Details
| Stereochemistry | RACEMIC |
| Molecular Formula | C16H19ClN2O.C4H4O4 |
| Molecular Weight | 406.86 |
| Optical Activity | ( + / - ) |
| Defined Stereocenters | 0 / 1 |
| E/Z Centers | 1 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
OC(=O)\C=C\C(O)=O.CN(C)CCOC(C1=CC=C(Cl)C=C1)C2=CC=CC=N2
InChI
InChIKey=GVNWHCVWDRNXAZ-WLHGVMLRSA-N
InChI=1S/C16H19ClN2O.C4H4O4/c1-19(2)11-12-20-16(15-5-3-4-10-18-15)13-6-8-14(17)9-7-13;5-3(6)1-2-4(7)8/h3-10,16H,11-12H2,1-2H3;1-2H,(H,5,6)(H,7,8)/b;2-1+
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 |
|---|---|---|
| [Antimycobacterial antihistaminics]. | 1989 Aug |
|
| [Serous otitis media. Comparative study of carbinoxamine- pseudoephedrine vs astemizole-pseudoephedrine]. | 1997 May-Jun |
|
| Over-the-counter cold medications-postmortem findings in infants and the relationship to cause of death. | 2005 Oct |
|
| Spectrophotometric determination of carbinoxamine maleate in pharmaceutical formulations by ternary complex formation with Cu(II) and eosin. | 2006 Jun 1 |
|
| 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 |
|
| Discovery of novel and cardioselective diltiazem-like calcium channel blockers via virtual screening. | 2008 Sep 25 |
|
| 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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Common Name | English | ||
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Systematic Name | English |
| Code System | Code | Type | Description | ||
|---|---|---|---|---|---|
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6506779
Created by
admin on Sat Dec 16 01:55:57 GMT 2023 , Edited by admin on Sat Dec 16 01:55:57 GMT 2023
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1E9GVB07FW
Created by
admin on Sat Dec 16 01:55:57 GMT 2023 , Edited by admin on Sat Dec 16 01:55:57 GMT 2023
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1078492-16-6
Created by
admin on Sat Dec 16 01:55:57 GMT 2023 , Edited by admin on Sat Dec 16 01:55:57 GMT 2023
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PRIMARY |
ACTIVE MOIETY
SUBSTANCE RECORD
