carbinoxamine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
antihistaminics	499	486-16-8

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: carbinoxamine tannate carbinoxamine carbinoxamine maleate paracarinoxamine paracarbinoxamine carbinoxamine diphenyldisulfonate	antihistamine with anticholinergic and sedative properties Molecular weight: 290.79 Formula: C16H19ClN2O CLOGP: 2.67 LIPINSKI: 0 HAC: 3 HDO: 0 TPSA: 25.36 ALOGS: -3.11 ROTB: 6 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

carbinoxamine tannate
carbinoxamine
carbinoxamine maleate
paracarinoxamine
paracarbinoxamine
carbinoxamine diphenyldisulfonate

antihistamine with anticholinergic and sedative properties

Molecular weight: 290.79
Formula: C16H19ClN2O
CLOGP: 2.67
LIPINSKI: 0
HAC: 3
HDO: 0
TPSA: 25.36
ALOGS: -3.11
ROTB: 6

Status: OFP

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

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
FDA EPC	N0000175587	Histamine-1 Receptor Antagonist
MeSH PA	D018494	Histamine Agents
MeSH PA	D006633	Histamine Antagonists
MeSH PA	D006634	Histamine H1 Antagonists
MeSH PA	D018377	Neurotransmitter Agents
CHEBI has role	CHEBI:37955	H1 receptor antagonists
CHEBI has role	CHEBI:48407	antiparkinson agent
CHEBI has role	CHEBI:48876	muscarinic antagonists
CHEBI has role	CHEBI:50857	anti-allergic 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	P35367	HRH1_HUMAN	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
DB00748	DRUGBANK_ID
CHEMBL1200974	ChEMBL_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

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
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	26 sections
KarbinalER	HUMAN PRESCRIPTION DRUG LABEL	1	23594-101	SUSPENSION, EXTENDED RELEASE	4 mg	ORAL	NDA	26 sections
Carbinoxamine Maleate	HUMAN PRESCRIPTION DRUG LABEL	1	44523-825	TABLET	4 mg	ORAL	ANDA	22 sections
Carbinoxamine Maleate	HUMAN PRESCRIPTION DRUG LABEL	1	51991-333	TABLET	4 mg	ORAL	ANDA	23 sections
Carbinoxamine Maleate	HUMAN PRESCRIPTION DRUG LABEL	1	51991-333	TABLET	4 mg	ORAL	ANDA	23 sections
Carbinoxamine Maleate	HUMAN PRESCRIPTION DRUG LABEL	1	51991-334	SYRUP	4 mg	ORAL	ANDA	23 sections
Carbinoxamine Maleate	HUMAN PRESCRIPTION DRUG LABEL	1	51991-334	SYRUP	4 mg	ORAL	ANDA	23 sections
Carbinoxamine Maleate	HUMAN PRESCRIPTION DRUG LABEL	1	64950-211	TABLET	4 mg	ORAL	ANDA	22 sections
CARBINOXZAMINE 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	69067-240	TABLET	6 mg	ORAL	ANDA	24 sections