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QuickView for Carbinoxamine (compound)

Summary
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PubChem

PubChem Compound 2564

PubChem Compound 2564

Name:	carbinoxamine
PubChem Compound ID:	2564
Molecular formula:	C₁₆H₁₉ClN₂O
Molecular weight:	290.788 g/mol
Synonyms:	KBio1_000819; Allergefon; KBioGR_000728; BRN 0250475; Rotoxamine; Spectrum4_000264; Spectrum2_001127; Spectrum_000100; (+-)-Carbinoxamine; McN-R 73Z. show more » KBio1_000819; Allergefon; KBioGR_000728; BRN 0250475; Rotoxamine; Spectrum4_000264; Spectrum2_001127; Spectrum_000100; (+-)-Carbinoxamine; McN-R 73Z; AIDS-033080; Ethanamine, 2-((4-chlorophenyl)-2-pyridinylmethoxy)-N,N-dimethyl- (9CI); DivK1c_000819; Pyridine, 2-(p-chloro-alpha-(2-(dimethylamino)ethoxy)benzyl)-; SPBio_002582; KBio2_003088; 486-16-8; Prestwick0_000801; 3505-38-2; Prestwick1_000801; Carbinoxamina [INN-Spanish]; AIDS033080; Paracarbinoxamine; 5-21-03-00492 (Beilstein Handbook Reference); Spectrum3_000327; Carbinoxaminum [INN-Latin]; SPBio_000993; KBio2_005656; Antihistamine compound; 59811-38-0; KBio2_000520; Ethanamine, 2-[(4-chlorophenyl)-2-pyridinylmethoxy]-N,N-dimethyl-; 2-(p-Chloro-alpha-(2-(dimethylamino)ethoxy)benzyl)pyridine; NINDS_000819; {2-[(4-Chlorophenyl)-2-pyridylmethoxy]ethyl}dimethylamine; KBio3_001153; Ethanamine, 2-[(4-chlorophenyl)-2-pyridinylmethoxy]-N,N-dimethyl-, (-)-; C06871; EINECS 207-628-6; Carbinoxamine; N,N-Dimethyl-2-(p-chloro-alpha-(2-pyridyl)benzyloxy)ethylamine; KBioSS_000520 show less «

DrugBank

Identification

Name:	carbinoxamine
Name (isomeric):	DB00748
Drug Type:	small molecule
Synonyms:	Paracarinoxamine; Paracarbinoxamine; Carbinoxamine Maleate
Brand:	Allergefon, Twiston, Clistin, Rotoxamine
Category:	Antihistamines
CAS number:	486-16-8

Pharmacology

Indication:	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.
Pharmacology:	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 ... show more » 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. show less «
Mechanism of Action:	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 responsibl... show more » 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. show less «
Half Life:	10 to 20 hours
Affected organisms:	Humans and other mammals

Interactions

Drug interaction:

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.
Donepezil	Possible antagonism of action
Trimethobenzamide	Trimethobenzamide and Carbinoxamine, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
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.
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.

Targets

Histamine H1 receptor

Enzymes

Cytochrome P450 2B6

Cytochrome P450 2C19

Cytochrome P450 2C8

Cytochrome P450 2C9

Cytochrome P450 2D6

Cytochrome P450 2E1

Cytochrome P450 3A4