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Details

Stereochemistry ACHIRAL
Molecular Formula C21H31N5O2
Molecular Weight 385.5031
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of BUSPIRONE

SMILES

O=C1CC2(CCCC2)CC(=O)N1CCCCN3CCN(CC3)C4=NC=CC=N4

InChI

InChIKey=QWCRAEMEVRGPNT-UHFFFAOYSA-N
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

HIDE SMILES / InChI

Molecular Formula C21H31N5O2
Molecular Weight 385.5031
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Description
Curator's Comment: Description was created based on several sources, including https://www.ncbi.nlm.nih.gov/pubmed/1796057 https://www.ncbi.nlm.nih.gov/pubmed/6151170

Buspirone is the first of a new class of anxioselective agents, the azaspirodecanediones. Animal studies have suggested antianxiety activity and the absence of abuse potential. Behavioural, electrophysiological and receptor binding experiments gradually led to the idea that buspirone owes much of its anxiolytic activity to its ability to attenuate central 5-hydroxytryptamine neurotransmission. In vitro preclinical studies have shown that buspirone has a high affinity for serotonin (5-HT1A) receptors. Some studies do suggest that buspirone may have indirect effects on other neurotransmitter systems. 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. The drug was approved by FDA for the treatment of anxiety.

Originator

Sources: ISBN-13: 978-1285845227

Approval Year

Targets

Targets

Primary TargetPharmacologyConditionPotency
24.0 nM [IC50]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
BUSPIRONE HYDROCHLORIDE

Approved Use

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.

Launch Date

9.8573759E11
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
1.613 ng/mL
15 mg 2 times / day steady-state, oral
dose: 15 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
BUSPIRONE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
1.711 ng/mL
15 mg single, oral
dose: 15 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
BUSPIRONE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
6.837 ng × h/mL
15 mg 2 times / day steady-state, oral
dose: 15 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
BUSPIRONE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
9.402 ng × h/mL
15 mg single, oral
dose: 15 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
BUSPIRONE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
3.062 h
15 mg single, oral
dose: 15 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
BUSPIRONE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
Funbound

Funbound

ValueDoseCo-administeredAnalytePopulation
14%
BUSPIRONE plasma
Homo sapiens
population: UNKNOWN
age: UNKNOWN
sex: UNKNOWN
food status: UNKNOWN
Doses

Doses

DosePopulationAdverse events​
30 mg 1 times / day steady, oral (median)
Highest studied dose
Dose: 30 mg, 1 times / day
Route: oral
Route: steady
Dose: 30 mg, 1 times / day
Sources:
unhealthy, 6–17 years
n = 334
Health Status: unhealthy
Condition: generalized anxiety disorder
Age Group: 6–17 years
Sex: M+F
Population Size: 334
Sources:
Other AEs: Headache, Asthenia...
Other AEs:
Headache (29 patients)
Asthenia (10 patients)
Accidental injury (16 patients)
Nausea (13 patients)
Dyspepsia (5 patients)
Diarrhea (6 patients)
Vomiting (34 patients)
Lightheadedness (14 patients)
Somnolence (5 patients)
Insomnia (5 patients)
Nervousness (5 patients)
Upper respiratory tract infection (5 patients)
Sources:
15 mg 2 times / day steady, oral
Dose: 15 mg, 2 times / day
Route: oral
Route: steady
Dose: 15 mg, 2 times / day
Sources:
unhealthy
n = 10
Health Status: unhealthy
Condition: Spinal Cord Injury
Population Size: 10
Sources:
Other AEs: Nausea, Headache...
Other AEs:
Nausea (below serious, 1 patient)
Headache (below serious, 1 patient)
Fatigue (below serious, 1 patient)
Sources:
20 mg 2 times / day steady, oral
Dose: 20 mg, 2 times / day
Route: oral
Route: steady
Dose: 20 mg, 2 times / day
Sources:
unhealthy
n = 19
Health Status: unhealthy
Condition: Marijuana Dependence
Population Size: 19
Sources:
Other AEs: Light headedness...
Other AEs:
Light headedness (below serious, 1 patient)
Sources:
30 mg 2 times / day steady, oral
Dose: 30 mg, 2 times / day
Route: oral
Route: steady
Dose: 30 mg, 2 times / day
Sources:
unhealthy
n = 88
Health Status: unhealthy
Condition: Marijuana Dependence
Population Size: 88
Sources:
Other AEs: Lightheadedness, Drowsiness...
Other AEs:
Lightheadedness (below serious, 36 patients)
Drowsiness (below serious, 17 patients)
Gastrointestinal disorder (below serious, 36 patients)
Headache (below serious, 28 patients)
Insomnia (below serious, 16 patients)
Allergic sinusitis (below serious, 13 patients)
Sources:
30 mg 2 times / day steady, oral
Dose: 30 mg, 2 times / day
Route: oral
Route: steady
Dose: 30 mg, 2 times / day
Sources:
unhealthy
n = 17
Health Status: unhealthy
Condition: Parkinson's disease
Population Size: 17
Sources:
Other AEs: Frozen gait, Tremor...
Other AEs:
Frozen gait (below serious, 5 patients)
Tremor (below serious, 3 patients)
Dizziness (below serious, 2 patients)
Fatigue (below serious, 2 patients)
Bradycardia (below serious, 1 patient)
Constipation (below serious, 1 patient)
Dysphagia (below serious, 1 patient)
Gastritis and duodenitis (below serious, 1 patient)
Gastrointestinal disorder (NOS) (below serious, 1 patient)
Cramp in hand (below serious, 1 patient)
Headache (below serious, 1 patient)
Increased agitation (below serious, 1 patient)
Increased appetite (below serious, 1 patient)
Balance impaired NOS (below serious, 1 patient)
Dystonia (below serious, 1 patient)
Irritability (below serious, 1 patient)
Pain in knee (below serious, 1 patient)
Pain (below serious, 1 patient)
Insomnia (below serious, 1 patient)
Joint stiffness (below serious, 1 patient)
Pain neck/shoulder (below serious, 1 patient)
Leg pain (below serious, 1 patient)
Nasal congestion (below serious, 1 patient)
Numbness (below serious, 1 patient)
Infection respiratory (below serious, 1 patient)
Sources:
AEs

AEs

AESignificanceDosePopulation
Asthenia 10 patients
30 mg 1 times / day steady, oral (median)
Highest studied dose
Dose: 30 mg, 1 times / day
Route: oral
Route: steady
Dose: 30 mg, 1 times / day
Sources:
unhealthy, 6–17 years
n = 334
Health Status: unhealthy
Condition: generalized anxiety disorder
Age Group: 6–17 years
Sex: M+F
Population Size: 334
Sources:
Nausea 13 patients
30 mg 1 times / day steady, oral (median)
Highest studied dose
Dose: 30 mg, 1 times / day
Route: oral
Route: steady
Dose: 30 mg, 1 times / day
Sources:
unhealthy, 6–17 years
n = 334
Health Status: unhealthy
Condition: generalized anxiety disorder
Age Group: 6–17 years
Sex: M+F
Population Size: 334
Sources:
Lightheadedness 14 patients
30 mg 1 times / day steady, oral (median)
Highest studied dose
Dose: 30 mg, 1 times / day
Route: oral
Route: steady
Dose: 30 mg, 1 times / day
Sources:
unhealthy, 6–17 years
n = 334
Health Status: unhealthy
Condition: generalized anxiety disorder
Age Group: 6–17 years
Sex: M+F
Population Size: 334
Sources:
Accidental injury 16 patients
30 mg 1 times / day steady, oral (median)
Highest studied dose
Dose: 30 mg, 1 times / day
Route: oral
Route: steady
Dose: 30 mg, 1 times / day
Sources:
unhealthy, 6–17 years
n = 334
Health Status: unhealthy
Condition: generalized anxiety disorder
Age Group: 6–17 years
Sex: M+F
Population Size: 334
Sources:
Headache 29 patients
30 mg 1 times / day steady, oral (median)
Highest studied dose
Dose: 30 mg, 1 times / day
Route: oral
Route: steady
Dose: 30 mg, 1 times / day
Sources:
unhealthy, 6–17 years
n = 334
Health Status: unhealthy
Condition: generalized anxiety disorder
Age Group: 6–17 years
Sex: M+F
Population Size: 334
Sources:
Vomiting 34 patients
30 mg 1 times / day steady, oral (median)
Highest studied dose
Dose: 30 mg, 1 times / day
Route: oral
Route: steady
Dose: 30 mg, 1 times / day
Sources:
unhealthy, 6–17 years
n = 334
Health Status: unhealthy
Condition: generalized anxiety disorder
Age Group: 6–17 years
Sex: M+F
Population Size: 334
Sources:
Dyspepsia 5 patients
30 mg 1 times / day steady, oral (median)
Highest studied dose
Dose: 30 mg, 1 times / day
Route: oral
Route: steady
Dose: 30 mg, 1 times / day
Sources:
unhealthy, 6–17 years
n = 334
Health Status: unhealthy
Condition: generalized anxiety disorder
Age Group: 6–17 years
Sex: M+F
Population Size: 334
Sources:
Insomnia 5 patients
30 mg 1 times / day steady, oral (median)
Highest studied dose
Dose: 30 mg, 1 times / day
Route: oral
Route: steady
Dose: 30 mg, 1 times / day
Sources:
unhealthy, 6–17 years
n = 334
Health Status: unhealthy
Condition: generalized anxiety disorder
Age Group: 6–17 years
Sex: M+F
Population Size: 334
Sources:
Nervousness 5 patients
30 mg 1 times / day steady, oral (median)
Highest studied dose
Dose: 30 mg, 1 times / day
Route: oral
Route: steady
Dose: 30 mg, 1 times / day
Sources:
unhealthy, 6–17 years
n = 334
Health Status: unhealthy
Condition: generalized anxiety disorder
Age Group: 6–17 years
Sex: M+F
Population Size: 334
Sources:
Somnolence 5 patients
30 mg 1 times / day steady, oral (median)
Highest studied dose
Dose: 30 mg, 1 times / day
Route: oral
Route: steady
Dose: 30 mg, 1 times / day
Sources:
unhealthy, 6–17 years
n = 334
Health Status: unhealthy
Condition: generalized anxiety disorder
Age Group: 6–17 years
Sex: M+F
Population Size: 334
Sources:
Upper respiratory tract infection 5 patients
30 mg 1 times / day steady, oral (median)
Highest studied dose
Dose: 30 mg, 1 times / day
Route: oral
Route: steady
Dose: 30 mg, 1 times / day
Sources:
unhealthy, 6–17 years
n = 334
Health Status: unhealthy
Condition: generalized anxiety disorder
Age Group: 6–17 years
Sex: M+F
Population Size: 334
Sources:
Diarrhea 6 patients
30 mg 1 times / day steady, oral (median)
Highest studied dose
Dose: 30 mg, 1 times / day
Route: oral
Route: steady
Dose: 30 mg, 1 times / day
Sources:
unhealthy, 6–17 years
n = 334
Health Status: unhealthy
Condition: generalized anxiety disorder
Age Group: 6–17 years
Sex: M+F
Population Size: 334
Sources:
Fatigue below serious, 1 patient
15 mg 2 times / day steady, oral
Dose: 15 mg, 2 times / day
Route: oral
Route: steady
Dose: 15 mg, 2 times / day
Sources:
unhealthy
n = 10
Health Status: unhealthy
Condition: Spinal Cord Injury
Population Size: 10
Sources:
Headache below serious, 1 patient
15 mg 2 times / day steady, oral
Dose: 15 mg, 2 times / day
Route: oral
Route: steady
Dose: 15 mg, 2 times / day
Sources:
unhealthy
n = 10
Health Status: unhealthy
Condition: Spinal Cord Injury
Population Size: 10
Sources:
Nausea below serious, 1 patient
15 mg 2 times / day steady, oral
Dose: 15 mg, 2 times / day
Route: oral
Route: steady
Dose: 15 mg, 2 times / day
Sources:
unhealthy
n = 10
Health Status: unhealthy
Condition: Spinal Cord Injury
Population Size: 10
Sources:
Light headedness below serious, 1 patient
20 mg 2 times / day steady, oral
Dose: 20 mg, 2 times / day
Route: oral
Route: steady
Dose: 20 mg, 2 times / day
Sources:
unhealthy
n = 19
Health Status: unhealthy
Condition: Marijuana Dependence
Population Size: 19
Sources:
Allergic sinusitis below serious, 13 patients
30 mg 2 times / day steady, oral
Dose: 30 mg, 2 times / day
Route: oral
Route: steady
Dose: 30 mg, 2 times / day
Sources:
unhealthy
n = 88
Health Status: unhealthy
Condition: Marijuana Dependence
Population Size: 88
Sources:
Insomnia below serious, 16 patients
30 mg 2 times / day steady, oral
Dose: 30 mg, 2 times / day
Route: oral
Route: steady
Dose: 30 mg, 2 times / day
Sources:
unhealthy
n = 88
Health Status: unhealthy
Condition: Marijuana Dependence
Population Size: 88
Sources:
Drowsiness below serious, 17 patients
30 mg 2 times / day steady, oral
Dose: 30 mg, 2 times / day
Route: oral
Route: steady
Dose: 30 mg, 2 times / day
Sources:
unhealthy
n = 88
Health Status: unhealthy
Condition: Marijuana Dependence
Population Size: 88
Sources:
Headache below serious, 28 patients
30 mg 2 times / day steady, oral
Dose: 30 mg, 2 times / day
Route: oral
Route: steady
Dose: 30 mg, 2 times / day
Sources:
unhealthy
n = 88
Health Status: unhealthy
Condition: Marijuana Dependence
Population Size: 88
Sources:
Gastrointestinal disorder below serious, 36 patients
30 mg 2 times / day steady, oral
Dose: 30 mg, 2 times / day
Route: oral
Route: steady
Dose: 30 mg, 2 times / day
Sources:
unhealthy
n = 88
Health Status: unhealthy
Condition: Marijuana Dependence
Population Size: 88
Sources:
Lightheadedness below serious, 36 patients
30 mg 2 times / day steady, oral
Dose: 30 mg, 2 times / day
Route: oral
Route: steady
Dose: 30 mg, 2 times / day
Sources:
unhealthy
n = 88
Health Status: unhealthy
Condition: Marijuana Dependence
Population Size: 88
Sources:
Balance impaired NOS below serious, 1 patient
30 mg 2 times / day steady, oral
Dose: 30 mg, 2 times / day
Route: oral
Route: steady
Dose: 30 mg, 2 times / day
Sources:
unhealthy
n = 17
Health Status: unhealthy
Condition: Parkinson's disease
Population Size: 17
Sources:
Bradycardia below serious, 1 patient
30 mg 2 times / day steady, oral
Dose: 30 mg, 2 times / day
Route: oral
Route: steady
Dose: 30 mg, 2 times / day
Sources:
unhealthy
n = 17
Health Status: unhealthy
Condition: Parkinson's disease
Population Size: 17
Sources:
Constipation below serious, 1 patient
30 mg 2 times / day steady, oral
Dose: 30 mg, 2 times / day
Route: oral
Route: steady
Dose: 30 mg, 2 times / day
Sources:
unhealthy
n = 17
Health Status: unhealthy
Condition: Parkinson's disease
Population Size: 17
Sources:
Cramp in hand below serious, 1 patient
30 mg 2 times / day steady, oral
Dose: 30 mg, 2 times / day
Route: oral
Route: steady
Dose: 30 mg, 2 times / day
Sources:
unhealthy
n = 17
Health Status: unhealthy
Condition: Parkinson's disease
Population Size: 17
Sources:
Dysphagia below serious, 1 patient
30 mg 2 times / day steady, oral
Dose: 30 mg, 2 times / day
Route: oral
Route: steady
Dose: 30 mg, 2 times / day
Sources:
unhealthy
n = 17
Health Status: unhealthy
Condition: Parkinson's disease
Population Size: 17
Sources:
Dystonia below serious, 1 patient
30 mg 2 times / day steady, oral
Dose: 30 mg, 2 times / day
Route: oral
Route: steady
Dose: 30 mg, 2 times / day
Sources:
unhealthy
n = 17
Health Status: unhealthy
Condition: Parkinson's disease
Population Size: 17
Sources:
Gastritis and duodenitis below serious, 1 patient
30 mg 2 times / day steady, oral
Dose: 30 mg, 2 times / day
Route: oral
Route: steady
Dose: 30 mg, 2 times / day
Sources:
unhealthy
n = 17
Health Status: unhealthy
Condition: Parkinson's disease
Population Size: 17
Sources:
Gastrointestinal disorder (NOS) below serious, 1 patient
30 mg 2 times / day steady, oral
Dose: 30 mg, 2 times / day
Route: oral
Route: steady
Dose: 30 mg, 2 times / day
Sources:
unhealthy
n = 17
Health Status: unhealthy
Condition: Parkinson's disease
Population Size: 17
Sources:
Headache below serious, 1 patient
30 mg 2 times / day steady, oral
Dose: 30 mg, 2 times / day
Route: oral
Route: steady
Dose: 30 mg, 2 times / day
Sources:
unhealthy
n = 17
Health Status: unhealthy
Condition: Parkinson's disease
Population Size: 17
Sources:
Increased agitation below serious, 1 patient
30 mg 2 times / day steady, oral
Dose: 30 mg, 2 times / day
Route: oral
Route: steady
Dose: 30 mg, 2 times / day
Sources:
unhealthy
n = 17
Health Status: unhealthy
Condition: Parkinson's disease
Population Size: 17
Sources:
Increased appetite below serious, 1 patient
30 mg 2 times / day steady, oral
Dose: 30 mg, 2 times / day
Route: oral
Route: steady
Dose: 30 mg, 2 times / day
Sources:
unhealthy
n = 17
Health Status: unhealthy
Condition: Parkinson's disease
Population Size: 17
Sources:
Infection respiratory below serious, 1 patient
30 mg 2 times / day steady, oral
Dose: 30 mg, 2 times / day
Route: oral
Route: steady
Dose: 30 mg, 2 times / day
Sources:
unhealthy
n = 17
Health Status: unhealthy
Condition: Parkinson's disease
Population Size: 17
Sources:
Insomnia below serious, 1 patient
30 mg 2 times / day steady, oral
Dose: 30 mg, 2 times / day
Route: oral
Route: steady
Dose: 30 mg, 2 times / day
Sources:
unhealthy
n = 17
Health Status: unhealthy
Condition: Parkinson's disease
Population Size: 17
Sources:
Irritability below serious, 1 patient
30 mg 2 times / day steady, oral
Dose: 30 mg, 2 times / day
Route: oral
Route: steady
Dose: 30 mg, 2 times / day
Sources:
unhealthy
n = 17
Health Status: unhealthy
Condition: Parkinson's disease
Population Size: 17
Sources:
Joint stiffness below serious, 1 patient
30 mg 2 times / day steady, oral
Dose: 30 mg, 2 times / day
Route: oral
Route: steady
Dose: 30 mg, 2 times / day
Sources:
unhealthy
n = 17
Health Status: unhealthy
Condition: Parkinson's disease
Population Size: 17
Sources:
Leg pain below serious, 1 patient
30 mg 2 times / day steady, oral
Dose: 30 mg, 2 times / day
Route: oral
Route: steady
Dose: 30 mg, 2 times / day
Sources:
unhealthy
n = 17
Health Status: unhealthy
Condition: Parkinson's disease
Population Size: 17
Sources:
Nasal congestion below serious, 1 patient
30 mg 2 times / day steady, oral
Dose: 30 mg, 2 times / day
Route: oral
Route: steady
Dose: 30 mg, 2 times / day
Sources:
unhealthy
n = 17
Health Status: unhealthy
Condition: Parkinson's disease
Population Size: 17
Sources:
Numbness below serious, 1 patient
30 mg 2 times / day steady, oral
Dose: 30 mg, 2 times / day
Route: oral
Route: steady
Dose: 30 mg, 2 times / day
Sources:
unhealthy
n = 17
Health Status: unhealthy
Condition: Parkinson's disease
Population Size: 17
Sources:
Pain in knee below serious, 1 patient
30 mg 2 times / day steady, oral
Dose: 30 mg, 2 times / day
Route: oral
Route: steady
Dose: 30 mg, 2 times / day
Sources:
unhealthy
n = 17
Health Status: unhealthy
Condition: Parkinson's disease
Population Size: 17
Sources:
Pain neck/shoulder below serious, 1 patient
30 mg 2 times / day steady, oral
Dose: 30 mg, 2 times / day
Route: oral
Route: steady
Dose: 30 mg, 2 times / day
Sources:
unhealthy
n = 17
Health Status: unhealthy
Condition: Parkinson's disease
Population Size: 17
Sources:
Pain below serious, 1 patient
30 mg 2 times / day steady, oral
Dose: 30 mg, 2 times / day
Route: oral
Route: steady
Dose: 30 mg, 2 times / day
Sources:
unhealthy
n = 17
Health Status: unhealthy
Condition: Parkinson's disease
Population Size: 17
Sources:
Dizziness below serious, 2 patients
30 mg 2 times / day steady, oral
Dose: 30 mg, 2 times / day
Route: oral
Route: steady
Dose: 30 mg, 2 times / day
Sources:
unhealthy
n = 17
Health Status: unhealthy
Condition: Parkinson's disease
Population Size: 17
Sources:
Fatigue below serious, 2 patients
30 mg 2 times / day steady, oral
Dose: 30 mg, 2 times / day
Route: oral
Route: steady
Dose: 30 mg, 2 times / day
Sources:
unhealthy
n = 17
Health Status: unhealthy
Condition: Parkinson's disease
Population Size: 17
Sources:
Tremor below serious, 3 patients
30 mg 2 times / day steady, oral
Dose: 30 mg, 2 times / day
Route: oral
Route: steady
Dose: 30 mg, 2 times / day
Sources:
unhealthy
n = 17
Health Status: unhealthy
Condition: Parkinson's disease
Population Size: 17
Sources:
Frozen gait below serious, 5 patients
30 mg 2 times / day steady, oral
Dose: 30 mg, 2 times / day
Route: oral
Route: steady
Dose: 30 mg, 2 times / day
Sources:
unhealthy
n = 17
Health Status: unhealthy
Condition: Parkinson's disease
Population Size: 17
Sources:
Overview

Overview

CYP3A4CYP2C9CYP2D6hERG


OverviewOther

Other InhibitorOther SubstrateOther Inducer

Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
major
yes (co-administration study)
Comment: coadministration of buspirone (10 mg as a single dose) with verapamil (80 mg t.i.d.) or diltiazem (60 mg t.i.d.) increased plasma buspirone concentrations; coadministration of buspirone (10 mg as a single dose) with erythromycin (1.5 g/day for 4 days) increased plasma buspirone concentrations (5-fold increase in Cmax and 6-fold increase in AUC); coadministration of buspirone (10 mg as a single dose) with itraconazole (200 mg/day for 4 days) increased plasma buspirone concentrations (13-fold increase in Cmax and 19-fold increase in AUC); coadministration of buspirone (2.5 or 5 mg b.i.d.) with nefazodone (250 mg b.i.d.) resulted in marked increases in plasma buspirone concentrations (increases up to 20-fold in Cmax and up to 50-fold in AUC); coadministration of buspirone (30 mg as a single dose) with rifampin (600 mg/day for 5 days) decreased the plasma concentrations (83.7% decrease in Cmax; 89.6% decrease in AUC);
Page: 3.0
minor
minor
PubMed

PubMed

TitleDatePubMed
[Regulation of the central opioidergic nervous system on the emotional state of anxiety and its possible mechanisms].
1997 Jan
Effect of buspirone on sexual dysfunction in depressed patients treated with selective serotonin reuptake inhibitors.
1999 Jun
Reversal of morphine-induced apnea in the anesthetized rat by drugs that activate 5-hydroxytryptamine(1A) receptors.
2000 Feb
Possible serotonin syndrome associated with buspirone added to fluoxetine.
2000 Jul-Aug
Controversies in dyspepsia.
2001
Separation anxiety disorder in children and adolescents: epidemiology, diagnosis and management.
2001
Synthesis and pharmacological evaluation of aryl/heteroaryl piperazinyl alkyl benzotriazoles as ligands for some serotonin and dopamine receptor subtypes.
2001 Apr
A comparative multidose pharmacokinetic study of buspirone extended-release tablets with a reference immediate-release product.
2001 Aug
Ataxia from lithium toxicity successfully treated with high-dose buspirone: a single-case experimental design.
2001 Aug
Serotonergic regulation of inhibitory avoidance and one-way escape in the rat elevated T-maze.
2001 Dec
The impact of impulsivity on cocaine use and retention in treatment.
2001 Dec
Pharmacokinetics and tolerability of buspirone during oral administration to children and adolescents with anxiety disorder and normal healthy adults.
2001 Dec
Effects of cholecystokinin tetrapeptide (CCK(4)) and anxiolytic drugs on the electrically evoked [(3)H]5-hydroxytryptamine outflow from rat cortical slices.
2001 Dec 13
Anxiety-like behavior in elevated plus-maze tests in repeatedly cold-stressed mice.
2001 Feb
Prenatal stress and postnatal development of neonatal rats--sex-dependent effects on emotional behavior and learning ability of neonatal rats.
2001 Feb
Female sexual dysfunction and antidepressant use.
2001 Feb
Pharmacokinetics of buspirone extended-release tablets: a single-dose study.
2001 Jul
Common effects of chronically administered antipanic drugs on brainstem GABA(A) receptor subunit gene expression.
2001 Jul
Late-onset bipolar disorder due to hyperthyroidism.
2001 Jul
Characterization of alpha1-adrenoceptor-mediated contraction in the mouse thoracic aorta.
2001 Jul 20
Effect of citalopram and buspirone on the antinociceptive action of analgesic drugs.
2001 Jul-Aug
Behavioral and biochemical effects of L-tryptophan and buspirone in a model of cerebellar atrophy.
2001 Jul-Aug
Patients with severe depression may benefit from buspirone augmentation of selective serotonin reuptake inhibitors: results from a placebo-controlled, randomized, double-blind, placebo wash-in study.
2001 Jun
Potential involvement of S100B in the protective effects of a serotonin-1a agonist on ethanol-treated astrocytes.
2001 Jun 29
Discriminative stimulus properties of indorenate, a 5-HT1A, 5-HT1B and 5-HT2C agonist: a study in rats.
2001 Mar
Is imipramine or buspirone treatment effective in patients wishing to discontinue long-term benzodiazepine use?
2001 Mar
Generalized anxiety disorder in children and adolescents.
2001 Mar
Population pharmacokinetic-pharmacodynamic modelling of S 15535, a 5-HT(1A) receptor agonist, using a behavioural model in rats.
2001 Mar 2
Ligand induced conformational states of the 5-HT(1A) receptor.
2001 Mar 23
Conformational analysis and pharmacophore design for selected 1-(2-pyrimidinyl)piperazine derivatives with sedative-hypnotic activity.
2001 Mar-Apr
Neuropharmacological analysis of the role of the serotoninergic system in forming hyperalgesia in neurotic rats.
2001 May-Jun
Quantifying the 5-HT1A agonist action of buspirone in man.
2001 Nov
Astrocyte-mediated trophic support of developing serotonin neurons: effects of ethanol, buspirone, and S100B.
2001 Nov 26
Venlafaxine and generalised anxiety disorder: new preparation. Minimise recourse to drugs.
2001 Oct
Impact of cortisol on buspirone stimulated prolactin release: a double-blind placebo-controlled study.
2001 Oct
Diazepam, but not buspirone, induces similar anxiolytic-like actions in lactating and ovariectomized Wistar rats.
2001 Sep
Hypomania induced by herbal and pharmaceutical psychotropic medicines following mild traumatic brain injury.
2002 Apr
Tandospirone potentiates the fluoxetine-induced increases in extracellular dopamine via 5-HT(1A) receptors in the rat medial frontal cortex.
2002 Apr
Bupropion-induced acute dystonia.
2002 Feb
Benzodiazepine discontinuation in generalized anxiety disorder.
2002 Feb
Effect of drug proportion and mixing time on the content uniformity of a low dose drug in a high shear mixer.
2002 Jan
Contact leukoderma caused by buspirone patches.
2002 Mar
Patents

Sample Use Guides

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 mg to 30 mg per day were commonly employed.
Route of Administration: Oral
In Vitro Use Guide
Buspiron was incubated with hippocampal pyramidal cells at concentration of 50 uM. Buspirone was shown to attenuate the synaptic activation of cells.
Substance Class Chemical
Created
by admin
on Wed Jul 05 23:22:21 UTC 2023
Edited
by admin
on Wed Jul 05 23:22:21 UTC 2023
Record UNII
TK65WKS8HL
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
BUSPIRONE
INN   MI   VANDF   WHO-DD  
INN  
Official Name English
BUSPIRONE [VANDF]
Common Name English
buspirone [INN]
Common Name English
8-(4-(4-(2-PYRIMIDINYL)-1-PIPERIZINYL)BUTYL)-8-AZASPIRO(4,5)DECANE-7,9-DIONE
Systematic Name English
BUSPIRONE [MI]
Common Name English
BCI-024
Code English
GEN-BUSPIRONE
Brand Name English
Buspirone [WHO-DD]
Common Name English
Classification Tree Code System Code
WHO-VATC QN05BE01
Created by admin on Wed Jul 05 23:22:21 UTC 2023 , Edited by admin on Wed Jul 05 23:22:21 UTC 2023
LIVERTOX NBK547966
Created by admin on Wed Jul 05 23:22:21 UTC 2023 , Edited by admin on Wed Jul 05 23:22:21 UTC 2023
WHO-ATC N05BE01
Created by admin on Wed Jul 05 23:22:21 UTC 2023 , Edited by admin on Wed Jul 05 23:22:21 UTC 2023
NCI_THESAURUS C28197
Created by admin on Wed Jul 05 23:22:21 UTC 2023 , Edited by admin on Wed Jul 05 23:22:21 UTC 2023
Code System Code Type Description
SMS_ID
100000088473
Created by admin on Wed Jul 05 23:22:21 UTC 2023 , Edited by admin on Wed Jul 05 23:22:21 UTC 2023
PRIMARY
CAS
36505-84-7
Created by admin on Wed Jul 05 23:22:21 UTC 2023 , Edited by admin on Wed Jul 05 23:22:21 UTC 2023
PRIMARY
CHEBI
3223
Created by admin on Wed Jul 05 23:22:21 UTC 2023 , Edited by admin on Wed Jul 05 23:22:21 UTC 2023
PRIMARY
DAILYMED
TK65WKS8HL
Created by admin on Wed Jul 05 23:22:21 UTC 2023 , Edited by admin on Wed Jul 05 23:22:21 UTC 2023
PRIMARY
MERCK INDEX
M2777
Created by admin on Wed Jul 05 23:22:21 UTC 2023 , Edited by admin on Wed Jul 05 23:22:21 UTC 2023
PRIMARY Merck Index
ChEMBL
CHEMBL49
Created by admin on Wed Jul 05 23:22:21 UTC 2023 , Edited by admin on Wed Jul 05 23:22:21 UTC 2023
PRIMARY
PUBCHEM
2477
Created by admin on Wed Jul 05 23:22:21 UTC 2023 , Edited by admin on Wed Jul 05 23:22:21 UTC 2023
PRIMARY
EVMPD
SUB05992MIG
Created by admin on Wed Jul 05 23:22:21 UTC 2023 , Edited by admin on Wed Jul 05 23:22:21 UTC 2023
PRIMARY
IUPHAR
36
Created by admin on Wed Jul 05 23:22:21 UTC 2023 , Edited by admin on Wed Jul 05 23:22:21 UTC 2023
PRIMARY
RXCUI
1827
Created by admin on Wed Jul 05 23:22:21 UTC 2023 , Edited by admin on Wed Jul 05 23:22:21 UTC 2023
PRIMARY RxNorm
DRUG CENTRAL
437
Created by admin on Wed Jul 05 23:22:21 UTC 2023 , Edited by admin on Wed Jul 05 23:22:21 UTC 2023
PRIMARY
MESH
D002065
Created by admin on Wed Jul 05 23:22:21 UTC 2023 , Edited by admin on Wed Jul 05 23:22:21 UTC 2023
PRIMARY
ECHA (EC/EINECS)
253-072-2
Created by admin on Wed Jul 05 23:22:21 UTC 2023 , Edited by admin on Wed Jul 05 23:22:21 UTC 2023
PRIMARY
WIKIPEDIA
BUSPIRONE
Created by admin on Wed Jul 05 23:22:21 UTC 2023 , Edited by admin on Wed Jul 05 23:22:21 UTC 2023
PRIMARY
NCI_THESAURUS
C62013
Created by admin on Wed Jul 05 23:22:21 UTC 2023 , Edited by admin on Wed Jul 05 23:22:21 UTC 2023
PRIMARY
INN
3456
Created by admin on Wed Jul 05 23:22:21 UTC 2023 , Edited by admin on Wed Jul 05 23:22:21 UTC 2023
PRIMARY
FDA UNII
TK65WKS8HL
Created by admin on Wed Jul 05 23:22:21 UTC 2023 , Edited by admin on Wed Jul 05 23:22:21 UTC 2023
PRIMARY
DRUG BANK
DB00490
Created by admin on Wed Jul 05 23:22:21 UTC 2023 , Edited by admin on Wed Jul 05 23:22:21 UTC 2023
PRIMARY
EPA CompTox
DTXSID2022707
Created by admin on Wed Jul 05 23:22:21 UTC 2023 , Edited by admin on Wed Jul 05 23:22:21 UTC 2023
PRIMARY
LACTMED
Buspirone
Created by admin on Wed Jul 05 23:22:21 UTC 2023 , Edited by admin on Wed Jul 05 23:22:21 UTC 2023
PRIMARY
Related Record Type Details
TARGET->PARTIAL AGONIST
BINDER->LIGAND
BINDING
TARGET -> INHIBITOR
SALT/SOLVATE -> PARENT
METABOLIC ENZYME -> SUBSTRATE
METABOLIC ENZYME -> SUBSTRATE
Related Record Type Details
METABOLITE -> PARENT
METABOLITE -> PARENT
METABOLITE -> PARENT
METABOLITE ACTIVE -> PARENT
METABOLITE ACTIVE -> PARENT
Related Record Type Details
ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
Biological Half-life PHARMACOKINETIC
Volume of Distribution PHARMACOKINETIC