sufentanil ๐Ÿถ Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |

Stem definitionDrug idCAS RN
opioid receptor agonists, analgesics, fentanyl derivatives 2491 56030-54-7

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • sulfentanyl
  • sulfentanil
  • sulfentanil citrate
  • sufentanil
  • sufentanil citrate
An opioid analgesic that is used as an adjunct in anesthesia, in balanced anesthesia, and as a primary anesthetic agent.
  • Molecular weight: 386.55
  • Formula: C22H30N2O2S
  • CLOGP: 3.59
  • LIPINSKI: 0
  • HAC: 4
  • HDO: 0
  • TPSA: 32.78
  • ALOGS: -4.51
  • ROTB: 8
  • Status: OFP
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

None

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 1 Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine) 6 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 0.06 ยตM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability) 0 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution) 9.40 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 15 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.08 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 14 hours Lombardo F, Berellini G, Obach RS

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
kinase-safety-class ACVR2B,AKT2,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK4,CDK5,CDK9,DDR1,DYRK1B,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,ITK,JAK2,MAP3K7,MAPK10,MAPK12,MAPK7,MAPKAPK2,MET,NTRK2,PDK2,PDK4,PDPK1,PIK3CB,PIM2,PRKDC,SIK2,SIK3,STK33,TEK,TGFBR1 37
kinase-selectivity-class AXL,GRK2,SIK2,STK33,TEK 5
pfas-class PFAS structural alert (1 = True, 0 = False) 0

Approvals:

DateAgencyCompanyOrphan
May 4, 1984 FDA AKORN
June 25, 2018 EMA LABORATOIRE AGUETTANT

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
Anaphylactic shock 2663.89 31.93 623 8867 30994 90587963
Hypotension 490.58 31.93 344 9146 325053 90293904
Bronchospasm 376.63 31.93 123 9367 20586 90598371
Maternal exposure during delivery 376.08 31.93 86 9404 3760 90615197
Anaphylactic reaction 366.68 31.93 180 9310 87344 90531613
Acute generalised exanthematous pustulosis 239.41 31.93 79 9411 13624 90605333
Anaesthetic complication neurological 222.52 31.93 42 9448 699 90618258
Cardiac arrest 202.93 31.93 130 9360 104805 90514152
Exposure during pregnancy 155.73 31.93 156 9334 238254 90380703
Circulatory collapse 153.32 31.93 67 9423 24837 90594120
Tachycardia 131.13 31.93 118 9372 157555 90461402
Cardio-respiratory arrest 126.35 31.93 80 9410 63060 90555897
Anaphylactoid shock 126.32 31.93 24 9466 414 90618543
Shock 125.67 31.93 61 9429 28717 90590240
Haemodynamic instability 121.96 31.93 46 9444 11693 90607264
Type I hypersensitivity 119.06 31.93 35 9455 4120 90614837
Respiratory depression 102.71 31.93 44 9446 15531 90603426
Multiple organ dysfunction syndrome 97.01 31.93 70 9420 68266 90550691
Allergy test negative 94.04 31.93 17 9473 220 90618737
Toxic epidermal necrolysis 93.27 31.93 52 9438 32476 90586481
Ventricular fibrillation 90.38 31.93 39 9451 14005 90604952
Serotonin syndrome 88.48 31.93 53 9437 37834 90581123
Mixed liver injury 86.97 31.93 32 9458 7591 90611366
Rash maculo-papular 84.70 31.93 53 9437 40880 90578077
Fatigue 84.12 31.93 11 9479 1154012 89464945
Oliguria 83.44 31.93 34 9456 10590 90608367
Bradycardia 82.23 31.93 69 9421 83778 90535179
Peripheral nerve injury 80.18 31.93 18 9472 721 90618236
Spinal epidural haemorrhage 77.52 31.93 15 9475 286 90618671
Hepatocellular injury 76.82 31.93 44 9446 28914 90590043
Myoclonus 75.83 31.93 38 9452 19130 90599827
Eosinophilia 74.74 31.93 43 9447 28490 90590467
Myocardial stunning 70.84 31.93 14 9476 299 90618658
Drug reaction with eosinophilia and systemic symptoms 68.08 31.93 47 9443 42711 90576246
Hepatorenal failure 64.97 31.93 15 9475 682 90618275
Epidural haemorrhage 64.78 31.93 13 9477 301 90618656
Delayed recovery from anaesthesia 64.11 31.93 16 9474 1014 90617943
Oxygen saturation decreased 63.94 31.93 67 9423 107416 90511541
Cerebral haemorrhage foetal 63.45 31.93 13 9477 335 90618622
Stress cardiomyopathy 63.42 31.93 30 9460 13325 90605632
Mydriasis 63.05 31.93 31 9459 14981 90603976
Acute respiratory distress syndrome 61.50 31.93 38 9452 28648 90590309
Anticholinergic syndrome 60.95 31.93 19 9471 2724 90616233
Erythema 58.58 31.93 94 9396 229152 90389805
Hypocapnia 58.22 31.93 13 9477 508 90618449
Stevens-Johnson syndrome 58.17 31.93 37 9453 29339 90589618
Schizencephaly 57.78 31.93 12 9478 331 90618626
Cardiogenic shock 56.52 31.93 34 9456 24434 90594523
Sinus tachycardia 54.19 31.93 35 9455 28478 90590479
Negative pressure pulmonary oedema 54.17 31.93 9 9481 68 90618889
Metabolic acidosis 52.88 31.93 45 9445 55631 90563326
Anuria 51.71 31.93 27 9463 14791 90604166
Cholestasis 51.06 31.93 37 9453 36262 90582695
Hyperthermia malignant 51.03 31.93 14 9476 1284 90617673
Unwanted awareness during anaesthesia 50.06 31.93 11 9479 399 90618558
Foetal exposure during pregnancy 49.78 31.93 39 9451 42936 90576021
Suspected product quality issue 49.48 31.93 11 9479 421 90618536
Myoglobin blood increased 48.56 31.93 14 9476 1538 90617419
Carcinoid crisis 47.73 31.93 10 9480 288 90618669
Infantile apnoea 46.54 31.93 13 9477 1274 90617683
Spinal epidural haematoma 46.08 31.93 13 9477 1321 90617636
Propofol infusion syndrome 46.03 31.93 13 9477 1326 90617631
Torsade de pointes 45.50 31.93 25 9465 15157 90603800
Foetal heart rate abnormal 45.47 31.93 12 9478 950 90618007
Patent ductus arteriosus 44.19 31.93 17 9473 4552 90614405
Hyperlactacidaemia 42.20 31.93 16 9474 4120 90614837
Drug interaction 41.23 31.93 90 9400 276363 90342594
Epidural analgesia 40.84 31.93 8 9482 163 90618794
Procedure aborted 40.61 31.93 8 9482 168 90618789
Headache 40.45 31.93 20 9470 862726 89756231
Vasoplegia syndrome 40.36 31.93 14 9476 2800 90616157
Paralysis 40.30 31.93 21 9469 11457 90607500
Hepatic cytolysis 40.07 31.93 30 9460 30886 90588071
Foetal exposure during delivery 39.84 31.93 9 9481 371 90618586
Dermatitis bullous 39.47 31.93 20 9470 10296 90608661
Anaesthetic complication 38.22 31.93 13 9477 2452 90616505
Myocardial calcification 38.13 31.93 8 9482 232 90618725
Hypercapnia 37.96 31.93 17 9473 6660 90612297
Apallic syndrome 37.96 31.93 10 9480 786 90618171
Acute kidney injury 37.63 31.93 95 9395 320292 90298665
Generalised tonic-clonic seizure 36.85 31.93 30 9460 34873 90584084
Diarrhoea 36.71 31.93 27 9463 939163 89679794
Hyperthermia 36.54 31.93 19 9471 10316 90608641
Myelitis 36.35 31.93 12 9478 2066 90616891
Bezold-Jarisch reflex 36.27 31.93 6 9484 44 90618913
Uterine hypotonus 35.26 31.93 7 9483 153 90618804
Malaise 35.23 31.93 9 9481 585977 90032980
Arthralgia 35.06 31.93 19 9471 778503 89840454
Acute pulmonary oedema 34.99 31.93 18 9472 9562 90609395
Post procedural stroke 34.89 31.93 6 9484 57 90618900
Respiratory acidosis 34.79 31.93 17 9473 8102 90610855
Postpartum haemorrhage 34.65 31.93 12 9478 2389 90616568
Toxic encephalopathy 33.68 31.93 17 9473 8682 90610275
Abdominal discomfort 33.58 31.93 5 9485 477323 90141634
Altered state of consciousness 33.07 31.93 27 9463 31505 90587452
Swelling 32.92 31.93 3 9487 419055 90199902
Reversal of opiate activity 32.66 31.93 4 9486 0 90618957
Cauda equina syndrome 32.61 31.93 10 9480 1357 90617600
Congenital clavicular agenesis 32.36 31.93 6 9484 90 90618867
Ventricular tachycardia 32.07 31.93 24 9466 24684 90594273

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
Anaphylactic shock 1802.61 32.34 475 6942 23042 42590876
Anaphylactic reaction 309.42 32.34 150 7267 42593 42571325
Anaesthetic complication neurological 290.94 32.34 57 7360 679 42613239
Bronchospasm 219.43 32.34 83 7334 12802 42601116
Hyperthermia malignant 194.20 32.34 52 7365 2606 42611312
Hypotension 167.28 32.34 214 7203 257417 42356501
Tachycardia 158.64 32.34 135 7282 100952 42512966
Rash maculo-papular 129.91 32.34 81 7336 37422 42576496
Drug reaction with eosinophilia and systemic symptoms 107.13 32.34 75 7342 42000 42571918
Toxic epidermal necrolysis 98.25 32.34 60 7357 26690 42587228
Mechanical ventilation complication 97.56 32.34 23 7394 681 42613237
Eosinophilia 91.64 32.34 62 7355 32837 42581081
Hypertransaminasaemia 90.32 32.34 40 7377 9187 42604731
Shock 86.20 32.34 57 7360 29064 42584854
Circulatory collapse 81.66 32.34 51 7366 23585 42590333
Haemothorax 75.80 32.34 30 7387 5206 42608712
Urticaria 75.63 32.34 78 7339 73958 42539960
Erythema 69.58 32.34 90 7327 108703 42505215
Inspiratory capacity decreased 68.69 32.34 24 7393 2943 42610975
Cardio-respiratory arrest 67.63 32.34 66 7351 58570 42555348
Haemodynamic instability 67.13 32.34 36 7381 12521 42601397
Rhabdomyolysis 67.02 32.34 75 7342 77944 42535974
Cholestasis 66.43 32.34 51 7366 32828 42581090
Anaphylactoid shock 63.05 32.34 15 7402 462 42613456
Nervous system disorder 61.65 32.34 38 7379 17157 42596761
Adverse reaction 58.22 32.34 23 7394 3970 42609948
Emphysema 57.90 32.34 32 7385 11803 42602115
Face oedema 56.24 32.34 33 7384 13633 42600285
Shock haemorrhagic 55.97 32.34 35 7382 16207 42597711
Type I hypersensitivity 55.88 32.34 19 7398 2147 42611771
Postoperative delirium 54.70 32.34 14 7403 586 42613332
Hypovolaemia 53.31 32.34 30 7387 11455 42602463
Angiopathy 51.61 32.34 23 7394 5354 42608564
Cardiac arrest 51.32 32.34 78 7339 109242 42504676
Victim of crime 51.07 32.34 13 7404 532 42613386
Injury 50.36 32.34 37 7380 22279 42591639
Symmetrical drug-related intertriginous and flexural exanthema 49.57 32.34 14 7403 854 42613064
Confusion postoperative 48.63 32.34 10 7407 154 42613764
Hepatic cytolysis 48.51 32.34 39 7378 26805 42587113
Allergy test negative 48.45 32.34 10 7407 157 42613761
Septic shock 45.28 32.34 67 7350 91605 42522313
Multiple organ dysfunction syndrome 45.20 32.34 69 7348 96966 42516952
Hepatorenal failure 44.41 32.34 12 7405 621 42613297
Hepatocellular injury 44.06 32.34 35 7382 23643 42590275
Patent ductus arteriosus 43.70 32.34 18 7399 3458 42610460
Delayed recovery from anaesthesia 41.26 32.34 13 7404 1156 42612762
Rash morbilliform 40.62 32.34 18 7399 4135 42609783
Diarrhoea 40.34 32.34 15 7402 460834 42153084
Suspected product quality issue 39.04 32.34 9 7408 241 42613677
Coma 38.46 32.34 47 7370 53507 42560411
Respiratory depression 37.50 32.34 29 7388 18839 42595079
Post procedural haemorrhage 34.44 32.34 21 7396 9291 42604627
Haemolytic anaemia 34.08 32.34 23 7394 12104 42601814
Stress cardiomyopathy 33.58 32.34 14 7403 2771 42611147
Infantile apnoea 33.41 32.34 11 7406 1125 42612793
Torsade de pointes 33.38 32.34 20 7397 8574 42605344

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
Anaphylactic shock 4386.51 28.20 1089 14864 50457 110522889
Anaphylactic reaction 681.44 28.20 331 15622 113969 110459377
Bronchospasm 586.03 28.20 204 15749 30035 110543311
Hypotension 490.04 28.20 481 15472 523368 110049978
Maternal exposure during delivery 329.53 28.20 81 15872 3484 110569862
Tachycardia 292.75 28.20 250 15703 226395 110346951
Hyperthermia malignant 244.42 28.20 65 15888 3835 110569511
Acute generalised exanthematous pustulosis 236.18 28.20 96 15857 21568 110551778
Cardiac arrest 229.70 28.20 205 15748 196548 110376798
Circulatory collapse 218.64 28.20 112 15841 42881 110530465
Shock 203.57 28.20 115 15838 53473 110519873
Rash maculo-papular 193.30 28.20 125 15828 74097 110499249
Cardio-respiratory arrest 187.71 28.20 146 15807 115690 110457656
Drug reaction with eosinophilia and systemic symptoms 174.77 28.20 122 15831 81973 110491373
Anaphylactoid shock 174.53 28.20 38 15915 948 110572398
Type I hypersensitivity 166.79 28.20 54 15899 6339 110567007
Toxic epidermal necrolysis 166.33 28.20 103 15850 56624 110516722
Haemodynamic instability 150.29 28.20 71 15882 22817 110550529
Eosinophilia 149.41 28.20 97 15856 57839 110515507
Allergy test negative 132.31 28.20 26 15927 384 110572962
Fatigue 129.41 28.20 13 15940 1215945 109357401
Erythema 124.41 28.20 180 15773 291267 110282079
Multiple organ dysfunction syndrome 122.09 28.20 129 15824 151581 110421765
Cholestasis 114.72 28.20 86 15867 64432 110508914
Respiratory depression 114.30 28.20 66 15887 31935 110541411
Hepatocellular injury 111.81 28.20 77 15876 50565 110522781
Hepatorenal failure 106.18 28.20 27 15926 1333 110572013
Mixed liver injury 103.11 28.20 45 15908 12034 110561312
Delayed recovery from anaesthesia 102.08 28.20 29 15924 2186 110571160
Rhabdomyolysis 101.54 28.20 105 15848 120296 110453050
Mechanical ventilation complication 99.76 28.20 23 15930 748 110572598
Nervous system disorder 96.52 28.20 59 15894 31662 110541684
Myoclonus 94.37 28.20 59 15894 32939 110540407
Suspected product quality issue 88.99 28.20 20 15933 579 110572767
Stress cardiomyopathy 88.57 28.20 44 15909 15762 110557584
Bradycardia 81.26 28.20 106 15847 155411 110417935
Hypertransaminasaemia 78.65 28.20 47 15906 24208 110549138
Hepatic cytolysis 77.59 28.20 64 15889 54989 110518357
Torsade de pointes 76.44 28.20 45 15908 22555 110550791
Inspiratory capacity decreased 76.25 28.20 24 15929 2571 110570775
Oliguria 76.14 28.20 42 15911 18615 110554731
Haemothorax 76.06 28.20 31 15922 7000 110566346
Negative pressure pulmonary oedema 75.44 28.20 18 15935 681 110572665
Acute respiratory distress syndrome 71.15 28.20 60 15893 53138 110520208
Myocardial stunning 70.64 28.20 15 15938 331 110573015
Shock haemorrhagic 68.69 28.20 45 15908 27202 110546144
Septic shock 68.13 28.20 98 15855 157430 110415916
Headache 67.02 28.20 22 15931 882355 109690991
Ventricular fibrillation 66.67 28.20 52 15901 41261 110532085
Peripheral nerve injury 66.57 28.20 18 15935 1130 110572216
Spinal epidural haemorrhage 65.29 28.20 14 15939 324 110573022
Diarrhoea 64.18 28.20 43 15910 1139462 109433884
Symmetrical drug-related intertriginous and flexural exanthema 61.85 28.20 19 15934 1878 110571468
Respiratory acidosis 61.63 28.20 33 15920 13793 110559553
Anaesthetic complication 60.92 28.20 22 15931 3584 110569762
Face oedema 60.33 28.20 45 15908 33424 110539922
Propofol infusion syndrome 60.00 28.20 20 15933 2569 110570777
Rash morbilliform 59.45 28.20 27 15926 7924 110565422
Carcinoid crisis 58.38 28.20 14 15939 541 110572805
Oxygen saturation decreased 58.37 28.20 91 15862 156891 110416455
Arthralgia 58.20 28.20 20 15933 779612 109793734
Dizziness 57.39 28.20 15 15938 698178 109875168
Epidural haemorrhage 57.08 28.20 13 15940 400 110572946
Suspected product contamination 56.50 28.20 12 15941 265 110573081
Cardiogenic shock 55.65 28.20 54 15899 57284 110516062
Acute pulmonary oedema 55.27 28.20 33 15920 16963 110556383
Hypovolaemia 55.13 28.20 36 15917 21638 110551708
Coma 54.91 28.20 76 15877 117793 110455553
Hypercapnia 53.60 28.20 28 15925 11131 110562215
Postoperative delirium 51.44 28.20 14 15939 901 110572445
Malaise 50.52 28.20 17 15936 671802 109901544
Anaesthetic complication neurological 49.75 28.20 14 15939 1019 110572327
Mydriasis 49.62 28.20 34 15919 22123 110551223
Urticaria 49.21 28.20 128 15825 318729 110254617
Serotonin syndrome 48.77 28.20 51 15902 59102 110514244
Ventricular tachycardia 48.35 28.20 47 15906 49962 110523384
Emphysema 48.27 28.20 32 15921 19724 110553622
Drug interaction 48.15 28.20 170 15783 500013 110073333
Dermatitis bullous 46.76 28.20 30 15923 17499 110555847
Anticholinergic syndrome 46.74 28.20 19 15934 4261 110569085
Hypocapnia 46.71 28.20 13 15940 909 110572437
Unwanted awareness during anaesthesia 46.57 28.20 11 15942 398 110572948
Foetal heart rate abnormal 45.87 28.20 12 15941 663 110572683
Weight increased 45.77 28.20 4 15949 419640 110153706
Victim of crime 45.72 28.20 14 15939 1369 110571977
Angiopathy 45.09 28.20 23 15930 8707 110564639
Weight decreased 44.77 28.20 7 15946 468050 110105296
Anuria 44.48 28.20 33 15920 24308 110549038
Fibrinolysis increased 44.28 28.20 7 15946 25 110573321
Neuromuscular block prolonged 42.83 28.20 13 15940 1234 110572112
Altered state of consciousness 42.78 28.20 47 15906 57579 110515767
Fall 42.44 28.20 17 15936 603465 109969881
Confusion postoperative 42.44 28.20 10 15943 358 110572988
Vasoplegia syndrome 42.35 28.20 19 15934 5420 110567926
Nausea 42.26 28.20 71 15882 1235619 109337727
Hyperthermia 41.49 28.20 30 15923 21242 110552104
Stevens-Johnson syndrome 41.49 28.20 42 15911 46859 110526487
Exposure during pregnancy 41.27 28.20 81 15872 167343 110406003
Metabolic acidosis 40.13 28.20 60 15893 99684 110473662
Abdominal discomfort 39.75 28.20 5 15948 393853 110179493
Pneumothorax 39.55 28.20 36 15917 35249 110538097
Swelling 39.23 28.20 3 15950 351038 110222308
Spinal epidural haematoma 38.68 28.20 13 15940 1712 110571634
Alopecia 38.39 28.20 4 15949 364749 110208597
Anaphylactoid reaction 38.23 28.20 19 15934 6807 110566539
Epidural analgesia 38.19 28.20 8 15945 165 110573181
Infection 38.04 28.20 4 15949 362196 110211150
Procedure aborted 37.83 28.20 8 15945 173 110573173
Hyperlactacidaemia 37.55 28.20 20 15933 8266 110565080
Pain in extremity 37.17 28.20 12 15941 487106 110086240
Fear 37.00 28.20 29 15924 23164 110550182
Cough 35.88 28.20 11 15942 461630 110111716
Infusion related reaction 35.77 28.20 6 15947 381156 110192190
Apallic syndrome 35.73 28.20 11 15942 1095 110572251
Abdominal pain 35.17 28.20 15 15938 512974 110060372
Leukocytosis 35.02 28.20 41 15912 53787 110519559
Myocardial calcification 34.76 28.20 8 15945 258 110573088
Febrile neutropenia 34.58 28.20 3 15950 316764 110256582
Agitation 34.53 28.20 60 15893 112991 110460355
Sinus tachycardia 34.26 28.20 37 15916 44456 110528890
Brain hypoxia 34.13 28.20 11 15942 1271 110572075
Haemodilution 33.81 28.20 7 15946 136 110573210
Postpartum haemorrhage 33.70 28.20 12 15941 1877 110571469
Uterine hypotonus 33.43 28.20 7 15946 144 110573202
Drug diversion 33.34 28.20 11 15942 1369 110571977
Bezold-Jarisch reflex 33.16 28.20 6 15947 55 110573291
Insomnia 33.12 28.20 6 15947 360584 110212762
Asthenia 32.42 28.20 31 15922 688968 109884378
Angioedema 32.35 28.20 54 15899 98446 110474900
Tonic clonic movements 31.87 28.20 13 15940 2939 110570407
Renal injury 31.15 28.20 24 15929 18689 110554657
Myoglobin blood increased 30.47 28.20 14 15939 4218 110569128
Procedural hypotension 30.40 28.20 12 15941 2493 110570853
Pneumonia 30.26 28.20 50 15903 876664 109696682
Post procedural stroke 29.36 28.20 6 15947 109 110573237
Cauda equina syndrome 28.71 28.20 11 15942 2111 110571235
Hyperdynamic left ventricle 28.41 28.20 8 15945 584 110572762
Post procedural haemorrhage 28.27 28.20 21 15932 15491 110557855

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC N01AH03 NERVOUS SYSTEM
ANESTHETICS
ANESTHETICS, GENERAL
Opioid anesthetics
MeSH PA D000700 Analgesics
MeSH PA D000701 Analgesics, Opioid
MeSH PA D000759 Adjuvants, Anesthesia
MeSH PA D000777 Anesthetics
MeSH PA D002492 Central Nervous System Depressants
MeSH PA D009294 Narcotics
MeSH PA D018686 Anesthetics, Intravenous
MeSH PA D018689 Sensory System Agents
FDA MoA N0000175684 Full Opioid Agonists
FDA EPC N0000175690 Opioid Agonist
CHEBI has role CHEBI:35480 analgesic
CHEBI has role CHEBI:35482 opioid analgesic
CHEBI has role CHEBI:38877 intravenous anaesthetic
CHEBI has role CHEBI:55322 ฮผ-opioid receptor agonist
CHEBI has role CHEBI:60807 anaesthesia adjuvant
CHEBI has role CHEBI:67079 anti-inflammatory agent
CHEBI has role CHEBI:73336 vulnerary

Related Drugs by ATC class:

N01AH Opioid anesthetics 5 drugs
alfentanilanileridinefentanylphenoperidineremifentanil

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

DiseaseRelationSNOMED_IDDOID
General anesthesia indication 50697003
Postoperative pain indication 213299007
Asthenia contraindication 13791008
Chronic disease of respiratory system contraindication 17097001
Decreased cardiac function contraindication 43650005
Bradycardia contraindication 48867003
Injury of head contraindication 82271004
Kidney disease contraindication 90708001 DOID:557
Disease of liver contraindication 235856003 DOID:409




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 8.37 Basic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
EQ 0.03MG BASE DSUVIA VERTICAL PHARMS N209128 Nov. 2, 2018 DISCN TABLET SUBLINGUAL 10245228 Jan. 5, 2027 TREATMENT OF ACUTE PAIN
EQ 0.03MG BASE DSUVIA VERTICAL PHARMS N209128 Nov. 2, 2018 DISCN TABLET SUBLINGUAL 10507180 Jan. 5, 2027 TREATMENT OF ACUTE PAIN
EQ 0.03MG BASE DSUVIA VERTICAL PHARMS N209128 Nov. 2, 2018 DISCN TABLET SUBLINGUAL 8226978 Jan. 5, 2027 TREATMENT OF ACUTE PAIN
EQ 0.03MG BASE DSUVIA VERTICAL PHARMS N209128 Nov. 2, 2018 DISCN TABLET SUBLINGUAL 8535714 Jan. 5, 2027 TREATMENT OF ACUTE PAIN
EQ 0.03MG BASE DSUVIA VERTICAL PHARMS N209128 Nov. 2, 2018 DISCN TABLET SUBLINGUAL 8778393 Jan. 5, 2027 TREATMENT OF ACUTE PAIN
EQ 0.03MG BASE DSUVIA VERTICAL PHARMS N209128 Nov. 2, 2018 DISCN TABLET SUBLINGUAL 8778394 Jan. 5, 2027 TREATMENT OF ACUTE PAIN
EQ 0.03MG BASE DSUVIA VERTICAL PHARMS N209128 Nov. 2, 2018 DISCN TABLET SUBLINGUAL 8865211 Jan. 5, 2027 TREATMENT OF ACUTE PAIN
EQ 0.03MG BASE DSUVIA VERTICAL PHARMS N209128 Nov. 2, 2018 DISCN TABLET SUBLINGUAL 9320710 Jan. 5, 2027 TREATMENT OF ACUTE PAIN
EQ 0.03MG BASE DSUVIA VERTICAL PHARMS N209128 Nov. 2, 2018 DISCN TABLET SUBLINGUAL 8202535 Oct. 22, 2030 TREATMENT OF ACUTE PAIN
EQ 0.03MG BASE DSUVIA VERTICAL PHARMS N209128 Nov. 2, 2018 DISCN TABLET SUBLINGUAL 8865743 Oct. 22, 2030 TREATMENT OF ACUTE PAIN

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
Mu-type opioid receptor GPCR AGONIST EC50 8.13 WOMBAT-PK CHEMBL
Kappa-type opioid receptor GPCR EC50 6.70 WOMBAT-PK
Delta-type opioid receptor GPCR Ki 7.30 PDSP
Solute carrier family 22 member 1 Transporter IC50 4.71 CHEMBL
Mu-type opioid receptor GPCR Ki 9.66 CHEMBL
Sigma non-opioid intracellular receptor 1 Membrane other IC50 5.68 CHEMBL
Opioid receptor GPCR Ki 10.70 CHEMBL

External reference:

IDSource
4019936 VUID
N0000148021 NUI
D00845 KEGG_DRUG
60561-17-3 SECONDARY_CAS_RN
4019269 VANDF
4019936 VANDF
C0143993 UMLSCUI
CHEBI:9316 CHEBI
CHEMBL658 ChEMBL_ID
DB00708 DRUGBANK_ID
CHEMBL1201163 ChEMBL_ID
D017409 MESH_DESCRIPTOR_UI
41693 PUBCHEM_CID
3534 IUPHAR_LIGAND_ID
4048 INN_ID
AFE2YW0IIZ UNII
56795 RXNORM
10199 MMSL
32203 MMSL
5519 MMSL
d00378 MMSL
001570 NDDF
004630 NDDF
370275005 SNOMEDCT_US
37527009 SNOMEDCT_US
49998007 SNOMEDCT_US
AFE2YW0IIZ INXIGHT DRUGS

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Sufentanil Citrate HUMAN PRESCRIPTION DRUG LABEL 1 0409-3382 INJECTION, SOLUTION 50 ug EPIDURAL ANDA 37 sections
Sufentanil Citrate HUMAN PRESCRIPTION DRUG LABEL 1 17478-050 INJECTION 50 ug INTRAVENOUS NDA 29 sections
Dsuvia HUMAN PRESCRIPTION DRUG LABEL 1 61621-430 TABLET 30 ug SUBLINGUAL NDA 30 sections