Tìm theo
Diphenhydramine
Các tên gọi khác (10 ) :
  • 2-(Benzhydryloxy)-N,N-dimethylethylamine
  • 2-diphenylmethoxy-N,N-demthylethanamine
  • alpha-(2-Dimethylaminoethoxy)diphenylmethane
  • beta-Dimethylaminoethanol diphenylmethyl ether
  • beta-Dimethylaminoethyl benzhydryl ether
  • Difenhidramina
  • Diphenhydraminum
  • N-(2-(Diphenylmethoxy)ethyl)-N,N-dimethylamine
  • O-benzhydryldimethylaminoethanol
  • β-dimethylaminoethyl benzhydryl ether
Thuốc chống dị ứng & dùng trong các trường hợp quá mẫn
Thuốc Gốc
Small Molecule
CAS: 58-73-1
ATC: D04AA32, D04AA33
ĐG : Advance Pharmaceutical
CTHH: C17H21NO
PTK: 255.3547
A histamine H1 antagonist used as an antiemetic, antitussive, for dermatoses and pruritus, for hypersensitivity reactions, as a hypnotic, an antiparkinson, and as an ingredient in common cold preparations. It has some undesired antimuscarinic and sedative effects.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C17H21NO
Phân tử khối
255.3547
Monoisotopic mass
255.162314299
InChI
InChI=1S/C17H21NO/c1-18(2)13-14-19-17(15-9-5-3-6-10-15)16-11-7-4-8-12-16/h3-12,17H,13-14H2,1-2H3
InChI Key
InChIKey=ZZVUWRFHKOJYTH-UHFFFAOYSA-N
IUPAC Name
[2-(diphenylmethoxy)ethyl]dimethylamine
Traditional IUPAC Name
diphenhydramine
SMILES
CN(C)CCOC(C1=CC=CC=C1)C1=CC=CC=C1
Độ tan chảy
161-162
Độ sôi
150-165 °C at 2.00E+00 mm Hg
Độ hòa tan
3060 mg/L (at 37 °C)
logP
3.27
logS
-3.5
pKa (Strongest Basic)
8.87
PSA
12.47 Å2
Refractivity
79.93 m3·mol-1
Polarizability
29.86 Å3
Rotatable Bond Count
6
H Bond Acceptor Count
2
H Bond Donor Count
0
Physiological Charge
1
Number of Rings
2
Bioavailability
1
Rule of Five
true
Ghose Filter
true
pKa
8.98
Dược Lực Học : Diphenhydramine is an antihistamine of the ethanolamine class. Ethanolamine antihistamines have significant antimuscarinic activity and produce marked sedation in most patients. In addition to the usual allergic symptoms, the drug also treats irritant cough and nausea, vomiting, and vertigo associated with motion sickness. It also is used commonly to treat drug-induced extrapyramidal symptoms as well as to treat mild cases of Parkinson's disease. Rather than preventing the release of histamine, as do cromolyn and nedocromil, diphenhydramine competes with free histamine for binding at HA-receptor sites. Diphenhydramine competitively antagonizes the effects of histamine on HA-receptors in the GI tract, uterus, large blood vessels, and bronchial muscle. Ethanolamine derivatives have greater anticholinergic activity than do other antihistamines, which probably accounts for the antidyskinetic action of diphenhydramine. This anticholinergic action appears to be due to a central antimuscarinic effect, which also may be responsible for its antiemetic effects, although the exact mechanism is unknown.
Cơ Chế Tác Dụng : A histamine H1 antagonist used as an antiemetic, antitussive, for dermatoses and pruritus, for hypersensitivity reactions, as a hypnotic, an antiparkinson, and as an ingredient in common cold preparations. It has some undesired antimuscarinic and sedative effects. Diphenhydramine competes with free histamine for binding at HA-receptor sites. This antagonizes the effects of histamine on HA-receptors, leading to a reduction of the negative symptoms brought on by histamine HA-receptor binding.
Dược Động Học :
▧ Absorption :
Quickly absorbed with maximum activity occurring in approximately one hour.
▧ Protein binding :
98 to 99%
▧ Metabolism :
Hepatic and renal
▧ Route of Elimination :
Little, if any, is excreted unchanged in the urine; most appears as the degradation products of metabolic transformation in the liver, which are almost completely excreted within 24 hours.
▧ Half Life :
1-4 hours
Độc Tính : LD50=500 mg/kg (orally in rats). Considerable overdosage can lead to myocardial infarction (heart attack), serious ventricular dysrhythmias, coma and death.
Chỉ Định : For the treatment of symptoms associated with Vertigo/Meniere's disease, nausea and vomiting, motion sickness and insect bite.
Tương Tác Thuốc :
  • Atomoxetine Diphenhydramine, a moderate CYP2D6 inhibitor, may increase the therapeutic and adverse effects of atomoxetine by decreasing its metabolism.
  • Donepezil Possible antagonism of action
  • Galantamine Possible antagonism of action
  • Mesoridazine Increased risk of cardiotoxicity and arrhythmias
  • Rivastigmine Possible antagonism of action
  • Tacrine The therapeutic effects of the central acetylcholinesterase inhibitor, Tacrine, and/or the anticholinergic, Diphenhydramine, 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.
  • Tamoxifen Diphenhydramine may decrease the therapeutic effect of Tamoxifen by decreasing the production of active metabolites. Consider alternate therapy.
  • Tamsulosin Diphenhydramine, a CYP2D6 inhibitor, may decrease the metabolism and clearance of Tamsulosin, a CYP2D6 substrate. Monitor for changes in therapeutic/adverse effects of Tamsulosin if Diphenhydramine is initiated, discontinued, or dose changed.
  • Thioridazine Increased risk of cardiotoxicity and arrhythmias
  • Tramadol Diphenhydramine may decrease the effect of Tramadol by decreasing active metabolite production.
  • Trimethobenzamide Trimethobenzamide and Diphenhydramine, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
  • Triprolidine Triprolidine and Diphenhydramine, 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 Diphenhydramine, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Liều Lượng & Cách Dùng : Capsule - Oral
Cream - Topical
Elixir - Oral
Liquid - Intramuscular
Liquid - Intravenous
Liquid - Oral
Lozenge - Oral
Strip - Oral
Syrup - Oral
Tablet - Oral
Tablet, chewable - Oral
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
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    Sản phẩm biệt dược : Hyrexin
  • Công ty : GlaxoSmithKline
    Sản phẩm biệt dược : Nytol Quickcaps
  • Công ty : GlaxoSmithKline
    Sản phẩm biệt dược : Nytol Quickgels
  • Công ty : Kowa Souyaku
    Sản phẩm biệt dược : Restamin
  • Công ty :
    Sản phẩm biệt dược : Siladryl
  • Công ty :
    Sản phẩm biệt dược : Silphen Cough
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB01075
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=3100
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46505484
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00300
ChemSpider
http://www.chemspider.com/Chemical-Structure.2989.html
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0121-0489-05
PharmGKB
http://www.pharmgkb.org/drug/PA449349
Wikipedia
http://en.wikipedia.org/wiki/Diphenhydramine
RxList
http://www.rxlist.com/cgi/generic/dihydram.htm
Drugs.com
http://www.drugs.com/cdi/diphenhydramine.html
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