salmeterol ๐Ÿถ Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
bronchodilators, phenethylamine derivatives 2419 89365-50-4

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • serevent
  • salmeterol
  • salmeterol xinafoate
Salmeterol is a selective long acting beta2-adrenoceptor agonist. In vitro studies show salmeterol to be at least 50 times more selective for beta2-adrenoceptors than albuterol. Although beta2-adrenoceptors are the predominant adrenergic receptors in bronchial smooth muscle and beta1-adrenoceptors are the predominant receptors in the heart, there are also beta2-adrenoceptors in the human heart comprising 10% to 50% of the total beta-adrenoceptors. The precise function of these receptors has not been established, but their presence raises the possibility that even selective beta2-agonists may have cardiac effects. The pharmacologic effects of beta2-adrenoceptor agonist drugs, including salmeterol, are at least in part attributable to stimulation of intracellular adenyl cyclase, the enzyme that catalyzes the conversion of adenosine triphosphate (ATP) to cyclic-3',5'-adenosine monophosphate (cyclic AMP). Increased cyclic AMP levels cause relaxation of bronchial smooth muscle and inhibition of release of mediators of immediate hypersensitivity from cells, especially from mast cells. In vitro tests show that salmeterol is a potent and long-lasting inhibitor of the release of mast cell mediators, such as histamine, leukotrienes, and prostaglandin D2, from human lung. Salmeterol inhibits histamine-induced plasma protein extravasation and inhibits platelet-activating factor-induced eosinophil accumulation in the lungs of guinea pigs when administered by the inhaled route. In humans, single doses of salmeterol administered via inhalation aerosol attenuate allergen-induced bronchial hyper-responsiveness. It has received approval to be used in combination with fluticasone.
  • Molecular weight: 415.57
  • Formula: C25H37NO4
  • CLOGP: 3.06
  • LIPINSKI: 0
  • HAC: 5
  • HDO: 4
  • TPSA: 81.95
  • ALOGS: -5.26
  • ROTB: 16

  • Status: OFP

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

Drug dosage:

DoseUnitRoute
0.10 mg Inhal.aerosol
0.10 mg Inhal.powder

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 2 Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine) 2.50 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 0.00 ยตM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD

Approvals:

DateAgencyCompanyOrphan
March 26, 2021 EMA TEVA B.V.
Feb. 4, 1994 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
Asthma 234.44 11.85 256 22207 127305 63339254
Chronic obstructive pulmonary disease 178.77 11.85 160 22303 62526 63404033
Dyspnoea 169.56 11.85 565 21898 660748 62805811
Eosinophilic granulomatosis with polyangiitis 130.48 11.85 43 22420 2149 63464410
Product quality issue 123.46 11.85 102 22361 35763 63430796
Chest discomfort 122.95 11.85 172 22291 109797 63356762
Wheezing 90.11 11.85 138 22325 95457 63371102
Ventilation perfusion mismatch 83.53 11.85 22 22441 496 63466063
Cough 76.13 11.85 252 22211 292491 63174068
Bronchitis 68.14 11.85 142 22321 124793 63341766
Dysphonia 66.31 11.85 83 22380 47531 63419028
Pneumonia 62.86 11.85 323 22140 456444 63010115
Contraindicated product administered 61.29 11.85 4 22459 217644 63248915
Product complaint 58.32 11.85 43 22420 12766 63453793
Treatment failure 58.06 11.85 3 22460 199040 63267519
Off label use 57.53 11.85 94 22369 674368 62792191
Bronchospasm 55.01 11.85 47 22416 17233 63449326
Synovitis 51.00 11.85 4 22459 186914 63279645
Status asthmaticus 50.87 11.85 17 22446 887 63465672
Drug intolerance 44.63 11.85 27 22436 308634 63157925
Product use issue 40.06 11.85 14 22449 220506 63246053
Systemic lupus erythematosus 38.41 11.85 13 22450 208905 63257654
Completed suicide 37.37 11.85 4 22459 145669 63320890
Stress fracture 34.61 11.85 26 22437 7937 63458622
Laryngeal pain 32.22 11.85 20 22443 4478 63462081
Myocardial infarction 31.43 11.85 92 22371 99801 63366758
Increased upper airway secretion 30.62 11.85 18 22445 3654 63462905
Arthropathy 30.62 11.85 23 22440 234769 63231790
Abdominal discomfort 29.88 11.85 42 22421 320843 63145716
Throat irritation 29.49 11.85 50 22413 37597 63428962
Infusion related reaction 28.40 11.85 27 22436 245494 63221065
Glossodynia 28.22 11.85 14 22449 178862 63287697
Intentional product use issue 27.16 11.85 6 22457 127886 63338673
Product use in unapproved indication 26.80 11.85 15 22448 179065 63287494
Pericarditis 26.33 11.85 7 22456 131572 63334987
Dysmetropsia 25.88 11.85 6 22457 78 63466481
Chest pain 25.05 11.85 146 22317 215813 63250746
Rheumatoid arthritis 24.86 11.85 32 22431 253787 63212772
Joint swelling 24.83 11.85 49 22414 327617 63138942
Palpitations 24.82 11.85 92 22371 112678 63353881
Peripheral swelling 24.56 11.85 35 22428 265907 63200652
Erysipelas 24.14 11.85 21 22442 7884 63458675
Productive cough 23.62 11.85 62 22401 63146 63403413
International normalised ratio increased 23.23 11.85 51 22412 46374 63420185
Therapeutic product effect decreased 22.62 11.85 21 22442 193166 63273393
Cardiac failure congestive 22.55 11.85 78 22385 92355 63374204
Haemoptysis 22.29 11.85 38 22425 28688 63437871
Psoriatic arthropathy 22.26 11.85 3 22460 91517 63375042
Acute respiratory failure 22.14 11.85 42 22421 34443 63432116
Derealisation 21.96 11.85 10 22453 1198 63465361
Alopecia 21.87 11.85 55 22408 337481 63129078
Eczema impetiginous 21.56 11.85 4 22459 15 63466544
Anxiety 20.81 11.85 140 22323 217401 63249158
Middle insomnia 20.80 11.85 24 22439 12619 63453940
Toxicity to various agents 20.48 11.85 35 22428 247215 63219344
Respiratory failure 19.88 11.85 80 22383 101778 63364781
Varicella zoster oesophagitis 19.48 11.85 4 22459 28 63466531
Anaphylactic reaction 19.01 11.85 59 22404 66041 63400518
Varicella zoster gastritis 18.90 11.85 4 22459 33 63466526
Discomfort 18.66 11.85 19 22444 167355 63299204
Cortisol decreased 18.60 11.85 9 22454 1235 63465324
Fracture displacement 18.49 11.85 9 22454 1252 63465307
Musculoskeletal stiffness 18.35 11.85 23 22440 184595 63281964
Inhalation therapy 17.95 11.85 4 22459 43 63466516
Hypoxia 17.78 11.85 54 22409 59738 63406821
Impaired healing 17.78 11.85 7 22456 102535 63364024
Emotional distress 17.72 11.85 37 22426 32512 63434047
Candida infection 17.55 11.85 34 22429 28317 63438242
Calculus bladder 17.39 11.85 7 22456 620 63465939
Lung disorder 17.38 11.85 55 22408 62206 63404353
Peroneal nerve injury 17.25 11.85 4 22459 52 63466507
Neutropenia 17.19 11.85 22 22441 174983 63291576
Tremor 17.04 11.85 92 22371 132147 63334412
Granuloma 16.98 11.85 15 22448 5746 63460813
Intentional overdose 16.74 11.85 3 22460 74149 63392410
Emphysema 16.73 11.85 20 22443 10918 63455641
Ecchymosis 16.50 11.85 20 22443 11074 63455485
Investigation 16.44 11.85 9 22454 1596 63464963
Oedema peripheral 16.38 11.85 119 22344 189392 63277167
Drug abuse 16.23 11.85 3 22460 72515 63394044
Febrile neutropenia 16.22 11.85 11 22452 118438 63348121
Kounis syndrome 15.81 11.85 9 22454 1721 63464838
Hypercapnia 15.73 11.85 14 22449 5417 63461142
Oligohydramnios 15.70 11.85 15 22448 6351 63460208
Adrenal insufficiency 15.65 11.85 25 22438 17890 63448669
Rash 15.33 11.85 126 22337 560745 62905814
Nikolsky's sign 14.75 11.85 4 22459 101 63466458
Drug ineffective 14.74 11.85 271 22192 1044494 62422065
Hepatic enzyme increased 14.68 11.85 31 22432 202297 63264262
Pharyngeal oedema 14.62 11.85 21 22442 13700 63452859
Myoclonic dystonia 14.49 11.85 3 22460 22 63466537
Throat tightness 14.38 11.85 29 22434 24858 63441701
Uterine hypertonus 14.37 11.85 5 22458 295 63466264
Diarrhoea 13.66 11.85 175 22288 715191 62751368
Femur fracture 13.65 11.85 39 22424 41717 63424842
Urethral pain 13.41 11.85 5 22458 360 63466199
Choking 13.39 11.85 17 22446 9862 63456697
Cerebrovascular accident 13.14 11.85 74 22389 107950 63358609
Cholecystitis chronic 12.75 11.85 17 22446 10344 63456215
Wound 12.71 11.85 24 22439 163239 63303320
Irritable bowel syndrome 12.18 11.85 7 22456 82405 63384154

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
Asthma 220.20 13.56 151 11552 42505 34902723
Chronic obstructive pulmonary disease 150.04 13.56 127 11576 48791 34896437
Dyspnoea 104.72 13.56 319 11384 376463 34568765
Eosinophilic granulomatosis with polyangiitis 100.47 13.56 34 11669 1953 34943275
Cerebral artery thrombosis 75.82 13.56 22 11681 758 34944470
Brain scan abnormal 73.20 13.56 22 11681 858 34944370
Pneumonia 65.76 13.56 267 11436 362360 34582868
Wheezing 63.97 13.56 74 11629 41328 34903900
Product quality issue 51.67 13.56 44 11659 16991 34928237
Product complaint 50.96 13.56 29 11674 5861 34939367
Areflexia 49.82 13.56 23 11680 3008 34942220
Status asthmaticus 48.91 13.56 13 11690 322 34944906
Fractional exhaled nitric oxide increased 48.80 13.56 17 11686 1065 34944163
Toxicity to various agents 42.22 13.56 8 11695 200354 34744874
Plantar fasciitis 40.95 13.56 18 11685 2098 34943130
Sensation of foreign body 39.23 13.56 19 11684 2764 34942464
Myoglobin blood increased 31.98 13.56 17 11686 3006 34942222
Respiratory distress 30.78 13.56 48 11655 35617 34909611
Dysphonia 29.90 13.56 38 11665 23345 34921883
Brain natriuretic peptide increased 29.04 13.56 20 11683 5639 34939589
Hepatic cancer 28.47 13.56 23 11680 8252 34936976
Hemiplegia 27.48 13.56 21 11682 6951 34938277
Carcinoid tumour of the gastrointestinal tract 27.47 13.56 6 11697 62 34945166
Off label use 26.40 13.56 64 11639 419460 34525768
Cough 25.78 13.56 109 11594 150031 34795197
Facial paralysis 25.19 13.56 24 11679 10710 34934518
Respiratory failure 24.52 13.56 86 11617 108486 34836742
Obstructive airways disorder 24.42 13.56 28 11675 15466 34929762
Pneumothorax 24.37 13.56 31 11672 19061 34926167
Ischaemic stroke 23.87 13.56 30 11673 18220 34927008
Drug abuse 23.01 13.56 3 11700 99093 34846135
Exostosis 22.62 13.56 16 11687 4707 34940521
Eosinophilia 22.21 13.56 35 11668 26187 34919041
Sinusitis 21.89 13.56 45 11658 41357 34903871
Oral candidiasis 20.99 13.56 23 11680 12087 34933141
Benign prostatic hyperplasia 20.85 13.56 25 11678 14470 34930758
Coronary artery disease 20.44 13.56 48 11655 48257 34896971
Inhalation therapy 19.58 13.56 4 11699 29 34945199
Secretion discharge 19.44 13.56 16 11687 5889 34939339
Cardiac failure congestive 18.82 13.56 66 11637 83204 34862024
Cardiac disorder 17.32 13.56 42 11661 43084 34902144
Dyspnoea exertional 17.22 13.56 42 11661 43237 34901991
Carcinoid tumour of the stomach 17.13 13.56 4 11699 57 34945171
Atrial fibrillation 16.64 13.56 83 11620 122310 34822918
Increased upper airway secretion 15.89 13.56 9 11694 1801 34943427
Product use in unapproved indication 15.68 13.56 10 11693 117489 34827739
Lipohypertrophy 15.01 13.56 5 11698 273 34944955
Emphysema 14.65 13.56 17 11686 9508 34935720
Bronchospasm 14.61 13.56 18 11685 10713 34934515
Post streptococcal glomerulonephritis 14.22 13.56 4 11699 123 34945105
Febrile neutropenia 14.11 13.56 15 11688 136834 34808394
Pseudomonas infection 14.08 13.56 19 11684 12363 34932865
Bronchitis 13.89 13.56 38 11665 41925 34903303

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
Asthma 273.59 11.92 277 26154 134818 79583139
Eosinophilic granulomatosis with polyangiitis 231.52 11.92 74 26357 3586 79714371
Chronic obstructive pulmonary disease 229.75 11.92 205 26226 85214 79632743
Dyspnoea 176.38 11.92 652 25779 856373 78861584
Product quality issue 119.07 11.92 95 26336 33845 79684112
Chest discomfort 97.86 11.92 169 26262 137875 79580082
Pneumonia 94.27 11.92 450 25981 659796 79058161
Wheezing 82.90 11.92 143 26288 116521 79601436
Ventilation perfusion mismatch 80.34 11.92 22 26409 618 79717339
Product complaint 68.52 11.92 47 26384 13302 79704655
Bronchitis 66.59 11.92 139 26292 130505 79587452
Brain scan abnormal 66.28 11.92 22 26409 1201 79716756
Cerebral artery thrombosis 64.29 11.92 21 26410 1090 79716867
Cough 61.90 11.92 263 26168 366526 79351431
Off label use 61.40 11.92 131 26300 907084 78810873
Status asthmaticus 57.64 11.92 19 26412 1015 79716942
Toxicity to various agents 53.76 11.92 37 26394 421503 79296454
Completed suicide 48.53 11.92 11 26420 245756 79472201
Treatment failure 41.97 11.92 4 26427 170482 79547475
Bronchospasm 41.37 11.92 46 26385 24813 79693144
Drug abuse 39.57 11.92 4 26427 162687 79555270
Intentional product use issue 36.32 11.92 4 26427 152108 79565849
Increased upper airway secretion 34.80 11.92 20 26411 4157 79713800
Areflexia 32.04 11.92 21 26410 5513 79712444
Product use in unapproved indication 31.85 11.92 22 26409 250337 79467620
Haemoptysis 31.37 11.92 62 26369 55937 79662020
COVID-19 31.23 11.92 7 26424 157667 79560290
Contraindicated product administered 31.19 11.92 7 26424 157531 79560426
Myocardial infarction 30.19 11.92 131 26300 183998 79533959
Drug intolerance 30.05 11.92 26 26405 264093 79453864
Respiratory failure 29.88 11.92 129 26302 180782 79537175
Cerebrovascular accident 29.81 11.92 116 26315 155176 79562781
Cardiac failure congestive 29.50 11.92 109 26322 142293 79575664
Febrile neutropenia 28.46 11.92 21 26410 230978 79486979
Hypoxia 28.45 11.92 87 26344 103156 79614801
Inhalation therapy 28.18 11.92 6 26425 55 79717902
Productive cough 27.76 11.92 78 26353 88253 79629704
Dysphonia 27.20 11.92 59 26372 56813 79661144
Tremor 25.61 11.92 118 26313 169965 79547992
Carcinoid tumour of the gastrointestinal tract 25.60 11.92 6 26425 88 79717869
Laryngeal pain 25.56 11.92 19 26412 6095 79711862
Dysmetropsia 25.41 11.92 6 26425 91 79717866
Oral candidiasis 24.62 11.92 39 26392 29589 79688368
Stress fracture 24.57 11.92 19 26412 6461 79711496
Erysipelas 23.28 11.92 23 26408 10827 79707130
Acute respiratory failure 23.22 11.92 57 26374 59484 79658473
International normalised ratio increased 22.98 11.92 71 26360 84650 79633307
Throat irritation 22.53 11.92 45 26386 40901 79677056
Palpitations 22.23 11.92 92 26339 126518 79591439
Rheumatoid arthritis 21.96 11.92 22 26409 208448 79509509
Respiratory distress 21.86 11.92 55 26376 58284 79659673
Chest pain 21.13 11.92 163 26268 282141 79435816
Product use issue 20.05 11.92 24 26407 209798 79508159
Pericarditis 19.90 11.92 5 26426 104231 79613726
Varicella zoster oesophagitis 19.74 11.92 4 26427 28 79717929
Cortisol decreased 19.71 11.92 11 26420 2161 79715796
Derealisation 19.62 11.92 10 26421 1639 79716318
Varicella zoster gastritis 19.16 11.92 4 26427 33 79717924
Emphysema 18.71 11.92 25 26406 16275 79701682
Fracture displacement 18.60 11.92 9 26422 1319 79716638
Intentional overdose 18.53 11.92 6 26425 105954 79612003
Infective pulmonary exacerbation of cystic fibrosis 18.39 11.92 22 26409 12829 79705128
Peripheral swelling 18.08 11.92 39 26392 269578 79448379
Facial paralysis 17.87 11.92 28 26403 21044 79696913
Middle insomnia 17.46 11.92 24 26407 16045 79701912
Hypercapnia 17.45 11.92 18 26413 8917 79709040
Peroneal nerve injury 16.98 11.92 4 26427 60 79717897
Benign prostatic hyperplasia 16.81 11.92 20 26411 11592 79706365
Infusion related reaction 16.54 11.92 32 26399 230205 79487752
Psoriatic arthropathy 16.40 11.92 3 26428 77996 79639961
Systemic lupus erythematosus 16.27 11.92 10 26421 121139 79596818
Diffuse panbronchiolitis 16.02 11.92 3 26428 13 79717944
Malignant neoplasm progression 15.93 11.92 13 26418 135977 79581980
Hemiplegia 15.77 11.92 22 26409 14917 79703040
Lipohypertrophy 15.51 11.92 7 26424 877 79717080
Calculus bladder 15.40 11.92 8 26423 1364 79716593
Joint swelling 15.31 11.92 47 26384 288599 79429358
Emotional distress 15.30 11.92 38 26393 39931 79678026
Lung disorder 15.30 11.92 60 26371 80497 79637460
Sinusitis 15.25 11.92 114 26317 195387 79522570
Uterine hypertonus 15.19 11.92 5 26426 266 79717691
Pulseless electrical activity 15.17 11.92 21 26410 14139 79703818
Anxiety 15.13 11.92 137 26294 248375 79469582
Hepatic cancer 15.02 11.92 18 26413 10511 79707446
Granuloma 14.93 11.92 16 26415 8281 79709676
Therapeutic product effect decreased 14.35 11.92 20 26411 163843 79554114
Hepatic enzyme increased 14.35 11.92 24 26407 182586 79535371
Post streptococcal glomerulonephritis 14.14 11.92 4 26427 127 79717830
Neutropenia 13.78 11.92 49 26382 287661 79430296
Impaired healing 13.60 11.92 6 26425 87649 79630308
Central obesity 13.53 11.92 8 26423 1753 79716204
Coronary artery disease 13.45 11.92 50 26381 65424 79652533
Arthropathy 13.26 11.92 24 26407 177087 79540870
Candida infection 13.25 11.92 35 26396 38179 79679778
Lung hyperinflation 13.13 11.92 8 26423 1851 79716106
Swelling face 12.69 11.92 52 26379 71160 79646797
Ecchymosis 12.61 11.92 20 26411 15186 79702771
Carcinoid tumour of the stomach 12.49 11.92 4 26427 195 79717762
Pulmonary function test decreased 12.48 11.92 14 26417 7623 79710334
Pulmonary embolism 12.22 11.92 98 26333 171556 79546401
Urethral pain 12.18 11.92 5 26426 497 79717460
Sputum discoloured 12.09 11.92 24 26407 21719 79696238
C-reactive protein increased 12.07 11.92 15 26416 129012 79588945
White blood cell count decreased 11.99 11.92 28 26403 188260 79529697
Spirometry abnormal 11.95 11.92 6 26425 953 79717004
Oedema peripheral 11.93 11.92 132 26299 252156 79465801

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC R03AC12 RESPIRATORY SYSTEM
DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES
ADRENERGICS, INHALANTS
Selective beta-2-adrenoreceptor agonists
ATC R03AK06 RESPIRATORY SYSTEM
DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES
ADRENERGICS, INHALANTS
Adrenergics in combination with corticosteroids or other drugs, excl. anticholinergics
ATC R03AK12 RESPIRATORY SYSTEM
DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES
ADRENERGICS, INHALANTS
Adrenergics in combination with corticosteroids or other drugs, excl. anticholinergics
FDA MoA N0000009922 Adrenergic beta2-Agonists
MeSH PA D018663 Adrenergic Agents
MeSH PA D000322 Adrenergic Agonists
MeSH PA D058666 Adrenergic beta-2 Receptor Agonists
MeSH PA D000318 Adrenergic beta-Agonists
MeSH PA D018927 Anti-Asthmatic Agents
MeSH PA D001993 Bronchodilator Agents
MeSH PA D018377 Neurotransmitter Agents
MeSH PA D018373 Peripheral Nervous System Agents
MeSH PA D019141 Respiratory System Agents
CHEBI has role CHEBI:35522 beta-adrenergic agonists
CHEBI has role CHEBI:35523 bronchodilator
FDA EPC N0000175779 beta2-Adrenergic Agonist

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

DiseaseRelationSNOMED_IDDOID
Pulmonary emphysema indication 87433001
Non-allergic asthma indication 266361008 DOID:9360
Allergic asthma indication 389145006 DOID:9415
Adjunct Therapy to Achieve Long-term Asthma Control indication
Bronchospasm Prevention with COPD indication
Exercise-Induced Bronchospasm Prevention indication
COPD Associated with Chronic Bronchitis indication
Mycosis contraindication 3218000 DOID:1564
Disease caused by parasite contraindication 17322007
Glaucoma contraindication 23986001 DOID:1686
Acute tuberculosis contraindication 25629007
Hypertensive disorder contraindication 38341003 DOID:10763
Hypokalemia contraindication 43339004
Conduction disorder of the heart contraindication 44808001
Ketoacidosis contraindication 56051008
Osteoporosis contraindication 64859006 DOID:11476
Diabetes mellitus contraindication 73211009 DOID:9351
Hypopituitarism contraindication 74728003 DOID:9406
Candidiasis of mouth contraindication 79740000 DOID:14262
Hyperglycemia contraindication 80394007 DOID:4195
Thyrotoxicosis contraindication 90739004 DOID:7997
Bilateral cataracts contraindication 95722004
Prolonged QT interval contraindication 111975006
Seizure disorder contraindication 128613002
Ophthalmic herpes simplex contraindication 186542001
Exacerbation of asthma contraindication 281239006
Osteopenia contraindication 312894000
Chronic myocardial ischemia contraindication 413844008 DOID:3393
Congenital long QT syndrome contraindication 442917000
Uncontrolled Bacterial Infections contraindication




๐Ÿถ Veterinary Drug Use

None

๐Ÿถ Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 10.07 acidic
pKa2 9.28 Basic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
0.055MG/INH;EQ 0.014MG BASE/INH AIRDUO DIGIHALER TEVA PHARM N208799 July 12, 2019 RX POWDER INHALATION 9066957 Oct. 6, 2034 TREATMENT OF ASTHMA
0.055MG/INH;EQ 0.014MG BASE/INH AIRDUO RESPICLICK TEVA PHARM N208799 Jan. 27, 2017 RX POWDER INHALATION 9066957 Oct. 6, 2034 TREATMENT OF ASTHMA
0.055MG/INH;EQ 0.014MG BASE/INH AIRDUO DIGIHALER TEVA PHARM N208799 July 12, 2019 RX POWDER INHALATION 9415008 Oct. 6, 2034 TREATMENT OF ASTHMA
0.055MG/INH;EQ 0.014MG BASE/INH AIRDUO RESPICLICK TEVA PHARM N208799 Jan. 27, 2017 RX POWDER INHALATION 9415008 Oct. 6, 2034 TREATMENT OF ASTHMA
0.113MG/INH;EQ 0.014MG BASE/INH AIRDUO DIGIHALER TEVA PHARM N208799 July 12, 2019 RX POWDER INHALATION 9066957 Oct. 6, 2034 TREATMENT OF ASTHMA
0.113MG/INH;EQ 0.014MG BASE/INH AIRDUO RESPICLICK TEVA PHARM N208799 Jan. 27, 2017 RX POWDER INHALATION 9066957 Oct. 6, 2034 TREATMENT OF ASTHMA
0.232MG/INH;EQ 0.014MG BASE/INH AIRDUO DIGIHALER TEVA PHARM N208799 July 12, 2019 RX POWDER INHALATION 9066957 Oct. 6, 2034 TREATMENT OF ASTHMA
0.232MG/INH;EQ 0.014MG BASE/INH AIRDUO RESPICLICK TEVA PHARM N208799 Jan. 27, 2017 RX POWDER INHALATION 9066957 Oct. 6, 2034 TREATMENT OF ASTHMA

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
0.055MG/INH;EQ 0.014MG BASE/INH AIRDUO DIGIHALER TEVA PHARM N208799 July 12, 2019 RX POWDER INHALATION July 9, 2024 REVISIONS TO LABELING BASED ON DATA SUBMITTED IN RESPONSE TO PEDIATRIC WRITTEN REQUEST
0.055MG/INH;EQ 0.014MG BASE/INH AIRDUO RESPICLICK TEVA PHARM N208799 Jan. 27, 2017 RX POWDER INHALATION July 9, 2024 REVISIONS TO LABELING BASED ON DATA SUBMITTED IN RESPONSE TO PEDIATRIC WRITTEN REQUEST
0.055MG/INH;EQ 0.014MG BASE/INH AIRDUO DIGIHALER TEVA PHARM N208799 July 12, 2019 RX POWDER INHALATION Jan. 9, 2025 PEDIATRIC EXCLUSIVITY
0.055MG/INH;EQ 0.014MG BASE/INH AIRDUO RESPICLICK TEVA PHARM N208799 Jan. 27, 2017 RX POWDER INHALATION Jan. 9, 2025 PEDIATRIC EXCLUSIVITY

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Beta-2 adrenergic receptor GPCR AGONIST Ki 9.41 CHEMBL CHEMBL
D(2) dopamine receptor GPCR Ki 4.50 CHEMBL
D(3) dopamine receptor GPCR Ki 5.98 CHEMBL
Aldehyde oxidase Enzyme IC50 5.00 WOMBAT-PK
Beta-3 adrenergic receptor GPCR EC50 6 CHEMBL
Beta-1 adrenergic receptor GPCR Ki 6.10 CHEMBL
Beta-2 adrenergic receptor GPCR EC50 7.50 CHEMBL
Beta-1 adrenergic receptor GPCR Ki 6.26 CHEMBL

External reference:

IDSource
4023955 VUID
N0000021960 NUI
D00687 KEGG_DRUG
94749-08-3 SECONDARY_CAS_RN
4020873 VANDF
4023955 VANDF
C0245531 UMLSCUI
CHEBI:9011 CHEBI
K5Y PDB_CHEM_ID
CHEMBL1263 ChEMBL_ID
CHEMBL1082607 ChEMBL_ID
D000068299 MESH_DESCRIPTOR_UI
DB00938 DRUGBANK_ID
5152 PUBCHEM_CID
559 IUPHAR_LIGAND_ID
5578 INN_ID
2I4BC502BT UNII
203159 RXNORM
1605 MMSL
21564 MMSL
5440 MMSL
d03759 MMSL
004036 NDDF
004037 NDDF
108605008 SNOMEDCT_US
108606009 SNOMEDCT_US
372515005 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
fluticasone propionate and salmeterol HUMAN PRESCRIPTION DRUG LABEL 2 0054-0326 POWDER 50 ug RESPIRATORY (INHALATION) ANDA 28 sections
fluticasone propionate and salmeterol HUMAN PRESCRIPTION DRUG LABEL 2 0054-0326 POWDER 50 ug RESPIRATORY (INHALATION) ANDA 28 sections
fluticasone propionate and salmeterol HUMAN PRESCRIPTION DRUG LABEL 2 0054-0327 POWDER 50 ug RESPIRATORY (INHALATION) ANDA 28 sections
fluticasone propionate and salmeterol HUMAN PRESCRIPTION DRUG LABEL 2 0054-0327 POWDER 50 ug RESPIRATORY (INHALATION) ANDA 28 sections
Fluticasone Propionate and Salmeterol HUMAN PRESCRIPTION DRUG LABEL 2 0093-3607 POWDER, METERED 14 ug RESPIRATORY (INHALATION) NDA authorized generic 28 sections
Fluticasone Propionate and Salmeterol HUMAN PRESCRIPTION DRUG LABEL 2 0093-3607 POWDER, METERED 14 ug RESPIRATORY (INHALATION) NDA authorized generic 28 sections
Fluticasone Propionate and Salmeterol HUMAN PRESCRIPTION DRUG LABEL 2 0093-3607 POWDER, METERED 14 ug RESPIRATORY (INHALATION) NDA authorized generic 28 sections
Fluticasone Propionate and Salmeterol HUMAN PRESCRIPTION DRUG LABEL 2 0093-3608 POWDER, METERED 14 ug RESPIRATORY (INHALATION) NDA authorized generic 28 sections
Fluticasone Propionate and Salmeterol HUMAN PRESCRIPTION DRUG LABEL 2 0093-3608 POWDER, METERED 14 ug RESPIRATORY (INHALATION) NDA authorized generic 28 sections
Fluticasone Propionate and Salmeterol HUMAN PRESCRIPTION DRUG LABEL 2 0093-3608 POWDER, METERED 14 ug RESPIRATORY (INHALATION) NDA authorized generic 28 sections
Fluticasone Propionate and Salmeterol HUMAN PRESCRIPTION DRUG LABEL 2 0093-3609 POWDER, METERED 14 ug RESPIRATORY (INHALATION) NDA authorized generic 28 sections
Fluticasone Propionate and Salmeterol HUMAN PRESCRIPTION DRUG LABEL 2 0093-3609 POWDER, METERED 14 ug RESPIRATORY (INHALATION) NDA authorized generic 28 sections
Fluticasone Propionate and Salmeterol HUMAN PRESCRIPTION DRUG LABEL 2 0093-3609 POWDER, METERED 14 ug RESPIRATORY (INHALATION) NDA authorized generic 28 sections
fluticasone propionate and salmeterol HUMAN PRESCRIPTION DRUG LABEL 2 0093-7516 POWDER 50 ug RESPIRATORY (INHALATION) ANDA 28 sections
fluticasone propionate and salmeterol HUMAN PRESCRIPTION DRUG LABEL 2 0093-7516 POWDER 50 ug RESPIRATORY (INHALATION) ANDA 28 sections
fluticasone propionate and salmeterol HUMAN PRESCRIPTION DRUG LABEL 2 0093-7517 POWDER 50 ug RESPIRATORY (INHALATION) ANDA 28 sections
fluticasone propionate and salmeterol HUMAN PRESCRIPTION DRUG LABEL 2 0093-7517 POWDER 50 ug RESPIRATORY (INHALATION) ANDA 28 sections
fluticasone propionate and salmeterol HUMAN PRESCRIPTION DRUG LABEL 2 0093-7518 POWDER 50 ug RESPIRATORY (INHALATION) ANDA 28 sections
fluticasone propionate and salmeterol HUMAN PRESCRIPTION DRUG LABEL 2 0093-7518 POWDER 50 ug RESPIRATORY (INHALATION) ANDA 28 sections
SEREVENTDISKUS HUMAN PRESCRIPTION DRUG LABEL 1 0173-0520 POWDER, METERED 50 ug RESPIRATORY (INHALATION) NDA 29 sections
SEREVENTDISKUS HUMAN PRESCRIPTION DRUG LABEL 1 0173-0521 POWDER, METERED 50 ug RESPIRATORY (INHALATION) NDA 29 sections
SEREVENTDISKUS HUMAN PRESCRIPTION DRUG LABEL 1 0173-0521 POWDER, METERED 50 ug RESPIRATORY (INHALATION) NDA 29 sections
ADVAIRDISKUS HUMAN PRESCRIPTION DRUG LABEL 2 0173-0695 POWDER 50 ug RESPIRATORY (INHALATION) NDA 27 sections
ADVAIRDISKUS HUMAN PRESCRIPTION DRUG LABEL 2 0173-0695 POWDER 50 ug RESPIRATORY (INHALATION) NDA 27 sections
ADVAIRDISKUS HUMAN PRESCRIPTION DRUG LABEL 2 0173-0695 POWDER 50 ug RESPIRATORY (INHALATION) NDA 27 sections
ADVAIRDISKUS HUMAN PRESCRIPTION DRUG LABEL 2 0173-0696 POWDER 50 ug RESPIRATORY (INHALATION) NDA 27 sections
ADVAIRDISKUS HUMAN PRESCRIPTION DRUG LABEL 2 0173-0696 POWDER 50 ug RESPIRATORY (INHALATION) NDA 27 sections
ADVAIRDISKUS HUMAN PRESCRIPTION DRUG LABEL 2 0173-0696 POWDER 50 ug RESPIRATORY (INHALATION) NDA 27 sections
ADVAIRDISKUS HUMAN PRESCRIPTION DRUG LABEL 2 0173-0697 POWDER 50 ug RESPIRATORY (INHALATION) NDA 27 sections
ADVAIRDISKUS HUMAN PRESCRIPTION DRUG LABEL 2 0173-0697 POWDER 50 ug RESPIRATORY (INHALATION) NDA 27 sections