Tìm theo
Meclizine
Các tên gọi khác (3) :
  • Meclizine
  • Meclozine
  • Nevidoxine
Thuốc chống dị ứng
Thuốc Gốc
Small Molecule
CAS: 569-65-3
ATC: R06AE05
ĐG : Advanced Pharmaceutical Services Inc.
CTHH: C25H27ClN2
PTK: 390.948
A histamine H1 antagonist used in the treatment of motion sickness, vertigo, and nausea during pregnancy and radiation sickness. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
Phân tử khối
390.948
Monoisotopic mass
390.186276581
InChI
InChI=1S/C25H27ClN2/c1-20-6-5-7-21(18-20)19-27-14-16-28(17-15-27)25(22-8-3-2-4-9-22)23-10-12-24(26)13-11-23/h2-13,18,25H,14-17,19H2,1H3
InChI Key
InChIKey=OCJYIGYOJCODJL-UHFFFAOYSA-N
IUPAC Name
1-[(4-chlorophenyl)(phenyl)methyl]-4-[(3-methylphenyl)methyl]piperazine
Traditional IUPAC Name
meclizine
SMILES
CC1=CC(CN2CCN(CC2)C(C2=CC=CC=C2)C2=CC=C(Cl)C=C2)=CC=C1
Độ tan chảy
217-224
Độ hòa tan
0.1gm/100ml
logP
5.8
logS
-5.6
pKa (Strongest Basic)
8.16
PSA
6.48 Å2
Refractivity
119.39 m3·mol-1
Polarizability
44.87 Å3
Rotatable Bond Count
5
H Bond Acceptor Count
2
H Bond Donor Count
0
Physiological Charge
1
Number of Rings
4
Bioavailability
1
Dược Lực Học : Meclizine, a piperazine-derivative H1-receptor antagonist similar to buclizine, cyclizine, and hydroxyzine, is used as an antivertigo/antiemetic agent. Meclizine is used in the management of nausea, vomiting, and dizziness associated with motion sickness and vertigo in diseases affecting the vestibular apparatus.
Cơ Chế Tác Dụng : A histamine H1 antagonist used in the treatment of motion sickness, vertigo, and nausea during pregnancy and radiation sickness. [PubChem] Along with its actions as an antagonist at H1-receptors, meclizine also possesses anticholinergic, central nervous system depressant, and local anesthetic effects. Meclizine depresses labyrinth excitability and vestibular stimulation and may affect the medullary chemoreceptor trigger zone.
Dược Động Học :
▧ Absorption :
Well absorbed
▧ Metabolism :
Hepatic
▧ Half Life :
6 hours
Độc Tính : Symptoms of overdose include drowsiness and anticholinergic effects. LD50=mg/kg (orally in rat).
Chỉ Định : For the prevention and treatment of nausea, vomiting, or dizziness associated with motion sickness.
Tương Tác Thuốc :
  • Donepezil Possible antagonism of action
  • Galantamine Possible antagonism of action
  • Rivastigmine Possible antagonism of action
  • Tacrine The therapeutic effects of the central acetylcholinesterase inhibitor, Tacrine, and/or the anticholinergic, Meclizine, may be reduced due to antagonism. The interaction may be beneficial when the anticholinergic action is a side effect. Monitor for decreased efficacy of both agents.
  • Trimethobenzamide Trimethobenzamide and Meclizine, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
  • Triprolidine Triprolidine and Meclizine, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Additive CNS depressant effects may also occur. Monitor for enhanced anticholinergic and CNS depressant effects.
  • Trospium Trospium and Meclizine, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Liều Lượng & Cách Dùng : Tablet, chewable - Oral
Dữ Kiện Thương Mại
Giá thị trường
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