and reaches its peak concentration within the blood in less than an hour. It takes 2.5 hours for half of the initial dose to be removed from the body (half-life). However, like most anti-anxiety medications, it may take 3-4 weeks until you start to feel relief from symptoms [5, 3].

Uses of Buspirone

Buspirone was initially developed for the treatment of generalized anxiety disorder but has been found to be useful for several other indications. Generalized anxiety disorder is persistent, uncontrollable worry that requires professional therapy or medication to be resolved [3, 9].

1) Anxiety

Buspirone treatment is more effective than placebo in treating and maintaining stability for generalized anxiety based on a ten-week trial in 125 patients (double-blind randomized controlled trial) [10].

Buspirone is as effective as benzodiazepines, such as diazepam or lorazepam for treating generalized anxiety. This was shown in a study (double-blind randomized controlled trial) of 367 menstruating female patients, and 2 studies with 84 adults [11, 12, 13].

Buspirone is also equal to or better (after 2 and 4 weeks) than sertraline (an SSRI) for generalized anxiety disorder based on a study (single-blind randomized controlled trial) of 46 people [14].

2) Depression

Buspirone is more effective for treating major depressive disorder than placebo, based on a meta-analysis looking at the results of 15 randomized controlled trials with a total of 2,469 patients [15].

Two large studies performed in 300 adults for 8 weeks with both major depression and moderate anxiety resulted in significant improvement in symptoms for a majority of treated patients [16, 17].

Taking buspirone for 8 weeks improved major depression in 61% of 177 elderly patients (double-blind randomized controlled trial) [18].

A randomized study of 286 adults being treated for depression with citalopram, found that augmentation with 60 mg/day buspirone resulted in a 30% remission rate based on the Hamilton Rating Scale for Depression [19].

Buspirone increases cortisol secretion (via 5HT1A), which may improve depressive symptoms [20].

3) Substance Abuse

The use of buspirone to help overcome substance abuse has had somewhat disappointing results, as conflicting data have been published for substance abuse of many types.

Buspirone was useful in helping high anxiety patients stop smoking in a study with 101 people. Participants that were considered to be low anxiety did not experience any benefit from taking buspirone [21].

However, it did not help 35 crack cocaine users (60 mg/d) in their addiction [22].

The effects of buspirone treatment on marijuana dependence have been conflicting. One study of 50 adults found it helped, while it didn’t with another study of 175 people [23, 24].

Buspirone did not help methamphetamine use in 8 participants [25].

In primates, buspirone was found to be helpful in reducing nicotine and cocaine addiction [26].

4) May Reduce Sexual Risk Taking in Cocaine Users

There is an association between cocaine use and sexually transmitted diseases that are attributed to an increase in sexual desire and decrease in self-control when using cocaine. Buspirone improves impulse control in rats and reduced the reinforcing effects of cocaine in preclinical trials [27, 28].

Nine cocaine users were treated with 30 mg/day of buspirone for 3 days (repeated measures, inpatient protocol). Buspirone did not interact negatively with cocaine and users were found to be more likely to use a condom [28].

However, a placebo-controlled study of 11 cocaine users found no effect of buspirone on impulse control, but only a slower reaction time at the very highest dose tested (30mg) [29].

Chronic administration of buspirone has some beneficial effect on impulse control in both rodents and non-human primates [30, 31, 32].

5) Symptoms of Autism

In a study of 166 children with Autism, ages 2 to 6, small doses of buspirone (2.5 mg) helped alleviate repetitive behaviors [33].

In 40 kids with autism, low doses of buspirone in combination with an antipsychotic (risperidone) resulted in significantly decreased irritability [34].

A case study reported decreased hyperactivity and an increased ability to complete performance tasks in a child with autism [35].

6) Sleep

Many anti-anxiety medications also have a sedative effect, helping patients to sleep more soundly. There is limited data on the use of buspirone for improved sleep, and in fact, studies in animals have found no indication that buspirone improves sleep [36, 37, 38].

Studies have found that buspirone decreases REM sleep, which is often increased in depression [39, 40, 41].

An explorative study on 8 patients with anxiety found no clinical improvement for sleep structure, but patients did self-report improved sleep [36].

Side Effects

A meta-analysis 289 patients found that the most common side effects are dizziness, headache, and nausea [42].

Patients generally do not experience drowsiness, weakness, fatigue or depression as is common with other anti-anxiety medications [11, 12, 13].

There are some anecdotal reports of Buspirone causing weight gain, but there are no clinical reports that back this claim. However, a pilot study on 6 schizophrenic patients actually observed weight reduction for patients switching to buspirone from olanzapine or risperidone (which are known to cause weight gain) [43].

The following are other potential side effects reported on various sites, but they are not found in the scientific literature:

  • nervousness/restlessness
  • blurred vision
  • dry mouth
  • upset stomach
  • stuffy nose
  • sore throat
  • ringing in the ears

Drug Interactions

A study in 10 healthy volunteers found that taking buspirone in combination with grapefruit juice significantly increases the blood concentration of the drug, and should be avoided when taking this prescription medication [44].

There is a reported case study of serotonin syndrome in an individual taking buspirone and linezolid concomitantly. Consult your doctor before combining buspirone with other anti-anxiety or anti-depression medications [45].

A study performed in 24 healthy men found that alcohol (0.8 g/kg) and buspirone had little additive effect on intoxication and in some cases, buspirone seemed to reverse the effects of alcohol [46].

Another study in 12 young males found no interaction between buspirone and alcohol. However, alcohol affects everyone differently, so it’s extremely important to take caution whenever combining alcohol and prescription medications [47].

Contraindications

  • Buspirone hypersensitivity.
  • MAOIs within 14 days due to increased risk of serotonin syndrome and/or elevated blood pressure.

Pregnancy and Breast Feeding Considerations

Buspirone was a category B risk in pregnancy. In general, there are no definitive studies that have shown buspirone to be a risk to the fetus. However, caution is always advised if you are going to take the medication while pregnant, and the benefits of taking the medication should be weighed versus any potential risk to the fetus. Please speak to your doctor or a qualified healthcare professional. It is not known if buspirone is transferred to breast milk, but it is advised to not take it if you are breastfeeding [48].

Forms and Dosage

Buspirone is available in 5 mg, 7.5 mg, 10 mg, 15 mg, and 30 mg tablets, and is commonly taken at 15 mg/day for treatment of anxiety (divided into 2 or 3 doses), but the dosage is dependent on indication and clinical trials have found it is well tolerated up to 90 mg/day [5, 16, 17, 48].

Overdose/Toxicity

Buspirone is generally thought to have a more ideal side-effect profile than benzodiazepines. There is only a single report of buspirone overdose causing a seizure in a human, although there are additional animal model reports of this happening [49].

Buspirone vs. Xanax

Buspirone improves anxiety by acting on serotonin receptors in the brain, while Xanax alters the effect of GABA, another neurotransmitter. Buspirone does not have sedative, muscle relaxant or anti-convulsive effects that benzodiazepines such as Xanax have. Additionally, Buspirone has a much smaller potential for abuse and minimal withdrawal symptoms [50].

Genetics

CYP enzymes are responsible for breaking down or metabolizing drugs that enter the body. Buspirone is metabolized by CYP3A4, so mutations in this enzyme could change how buspirone is processed and how it affects you. Specifically, the T variant of the rs35599367 SNP is associated with decreased enzymatic activity in the liver, which could lead to higher drug levels in the bloodstream [51].

Natural Options

Before getting off of any medication, speak to your doctor.

1) Exercise

Exercise has been shown in numerous studies to be effective for reducing anxiety. Aerobic exercise, such as running, biking or hiking, is most effective. Similar to buspirone, exercise reduces anxiety by increasing beneficial neurotransmitters such as serotonin, dopamine, norepinephrine, and endorphins [52, 53, 54, 55, 56, 57].

2) Probiotics

A large proportion of people with anxiety have also been found to have GI disorders and evidence for a link between the gut microbiota and brain function is quickly growing. More specifically, the gut microbiota is being shown to play an important role in Serotonin production [58, 59, 60, 61].

Like buspirone, increasing the health of your gut-flora by supplementing with probiotics can improve serotonin transmission and help reduce anxiety. The following strains have been specifically shown to improve psychological health:

3) 5-Hydroxytryptophan (5-HTP)

5-Hydroxytryptophan (5-HTP) is an over the counter supplement that is a precursor to serotonin. Similarly to the way that buspirone treats anxiety by boosting serotonin activity, supplementing with 5-HTP has been shown to reduce anxiety and panic attacks in humans [66, 67].

4) Cannabidiol (CBD)

CBD is a component of hemp that is non-psychoactive and has many proven health benefits. CBD has been shown to reduce anxiety in both healthy patients and those that have been clinically diagnosed with social anxiety disorder. CBD interacts with the same serotonin receptors (5-HT1A) as buspirone [68, 69, 70, 71].

5) Ashwagandha

Ashwagandha is an Indian herb that helps to restore hormonal imbalance and improve immune function. It has been shown in humans to help stabilize mood fluctuations and has proven anti-anxiety effects in animal models [72, 73, 74, 75].

Based on a study in mice, the anti-anxiety effects of ashwagandha could be due to a resulting increase in both GABA and serotonin [76].

6) Lemon Balm

Lemon balm is an herb commonly consumed as a tea that has been shown in several small human trials to reduce anxiety. A study performed in rats suggests that lemon balm may increase the activity of serotonin, similar to the effect of buspirone [77, 78, 79, 80, 81].

7 ) Lavender

Lavender is a flowering plant with a pleasant smell that is often associated with calmness and sleep. Silexan is an oil derived from lavender that can be taken by mouth. Clinical trials in humans have shown that Silexan can reduce anxiety in patients with post traumatic stress and anxiety disorders [82, 83, 84].

Animal studies have shown that similarly to buspirone, the serotonin system plays an important role in the anti-anxiety effects of lavender oil [85, 86].

Want More Targeted Ways to Improve Your Mood?

If you’re interested in natural and more targeted ways of improving your mood, we at SelfHacked recommend checking out this mood wellness report. It gives genetic-based diet, lifestyle and supplement tips that can help improve your mood. The recommendations are personalized based on your genes.

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About the Author

Chelsea Paresi, PhD (biomedical science)

PhD (biomedical science)

Chelsea has PhD from Cornell University and a BS in Chemistry from Westminster College.

Chelsea spent more than 8 years in the laboratory researching a wide range of topics including small molecule discovery for the treatment of Alzheimer's disease and cancer. She also has experience as a clinical scientist working in an embryology lab. She is passionate about using food as medicine and feels that the future of treating disease will rely on a better understanding of personalized medicine based on genetics.

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