Buspirone

Synonyms :
8-(4-(4-(2-Pyrimidinyl)-1-piperizinyl)butyl)-8-azaspiro(4,5)decane-7,9-dione, Buspiron, Buspirona, Buspirone, Buspironum

Status : approved

Category

Anti-Anxiety Agents

Therapeutic Classification

ANXIOLYTICS

NERVOUS SYSTEM
PSYCHOLEPTICS
ANXIOLYTICS
Hypnotics and Sedatives

Description

An anxiolytic agent and a serotonin receptor agonist belonging to the azaspirodecanedione class of compounds. Its structure is unrelated to those of the benzodiazepines, but it has an efficacy comparable to diazepam. [PubChem]

Used

For the management of anxiety disorders or the short-term relief of the symptoms of anxiety, and also as an augmention of SSRI-treatment against depression.

Mechanism Of Action

Buspirone binds to 5-HT type 1A serotonin receptors on presynaptic neurons in the dorsal raphe and on postsynaptic neurons in the hippocampus, thus inhibiting the firing rate of 5-HT-containing neurons in the dorsal raphe. Buspirone also binds at dopamine type 2 (DA2) receptors, blocking presynaptic dopamine receptors. Buspirone increases firing in the locus ceruleus, an area of brain where norepinephrine cell bodies are found in high concentration. The net result of buspirone actions is that serotonergic activity is suppressed while noradrenergic and dopaminergic cell firing is enhanced.

Dosage

Form Route Strength
Tablet oral 10 mg
Tablet oral 15 mg
Tablet oral 30 mg
Tablet oral 5 mg
Tablet oral 7.5 mg

Pharmacodynamics

Buspirone is used in the treatment of generalized anxiety where it has advantages over other antianxiety drugs because it does not cause sedation (drowsiness) and does not cause tolerance or physical dependence. Buspirone differs from typical benzodiazepine anxiolytics in that it does not exert anticonvulsant or muscle relaxant effects. It also lacks the prominent sedative effect that is associated with more typical anxiolytics. in vitro preclinical studies have shown that buspirone has a high affinity for serotonin (5-HT1A) receptors. Buspirone has no significant affinity for benzodiazepine receptors and does not affect GABA binding in vitro or in vivo when tested in preclinical models. Buspirone has moderate affinity for brain D2-dopamine receptors. Some studies do suggest that buspirone may have indirect effects on other neurotransmitter systems.

Toxic Effect

Oral, rat LD50 = 136 mg/kg. Symptoms of overdose include dizziness, drowsiness, nausea or vomiting, severe stomach upset, and unusually small pupils.

Metabolism

Metabolized hepatically, primarily by oxidation by cytochrome P450 3A4 producing several hydroxylated derivatives and a pharmacologically active metabolite, 1-pyrimidinylpiperazine (1-PP)

Absorption

Rapidly absorbed in man. Bioavailability is low and variable (approximately 5%) due to extensive first pass metabolism.

Half Life

2-3 hours (although the action of a single dose is much longer than the short halflife indicates).

Protein Binding

95% (approximately 70% bound to albumin, 30% bound to alpha 1 -acid glycoprotein)

Elimination Route

In a single-dose study using 14C-labeled buspirone, 29% to 63% of the dose was excreted in the urine within 24 hours, primarily as metabolites; fecal excretion accounted for 18% to 38% of the dose.

Chemical Classification

This compound belongs to the class of organic compounds known as n-arylpiperazines. These are organic compounds containing a piperazine ring where the nitrogen ring atom carries an aryl group.

N-arylpiperazines

Organic compounds

Organoheterocyclic compounds

Diazinanes

Piperazines

Salt : Buspirone Hydrochloride

Chemical Name

8-(4-(4-(2-Pyrimidinyl)-1-piperizinyl)butyl)-8-azaspiro(4,5)decane-7,9-dione

Brands

name Dosage form Country
Apo-buspirone – Tab 10mg tablet Canada
Buspar Tab 10mg tablet Canada
Buspirone tablet US
Buspirone Hcl tablet US
Buspirone Hcl tablet US
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Buspirone Hydrochloride tablet US
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Buspirone Hydrochloride tablet US
Buspirone Hydrochloride tablet US
Buspirone-10 – Tab 10mg tablet Canada
Bustab tablet Canada
Bustab tablet Canada
Co Buspirone tablet Canada
Dom-buspirone tablet Canada
Ftp-buspirone tablet Canada
Linbuspirone tablet Canada
Mylan-buspirone tablet Canada
Nu-buspirone – Tab 10mg tablet Canada
Penta-buspirone tablet Canada
PMS-buspirone tablet Canada
PMS-buspirone tablet Canada
Ratio-buspirone tablet Canada
Riva-buspirone 10 mg tablet Canada
Teva-buspirone tablet Canada

Drug Drug Interactions

  •  Acepromazine  : Serotonin Modulators may enhance the adverse/toxic effect of Antipsychotic Agents. Specifically, serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant syndrome. Antipsychotic Agents may enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome.
  •  Acetophenazine  : Serotonin Modulators may enhance the adverse/toxic effect of Antipsychotic Agents. Specifically, serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant syndrome. Antipsychotic Agents may enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome.
  •  Amisulpride  : Serotonin Modulators may enhance the adverse/toxic effect of Antipsychotic Agents. Specifically, serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant syndrome. Antipsychotic Agents may enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome.
  •  Aprepitant  : May increase the serum concentration of CYP3A4 Substrates.
  •  Aripiprazole  : Serotonin Modulators may enhance the adverse/toxic effect of Antipsychotic Agents. Specifically, serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant syndrome. Antipsychotic Agents may enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome.
  •  Benzquinamide  : Serotonin Modulators may enhance the adverse/toxic effect of Antipsychotic Agents. Specifically, serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant syndrome. Antipsychotic Agents may enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome.
  •  Bosentan  : May decrease the serum concentration of CYP3A4 Substrates.
  •  Buprenorphine  : CNS Depressants may enhance the CNS depressant effect of Buprenorphine.
  •  Carphenazine  : Serotonin Modulators may enhance the adverse/toxic effect of Antipsychotic Agents. Specifically, serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant syndrome. Antipsychotic Agents may enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome.
  •  Chlormezanone  : Serotonin Modulators may enhance the adverse/toxic effect of Antipsychotic Agents. Specifically, serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant syndrome. Antipsychotic Agents may enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome.
  •  Chlorpromazine  : Serotonin Modulators may enhance the adverse/toxic effect of Antipsychotic Agents. Specifically, serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant syndrome. Antipsychotic Agents may enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome.
  •  Chlorprothixene  : Serotonin Modulators may enhance the adverse/toxic effect of Antipsychotic Agents. Specifically, serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant syndrome. Antipsychotic Agents may enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome.
  •  Citalopram  : May enhance the serotonergic effect of Selective Serotonin Reuptake Inhibitors. This may cause serotonin syndrome. Selective Serotonin Reuptake Inhibitors may decrease the metabolism of Buspirone.
  •  Clarithromycin  : Macrolide Antibiotics may decrease the metabolism of Buspirone.
  •  Clozapine  : Serotonin Modulators may enhance the adverse/toxic effect of Antipsychotic Agents. Specifically, serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant syndrome. Antipsychotic Agents may enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome.
  •  Conivaptan  : May increase the serum concentration of CYP3A4 Substrates.
  •  Dabrafenib  : May decrease the serum concentration of CYP3A4 Substrates.
  •  Dapoxetine  : May enhance the adverse/toxic effect of Serotonin Modulators.
  •  Dasatinib  : May increase the serum concentration of CYP3A4 Substrates.
  •  Deferasirox  : May decrease the serum concentration of CYP3A4 Substrates.
  •  Diltiazem  : Calcium Channel Blockers (Nondihydropyridine) may decrease the metabolism of Buspirone.
  •  Doxylamine  : May enhance the CNS depressant effect of CNS Depressants.
  •  Dronabinol  : May enhance the CNS depressant effect of CNS Depressants.
  •  Dronabinol  : May enhance the CNS depressant effect of CNS Depressants.
  •  Droperidol  : May enhance the CNS depressant effect of CNS Depressants.
  •  Erythromycin  : Macrolide Antibiotics may decrease the metabolism of Buspirone.
  •  Escitalopram  : May enhance the serotonergic effect of Selective Serotonin Reuptake Inhibitors. This may cause serotonin syndrome. Selective Serotonin Reuptake Inhibitors may decrease the metabolism of Buspirone.
  •  Fencamfamine  : Serotonin Modulators may enhance the adverse/toxic effect of Antipsychotic Agents. Specifically, serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant syndrome. Antipsychotic Agents may enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome.
  •  Fluconazole  : Antifungal Agents (Azole Derivatives, Systemic) may decrease the metabolism of Buspirone. Isavuconazonium considerations are addressed in separate monographs.
  •  Fluoxetine  : May enhance the serotonergic effect of Selective Serotonin Reuptake Inhibitors. This may cause serotonin syndrome. Selective Serotonin Reuptake Inhibitors may decrease the metabolism of Buspirone.
  •  Flupentixol  : Serotonin Modulators may enhance the adverse/toxic effect of Antipsychotic Agents. Specifically, serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant syndrome. Antipsychotic Agents may enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome.
  •  Fluphenazine  : Serotonin Modulators may enhance the adverse/toxic effect of Antipsychotic Agents. Specifically, serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant syndrome. Antipsychotic Agents may enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome.
  •  Fluspirilene  : Serotonin Modulators may enhance the adverse/toxic effect of Antipsychotic Agents. Specifically, serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant syndrome. Antipsychotic Agents may enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome.
  •  Fluvoxamine  : May enhance the serotonergic effect of Selective Serotonin Reuptake Inhibitors. This may cause serotonin syndrome. Selective Serotonin Reuptake Inhibitors may decrease the metabolism of Buspirone.
  •  Fosaprepitant  : May increase the serum concentration of CYP3A4 Substrates.
  •  Haloperidol  : Serotonin Modulators may enhance the adverse/toxic effect of Antipsychotic Agents. Specifically, serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant syndrome. Antipsychotic Agents may enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome.
  •  Hydrocodone  : CNS Depressants may enhance the CNS depressant effect of Hydrocodone.
  •  Hydroxyzine  : May enhance the CNS depressant effect of CNS Depressants.
  •  Idelalisib  : May increase the serum concentration of CYP3A4 Substrates.
  •  Ioflupane I 123  : Buspirone may diminish the diagnostic effect of Ioflupane I 123.
  •  Isocarboxazid  : May enhance the adverse/toxic effect of MAO Inhibitors. Specifically, blood pressure elevations been reported.
  •  Itraconazole  : Antifungal Agents (Azole Derivatives, Systemic) may decrease the metabolism of Buspirone. Isavuconazonium considerations are addressed in separate monographs.
  •  Ivacaftor  : May increase the serum concentration of CYP3A4 Substrates.
  •  Ketoconazole  : Antifungal Agents (Azole Derivatives, Systemic) may decrease the metabolism of Buspirone. Isavuconazonium considerations are addressed in separate monographs.
  •  Linezolid  : May enhance the adverse/toxic effect of MAO Inhibitors. Specifically, blood pressure elevations been reported.
  •  Loxapine  : Serotonin Modulators may enhance the adverse/toxic effect of Antipsychotic Agents. Specifically, serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant syndrome. Antipsychotic Agents may enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome.
  •  Luliconazole  : May increase the serum concentration of CYP3A4 Substrates.
  •  Magnesium Sulfate  : May enhance the CNS depressant effect of CNS Depressants.
  •  Mesoridazine  : Serotonin Modulators may enhance the adverse/toxic effect of Antipsychotic Agents. Specifically, serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant syndrome. Antipsychotic Agents may enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome.
  •  Methotrimeprazine  : CNS Depressants may enhance the CNS depressant effect of Methotrimeprazine. Methotrimeprazine may enhance the CNS depressant effect of CNS Depressants.
  •  Metoclopramide  : Serotonin Modulators may enhance the adverse/toxic effect of Metoclopramide. This may be manifest as symptoms consistent with serotonin syndrome or neuroleptic malignant syndrome.
  •  Metyrosine  : CNS Depressants may enhance the sedative effect of Metyrosine.
  •  Mifepristone  : May increase the serum concentration of CYP3A4 Substrates.
  •  Minocycline  : May enhance the CNS depressant effect of CNS Depressants.
  •  Mitotane  : May decrease the serum concentration of CYP3A4 Substrates.
  •  Moclobemide  : May enhance the adverse/toxic effect of MAO Inhibitors. Specifically, blood pressure elevations been reported.
  •  Molindone  : Serotonin Modulators may enhance the adverse/toxic effect of Antipsychotic Agents. Specifically, serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant syndrome. Antipsychotic Agents may enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome.
  •  Nabilone  : May enhance the CNS depressant effect of CNS Depressants.
  •  Nefazodone  : May enhance the serotonergic effect of Antidepressants (Serotonin Reuptake Inhibitor/Antagonist).
  •  Netupitant  : May increase the serum concentration of CYP3A4 Substrates.
  •  Olanzapine  : Serotonin Modulators may enhance the adverse/toxic effect of Antipsychotic Agents. Specifically, serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant syndrome. Antipsychotic Agents may enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome.
  •  Ondansetron  : Serotonin Modulators may enhance the adverse/toxic effect of Antipsychotic Agents. Specifically, serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant syndrome. Antipsychotic Agents may enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome.
  •  Orphenadrine  : CNS Depressants may enhance the CNS depressant effect of Orphenadrine.
  •  Palbociclib  : May increase the serum concentration of CYP3A4 Substrates.
  •  Paliperidone  : Serotonin Modulators may enhance the adverse/toxic effect of Antipsychotic Agents. Specifically, serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant syndrome. Antipsychotic Agents may enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome.
  •  Paraldehyde  : CNS Depressants may enhance the CNS depressant effect of Paraldehyde.
  •  Paroxetine  : May enhance the serotonergic effect of Selective Serotonin Reuptake Inhibitors. This may cause serotonin syndrome. Selective Serotonin Reuptake Inhibitors may decrease the metabolism of Buspirone.
  •  Perampanel  : May enhance the CNS depressant effect of CNS Depressants.
  •  Perphenazine  : Serotonin Modulators may enhance the adverse/toxic effect of Antipsychotic Agents. Specifically, serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant syndrome. Antipsychotic Agents may enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome.
  •  Phenelzine  : May enhance the adverse/toxic effect of MAO Inhibitors. Specifically, blood pressure elevations been reported.
  •  Pimozide  : Serotonin Modulators may enhance the adverse/toxic effect of Antipsychotic Agents. Specifically, serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant syndrome. Antipsychotic Agents may enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome.
  •  Piperacetazine  : Serotonin Modulators may enhance the adverse/toxic effect of Antipsychotic Agents. Specifically, serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant syndrome. Antipsychotic Agents may enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome.
  •  Posaconazole  : Antifungal Agents (Azole Derivatives, Systemic) may decrease the metabolism of Buspirone. Isavuconazonium considerations are addressed in separate monographs.
  •  Pramipexole  : CNS Depressants may enhance the sedative effect of Pramipexole.
  •  Procarbazine  : May enhance the adverse/toxic effect of MAO Inhibitors. Specifically, blood pressure elevations been reported.
  •  Prochlorperazine  : Serotonin Modulators may enhance the adverse/toxic effect of Antipsychotic Agents. Specifically, serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant syndrome. Antipsychotic Agents may enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome.
  •  Promazine  : Serotonin Modulators may enhance the adverse/toxic effect of Antipsychotic Agents. Specifically, serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant syndrome. Antipsychotic Agents may enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome.
  •  Quetiapine  : Serotonin Modulators may enhance the adverse/toxic effect of Antipsychotic Agents. Specifically, serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant syndrome. Antipsychotic Agents may enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome.
  •  Rasagiline  : May enhance the adverse/toxic effect of MAO Inhibitors. Specifically, blood pressure elevations been reported.
  •  Remoxipride  : Serotonin Modulators may enhance the adverse/toxic effect of Antipsychotic Agents. Specifically, serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant syndrome. Antipsychotic Agents may enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome.
  •  Reserpine  : Serotonin Modulators may enhance the adverse/toxic effect of Antipsychotic Agents. Specifically, serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant syndrome. Antipsychotic Agents may enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome.
  •  Rifabutin  : Rifamycin Derivatives may decrease the serum concentration of Buspirone.
  •  Rifampicin  : Rifamycin Derivatives may decrease the serum concentration of Buspirone.
  •  Rifapentine  : Rifamycin Derivatives may decrease the serum concentration of Buspirone.
  •  Risperidone  : Serotonin Modulators may enhance the adverse/toxic effect of Antipsychotic Agents. Specifically, serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant syndrome. Antipsychotic Agents may enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome.
  •  Ropinirole  : CNS Depressants may enhance the sedative effect of Ropinirole.
  •  Rotigotine  : CNS Depressants may enhance the sedative effect of Rotigotine.
  •  Rufinamide  : May enhance the adverse/toxic effect of CNS Depressants. Specifically, sleepiness and dizziness may be enhanced.
  •  Selegiline  : May enhance the adverse/toxic effect of MAO Inhibitors. Specifically, blood pressure elevations been reported.
  •  Sertindole  : Serotonin Modulators may enhance the adverse/toxic effect of Antipsychotic Agents. Specifically, serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant syndrome. Antipsychotic Agents may enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome.
  •  Sertraline  : May enhance the serotonergic effect of Selective Serotonin Reuptake Inhibitors. This may cause serotonin syndrome. Selective Serotonin Reuptake Inhibitors may decrease the metabolism of Buspirone.
  •  Siltuximab  : May decrease the serum concentration of CYP3A4 Substrates.
  •  Simeprevir  : May increase the serum concentration of CYP3A4 Substrates.
  •  Sodium oxybate  : May enhance the CNS depressant effect of CNS Depressants.
  •  Stiripentol  : May increase the serum concentration of CYP3A4 Substrates.
  •  Sulfisoxazole  : Macrolide Antibiotics may decrease the metabolism of Buspirone.
  •  Sulpiride  : Serotonin Modulators may enhance the adverse/toxic effect of Antipsychotic Agents. Specifically, serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant syndrome. Antipsychotic Agents may enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome.
  •  Suvorexant  : CNS Depressants may enhance the CNS depressant effect of Suvorexant.
  •  Tapentadol  : May enhance the CNS depressant effect of CNS Depressants.
  •  Tedizolid Phosphate  : May enhance the adverse/toxic effect of MAO Inhibitors. Specifically, blood pressure elevations been reported.
  •  Telithromycin  : Macrolide Antibiotics may decrease the metabolism of Buspirone.
  •  Thalidomide  : CNS Depressants may enhance the CNS depressant effect of Thalidomide.
  •  Thioridazine  : Serotonin Modulators may enhance the adverse/toxic effect of Antipsychotic Agents. Specifically, serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant syndrome. Antipsychotic Agents may enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome.
  •  Thiothixene  : Serotonin Modulators may enhance the adverse/toxic effect of Antipsychotic Agents. Specifically, serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant syndrome. Antipsychotic Agents may enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome.
  •  Tocilizumab  : May decrease the serum concentration of CYP3A4 Substrates.
  •  Tranylcypromine  : May enhance the adverse/toxic effect of MAO Inhibitors. Specifically, blood pressure elevations been reported.
  •  Trazodone  : May enhance the serotonergic effect of Antidepressants (Serotonin Reuptake Inhibitor/Antagonist).
  •  Trifluoperazine  : Serotonin Modulators may enhance the adverse/toxic effect of Antipsychotic Agents. Specifically, serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant syndrome. Antipsychotic Agents may enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome.
  •  Triflupromazine  : Serotonin Modulators may enhance the adverse/toxic effect of Antipsychotic Agents. Specifically, serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant syndrome. Antipsychotic Agents may enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome.
  •  Verapamil  : Calcium Channel Blockers (Nondihydropyridine) may decrease the metabolism of Buspirone.
  •  Vilazodone  : May enhance the serotonergic effect of Selective Serotonin Reuptake Inhibitors. This may cause serotonin syndrome. Selective Serotonin Reuptake Inhibitors may decrease the metabolism of Buspirone.
  •  Voriconazole  : Antifungal Agents (Azole Derivatives, Systemic) may decrease the metabolism of Buspirone. Isavuconazonium considerations are addressed in separate monographs.
  •  Vortioxetine  : May enhance the serotonergic effect of Selective Serotonin Reuptake Inhibitors. This may cause serotonin syndrome. Selective Serotonin Reuptake Inhibitors may decrease the metabolism of Buspirone.
  •  Yohimbine  : May diminish the therapeutic effect of Antianxiety Agents.
  •  Ziprasidone  : Serotonin Modulators may enhance the adverse/toxic effect of Antipsychotic Agents. Specifically, serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant syndrome. Antipsychotic Agents may enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome.
  •  Zolpidem  : CNS Depressants may enhance the CNS depressant effect of Zolpidem.
  •  Zuclopenthixol  : Serotonin Modulators may enhance the adverse/toxic effect of Antipsychotic Agents. Specifically, serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant syndrome. Antipsychotic Agents may enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome.

Food Interactions

  • Always take at the same time with respect to meals., Avoid alcohol., Avoid taking grapefruit or grapefruit juice throughout treatment., Take with food.

Calculated Property

kind Value Source
logP 1.95 ALOGPS
logS -2.8 ALOGPS
Water Solubility 5.88e-01 g/l ALOGPS
logP 1.78 ChemAxon
IUPAC Name 8-{4-[4-(pyrimidin-2-yl)piperazin-1-yl]butyl}-8-azaspiro[4.5]decane-7,9-dione ChemAxon
Traditional IUPAC Name buspirone ChemAxon
Molecular Weight 385.5031 ChemAxon
Monoisotopic Weight 385.247775261 ChemAxon
SMILES O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)C1=NC=CC=N1 ChemAxon
Molecular Formula C21H31N5O2 ChemAxon
InChI InChI=1S/C21H31N5O2/c27-18-16-21(6-1-2-7-21)17-19(28)26(18)11-4-3-10-24-12-14-25(15-13-24)20-22-8-5-9-23-20/h5,8-9H,1-4,6-7,10-17H2 ChemAxon
InChIKey InChIKey=QWCRAEMEVRGPNT-UHFFFAOYSA-N ChemAxon
Polar Surface Area (PSA) 69.64 ChemAxon
Refractivity 108.89 ChemAxon
Polarizability 44.12 ChemAxon
Rotatable Bond Count 6 ChemAxon
H Bond Acceptor Count 6 ChemAxon
H Bond Donor Count 0 ChemAxon
pKa (strongest basic) 7.62 ChemAxon
Physiological Charge 1 ChemAxon
Number of Rings 4 ChemAxon
Bioavailability 1 ChemAxon
Rule of Five 1 ChemAxon
Ghose Filter 1 ChemAxon
MDDR-Like Rule 1 ChemAxon

Affected organism

Humans and other mammals

Target within organism

  • 5-hydroxytryptamine receptor 1A : in Human
  • D(2) dopamine receptor : in Human