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

Stem definitionDrug idCAS RN
2763 486-12-4

Description:

MoleculeDescription

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:

DoseUnitRoute
7.50 mg O

ADMET properties:

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

Approvals:

DateAgencyCompanyOrphan
May 17, 1983 FDA SANDOZ

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
COVID-19 88.92 25.26 48 2183 75010 56214826
Disease recurrence 61.25 25.26 26 2205 23834 56266002
Sinusitis 56.64 25.26 53 2178 197528 56092308
Salpingo-oophorectomy unilateral 49.04 25.26 10 2221 682 56289154
Sinusitis fungal 46.15 25.26 11 2220 1539 56288297
Asthma 45.91 25.26 37 2194 112733 56177103
Sputum increased 42.71 25.26 11 2220 2113 56287723
Respiratory symptom 39.74 25.26 11 2220 2779 56287057
Embolism venous 39.51 25.26 11 2220 2837 56286999
Chronic sinusitis 38.76 25.26 14 2217 8364 56281472
Nasal polyps 38.03 25.26 11 2220 3254 56286582
Diastolic dysfunction 36.04 25.26 12 2219 5633 56284203
Female genital tract fistula 34.57 25.26 11 2220 4481 56285355
Hysterectomy 31.12 25.26 12 2219 8579 56281257
Emphysema 29.38 25.26 12 2219 9964 56279872
Impaired quality of life 27.74 25.26 11 2220 8463 56281373
Infusion site mass 26.49 25.26 7 2224 1485 56288351
Eczema 26.16 25.26 15 2216 26138 56263698

FDA Adverse Event Reporting System (Male)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
COVID-19 60.07 34.15 25 485 54796 31642038

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
COVID-19 113.34 27.08 58 2112 105699 70820575
Disease recurrence 72.47 27.08 31 2139 37572 70888702
Salpingo-oophorectomy unilateral 52.32 27.08 10 2160 635 70925639
Asthma 52.19 27.08 37 2133 120756 70805518
Sinusitis 51.42 27.08 42 2128 169153 70757121
Sinusitis fungal 45.74 27.08 11 2159 2074 70924200
Female genital tract fistula 41.40 27.08 11 2159 3092 70923182
Respiratory symptom 39.25 27.08 11 2159 3770 70922504
Embolism venous 39.06 27.08 11 2159 3834 70922440
Sputum increased 38.44 27.08 11 2159 4061 70922213
Nasal polyps 37.32 27.08 11 2159 4505 70921769
Hysterectomy 34.96 27.08 11 2159 5601 70920673
Chronic sinusitis 34.34 27.08 12 2158 8439 70917835
Diastolic dysfunction 33.05 27.08 12 2158 9421 70916853
Emphysema 27.61 27.08 12 2158 15048 70911226

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
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|

DiseaseRelationSNOMED_IDDOID
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 levelDissociation constantType (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:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
Histamine H1 receptor GPCR ANTAGONIST Ki 9.90 CHEMBL CHEMBL
Histamine H1 receptor GPCR Kd 9.90 CHEMBL

External reference:

IDSource
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:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
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
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
Aprodine HUMAN OTC DRUG LABEL 2 0904-7302 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
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
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