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

Stem definitionDrug idCAS RN
4484 320345-99-1

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • aclidinium bromide
  • Tudorza Pressair
  • aclidinium
  • LAS 34273
  • LAS W-330
a long-acting, inhaled antimuscarinic; in phase I trial 8/2008
  • Molecular weight: 484.65
  • Formula: C26H30NO4S2
  • CLOGP: 2.34
  • LIPINSKI: 0
  • HAC: 5
  • HDO: 1
  • TPSA: 55.76
  • ALOGS: -5.53
  • ROTB: 10
  • Status: OFP
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
0.64 mg Inhal.powder

ADMET properties:

PropertyValueReference
Vd (Volume of distribution) 4.30 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 48.50 mL/min/kg Lombardo F, Berellini G, Obach RS
BA (Bioavailability) 0.04 % Kawashima H, Watanabe R, Esaki T, Kuroda M, Nagao C, Natsume-Kitatani Y, Ohashi R, Komura H, Mizuguchi K

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
azlogd74 LogD at pH 7.4 1.350 High 1
caco2-efflux Caco-2 efflux ratio (BA/AB) 25.704 High 1
caco2-intrinsic-papp Caco-2 intrinsic apparent permeability 0.562 10^-6 cm/s High 1
dh-clint Dog hepatocyte intrinsic clearance 12.764 uL/min/10^6 cells High 1
dppb Dog plasma protein binding (% unbound) 9.620 % High 1
fcs-ppb Fetal calf serum protein binding (% unbound) 23.240 % High 1
herg hERG pIC50 5.295 pIC50 High 1
hh-clint Human hepatocyte intrinsic clearance 7.603 uL/min/10^6 cells High 1
hlm-clint Human liver microsomal intrinsic clearance 52.966 uL/min/mg protein High 1
hppb Human plasma protein binding (% unbound) 9.880 % High 1
kinase-safety-class ACVR2B,AXL,BRAF,BTK,CAMK2D,CDK5,CDK9,EIF2AK3,EPHB4,ERBB2,GRK2,ITK,MAPK10,MAPK7,NTRK2,PDK1,PDK2,PDK4,PIK3CB,PRKDC,TEK,TGFBR1 22
kinase-selectivity-class AXL,EIF2AK3,GRK2,PDK4,STK33,TEK 6
mdck-mdr1-bcrp-efflux MDCK-MDR1-BCRP efflux ratio 21.979 High 1
mdck-mdr1-efflux MDCK-MDR1 efflux ratio 6.745 High 1
mh-clint Mouse hepatocyte intrinsic clearance 69.502 High 1
mppb Mouse plasma protein binding (% unbound) 8.980 High 1
nih-mdck-mdr1-efflux NIH MDCK-MDR1 efflux ratio 11.722 High 1
pfas-class PFAS structural alert (1 = True, 0 = False) 0
pppb Pig plasma protein binding (% unbound) 25.480 % High 1
rat-kpuu-brain Rat brain Kpuu 0.027 % High 1
rh-clint Rat hepatocyte intrinsic clearance 147.571 uL/min/10^6 cells High 1
rh-fuinc Rat hepatocyte fraction unbound in incubation 45.860 % High 1
rppb Rat plasma protein binding (% unbound) 14.180 % High 1
solubility-dd Solubility at pH 7.4 in DMSO 847.227 uM High 1

Approvals:

DateAgencyCompanyOrphan
July 20, 2012 EMA
July 23, 2012 FDA ASTRAZENECA PHARMS

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
Nasal polyps 660.68 33.88 183 15227 10697 90602340
Bronchiectasis 613.83 33.88 204 15206 22126 90590911
Obstructive airways disorder 595.98 33.88 207 15203 25662 90587375
Asthma-chronic obstructive pulmonary disease overlap syndrome 477.72 33.88 120 15290 4779 90608258
Total lung capacity increased 464.90 33.88 118 15292 4903 90608134
Sarcoidosis 381.06 33.88 119 15291 10554 90602483
Rhinitis allergic 324.48 33.88 118 15292 16667 90596370
Cardiac murmur 315.20 33.88 118 15292 18076 90594961
Wheezing 298.03 33.88 277 15133 237803 90375234
Lung neoplasm malignant 272.17 33.88 115 15295 24158 90588879
Urinary tract discomfort 262.30 33.88 54 15356 858 90612179
Alveolar osteitis 248.57 33.88 54 15356 1123 90611914
Jaundice cholestatic 237.39 33.88 82 15328 9961 90603076
Hypomania 235.19 33.88 79 15331 8818 90604219
Polymyalgia rheumatica 231.27 33.88 68 15342 4909 90608128
Tunnel vision 228.78 33.88 54 15356 1647 90611390
Chronic obstructive pulmonary disease 220.45 33.88 144 15266 73685 90539352
Animal scratch 219.70 33.88 53 15357 1777 90611260
Asthma 213.21 33.88 233 15177 241927 90371110
Sinus pain 213.07 33.88 65 15345 5324 90607713
Schizophrenia 205.79 33.88 82 15328 14832 90598205
Bladder pain 203.27 33.88 54 15356 2683 90610354
Ear congestion 191.01 33.88 54 15356 3388 90609649
Bronchopulmonary aspergillosis allergic 190.66 33.88 55 15355 3711 90609326
Gastrooesophageal reflux disease 189.65 33.88 184 15226 166153 90446884
Myopathy 185.38 33.88 74 15336 13444 90599593
Full blood count abnormal 178.66 33.88 98 15312 36499 90576538
Wound complication 173.69 33.88 54 15356 4709 90608328
Blood iron decreased 171.52 33.88 76 15334 17883 90595154
Wound secretion 171.22 33.88 54 15356 4936 90608101
Paranasal sinus discomfort 159.61 33.88 54 15356 6156 90606881
Device malfunction 151.10 33.88 73 15337 20904 90592133
Productive cough 150.41 33.88 116 15294 76947 90536090
Psychotic disorder 147.94 33.88 82 15328 31148 90581889
Dyspnoea 147.75 33.88 403 15007 880552 89732485
Sputum discoloured 143.97 33.88 70 15340 20321 90592716
Sinus disorder 140.45 33.88 82 15328 34365 90578672
Drug dependence 136.17 33.88 76 15334 29251 90583786
Cough 135.08 33.88 232 15178 368730 90244307
Limb injury 131.09 33.88 76 15334 31432 90581605
Pneumonia 128.50 33.88 313 15097 637746 89975291
Hyper IgE syndrome 128.38 33.88 27 15383 478 90612559
Rales 125.96 33.88 59 15351 15768 90597269
Blood bilirubin increased 125.32 33.88 83 15327 43387 90569650
Restrictive pulmonary disease 121.81 33.88 35 15375 2327 90610710
Blood urine present 121.03 33.88 59 15351 17219 90595818
Hepatotoxicity 118.94 33.88 82 15328 45760 90567277
Hypoaesthesia oral 114.49 33.88 55 15355 15545 90597492
Hypokinesia 114.17 33.88 55 15355 15642 90597395
Body temperature increased 113.71 33.88 79 15331 44631 90568406
Cholelithiasis 111.17 33.88 83 15327 52423 90560614
Hypoacusis 89.64 33.88 57 15353 27793 90585244
Skin laceration 88.09 33.88 55 15355 25980 90587057
Panic attack 84.95 33.88 54 15356 26311 90586726
Feeling cold 82.93 33.88 54 15356 27411 90585626
Dysuria 82.76 33.88 62 15348 39339 90573698
Calculus urinary 82.40 33.88 24 15386 1674 90611363
Movement disorder 80.22 33.88 54 15356 28965 90584072
Joint injury 79.04 33.88 56 15354 32608 90580429
Oedema peripheral 76.23 33.88 148 15262 257767 90355270
Bronchitis chronic 75.72 33.88 29 15381 4714 90608323
Pollakiuria 73.95 33.88 54 15356 32951 90580086
Procedural pain 73.43 33.88 54 15356 33306 90579731
Haematuria 73.42 33.88 55 15355 34882 90578155
Breath sounds abnormal 71.75 33.88 40 15370 15346 90597691
Occupational asthma 71.72 33.88 14 15396 167 90612870
Heart rate increased 71.54 33.88 92 15318 112810 90500227
Polycystic ovaries 70.78 33.88 29 15381 5625 90607412
Bronchitis 69.17 33.88 106 15304 152821 90460216
Joint swelling 66.59 33.88 5 15405 503295 90109742
Fatigue 65.74 33.88 60 15350 1153963 89459074
Chills 64.70 33.88 95 15315 131886 90481151
Blood pressure systolic increased 63.47 33.88 63 15347 58282 90554755
Middle insomnia 63.34 33.88 38 15372 16713 90596324
Neurosensory hypoacusis 62.70 33.88 13 15397 214 90612823
Influenza 60.83 33.88 95 15315 139169 90473868
Emphysema 60.53 33.88 33 15377 12122 90600915
Nephrolithiasis 59.02 33.88 56 15354 49029 90564008
Blood test abnormal 57.93 33.88 39 15371 20913 90592124
Coronary artery disease 57.79 33.88 47 15363 33576 90579461
Dyslipidaemia 57.54 33.88 30 15380 10077 90602960
Cardiac failure 56.84 33.88 81 15329 109415 90503622
Forced expiratory volume decreased 56.79 33.88 25 15385 5783 90607254
Oesophageal dilatation 56.76 33.88 14 15396 515 90612522
Influenza like illness 56.33 33.88 69 15341 80542 90532495
Infusion related reaction 55.52 33.88 4 15406 416776 90196261
Ear pain 51.42 33.88 56 15354 57646 90555391
Therapeutic product effect incomplete 50.94 33.88 106 15304 193790 90419247
Confusional state 50.60 33.88 4 15406 386201 90226836
Choking 49.96 33.88 29 15381 12004 90601033
Skin lesion 49.50 33.88 45 15365 37320 90575717
Dysarthria 48.77 33.88 53 15357 54429 90558608
Pneumothorax spontaneous 48.71 33.88 14 15396 931 90612106
Female sterilisation 48.46 33.88 13 15397 670 90612367
Lipohypertrophy 47.44 33.88 13 15397 726 90612311
Crepitations 46.77 33.88 25 15385 8827 90604210
Glaucoma 46.58 33.88 34 15376 20721 90592316
Abdominal discomfort 46.38 33.88 12 15398 477316 90135721
Swelling 45.89 33.88 8 15402 419050 90193987
Burning sensation 45.44 33.88 55 15355 63397 90549640
Incorrect dose administered 44.85 33.88 61 15349 78869 90534168
Pulmonary function test decreased 42.83 33.88 19 15391 4475 90608562
Dyspnoea exertional 42.80 33.88 57 15353 72231 90540806
Stress urinary incontinence 42.78 33.88 16 15394 2436 90610601
Angioplasty 42.55 33.88 14 15396 1463 90611574
Hypoaesthesia 41.87 33.88 3 15407 314207 90298830
Oropharyngeal pain 41.41 33.88 72 15338 115115 90497922
Breast conserving surgery 41.38 33.88 13 15397 1172 90611865
Intentional device misuse 40.90 33.88 12 15398 858 90612179
Cellulitis 40.83 33.88 63 15347 91274 90521763
Drug ineffective 40.70 33.88 112 15298 1384186 89228851
Vital capacity decreased 39.69 33.88 14 15396 1805 90611232
Haemoglobin decreased 39.58 33.88 86 15324 161870 90451167
Abscess 38.04 33.88 29 15381 18862 90594175
Chest discomfort 37.92 33.88 77 15333 138288 90474749
Sleep apnoea syndrome 37.74 33.88 36 15374 31711 90581326
Breast neoplasm 37.71 33.88 13 15397 1567 90611470
Rheumatoid arthritis 37.41 33.88 8 15402 362606 90250431
Lower respiratory tract infection 36.12 33.88 109 15301 250550 90362487
Rash 35.81 33.88 50 15360 796050 89816987
Restless legs syndrome 35.67 33.88 30 15380 22440 90590597
Stomatitis 35.53 33.88 3 15407 274695 90338342
Eczema 34.91 33.88 44 15366 52826 90560211
Pseudomonas infection 34.83 33.88 25 15385 14840 90598197

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
Wheezing 259.14 28.66 137 6201 54644 42560353
Breath sounds abnormal 256.75 28.66 88 6250 12005 42602992
Chronic obstructive pulmonary disease 240.95 28.66 137 6201 62977 42552020
Obstructive airways disorder 227.98 28.66 98 6240 24661 42590336
Congenital hiatus hernia 221.70 28.66 67 6271 6107 42608890
Malignant melanoma in situ 214.89 28.66 55 6283 2712 42612285
Asthma 213.20 28.66 126 6212 62188 42552809
Dyspnoea 202.38 28.66 285 6053 442336 42172661
Productive cough 188.80 28.66 109 6229 51458 42563539
Bronchiectasis 188.07 28.66 78 6260 17941 42597056
Full blood count abnormal 173.80 28.66 86 6252 29790 42585207
Joint injury 171.84 28.66 69 6269 14607 42600390
Micturition urgency 171.33 28.66 65 6273 11833 42603164
Hypercholesterolaemia 170.02 28.66 66 6272 12783 42602214
Dyspnoea exertional 167.74 28.66 100 6238 50048 42564949
Benign prostatic hyperplasia 154.12 28.66 71 6267 20981 42594016
Therapeutic product effect incomplete 152.19 28.66 107 6231 70832 42544165
Loss of personal independence in daily activities 135.22 28.66 87 6251 49729 42565268
Transient ischaemic attack 117.21 28.66 69 6269 33670 42581327
Gastrooesophageal reflux disease 103.68 28.66 71 6267 44952 42570045
Device malfunction 94.64 28.66 43 6295 12284 42602713
Coronary artery disease 88.06 28.66 69 6269 53651 42561346
Mycobacterium test positive 65.43 28.66 15 6323 461 42614536
Hypertension 63.09 28.66 99 6239 167105 42447892
Bronchial obstruction 63.04 28.66 19 6319 1710 42613287
Intentional device misuse 62.00 28.66 13 6325 261 42614736
Lung diffusion test decreased 56.29 28.66 15 6323 864 42614133
Nephrectomy 55.82 28.66 15 6323 892 42614105
Lung diffusion disorder 55.61 28.66 11 6327 163 42614834
Inguinal hernia repair 48.97 28.66 11 6327 308 42614689
Fungal disease carrier 46.22 28.66 11 6327 399 42614598
Carotid arteriosclerosis 45.67 28.66 16 6322 2316 42612681
Product quality issue 45.41 28.66 30 6308 17852 42597145
Bronchiolitis 41.00 28.66 17 6321 3889 42611108
Obstruction 37.70 28.66 15 6323 3088 42611909
Lower respiratory tract infection 37.55 28.66 38 6300 41168 42573829
Oropharyngeal candidiasis 37.30 28.66 11 6327 918 42614079
Granuloma 37.13 28.66 16 6322 4025 42610972
Chest discomfort 34.74 28.66 45 6293 63571 42551426
Cough 32.95 28.66 78 6260 178025 42436972
Blood immunoglobulin E increased 32.15 28.66 14 6324 3611 42611386
Pulmonary mass 31.25 28.66 23 6315 16242 42598755
Eosinophilic bronchitis 29.54 28.66 7 6331 249 42614748
Pulmonary eosinophilia 28.87 28.66 7 6331 275 42614722

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
Bronchiectasis 762.33 27.72 274 19214 36219 110533592
Obstructive airways disorder 696.16 27.72 273 19215 45876 110523935
Nasal polyps 619.02 27.72 183 19305 13017 110556794
Total lung capacity increased 468.30 27.72 120 19368 4992 110564819
Wheezing 465.95 27.72 374 19114 254856 110314955
Asthma-chronic obstructive pulmonary disease overlap syndrome 451.98 27.72 122 19366 6222 110563589
Chronic obstructive pulmonary disease 440.37 27.72 261 19227 108897 110460914
Asthma 370.24 27.72 325 19163 249966 110319845
Sarcoidosis 365.55 27.72 121 19367 12458 110557353
Rhinitis allergic 327.31 27.72 122 19366 17800 110552011
Breath sounds abnormal 296.03 27.72 125 19363 25279 110544532
Full blood count abnormal 293.26 27.72 159 19329 55893 110513918
Cardiac murmur 283.04 27.72 120 19368 24508 110545303
Productive cough 282.38 27.72 201 19287 114104 110455707
Gastrooesophageal reflux disease 278.56 27.72 240 19248 179736 110390075
Lung neoplasm malignant 240.52 27.72 118 19370 33724 110536087
Urinary tract discomfort 239.33 27.72 51 19437 929 110568882
Alveolar osteitis 234.16 27.72 51 19437 1034 110568777
Dyspnoea 233.45 27.72 564 18924 1106308 109463503
Hypomania 229.34 27.72 81 19407 10129 110559682
Joint injury 221.89 27.72 118 19370 39876 110529935
Congenital hiatus hernia 213.48 27.72 68 19420 6191 110563620
Jaundice cholestatic 211.51 27.72 84 19404 14524 110555287
Tunnel vision 202.75 27.72 51 19437 1964 110567847
Animal scratch 201.79 27.72 50 19438 1809 110568002
Polymyalgia rheumatica 199.33 27.72 65 19423 6377 110563434
Sinus pain 192.82 27.72 62 19426 5817 110563994
Malignant melanoma in situ 192.03 27.72 55 19433 3487 110566324
Bladder pain 186.02 27.72 51 19437 2754 110567057
Schizophrenia 179.05 27.72 84 19404 21742 110548069
Ear congestion 172.53 27.72 51 19437 3614 110566197
Benign prostatic hyperplasia 155.21 27.72 72 19416 18162 110551649
Blood iron decreased 154.68 27.72 73 19415 19141 110550670
Coronary artery disease 149.68 27.72 114 19374 71576 110498235
Dyspnoea exertional 147.22 27.72 132 19356 103928 110465883
Wound complication 146.35 27.72 51 19437 6126 110563685
Myopathy 145.09 27.72 76 19412 24884 110544927
Paranasal sinus discomfort 144.54 27.72 51 19437 6354 110563457
Wound secretion 140.83 27.72 51 19437 6850 110562961
Bronchopulmonary aspergillosis allergic 138.03 27.72 53 19435 8373 110561438
Micturition urgency 136.14 27.72 67 19421 19253 110550558
Therapeutic product effect incomplete 131.70 27.72 179 19309 223626 110346185
Cough 131.37 27.72 266 19222 461375 110108436
Sinus disorder 125.86 27.72 76 19412 32652 110537159
Transient ischaemic attack 121.07 27.72 96 19392 63886 110505925
Hyper IgE syndrome 119.37 27.72 27 19461 654 110569157
Restrictive pulmonary disease 113.58 27.72 36 19452 3223 110566588
Psychotic disorder 112.97 27.72 84 19404 50853 110518958
Sputum discoloured 112.93 27.72 67 19421 27878 110541933
Limb injury 111.25 27.72 74 19414 37562 110532249
Loss of personal independence in daily activities 102.18 27.72 129 19359 149891 110419920
Cholelithiasis 98.77 27.72 85 19403 63337 110506474
Hepatotoxicity 96.77 27.72 84 19404 63316 110506495
Hypoaesthesia oral 96.62 27.72 51 19437 16951 110552860
Rales 96.54 27.72 58 19430 24681 110545130
Blood urine present 92.44 27.72 56 19432 24189 110545622
Drug dependence 92.37 27.72 74 19414 49946 110519865
Body temperature increased 90.67 27.72 76 19412 54637 110515174
Hypokinesia 87.32 27.72 52 19436 21774 110548037
Blood bilirubin increased 85.63 27.72 85 19403 75887 110493924
Device malfunction 84.71 27.72 54 19434 25504 110544307
Pneumonia 82.78 27.72 339 19149 876375 109693436
Polycystic ovaries 74.40 27.72 29 19459 4767 110565044
Bronchitis 73.85 27.72 113 19375 156919 110412892
Skin laceration 73.35 27.72 55 19433 33698 110536113
Panic attack 71.59 27.72 51 19437 28889 110540922
Lung neoplasm 69.06 27.72 32 19456 8044 110561767
Emphysema 68.61 27.72 43 19445 19713 110550098
Feeling cold 68.60 27.72 53 19435 33934 110535877
Calculus urinary 66.96 27.72 24 19464 3128 110566683
Hypoacusis 64.83 27.72 52 19436 35139 110534672
Middle insomnia 64.68 27.72 42 19446 20460 110549351
Hypercholesterolaemia 63.23 27.72 79 19409 90758 110479053
Procedural pain 62.24 27.72 51 19437 35514 110534297
Lower respiratory tract infection 61.86 27.72 134 19354 242972 110326839
Movement disorder 61.20 27.72 51 19437 36353 110533458
Heart rate increased 60.01 27.72 98 19390 143736 110426075
Joint swelling 59.44 27.72 5 19483 442840 110126971
Mycobacterium test positive 58.45 27.72 15 19473 626 110569185
Dysuria 58.11 27.72 62 19426 60169 110509642
Oedema peripheral 57.74 27.72 157 19331 328503 110241308
Neurosensory hypoacusis 55.00 27.72 12 19476 245 110569566
Fatigue 54.94 27.72 81 19407 1215877 109353934
Sleep disorder due to a general medical condition 54.49 27.72 56 19432 52056 110517755
Chest discomfort 53.89 27.72 104 19384 173744 110396067
Pollakiuria 52.68 27.72 51 19437 44144 110525667
Infusion related reaction 51.99 27.72 4 19484 381158 110188653
Toxicity to various agents 51.37 27.72 11 19477 480544 110089267
Neutropenia 50.90 27.72 4 19484 374616 110195195
Influenza like illness 50.83 27.72 70 19418 88342 110481469
Drug ineffective 49.73 27.72 123 19365 1520417 109049394
Confusional state 49.55 27.72 11 19477 468669 110101142
Crepitations 49.12 27.72 28 19460 10807 110559004
Forced expiratory volume decreased 49.11 27.72 30 19458 13146 110556665
Influenza 48.59 27.72 98 19390 169003 110400808
Blood pressure systolic increased 48.15 27.72 66 19422 82925 110486886
Lung diffusion disorder 47.99 27.72 11 19477 283 110569528
Ear pain 46.49 27.72 52 19436 53174 110516637
Hypercapnia 45.71 27.72 27 19461 11132 110558679
Bronchial obstruction 45.58 27.72 18 19470 3061 110566750
Choking 45.34 27.72 30 19458 15080 110554731
Inguinal hernia repair 45.10 27.72 11 19477 372 110569439
Breast conserving surgery 44.35 27.72 13 19475 894 110568917
Lung diffusion test decreased 44.31 27.72 15 19473 1650 110568161
Fungal disease carrier 42.37 27.72 11 19477 481 110569330
Cellulitis 42.28 27.72 78 19410 125938 110443873
Blood test abnormal 41.88 27.72 37 19451 28517 110541294
Angioplasty 41.84 27.72 15 19473 1956 110567855
Thrombocytopenia 41.60 27.72 6 19482 348879 110220932
Dyslipidaemia 41.49 27.72 29 19459 15936 110553875
Acute kidney injury 41.33 27.72 31 19457 635399 109934412
Nephrolithiasis 40.45 27.72 54 19434 66158 110503653
Chills 39.57 27.72 97 19391 190483 110379328
Pneumothorax spontaneous 39.22 27.72 14 19474 1803 110568008
Pulmonary mass 38.84 27.72 40 19448 37261 110532550
Carotid arteriosclerosis 38.80 27.72 16 19472 3041 110566770
Lipohypertrophy 38.76 27.72 12 19476 994 110568817
Breast neoplasm 38.17 27.72 12 19476 1046 110568765
Kyphosis 38.16 27.72 16 19472 3171 110566640
Nephrectomy 37.57 27.72 15 19473 2625 110567186
Incorrect dose administered 37.12 27.72 66 19422 103575 110466236
Sleep apnoea syndrome 36.15 27.72 40 19448 40407 110529404
Intentional device misuse 36.11 27.72 11 19477 863 110568948
Rheumatoid arthritis 36.07 27.72 5 19483 299608 110270203
Burning sensation 35.64 27.72 52 19436 69160 110500651
Haematuria 35.20 27.72 57 19431 82948 110486863
Hypertension 35.09 27.72 180 19308 509904 110059907
Skin lesion 34.48 27.72 44 19444 51587 110518224
Oropharyngeal pain 33.73 27.72 74 19414 135202 110434609
Abdominal discomfort 33.07 27.72 14 19474 393844 110175967
Pulmonary function test decreased 32.91 27.72 20 19468 8680 110561131
Bronchiolitis 32.69 27.72 17 19471 5476 110564335
Swelling 31.93 27.72 11 19477 351030 110218781
Completed suicide 31.79 27.72 3 19485 242378 110327433
Balance disorder 31.63 27.72 66 19422 116494 110453317
Rash 31.17 27.72 61 19427 820903 109748908
Musculoskeletal stiffness 30.72 27.72 6 19482 279816 110289995
Restless legs syndrome 30.44 27.72 29 19459 24597 110545214
Wrist fracture 30.22 27.72 23 19465 14394 110555417
Intentional product use issue 30.16 27.72 4 19484 247902 110321909
Obstruction 29.16 27.72 16 19472 5736 110564075
Pain 28.99 27.72 80 19408 954875 109614936
Febrile neutropenia 28.68 27.72 10 19478 316757 110253054
Eczema 28.44 27.72 48 19440 72245 110497566
Cardiac failure 28.39 27.72 85 19403 187541 110382270
Chronic sinusitis 28.12 27.72 28 19460 25056 110544755
Peripheral vascular disorder 28.11 27.72 18 19470 8558 110561253
Abscess 27.77 27.72 29 19459 27440 110542371

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC R03AL05 RESPIRATORY SYSTEM
DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES
ADRENERGICS, INHALANTS
Adrenergics in combination with anticholinergics incl. triple combinations with corticosteroids
ATC R03BB05 RESPIRATORY SYSTEM
DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES
OTHER DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES, INHALANTS
Anticholinergics
FDA MoA N0000175370 Cholinergic Antagonists
FDA EPC N0000175574 Anticholinergic
CHEBI has role CHEBI:35523 bronchodilator agent
CHEBI has role CHEBI:48876 muscarinic antagonist
CHEBI has role CHEBI:53784 antispasmodic drug

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beclometasone dipropionatebudesonidefenoterolfluticasone furoateformoterolglycopyrronium bromideindacaterolipratropiummometasone furoateolodaterolsalbutamoltiotropium bromide show all 14 →
R03BB Anticholinergics 6 drugs
glycopyrronium bromideipratropiumoxitropiumrevefenacintiotropium bromideumeclidinium

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

DiseaseRelationSNOMED_IDDOID
Chronic obstructive lung disease indication 13645005 DOID:3083




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 13.97 acidic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
0.4MG/INH TUDORZA PRESSAIR AZURITY N202450 July 23, 2012 RX POWDER, METERED INHALATION 10085974 March 13, 2029 MAINTENANCE TREATMENT OF CHRONIC OBSTRUCTIVE PULMONARY DISEASE (COPD)
0.4MG/INH TUDORZA PRESSAIR AZURITY N202450 July 23, 2012 RX POWDER, METERED INHALATION 11000517 March 13, 2029 MAINTENANCE TREATMENT OF CHRONIC OBSTRUCTIVE PULMONARY DISEASE (COPD)
0.4MG/INH;0.012MG/INH DUAKLIR PRESSAIR AZURITY N210595 March 29, 2019 RX POWDER, METERED INHALATION 10085974 March 13, 2029 MAINTENANCE TREATMENT OF CHRONIC OBSTRUCTIVE PULMONARY DISEASE (COPD)
0.4MG/INH;0.012MG/INH DUAKLIR PRESSAIR AZURITY N210595 March 29, 2019 RX POWDER, METERED INHALATION 11000517 March 13, 2029 MAINTENANCE TREATMENT OF CHRONIC OBSTRUCTIVE PULMONARY DISEASE (COPD)

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
Muscarinic acetylcholine receptor M3 GPCR ANTAGONIST Ki 10.15 CHEMBL CHEMBL
Muscarinic acetylcholine receptor M1 GPCR Ki 10.10 CHEMBL
Muscarinic acetylcholine receptor M2 GPCR Ki 10.10 CHEMBL
Muscarinic acetylcholine receptor M4 GPCR IC50 9.70 CHEMBL
Muscarinic acetylcholine receptor M5 GPCR IC50 9.80 CHEMBL

External reference:

IDSource
D08837 KEGG_DRUG
4031720 VUID
N0000185730 NUI
4031719 VANDF
4031720 VANDF
CHEBI:65344 CHEBI
CHEMBL551466 ChEMBL_ID
CHEMBL1194325 ChEMBL_ID
C542859 MESH_SUPPLEMENTAL_RECORD_UI
8544 INN_ID
727649-81-2 SECONDARY_CAS_RN
UQW7UF9N91 UNII
DB08897 DRUGBANK_ID
1303097 RXNORM
192177 MMSL
28687 MMSL
d07885 MMSL
014613 NDDF
014614 NDDF
703921008 SNOMEDCT_US
703922001 SNOMEDCT_US
703923006 SNOMEDCT_US
C2699758 UMLSCUI
11519741 PUBCHEM_CID
7449 IUPHAR_LIGAND_ID
UQW7UF9N91 INXIGHT DRUGS

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
DUAKLIR PRESSAIR HUMAN PRESCRIPTION DRUG LABEL 2 70515-001 POWDER, METERED 400 ug RESPIRATORY (INHALATION) NDA 27 sections
Tudorza Pressair HUMAN PRESCRIPTION DRUG LABEL 1 70515-002 POWDER, METERED 400 ug RESPIRATORY (INHALATION) NDA 27 sections