Buspirone

(byoo-SPY-rone)A drug that is used to treat certain anxiety disorders. It belongs to the family of drugs called antianxiety agents

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Buspirone 200

What is Buspirone?

Buspirone, sold under the brand name Buspar, among others, is a medication primarily used to treat anxiety disorders, particularly generalized anxiety disorder.

What are the uses of this medicine?

Anxiety

Buspirone is used for the short-term and long-term treatment of anxiety disorders or symptoms of anxiety. It is generally less preferred than selective serotonin reuptake inhibitors (SSRIs).

Buspirone has no immediate anxiolytic effects, and hence has a delayed onset of action; its full clinical effectiveness may require 2–4 weeks to manifest itself. The drug has been shown to be similarly effective in the treatment of generalized anxiety disorder (GAD) to benzodiazepines including diazepam, alprazolam, lorazepam, and clorazepate. Buspirone is not known to be effective in the treatment of other anxiety disorders besides GAD, although there is some limited evidence that it may be useful in the treatment of social phobia as an adjunct to selective serotonin reuptake inhibitors (SSRIs).

Other uses:

• Sexual dysfunction: There is some evidence that buspirone on its own may be useful in the treatment of hypoactive sexual desire disorder (HSDD) in women.

• Miscellaneous: Buspirone is not effective as a treatment for benzodiazepine withdrawal, barbiturate withdrawal, or alcohol withdrawal/delirium tremens. SSRI and SNRI antidepressants such as paroxetine and venlafaxine may cause jaw pain/jaw spasm reversible syndrome (although it is not common), and buspirone appears to be successful in treating bruxism on SSRI/SNRI-induced jaw clenching

How does this medicine work?

Buspirone acts as an agonist of the serotonin 5-HT1A receptor with high affinity. It is a partial agonist of both presynaptic 5-HT1A receptors, which are inhibitory autoreceptors, and postsynaptic 5-HT1A receptors. It is thought that the main effects of buspirone are mediated via its interaction with the presynaptic 5-HT1A receptor, thus reducing the firing of serotonin-producing neurons. Buspirone also has lower affinities for the serotonin 5-HT2A, 5-HT2B, 5-HT2C, 5-HT6, and 5-HT7 receptors.

Less Technically, BuSpar has effects on neurotransmitters in the brain such as serotonin and dopamine. Specifically, it is a serotonin receptor agonist, which means that it increases action at serotonin receptors in your brain, which in turn helps to alleviate anxiety.

Who Should Not Use this medicine?

Buspirone has these contraindications:

• Hypersensitivity to buspirone
• Metabolic acidosis, as in diabetes
• Should not be used with MAO inhibitors
• Severely compromised liver and/or kidney function

Is this medicine FDA approved?

Buspar is currently listed as discontinued by the US Federal Drug Administration. In 2010, in response to a citizen petition, the US FDA determined that Buspar was not withdrawn for sale because of reasons of safety or effectiveness.

How should this medicine be used?

The recommended initial dose is 15 mg daily (7.5 mg b.i.d.). To achieve an optimal therapeutic response, at intervals of 2 to 3 days the dosage may be increased 5 mg per day, as needed. The maximum daily dosage should not exceed 60 mg per day.

What are the dosage forms and brand names of this medicine?

Buspirone was primarily sold under the brand name Buspar.

Buspirone hydrochloride tablets, USP 5 mg, 7.5 mg, 10 mg, 15mg or 30 mg are available as:

What side effects can this medication cause?

Bupropion Side effects

Very common (>10% incidence)	Dizziness/lightheadedness Headache Somnolence (sleepiness)
Common (1–10% incidence)	Insomnia Sleep disorder Disturbance in attention Depression Confusional state Anger Tachycardia (fast heart rate) Chest pain Sinusitis (nasal congestion) Pharyngolaryngeal pain Paraesthesia (tingling skin) Blurred vision Abnormal coordination Tremor Cold sweat Rash Nausea Abdominal pain Dry mouth Diarrhea Constipation Vomiting Fatigue Musculoskeletal pain
Uncommon (0.1–1%)	Syncope Hypotension Hypertension Redness and itching of the eyes Altered taste Conjunctivitis Flatulence Anorexia Increased appetite Salivation Rectal bleeding Urinary frequency Urinary hesitancy Menstrual irregularity or spotting Dysuria Muscle cramps Muscle spasms Muscle rigidity/stiffness Involuntary movements Shortness of breath Chest congestion Changes in libido Oedema Pruritus Flushing Easy bruising Dry skin Facial oedema Mild increases in hepatic aminotransferases (AST, ALT) Weight gain Fever Roaring sensation in the head Weight loss Malaise Depersonalisation Noise intolerance Euphoria Akathisia Fearfulness Loss of interest Dissociative reaction
Rare (<0.1% incidence)	Cerebrovascular accident (stroke) Myocardial infarction (heart attack) Cardiomyopathy Congestive heart failure Bradycardia Dysphoria Hallucinations Feelings of claustrophobia Cold intolerance Stupor Seizures Slurred speech Extrapyramidal symptoms including dyskinesias (acute & delayed) Dystonic reactions Cogwheel rigidity Emotional lability Psychosis Suicidal ideation Ataxias

What special precautions should I follow?

Special Populations

• Age and Gender Effects: After single or multiple doses in adults, no significant differences in buspirone pharmacokinetics (AUC and C max) were observed between elderly and younger subjects or between men and women.

• Hepatic Impairment: After multiple-dose administration of buspirone to patients with hepatic impairment, steady-state AUC of buspirone increased 13-fold compared with healthy subjects (see PRECAUTIONS).

• Renal Impairment: After multiple-dose administration of buspirone to renally impaired (Cl Cr = 10– 70 mL/min/1.73 m 2) patients, steady-state AUC of buspirone increased 4-fold compared with healthy (Cl Cr ≥80 mL/min/1.73 m 2) subjects (see PRECAUTIONS).

• Race Effects: The effects of race on the pharmacokinetics of buspirone have not been studied.

What to do in case of emergency/overdose?

In case of overdose, call the poison control helpline of your country. In the United States, call 1-800-222-1222.

• Overdose related information is also available online at poisonhelp.org/help.
• In the event that the victim has collapsed, had a seizure, has trouble breathing, or can't be awakened, immediately call emergency services. In the United States, call 911.

Can this medicine be used in pregnancy?

Limited information indicates that maternal doses of buspirone up to 45 mg daily produce low levels in milk. Because no information is available on the long-term use of buspirone during breastfeeding, an alternate drug may be preferred, especially while nursing a newborn or preterm infant.

Can this medicine be used in children?

So far, Buspirone is well tolerated in pediatric patients with GAD, although two randomized controlled trials were underpowered to detect small effect sizes (Cohen's d < 0.15). Finally, Bayesian approaches may facilitate re-examination of data from abandoned clinical trials.

What should I know about storage and disposal of this medication?

Store at 20°C to 25°C (68°F to 77°F) [See USP Controlled Room Temperature]. Dispense in a tight, light-resistant container, as defined in the USP.

Buspirone Resources
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The following are antidepressant subclasses and drugs

MAO Inhibitors Isocarboxazid, Phenelzine, Tranylcypromine

SNRIs Duloxetine, Levomilnacipran, Venlafaxine

SSRIs Citalopram, Escitalopram, Fluoxetine, Fluvoxamine, Paroxetine, Sertraline, Vilazodone, Vortioxetine

Tricyclics Amitriptyline, Amoxapine, Clomipramine, Desipramine, Doxepin, Imipramine, Nortriptyline, Protriptyline, Trimipramine

Miscellaneous Bupropion, Flibanserin, Mirtazapine, Nefazodone, Trazodone