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

Stem definition	Drug id	CAS RN
	2763	486-12-4

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: actidil triprolidine triprolidin tripyrolidine triprolidine hydrochloride triprolidine HCl	Histamine H1 antagonist used in allergic rhinitis; ASTHMA; and URTICARIA. It is a component of COUGH and COLD medicines. It may cause drowsiness. Molecular weight: 278.40 Formula: C19H22N2 CLOGP: 3.63 LIPINSKI: 0 HAC: 2 HDO: 0 TPSA: 16.13 ALOGS: -3.72 ROTB: 4 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

actidil
triprolidine
triprolidin
tripyrolidine
triprolidine hydrochloride
triprolidine HCl

Histamine H1 antagonist used in allergic rhinitis; ASTHMA; and URTICARIA. It is a component of COUGH and COLD medicines. It may cause drowsiness.

Molecular weight: 278.40
Formula: C19H22N2
CLOGP: 3.63
LIPINSKI: 0
HAC: 2
HDO: 0
TPSA: 16.13
ALOGS: -3.72
ROTB: 4

Status: OFP

Legend:
OFP - off patent
OFM - off market
ONP - on patent

Drug dosage:

Dose	Unit	Route
7.50	mg	O

ADMET properties:

Property	Value	Reference
BA (Bioavailability)	4 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H

Approvals:

Date	Agency	Company	Orphan
May 17, 1983	FDA	SANDOZ

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	R06AX07	RESPIRATORY SYSTEM ANTIHISTAMINES FOR SYSTEMIC USE ANTIHISTAMINES FOR SYSTEMIC USE Other antihistamines for systemic use
MeSH PA	D018926	Anti-Allergic Agents
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

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
Ocular hypertension	contraindication	4210003	DOID:9282
Dependent drug abuse	contraindication	6525002
Peptic ulcer	contraindication	13200003	DOID:750
Asthenia	contraindication	13791008
Chronic disease of respiratory system	contraindication	17097001
Mood swings	contraindication	18963009
Myocardial infarction	contraindication	22298006	DOID:5844
Inflammatory bowel disease	contraindication	24526004	DOID:0050589
Ventricular tachycardia	contraindication	25569003
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
Conduction disorder of the heart	contraindication	44808001
Low blood pressure	contraindication	45007003
Chronic heart failure	contraindication	48447003
Bradycardia	contraindication	48867003
Acidosis	contraindication	51387008
Coronary arteriosclerosis	contraindication	53741008	DOID:3393
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
Decreased respiratory function	contraindication	80954004
Injury of head	contraindication	82271004
Chronic idiopathic constipation	contraindication	82934008
Epilepsy	contraindication	84757009	DOID:1826
Kidney disease	contraindication	90708001	DOID:557
Acute abdominal pain	contraindication	116290004
Procedure on urinary system	contraindication	118677009
Partial atrioventricular block	contraindication	195039008
Acute pancreatitis	contraindication	197456007	DOID:2913
Disease of liver	contraindication	235856003	DOID:409
Bladder outflow obstruction	contraindication	236645006
Benign prostatic hyperplasia	contraindication	266569009
Retention of urine	contraindication	267064002
Lesion of brain	contraindication	301766008
Primary adrenocortical insufficiency	contraindication	373662000
Operation on gastrointestinal tract	contraindication	386621005
Hypoxia	contraindication	389086002
Angle-closure glaucoma	contraindication	392291006	DOID:13550
Pseudomembranous enterocolitis	contraindication	397683000
Disorder of coronary artery	contraindication	414024009
Central nervous system depression	contraindication	418072004
Ultrarapid metabolizer due to cytochrome p450 CYP2D6 variant	contraindication	422681000
Dysfunction of sphincter of Oddi	contraindication	430887001
Hypertensive urgency	contraindication	443482000
Acute exacerbation of asthma	contraindication	708038006

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	9.42	Basic
pKa2	3.34	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	Ki	9.90		CHEMBL	CHEMBL
Histamine H1 receptor	GPCR		HRH1_CAVPO		Kd	9.90		CHEMBL

External reference:

ID	Source
4019964	VUID
N0000148049	NUI
D08648	KEGG_DRUG
6138-79-0	SECONDARY_CAS_RN
4018541	VANDF
4019964	VANDF
C0041098	UMLSCUI
CHEBI:84116	CHEBI
CHEMBL855	ChEMBL_ID
CHEMBL3188034	ChEMBL_ID
CHEMBL1200450	ChEMBL_ID
DB00427	DRUGBANK_ID
D014311	MESH_DESCRIPTOR_UI
5282443	PUBCHEM_CID
1228	IUPHAR_LIGAND_ID
502	INN_ID
2L8T9S52QM	UNII
10849	RXNORM
10773	MMSL
330097	MMSL
5639	MMSL
80877	MMSL
d00786	MMSL
003401	NDDF
004799	NDDF
25995007	SNOMEDCT_US
372678008	SNOMEDCT_US
65982003	SNOMEDCT_US

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Wal-Act	HUMAN OTC DRUG LABEL	2	0363-0178	TABLET, FILM COATED	2.50 mg	ORAL	OTC monograph final	16 sections
Cold and Allergy D	HUMAN OTC DRUG LABEL	2	0363-1780	TABLET, FILM COATED	2.50 mg	ORAL	OTC monograph final	16 sections
Overnight Cold and Flu	HUMAN OTC DRUG LABEL	3	0363-6980	SOLUTION	2.50 mg	ORAL	OTC monograph final	17 sections
ED-A-HIST PSE	HUMAN OTC DRUG LABEL	2	0485-0210	TABLET, COATED	2.50 mg	ORAL	OTC monograph final	16 sections
TRIPROLIDINE HYDROCHLORIDE	HUMAN OTC DRUG LABEL	1	0536-1257	LIQUID	0.94 mg	ORAL	OTC monograph final	15 sections
TRIPROLIDINE HYDROCHLORIDE	HUMAN OTC DRUG LABEL	1	0536-1258	LIQUID	2.50 mg	ORAL	OTC monograph final	15 sections
Aprodine	HUMAN OTC DRUG LABEL	2	0904-0250	TABLET, FILM COATED	2.50 mg	ORAL	OTC monograph final	16 sections
Target Overnight Cold and Flu	HUMAN OTC DRUG LABEL	3	11673-698	SOLUTION	2.50 mg	ORAL	OTC monograph final	17 sections
Triprolidine HCl Drops	HUMAN OTC DRUG LABEL	1	15310-112	LIQUID	0.94 mg	ORAL	OTC monograph final	13 sections
Aprodine	HUMAN OTC DRUG LABEL	2	21695-929	TABLET, FILM COATED	2.50 mg	ORAL	OTC monograph final	16 sections
HISTEX AC	HUMAN OTC DRUG LABEL	3	28595-250	SYRUP	2.50 mg	ORAL	OTC MONOGRAPH FINAL	17 sections
HISTEX PD Drops	HUMAN OTC DRUG LABEL	1	28595-801	SYRUP	0.94 mg	ORAL	OTC MONOGRAPH FINAL	14 sections
HISTEX	HUMAN OTC DRUG LABEL	1	28595-802	SYRUP	2.50 mg	ORAL	OTC MONOGRAPH FINAL	15 sections
HISTEX-DM	HUMAN OTC DRUG LABEL	3	28595-804	SYRUP	2.50 mg	ORAL	OTC MONOGRAPH FINAL	16 sections
Meijer Nighttime Cold and Flu	HUMAN OTC DRUG LABEL	3	41250-869	SOLUTION	2.50 mg	ORAL	OTC monograph final	17 sections
Aprodine	HUMAN OTC DRUG LABEL	2	50090-0622	TABLET, FILM COATED	2.50 mg	ORAL	OTC MONOGRAPH FINAL	17 sections
Silafed	HUMAN OTC DRUG LABEL	2	54838-101	SYRUP	1.25 mg	ORAL	OTC MONOGRAPH FINAL	14 sections
Triponel	HUMAN OTC DRUG LABEL	3	54859-508	LIQUID	1.25 mg	ORAL	OTC monograph final	9 sections
Triponel	HUMAN OTC DRUG LABEL	3	54859-514	LIQUID	30 mg	ORAL	OTC monograph final	9 sections
Triacin-C	HUMAN PRESCRIPTION DRUG LABEL	3	54879-005	SYRUP	1.25 mg	ORAL	ANDA	13 sections
Colcol Co Tab.	HUMAN OTC DRUG LABEL	2	58354-110	TABLET	2.50 mg	ORAL	OTC monograph final	8 sections
STAHIST TP	HUMAN OTC DRUG LABEL	2	58407-010	TABLET	2.50 mg	ORAL	OTC monograph final	16 sections
Maxifed TR	HUMAN OTC DRUG LABEL	2	58605-106	TABLET	1.25 mg	ORAL	OTC MONOGRAPH FINAL	16 sections
Maxi-Tuss TR	HUMAN OTC DRUG LABEL	2	58605-305	LIQUID	1.25 mg	ORAL	OTC MONOGRAPH FINAL	17 sections
Childrens PediaClear PD	HUMAN OTC DRUG LABEL	1	58809-651	LIQUID	1.25 mg	ORAL	OTC monograph final	15 sections
Childrens PediaClear PD	HUMAN OTC DRUG LABEL	1	58809-651	LIQUID	1.25 mg	ORAL	OTC monograph final	15 sections
Delsym Nighttime Cough	HUMAN OTC DRUG LABEL	3	63824-223	SOLUTION	2.50 mg	ORAL	OTC MONOGRAPH FINAL	17 sections
Mucinex Nightshift Sinus	HUMAN OTC DRUG LABEL	4	63824-269	SOLUTION	2.50 mg	ORAL	OTC MONOGRAPH FINAL	17 sections
Mucinex Nightshift Sinus Clear and Cool	HUMAN OTC DRUG LABEL	4	63824-270	SOLUTION	2.50 mg	ORAL	OTC MONOGRAPH FINAL	17 sections
Mucinex Nightshift Cold and Flu Clear and Cool	HUMAN OTC DRUG LABEL	4	63824-501	SOLUTION	2.50 mg	ORAL	OTC MONOGRAPH FINAL	17 sections