Tìm theo
Bromodiphenhydramine
Các tên gọi khác (7 ) :
  • 2-(P-Bromo-alpha-phenylbenzyloxy)-N,N-dimethylethylamine
  • beta-(P-Bromobenzhydryloxy)ethyldimethylamine
  • beta-Dimethylaminoethyl P-bromobenzhydryl ether
  • Bromazina
  • Bromazine
  • Bromazinum
  • Bromodiphenhydramine
histamine antagonists
Thuốc Gốc
Small Molecule
CAS: 118-23-0
CTHH: C17H20BrNO
PTK: 334.251
Bromodiphenhydramine is an ethanolamine antihistamine with antimicrobial property. Bromodiphenhydramine is used in the control of cutaneous allergies. Ethanolamine antihistamines produce marked sedation in most patients
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C17H20BrNO
Phân tử khối
334.251
Monoisotopic mass
333.072826914
InChI
InChI=1S/C17H20BrNO/c1-19(2)12-13-20-17(14-6-4-3-5-7-14)15-8-10-16(18)11-9-15/h3-11,17H,12-13H2,1-2H3
InChI Key
InChIKey=NUNIWXHYABYXKF-UHFFFAOYSA-N
IUPAC Name
{2-[(4-bromophenyl)(phenyl)methoxy]ethyl}dimethylamine
Traditional IUPAC Name
bromodiphenhydramine
SMILES
CN(C)CCOC(C1=CC=CC=C1)C1=CC=C(Br)C=C1
Độ hòa tan
3.45e-03 g/l
logP
4
logS
-5
pKa (Strongest Basic)
8.87
PSA
12.47 Å2
Refractivity
87.55 m3·mol-1
Polarizability
33.48 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
Dược Lực Học : Bromodiphenhydramine 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, Bromodiphenhydramine competes with free histamine for binding at HA-receptor sites. Bromodiphenhydramine 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 Bromodiphenhydramine. 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 : Bromodiphenhydramine is an ethanolamine antihistamine with antimicrobial property. Bromodiphenhydramine is used in the control of cutaneous allergies. Ethanolamine antihistamines produce marked sedation in most patients Bromodiphenhydramine 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 :
Well absorbed in the digestive tract.
▧ Protein binding :
96%
▧ Metabolism :
Hepatic (cytochrome P-450 system); some renal.
▧ Half Life :
1 to 4 hours
Độc Tính : Signs of overdose include wheezing, tightness in the chest, fever, itching, bad cough, blue skin color, fits, swelling of face, lips, tongue, or throat.
Chỉ Định : For management of symptoms related to hay fever and other types of allergy and used to help bring up phlegm, thin secretions, and make a cough productive.
Tương Tác Thuốc :
  • Tacrine The therapeutic effects of the central acetylcholinesterase inhibitor, Tacrine, and/or the anticholinergic, Bromodiphenhydramine, 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 Bromodiphenhydramine, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
  • Triprolidine Triprolidine and Bromodiphenhydramine, 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 Bromodiphenhydramine, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB01237
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=2444
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46506082
ChemSpider
http://www.chemspider.com/Chemical-Structure.2350.html
PharmGKB
http://www.pharmgkb.org/drug/PA164760854
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