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BuSpar Anti-Anxiety Medication

Updated on July 27, 2016
Buspirone 30mg, manufacturer Teva.
Buspirone 30mg, manufacturer Teva. | Source

Generalized Anxiety Disorder

Generalized anxiety disorder (GAD) is more prevalent than most people realize. It affects about 9.5 million people over the age of 18 every year and is characterized by chronic and excessive worry. Symptoms of GAD include:

  • Fatigue
  • Irritability
  • Constant worry or obsession over either trivial or large problems
  • Restlessness
  • A sense of feeling “on edge”
  • Muscle tension or muscle aches
  • Trembling, feeling twitchy or being easily startled
  • Difficulty sleeping or falling asleep
  • Sweating, nausea, or diarrhea
  • Shortness of breath or rapid heartbeat


BuSpar is the brand name of the generic drug buspirone developed by Bristol-Meyers Squibb in 1986 for the treatment of generalized anxiety disorder or GAD. It is a non-benzodiazepine anxiolytic that acts as a 5-HT-1a receptor selective partial agonist.

5-HT-1a Receptors

The 5-HT-1a receptors are found in high densities in various areas of the brain including:

  • Cerebral cortex
  • Hippocampus
  • Septum
  • Amygdala
  • Raphne nucleus

These receptors are also found in much lower quantities in the basal ganglia and the thymus. The 5-HT-1a receptors have several functions including:

  • Decreasing blood pressure
  • Lowering heart rate
  • Inducing peripheral vasodilation (dilating the blood vessels found in the extremities)
  • Stimulating the vagus nerve

5-HT-1a receptors generally bind with and are activated by the neurotransmitter serotonin. Buspirone binds to these receptors in place of serotonin and activates them, which produces the drug’s antidepressant and anxiolytic effects.

The benzodiazepine class of anxiolytics includes Valium and Xanax, medications that are well-known for producing sedation. Because it is a non-benzodiazepine, one of buspirone’s advantages is that it does not produce sedative effects, yet it has the same efficacy as the benzodiazepines. Valium and Xanax have addictive qualities as well and are listed as controlled substances. Buspirone is not.

Source

Dosages

Buspirone comes in several different dosages, and the pills are scored so that they can easily be divided (called a dividose). Buspirone is typically taken twice a day and is available in:

  • 5mg
  • 7.5mg
  • 10mg
  • 15mg
  • 30mg

The maximum dosage of buspirone is 60 mg per day. However, it is most commonly taken at 15 mg twice a day.

Buspirone is metabolized by the liver and excreted in both the urine and the feces. It has a half-life of approximately two to three hours. This means after the medication reaches its peak efficacy, the concentration of the drug in the bloodstream will reach half of its original strength in two to three hours.

Buspirone 30mg tablets. Right side: manufactured by Mylan; Left side: manufactured by Teva
Buspirone 30mg tablets. Right side: manufactured by Mylan; Left side: manufactured by Teva | Source
Buspirone 30mg (manufacturer: Teva)
Buspirone 30mg (manufacturer: Teva) | Source

Contraindications of Buspirone

If you have hypersensitivity or allergy to buspirone or any other drugs in its class, you should avoid taking the medication.

Anyone with hepatic (liver) or renal (kidney) impairment or failure should not take buspirone. MAO inhibitors should not be taken within 14 days of buspirone. Other medications that should be avoided include:

  • Amiodarone
  • Ciprofloxacin
  • Crizotinib
  • Diltiazem
  • Erythromycin
  • HIV protease inhibitors
  • Nefazodone
  • Rifampin
  • Rifampin/isoniazid
  • Rifampin/isoniazid/pyrazinamide
  • Sibutramine
  • Verapamils

There are a number of medications that can interact with buspirone, but that can be safely taken with it; however, there are too many to list. If you are taking any medications, it is imperative that you discuss these with your doctor prior to starting ANY new medication.

Grapefruit should be avoided when taking buspirone. Grapefruit contains furanocoumarins derivatives. These interfere with hepatic and intestinal enzymes (specifically cytochrome P450 isoform CYP3A4). Bioactive compounds in grapefruit juice can also interfere with P-glycoprotein and organic anion transporting polypeptides (OATPs).

Essentially, this means that grapefruit changes the way the pill is digested in the intestines which can cause more of the medication to be bioavailable at one time. In other words, it could lead to an overdose. If you take buspirone on a regular basis, you should avoid consuming grapefruit and drinking grapefruit juice.

Buspirone 30mg, (manufacturer: Teva)
Buspirone 30mg, (manufacturer: Teva) | Source

Side Effects of BuSpar

As with any medication, there are side effects. Buspirone has a number of different adverse reactions, but substantially less than many antidepressants. Some of the more serious reactions include:

  • Serotonin syndrome (an overdose of the neurotransmitter serotonin, also known as serotonin storm)
  • Akathisia (an inability to remain motionless because of the inner sensation of restlessness. The best example of this is restless leg syndrome or RLS.)
  • Extrapyramidal symptoms (any of the various movement disorders such as akathisia)
  • Tardive dyskinesia (involuntary, repetitive body movements with a slow or belated onset)
  • Dystonia (a neurological movement disorder in which sustained muscle contractions cause twisting and repetitive movements or abnormal postures)
  • Hostility
  • Depression

Treatment for GAD

Treatment for GAD can involve cognitive behavioral therapy, which is the most common psychotherapy for the disorder or other types of psychotherapy including:

  • Acceptance and commitment therapy
  • Intolerance of uncertainty therapy
  • Motivational interviewing.

Medications used to treat GAD include:

  • Antidepressants (Zoloft, Paxil, Prozac)
  • Buspirone
  • Tofranil
  • Effexor
  • Lyrica
  • Any of the benzodiazepine class (Valium, Xanax, Ativan, Klonopin)

The more common side effects include:

  • Dizziness
  • Drowsiness
  • Nausea
  • Headache
  • Nervousness
  • Fatigue
  • Insomnia
  • Xerostomia (dry mouth, aka “cottonmouth”)
  • Impaired concentration
  • Hostility
  • Confusion
  • Depression
  • Blurred vision
  • Diarrhea
  • Abdominal pain
  • Numbness
  • Weakness

It bears repeating that if you are currently taking any medications you should tell you physician what you are taking prior to starting buspirone (or any other medication). If you are already taking buspirone and you notice any of the above side effects, contact your physician immediately.

© Copyright 2012 - 2016 by Melissa "Daughter of Maat" Flagg ALL RIGHTS RESERVED

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    • SoundNFury profile image

      Michael Valencia 4 years ago from Los Angeles, CA

      Very useful information about this drug. I was prescribed this medication years ago for GAD but the side effect of tremors was too much for me. I now take Lorazepam 10 mg and it works for me, but I know my doc wants to eventually get me off that, so I don't know if possibly a lower dosage of BuSpar may work for me. Besides, it was about 15 years ago that I had tried taking it. Voted up and useful.

    • Daughter Of Maat profile image
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      Melissa Flagg 4 years ago from Rural Central Florida

      Thank you! I've been taking Buspar for about 15 years now, and when I went from 30mg a day to 60mg, I noticed the tremors too, and I ended up with RLS. I stuck it out though and both of those symptoms subsided after taking the med for a bit. It just worked so well for me, it was worth it. BUt I know not everyone had the same reaction. It may be worth another shot, but you still may get the same side effects. Thanks for reading and voting! :)

    • Arghness profile image

      Edward 4 years ago from O'Fallon

      My brother takes Buspar and says it works for him. I, myself am on antidepressants, lithium, and benzodiazipines to control my bipolar and anxiety. From what I've read, and observed, Buspar is effective at treating mild to moderate anxiety, and is great in conjunction with an antidepressant as it can have a potentiating effect.

    • Daughter Of Maat profile image
      Author

      Melissa Flagg 4 years ago from Rural Central Florida

      I take buspar as well as an antidepressant. Most people I have talked with say the same thing, that it works better for mild to moderate than the more severe types that require the benzodiazepines.

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