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
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

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
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
Treatment failure 85.15 10.74 20 46082 199023 63243897
Off label use 84.39 10.74 233 45869 674229 62768691
Pericarditis 82.26 10.74 3 46099 131576 63311344
Drug ineffective 81.73 10.74 437 45665 1044328 62398592
Drug interaction 77.01 10.74 35 46067 229096 63213824
Anxiety 76.66 10.74 337 45765 217204 63225716
Cough 68.39 10.74 404 45698 292339 63150581
Bronchitis 67.57 10.74 222 45880 124713 63318207
Therapeutic product effect decreased 65.70 10.74 29 46073 193158 63249762
Wound 63.07 10.74 20 46082 163243 63279677
Chest discomfort 62.72 10.74 199 45903 109770 63333150
Infective pulmonary exacerbation of cystic fibrosis 59.19 10.74 50 46052 8767 63434153
Hepatic enzyme increased 59.03 10.74 37 46065 202291 63240629
Infusion related reaction 58.77 10.74 55 46047 245466 63197454
Joint swelling 57.80 10.74 93 46009 327573 63115347
General physical health deterioration 57.16 10.74 38 46064 201364 63241556
Sputum increased 56.44 10.74 30 46072 2429 63440491
Gastrooesophageal reflux disease 55.38 10.74 174 45928 95465 63347455
Diverticulum 55.11 10.74 55 46047 11936 63430984
Dyspnoea 54.95 10.74 726 45376 660587 62782333
Salpingo-oophorectomy unilateral 52.96 10.74 21 46081 860 63442060
Product dose omission issue 51.89 10.74 319 45783 233994 63208926
Deep vein thrombosis 51.81 10.74 156 45946 83644 63359276
Product quality issue 50.20 10.74 92 46010 35773 63407147
Arthropathy 50.09 10.74 58 46044 234734 63208186
Sinusitis fungal 49.69 10.74 25 46077 1806 63441114
Alopecia 49.62 10.74 107 45995 337429 63105491
Rheumatoid factor positive 49.28 10.74 3 46099 84403 63358517
Emotional distress 47.47 10.74 85 46017 32464 63410456
Nasal congestion 47.15 10.74 129 45973 65531 63377389
Helicobacter infection 46.91 10.74 6 46096 92779 63350141
Pulmonary embolism 46.68 10.74 188 45914 116496 63326424
Upper respiratory tract infection 46.33 10.74 148 45954 81899 63361021
Depression 43.16 10.74 267 45835 196225 63246695
Headache 42.90 10.74 671 45431 632570 62810350
Sleep apnoea syndrome 41.11 10.74 75 46027 29058 63413862
Discomfort 40.61 10.74 37 46065 167337 63275583
Diastolic dysfunction 39.99 10.74 35 46067 6436 63436484
Chronic obstructive pulmonary disease 39.98 10.74 118 45984 62568 63380352
Chronic sinusitis 38.36 10.74 47 46055 12796 63430124
Nasal polyps 38.00 10.74 33 46069 6006 63436914
Embolism venous 37.05 10.74 25 46077 3129 63439791
Folliculitis 36.90 10.74 4 46098 70313 63372607
Drug abuse 35.91 10.74 5 46097 72513 63370407
Infusion site erythema 35.30 10.74 43 46059 11636 63431284
C-reactive protein increased 34.15 10.74 13 46089 94694 63348226
Ear infection 33.55 10.74 81 46021 38132 63404788
Respiratory symptom 33.40 10.74 24 46078 3323 63439597
Pneumonia 32.39 10.74 488 45614 456279 62986641
Hiatus hernia 32.27 10.74 57 46045 21537 63421383
Sinus disorder 31.88 10.74 61 46041 24492 63418428
Acute respiratory failure 30.17 10.74 73 46029 34412 63408508
Febrile neutropenia 30.16 10.74 25 46077 118424 63324496
Blister 29.96 10.74 30 46072 129784 63313136
Rheumatoid arthritis 29.89 10.74 90 46012 253729 63189191
Tricuspid valve incompetence 29.19 10.74 44 46058 14577 63428343
Candida infection 28.07 10.74 63 46039 28288 63414632
Emphysema 27.88 10.74 37 46065 10901 63432019
Rhinitis allergic 27.36 10.74 38 46064 11689 63431231
Infusion site pruritus 26.48 10.74 27 46075 6008 63436912
Iron deficiency anaemia 26.41 10.74 50 46052 19919 63423001
Infusion site swelling 26.38 10.74 34 46068 9736 63433184
Chest pain 25.90 10.74 255 45847 215704 63227216
Poor quality device used 25.74 10.74 17 46085 2054 63440866
Hysterectomy 25.56 10.74 33 46069 9466 63433454
Urinary tract infection 25.01 10.74 298 45804 264386 63178534
Cholecystitis chronic 24.81 10.74 34 46068 10327 63432593
Seasonal allergy 24.72 10.74 50 46052 20900 63422020
Dizziness 24.41 10.74 443 45659 429482 63013438
Migraine 24.30 10.74 143 45959 103203 63339717
Product use issue 23.99 10.74 81 46021 220439 63222481
Acute sinusitis 23.97 10.74 21 46081 3866 63439054
Intentional overdose 23.85 10.74 12 46090 74140 63368780
Swelling 23.71 10.74 111 45991 275267 63167653
Neutropenia 23.64 10.74 58 46044 174947 63267973
C-reactive protein abnormal 23.25 10.74 3 46099 46093 63396827
Coma 22.93 10.74 9 46093 64355 63378565
Product use in unapproved indication 22.92 10.74 61 46041 179019 63263901
Wheezing 22.29 10.74 132 45970 95463 63347457
Hypervolaemia 21.57 10.74 57 46045 28356 63414564
Female genital tract fistula 21.51 10.74 27 46075 7532 63435388
Malignant neoplasm progression 21.32 10.74 17 46085 82104 63360816
Disease recurrence 21.04 10.74 56 46046 27974 63414946
Injury 21.01 10.74 107 45995 73140 63369780
Pulmonary hypertension 20.98 10.74 67 46035 37056 63405864
Liver injury 20.69 10.74 9 46093 60511 63382409
Coronary artery disease 20.69 10.74 61 46041 32316 63410604
Infusion site nodule 20.39 10.74 13 46089 1479 63441441
Oedema peripheral 19.98 10.74 218 45884 189293 63253627
Musculoskeletal stiffness 19.95 10.74 68 46034 184550 63258370
Gastroenteritis viral 19.49 10.74 49 46053 23651 63419269
Hyponatraemia 19.46 10.74 32 46070 111868 63331052
Lower respiratory tract infection 19.35 10.74 42 46060 132265 63310655
Abdominal discomfort 19.31 10.74 145 45957 320740 63122180
Anhedonia 19.09 10.74 31 46071 10943 63431977
Muscle spasms 19.01 10.74 185 45917 155965 63286955
Thrombocytopenia 18.95 10.74 52 46050 151105 63291815
Infusion site extravasation 18.88 10.74 30 46072 10396 63432524
Infusion site mass 18.76 10.74 14 46088 2054 63440866
Anosmia 18.72 10.74 24 46078 6836 63436084
Dyspnoea exertional 18.65 10.74 90 46012 60212 63382708
Palpitations 18.65 10.74 143 45959 112627 63330293
Hereditary angioedema 18.39 10.74 25 46077 7537 63435383
Red blood cell sedimentation rate increased 17.67 10.74 5 46097 43977 63398943
Feeling abnormal 17.67 10.74 175 45927 148217 63294703
Insurance issue 17.63 10.74 22 46080 6099 63436821
Multiple allergies 17.56 10.74 34 46068 13768 63429152
Biliary dyskinesia 17.35 10.74 15 46087 2714 63440206
Low turnover osteopathy 17.06 10.74 18 46084 4167 63438753
Neck pain 16.99 10.74 97 46005 69221 63373699
Back pain 16.69 10.74 277 45825 263868 63179052
Gallbladder disorder 16.60 10.74 40 46062 18802 63424118
Pancytopenia 16.60 10.74 28 46074 96905 63346015
Cardiac failure congestive 16.29 10.74 119 45983 92314 63350606
Panic attack 16.15 10.74 44 46058 22287 63420633
Mucosal inflammation 16.01 10.74 7 46095 46921 63395999
Sinus headache 15.88 10.74 20 46082 5596 63437324
Mobility decreased 15.70 10.74 41 46061 121118 63321802
Multiple organ dysfunction syndrome 15.69 10.74 11 46091 56741 63386179
Flatulence 15.56 10.74 58 46044 34644 63408276
Leukopenia 15.50 10.74 20 46082 77270 63365650
Viral infection 15.49 10.74 59 46043 35604 63407316
Impaired healing 15.46 10.74 32 46070 102510 63340410
Liver disorder 15.39 10.74 10 46092 53677 63389243
Drug-induced liver injury 15.39 10.74 5 46097 40217 63402703
Fungal infection 15.20 10.74 60 46042 36814 63406106
Depressed level of consciousness 14.72 10.74 14 46088 62064 63380856
Anaphylactic reaction 14.60 10.74 90 46012 66010 63376910
Pulmonary function test decreased 14.38 10.74 16 46086 3931 63438989
Uterine perforation 13.96 10.74 21 46081 6942 63435978
Vitamin D deficiency 13.90 10.74 31 46071 13861 63429059
Rhinorrhoea 13.68 10.74 88 46014 65489 63377431
Transient ischaemic attack 13.65 10.74 59 46043 37694 63405226
Device dislocation 13.27 10.74 45 46057 25660 63417260
Infusion site bruising 13.05 10.74 15 46087 3817 63439103
Premature delivery 13.02 10.74 3 46099 30278 63412642
Impaired quality of life 12.95 10.74 30 46072 13753 63429167
Spinal osteoarthritis 12.83 10.74 33 46069 16153 63426767
Essential hypertension 12.79 10.74 17 46085 5016 63437904
Confusional state 12.74 10.74 110 45992 236270 63206650
Overdose 12.69 10.74 42 46060 115036 63327884
Dermatitis contact 12.66 10.74 26 46076 10982 63431938
Hyperlipidaemia 12.62 10.74 37 46065 19534 63423386
Insomnia 12.60 10.74 223 45879 215029 63227891
Cardio-respiratory arrest 12.56 10.74 15 46087 59944 63382976
Hypoxia 12.33 10.74 80 46022 59712 63383208
Foetal exposure during pregnancy 12.18 10.74 4 46098 31958 63410962
Myalgia 12.12 10.74 161 45941 146368 63296552
Urticaria 12.03 10.74 178 45924 165624 63277296
Infusion site pain 11.96 10.74 33 46069 16836 63426084
Ageusia 11.94 10.74 29 46073 13699 63429221
Ill-defined disorder 11.91 10.74 26 46076 81729 63361191
Dysphonia 11.91 10.74 67 46035 47547 63395373
Acute kidney injury 11.90 10.74 128 45974 263287 63179633
Atrophic vulvovaginitis 11.81 10.74 10 46092 1758 63441162
Gallbladder injury 11.51 10.74 9 46093 1414 63441506
Diverticulitis 11.49 10.74 58 46044 39499 63403421
Memory impairment 11.47 10.74 121 45981 104137 63338783
Cellulitis 11.43 10.74 100 46002 81858 63361062
Urine analysis abnormal 11.32 10.74 16 46086 5000 63437920
Exercise test abnormal 11.20 10.74 4 46098 122 63442798
Rash 11.18 10.74 316 45786 560555 62882365
Infusion site haemorrhage 11.15 10.74 16 46086 5070 63437850
Hepatic failure 11.12 10.74 6 46096 35650 63407270
Hip arthroplasty 11.00 10.74 11 46091 47635 63395285
Therapeutic product effect incomplete 10.99 10.74 50 46052 125006 63317914
Hyperkalaemia 10.90 10.74 14 46088 54189 63388731
Metabolic acidosis 10.88 10.74 10 46092 45059 63397861

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
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
Product dose omission issue 28.20 12.51 132 18416 119579 34818804
Off label use 27.51 12.51 122 18426 419402 34518981
Nasal congestion 27.19 12.51 46 18502 23011 34915372
Pneumonia 24.64 12.51 297 18251 362330 34576053
Bronchitis 23.80 12.51 62 18486 41901 34896482
Cystic fibrosis 22.89 12.51 13 18535 1645 34936738
Headache 21.14 12.51 180 18368 200455 34737928
Anxiety 20.80 12.51 106 18442 99322 34839061
Ear infection 20.17 12.51 26 18522 10205 34928178
Productive cough 19.56 12.51 54 18494 37759 34900624
Chest pain 19.20 12.51 124 18424 126638 34811745
General physical health deterioration 19.10 12.51 24 18524 128245 34810138
Febrile neutropenia 18.96 12.51 27 18521 136822 34801561
Sinus disorder 18.89 12.51 21 18527 7064 34931319
Personality change 18.70 12.51 18 18530 5121 34933262
Infusion site pruritus 18.67 12.51 9 18539 814 34937569
Product complaint 18.43 12.51 19 18529 5871 34932512
Rhinorrhoea 17.83 12.51 41 18507 25627 34912756
Back pain 17.75 12.51 118 18430 121671 34816712
Sputum discoloured 17.23 12.51 21 18527 7791 34930592
Myalgia 17.12 12.51 89 18459 84021 34854362
Gastroenteritis viral 17.11 12.51 20 18528 7104 34931279
Infusion site erythema 16.78 12.51 12 18536 2261 34936122
Acute kidney injury 16.35 12.51 95 18453 304893 34633490
Drug ineffective 16.10 12.51 160 18388 456591 34481792
Rhinitis allergic 15.71 12.51 13 18535 3037 34935346
Vision blurred 14.97 12.51 56 18492 45907 34892476
Wheezing 14.80 12.51 52 18496 41350 34897033
Cystic fibrosis related diabetes 14.73 12.51 5 18543 181 34938202
Sleep apnoea syndrome 14.71 12.51 33 18515 20288 34918095
Thrombocytopenia 14.55 12.51 39 18509 156208 34782175
Hepatic function abnormal 14.37 12.51 3 18545 44360 34894023
Intentional overdose 14.05 12.51 3 18545 43671 34894712
Neutropenia 13.95 12.51 40 18508 156738 34781645
Pulmonary function test decreased 13.71 12.51 15 18533 4960 34933423
Dyspnoea paroxysmal nocturnal 13.63 12.51 9 18539 1490 34936893
Overdose 13.59 12.51 17 18531 91042 34847341
Blood testosterone decreased 13.53 12.51 14 18534 4343 34934040
Seasonal allergy 13.21 12.51 17 18531 6658 34931725
Hypoxia 13.13 12.51 61 18487 55034 34883349
Dizziness 13.08 12.51 175 18373 218346 34720037
Pancreatic failure 13.06 12.51 7 18541 791 34937592
Completed suicide 12.97 12.51 20 18528 98148 34840235
Nasopharyngitis 12.85 12.51 72 18476 69896 34868487
Malignant neoplasm progression 12.56 12.51 17 18531 88029 34850354

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
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
Cough 79.06 10.66 436 48215 366353 79329384
Dyspnoea 73.23 10.66 821 47830 856204 78839533
Gastrooesophageal reflux disease 69.96 10.66 179 48472 104067 79591670
Drug ineffective 67.50 10.66 386 48265 1080527 78615210
Deep vein thrombosis 66.53 10.66 193 48458 120726 79575011
Upper respiratory tract infection 65.85 10.66 161 48490 91007 79604730
Sputum increased 63.74 10.66 38 48613 4575 79691162
Product dose omission issue 63.50 10.66 309 48342 247228 79448509
Chest discomfort 62.63 10.66 206 48445 137838 79557899
Synovitis 59.84 10.66 10 48641 150724 79545013
Nasal congestion 58.30 10.66 138 48513 76414 79619323
Salpingo-oophorectomy unilateral 57.64 10.66 21 48630 813 79694924
C-reactive protein increased 57.33 10.66 6 48645 129021 79566716
Treatment failure 54.51 10.66 18 48633 170468 79525269
Product quality issue 54.38 10.66 84 48567 33856 79661881
General physical health deterioration 53.94 10.66 53 48598 275185 79420552
Emotional distress 51.96 10.66 90 48561 39879 79655858
Hand deformity 51.29 10.66 3 48648 103916 79591821
Pulmonary embolism 49.67 10.66 222 48429 171432 79524305
Pericarditis 48.57 10.66 4 48647 104232 79591505
Maternal exposure during pregnancy 48.10 10.66 12 48639 136526 79559211
Sinusitis fungal 47.67 10.66 25 48626 2349 79693388
Bronchitis 47.26 10.66 181 48470 130463 79565274
Drug intolerance 46.06 10.66 56 48595 264063 79431674
Depression 44.82 10.66 255 48396 216535 79479202
Sleep apnoea syndrome 44.65 10.66 80 48571 36398 79659339
Headache 44.27 10.66 600 48051 653172 79042565
Hiatus hernia 43.53 10.66 62 48589 23250 79672487
Febrile neutropenia 43.52 10.66 46 48605 230953 79464784
Chest pain 42.87 10.66 307 48344 281997 79413740
Diastolic dysfunction 40.52 10.66 41 48610 10770 79684967
Pneumonia 40.30 10.66 595 48056 659651 79036086
Infusion related reaction 38.90 10.66 50 48601 230187 79465550
Neutropenia 38.59 10.66 73 48578 287637 79408100
Nasal polyps 37.45 10.66 33 48618 7294 79688443
Thrombocytopenia 36.73 10.66 66 48585 265193 79430544
Intentional overdose 36.01 10.66 10 48641 105950 79589787
Systemic lupus erythematosus 35.03 10.66 15 48636 121134 79574603
Acute kidney injury 34.71 10.66 181 48470 519223 79176514
Diverticulum 34.50 10.66 44 48607 14852 79680885
Chronic sinusitis 34.23 10.66 41 48610 12985 79682752
Rhinitis allergic 32.87 10.66 39 48612 12230 79683507
Chronic obstructive pulmonary disease 32.25 10.66 120 48531 85299 79610438
Embolism venous 32.06 10.66 24 48627 4215 79691522
Dizziness 31.91 10.66 474 48177 525967 79169770
Wheezing 31.58 10.66 148 48503 116516 79579221
Hysterectomy 31.56 10.66 28 48623 6244 79689493
Female genital tract fistula 30.72 10.66 27 48624 5948 79689789
Product use in unapproved indication 30.61 10.66 67 48584 250292 79445445
Infusion site pruritus 30.45 10.66 23 48628 4095 79691642
Infusion site erythema 30.32 10.66 33 48618 9427 79686310
Acute respiratory failure 29.85 10.66 92 48559 59449 79636288
Coma 29.84 10.66 12 48639 100637 79595100
Sinus disorder 29.74 10.66 51 48600 22413 79673324
Injury 29.36 10.66 109 48542 77387 79618350
Joint swelling 29.27 10.66 85 48566 288561 79407176
Helicobacter infection 29.09 10.66 4 48647 69700 79626037
Urinary tract infection 28.98 10.66 275 48376 274237 79421500
Acute sinusitis 28.33 10.66 23 48628 4547 79691190
Hypervolaemia 28.31 10.66 73 48578 42617 79653120
Respiratory symptom 27.37 10.66 23 48628 4768 79690969
Fatigue 27.06 10.66 750 47901 928977 78766760
Pulmonary hypertension 26.67 10.66 77 48574 48003 79647734
Glossodynia 26.53 10.66 15 48636 103322 79592415
Rheumatoid factor positive 26.02 10.66 3 48648 59836 79635901
Pancytopenia 25.97 10.66 38 48613 165707 79530030
Hypoxia 25.80 10.66 128 48523 103115 79592622
Cholecystitis chronic 25.74 10.66 31 48620 9875 79685862
Malignant neoplasm progression 25.69 10.66 27 48624 135963 79559774
Therapeutic product effect decreased 25.25 10.66 38 48613 163825 79531912
Migraine 25.16 10.66 113 48538 87380 79608357
Cystic fibrosis 25.05 10.66 20 48631 3860 79691877
Iron deficiency anaemia 24.89 10.66 51 48600 25621 79670116
Gastroenteritis viral 24.87 10.66 50 48601 24781 79670956
Dyspnoea exertional 24.70 10.66 112 48539 86961 79608776
Poor quality device used 24.44 10.66 16 48635 2269 79693468
Candida infection 23.96 10.66 64 48587 38150 79657587
Coronary artery disease 23.90 10.66 91 48560 65383 79630354
Myalgia 23.20 10.66 193 48458 185448 79510289
Gamma-glutamyltransferase increased 23.14 10.66 3 48648 54677 79641060
Product complaint 22.74 10.66 34 48617 13315 79682422
Oedema peripheral 22.43 10.66 244 48407 252044 79443693
Sinus headache 22.28 10.66 21 48630 5059 79690678
Cardiac failure congestive 22.24 10.66 156 48495 142246 79553491
Depressed level of consciousness 22.12 10.66 16 48635 96636 79599101
Hyperlipidaemia 22.02 10.66 49 48602 26044 79669693
Overdose 21.93 10.66 50 48601 184156 79511581
Ear infection 21.93 10.66 58 48593 34374 79661363
Palpitations 21.75 10.66 142 48509 126468 79569269
Back pain 21.67 10.66 282 48369 303898 79391839
Interstitial lung disease 21.67 10.66 22 48629 112578 79583159
Emphysema 21.57 10.66 37 48614 16263 79679474
Tricuspid valve incompetence 21.32 10.66 41 48610 19671 79676066
Hepatotoxicity 21.30 10.66 3 48648 51349 79644388
Folliculitis 21.26 10.66 4 48647 55376 79640361
Hepatic function abnormal 21.21 10.66 9 48642 73098 79622639
Disease recurrence 21.04 10.66 67 48584 44042 79651695
Muscle spasms 20.95 10.66 180 48471 174550 79521187
Wound 20.91 10.66 24 48627 116155 79579582
Biliary dyskinesia 20.58 10.66 15 48636 2530 79693207
Multiple organ dysfunction syndrome 20.41 10.66 26 48625 120220 79575517
Cerebrovascular accident 20.23 10.66 163 48488 155129 79540608
Device dislocation 19.96 10.66 47 48604 25923 79669814
Drug-induced liver injury 19.41 10.66 8 48643 66109 79629628
Hyperkalaemia 19.15 10.66 25 48626 114373 79581364
Infusion site mass 19.13 10.66 12 48639 1581 79694156
Blister 19.10 10.66 27 48624 119449 79576288
Feeling abnormal 19.09 10.66 164 48487 159035 79536702
Seasonal allergy 18.83 10.66 35 48616 16371 79679366
Renal impairment 18.64 10.66 43 48608 157740 79537997
Metabolic acidosis 18.44 10.66 14 48637 82515 79613222
Intentional product use issue 18.34 10.66 41 48610 152071 79543666
Rhinorrhoea 18.07 10.66 93 48558 75981 79619756
Mucosal inflammation 17.97 10.66 12 48639 75568 79620169
Infusion site swelling 17.94 10.66 23 48628 7803 79687934
Neck pain 17.78 10.66 92 48559 75325 79620412
Bradycardia 17.63 10.66 35 48616 135522 79560215
Hepatic enzyme increased 17.62 10.66 55 48596 182555 79513182
Sleep disorder due to general medical condition, insomnia type 17.04 10.66 3 48648 43553 79652184
Leukopenia 17.02 10.66 28 48623 116485 79579252
Spinal osteoarthritis 16.85 10.66 34 48617 16893 79678844
Uterine perforation 16.83 10.66 20 48631 6283 79689454
Rheumatoid arthritis 16.64 10.66 68 48583 208402 79487335
Liver disorder 16.55 10.66 12 48639 72405 79623332
Drug resistance 16.31 10.66 3 48648 42210 79653527
Rhabdomyolysis 15.80 10.66 24 48627 103107 79592630
Septic shock 15.72 10.66 32 48619 122769 79572968
Insomnia 15.69 10.66 223 48428 244947 79450790
Toxic epidermal necrolysis 15.54 10.66 4 48647 44577 79651160
Mood swings 15.30 10.66 36 48615 19844 79675893
Pulmonary fibrosis 15.29 10.66 4 48647 44108 79651629
Pulmonary function test decreased 15.28 10.66 21 48630 7616 79688121
Nervousness 15.25 10.66 50 48601 33365 79662372
Altered state of consciousness 15.14 10.66 4 48647 43818 79651919
Pain in extremity 15.10 10.66 309 48342 364229 79331508
Cardio-respiratory arrest 15.00 10.66 27 48624 108483 79587254
Anhedonia 14.92 10.66 30 48621 14868 79680869
Gallbladder disorder 14.86 10.66 35 48616 19305 79676432
Blood lactate dehydrogenase increased 14.68 10.66 3 48648 39167 79656570
Panic attack 14.62 10.66 40 48611 24176 79671561
Productive cough 14.52 10.66 98 48553 88233 79607504
Cellulitis 14.49 10.66 115 48536 108945 79586792
Hepatitis 14.43 10.66 8 48643 55719 79640018
Right ventricular failure 14.37 10.66 39 48612 23458 79672279
Essential hypertension 14.21 10.66 18 48633 6035 79689702
Cholestasis 14.20 10.66 7 48644 52102 79643635
Eosinophilia 14.12 10.66 5 48646 45340 79650397
Ear canal erythema 14.01 10.66 3 48648 14 79695723
Nasal discomfort 13.98 10.66 17 48634 5466 79690271
Delirium 13.65 10.66 19 48632 84608 79611129
Therapy cessation 13.53 10.66 52 48599 37510 79658227
Viral infection 13.46 10.66 57 48594 42959 79652778
Eye pruritus 13.45 10.66 35 48616 20535 79675202
Liver injury 13.44 10.66 9 48642 56605 79639132
Insurance issue 13.38 10.66 17 48634 5716 79690021
Arthropathy 13.38 10.66 59 48592 177052 79518685
Dyspnoea paroxysmal nocturnal 13.36 10.66 11 48640 2217 79693520
Sputum discoloured 13.21 10.66 36 48615 21707 79674030
Vision blurred 13.17 10.66 110 48541 105788 79589949
Cystic fibrosis related diabetes 13.09 10.66 5 48646 221 79695516
Alopecia 13.07 10.66 85 48566 231270 79464467
Status asthmaticus 12.95 10.66 8 48643 1026 79694711
Hepatic failure 12.91 10.66 11 48640 61201 79634536
Pain in jaw 12.81 10.66 59 48592 46092 79649645
Red blood cell sedimentation rate increased 12.79 10.66 6 48645 45936 79649801
Pulmonary arterial hypertension 12.55 10.66 42 48609 28324 79667413
Carpal tunnel syndrome 12.54 10.66 33 48618 19495 79676242
Tubulointerstitial nephritis 12.28 10.66 4 48647 38231 79657506
Musculoskeletal stiffness 12.21 10.66 60 48591 174948 79520789
Sinus operation 12.17 10.66 11 48640 2514 79693223
Lactic acidosis 12.16 10.66 15 48636 70344 79625393
Suicidal ideation 12.13 10.66 84 48567 76256 79619481
Complex regional pain syndrome 12.05 10.66 10 48641 2038 79693699
Cardiac arrest 12.01 10.66 59 48592 172037 79523700
Discomfort 12.00 10.66 38 48613 125579 79570158
Eczema 11.94 10.66 53 48598 40765 79654972
Hyponatraemia 11.83 10.66 62 48589 177786 79517951
Stomatitis 11.63 10.66 48 48603 146709 79549028
Transient ischaemic attack 11.54 10.66 63 48588 52632 79643105
Atrophic vulvovaginitis 11.50 10.66 8 48643 1253 79694484
Transplant evaluation 11.50 10.66 9 48642 1688 79694049
Therapeutic product effect incomplete 11.43 10.66 46 48605 141599 79554138
Device breakage 11.30 10.66 22 48629 10653 79685084
Urticaria 11.27 10.66 167 48484 185034 79510703
Cytomegalovirus infection 11.22 10.66 6 48645 42638 79653099
Hereditary angioedema 11.18 10.66 15 48636 5320 79690417
Staphylococcal infection 11.01 10.66 67 48584 58228 79637509
Optic disc drusen 10.98 10.66 3 48648 44 79695693
Right ventricular systolic pressure increased 10.94 10.66 7 48644 955 79694782

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
FLONASENighttime Allergy Relief HUMAN OTC DRUG LABEL 1 0135-1329 TABLET 2.50 mg ORAL OTC monograph final 15 sections
Wal-Act HUMAN OTC DRUG LABEL 2 0363-0178 TABLET, FILM COATED 2.50 mg ORAL OTC monograph final 16 sections
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 0363-0287 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
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 0904-0250 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
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 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 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
HISTEX-DM HUMAN OTC DRUG LABEL 3 28595-804 SYRUP 2.50 mg ORAL OTC MONOGRAPH FINAL 16 sections
HISTEX PDX Drops HUMAN OTC DRUG LABEL 1 28595-808 SYRUP 1.25 mg ORAL OTC monograph final 17 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
Aprodine HUMAN OTC DRUG LABEL 2 50090-0622 TABLET, FILM COATED 2.50 mg ORAL OTC MONOGRAPH FINAL 17 sections