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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

2001
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
Contemporary management of comorbid anxiety and depression in geriatric patients.
2001
Synthesis and pharmacological evaluation of aryl/heteroaryl piperazinyl alkyl benzotriazoles as ligands for some serotonin and dopamine receptor subtypes.
2001 Apr
Gepirone. Organon.
2001 Aug
Ataxia from lithium toxicity successfully treated with high-dose buspirone: a single-case experimental design.
2001 Aug
The impact of impulsivity on cocaine use and retention in treatment.
2001 Dec
Effect of nonnicotine pharmacotherapy on smoking behavior.
2001 Dec
Comparison of antidepressant activity in 4- and 40-week-old male mice in the forced swimming test: involvement of 5-HT1A and 5-HT1B receptors in old 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
Acute hypokalemic paralysis associated with long-term lithium therapy.
2001 Feb
Citalopram-induced bruxism.
2001 Feb
Female sexual dysfunction and antidepressant use.
2001 Feb
Late-onset bipolar disorder due to hyperthyroidism.
2001 Jul
An investigation of the mechanisms responsible for acute fluoxetine-induced anxiogenic-like effects in mice.
2001 Jun
Generalized anxiety disorder in children and adolescents.
2001 Mar
Conformational analysis and pharmacophore design for selected 1-(2-pyrimidinyl)piperazine derivatives with sedative-hypnotic activity.
2001 Mar-Apr
5-HT1A receptor activation and antidepressant-like effects: F 13714 has high efficacy and marked antidepressant potential.
2001 May 25
Pattern of symptom improvement following treatment with venlafaxine XR in patients with generalized anxiety disorder.
2001 Nov
Acoustic startle, conditioned startle potentiation and the effects of 8-OH-DPAT and buspirone in rats selectively bred for differences in 8-OH-DPAT-induced hypothermia.
2001 Nov
Astrocyte-mediated trophic support of developing serotonin neurons: effects of ethanol, buspirone, and S100B.
2001 Nov 26
The effect of glucocorticoids on the anxiolytic efficacy of buspirone.
2001 Oct
Small platform stress increases exploratory activity of mice in staircase test.
2001 Oct
Hypomania induced by herbal and pharmaceutical psychotropic medicines following mild traumatic brain injury.
2002 Apr
Effect of drug proportion and mixing time on the content uniformity of a low dose drug in a high shear mixer.
2002 Jan
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 Fri Dec 15 15:53:53 GMT 2023
Edited
by admin
on Fri Dec 15 15:53:53 GMT 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 Fri Dec 15 15:53:53 GMT 2023 , Edited by admin on Fri Dec 15 15:53:53 GMT 2023
LIVERTOX NBK547966
Created by admin on Fri Dec 15 15:53:53 GMT 2023 , Edited by admin on Fri Dec 15 15:53:53 GMT 2023
WHO-ATC N05BE01
Created by admin on Fri Dec 15 15:53:53 GMT 2023 , Edited by admin on Fri Dec 15 15:53:53 GMT 2023
NCI_THESAURUS C28197
Created by admin on Fri Dec 15 15:53:53 GMT 2023 , Edited by admin on Fri Dec 15 15:53:53 GMT 2023
Code System Code Type Description
SMS_ID
100000088473
Created by admin on Fri Dec 15 15:53:53 GMT 2023 , Edited by admin on Fri Dec 15 15:53:53 GMT 2023
PRIMARY
CAS
36505-84-7
Created by admin on Fri Dec 15 15:53:53 GMT 2023 , Edited by admin on Fri Dec 15 15:53:53 GMT 2023
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CHEBI
3223
Created by admin on Fri Dec 15 15:53:53 GMT 2023 , Edited by admin on Fri Dec 15 15:53:53 GMT 2023
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DAILYMED
TK65WKS8HL
Created by admin on Fri Dec 15 15:53:53 GMT 2023 , Edited by admin on Fri Dec 15 15:53:53 GMT 2023
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MERCK INDEX
m2777
Created by admin on Fri Dec 15 15:53:53 GMT 2023 , Edited by admin on Fri Dec 15 15:53:53 GMT 2023
PRIMARY Merck Index
ChEMBL
CHEMBL49
Created by admin on Fri Dec 15 15:53:53 GMT 2023 , Edited by admin on Fri Dec 15 15:53:53 GMT 2023
PRIMARY
PUBCHEM
2477
Created by admin on Fri Dec 15 15:53:53 GMT 2023 , Edited by admin on Fri Dec 15 15:53:53 GMT 2023
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EVMPD
SUB05992MIG
Created by admin on Fri Dec 15 15:53:53 GMT 2023 , Edited by admin on Fri Dec 15 15:53:53 GMT 2023
PRIMARY
IUPHAR
36
Created by admin on Fri Dec 15 15:53:53 GMT 2023 , Edited by admin on Fri Dec 15 15:53:53 GMT 2023
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RXCUI
1827
Created by admin on Fri Dec 15 15:53:53 GMT 2023 , Edited by admin on Fri Dec 15 15:53:53 GMT 2023
PRIMARY RxNorm
DRUG CENTRAL
437
Created by admin on Fri Dec 15 15:53:53 GMT 2023 , Edited by admin on Fri Dec 15 15:53:53 GMT 2023
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MESH
D002065
Created by admin on Fri Dec 15 15:53:53 GMT 2023 , Edited by admin on Fri Dec 15 15:53:53 GMT 2023
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ECHA (EC/EINECS)
253-072-2
Created by admin on Fri Dec 15 15:53:53 GMT 2023 , Edited by admin on Fri Dec 15 15:53:53 GMT 2023
PRIMARY
WIKIPEDIA
BUSPIRONE
Created by admin on Fri Dec 15 15:53:53 GMT 2023 , Edited by admin on Fri Dec 15 15:53:53 GMT 2023
PRIMARY
NCI_THESAURUS
C62013
Created by admin on Fri Dec 15 15:53:53 GMT 2023 , Edited by admin on Fri Dec 15 15:53:53 GMT 2023
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INN
3456
Created by admin on Fri Dec 15 15:53:53 GMT 2023 , Edited by admin on Fri Dec 15 15:53:53 GMT 2023
PRIMARY
FDA UNII
TK65WKS8HL
Created by admin on Fri Dec 15 15:53:53 GMT 2023 , Edited by admin on Fri Dec 15 15:53:53 GMT 2023
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DRUG BANK
DB00490
Created by admin on Fri Dec 15 15:53:53 GMT 2023 , Edited by admin on Fri Dec 15 15:53:53 GMT 2023
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EPA CompTox
DTXSID2022707
Created by admin on Fri Dec 15 15:53:53 GMT 2023 , Edited by admin on Fri Dec 15 15:53:53 GMT 2023
PRIMARY
LACTMED
Buspirone
Created by admin on Fri Dec 15 15:53:53 GMT 2023 , Edited by admin on Fri Dec 15 15:53:53 GMT 2023
PRIMARY
Related Record Type Details
METABOLIC ENZYME -> SUBSTRATE
TARGET->PARTIAL AGONIST
BINDER->LIGAND
BINDING
TARGET -> INHIBITOR
METABOLIC ENZYME -> SUBSTRATE
SALT/SOLVATE -> PARENT
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METABOLITE -> PARENT
METABOLITE -> PARENT
METABOLITE -> PARENT
METABOLITE ACTIVE -> PARENT
METABOLITE ACTIVE -> PARENT
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ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
Biological Half-life PHARMACOKINETIC
Volume of Distribution PHARMACOKINETIC