Tìm theo
Hydroxyzine
Các tên gọi khác (10 ) :
  • Hidroxizina
  • Hychotine
  • Hydroksyzyny
  • Hydroxine
  • Hydroxizine
  • Hydroxizinum
  • Hydroxycine
  • Hydroxyzin
  • Hydroxyzine
  • Hydroxyzinum
Thuốc điều trị về tâm thần
Thuốc Gốc
Small Molecule
CAS: 68-88-2
ATC: N05BB01
ĐG : Advanced Pharmaceutical Services Inc.
CTHH: C21H27ClN2O2
PTK: 374.904
A histamine H1 receptor antagonist that is effective in the treatment of chronic urticaria, dermatitis, and histamine-mediated pruritus. Unlike its major metabolite cetirizine, it does cause drowsiness. It is also effective as an antiemetic, for relief of anxiety and tension, and as a sedative. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C21H27ClN2O2
Phân tử khối
374.904
Monoisotopic mass
374.176105825
InChI
InChI=1S/C21H27ClN2O2/c22-20-8-6-19(7-9-20)21(18-4-2-1-3-5-18)24-12-10-23(11-13-24)14-16-26-17-15-25/h1-9,21,25H,10-17H2
InChI Key
InChIKey=ZQDWXGKKHFNSQK-UHFFFAOYSA-N
IUPAC Name
2-(2-{4-[(4-chlorophenyl)(phenyl)methyl]piperazin-1-yl}ethoxy)ethan-1-ol
Traditional IUPAC Name
hydroxyzine
SMILES
OCCOCCN1CCN(CC1)C(C1=CC=CC=C1)C1=CC=C(Cl)C=C1
Độ tan chảy
193 °C
Độ hòa tan
< 700 mg/mL
logP
2.7
logS
-3.6
pKa (strongest acidic)
15.12
pKa (Strongest Basic)
7.82
PSA
35.94 Å2
Refractivity
107.07 m3·mol-1
Polarizability
41.99 Å3
Rotatable Bond Count
8
H Bond Acceptor Count
4
H Bond Donor Count
1
Physiological Charge
1
Number of Rings
3
Bioavailability
1
Rule of Five
true
Ghose Filter
true
MDDR-Like Rule
true
Dược Lực Học : Hydroxyzine, a piperazine antihistamine structurally related to buclizine, cyclizine, and meclizine, is used to treat histamine-mediated pruritus or pruritus due to allergy, nausea and vomiting, and, in combination with an opiate agonist, anxiolytic pain. Hydroxyzine is also used as a perioperative sedative and anxiolytic and to manage acute alcohol withdrawal. Hydroxyzine's active metabolite, cetirizine, is also used as an H1-antagonist.
Cơ Chế Tác Dụng : A histamine H1 receptor antagonist that is effective in the treatment of chronic urticaria, dermatitis, and histamine-mediated pruritus. Unlike its major metabolite cetirizine, it does cause drowsiness. It is also effective as an antiemetic, for relief of anxiety and tension, and as a sedative. [PubChem] Hydroxyzine competes with histamine for binding at H1-receptor sites on the effector cell surface, resulting in suppression of histaminic edema, flare, and pruritus. The sedative properties of hydroxyzine occur at the subcortical level of the CNS. Secondary to its central anticholinergic actions, hydroxyzine may be effective as an antiemetic.
Dược Động Học :
▧ Absorption :
Rapidly absorbed from the gastrointestinal tract
▧ Protein binding :
93%
▧ Metabolism :
Hepatic
▧ Half Life :
20 to 25 hours
Độc Tính : Oral, rat LD50: 950 mg/kg. Symptoms of overexposure include hypersedation.
Chỉ Định : For symptomatic relief of anxiety and tension associated with psychoneurosis and as an adjunct in organic disease states in which anxiety is manifested. Useful in the management of pruritus due to allergic conditions such as chronic urticaria.
Tương Tác Thuốc :
  • Butabarbital Hydroxyzine may enhance the CNS depressant effect of barbiturates like butabarbital. Consider a decrease in the barbiturate dose, as appropriate, when used together with hydroxyzine. With concurrent use, monitor patients closely for excessive response to the combination.
  • Butalbital Hydroxyzine may enhance the CNS depressant effect of barbiturates such as butalbital. Consider a decrease in the barbiturate dose, as appropriate, when used together with hydroxyzine. With concurrent use, monitor patients closely for excessive response to the combination.
  • Dihydrocodeine May enhance CNS depressant effects of CNS depressants. It is recommended to monitor therapy.
  • 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, Hydroxyzine, 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 Hydroxyzine, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
  • Triprolidine Triprolidine and Hydroxyzine, 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 Hydroxyzine, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Liều Lượng & Cách Dùng : Capsule - Oral
Liquid - Intramuscular
Syrup - Oral
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty : UCB
    Sản phẩm biệt dược : Atarax
  • Công ty : Hyrex
    Sản phẩm biệt dược : Hyzine
  • Công ty : Pfizer
    Sản phẩm biệt dược : Masmoran
  • Công ty :
    Sản phẩm biệt dược : Rezine
  • Công ty :
    Sản phẩm biệt dược : Vistaject-50
  • Công ty : Prizer
    Sản phẩm biệt dược : Vistaril
  • Công ty :
    Sản phẩm biệt dược : Vistazine
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00557
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=3658
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46508556
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C07045
ChemSpider
http://www.chemspider.com/Chemical-Structure.3531.html
BindingDB
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=22875
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0049-5460-74
PharmGKB
http://www.pharmgkb.org/drug/PA449943
Wikipedia
http://en.wikipedia.org/wiki/Hydroxyzine
RxList
http://www.rxlist.com/cgi/generic/hydrox.htm
PDRhealth
http://www.pdrhealth.com/drug_info/rxdrugprofiles/drugs/ata1035.shtml
Drugs.com
http://www.drugs.com/hydroxyzine.html
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