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Details

Stereochemistry ACHIRAL
Molecular Formula C21H31N5O2.ClH
Molecular Weight 421.9648
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of BUSPIRONE HYDROCHLORIDE

SMILES

C1CCC2(C1)CC(=O)N(CCCCN3CCN(CC3)c4ncccn4)C(=O)C2.Cl

InChI

InChIKey=RICLFGYGYQXUFH-UHFFFAOYSA-N
InChI=1S/C21H31N5O2.ClH/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;1H

HIDE SMILES / InChI
Molecular Formula C21H31N5O2
Molecular Weight 385.5039
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE
Molecular Formula ClH
Molecular Weight 36.4609
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.

CNS Activity

Originator

Bristol-Myers Squibb
140
Sources: ISBN-13: 978-1285845227

Approval Year

1986
100
Targets

Targets

Primary TargetPharmacologyConditionPotency
Partial Agonist
266
 24.0 nM [IC50]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Approved
8043
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
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/11504277
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
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/11504277
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
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/11504277
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
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/11504277
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
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/11504277
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%
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2001/18731s39s45lbl.pdf
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:
https://pubmed.ncbi.nlm.nih.gov/28846022/
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:
https://pubmed.ncbi.nlm.nih.gov/28846022/
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:
https://pubmed.ncbi.nlm.nih.gov/28846022/
15 mg 2 times / day steady, oral
Dose: 15 mg, 2 times / day
Route: oral
Route: steady
Dose: 15 mg, 2 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT02458469
unhealthy
n = 10
Health Status: unhealthy
Condition: Spinal Cord Injury
Population Size: 10
Sources:
https://clinicaltrials.gov/ct2/show/NCT02458469
Other AEs: Nausea, Headache...
Other AEs:
Nausea (below serious, 1 patient)
Headache (below serious, 1 patient)
Fatigue (below serious, 1 patient)
Sources:
https://clinicaltrials.gov/ct2/show/NCT02458469
20 mg 2 times / day steady, oral
Dose: 20 mg, 2 times / day
Route: oral
Route: steady
Dose: 20 mg, 2 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT02132832
unhealthy
n = 19
Health Status: unhealthy
Condition: Marijuana Dependence
Population Size: 19
Sources:
https://clinicaltrials.gov/ct2/show/NCT02132832
Other AEs: Light headedness...
Other AEs:
Light headedness (below serious, 1 patient)
Sources:
https://clinicaltrials.gov/ct2/show/NCT02132832
30 mg 2 times / day steady, oral
Dose: 30 mg, 2 times / day
Route: oral
Route: steady
Dose: 30 mg, 2 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT00875836
unhealthy
n = 88
Health Status: unhealthy
Condition: Marijuana Dependence
Population Size: 88
Sources:
https://clinicaltrials.gov/ct2/show/NCT00875836
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:
https://clinicaltrials.gov/ct2/show/NCT00875836
30 mg 2 times / day steady, oral
Dose: 30 mg, 2 times / day
Route: oral
Route: steady
Dose: 30 mg, 2 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT02803749
unhealthy
n = 17
Health Status: unhealthy
Condition: Parkinson's disease
Population Size: 17
Sources:
https://clinicaltrials.gov/ct2/show/NCT02803749
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:
https://clinicaltrials.gov/ct2/show/NCT02803749
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:
https://pubmed.ncbi.nlm.nih.gov/28846022/
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:
https://pubmed.ncbi.nlm.nih.gov/28846022/
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:
https://pubmed.ncbi.nlm.nih.gov/28846022/
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:
https://pubmed.ncbi.nlm.nih.gov/28846022/
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:
https://pubmed.ncbi.nlm.nih.gov/28846022/
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:
https://pubmed.ncbi.nlm.nih.gov/28846022/
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:
https://pubmed.ncbi.nlm.nih.gov/28846022/
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:
https://pubmed.ncbi.nlm.nih.gov/28846022/
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:
https://pubmed.ncbi.nlm.nih.gov/28846022/
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:
https://pubmed.ncbi.nlm.nih.gov/28846022/
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:
https://pubmed.ncbi.nlm.nih.gov/28846022/
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:
https://pubmed.ncbi.nlm.nih.gov/28846022/
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:
https://pubmed.ncbi.nlm.nih.gov/28846022/
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:
https://pubmed.ncbi.nlm.nih.gov/28846022/
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:
https://pubmed.ncbi.nlm.nih.gov/28846022/
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:
https://pubmed.ncbi.nlm.nih.gov/28846022/
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:
https://pubmed.ncbi.nlm.nih.gov/28846022/
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:
https://pubmed.ncbi.nlm.nih.gov/28846022/
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:
https://pubmed.ncbi.nlm.nih.gov/28846022/
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:
https://pubmed.ncbi.nlm.nih.gov/28846022/
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:
https://pubmed.ncbi.nlm.nih.gov/28846022/
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:
https://pubmed.ncbi.nlm.nih.gov/28846022/
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:
https://pubmed.ncbi.nlm.nih.gov/28846022/
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:
https://pubmed.ncbi.nlm.nih.gov/28846022/
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:
https://clinicaltrials.gov/ct2/show/NCT02458469
unhealthy
n = 10
Health Status: unhealthy
Condition: Spinal Cord Injury
Population Size: 10
Sources:
https://clinicaltrials.gov/ct2/show/NCT02458469
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:
https://clinicaltrials.gov/ct2/show/NCT02458469
unhealthy
n = 10
Health Status: unhealthy
Condition: Spinal Cord Injury
Population Size: 10
Sources:
https://clinicaltrials.gov/ct2/show/NCT02458469
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:
https://clinicaltrials.gov/ct2/show/NCT02458469
unhealthy
n = 10
Health Status: unhealthy
Condition: Spinal Cord Injury
Population Size: 10
Sources:
https://clinicaltrials.gov/ct2/show/NCT02458469
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:
https://clinicaltrials.gov/ct2/show/NCT02132832
unhealthy
n = 19
Health Status: unhealthy
Condition: Marijuana Dependence
Population Size: 19
Sources:
https://clinicaltrials.gov/ct2/show/NCT02132832
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:
https://clinicaltrials.gov/ct2/show/NCT00875836
unhealthy
n = 88
Health Status: unhealthy
Condition: Marijuana Dependence
Population Size: 88
Sources:
https://clinicaltrials.gov/ct2/show/NCT00875836
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:
https://clinicaltrials.gov/ct2/show/NCT00875836
unhealthy
n = 88
Health Status: unhealthy
Condition: Marijuana Dependence
Population Size: 88
Sources:
https://clinicaltrials.gov/ct2/show/NCT00875836
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:
https://clinicaltrials.gov/ct2/show/NCT00875836
unhealthy
n = 88
Health Status: unhealthy
Condition: Marijuana Dependence
Population Size: 88
Sources:
https://clinicaltrials.gov/ct2/show/NCT00875836
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:
https://clinicaltrials.gov/ct2/show/NCT00875836
unhealthy
n = 88
Health Status: unhealthy
Condition: Marijuana Dependence
Population Size: 88
Sources:
https://clinicaltrials.gov/ct2/show/NCT00875836
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:
https://clinicaltrials.gov/ct2/show/NCT00875836
unhealthy
n = 88
Health Status: unhealthy
Condition: Marijuana Dependence
Population Size: 88
Sources:
https://clinicaltrials.gov/ct2/show/NCT00875836
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:
https://clinicaltrials.gov/ct2/show/NCT00875836
unhealthy
n = 88
Health Status: unhealthy
Condition: Marijuana Dependence
Population Size: 88
Sources:
https://clinicaltrials.gov/ct2/show/NCT00875836
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:
https://clinicaltrials.gov/ct2/show/NCT02803749
unhealthy
n = 17
Health Status: unhealthy
Condition: Parkinson's disease
Population Size: 17
Sources:
https://clinicaltrials.gov/ct2/show/NCT02803749
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:
https://clinicaltrials.gov/ct2/show/NCT02803749
unhealthy
n = 17
Health Status: unhealthy
Condition: Parkinson's disease
Population Size: 17
Sources:
https://clinicaltrials.gov/ct2/show/NCT02803749
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:
https://clinicaltrials.gov/ct2/show/NCT02803749
unhealthy
n = 17
Health Status: unhealthy
Condition: Parkinson's disease
Population Size: 17
Sources:
https://clinicaltrials.gov/ct2/show/NCT02803749
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:
https://clinicaltrials.gov/ct2/show/NCT02803749
unhealthy
n = 17
Health Status: unhealthy
Condition: Parkinson's disease
Population Size: 17
Sources:
https://clinicaltrials.gov/ct2/show/NCT02803749
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:
https://clinicaltrials.gov/ct2/show/NCT02803749
unhealthy
n = 17
Health Status: unhealthy
Condition: Parkinson's disease
Population Size: 17
Sources:
https://clinicaltrials.gov/ct2/show/NCT02803749
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:
https://clinicaltrials.gov/ct2/show/NCT02803749
unhealthy
n = 17
Health Status: unhealthy
Condition: Parkinson's disease
Population Size: 17
Sources:
https://clinicaltrials.gov/ct2/show/NCT02803749
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:
https://clinicaltrials.gov/ct2/show/NCT02803749
unhealthy
n = 17
Health Status: unhealthy
Condition: Parkinson's disease
Population Size: 17
Sources:
https://clinicaltrials.gov/ct2/show/NCT02803749
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:
https://clinicaltrials.gov/ct2/show/NCT02803749
unhealthy
n = 17
Health Status: unhealthy
Condition: Parkinson's disease
Population Size: 17
Sources:
https://clinicaltrials.gov/ct2/show/NCT02803749
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:
https://clinicaltrials.gov/ct2/show/NCT02803749
unhealthy
n = 17
Health Status: unhealthy
Condition: Parkinson's disease
Population Size: 17
Sources:
https://clinicaltrials.gov/ct2/show/NCT02803749
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:
https://clinicaltrials.gov/ct2/show/NCT02803749
unhealthy
n = 17
Health Status: unhealthy
Condition: Parkinson's disease
Population Size: 17
Sources:
https://clinicaltrials.gov/ct2/show/NCT02803749
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:
https://clinicaltrials.gov/ct2/show/NCT02803749
unhealthy
n = 17
Health Status: unhealthy
Condition: Parkinson's disease
Population Size: 17
Sources:
https://clinicaltrials.gov/ct2/show/NCT02803749
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:
https://clinicaltrials.gov/ct2/show/NCT02803749
unhealthy
n = 17
Health Status: unhealthy
Condition: Parkinson's disease
Population Size: 17
Sources:
https://clinicaltrials.gov/ct2/show/NCT02803749
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:
https://clinicaltrials.gov/ct2/show/NCT02803749
unhealthy
n = 17
Health Status: unhealthy
Condition: Parkinson's disease
Population Size: 17
Sources:
https://clinicaltrials.gov/ct2/show/NCT02803749
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:
https://clinicaltrials.gov/ct2/show/NCT02803749
unhealthy
n = 17
Health Status: unhealthy
Condition: Parkinson's disease
Population Size: 17
Sources:
https://clinicaltrials.gov/ct2/show/NCT02803749
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:
https://clinicaltrials.gov/ct2/show/NCT02803749
unhealthy
n = 17
Health Status: unhealthy
Condition: Parkinson's disease
Population Size: 17
Sources:
https://clinicaltrials.gov/ct2/show/NCT02803749
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:
https://clinicaltrials.gov/ct2/show/NCT02803749
unhealthy
n = 17
Health Status: unhealthy
Condition: Parkinson's disease
Population Size: 17
Sources:
https://clinicaltrials.gov/ct2/show/NCT02803749
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:
https://clinicaltrials.gov/ct2/show/NCT02803749
unhealthy
n = 17
Health Status: unhealthy
Condition: Parkinson's disease
Population Size: 17
Sources:
https://clinicaltrials.gov/ct2/show/NCT02803749
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:
https://clinicaltrials.gov/ct2/show/NCT02803749
unhealthy
n = 17
Health Status: unhealthy
Condition: Parkinson's disease
Population Size: 17
Sources:
https://clinicaltrials.gov/ct2/show/NCT02803749
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:
https://clinicaltrials.gov/ct2/show/NCT02803749
unhealthy
n = 17
Health Status: unhealthy
Condition: Parkinson's disease
Population Size: 17
Sources:
https://clinicaltrials.gov/ct2/show/NCT02803749
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:
https://clinicaltrials.gov/ct2/show/NCT02803749
unhealthy
n = 17
Health Status: unhealthy
Condition: Parkinson's disease
Population Size: 17
Sources:
https://clinicaltrials.gov/ct2/show/NCT02803749
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:
https://clinicaltrials.gov/ct2/show/NCT02803749
unhealthy
n = 17
Health Status: unhealthy
Condition: Parkinson's disease
Population Size: 17
Sources:
https://clinicaltrials.gov/ct2/show/NCT02803749
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:
https://clinicaltrials.gov/ct2/show/NCT02803749
unhealthy
n = 17
Health Status: unhealthy
Condition: Parkinson's disease
Population Size: 17
Sources:
https://clinicaltrials.gov/ct2/show/NCT02803749
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:
https://clinicaltrials.gov/ct2/show/NCT02803749
unhealthy
n = 17
Health Status: unhealthy
Condition: Parkinson's disease
Population Size: 17
Sources:
https://clinicaltrials.gov/ct2/show/NCT02803749
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:
https://clinicaltrials.gov/ct2/show/NCT02803749
unhealthy
n = 17
Health Status: unhealthy
Condition: Parkinson's disease
Population Size: 17
Sources:
https://clinicaltrials.gov/ct2/show/NCT02803749
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:
https://clinicaltrials.gov/ct2/show/NCT02803749
unhealthy
n = 17
Health Status: unhealthy
Condition: Parkinson's disease
Population Size: 17
Sources:
https://clinicaltrials.gov/ct2/show/NCT02803749
Overview

Overview

CYP3A4CYP2C9CYP2D6hERG
substrate
1601
substrate
1118

OverviewOther

Other InhibitorOther SubstrateOther Inducer
CYP3A5
367
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
CYP3A4
1601
 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
CYP2D6
1118
 minor
CYP3A5
367
 minor
Sourcing

Sourcing

Vendor/AggregatorIDURL
ChEBI
CHEBI:3223
https://www.ebi.ac.uk/chebi/searchId.do?chebiId=CHEBI:3223
ChemicalBook
CB1367137
https://www.chemicalbook.com/ChemicalProductProperty_EN_CB1367137
ChemicalBook
CB63118898
https://www.chemicalbook.com/ChemicalProductProperty_EN_CB63118898
ChemicalBook
CB73118901
https://www.chemicalbook.com/ChemicalProductProperty_EN_CB73118901
ChemicalBook
CB93118899
https://www.chemicalbook.com/ChemicalProductProperty_EN_CB93118899
ZINC
ZINC000001530571
http://zinc15.docking.org/substances/ZINC000001530571
eMolecules
1933757
https://www.emolecules.com/cgi-bin/more?vid=1933757
PubMed

PubMed

TitleDatePubMed
Overview of different pharmacotherapies for attaining remission in generalized anxiety disorder.
2001
Separation anxiety disorder in children and adolescents: epidemiology, diagnosis and management.
2001
Contemporary management of comorbid anxiety and depression in geriatric patients.
2001
Pharmacotherapy of generalized anxiety disorder.
2001
Effect of anxiolytics on blood sugar level in rabbits.
2001 Apr
Synthesis and pharmacological evaluation of aryl/heteroaryl piperazinyl alkyl benzotriazoles as ligands for some serotonin and dopamine receptor subtypes.
2001 Apr
Switching from benzodiazepines to buspirone using a tapered overlap method in generalized anxiety disorder.
2001 Aug
Review of pharmacokinetic and pharmacodynamic interaction studies with citalopram.
2001 Aug
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
An open study of buspirone augmentation of neuroleptics in patients with schizophrenia.
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
Effect of nonnicotine pharmacotherapy on smoking behavior.
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
Treatment of the agitation of late-life psychosis and Alzheimer's disease.
2001 Jan
Drug-induced potentiation of prepulse inhibition of acoustic startle reflex in mice: a model for detecting antipsychotic activity?
2001 Jul
An open trial of divalproex sodium in autism spectrum disorders.
2001 Jul
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
Serotonin-based pharmacotherapy for acute neuroleptic-induced akathisia: a new approach to an old problem.
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
[New drugs for the treatment of functional dyspepsia].
2001 Jul-Sep
An investigation of the mechanisms responsible for acute fluoxetine-induced anxiogenic-like effects in mice.
2001 Jun
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
Compounds with affinity for serotonergic receptors in the treatment of premenstrual dysphoria: a comparison of buspirone, nefazodone and placebo.
2001 May
Neuropharmacological analysis of the role of the serotoninergic system in forming hyperalgesia in neurotic rats.
2001 May-Jun
Pattern of symptom improvement following treatment with venlafaxine XR in patients with generalized anxiety disorder.
2001 Nov
Quantifying the 5-HT1A agonist action of buspirone in man.
2001 Nov
Buspirone and meperidine synergistically reduce the shivering threshold.
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
The effect of glucocorticoids on the anxiolytic efficacy of buspirone.
2001 Oct
A double-blind placebo-controlled study of buspirone-stimulated prolactin release in non-ulcer dyspepsia--are central serotoninergic responses enhanced?
2001 Oct
Small platform stress increases exploratory activity of mice in staircase test.
2001 Oct
Impact of cortisol on buspirone stimulated prolactin release: a double-blind placebo-controlled study.
2001 Oct
Effectiveness of pharmacotherapy for body dysmorphic disorder: a chart-review study.
2001 Sep
Diazepam, but not buspirone, induces similar anxiolytic-like actions in lactating and ovariectomized Wistar rats.
2001 Sep
[The role of neuropeptide Y in anxiety].
2001 Sep-Oct
Tandospirone potentiates the fluoxetine-induced increases in extracellular dopamine via 5-HT(1A) receptors in the rat medial frontal cortex.
2002 Apr
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
Short term aerobic exercise training in young males does not alter sensitivity to a central serotonin agonist.
2002 Jan
Pharmacological and endocrinological characterisation of stress-induced hyperthermia in singly housed mice using classical and candidate anxiolytics (LY314582, MPEP and NKP608).
2002 Jan 25
Anxiogenic activity of Myristica fragrans seeds.
2002 Jan-Feb
The stimulus effect of 5,6,7,8-tetrahydro-1,3-dioxolo[4,5-g]isoquinoline is similar to that of cocaine but different from that of amphetamine.
2002 Jan-Feb
Patents

Patents

05473072
2
06686361
2
07071194
2
JP2003527422A
12
JP2007516949A
8
JP2013237690A
2
JPH00826997A
2
JPH07165755A
2
JPS57122082A
2

Sample Use Guides

In Vivo Use Guide
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 Jun 25 21:01:11 UTC 2021
Edited
by admin
on Fri Jun 25 21:01:11 UTC 2021
Record UNII
207LT9J9OC
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
BUSPIRONE HYDROCHLORIDE
EP   MART.   MI   ORANGE BOOK   USAN   USP   USP-RS   VANDF   WHO-DD  
USAN  
Official Name English
8-AZASPIRO(4,5)DECANE-7,9-DIONE, 8-(4-(4-(2-PYRIMIDINYL)-1-PIPERAZINYL)BUTYL)-, MONOHYDROCHLORIDE
Common Name English
BUSPAR
Brand Name English
BUSPIRONE HYDROCHLORIDE [MART.]
Common Name English
MJ 9022-1
Code English
BUSPIRONE HYDROCHLORIDE [VANDF]
Common Name English
BUSPIRONE HYDROCHLORIDE [USP-RS]
Common Name English
BUSPIRONE HYDROCHLORIDE [ORANGE BOOK]
Common Name English
BUSPIRONE HYDROCHLORIDE [EP MONOGRAPH]
Common Name English
N-(4-(4-(2-PYRIMIDINYL)-1-PIPERAZINYL)BUTYL)-1,1-CYCLOPENTANEDIACETAMIDE MONOHYDROCHLORIDE
Systematic Name English
APD-405
Code English
BUSPIRONE HCL
Common Name English
APD405
Code English
BUSPIRONE HYDROCHLORIDE [USAN]
Common Name English
NSC-759571
Code English
BUSPIRONE HYDROCHLORIDE [WHO-DD]
Common Name English
BUSPIRONE HYDROCHLORIDE [MI]
Common Name English
BUSPIRONE HYDROCHLORIDE [USP MONOGRAPH]
Common Name English
NSC-751138
Code English
MJ-9022-1
Code English
BUSPIRONE HYDROCHLORIDE [JAN]
Common Name English
Classification Tree Code System Code
NCI_THESAURUS C28197
Created by admin on Fri Jun 25 21:01:11 UTC 2021 , Edited by admin on Fri Jun 25 21:01:11 UTC 2021
Code System Code Type Description
MERCK INDEX
M2777
Created by admin on Fri Jun 25 21:01:11 UTC 2021 , Edited by admin on Fri Jun 25 21:01:11 UTC 2021
PRIMARY Merck Index
USP_CATALOG
1078802
Created by admin on Fri Jun 25 21:01:11 UTC 2021 , Edited by admin on Fri Jun 25 21:01:11 UTC 2021
PRIMARY USP-RS
ECHA (EC/EINECS)
251-489-4
Created by admin on Fri Jun 25 21:01:11 UTC 2021 , Edited by admin on Fri Jun 25 21:01:11 UTC 2021
PRIMARY
FDA UNII
207LT9J9OC
Created by admin on Fri Jun 25 21:01:11 UTC 2021 , Edited by admin on Fri Jun 25 21:01:11 UTC 2021
PRIMARY
RXCUI
203116
Created by admin on Fri Jun 25 21:01:11 UTC 2021 , Edited by admin on Fri Jun 25 21:01:11 UTC 2021
PRIMARY RxNorm
EPA CompTox
33386-08-2
Created by admin on Fri Jun 25 21:01:11 UTC 2021 , Edited by admin on Fri Jun 25 21:01:11 UTC 2021
PRIMARY
EVMPD
SUB00906MIG
Created by admin on Fri Jun 25 21:01:11 UTC 2021 , Edited by admin on Fri Jun 25 21:01:11 UTC 2021
PRIMARY
ChEMBL
CHEMBL49
Created by admin on Fri Jun 25 21:01:11 UTC 2021 , Edited by admin on Fri Jun 25 21:01:11 UTC 2021
PRIMARY
CAS
33386-08-2
Created by admin on Fri Jun 25 21:01:11 UTC 2021 , Edited by admin on Fri Jun 25 21:01:11 UTC 2021
PRIMARY
PUBCHEM
36431
Created by admin on Fri Jun 25 21:01:11 UTC 2021 , Edited by admin on Fri Jun 25 21:01:11 UTC 2021
PRIMARY
NCI_THESAURUS
C26641
Created by admin on Fri Jun 25 21:01:11 UTC 2021 , Edited by admin on Fri Jun 25 21:01:11 UTC 2021
PRIMARY
DRUG BANK
DBSALT000313
Created by admin on Fri Jun 25 21:01:11 UTC 2021 , Edited by admin on Fri Jun 25 21:01:11 UTC 2021
PRIMARY
Related Record Type Details
Structure of BUSPIRONE
PARENT -> SALT/SOLVATE
Related Record Type Details
BIS(4-(4-(PYRIMIDIN-2-YL)PIPERAZIN-1-YL)BUTYL) 2,2'-(CYCLOPENTANE-1,1-DIYL)DIACETATE.
IMPURITY -> PARENT
impurity detected at UV 240 nm
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
8,8-(BUTANE-1,4-DIYL)BIS(8-AZASPIRO(4.5)DECANE-7,9-DIONE).
IMPURITY -> PARENT
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
Structure of 1-(2-PYRIMIDINYL)PIPERAZINE
IMPURITY -> PARENT
impurity detected at UV 240 nm
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
4-(7,9-DIOXO-8-AZASPIRO(4.5)DECAN-8-YL)BUTYL 2-(1-(2-OXO-2-((4-(4-(PYRIMIDIN-2-YL)PIPERAZIN-1-YL)BUTYL)AMINO)ETHYL)CYCLOPENTYL)ACETATE
IMPURITY -> PARENT
impurity detected at UV 240 nm
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
BISPYRIMIDINYLPIPERAZINYLBUTYL ETHER
IMPURITY -> PARENT
impurity detected at UV 240 nm
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
1,4-BIS(4-(PYRIMIDIN-2-YL)PIPERAZIN-1-YL)BUTANE
IMPURITY -> PARENT
impurity detected at UV 240 nm
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
Structure of 3,3-TETRAMETHYLENEGLUTARIMIDE
IMPURITY -> PARENT
impurity detected at UV 210 nm
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
BUSPIRONE OPEN RING DIMER
IMPURITY -> PARENT
impurity detected at UV 240 nm
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
CHLOROBUSPIRONE
IMPURITY -> PARENT
impurity detected at UV 240 nm
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
8-(4-CHLOROBUTYL)-8-AZASPIRO(4.5)DECANE-7,9-DIONE
IMPURITY -> PARENT
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
1,4-DI(PYRIMIDIN-2-YL)PIPERAZINE
IMPURITY -> PARENT
impurity detected at UV 240 nm
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
BUSPIRONE OPEN RING
IMPURITY -> PARENT
impurity detected at UV 240 nm
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
8-(2-PYRIMIDINYL)-8-AZA-5-AZONIASPIRO(4.5)DECANE
IMPURITY -> PARENT
impurity detected at UV 240 nm
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
8-(4-BROMOBUTYL)-8-AZASPIRO(4.5)DECANE-7,9-DIONE
IMPURITY -> PARENT
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
Related Record Type Details
Structure of BUSPIRONE
ACTIVE MOIETY
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