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Details

Stereochemistry RACEMIC
Molecular Formula C28H33ClN2
Molecular Weight 433.029
Optical Activity ( + / - )
Defined Stereocenters 0 / 1
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of BUCLIZINE

SMILES

CC(C)(C)c1ccc(cc1)CN2CCN(CC2)C(c3ccccc3)c4ccc(cc4)Cl

InChI

InChIKey=MOYGZHXDRJNJEP-UHFFFAOYSA-N
InChI=1S/C28H33ClN2/c1-28(2,3)25-13-9-22(10-14-25)21-30-17-19-31(20-18-30)27(23-7-5-4-6-8-23)24-11-15-26(29)16-12-24/h4-16,27H,17-21H2,1-3H3

HIDE SMILES / InChI

Molecular Formula C28H33ClN2
Molecular Weight 433.029
Charge 0
Count
Stereochemistry RACEMIC
Additional Stereochemistry No
Defined Stereocenters 0 / 1
E/Z Centers 0
Optical Activity ( + / - )

Description
Curator's Comment:: description was created based on several sources, including: https://www.ncbi.nlm.nih.gov/pubmed/22469258 | http://edudrugs.com/B/Bucladin-S.html

Buclizine, a piperazine derivative, is a sedating antihistamine with antimuscarinic and moderate sedative action. The drug is used mainly for its antiemetic action, particularly in the prevention of motion sickness, and in the treatment of migraine in combination with analgesics. The following side/adverse effects have been selected on the basis of their potential clinical significance: drowsiness; Incidence less frequent; blurred vision; dryness of mouth, nose, and throat; headache; nervousness, restlessness, or trouble in sleeping; upset stomach. The following drug interactions have been selected on the basis of their potential clinical significance: alcohol; anticholinergics or other medications with anticholinergic activity; apomorphine.

CNS Activity

Curator's Comment:: Buclizine is the drug of the first antihistamine generation.Firstgeneration histamine H1-receptor antagonists readily penetrate the blood brain barrier and produce histamine blockade at histamine H1-receptors in the central nervous system.

Originator

Curator's Comment:: https://www.ncbi.nlm.nih.gov/pubmed/22469258

Approval Year

TargetsConditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Preventing
BUCLADIN-S

Approved Use

For prevention and treatment of nausea, vomiting, and dizziness associated with motion sickness and vertigo (dizziness caused by other medical problems).
Preventing
BUCLADIN-S

Approved Use

For prevention and treatment of nausea, vomiting, and dizziness associated with motion sickness and vertigo (dizziness caused by other medical problems).
Palliative
Migraleve pink

Approved Use

Treating nausea and headache associated with migraine attacks that are not relieved by paracetamol, ibuprofen or aspirin alone.

Launch Date

1.43251197E12
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
0.45 μg/mL
25 mg single, oral
dose: 25 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
BUCLIZINE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
5.22 μg × h/mL
25 mg single, oral
dose: 25 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
BUCLIZINE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
5.3 h
25 mg single, oral
dose: 25 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
BUCLIZINE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
Sourcing

Sourcing

Vendor/AggregatorIDURL
PubMed

PubMed

TitleDatePubMed
Quantitation of buclizine hydrochloride in pharmaceutical formulations and human serum by RP-HPLC.
2006 Oct
Development of a list of potentially inappropriate drugs for the korean elderly using the delphi method.
2010 Dec
Simultaneous determination of gliquidone, fexofenadine, buclizine, and levocetirizine in dosage formulation and human serum by RP-HPLC.
2010 May-Jun
Patents

Sample Use Guides

50 mg thirty minutes before travel. Dose may be repeated every four to six hours as needed. Usual adult prescribing limits - up to 150 mg daily.
Route of Administration: Oral
Treatment of MCF-7 cells with different concentrations for 72 h showed that buclizine (IC50: 19.18 ± 5.32 μM) revealed considerable growth inhibition.
Substance Class Chemical
Created
by admin
on Sat Jun 26 07:59:59 UTC 2021
Edited
by admin
on Sat Jun 26 07:59:59 UTC 2021
Record UNII
0C94V6X681
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
BUCLIZINE
INN   MI   VANDF   WHO-DD  
INN  
Official Name English
BUCLIZINE [INN]
Common Name English
BUCLIZINE [MI]
Common Name English
BUCLIZINE [WHO-DD]
Common Name English
1-(P-TERT-BUTYLBENZYL)-4-(P-CHLORO-.ALPHA.-PHENYLBENZYL)PIPERAZINE
Common Name English
BUCLIZINE [VANDF]
Common Name English
Classification Tree Code System Code
WHO-ATC R06AE01
Created by admin on Sat Jun 26 08:00:00 UTC 2021 , Edited by admin on Sat Jun 26 08:00:00 UTC 2021
WHO-VATC QR06AE01
Created by admin on Sat Jun 26 08:00:00 UTC 2021 , Edited by admin on Sat Jun 26 08:00:00 UTC 2021
WHO-ATC R06AE51
Created by admin on Sat Jun 26 08:00:00 UTC 2021 , Edited by admin on Sat Jun 26 08:00:00 UTC 2021
NCI_THESAURUS C29578
Created by admin on Sat Jun 26 08:00:00 UTC 2021 , Edited by admin on Sat Jun 26 08:00:00 UTC 2021
WHO-VATC QR06AE51
Created by admin on Sat Jun 26 08:00:00 UTC 2021 , Edited by admin on Sat Jun 26 08:00:00 UTC 2021
Code System Code Type Description
ECHA (EC/EINECS)
201-448-1
Created by admin on Sat Jun 26 08:00:00 UTC 2021 , Edited by admin on Sat Jun 26 08:00:00 UTC 2021
PRIMARY
MESH
C046894
Created by admin on Sat Jun 26 08:00:00 UTC 2021 , Edited by admin on Sat Jun 26 08:00:00 UTC 2021
PRIMARY
ChEMBL
CHEMBL1201271
Created by admin on Sat Jun 26 08:00:00 UTC 2021 , Edited by admin on Sat Jun 26 08:00:00 UTC 2021
PRIMARY
EVMPD
SUB05947MIG
Created by admin on Sat Jun 26 08:00:00 UTC 2021 , Edited by admin on Sat Jun 26 08:00:00 UTC 2021
PRIMARY
RXCUI
59636
Created by admin on Sat Jun 26 08:00:00 UTC 2021 , Edited by admin on Sat Jun 26 08:00:00 UTC 2021
PRIMARY RxNorm
DRUG BANK
DB00354
Created by admin on Sat Jun 26 08:00:00 UTC 2021 , Edited by admin on Sat Jun 26 08:00:00 UTC 2021
PRIMARY
INN
291
Created by admin on Sat Jun 26 08:00:00 UTC 2021 , Edited by admin on Sat Jun 26 08:00:00 UTC 2021
PRIMARY
EPA CompTox
82-95-1
Created by admin on Sat Jun 26 08:00:00 UTC 2021 , Edited by admin on Sat Jun 26 08:00:00 UTC 2021
PRIMARY
NCI_THESAURUS
C65273
Created by admin on Sat Jun 26 08:00:00 UTC 2021 , Edited by admin on Sat Jun 26 08:00:00 UTC 2021
PRIMARY
WIKIPEDIA
BUCLIZINE
Created by admin on Sat Jun 26 08:00:00 UTC 2021 , Edited by admin on Sat Jun 26 08:00:00 UTC 2021
PRIMARY
FDA UNII
0C94V6X681
Created by admin on Sat Jun 26 08:00:00 UTC 2021 , Edited by admin on Sat Jun 26 08:00:00 UTC 2021
PRIMARY
CAS
82-95-1
Created by admin on Sat Jun 26 08:00:00 UTC 2021 , Edited by admin on Sat Jun 26 08:00:00 UTC 2021
PRIMARY
MERCK INDEX
M2744
Created by admin on Sat Jun 26 08:00:00 UTC 2021 , Edited by admin on Sat Jun 26 08:00:00 UTC 2021
PRIMARY Merck Index
DRUG CENTRAL
416
Created by admin on Sat Jun 26 08:00:00 UTC 2021 , Edited by admin on Sat Jun 26 08:00:00 UTC 2021
PRIMARY
IUPHAR
7134
Created by admin on Sat Jun 26 08:00:00 UTC 2021 , Edited by admin on Sat Jun 26 08:00:00 UTC 2021
PRIMARY
PUBCHEM
6729
Created by admin on Sat Jun 26 08:00:00 UTC 2021 , Edited by admin on Sat Jun 26 08:00:00 UTC 2021
PRIMARY
Related Record Type Details
SALT/SOLVATE -> PARENT
TARGET -> INHIBITOR
ENANTIOMER -> RACEMATE
ENANTIOMER -> RACEMATE
Related Record Type Details
ACTIVE MOIETY