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

Stem definitionDrug idCAS RN
4411 25523-97-1

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • dexchlorpheniramine
  • (+)-Chloropheniramine
  • (+)-Chlorpheniramine
  • S-Chlorpheniramine
  • d-Chlorpheniramine
  • dexchlorpheniramine maleate
  • Molecular weight: 274.79
  • Formula: C16H19ClN2
  • CLOGP: 3.15
  • LIPINSKI: 0
  • HAC: 2
  • HDO: 0
  • TPSA: 16.13
  • ALOGS: -3.72
  • ROTB: 5

  • Status: OFP

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

Drug dosage:

DoseUnitRoute
6 mg O
6 mg P

ADMET properties:

PropertyValueReference
S (Water solubility) 3 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 1.592 High 1
caco2-efflux Caco-2 efflux ratio (BA/AB) 0.406 High 1
caco2-intrinsic-papp Caco-2 intrinsic apparent permeability 30.690 10^-6 cm/s High 1
dh-clint Dog hepatocyte intrinsic clearance 29.785 uL/min/10^6 cells High 1
dppb Dog plasma protein binding (% unbound) 46.550 % High 1
fcs-ppb Fetal calf serum protein binding (% unbound) 57.150 % High 1
herg hERG pIC50 5.375 pIC50 High 1
hh-clint Human hepatocyte intrinsic clearance 4.093 uL/min/10^6 cells High 1
hlm-clint Human liver microsomal intrinsic clearance 11.482 uL/min/mg protein High 1
hppb Human plasma protein binding (% unbound) 50.580 % High 1
kinase-safety-class ACVR2A,ACVR2B,AKT1,AKT2,AKT3,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK4,CDK5,CDK9,CHEK1,DDR1,DYRK1B,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,ITK,JAK2,JAK3,MAP3K21,MAP3K7,MAPK10,MAPK12,MAPK7,MET,NTRK2,PDK2,PDK4,PDPK1,PIM2,PRKCD,PRKDC,SIK2,SIK3,STK33,SYK,TEK,TGFBR1,TTK 44
kinase-selectivity-class AKT2,AKT3,AXL,EIF2AK3,PDK4,PRKCD,STK33 7
mdck-mdr1-bcrp-efflux MDCK-MDR1-BCRP efflux ratio 0.490 High 1
mdck-mdr1-efflux MDCK-MDR1 efflux ratio 0.306 High 1
mh-clint Mouse hepatocyte intrinsic clearance 87.498 High 1
mppb Mouse plasma protein binding (% unbound) 45.070 High 1
nih-mdck-mdr1-efflux NIH MDCK-MDR1 efflux ratio 1.038 High 1
pfas-class PFAS structural alert (1 = True, 0 = False) 0
pppb Pig plasma protein binding (% unbound) 64.380 % High 1
rat-kpuu-brain Rat brain Kpuu 1.854 % High 1
rh-clint Rat hepatocyte intrinsic clearance 84.528 uL/min/10^6 cells High 1
rh-fuinc Rat hepatocyte fraction unbound in incubation 75.300 % High 1
rppb Rat plasma protein binding (% unbound) 46.720 % High 1
solubility-dd Solubility at pH 7.4 in DMSO 950.605 uM High 1

Approvals:

DateAgencyCompanyOrphan
July 14, 1981 FDA

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
Erythema 384.43 26.33 269 10179 228977 90389022
Cytokine release syndrome 317.87 26.33 120 10328 27853 90590146
Infusion related reaction 200.76 26.33 243 10205 416537 90201462
Anaphylactic shock 199.38 26.33 89 10359 31528 90586471
Febrile neutropenia 170.36 26.33 143 10305 158206 90459793
Hepatocellular injury 168.25 26.33 77 10371 28881 90589118
Rash maculo-papular 151.43 26.33 80 10368 40853 90577146
Oxygen saturation decreased 115.34 26.33 97 10351 107386 90510613
Hypersensitivity 100.30 26.33 184 10264 454493 90163506
Sense of oppression 96.76 26.33 23 10425 1077 90616922
Neutropenia 88.68 26.33 119 10329 224785 90393214
Pyrexia 88.43 26.33 218 10230 660267 89957732
Neutrophil count decreased 88.14 26.33 70 10378 71462 90546537
Anaphylactic reaction 77.80 26.33 71 10377 87453 90530546
Hypotension 74.56 26.33 134 10314 325263 90292736
Fatigue 70.26 26.33 23 10425 1154000 89463999
Bronchospasm 66.85 26.33 37 10411 20672 90597327
Dyspnoea 64.57 26.33 235 10213 880720 89737279
Hepatic cytolysis 62.78 26.33 41 10407 30875 90587124
Lymphopenia 60.78 26.33 36 10412 22845 90595154
Febrile bone marrow aplasia 60.02 26.33 27 10421 9711 90608288
Chest discomfort 57.22 26.33 75 10373 138290 90479709
Hyperthermia 55.38 26.33 26 10422 10309 90607690
Type I hypersensitivity 55.13 26.33 20 10428 4135 90613864
Anaphylactoid reaction 53.72 26.33 20 10428 4448 90613551
Face oedema 52.48 26.33 33 10415 23285 90594714
Tachycardia 51.06 26.33 76 10372 157597 90460402
Serum sickness 50.57 26.33 18 10430 3524 90614475
Hepatic function abnormal 50.05 26.33 42 10406 46246 90571753
Chills 49.16 26.33 68 10380 131913 90486086
Toxic skin eruption 47.69 26.33 27 10421 15747 90602252
Drug ineffective 47.61 26.33 54 10394 1384244 89233755
Pain 46.30 26.33 29 10419 996312 89621687
Platelet count decreased 44.31 26.33 66 10382 136903 90481096
Cytomegalovirus infection 43.82 26.33 31 10417 26571 90591428
Hypoxia 42.65 26.33 47 10401 72352 90545647
Endocrine toxicity 42.32 26.33 7 10441 46 90617953
Diffuse large B-cell lymphoma refractory 41.00 26.33 13 10435 1787 90616212
Immune effector cell-associated neurotoxicity syndrome 38.78 26.33 17 10431 5751 90612248
Abdominal discomfort 38.16 26.33 5 10443 477323 90140676
Drug intolerance 37.48 26.33 4 10444 447587 90170412
Acute polyneuropathy 37.24 26.33 9 10439 452 90617547
Swelling 37.07 26.33 3 10445 419055 90198944
Hypogammaglobulinaemia 37.01 26.33 20 10428 10654 90607345
Peripheral sensory neuropathy 36.81 26.33 19 10429 9231 90608768
Livedo reticularis 36.23 26.33 14 10434 3445 90614554
Thrombocytopenia 34.45 26.33 75 10373 208650 90409349
Organising pneumonia 34.31 26.33 17 10431 7580 90610419
Mixed liver injury 34.25 26.33 17 10431 7606 90610393
Oropharyngeal discomfort 34.02 26.33 17 10431 7718 90610281
Peripheral swelling 33.81 26.33 4 10444 413102 90204897
Cholestasis 33.31 26.33 30 10418 36269 90581730
Drug reaction with eosinophilia and systemic symptoms 32.82 26.33 32 10416 42726 90575273
Wrong patient received product 32.64 26.33 13 10435 3464 90614535
Cryoglobulinaemia 32.21 26.33 9 10439 801 90617198
White blood cell count decreased 32.20 26.33 64 10384 167045 90450954
Enterocolitis 31.83 26.33 18 10430 10472 90607527
Agranulocytosis 30.30 26.33 28 10420 34974 90583025
Pruritus 30.26 26.33 133 10315 541392 90076607
Hypothermia 30.02 26.33 20 10428 15555 90602444
Weight increased 29.77 26.33 6 10442 417921 90200078
Venous oxygen saturation increased 29.59 26.33 5 10443 38 90617961
Interstitial lung disease 29.38 26.33 40 10408 76365 90541634
Skin reaction 29.13 26.33 21 10427 18532 90599467
Feeling hot 28.74 26.33 40 10408 77968 90540031
Capillary leak syndrome 28.27 26.33 11 10437 2756 90615243
Psychiatric decompensation 28.22 26.33 10 10438 1933 90616066
Alopecia 28.07 26.33 11 10437 495060 90122939
Cardiac failure 27.47 26.33 47 10401 109449 90508550
Persecutory delusion 26.69 26.33 11 10437 3197 90614802
Angioedema 26.53 26.33 35 10413 64841 90553158

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
Cytokine release syndrome 458.23 21.81 224 10604 44303 42566204
Infusion related reaction 198.18 21.81 146 10682 60660 42549847
Febrile neutropenia 167.30 21.81 220 10608 185483 42425024
Febrile bone marrow aplasia 163.67 21.81 70 10758 10111 42600396
Pyrexia 148.37 21.81 315 10513 393727 42216780
Hypogammaglobulinaemia 146.97 21.81 68 10760 11823 42598684
Erythema 145.88 21.81 158 10670 108635 42501872
Neutropenia 126.32 21.81 200 10628 199231 42411276
Hypersensitivity 101.98 21.81 108 10720 72262 42538245
Blood immunoglobulin G decreased 100.55 21.81 33 10795 2281 42608226
Anaphylactic shock 86.84 21.81 61 10767 23456 42587051
Alveolar lung disease 77.78 21.81 19 10809 443 42610064
Pulmonary interstitial emphysema syndrome 74.05 21.81 19 10809 544 42609963
Fibrin D dimer increased 63.10 21.81 29 10799 4956 42605551
Fatigue 62.24 21.81 17 10811 435624 42174883
Generalised oedema 61.83 21.81 42 10786 15294 42595213
Neutrophil count decreased 58.17 21.81 76 10752 63339 42547168
Eosinophilia 55.21 21.81 54 10774 32845 42577662
Hyperthermia 54.44 21.81 36 10792 12538 42597969
Diffuse alveolar damage 48.95 21.81 20 10808 2572 42607935
Drug ineffective 47.94 21.81 54 10774 630143 41980364
Septic shock 47.22 21.81 84 10744 91588 42518919
Toxicity to various agents 46.46 21.81 3 10825 229133 42381374
Hypotension 45.33 21.81 156 10672 257475 42353032
Oesophagitis 43.77 21.81 34 10794 15213 42595294
Blood immunoglobulin A decreased 43.00 21.81 13 10815 686 42609821
Chills 41.92 21.81 81 10747 93985 42516522
Hyperammonaemia 40.19 21.81 25 10803 7841 42602666
Rash maculo-papular 39.21 21.81 48 10780 37455 42573052
Tumour lysis syndrome 38.24 21.81 37 10791 22194 42588313
Face oedema 38.20 21.81 30 10798 13636 42596871
Sense of oppression 36.99 21.81 11 10817 548 42609959
Immune effector cell-associated neurotoxicity syndrome 35.98 21.81 25 10803 9436 42601071
Thrombocytopenia 34.98 21.81 117 10711 190162 42420345
Platelet count decreased 34.67 21.81 95 10733 138486 42472021
Urticaria 34.51 21.81 65 10763 73971 42536536
Necrotising retinitis 34.18 21.81 12 10816 1018 42609489
Eosinophilic pneumonia 34.14 21.81 19 10809 4855 42605652
Interstitial lung disease 33.05 21.81 66 10762 78396 42532111
Drug interaction 31.87 21.81 14 10814 266985 42343522
Kounis syndrome 31.72 21.81 16 10812 3352 42607155
Oxygen saturation decreased 31.66 21.81 58 10770 64629 42545878
Cytomegalovirus test positive 30.70 21.81 17 10811 4302 42606205
Anaphylactic reaction 29.89 21.81 45 10783 42698 42567809
Cardiac ventricular disorder 29.66 21.81 8 10820 279 42610228
Type I hypersensitivity 28.67 21.81 13 10815 2153 42608354
Staphylococcal bacteraemia 28.07 21.81 23 10805 11098 42599409
Disseminated intravascular coagulation 27.98 21.81 33 10795 24761 42585746
Acute coronary syndrome 27.96 21.81 26 10802 14839 42595668
Rash 26.22 21.81 139 10689 276815 42333692
C-reactive protein increased 26.20 21.81 53 10775 63507 42547000
Escherichia sepsis 26.20 21.81 17 10811 5730 42604777
Product dose omission issue 26.14 21.81 4 10824 154361 42456146
Abdominal compartment syndrome 26.02 21.81 10 10818 1095 42609412
Hepatic encephalopathy 25.74 21.81 26 10802 16416 42594091
Tumour flare 25.60 21.81 10 10818 1143 42609364
Bronchospasm 25.13 21.81 23 10805 12862 42597645
Malaise 24.71 21.81 113 10715 212043 42398464
Pain in extremity 23.14 21.81 5 10823 150599 42459908
Bronchitis 22.68 21.81 42 10786 47159 42563348
Sepsis 22.34 21.81 105 10723 199229 42411278
Anaphylactoid reaction 21.91 21.81 12 10816 2971 42607536

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
Cytokine release syndrome 768.69 20.61 340 21172 69966 110497821
Erythema 478.86 20.61 419 21093 291028 110276759
Infusion related reaction 333.94 20.61 390 21122 380772 110187015
Febrile neutropenia 321.51 20.61 350 21162 316417 110251370
Anaphylactic shock 252.82 20.61 145 21367 51401 110516386
Pyrexia 225.75 20.61 521 20991 897744 109670043
Neutropenia 223.32 20.61 317 21195 374303 110193484
Febrile bone marrow aplasia 185.80 20.61 83 21429 17382 110550405
Hypogammaglobulinaemia 180.89 20.61 85 21427 19991 110547796
Rash maculo-papular 166.06 20.61 128 21384 74094 110493693
Hypersensitivity 157.87 20.61 282 21230 403716 110164071
Neutrophil count decreased 149.93 20.61 149 21363 120792 110446995
Hepatocellular injury 146.46 20.61 102 21410 50540 110517247
Fatigue 129.97 20.61 38 21474 1215920 109351867
Sense of oppression 124.92 20.61 34 21478 1614 110566173
Oxygen saturation decreased 124.45 20.61 153 21359 156829 110410958
Hypotension 111.85 20.61 286 21226 523563 110044224
Hyperthermia 104.66 20.61 60 21452 21212 110546575
Chills 95.64 20.61 149 21363 190431 110377356
Anaphylactic reaction 94.77 20.61 114 21398 114186 110453601
Blood immunoglobulin G decreased 88.79 20.61 35 21477 5365 110562422
Platelet count decreased 86.17 20.61 158 21354 230285 110337502
Drug ineffective 81.85 20.61 106 21406 1520434 109047353
Pulmonary interstitial emphysema syndrome 78.69 20.61 19 21493 556 110567231
Type I hypersensitivity 76.46 20.61 33 21479 6360 110561427
Immune effector cell-associated neurotoxicity syndrome 76.23 20.61 43 21469 14739 110553048
Alveolar lung disease 74.47 20.61 19 21493 700 110567087
Toxicity to various agents 74.02 20.61 5 21507 480550 110087237
Thrombocytopenia 72.79 20.61 189 21323 348696 110219091
Anaphylactoid reaction 71.18 20.61 32 21480 6794 110560993
Face oedema 71.08 20.61 56 21456 33413 110534374
Bronchospasm 69.45 20.61 53 21459 30186 110537601
Septic shock 69.23 20.61 116 21396 157412 110410375
Hepatic function abnormal 67.45 20.61 85 21427 89210 110478577
Serum sickness 67.03 20.61 27 21485 4379 110563408
Tumour lysis syndrome 66.41 20.61 52 21460 30749 110537038
Fibrin D dimer increased 65.74 20.61 34 21478 9811 110557976
Peripheral swelling 62.81 20.61 4 21508 404030 110163757
Diffuse large B-cell lymphoma refractory 62.18 20.61 22 21490 2499 110565288
Eosinophilia 62.00 20.61 66 21446 57870 110509917
Pain 61.81 20.61 57 21455 954898 109612889
Interstitial lung disease 60.42 20.61 102 21410 139232 110428555
Hypoxia 59.08 20.61 97 21415 129418 110438369
Hepatic cytolysis 55.90 20.61 61 21451 54992 110512795
Cytomegalovirus infection 54.71 20.61 60 21452 54384 110513403
Dyspnoea 54.15 20.61 384 21128 1106488 109461299
White blood cell count decreased 53.80 20.61 130 21382 229260 110338527
Swelling 53.03 20.61 4 21508 351037 110216750
Lymphopenia 52.53 20.61 51 21461 40119 110527668
Toxic skin eruption 51.98 20.61 43 21469 27472 110540315
Tachycardia 49.51 20.61 125 21387 226520 110341267
Arthralgia 48.69 20.61 48 21464 779584 109788203
Drug intolerance 48.51 20.61 10 21502 406502 110161285
Oesophagitis 48.35 20.61 42 21470 28673 110539114
Generalised oedema 47.89 20.61 43 21469 30661 110537126
Product dose omission issue 47.67 20.61 4 21508 321778 110246009
Diffuse alveolar damage 45.50 20.61 20 21492 4027 110563760
Abdominal discomfort 44.36 20.61 11 21501 393847 110173940
Pain in extremity 43.77 20.61 20 21492 487098 110080689
Cytomegalovirus test positive 43.28 20.61 23 21489 7013 110560774
Enterocolitis 43.04 20.61 33 21479 18916 110548871
Hyperammonaemia 42.85 20.61 29 21483 13703 110554084
Sepsis 42.37 20.61 150 21362 327196 110240591
Urticaria 42.04 20.61 147 21365 318710 110249077
Weight increased 41.32 20.61 15 21497 419629 110148158
Mucosal inflammation 41.16 20.61 70 21442 96071 110471716
Disseminated intravascular coagulation 40.61 20.61 45 21467 41241 110526546
Acute coronary syndrome 39.31 20.61 34 21478 23078 110544709
Kounis syndrome 38.24 20.61 20 21492 5905 110561882
Sinusitis 38.19 20.61 6 21506 296682 110271105
Oropharyngeal discomfort 37.55 20.61 24 21488 10303 110557484
Hypothermia 37.44 20.61 35 21477 26267 110541520
Contraindicated product administered 37.01 20.61 3 21509 248264 110319523
Malaise 36.24 20.61 239 21273 671580 109896207
Chest discomfort 36 20.61 94 21418 173754 110394033
Triple negative breast cancer 35.82 20.61 10 21502 522 110567265
Peripheral sensory neuropathy 35.61 20.61 28 21484 16652 110551135
Pruritus 35.14 20.61 213 21299 581347 109986440
Endocrine toxicity 35.11 20.61 7 21505 81 110567706
Livedo reticularis 33.87 20.61 18 21494 5488 110562299
Haemophagocytic lymphohistiocytosis 33.84 20.61 36 21476 31523 110536264
Therapeutic product effect decreased 33.67 20.61 4 21508 244312 110323475
Pancytopenia 33.31 20.61 103 21409 209510 110358277
Acute pulmonary oedema 33.02 20.61 27 21485 16969 110550818
Condition aggravated 32.79 20.61 58 21454 734778 109833009
Alopecia 32.72 20.61 15 21497 364738 110203049
Necrotising retinitis 32.17 20.61 12 21500 1584 110566203
Eosinophilic pneumonia 31.89 20.61 19 21493 7208 110560579
Upper respiratory tract inflammation 31.81 20.61 16 21496 4355 110563432
Hypertension 31.55 20.61 188 21324 509896 110057891
Blood immunoglobulin A decreased 31.54 20.61 13 21499 2235 110565552
Cardiac failure 31.50 20.61 94 21418 187532 110380255
Hypoalbuminaemia 30.98 20.61 33 21479 28941 110538846
Gastrointestinal disorder 30.90 20.61 5 21507 241947 110325840
Cardiac ventricular disorder 30.18 20.61 8 21504 343 110567444
Dizziness 29.47 20.61 57 21455 698136 109869651
Musculoskeletal stiffness 29.28 20.61 9 21503 279813 110287974
Agranulocytosis 29.16 20.61 47 21465 61713 110506074
Acute kidney injury 28.94 20.61 217 21295 635213 109932574
Tumour flare 28.75 20.61 11 21501 1556 110566231
Erythrosis 28.57 20.61 7 21505 218 110567569
Feeling hot 28.53 20.61 58 21454 91048 110476739
Escherichia sepsis 28.08 20.61 20 21492 10252 110557535
Acute polyneuropathy 28.04 20.61 9 21503 759 110567028
Contusion 27.29 20.61 6 21506 233355 110334432
Venous oxygen saturation increased 26.98 20.61 5 21507 38 110567749
COVID-19 26.46 20.61 106 21406 244954 110322833
Cardio-respiratory arrest 26.44 20.61 65 21447 115771 110452016
Organising pneumonia 26.36 20.61 22 21490 14221 110553566
Erythema multiforme 26.12 20.61 26 21486 21071 110546716
Petit mal epilepsy 26.11 20.61 17 21495 7530 110560257
Anaemia 25.56 20.61 188 21324 546898 110020889
Blood cholesterol increased 25.52 20.61 3 21509 184782 110383005
Staphylococcal bacteraemia 25.29 20.61 23 21489 16665 110551122
Cholestasis 25.04 20.61 45 21467 64473 110503314
Pericarditis 24.89 20.61 6 21506 219108 110348679
Aspartate aminotransferase increased 24.86 20.61 78 21434 159858 110407929
Capillary leak syndrome 24.55 20.61 14 21498 4894 110562893
Asthma 24.53 20.61 9 21503 250282 110317505
Blister 24.36 20.61 7 21505 227369 110340418
Diffuse large B-cell lymphoma 24.27 20.61 22 21490 15876 110551911
Skin reaction 24.24 20.61 25 21487 21119 110546668
Larynx irritation 24.04 20.61 6 21506 202 110567585
Hyperamylasaemia 23.95 20.61 9 21503 1212 110566575
Therapeutic product effect incomplete 23.77 20.61 7 21505 223798 110343989
Maternal exposure during pregnancy 23.61 20.61 10 21502 254873 110312914
Cryoglobulinaemia 23.55 20.61 9 21503 1270 110566517
Cyanosis 23.55 20.61 29 21483 29712 110538075
Hepatic enzyme increased 23.36 20.61 17 21495 320875 110246912
Off label use 23.32 20.61 415 21097 1499770 109068017
Abdominal compartment syndrome 23.22 20.61 10 21502 1917 110565870
Migraine 23.18 20.61 3 21509 171649 110396138
Haemophilus bacteraemia 23.16 20.61 6 21506 235 110567552
Hepatic encephalopathy 23.10 20.61 28 21484 28228 110539559
Meningitis noninfective 23.04 20.61 6 21506 240 110567547
Depression 22.85 20.61 17 21495 317318 110250469
Osteoarthritis 22.81 20.61 4 21508 182619 110385168
Nasopharyngitis 22.64 20.61 26 21486 394335 110173452
Arthritis 22.46 20.61 3 21509 167583 110400204
Duodenal ulcer perforation 21.96 20.61 4 21508 177696 110390091
Rash 21.94 20.61 250 21262 820714 109747073
Drug reaction with eosinophilia and systemic symptoms 21.93 20.61 49 21463 82046 110485741
Hot flush 21.82 20.61 43 21469 65993 110501794
Dry mouth 21.71 20.61 6 21506 199942 110367845
Treatment failure 21.09 20.61 14 21498 277220 110290567
Alanine aminotransferase increased 21.05 20.61 81 21431 183692 110384095
Fall 20.78 20.61 55 21457 603427 109964360
Anxiety 20.63 20.61 22 21490 345056 110222731

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC R06AB02 RESPIRATORY SYSTEM
ANTIHISTAMINES FOR SYSTEMIC USE
ANTIHISTAMINES FOR SYSTEMIC USE
Substituted alkylamines
ATC R06AB52 RESPIRATORY SYSTEM
ANTIHISTAMINES FOR SYSTEMIC USE
ANTIHISTAMINES FOR SYSTEMIC USE
Substituted alkylamines
MeSH PA D006633 Histamine Antagonists
MeSH PA D006634 Histamine H1 Antagonists
MeSH PA D018377 Neurotransmitter Agents
MeSH PA D018494 Histamine Agents
CHEBI has role CHEBI:35705 immunosuppressive agent
CHEBI has role CHEBI:50857 anti-allergic agent
CHEBI has role CHEBI:66981 ophthalmology drug

Related Drugs by ATC class:

R06AB Substituted alkylamines 6 drugs

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
Urticaria indication 126485001
Seasonal allergic rhinitis indication 367498001
Itching of skin indication 418363000
Allergic conjunctivitis indication 473460002 DOID:11204
Brain damage contraindication 2470005
Ocular hypertension contraindication 4210003 DOID:9282
Tachyarrhythmia contraindication 6285003
Suicidal thoughts contraindication 6471006
Dependent drug abuse contraindication 6525002
Urinary tract obstruction contraindication 7163005 DOID:5200
Alcoholism contraindication 7200002
Alcohol withdrawal delirium contraindication 8635005
Peptic ulcer contraindication 13200003 DOID:750
Asthenia contraindication 13791008
Severe chronic ulcerative colitis contraindication 14311001
Constipation contraindication 14760008 DOID:2089
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
Alcohol intoxication contraindication 25702006
Shock contraindication 27942005
Toxic megacolon contraindication 28536002 DOID:1770
Atony of colon contraindication 29479008
Hypercapnia contraindication 29596007
Dehydration contraindication 34095006
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
Complete trisomy 21 syndrome contraindication 41040004 DOID:14250
Conduction disorder of the heart contraindication 44808001
Low blood pressure contraindication 45007003
Achalasia of esophagus contraindication 45564002 DOID:9164
Chronic heart failure contraindication 48447003
Bradycardia contraindication 48867003
Disorder of cardiovascular system contraindication 49601007 DOID:1287
Acidosis contraindication 51387008
Coronary arteriosclerosis contraindication 53741008 DOID:3393
Paralytic ileus contraindication 55525008 DOID:8442
Peptic reflux disease contraindication 57643001
Hepatic failure contraindication 59927004
Ulcerative colitis contraindication 64766004 DOID:8577
Arterial thrombosis contraindication 65198009
Drug AND/OR toxin-induced diarrhea contraindication 65979008
Substance abuse contraindication 66214007
Benign intracranial hypertension contraindication 68267002 DOID:11459
Poisoning by acetaminophen contraindication 70273001
Arteriosclerotic vascular disease contraindication 72092001
Diabetes mellitus contraindication 73211009 DOID:9351
Urethral stricture contraindication 76618002
Spastic paralysis contraindication 78403003
Disturbance of salivary secretion contraindication 78948009
Decreased respiratory function contraindication 80954004
Injury of head contraindication 82271004
Chronic idiopathic constipation contraindication 82934008
Cor pulmonale contraindication 83291003 DOID:8515
Hiatal hernia contraindication 84089009 DOID:12642
Epilepsy contraindication 84757009 DOID:1826
Pulmonary emphysema contraindication 87433001
Kidney disease contraindication 90708001 DOID:557
Myasthenia gravis contraindication 91637004 DOID:437
Acute abdominal pain contraindication 116290004
Procedure on urinary system contraindication 118677009
Gastrointestinal obstruction contraindication 126765001
Neoplasm of brain contraindication 126952004 DOID:1319
Seizure disorder contraindication 128613002
Autonomic dysreflexia contraindication 129618003
Bleeding contraindication 131148009
Drug-induced psychosis contraindication 191483003 DOID:1742
Partial atrioventricular block contraindication 195039008
Acute pancreatitis contraindication 197456007 DOID:2913
Myocardial dysfunction contraindication 233928007
Disease of liver contraindication 235856003 DOID:409
Bladder outflow obstruction contraindication 236645006
Morbid obesity contraindication 238136002 DOID:11981
Pyloric obstruction contraindication 244815007
Benign prostatic hyperplasia contraindication 266569009
Retention of urine contraindication 267064002
Drowsy contraindication 271782001
Exacerbation of asthma contraindication 281239006
Lesion of brain contraindication 301766008
Coma contraindication 371632003
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
Gastric ulcer contraindication 397825006 DOID:10808
Breastfeeding (mother) contraindication 413712001
Chronic lung disease contraindication 413839001
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 9.47 Basic
pKa2 4.14 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 9.14 CHEMBL CHEMBL
Sigma non-opioid intracellular receptor 1 Membrane receptor Ki 6.16 DRUG MATRIX
Sodium-dependent serotonin transporter Transporter Ki 7.89 DRUG MATRIX
Sodium-dependent noradrenaline transporter Transporter Ki 5.31 DRUG MATRIX
5-hydroxytryptamine receptor 2A GPCR Ki 5.98 DRUG MATRIX
5-hydroxytryptamine receptor 2C GPCR Ki 5.92 DRUG MATRIX
Alpha-2B adrenergic receptor GPCR Ki 5.68 DRUG MATRIX
Histamine H2 receptor GPCR Ki 5.09 DRUG MATRIX
Muscarinic acetylcholine receptor M1 GPCR Ki 6.48 DRUG MATRIX
Muscarinic acetylcholine receptor M2 GPCR Ki 5.60 DRUG MATRIX
Muscarinic acetylcholine receptor M3 GPCR Ki 6.26 DRUG MATRIX
Muscarinic acetylcholine receptor M4 GPCR Ki 6.56 DRUG MATRIX
Muscarinic acetylcholine receptor M5 GPCR Ki 6.13 DRUG MATRIX
Sodium-dependent dopamine transporter Transporter Ki 6.13 DRUG MATRIX
Alpha-1D adrenergic receptor GPCR Ki 4.78 DRUG MATRIX
Alpha-2A adrenergic receptor GPCR Ki 5.12 DRUG MATRIX
Alpha-1B adrenergic receptor GPCR Ki 5.07 DRUG MATRIX
Membrane-associated progesterone receptor component 1 Membrane receptor Ki 4.93 DRUG MATRIX

External reference:

IDSource
D07803 KEGG_DRUG
4019712 VUID
N0000147804 NUI
2438-32-6 SECONDARY_CAS_RN
4018792 VANDF
4019712 VANDF
C0057606 UMLSCUI
CHEBI:4464 CHEBI
CHEMBL1201353 ChEMBL_ID
CHEMBL1200927 ChEMBL_ID
DB13679 DRUGBANK_ID
C018904 MESH_SUPPLEMENTAL_RECORD_UI
955 INN_ID
3Q9Q0B929N UNII
33036 PUBCHEM_CID
DB09555 DRUGBANK_ID
22697 RXNORM
1479 MMSL
4556 MMSL
d00784 MMSL
003393 NDDF
004796 NDDF
16031005 SNOMEDCT_US
372663001 SNOMEDCT_US
68680008 SNOMEDCT_US
1210 IUPHAR_LIGAND_ID
3Q9Q0B929N INXIGHT DRUGS

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
RYMED HUMAN OTC DRUG LABEL 2 0485-0080 TABLET, COATED 2 mg ORAL OTC Monograph Drug 16 sections
RYCLORA HUMAN PRESCRIPTION DRUG LABEL 1 15370-150 LIQUID 2 mg ORAL ANDA 13 sections
POLY-HIST DM HUMAN OTC DRUG LABEL 2 50991-271 LIQUID 1 mg ORAL OTC Monograph Drug 9 sections
DELTUSS DMX Cough Suppressant Nasal Decongestant Antihistamine GRAPE Flavor HUMAN OTC DRUG LABEL 3 58238-225 LIQUID 1 mg ORAL OTC monograph final 16 sections
DELTUSS DP Nasal Decongestant Antihistamine CHERRY Flavor HUMAN OTC DRUG LABEL 2 58238-226 LIQUID 1 mg ORAL OTC monograph final 16 sections
VanaCof 2 HUMAN OTC DRUG LABEL 2 58809-190 SOLUTION 1 mg ORAL OTC Monograph Drug 16 sections
VANACOF HUMAN OTC DRUG LABEL 3 58809-999 LIQUID 1 mg ORAL OTC Monograph Drug 16 sections
VANACOF HUMAN OTC DRUG LABEL 3 58809-999 LIQUID 1 mg ORAL OTC Monograph Drug 16 sections
Dexchlorpheniramine Maleate, Phenylephrine HCl HUMAN OTC DRUG LABEL 2 66576-080 TABLET 2 mg ORAL OTC monograph final 8 sections
PRO-REDAC HUMAN OTC DRUG LABEL 3 66594-499 SYRUP 1 mg ORAL OTC monograph final 16 sections
WesTussin DM HUMAN OTC DRUG LABEL 3 69367-334 SYRUP 1 mg ORAL OTC MONOGRAPH DRUG 17 sections
Corphena HUMAN PRESCRIPTION DRUG LABEL 1 73684-300 SOLUTION 2 mg ORAL ANDA 13 sections