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Buspirone is a prescription medication indicated primarily for anxiety, but can also be used for other disorders such as depression or 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.
Note: By 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 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 [R, R].
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 [R, R].
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 [R, R].
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 adrenaline activates (α2-adrenergic), which could account for some of the anti-depressant effects of buspirone [R, R, R, R].
When taken by mouth (20mg) 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 [R, R].
What Is Buspirone Used For?
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 [R, R].
1) Buspirone For 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 [R].
Buspirone is as effective as benzodiazepines, such as diazepam or lorazepam for treating generalized anxiety. This was shown in a study of 367 menstruating female patients, and 2 studies with 84 adults [R, R, R].
Buspirone is also equal to or better than sertraline (SSRI) for generalized anxiety disorder based on a study of 46 people [R].
2) Buspirone For Depression
Buspirone is more effective for treating major depressive disorder than placebo, based on a meta-analysis looking at the results of 15 RCTs with a total of 2469 patients [R].
Taking buspirone for 8 weeks improved major depression in 61% of elderly patients (n=177) [R].
A randomized study of 286 adults being treated for depression with citalopram, found that augmentation with 60mg/day buspirone resulted in a 30% remission rate based on the Hamilton Rating Scale for Depression [R].
3) Buspirone For 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 (n=101). Participants that were considered to be low anxiety did not experience any benefit from taking buspirone [R].
Buspirone did not help methamphetamine use in 8 participants [R].
4) Buspirone 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 [R, R].
Nine cocaine users were treated with 30mg/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 [R].
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) [R].
5) Buspirone For Symptoms of Autism
In children with Autism, small doses of buspirone (2.5mg) can help alleviate repetitive behaviors (n=166, ages 2-6) [R].
In 40 kids with autism, low doses of buspirone in combination with an antipsychotic (risperidone) resulted in significantly decreased irritability [R].
A case study reported decreased hyperactivity and an increased ability to complete performance tasks in a child with autism [R].
6) Buspirone For 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 [R, R, R].
An explorative study on 8 patients with anxiety found no clinical improvement for sleep structure, but patients did self-report improved sleep [R].
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 [R].
Buspirone Side Effects
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) [R].
The following are other potential side effects reported on various sites, but they are not found in scientific literature:
- blurred vision
- dry mouth
- upset stomach
- stuffy nose
- sore throat
- ringing in the ears
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 [R].
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 [R].
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 [R].
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 [R].
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 [R].
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 CYP3A4*22 variant is associated with decreased enzymatic activity which could lead to higher drug levels in the bloodstream [R, R].
Natural Alternatives to Buspirone
Before getting off of any medication, speak to your doctor.
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 [R, R, R, R, R, R].
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 [R, R, R, R].
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:
- Lactobacillus Plantarum [R]
- Lactobacillus Rhamnosus [R]
- Lactobacillus Helveticus [R]
- Lactobacillus Longum [R]
- Lactobacillus Fermentum [R]
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 [R, R].
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. [R, R, R, R].
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 [R, R, R, R].
Based on a study in mice, the anti-anxiety effects of ashwagandha could be due to a resulting increase in both GABA and serotonin [R].
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 [R, R, R, R, R].
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 [R, R, R].
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