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Details

Stereochemistry RACEMIC
Molecular Formula C16H19ClN2O
Molecular Weight 290.7884
Optical Activity ( + / - )
Defined Stereocenters 0 / 1
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of CARBINOXAMINE

SMILES

CN(C)CCOC(c1ccc(cc1)Cl)c2ccccn2

InChI

InChIKey=OJFSXZCBGQGRNV-UHFFFAOYSA-N
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

HIDE SMILES / InChI

Molecular Formula C16H19ClN2O
Molecular Weight 290.7884
Charge 0
Count
Stereochemistry RACEMIC
Additional Stereochemistry No
Defined Stereocenters 0 / 1
E/Z Centers 0
Optical Activity ( + / - )

Description
Curator's Comment:: description was created based on several sources, including: https://www.drugs.com/pro/carbinoxamine.html

Carbinoxamine is a histamine-H1 receptor blocking agent. It is an antihistamine with anticholinergic (drying) and sedative properties. Carbinoxamine appears to compete with histamine (type H1) for receptor sites on effector cells in the gastrointestinal tract, blood vessels and respiratory tract. Carbinoxamine is effective for the symptomatic treatment of seasonal and perennial allergic rhinitis; vasomotor rhinitis; allergic conjunctivitis due to inhalant allergens and foods; mild, uncomplicated allergic skin manifestations of urticaria and angioedema; dermatographism; as therapy for anaphylactic reactions adjunctive to epinephrine and other standard measures after the acute manifestations have been controlled. Most common adverse reactions are: sedation, sleepiness, dizziness, disturbed coordination, epigastric distress, and thickening of bronchial secretions. Avoid concomitant use of alcohol and CNS depressants (hypnotics sedatives, tranquilizers, etc.) due to additive adverse effects.

Approval Year

Targets

Targets

Primary TargetPharmacologyConditionPotency
2.3 nM [Ki]
Target ID: CHEMBL289
Sources: DOI: 10.14896/jssxmeeting.21.0.296.1
25.0 µM [Ki]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Palliative
CARBINOXAMINE MALEATE

Approved Use

Carbinoxamine maleate is effective for the symptomatic treatment of: Seasonal and perennial allergic rhinitis. Vasomotor rhinitis. Allergic conjunctivitis due to inhalant allergens and foods. Mild, uncomplicated allergic skin manifestations of urticaria and angioedema. Dermatographism. As therapy for anaphylactic reactions adjunctive to epinephrine and other standard measures after the acute manifestations have been controlled. Amelioration of the severity of allergic reactions to blood or plasma.

Launch Date

1.04803199E12
Palliative
CARBINOXAMINE MALEATE

Approved Use

Carbinoxamine maleate is effective for the symptomatic treatment of: Seasonal and perennial allergic rhinitis. Vasomotor rhinitis. Allergic conjunctivitis due to inhalant allergens and foods. Mild, uncomplicated allergic skin manifestations of urticaria and angioedema. Dermatographism. As therapy for anaphylactic reactions adjunctive to epinephrine and other standard measures after the acute manifestations have been controlled. Amelioration of the severity of allergic reactions to blood or plasma.

Launch Date

1.04803199E12
Palliative
CARBINOXAMINE MALEATE

Approved Use

Carbinoxamine maleate is effective for the symptomatic treatment of: Seasonal and perennial allergic rhinitis. Vasomotor rhinitis. Allergic conjunctivitis due to inhalant allergens and foods. Mild, uncomplicated allergic skin manifestations of urticaria and angioedema. Dermatographism. As therapy for anaphylactic reactions adjunctive to epinephrine and other standard measures after the acute manifestations have been controlled. Amelioration of the severity of allergic reactions to blood or plasma.

Launch Date

1.04803199E12
Palliative
CARBINOXAMINE MALEATE

Approved Use

Carbinoxamine maleate is effective for the symptomatic treatment of: Seasonal and perennial allergic rhinitis. Vasomotor rhinitis. Allergic conjunctivitis due to inhalant allergens and foods. Mild, uncomplicated allergic skin manifestations of urticaria and angioedema. Dermatographism. As therapy for anaphylactic reactions adjunctive to epinephrine and other standard measures after the acute manifestations have been controlled. Amelioration of the severity of allergic reactions to blood or plasma.

Launch Date

1.04803199E12
Palliative
CARBINOXAMINE MALEATE

Approved Use

Carbinoxamine maleate is effective for the symptomatic treatment of: Seasonal and perennial allergic rhinitis. Vasomotor rhinitis. Allergic conjunctivitis due to inhalant allergens and foods. Mild, uncomplicated allergic skin manifestations of urticaria and angioedema. Dermatographism. As therapy for anaphylactic reactions adjunctive to epinephrine and other standard measures after the acute manifestations have been controlled. Amelioration of the severity of allergic reactions to blood or plasma.

Launch Date

1.04803199E12
Palliative
CARBINOXAMINE MALEATE

Approved Use

Carbinoxamine maleate is effective for the symptomatic treatment of: Seasonal and perennial allergic rhinitis. Vasomotor rhinitis. Allergic conjunctivitis due to inhalant allergens and foods. Mild, uncomplicated allergic skin manifestations of urticaria and angioedema. Dermatographism. As therapy for anaphylactic reactions adjunctive to epinephrine and other standard measures after the acute manifestations have been controlled. Amelioration of the severity of allergic reactions to blood or plasma.

Launch Date

1.04803199E12
Palliative
CARBINOXAMINE MALEATE

Approved Use

Carbinoxamine maleate is effective for the symptomatic treatment of: Seasonal and perennial allergic rhinitis. Vasomotor rhinitis. Allergic conjunctivitis due to inhalant allergens and foods. Mild, uncomplicated allergic skin manifestations of urticaria and angioedema. Dermatographism. As therapy for anaphylactic reactions adjunctive to epinephrine and other standard measures after the acute manifestations have been controlled. Amelioration of the severity of allergic reactions to blood or plasma.

Launch Date

1.04803199E12
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
16.9 ng/mL
8 mg single, oral
dose: 8 mg
route of administration: Oral
experiment type: SINGLE
co-administered: PHENYLPROPANOLAMINE
CARBINOXAMINE MALEATE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
13.5 ng/mL
4 mg 2 times / day multiple, oral
dose: 4 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered: PHENYLEPHRINE
CARBINOXAMINE MALEATE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
4.5 ng/mL
4 mg single, oral
dose: 4 mg
route of administration: Oral
experiment type: SINGLE
co-administered: PHENYLEPHRINE
CARBINOXAMINE MALEATE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
14.5 h
8 mg single, oral
dose: 8 mg
route of administration: Oral
experiment type: SINGLE
co-administered: PHENYLPROPANOLAMINE
CARBINOXAMINE MALEATE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
22 h
4 mg 2 times / day multiple, oral
dose: 4 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered: PHENYLEPHRINE
CARBINOXAMINE MALEATE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
30 h
4 mg single, oral
dose: 4 mg
route of administration: Oral
experiment type: SINGLE
co-administered: PHENYLEPHRINE
CARBINOXAMINE MALEATE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
Funbound

Funbound

ValueDoseCo-administeredAnalytePopulation
31%
unknown, unknown
CARBINOXAMINE MALEATE plasma
Homo sapiens
population: UNKNOWN
age: UNKNOWN
sex: UNKNOWN
food status: UNKNOWN
PubMed

PubMed

TitleDatePubMed
Clistin maleate; a clinical appraisal of a new antihistaminic.
1954 Nov
[Antimycobacterial antihistaminics].
1989 Aug
The need for rational therapeutics in the use of cough and cold medicine in infants.
1992 Apr
[Serous otitis media. Comparative study of carbinoxamine- pseudoephedrine vs astemizole-pseudoephedrine].
1997 May-Jun
Cold-syrup induced movement disorder.
2001 Jun
Simultaneous determination of ingredients in a cold medicine by cyclodextrin-modified microemulsion electrokinetic chromatography.
2005 Mar 9
Mechanism of the condensation of homocysteine thiolactone with aldehydes.
2006 Oct 25
Characterization of antihistamine-human serum protein interactions by capillary electrophoresis.
2007 Apr 20
Development of a list of potentially inappropriate drugs for the korean elderly using the delphi method.
2010 Dec
LC for analysis of two sustained-release mixtures containing cough cold suppressant drugs.
2010 Jul
4-(4-Chloro-phen-yl)-4-hy-droxy-piperidinium maleate maleic acid solvate.
2010 Jul 14
Profiling of a prescription drug library for potential renal drug-drug interactions mediated by the organic cation transporter 2.
2011 Jul 14
Patents

Sample Use Guides

Tablets: 1 or 2 tablets (4 to 8 mg) 3 to 4 times daily Oral Solution: 1 or 2 teaspoonfuls (4 to 8 mg) 3 to 4 times daily.
Route of Administration: Oral
In Vitro Use Guide
Unknown
Substance Class Chemical
Created
by admin
on Sat Jun 26 06:39:22 UTC 2021
Edited
by admin
on Sat Jun 26 06:39:22 UTC 2021
Record UNII
982A7M02H5
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
CARBINOXAMINE
INN   MI   VANDF   WHO-DD  
INN  
Official Name English
CARBINOXAMINE [MI]
Common Name English
ETHANAMINE, 2-((4-CHLOROPHENYL)-2-PYRIDINYLMETHOXY)-N,N-DIMETHYL-
Systematic Name English
CARBINOXAMINE [WHO-DD]
Common Name English
2-(P-CHLORO-.ALPHA.-(2-(DIMETHYLAMINO)ETHOXY)BENZYL)PYRIDINE
Common Name English
CARBINOXAMINE [INN]
Common Name English
CARBINOXAMINE [VANDF]
Common Name English
Classification Tree Code System Code
NCI_THESAURUS C29578
Created by admin on Sat Jun 26 06:39:22 UTC 2021 , Edited by admin on Sat Jun 26 06:39:22 UTC 2021
WHO-ATC R06AA08
Created by admin on Sat Jun 26 06:39:22 UTC 2021 , Edited by admin on Sat Jun 26 06:39:22 UTC 2021
WHO-VATC QR06AA08
Created by admin on Sat Jun 26 06:39:22 UTC 2021 , Edited by admin on Sat Jun 26 06:39:22 UTC 2021
NDF-RT N0000175587
Created by admin on Sat Jun 26 06:39:22 UTC 2021 , Edited by admin on Sat Jun 26 06:39:22 UTC 2021
LIVERTOX 149
Created by admin on Sat Jun 26 06:39:22 UTC 2021 , Edited by admin on Sat Jun 26 06:39:22 UTC 2021
Code System Code Type Description
DRUG BANK
DB00748
Created by admin on Sat Jun 26 06:39:22 UTC 2021 , Edited by admin on Sat Jun 26 06:39:22 UTC 2021
PRIMARY
EPA CompTox
486-16-8
Created by admin on Sat Jun 26 06:39:22 UTC 2021 , Edited by admin on Sat Jun 26 06:39:22 UTC 2021
PRIMARY
FDA UNII
982A7M02H5
Created by admin on Sat Jun 26 06:39:22 UTC 2021 , Edited by admin on Sat Jun 26 06:39:22 UTC 2021
PRIMARY
CAS
486-16-8
Created by admin on Sat Jun 26 06:39:22 UTC 2021 , Edited by admin on Sat Jun 26 06:39:22 UTC 2021
PRIMARY
MERCK INDEX
M3070
Created by admin on Sat Jun 26 06:39:22 UTC 2021 , Edited by admin on Sat Jun 26 06:39:22 UTC 2021
PRIMARY Merck Index
LACTMED
Carbinoxamine
Created by admin on Sat Jun 26 06:39:22 UTC 2021 , Edited by admin on Sat Jun 26 06:39:22 UTC 2021
PRIMARY
ECHA (EC/EINECS)
207-628-6
Created by admin on Sat Jun 26 06:39:22 UTC 2021 , Edited by admin on Sat Jun 26 06:39:22 UTC 2021
PRIMARY
MESH
C004649
Created by admin on Sat Jun 26 06:39:22 UTC 2021 , Edited by admin on Sat Jun 26 06:39:22 UTC 2021
PRIMARY
DRUG CENTRAL
499
Created by admin on Sat Jun 26 06:39:22 UTC 2021 , Edited by admin on Sat Jun 26 06:39:22 UTC 2021
PRIMARY
WIKIPEDIA
CARBINOXAMINE
Created by admin on Sat Jun 26 06:39:22 UTC 2021 , Edited by admin on Sat Jun 26 06:39:22 UTC 2021
PRIMARY
PUBCHEM
2564
Created by admin on Sat Jun 26 06:39:22 UTC 2021 , Edited by admin on Sat Jun 26 06:39:22 UTC 2021
PRIMARY
INN
359
Created by admin on Sat Jun 26 06:39:22 UTC 2021 , Edited by admin on Sat Jun 26 06:39:22 UTC 2021
PRIMARY
RXCUI
20220
Created by admin on Sat Jun 26 06:39:22 UTC 2021 , Edited by admin on Sat Jun 26 06:39:22 UTC 2021
PRIMARY RxNorm
ChEMBL
CHEMBL864
Created by admin on Sat Jun 26 06:39:22 UTC 2021 , Edited by admin on Sat Jun 26 06:39:22 UTC 2021
PRIMARY
IUPHAR
7139
Created by admin on Sat Jun 26 06:39:22 UTC 2021 , Edited by admin on Sat Jun 26 06:39:22 UTC 2021
PRIMARY
NCI_THESAURUS
C65286
Created by admin on Sat Jun 26 06:39:22 UTC 2021 , Edited by admin on Sat Jun 26 06:39:22 UTC 2021
PRIMARY
EVMPD
SUB06128MIG
Created by admin on Sat Jun 26 06:39:22 UTC 2021 , Edited by admin on Sat Jun 26 06:39:22 UTC 2021
PRIMARY
Related Record Type Details
SALT/SOLVATE -> PARENT
SALT/SOLVATE -> PARENT
SALT/SOLVATE -> PARENT
ENANTIOMER -> RACEMATE
ENANTIOMER -> RACEMATE
SALT/SOLVATE -> PARENT
TARGET -> INHIBITOR
Related Record Type Details
ACTIVE MOIETY