triprolidine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | 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
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

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
azlogd74 LogD at pH 7.4 1.309 High 1
caco2-efflux Caco-2 efflux ratio (BA/AB) 0.863 High 1
caco2-intrinsic-papp Caco-2 intrinsic apparent permeability 35.481 10^-6 cm/s High 1
dh-clint Dog hepatocyte intrinsic clearance 60.674 uL/min/10^6 cells High 1
dppb Dog plasma protein binding (% unbound) 61.420 % High 1
fcs-ppb Fetal calf serum protein binding (% unbound) 71.530 % High 1
herg hERG pIC50 5.060 pIC50 High 1
hh-clint Human hepatocyte intrinsic clearance 3.846 uL/min/10^6 cells High 1
hlm-clint Human liver microsomal intrinsic clearance 9.036 uL/min/mg protein High 1
hppb Human plasma protein binding (% unbound) 61.970 % High 1
kinase-safety-class ACVR2B,AKT2,AKT3,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK5,CDK9,DDR1,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,ITK,JAK2,JAK3,MAP3K7,MAPK10,MAPK12,MAPK7,MAPKAPK2,MET,NTRK2,PDK2,PDK4,PDPK1,PIK3CB,PIM2,PRKDC,SIK2,SIK3,STK33,TEK,TGFBR1,TTK 38
kinase-selectivity-class ACVR2B,AXL,BRAF,EIF2AK3,ERBB2,GRK2,SIK2,STK33 8
mdck-mdr1-efflux MDCK-MDR1 efflux ratio 0.157 High 1
mh-clint Mouse hepatocyte intrinsic clearance 210.863 High 1
mppb Mouse plasma protein binding (% unbound) 64.480 High 1
nih-mdck-mdr1-efflux NIH MDCK-MDR1 efflux ratio 0.910 High 1
pfas-class PFAS structural alert (1 = True, 0 = False) 0
pppb Pig plasma protein binding (% unbound) 70.770 % High 1
rh-clint Rat hepatocyte intrinsic clearance 283.792 uL/min/10^6 cells High 1
rh-fuinc Rat hepatocyte fraction unbound in incubation 83.460 % High 1
rppb Rat plasma protein binding (% unbound) 62.450 % High 1
solubility-dd Solubility at pH 7.4 in DMSO 877.001 uM High 1

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
Ulcer haemorrhage 241.84 33.94 81 5240 26240 90596886
Pulmonary fibrosis 148.17 33.94 87 5234 107416 90515710
Type 2 diabetes mellitus 127.40 33.94 101 5220 203143 90419983
Oedema 126.55 33.94 100 5221 200195 90422931
Psoriatic arthropathy 119.14 33.94 102 5219 228233 90394893
Injury 117.13 33.94 95 5226 197254 90425872
Liver injury 113.84 33.94 88 5233 170479 90452647
Sleep disorder 104.34 33.94 89 5232 197941 90425185
Pericarditis 100.66 33.94 100 5221 270051 90353075
Mobility decreased 97.47 33.94 95 5226 250639 90372487
Dyspepsia 92.20 33.94 83 5238 198077 90425049
Migraine 89.07 33.94 80 5241 190312 90432814
Gait disturbance 83.55 33.94 89 5232 260407 90362719
Urticaria 83.40 33.94 97 5224 312637 90310489
Pemphigus 81.57 33.94 98 5223 326766 90296360
Stomatitis 77.93 33.94 88 5233 274610 90348516
Sinusitis 77.76 33.94 98 5223 342990 90280136
Insomnia 62.77 33.94 87 5234 333387 90289739
Weight increased 58.61 33.94 95 5226 417832 90205294
Joint swelling 48.28 33.94 97 5224 503203 90119923
Pain in extremity 42.18 33.94 86 5235 450443 90172683

FDA Adverse Event Reporting System (Male)

None

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
Ulcer haemorrhage 158.26 40.35 49 3522 22522 110563206
Type 2 diabetes mellitus 106.57 40.35 68 3503 177164 110408564
Pulmonary fibrosis 103.49 40.35 55 3516 101987 110483741
Oedema 100.76 40.35 70 3501 209906 110375822
Injury 99.15 40.35 65 3506 177200 110408528
Psoriatic arthropathy 97.70 40.35 67 3504 196694 110389034
Pemphigus 90.19 40.35 66 3505 214504 110371224
Pericarditis 88.95 40.35 66 3505 219048 110366680
Liver injury 88.61 40.35 57 3514 150356 110435372
Mobility decreased 82.07 40.35 65 3506 237357 110348371
Sleep disorder 76.50 40.35 58 3513 198586 110387142
Sinusitis 69.47 40.35 65 3506 296623 110289105
Migraine 68.02 40.35 51 3520 171601 110414127
Dyspepsia 67.49 40.35 53 3518 190912 110394816
Urticaria 61.80 40.35 63 3508 318794 110266934
Gait disturbance 61.38 40.35 59 3512 278149 110307579
Stomatitis 55.28 40.35 55 3516 270187 110315541
Joint swelling 49.62 40.35 66 3505 442779 110142949
Insomnia 48.70 40.35 59 3512 360531 110225197
Weight increased 46.17 40.35 62 3509 419582 110166146

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 D006633 Histamine Antagonists
MeSH PA D006634 Histamine H1 Antagonists
MeSH PA D018377 Neurotransmitter Agents
MeSH PA D018926 Anti-Allergic Agents
CHEBI has role CHEBI:37955 H<small><sub>1</sub></small>-receptor antagonist
CHEBI has role CHEBI:77715 nasal decongestant

Related Drugs by ATC class:

R06AX Other antihistamines for systemic use 26 drugs
acrivastineantazolineastemizoleazatadineazelastinebamipinebilastinecyproheptadinedeptropinedesloratadineebastineepinastine show all 26 →

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
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
2L8T9S52QM INXIGHT DRUGS

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Cold and Allergy D HUMAN OTC DRUG LABEL 2 0363-0287 TABLET, FILM COATED 2.50 mg ORAL OTC Monograph Drug 16 sections
Overnight Cold and Flu HUMAN OTC DRUG LABEL 3 0363-6980 SOLUTION 2.50 mg ORAL OTC Monograph Drug 17 sections
Cold and FluNighttime HUMAN OTC DRUG LABEL 3 0363-8063 SOLUTION 2.50 mg ORAL OTC Monograph Drug 16 sections
Cold and FluNighttime HUMAN OTC DRUG LABEL 3 0363-8063 SOLUTION 2.50 mg ORAL OTC Monograph Drug 16 sections
Cold and FluSevere HUMAN OTC DRUG LABEL 4 0363-8078 SOLUTION 2.50 mg ORAL OTC Monograph Drug 16 sections
Cold and FluSevere HUMAN OTC DRUG LABEL 4 0363-8078 SOLUTION 2.50 mg ORAL OTC Monograph Drug 16 sections
ED-A-HIST PSE HUMAN OTC DRUG LABEL 2 0485-0210 TABLET, 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 Drug 16 sections
Target Overnight Cold and Flu HUMAN OTC DRUG LABEL 3 11673-698 SOLUTION 2.50 mg ORAL OTC Monograph Drug 17 sections
Target Overnight Cold and Flu HUMAN OTC DRUG LABEL 3 11673-698 SOLUTION 2.50 mg ORAL OTC Monograph Drug 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-DM New Formulation HUMAN OTC DRUG LABEL 3 28595-310 SYRUP 2.50 mg ORAL OTC Monograph Drug 16 sections
HISTEX HUMAN OTC DRUG LABEL 1 28595-802 SYRUP 2.50 mg ORAL OTC Monograph Drug 15 sections
HISTEX-DM HUMAN OTC DRUG LABEL 3 28595-804 SYRUP 2.50 mg ORAL OTC Monograph Drug 16 sections
HISTEX PD Drops New Formulation HUMAN OTC DRUG LABEL 1 28595-809 SYRUP 1.25 mg ORAL OTC Monograph Drug 16 sections
Meijer Nighttime Cold and Flu HUMAN OTC DRUG LABEL 3 41250-869 SOLUTION 2.50 mg ORAL OTC Monograph Drug 17 sections
Meijer Nighttime Cold and Flu HUMAN OTC DRUG LABEL 3 41250-869 SOLUTION 2.50 mg ORAL OTC Monograph Drug 17 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 50090-7085 TABLET, FILM COATED 2.50 mg ORAL OTC Monograph Drug 17 sections
Endal HUMAN OTC DRUG LABEL 2 50991-136 LIQUID 1.25 mg ORAL OTC Monograph Drug 16 sections
Endal HUMAN OTC DRUG LABEL 2 50991-136 LIQUID 1.25 mg ORAL OTC Monograph Drug 16 sections
Cold and FluNighttime HUMAN OTC DRUG LABEL 3 51316-963 SOLUTION 2.50 mg ORAL OTC Monograph Drug 16 sections
Triponel HUMAN OTC DRUG LABEL 3 54859-508 LIQUID 1.25 mg ORAL OTC Monograph Drug 9 sections
Triponel HUMAN OTC DRUG LABEL 3 54859-514 LIQUID 30 mg ORAL OTC Monograph Drug 9 sections
Triacin-C HUMAN PRESCRIPTION DRUG LABEL 3 54879-005 SYRUP 1.25 mg ORAL ANDA 13 sections
STAHIST TP HUMAN OTC DRUG LABEL 2 58407-010 TABLET 2.50 mg ORAL OTC Monograph Drug 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 Drug 14 sections