Tìm theo
Carbinoxamine
Các tên gọi khác (9 ) :
  • (+-)-Carbinoxamine
  • {2-[(4-chloro-phenyl)-pyridin-2-yl-methoxy]-ethyl}-dimethyl-amine
  • 2-(P-chloro-alpha-(2-(dimethylamino)Ethoxy)benzyl)pyridine
  • Carbinoxamin
  • Carbinoxamina
  • Carbinoxamine
  • Carbinoxamine base
  • Carbinoxaminum
  • Paracarbinoxamine
histamine h1 antagonists, histamine antagonists
Thuốc Gốc
Small Molecule
CAS: 486-16-8
ATC: R06AA08
ĐG : Boca Pharmacal , http://www.bocapharmacal.com
CTHH: C16H19ClN2O
PTK: 290.788
Carbinoxamine is a first generation antihistamine that 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. The product label for carbinoxamine as an over the counter cough and cold medicine is being modified to state "do not use" in children under 4 years of age in order to prevent and reduce misuse, as many unapproved carbinoxamine-containing preparations contained inappropriate labeling, which promoted unapproved uses (including management of congestion, cough, the common cold, and the use in children under 2 years of age), which can potentially cause serious health risks.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C16H19ClN2O
Phân tử khối
290.788
Monoisotopic mass
290.118590947
InChI
InChI=1S/C16H19ClN2O/c1-19(2)11-12-20-16(15-5-3-4-10-18-15)13-6-8-14(17)9-7-13/h3-10,16H,11-12H2,1-2H3
InChI Key
InChIKey=OJFSXZCBGQGRNV-UHFFFAOYSA-N
IUPAC Name
{2-[(4-chlorophenyl)(pyridin-2-yl)methoxy]ethyl}dimethylamine
Traditional IUPAC Name
(+-)-carbinoxamine
SMILES
CN(C)CCOC(C1=CC=C(Cl)C=C1)C1=CC=CC=N1
Độ tan chảy
< 25 °C
Độ sôi
160 °C at 1.00E-01 mm Hg
Độ hòa tan
2.28e-01 g/l
logP
2.6
logS
-3.1
pKa (Strongest Basic)
8.87
PSA
25.36 Å2
Refractivity
82.13 m3·mol-1
Polarizability
31.7 Å3
Rotatable Bond Count
6
H Bond Acceptor Count
3
H Bond Donor Count
0
Physiological Charge
1
Number of Rings
2
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Carbinoxamine is a first generation 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, carbinoxamine competes with free histamine for binding at HA-receptor sites. Carbinoxamine 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 carbinoxamine.
Cơ Chế Tác Dụng : Carbinoxamine is a first generation antihistamine that 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. The product label for carbinoxamine as an over the counter cough and cold medicine is being modified to state "do not use" in children under 4 years of age in order to prevent and reduce misuse, as many unapproved carbinoxamine-containing preparations contained inappropriate labeling, which promoted unapproved uses (including management of congestion, cough, the common cold, and the use in children under 2 years of age), which can potentially cause serious health risks. Carbinoxamine 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. Carbinoxamine's 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.
Dược Động Học :

▧ Half Life :
10 to 20 hours
Chỉ Định : For symptomatic relief of seasonal and perennial allergic rhinitis and vasomotor rhinitis, as well as allergic conjunctivitis caused by foods and inhaled allergens. Also for the relief of allergic reactions to blood or plasma, and the symptomatic management of mild, uncomplicated allergic skin manifestations of urticaria and angioedema.
Tương Tác Thuốc :
  • Benzylpenicilloyl Polylysine Antihistamines may diminish the diagnostic effect of Benzylpenicilloyl Polylysine. Treatment with systemic histamine H1 antagonists such as carbinoxamine should be suspended for benzylpenicilloyl-polylysine skin testing to minimize the potential for false negative results. Delay skin testing until the systemic effects of the antihistamine have dissipated. A histamine skin test may be used to assess residual antihistaminic effects.
  • Donepezil Possible antagonism of action
  • Galantamine Possible antagonism of action
  • Pramlintide Pramlintide may enhance the anticholinergic effect of Anticholinergics such as carbinoxamine. These effects are specific to the gastrointestinal tract. Use caution during concomitant therapy with pramlintide and anticholinergics. Additive effects on reduced gastrointestinal motility may occur.
  • Tacrine The therapeutic effects of the central acetylcholinesterase inhibitor, Tacrine, and/or the anticholinergic, Carbinoxamine, 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 Carbinoxamine, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
  • Triprolidine Triprolidine and Carbinoxamine, 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 Carbinoxamine, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Liều Lượng & Cách Dùng : Solution / drops - Oral
Syrup - Oral
Tablet - Oral
Tablet, extended release - Oral
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty : SERP
    Sản phẩm biệt dược : Allergefon
  • Công ty :
    Sản phẩm biệt dược : Arbinoxa
  • Công ty :
    Sản phẩm biệt dược : Clistin
  • Công ty : Kenyaku
    Sản phẩm biệt dược : Histin
  • Công ty :
    Sản phẩm biệt dược : Karbinal
  • Công ty :
    Sản phẩm biệt dược : Palgic
  • Công ty :
    Sản phẩm biệt dược : Rotoxamine
  • Công ty : Shou Chan
    Sản phẩm biệt dược : Satinmin
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00748
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=2564
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46506787
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C06871
ChemSpider
http://www.chemspider.com/Chemical-Structure.2466.html
BindingDB
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=50240487
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0525-6748-01
PharmGKB
http://www.pharmgkb.org/drug/PA164746898
Wikipedia
http://en.wikipedia.org/wiki/Carbinoxamine
RxList
http://www.rxlist.com/cgi/generic3/rondecsyr.htm
Drugs.com
http://www.drugs.com/cdi/carbinoxamine-maleate.html
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