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Details

Stereochemistry RACEMIC
Molecular Formula C28H33ClN2
Molecular Weight 433.028
Optical Activity ( + / - )
Defined Stereocenters 0 / 1
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of BUCLIZINE

SMILES

CC(C)(C)C1=CC=C(CN2CCN(CC2)C(C3=CC=CC=C3)C4=CC=C(Cl)C=C4)C=C1

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

Description

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

Originator

Approval Year

Targets

Primary TargetPharmacologyConditionPotency

Conditions

ConditionModalityTargetsHighest PhaseProduct
Preventing
BUCLADIN-S
Preventing
BUCLADIN-S
Palliative
Migraleve pink

Cmax

ValueDoseCo-administeredAnalytePopulation
0.45 μg/mL
25 mg single, oral
BUCLIZINE plasma
Homo sapiens

AUC

ValueDoseCo-administeredAnalytePopulation
5.22 μg × h/mL
25 mg single, oral
BUCLIZINE plasma
Homo sapiens

T1/2

ValueDoseCo-administeredAnalytePopulation
5.3 h
25 mg single, oral
BUCLIZINE plasma
Homo sapiens

Sourcing

PubMed

Sample Use Guides

In Vivo Use Guide
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
In Vitro Use Guide
Treatment of MCF-7 cells with different concentrations for 72 h showed that buclizine (IC50: 19.18 ± 5.32 μM) revealed considerable growth inhibition.