Tìm theo
Dimenhydrinate
Các tên gọi khác (12 ) :
  • (O-Benzhydryl(dimethylamino)ethanol) 8-chlorotheophyllinate
  • 8-chloro-1,3-Dimethyl-3,7-dihydro-1H-purine-2,6-dione - 2-(diphenylmethoxy)-N,N-dimethylethanamine (1:1)
  • Benzhydryl-beta-dimethylaminoethylether 8-chlorotheophylline
  • beta-Dimethylaminoethyl benzhydryl ether 1,3-dimethyl-8-chloroxanthine
  • Dimenhidrinato
  • Dimenhydrinatum
  • Diphenhydramine 8-chlorotheophyllinate
  • Diphenhydramine 8-chlorotheophylline
  • Diphenhydramine theoclate
  • Diphenhydrinate
  • N,N-Dimethyl-2-diphenylmethoxyethylamine 8-chlorotheophyllinate
  • O-Benzhydryldimethylaminoethanol 8-chlorotheophyllinate
Thuốc đường tiêu hóa
Thuốc Gốc
Small Molecule
CAS: 523-87-5
ATC: R06AA02
ĐG : APP Pharmaceuticals , http://www.apppharma.com
CTHH: C24H28ClN5O3
PTK: 469.964
Dimenhydrinate (Dramamine, Gravol and Vertirosan) is an over-the-counter drug used to prevent motion sickness. It is closely related to diphenhydramine HCl, or Benadryl. It is primarily a H1-antagonist, but also possesses an antimuscarinic effect.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C24H28ClN5O3
Phân tử khối
469.964
Monoisotopic mass
469.188067494
InChI
InChI=1S/C17H21NO.C7H7ClN4O2/c1-18(2)13-14-19-17(15-9-5-3-6-10-15)16-11-7-4-8-12-16;1-11-4-3(9-6(8)10-4)5(13)12(2)7(11)14/h3-12,17H,13-14H2,1-2H3;1-2H3,(H,9,10,13)
InChI Key
InChIKey=DKHVTDUUNTVKOW-UHFFFAOYSA-N
IUPAC Name
8-chloro-1,3-dimethyl-2,6-dioxo-2,3,6,7-tetrahydro-1H-purin-7-ide; [2-(diphenylmethoxy)ethyl]dimethylazanium
Traditional IUPAC Name
8-chloro-1,3-dimethyl-2,6-dioxo-7H-purin-7-ide; [2-(diphenylmethoxy)ethyl]dimethylazanium
SMILES
CN1C2=C([N-]C(Cl)=N2)C(=O)N(C)C1=O.C[NH+](C)CCOC(C1=CC=CC=C1)C1=CC=CC=C1
Độ tan chảy
102.5-104
Độ hòa tan
3000 mg/L
logP
-0.39
logS
-5.6
pKa (Strongest Basic)
8.87
PSA
13.67 Å2
Refractivity
90.94 m3·mol-1
Polarizability
30.28 Å3
Rotatable Bond Count
6
H Bond Acceptor Count
1
H Bond Donor Count
1
Physiological Charge
1
Number of Rings
4
Bioavailability
1
Rule of Five
true
Ghose Filter
true
MDDR-Like Rule
true
Dược Lực Học : Dimenhydrinate is an antiemetics drug combination that contains diphenhydramine and theophylline. It is not effective in the treatment of nausea associated with cancer chemotherapy. Dimenhydrinate directly inhibits the stimulation of certain nerves in the brain and inner ear to suppress nausea, vomiting, dizziness, and vertigo. Diphenhydramine and dimenhydinate both reduce vestibular neuronal excitation due to angular or linear acceleration motions.
Cơ Chế Tác Dụng : Dimenhydrinate (Dramamine, Gravol and Vertirosan) is an over-the-counter drug used to prevent motion sickness. It is closely related to diphenhydramine HCl, or Benadryl. It is primarily a H1-antagonist, but also possesses an antimuscarinic effect. The mechanism by which some antihistamines exert their antiemetic, anti–motion sickness, and antivertigo effects is not precisely known but may be related to their central anticholinergic actions. They diminish vestibular stimulation and depress labyrinthine function. An action on the medullary chemoreceptive trigger zone may also be involved in the antiemetic effect. Dimenhydrinate is a competitive antagonist at the histamine H1 receptor, which is widely distributed in the human brain. Dimenhydrinate's anti-emetic effect is probably due to H1 antagonism in the vestibular system in the brain.
Dược Động Học :
▧ Absorption :
Well absorbed after oral administration.
▧ Protein binding :
98 to 99%.
▧ Metabolism :
Hepatic (cytochrome P-450 system).
▧ Half Life :
1 to 4 hours
Độc Tính : Symptoms of overdose include delerium, hallucinations, and excitment. Patients may be violent and confused.
Chỉ Định : Used for treating vertigo, motion sickness, and nausea associated with pregnancy.
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, Dimenhydrinate, 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 Dimenhydrinate, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
  • Triprolidine Triprolidine and Dimenhydrinate, 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 Dimenhydrinate, 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
Liquid - Intravenous
Liquid - Oral
Solution - Intramuscular
Solution - Intravenous
Suppository - Rectal
Syrup - Oral
Tablet - Oral
Tablet, multilayer - Oral
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty : Johnson
    Sản phẩm biệt dược : Dramamine
  • Công ty : YSP
    Sản phẩm biệt dược : Driminate
  • Công ty : Church & Dwight
    Sản phẩm biệt dược : Gravol
  • Công ty : Astellas
    Sản phẩm biệt dược : Vertirosan
  • Công ty : Astellas
    Sản phẩm biệt dược : Vomex A
  • Công ty : Adilna
    Sản phẩm biệt dược : Xamamina
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00985
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=441281
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46504881
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00520
ChemSpider
http://www.chemspider.com/Chemical-Structure.390044.html
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0409-0468-05
PharmGKB
http://www.pharmgkb.org/drug/PA449338
Wikipedia
http://en.wikipedia.org/wiki/Dimenhydrinate
Drugs.com
http://www.drugs.com/cdi/dimenhydrinate.html
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