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carbinoxamine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| antihistaminics | 499 | 486-16-8 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
antihistamine with anticholinergic and sedative properties
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 16 | mg | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 1 | Hosey CM, Chan R, Benet LZ |
| S (Water solubility) | 81 mg/mL | Bocci G, Oprea TI, Benet LZ |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| kinase-safety-class | ACVR2B,AKT1,AKT2,AKT3,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK4,CDK5,CDK9,DDR1,DYRK1B,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,ITK,JAK2,JAK3,MAP3K21,MAP3K7,MAPK10,MAPK12,MAPK7,MET,NTRK2,PDK2,PDK4,PDPK1,PIK3CB,PIM2,PRKDC,SIK2,SIK3,STK33,TEK,TTK | 40 | |||
| kinase-selectivity-class | AKT3,AXL,EIF2AK3,ERBB2,PDK4 | 5 | |||
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Dec. 27, 1974 | FDA | MCNEIL |
FDA Adverse Event Reporting System (Female)
None
FDA Adverse Event Reporting System (Male)
None
FDA Adverse Event Reporting System (Geriatric)
None
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | R06AA08 | RESPIRATORY SYSTEM ANTIHISTAMINES FOR SYSTEMIC USE ANTIHISTAMINES FOR SYSTEMIC USE Aminoalkyl ethers |
| FDA MoA | N0000000190 | Histamine H1 Receptor Antagonists |
| MeSH PA | D006633 | Histamine Antagonists |
| MeSH PA | D006634 | Histamine H1 Antagonists |
| MeSH PA | D018377 | Neurotransmitter Agents |
| MeSH PA | D018494 | Histamine Agents |
| CHEBI has role | CHEBI:37955 | H<small><sub>1</sub></small>-receptor antagonist |
| CHEBI has role | CHEBI:48407 | antiparkinson drug |
| CHEBI has role | CHEBI:48876 | muscarinic antagonist |
| CHEBI has role | CHEBI:50857 | anti-allergic agent |
| FDA EPC | N0000175587 | Histamine-1 Receptor Antagonist |
| CHEBI has role | CHEBI:66981 | ophthalmology drug |
Related Drugs by ATC class:
R06AA Aminoalkyl ethers 8 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Dermatographic urticaria | indication | 7632005 | DOID:743 |
| Vasomotor rhinitis | indication | 8229003 | DOID:4730 |
| Allergic rhinitis | indication | 61582004 | |
| Nasal discharge | indication | 64531003 | |
| Common cold | indication | 82272006 | DOID:10459 |
| Urticaria | indication | 126485001 | |
| Seasonal allergic rhinitis | indication | 367498001 | |
| Itching of skin | indication | 418363000 | |
| Allergic conjunctivitis | indication | 473460002 | DOID:11204 |
| Brain damage | contraindication | 2470005 | |
| Ocular hypertension | contraindication | 4210003 | DOID:9282 |
| Tachyarrhythmia | contraindication | 6285003 | |
| Suicidal thoughts | contraindication | 6471006 | |
| Dependent drug abuse | contraindication | 6525002 | |
| Urinary tract obstruction | contraindication | 7163005 | DOID:5200 |
| Alcohol withdrawal delirium | contraindication | 8635005 | |
| Peptic ulcer | contraindication | 13200003 | DOID:750 |
| Asthenia | contraindication | 13791008 | |
| Severe chronic ulcerative colitis | contraindication | 14311001 | |
| Constipation | contraindication | 14760008 | DOID:2089 |
| Mood swings | contraindication | 18963009 | |
| Myocardial infarction | contraindication | 22298006 | DOID:5844 |
| Inflammatory bowel disease | contraindication | 24526004 | DOID:0050589 |
| Ventricular tachycardia | contraindication | 25569003 | |
| Alcohol intoxication | contraindication | 25702006 | |
| Shock | contraindication | 27942005 | |
| Toxic megacolon | contraindication | 28536002 | DOID:1770 |
| Atony of colon | contraindication | 29479008 | |
| Hypercapnia | contraindication | 29596007 | |
| Dehydration | contraindication | 34095006 | |
| Hyperthyroidism | contraindication | 34486009 | DOID:7998 |
| Acute hepatitis | contraindication | 37871000 | |
| Hypertensive disorder | contraindication | 38341003 | DOID:10763 |
| Disorder of gallbladder | contraindication | 39621005 | DOID:0060262 |
| Hypothyroidism | contraindication | 40930008 | DOID:1459 |
| Complete trisomy 21 syndrome | contraindication | 41040004 | DOID:14250 |
| Conduction disorder of the heart | contraindication | 44808001 | |
| Low blood pressure | contraindication | 45007003 | |
| Achalasia of esophagus | contraindication | 45564002 | DOID:9164 |
| Chronic heart failure | contraindication | 48447003 | |
| Bradycardia | contraindication | 48867003 | |
| Disorder of cardiovascular system | contraindication | 49601007 | DOID:1287 |
| Acidosis | contraindication | 51387008 | |
| Coronary arteriosclerosis | contraindication | 53741008 | DOID:3393 |
| Paralytic ileus | contraindication | 55525008 | DOID:8442 |
| Peptic reflux disease | contraindication | 57643001 | |
| Ulcerative colitis | contraindication | 64766004 | DOID:8577 |
| Arterial thrombosis | contraindication | 65198009 | |
| Drug AND/OR toxin-induced diarrhea | contraindication | 65979008 | |
| Substance abuse | contraindication | 66214007 | |
| Benign intracranial hypertension | contraindication | 68267002 | DOID:11459 |
| Arteriosclerotic vascular disease | contraindication | 72092001 | |
| Diabetes mellitus | contraindication | 73211009 | DOID:9351 |
| Urethral stricture | contraindication | 76618002 | |
| Spastic paralysis | contraindication | 78403003 | |
| Disturbance of salivary secretion | contraindication | 78948009 | |
| Decreased respiratory function | contraindication | 80954004 | |
| Injury of head | contraindication | 82271004 | |
| Chronic idiopathic constipation | contraindication | 82934008 | |
| Cor pulmonale | contraindication | 83291003 | DOID:8515 |
| Hiatal hernia | contraindication | 84089009 | DOID:12642 |
| Pulmonary emphysema | contraindication | 87433001 | |
| Kidney disease | contraindication | 90708001 | DOID:557 |
| Myasthenia gravis | contraindication | 91637004 | DOID:437 |
| Acute abdominal pain | contraindication | 116290004 | |
| Gastrointestinal obstruction | contraindication | 126765001 | |
| Neoplasm of brain | contraindication | 126952004 | DOID:1319 |
| Seizure disorder | contraindication | 128613002 | |
| Autonomic dysreflexia | contraindication | 129618003 | |
| Bleeding | contraindication | 131148009 | |
| Drug-induced psychosis | contraindication | 191483003 | DOID:1742 |
| Partial atrioventricular block | contraindication | 195039008 | |
| Acute pancreatitis | contraindication | 197456007 | DOID:2913 |
| Myocardial dysfunction | contraindication | 233928007 | |
| Disease of liver | contraindication | 235856003 | DOID:409 |
| Bladder outflow obstruction | contraindication | 236645006 | |
| Morbid obesity | contraindication | 238136002 | DOID:11981 |
| Pyloric obstruction | contraindication | 244815007 | |
| Benign prostatic hyperplasia | contraindication | 266569009 | |
| Retention of urine | contraindication | 267064002 | |
| Drowsy | contraindication | 271782001 | |
| Exacerbation of asthma | contraindication | 281239006 | |
| Lesion of brain | contraindication | 301766008 | |
| Coma | contraindication | 371632003 | |
| Primary adrenocortical insufficiency | contraindication | 373662000 | |
| Operation on gastrointestinal tract | contraindication | 386621005 | |
| Hypoxia | contraindication | 389086002 | |
| Angle-closure glaucoma | contraindication | 392291006 | DOID:13550 |
| Gastric ulcer | contraindication | 397825006 | DOID:10808 |
| Breastfeeding (mother) | contraindication | 413712001 | |
| Chronic lung disease | contraindication | 413839001 | |
| Disorder of coronary artery | contraindication | 414024009 | |
| Central nervous system depression | contraindication | 418072004 | |
| Dysfunction of sphincter of Oddi | contraindication | 430887001 | |
| Hypertensive urgency | contraindication | 443482000 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 8.79 | Basic |
| pKa2 | 4.21 | Basic |
Orange Book patent data (new drug applications)
None
Orange Book exclusivity data (new drug applications)
None
Bioactivity Summary:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| Histamine H1 receptor | GPCR | ANTAGONIST | CHEMBL | CHEMBL |
External reference:
| ID | Source |
|---|---|
| D01336 | KEGG_DRUG |
| 3505-38-2 | SECONDARY_CAS_RN |
| 20220 | RXNORM |
| C0054672 | UMLSCUI |
| CHEBI:3398 | CHEBI |
| CHEMBL864 | ChEMBL_ID |
| CHEMBL1200974 | ChEMBL_ID |
| DB00748 | DRUGBANK_ID |
| C004649 | MESH_SUPPLEMENTAL_RECORD_UI |
| 2564 | PUBCHEM_CID |
| 7139 | IUPHAR_LIGAND_ID |
| 359 | INN_ID |
| 982A7M02H5 | UNII |
| 17660 | MMSL |
| 4356 | MMSL |
| 72187 | MMSL |
| 74825 | MMSL |
| d03569 | MMSL |
| 19499001 | SNOMEDCT_US |
| 372896001 | SNOMEDCT_US |
| 90882008 | SNOMEDCT_US |
| 4018478 | VANDF |
| 4019656 | VANDF |
| 003239 | NDDF |
| 003373 | NDDF |
| 004790 | NDDF |
| 982A7M02H5 | INXIGHT DRUGS |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| RyVent | HUMAN PRESCRIPTION DRUG LABEL | 1 | 15370-130 | TABLET | 6 mg | ORAL | ANDA | 21 sections |
| KarbinalER | HUMAN PRESCRIPTION DRUG LABEL | 1 | 23594-101 | SUSPENSION, EXTENDED RELEASE | 4 mg | ORAL | NDA | 25 sections |
| Carbinoxamine Maleate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 44523-825 | TABLET | 4 mg | ORAL | ANDA | 22 sections |
| Carbinoxamine Maleate Extended-Release Oral Suspension | HUMAN PRESCRIPTION DRUG LABEL | 1 | 62542-101 | SUSPENSION, EXTENDED RELEASE | 4 mg | ORAL | NDA authorized generic | 18 sections |
| Carbinoxamine Maleate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 64950-211 | TABLET | 4 mg | ORAL | ANDA | 22 sections |
| Carbinoxamine Maleate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 64950-243 | SOLUTION | 4 mg | ORAL | ANDA | 22 sections |
| Carbinoxamine Maleate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 69067-240 | TABLET | 6 mg | ORAL | ANDA | 24 sections |
| CARBINOXAMINE MALEATE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 69315-239 | TABLET | 6 mg | ORAL | ANDA | 21 sections |
| CARBZAH | HUMAN PRESCRIPTION DRUG LABEL | 1 | 71085-080 | SOLUTION | 4 mg | ORAL | ANDA | 22 sections |
| Carbinoxamine Maleate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 73684-110 | TABLET | 6 mg | ORAL | ANDA | 24 sections |
| Carbinoxamine Maleate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 80705-120 | TABLET | 6 mg | ORAL | ANDA | 24 sections |