Tìm theo
Cyclizine
Các tên gọi khác (10 ) :
  • (+-)-1-Diphenylmethyl-4-methylpiperazine
  • (±)-1-diphenylmethyl-4-methylpiperazine
  • (N-Benzhydryl)(n'-methyl)diethylenediamine
  • 1-(Diphenylmethyl)-4-methylpiperazine
  • 1-Benzhydryl-4-methylpiperazin
  • Ciclizina
  • Cyclizine
  • Cyclizinum
  • N-Benzhydryl-N'-methylpiperazine
  • N-methyl-N'-benzhydrylpiperazine
histamine h1 antagonists, antiemetics
Thuốc Gốc
Small Molecule
CAS: 82-92-8
ATC: R06AE03, R06AE04
CTHH: C18H22N2
PTK: 266.3807
A histamine H1 antagonist given by mouth or parenterally for the control of postoperative and drug-induced vomiting and in motion sickness. (From Martindale, The Extra Pharmacopoeia, 30th ed, p935)
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C18H22N2
Phân tử khối
266.3807
Monoisotopic mass
266.178298714
InChI
InChI=1S/C18H22N2/c1-19-12-14-20(15-13-19)18(16-8-4-2-5-9-16)17-10-6-3-7-11-17/h2-11,18H,12-15H2,1H3
InChI Key
InChIKey=UVKZSORBKUEBAZ-UHFFFAOYSA-N
IUPAC Name
1-(diphenylmethyl)-4-methylpiperazine
Traditional IUPAC Name
cyclizine
SMILES
CN1CCN(CC1)C(C1=CC=CC=C1)C1=CC=CC=C1
Độ tan chảy
105.5-107.5
Độ hòa tan
1000 mg/L (at 25 °C)
logP
3
logS
-3.5
pKa (Strongest Basic)
8.51
PSA
6.48 Å2
Refractivity
84.93 m3·mol-1
Polarizability
31.53 Å3
Rotatable Bond Count
3
H Bond Acceptor Count
2
H Bond Donor Count
0
Physiological Charge
1
Number of Rings
3
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Cyclizine is a piperazine-derivative antihistamine used as an antivertigo/antiemetic agent. Cyclizine is used in the prevention and treatment of nausea, vomiting, and dizziness associated with motion sickness. Additionally, it has been used in the management of vertigo in diseases affecting the vestibular apparatus. Although the mechanism by which cyclizine exerts its antiemetic and antivertigo effects has not been fully elucidated, its central anticholinergic properties are partially responsible. The drug depresses labyrinth excitability and vestibular stimulation, and it may affect the medullary chemoreceptor trigger zone. It also possesses anticholinergic, antihistaminic, central nervous system depressant, and local anesthetic effects.
Cơ Chế Tác Dụng : A histamine H1 antagonist given by mouth or parenterally for the control of postoperative and drug-induced vomiting and in motion sickness. (From Martindale, The Extra Pharmacopoeia, 30th ed, p935) Vomiting (emesis) is essentially a protective mechanism for removing irritant or otherwise harmful substances from the upper GI tract. Emesis or vomiting is controlled by the vomiting centre in the medulla region of the brain, an important part of which is the chemotrigger zone (CTZ). The vomiting centre possesses neurons which are rich in muscarinic cholinergic and histamine containing synapses. These types of neurons are especially involved in transmission from the vestibular apparatus to the vomiting centre. Motion sickness principally involves overstimulation of these pathways due to various sensory stimuli. Hence the action of cyclizine which acts to block the histamine receptors in the vomiting centre and thus reduce activity along these pathways. Furthermore since cyclizine possesses anti-cholinergic properties as well, the muscarinic receptors are similarly blocked.
Dược Động Học :

▧ Metabolism :
Cyclizine is metabolised to its N-demethylated derivative, norcyclizine, which has little antihistaminic (H1) activity compared to Cyclizine.
▧ Half Life :
20 hours
Chỉ Định : For prevention and treatment of nausea, vomiting, and dizziness associated with motion sickness, and vertigo (dizziness caused by other medical problems).
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, Cyclizine, 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 Cyclizine, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
  • Triprolidine Triprolidine and Cyclizine, 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 Cyclizine, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Liều Lượng & Cách Dùng : Solution - Intramuscular
Solution - Intravenous
Tablet - Oral
Dữ Kiện Thương Mại
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Bonine
  • Công ty :
    Sản phẩm biệt dược : Emoquil
  • Công ty :
    Sản phẩm biệt dược : Marezine
  • Công ty : GlaxoSmithKline
    Sản phẩm biệt dược : Marzine
  • Công ty : GlaxoSmithKline
    Sản phẩm biệt dược : Valoid
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB01176
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=6726
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46506232
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C06930
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D03621
ChemSpider
http://www.chemspider.com/Chemical-Structure.6470.html
PharmGKB
http://www.pharmgkb.org/drug/PA164742937
Wikipedia
http://en.wikipedia.org/wiki/Cyclizine
Drugs.com
http://www.drugs.com/cdi/cyclizine.html
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