Details
| Stereochemistry | RACEMIC |
| Molecular Formula | C16H19ClN2O.ClH |
| Molecular Weight | 327.249 |
| Optical Activity | ( + / - ) |
| Defined Stereocenters | 0 / 1 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
Cl.CN(C)CCOC(C1=CC=C(Cl)C=C1)C2=CC=CC=N2
InChI
InChIKey=QXDXEJNSYADHPX-UHFFFAOYSA-N
InChI=1S/C16H19ClN2O.ClH/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;1H
DescriptionCurator's Comment: description was created based on several sources, including:
https://www.drugs.com/pro/carbinoxamine.html
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.
Originator
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
Target ID: CHEMBL231 |
2.3 nM [Ki] | ||
Target ID: CHEMBL289 Sources: DOI: 10.14896/jssxmeeting.21.0.296.1 |
25.0 µM [Ki] |
Conditions
| Condition | Modality | Targets | Highest Phase | Product |
|---|---|---|---|---|
| Palliative | CARBINOXAMINE MALEATE Approved UseCarbinoxamine 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 Date2003 |
|||
| Palliative | CARBINOXAMINE MALEATE Approved UseCarbinoxamine 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 Date2003 |
|||
| Palliative | CARBINOXAMINE MALEATE Approved UseCarbinoxamine 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 Date2003 |
|||
| Palliative | CARBINOXAMINE MALEATE Approved UseCarbinoxamine 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 Date2003 |
|||
| Palliative | CARBINOXAMINE MALEATE Approved UseCarbinoxamine 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 Date2003 |
|||
| Palliative | CARBINOXAMINE MALEATE Approved UseCarbinoxamine 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 Date2003 |
|||
| Palliative | CARBINOXAMINE MALEATE Approved UseCarbinoxamine 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 Date2003 |
Cmax
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
16.9 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1363194 |
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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/7488301 |
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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/7488301 |
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
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
14.5 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1363194 |
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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/7488301 |
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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/7488301 |
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
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
31% EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/17339039 |
unknown, unknown |
CARBINOXAMINE MALEATE plasma | Homo sapiens population: UNKNOWN age: UNKNOWN sex: UNKNOWN food status: UNKNOWN |
PubMed
| Title | Date | PubMed |
|---|---|---|
| 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 |
|
| Chromatographic analysis of phenethylamine-antihistamine combinations using C8, C18 or cyano columns and micellar sodium dodecyl sulfate-pentanol mixtures. | 2001 Apr |
|
| 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 |
|
| Possible role of pseudoephedrine and other over-the-counter cold medications in the deaths of very young children. | 2007 Mar |
|
| 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
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| Code System | Code | Type | Description | ||
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6033-93-8
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VLF7M9C64J
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18913831
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DTXSID20975741
Created by
admin on Sat Dec 16 07:23:25 GMT 2023 , Edited by admin on Sat Dec 16 07:23:25 GMT 2023
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ACTIVE MOIETY
SUBSTANCE RECORD
