pharmacopeia
GET
/api/v1/drug/buspirone
2D structure
8-[4-(4-pyrimidin-2-ylpiperazin-1-yl)butyl]-8-azaspiro[4.5]decane-7,9-dione
SMILES C1CCC2(C1)CC(=O)N(C(=O)C2)CCCCN3CCN(CC3)C4=NC=CC=N4
InChIKey QWCRAEMEVRGPNT-UHFFFAOYSA-N

Mechanism of action

Sourced from openFDA

Mechanism-of-action classes: Serotonin Agonists; Unknown Cellular or Molecular Interaction.

Serotonin

Indications

Sourced from openFDA
  • Buspirone hydrochloride tablets are indicated for the management of anxiety disorders or the short-term relief of the symptoms of anxiety. Anxiety or tension associated with the stress of everyday life usually does not require treatment with an anxiolytic.

Contraindications

Sourced from openFDA
  • Buspirone hydrochloride tablets are contraindicated in patients hypersensitive to buspirone hydrochloride. The use of monoamine oxidase inhibitors (MAOIs) intended to treat depression with buspirone or within 14 days of stopping treatment with buspirone is contraindicated because of an increased risk of serotonin syndrome and/or elevated blood pressure.contraindicated

Dosage & administration

Sourced from openFDA

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. In clinical trials allowing dose titration, divided doses of 20 to 30 mg per day were commonly employed. The bioavailability of buspirone is increased when given with food as compared to the fasted state (see CLINICAL PHARMACOLOGY ). Consequently, patients should take buspirone in a consistent manner with regard to the timing of dosing; either always with or always without food. When buspirone is to be given with a potent inhibitor of CYP3A4, the dosage recommendations described in the PRECAUTIONS, Drug Interactions section should be followed. Switching a Patient To or From a Monoamine Oxidase Inhibitor (MAOI) Antidepressant At least 14 days should elapse between discontinuation of an MAOI intended to treat depression and initiation of therapy with buspirone hydrochloride tablets. Conversely, at least 14 days should be allowed after stopping buspirone hydrochloride tablets before starting an MAOI antidepressant (see CONTRAINDICATIONS and DRUG INTERACTIONS ). Use of Buspirone with (Reversible) MAOIs, Such as Linezolid or Methylene Blue Do not start buspirone hydrochloride tablets in a patient who is being treated with a reversible MAOI such as linezolid or intravenous methylene blue because there is an increased risk of serotonin syndrome.

Warnings & precautions

Sourced from openFDA

The administration of buspirone hydrochloride tablets to a patient taking a monoamine oxidase inhibitor (MAOI) may pose a hazard. There have been reports of the occurrence of elevated blood pressure when buspirone hydrochloride has been added to a regimen including an MAOI. Therefore, it is recommended that buspirone hydrochloride tablets not be used concomitantly with an MAOI. Serotonin Syndrome The development of a potentially life-threatening serotonin syndrome has been reported with SNRIs SSRIs, and other serotonergic drugs, including buspirone, alone but particularly with concomitant use of other serotonergic drugs (including triptans), with drugs that impair metabolism of serotonin (in particular, MAOIs, including reversible MAOIs such as linezolid and intravenous methylene blue), or with antipsychotics or other dopamine antagonists. Serotonin syndrome symptoms may include mental status changes (e.g., agitation, hallucinations, delirium, and coma), autonomic instability (e.g., tachycardia, labile blood pressure, dizziness, diaphoresis, flushing, hyperthermia), neuromuscular changes (e.g., tremor, rigidity, myoclonus, hyperreflexia, incoordination), seizures, and/or gastrointestinal symptoms (e.g., nausea, vomiting, diarrhea). Patients should be monitored for emergence of serotonin syndrome. The concomitant use of buspirone with MAOIs intended to treat depression is contraindicated. Buspirone should also not be started in a patient who is being treated with reversible MAOIs such as linezolid or intravenous methylene blue.

Adverse reactions

Sourced from openFDA

(See also PRECAUTIONS .) Commonly Observed The more commonly observed untoward events associated with the use of buspirone hydrochloride tablets not seen at an equivalent incidence among placebo-treated patients include dizziness, nausea, headache, nervousness, lightheadedness, and excitement. Associated with Discontinuation of Treatment One guide to the relative clinical importance of adverse events associated with buspirone hydrochloride tablets is provided by the frequency with which they caused drug discontinuation during clinical testing. Approximately 10% of the 2200 anxious patients who participated in the buspirone hydrochloride tablets premarketing clinical efficacy trials in anxiety disorders lasting 3 to 4 weeks discontinued treatment due to an adverse event. The more common events causing discontinuation included: central nervous system disturbances (3.4%), primarily dizziness, insomnia, nervousness, drowsiness, and lightheaded feeling; gastrointestinal disturbances (1.2%), primarily nausea; and miscellaneous disturbances (1.1%), primarily headache and fatigue. In addition, 3.4% of patients had multiple complaints, none of which could be characterized as primary. Incidence in Controlled Clinical Trials The table that follows enumerates adverse events that occurred at a frequency of 1% or more among buspirone hydrochloride patients who participated in 4-week, controlled trials comparing buspirone hydrochloride with placebo. The frequencies were obtained from pooled data for 17 trials.

Use in specific populations

Sourced from openFDA

Pregnancy: Teratogenic Effects Pregnancy Category B No fertility impairment or fetal damage was observed in reproduction studies performed in rats and rabbits at buspirone doses of approximately 30 times the maximum recommended human dose. In humans, however, adequate and well-controlled studies during pregnancy have not been performed. Because animal reproduction studies are not always predictive of human response, this drug should be used during pregnancy only if clearly needed.

Overdosage

Sourced from openFDA

Signs and Symptoms In clinical pharmacology trials, doses as high as 375 mg/day were administered to healthy male volunteers. As this dose was approached, the following symptoms were observed: nausea, vomiting, dizziness, drowsiness, miosis, and gastric distress. A few cases of overdosage have been reported, with complete recovery as the usual outcome. No deaths have been reported following overdosage with buspirone hydrochloride tablets alone. Rare cases of intentional overdosage with a fatal outcome were invariably associated with ingestion of multiple drugs and/or alcohol, and a causal relationship to buspirone could not be determined. Toxicology studies of buspirone yielded the following LD 50 values: mice, 655 mg/kg; rats, 196 mg/kg; dogs, 586 mg/kg; and monkeys, 356 mg/kg. These dosages are 160 to 550 times the recommended human daily dose. Recommended Overdose Treatment General symptomatic and supportive measures should be used along with immediate gastric lavage. Respiration, pulse, and blood pressure should be monitored as in all cases of drug overdosage. No specific antidote is known to buspirone, and dialyzability of buspirone has not been determined.

Approval history

Sourced from openFDA
  • Jun 28, 2001ANDAANDA076008Mylan
  • Feb 28, 2002ANDAANDA075022Teva
  • Mar 19, 2002ANDAANDA075413Rising
  • Apr 5, 2002ANDAANDA075521Rubicon Research
  • May 9, 2002ANDAANDA075388Oxford Pharms
  • Dec 17, 2007ANDAANDA078302Oxford Pharms
  • Feb 27, 2009ANDAANDA078246Aurobindo Pharma Ltd
  • Feb 7, 2014ANDAANDA078888Zydus Pharms

FAERS reports

View JSON
Reference statistics only. FAERS reports are voluntarily submitted and are not incidence rates, safety signals, or causal evidence. Counts reflect reporting volume — how often a reaction was reported, not how often it occurs. For decision-grade use, consult openFDA and the FAERS Public Dashboard directly.
10,587 total reports matchedLatest report Share = reports listing the reaction ÷ total matched reports. Rows can sum to >100% because a single report often lists multiple reactions.
  1. 1Fatigue7807.4%
  2. 2Nausea7687.3%
  3. 3Headache6946.6%
  4. 4Anxiety6576.2%
  5. 5Drug Ineffective6466.1%
  6. 6Pain5565.3%
  7. 7Dyspnoea5455.1%
  8. 8Depression4934.7%
  9. 9Dizziness4854.6%
  10. 10Diarrhoea4834.6%
  11. 11Product Dose Omission Issue4614.4%
  12. 12Fall4023.8%
  13. 13Off Label Use3513.3%
  14. 14Vomiting3443.2%
  15. 15Malaise3313.1%

Literature

View JSON

Recent PubMed references pinned to Buspirone as a MeSH major topic. Citations link to pubmed.ncbi.nlm.nih.gov.

Clinical trials

View JSON

The 10 most recently updated of 72 ClinicalTrials.gov registrations naming Buspirone as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

Frequently asked questions

How does Buspirone work?
Mechanism-of-action classes: Serotonin Agonists; Unknown Cellular or Molecular Interaction.
What is Buspirone used for?
According to FDA labeling, Buspirone carries indications including: Buspirone hydrochloride tablets are indicated for the management of anxiety disorders or the short-term relief of the symptoms of anxiety. Anxiety or tension associated with the stress of everyday life usually does not require treatment with an anxiolytic.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.
What class of drug is Buspirone?
Buspirone is classified as Azaspirodecanedione derivatives, Serotonin Agonists, Unknown Cellular or Molecular Interaction, Increased Serotonin Activity.
What are the brand names for Buspirone?
Buspirone is marketed under brand names including Bucapsol, Buspar.
What are the contraindications for Buspirone?
Buspirone labeling lists contraindications including: Buspirone hydrochloride tablets are contraindicated in patients hypersensitive to buspirone hydrochloride. The use of monoamine oxidase inhibitors (MAOIs) intended to treat depression with buspirone or within 14 days of stopping treatment with buspirone is contraindicated because of an increased risk of serotonin syndrome and/or elevated blood pressure.. Always consult the full prescribing information and a clinician.
Note. Data for buspirone is illustrative MVP content compiled from public sources. pharmacopeia is for educational and informational use only and is not a substitute for professional medical advice.

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