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:

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Property	Value	Reference
BA (Bioavailability)	4 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
S (Water solubility)	100 mg/mL	Bocci G, Oprea TI, Benet LZ
BDDCS (Biopharmaceutical Drug Disposition Classification System)	1	Bocci G, Oprea TI, Benet LZ

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Approvals:

Date	Agency	Company	Orphan
May 17, 1983	FDA	SANDOZ

FDA Adverse Event Reporting System (Female)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Sinusitis	177.30	10.74	459	45643	226194	63216726
Contraindicated product administered	136.03	10.74	5	46097	217643	63225277
Asthma	120.53	10.74	278	45824	127283	63315637
Toxicity to various agents	115.92	10.74	20	46082	247230	63195690
Hand deformity	101.97	10.74	3	46099	159454	63283466
Synovitis	99.82	10.74	10	46092	186908	63256012
Maternal exposure during pregnancy	96.39	10.74	21	46081	220041	63222879
Drug intolerance	93.59	10.74	54	46048	308607	63134313
Glossodynia	87.12	10.74	13	46089	178863	63264057
Systemic lupus erythematosus	85.50	10.74	23	46079	208895	63234025

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FDA Adverse Event Reporting System (Male)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Sinusitis	111.13	12.51	123	18425	41279	34897104
Asthma	66.95	12.51	97	18451	42559	34895824
Toxicity to various agents	66.23	12.51	13	18535	200349	34738034
Infective pulmonary exacerbation of cystic fibrosis	57.47	12.51	39	18509	6762	34931621
Drug interaction	52.87	12.51	27	18521	225919	34712464
Upper respiratory tract infection	51.60	12.51	75	18473	32984	34905399
Fatigue	35.88	12.51	326	18222	370327	34568056
Drug abuse	35.88	12.51	5	18543	99091	34839292
Cough	35.00	12.51	165	18383	149975	34788408
Dyspnoea	28.96	12.51	316	18232	376466	34561917

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FDA Adverse Event Reporting System (Geriatric)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Toxicity to various agents	181.66	10.66	22	48629	421518	79274219
Drug interaction	132.73	10.66	44	48607	415139	79280598
Asthma	122.60	10.66	261	48390	134834	79560903
Sinusitis	121.50	10.66	326	48325	195175	79500562
Infective pulmonary exacerbation of cystic fibrosis	113.71	10.66	80	48571	12771	79682966
Completed suicide	102.93	10.66	14	48637	245753	79449984
Off label use	102.57	10.66	254	48397	906961	78788776
Contraindicated product administered	79.48	10.66	4	48647	157534	79538203
Drug abuse	79.41	10.66	5	48646	162686	79533051
Anxiety	79.39	10.66	331	48320	248181	79447556

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	R06AX07	RESPIRATORY SYSTEM ANTIHISTAMINES FOR SYSTEMIC USE ANTIHISTAMINES FOR SYSTEMIC USE Other antihistamines for systemic use
CHEBI has role	CHEBI:37955	H1 receptor antagonists
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

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Drug Use | Suggest Off label Use Form| |View source of the data|

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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

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🐶 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:

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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

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External reference:

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ID	Source
003401	NDDF
004799	NDDF
10773	MMSL
10849	RXNORM
1228	IUPHAR_LIGAND_ID
25995007	SNOMEDCT_US
2L8T9S52QM	UNII
330097	MMSL
372678008	SNOMEDCT_US
4018541	VANDF

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Aprodine	HUMAN OTC DRUG LABEL	2	0904-0250	TABLET, FILM COATED	2.50 mg	ORAL	OTC monograph final	16 sections
Aprodine	HUMAN OTC DRUG LABEL	2	0904-0250	TABLET, FILM COATED	2.50 mg	ORAL	OTC monograph final	16 sections
Aprodine	HUMAN OTC DRUG LABEL	2	0904-7302	TABLET, FILM COATED	2.50 mg	ORAL	OTC monograph final	16 sections
Aprodine	HUMAN OTC DRUG LABEL	2	0904-7302	TABLET, FILM COATED	2.50 mg	ORAL	OTC monograph final	16 sections
Aprodine	HUMAN OTC DRUG LABEL	2	21695-929	TABLET, FILM COATED	2.50 mg	ORAL	OTC monograph final	16 sections
Aprodine	HUMAN OTC DRUG LABEL	2	50090-0622	TABLET, FILM COATED	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
Cold and Allergy D	HUMAN OTC DRUG LABEL	2	0363-0287	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
Cold and Allergy D	HUMAN OTC DRUG LABEL	2	0363-1780	TABLET, FILM COATED	2.50 mg	ORAL	OTC monograph final	16 sections

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