BUSPIRONE HYDROCHLORIDE

First approved in 1986

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 Search

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
Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2010/018731s051lbl.pdf
Curator's Comment:: 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

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Serotonin 1a (5-HT1a) receptor 162 Target ID: CHEMBL214 Sources: http://psychopharmacologyinstitute.com/cns-receptors/5-ht1a-receptors/	Partial Agonist 259	Anxiety	24 nM [IC50]

Conditions

Condition	Modality	Targets	Highest Phase	Product
Anxiety 245 Sources: https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=c78cf4ff-51b2-851e-89cc-98ea543e3865	Primary	Serotonin 1a (5-HT1a) receptor	Approved 7968	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 985737600000

C_max

Value	Dose	Co-administered	Analyte	Population
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

Value	Dose	Co-administered	Analyte	Population
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

T_1/2

Value	Dose	Co-administered	Analyte	Population
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

F_unbound

Value	Dose	Co-administered	Analyte	Population
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

Dose	Population	Adverse events
30 mg 1 times / day steady, oral 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 Health Status: unhealthy Age Group: 6–17 years Sex: M+F 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 Health Status: unhealthy 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 Health Status: unhealthy 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 Health Status: unhealthy 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 Health Status: unhealthy 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

Overview

CYP3A4	CYP2C9	CYP2D6	hERG
substrate 1469		substrate 1038

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
	CYP3A5 346

Drug as victim

Target	Modality	Activity	Clinical evidence
CYP3A4 1469	substrate 2751 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2010/018731s051lbl.pdf#page=3 Page: 3	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); Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2010/018731s051lbl.pdf#page=3 Page: 3
CYP2D6 1038	substrate 2751 Sources: https://pubmed.ncbi.nlm.nih.gov/15640381/	minor
CYP3A5 346	substrate 2751 Sources: https://pubmed.ncbi.nlm.nih.gov/15640381/	minor

Sourcing

Vendor/Aggregator	ID	URL
ChEBI	CHEBI:3223	https://www.ebi.ac.uk/chebi/searchId.do?chebiId=CHEBI:3223
ZINC	ZINC000001530571	http://zinc15.docking.org/substances/ZINC000001530571

PubMed

Title	Date	PubMed
5-HT1A receptor agonists buspirone and gepirone attenuate apomorphine-induced aggressive behaviour in adult male Wistar rats.	2000 Dec	11220492
Cerebellar Ataxia.	2000 May	11096749
Involvement of 5-hydroxytryptamine(1A) receptors in nicotine-induced tail tremor in rats.	2000 Nov 10	11070179
Separation anxiety disorder in children and adolescents: epidemiology, diagnosis and management.	2001	11460893
Contemporary management of comorbid anxiety and depression in geriatric patients.	2001	11430616
Pharmacotherapy of generalized anxiety disorder.	2001	11414551
New developments in the pharmacotherapy of alcohol dependence.	2001	11268820
Strategies for the treatment of antidepressant-related sexual dysfunction.	2001	11229451
Effect of anxiolytics on blood sugar level in rabbits.	2001 Apr	11491585
Synthesis and pharmacological evaluation of aryl/heteroaryl piperazinyl alkyl benzotriazoles as ligands for some serotonin and dopamine receptor subtypes.	2001 Apr	11421254
Molecular dynamics of buspirone analogues interacting with the 5-HT1A and 5-HT2A serotonin receptors.	2001 Apr	11354671
Does pretreatment anxiety predict response to either bupropion SR or sertraline?	2001 Apr	11292522
A comparative multidose pharmacokinetic study of buspirone extended-release tablets with a reference immediate-release product.	2001 Aug	11504277
Ataxia from lithium toxicity successfully treated with high-dose buspirone: a single-case experimental design.	2001 Aug	11494197
An open study of buspirone augmentation of neuroleptics in patients with schizophrenia.	2001 Aug	11476132
The impact of impulsivity on cocaine use and retention in treatment.	2001 Dec	11777668
Anxiety-like behavior in elevated plus-maze tests in repeatedly cold-stressed mice.	2001 Feb	11286402
Behavioral effects of buspirone in the marmoset employing a predator confrontation test of fear and anxiety.	2001 Feb	11267630
Extracellular serotonin is enhanced in the striatum, but not in the dorsal hippocampus or prefrontal cortex, in rats subjected to an operant conflict procedure.	2001 Feb	11256436
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	11243491
Prenatal stress and postnatal development of neonatal rats--sex-dependent effects on emotional behavior and learning ability of neonatal rats.	2001 Feb	11226753
Acute hypokalemic paralysis associated with long-term lithium therapy.	2001 Feb	11180215
Citalopram-induced bruxism.	2001 Feb	11157444
Female sexual dysfunction and antidepressant use.	2001 Feb	11156829
Treatment of the agitation of late-life psychosis and Alzheimer's disease.	2001 Jan	11520475
Use of negatively reinforcing electrical brain stimulation to detect conventional and nonconventional anxiolytics as well as an anxiogenic drug.	2001 Jan	11274705
Recovery from chronic fatigue syndrome associated with changes in neuroendocrine function.	2001 Jan	11220065
Enhanced cortical extracellular levels of cholecystokinin-like material in a model of anticipation of social defeat in the rat.	2001 Jan 1	11150343
An open trial of divalproex sodium in autism spectrum disorders.	2001 Jul	11488363
Pharmacokinetics of buspirone extended-release tablets: a single-dose study.	2001 Jul	11452712
Common effects of chronically administered antipanic drugs on brainstem GABA(A) receptor subunit gene expression.	2001 Jul	11443524
Behavioral and biochemical effects of L-tryptophan and buspirone in a model of cerebellar atrophy.	2001 Jul-Aug	11509189
SSRI discontinuation and buspirone.	2001 Jun	11384915
Potential involvement of S100B in the protective effects of a serotonin-1a agonist on ethanol-treated astrocytes.	2001 Jun 29	11412901
Discriminative stimulus properties of indorenate in a conditioned taste aversion paradigm.	2001 Mar	11325395
Discriminative stimulus properties of indorenate, a 5-HT1A, 5-HT1B and 5-HT2C agonist: a study in rats.	2001 Mar	11277605
Is imipramine or buspirone treatment effective in patients wishing to discontinue long-term benzodiazepine use?	2001 Mar	11252203
Generalized anxiety disorder in children and adolescents.	2001 Mar	11225504
Pharmacologic treatment of generalized anxiety disorder.	2001 Mar	11225503
Population pharmacokinetic-pharmacodynamic modelling of S 15535, a 5-HT(1A) receptor agonist, using a behavioural model in rats.	2001 Mar 2	11239924
Ligand induced conformational states of the 5-HT(1A) receptor.	2001 Mar 23	11282110
Quantifying drug-related 5-HT1A receptor occupancy with.	2001 May	11401009
Biochemical, electrophysiological and neurohormonal studies with B-20991, a selective 5-HT1A receptor agonist.	2001 May	11360001
5-HT1A receptor activation and antidepressant-like effects: F 13714 has high efficacy and marked antidepressant potential.	2001 May 25	11408031
Neuropharmacological analysis of the role of the serotoninergic system in forming hyperalgesia in neurotic rats.	2001 May-Jun	11430580
Small platform stress increases exploratory activity of mice in staircase test.	2001 Oct	11513357
Effectiveness of pharmacotherapy for body dysmorphic disorder: a chart-review study.	2001 Sep	11681769
Tandospirone potentiates the fluoxetine-induced increases in extracellular dopamine via 5-HT(1A) receptors in the rat medial frontal cortex.	2002 Apr	11792466
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	11812524
Contact leukoderma caused by buspirone patches.	2002 Mar	11911108

Patents

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

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Name

Type

Language

BUSPIRONE HYDROCHLORIDE

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


					TK65WKS8HL

BUSPIRONE

PARENT -> SALT/SOLVATE

Related Record Type Details


					W4Y50EQ8WB

BIS(4-(4-(PYRIMIDIN-2-YL)PIPERAZIN-1-YL)BUTYL) 2,2'-(CYCLOPENTANE-1,1-DIYL)DIACETATE.

IMPURITY -> PARENT

Comments:

impurity detected at UV 240 nm

Interaction Type:

CHROMATOGRAPHIC PURITY (HPLC/UV)

Qualification:

USP

Amount:


					TMA649P5OQ

8,8-(BUTANE-1,4-DIYL)BIS(8-AZASPIRO(4.5)DECANE-7,9-DIONE).

IMPURITY -> PARENT

Interaction Type:

CHROMATOGRAPHIC PURITY (HPLC/UV)

Qualification:

USP

Amount:


					H3B5B38F56

1-(2-PYRIMIDINYL)PIPERAZINE

IMPURITY -> PARENT

Comments:

impurity detected at UV 240 nm

Interaction Type:

CHROMATOGRAPHIC PURITY (HPLC/UV)

Qualification:

USP

Amount:


					M9967CS82V

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

Comments:

impurity detected at UV 240 nm

Interaction Type:

CHROMATOGRAPHIC PURITY (HPLC/UV)

Qualification:

USP

Amount:


					J1AZH0VS74

BISPYRIMIDINYLPIPERAZINYLBUTYL ETHER

IMPURITY -> PARENT

Comments:

impurity detected at UV 240 nm

Interaction Type:

CHROMATOGRAPHIC PURITY (HPLC/UV)

Qualification:

USP

Amount:


					GFL4F0BM3Z

1,4-BIS(4-(PYRIMIDIN-2-YL)PIPERAZIN-1-YL)BUTANE

IMPURITY -> PARENT

Comments:

impurity detected at UV 240 nm

Interaction Type:

CHROMATOGRAPHIC PURITY (HPLC/UV)

Qualification:

USP

Amount:


					VVJ9W0K7W1

3,3-TETRAMETHYLENEGLUTARIMIDE

IMPURITY -> PARENT

Comments:

impurity detected at UV 210 nm

Interaction Type:

CHROMATOGRAPHIC PURITY (HPLC/UV)

Qualification:

USP

Amount:


					CTI4QD21VS

BUSPIRONE OPEN RING DIMER

IMPURITY -> PARENT

Comments:

impurity detected at UV 240 nm

Interaction Type:

CHROMATOGRAPHIC PURITY (HPLC/UV)

Qualification:

USP

Amount:


					T1W138PH08

CHLOROBUSPIRONE

IMPURITY -> PARENT

Comments:

impurity detected at UV 240 nm

Interaction Type:

CHROMATOGRAPHIC PURITY (HPLC/UV)

Qualification:

USP

Amount:


					VT52GF46TT

8-(4-CHLOROBUTYL)-8-AZASPIRO(4.5)DECANE-7,9-DIONE

IMPURITY -> PARENT

Interaction Type:

CHROMATOGRAPHIC PURITY (HPLC/UV)

Qualification:

USP

Amount:


					XZ3J1GA4R4

1,4-DI(PYRIMIDIN-2-YL)PIPERAZINE

IMPURITY -> PARENT

Comments:

impurity detected at UV 240 nm

Interaction Type:

CHROMATOGRAPHIC PURITY (HPLC/UV)

Qualification:

USP

Amount:


					1VPY2M0SUT

BUSPIRONE OPEN RING

IMPURITY -> PARENT

Comments:

impurity detected at UV 240 nm

Interaction Type:

CHROMATOGRAPHIC PURITY (HPLC/UV)

Qualification:

USP

Amount:


					PJU7BDG7TD

8-(2-PYRIMIDINYL)-8-AZA-5-AZONIASPIRO(4.5)DECANE

IMPURITY -> PARENT

Comments:

impurity detected at UV 240 nm

Interaction Type:

CHROMATOGRAPHIC PURITY (HPLC/UV)

Qualification:

USP

Amount:


					2EN6PP2W1M

8-(4-BROMOBUTYL)-8-AZASPIRO(4.5)DECANE-7,9-DIONE

IMPURITY -> PARENT

Interaction Type:

CHROMATOGRAPHIC PURITY (HPLC/UV)

Qualification:

USP

Amount:

Related Record Type Details


					TK65WKS8HL

BUSPIRONE

ACTIVE MOIETY

AE	Significance	Dose	Population
Asthenia	10 patients	30 mg 1 times / day steady, oral 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 Health Status: unhealthy Age Group: 6–17 years Sex: M+F Sources: https://pubmed.ncbi.nlm.nih.gov/28846022/
Nausea	13 patients	30 mg 1 times / day steady, oral 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 Health Status: unhealthy Age Group: 6–17 years Sex: M+F Sources: https://pubmed.ncbi.nlm.nih.gov/28846022/
Lightheadedness	14 patients	30 mg 1 times / day steady, oral 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 Health Status: unhealthy Age Group: 6–17 years Sex: M+F Sources: https://pubmed.ncbi.nlm.nih.gov/28846022/
Accidental injury	16 patients	30 mg 1 times / day steady, oral 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 Health Status: unhealthy Age Group: 6–17 years Sex: M+F Sources: https://pubmed.ncbi.nlm.nih.gov/28846022/
Headache	29 patients	30 mg 1 times / day steady, oral 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 Health Status: unhealthy Age Group: 6–17 years Sex: M+F Sources: https://pubmed.ncbi.nlm.nih.gov/28846022/
Vomiting	34 patients	30 mg 1 times / day steady, oral 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 Health Status: unhealthy Age Group: 6–17 years Sex: M+F Sources: https://pubmed.ncbi.nlm.nih.gov/28846022/
Dyspepsia	5 patients	30 mg 1 times / day steady, oral 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 Health Status: unhealthy Age Group: 6–17 years Sex: M+F Sources: https://pubmed.ncbi.nlm.nih.gov/28846022/
Insomnia	5 patients	30 mg 1 times / day steady, oral 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 Health Status: unhealthy Age Group: 6–17 years Sex: M+F Sources: https://pubmed.ncbi.nlm.nih.gov/28846022/
Nervousness	5 patients	30 mg 1 times / day steady, oral 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 Health Status: unhealthy Age Group: 6–17 years Sex: M+F Sources: https://pubmed.ncbi.nlm.nih.gov/28846022/
Somnolence	5 patients	30 mg 1 times / day steady, oral 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 Health Status: unhealthy Age Group: 6–17 years Sex: M+F Sources: https://pubmed.ncbi.nlm.nih.gov/28846022/
Upper respiratory tract infection	5 patients	30 mg 1 times / day steady, oral 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 Health Status: unhealthy Age Group: 6–17 years Sex: M+F Sources: https://pubmed.ncbi.nlm.nih.gov/28846022/
Diarrhea	6 patients	30 mg 1 times / day steady, oral 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 Health Status: unhealthy Age Group: 6–17 years Sex: M+F 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 Health Status: unhealthy 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 Health Status: unhealthy 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 Health Status: unhealthy 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 Health Status: unhealthy 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 Health Status: unhealthy 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 Health Status: unhealthy 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 Health Status: unhealthy 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 Health Status: unhealthy 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 Health Status: unhealthy 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 Health Status: unhealthy 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 Health Status: unhealthy 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 Health Status: unhealthy 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 Health Status: unhealthy 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 Health Status: unhealthy 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 Health Status: unhealthy 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 Health Status: unhealthy 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 Health Status: unhealthy 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 Health Status: unhealthy 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 Health Status: unhealthy 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 Health Status: unhealthy 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 Health Status: unhealthy 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 Health Status: unhealthy 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 Health Status: unhealthy 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 Health Status: unhealthy 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 Health Status: unhealthy 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 Health Status: unhealthy 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 Health Status: unhealthy 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 Health Status: unhealthy 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 Health Status: unhealthy 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 Health Status: unhealthy 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 Health Status: unhealthy 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 Health Status: unhealthy 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 Health Status: unhealthy 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 Health Status: unhealthy 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 Health Status: unhealthy Sources: https://clinicaltrials.gov/ct2/show/NCT02803749

Details

SMILES

InChI

DescriptionSources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2010/018731s051lbl.pdfCurator's Comment:: https://www.ncbi.nlm.nih.gov/pubmed/6151170

CNS Activity

Originator

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Conditions

Approved Use

Launch Date

Cmax

AUC

T1/2

Funbound

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AEs

Overview

OverviewOther

Drug as victim

Sourcing

PubMed

Patents

Sample Use Guides

Description
Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2010/018731s051lbl.pdf
Curator's Comment:: https://www.ncbi.nlm.nih.gov/pubmed/6151170

C_max

T_1/2

F_unbound