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

Stem definitionDrug idCAS RN
analgesics 4283 175591-09-0

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • tapentadol
  • tapentadol hydrochloride
  • nucynta
  • tapentadol HCl
An opioid analgesic, MU OPIOID RECEPTOR agonist, and noradrenaline reuptake inhibitor that is used in the treatment of moderate to severe pain, and of pain associated with DIABETIC NEUROPATHIES.
  • Molecular weight: 221.34
  • Formula: C14H23NO
  • CLOGP: 3.15
  • LIPINSKI: 0
  • HAC: 2
  • HDO: 1
  • TPSA: 23.47
  • ALOGS: -2.45
  • ROTB: 5
  • Status: OFP
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
0.40 g O

ADMET properties:

PropertyValueReference
Vd (Volume of distribution) 4.64 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 21.33 mL/min/kg Lombardo F, Berellini G, Obach RS
t_half (Half-life) 2.39 hours Lombardo F, Berellini G, Obach RS
S (Water solubility) 1.16 mg/mL Bocci G, Oprea TI, Benet LZ
BDDCS (Biopharmaceutical Drug Disposition Classification System) 1 Bocci G, Oprea TI, Benet LZ
BA (Bioavailability) 32 %

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
kinase-safety-class ACVR2A,ACVR2B,AKT2,AKT3,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK4,CDK5,CDK9,DDR1,DYRK1B,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,IGF1R,ITK,JAK2,JAK3,MAP2K6,MAP3K21,MAP3K7,MAPK10,MAPK7,MAPK9,MAPKAPK2,MET,MTOR,NTRK2,PDK2,PDK4,PDPK1,PIK3CB,PIM2,PLK1,PRKCD,PRKDC,SIK2,SIK3,STK33,SYK,TEK,TGFBR1,TTK,ZAP70 49
kinase-selectivity-class ACVR2B,AXL,CAMK2D,CDK4,DDR1,EIF2AK3,EPHA2,EPHB4,FLT3,GAK,INSR,LCK,MAP3K7,MAP4K1,PDK4,SIK2,SIK3,TEK 18
pfas-class PFAS structural alert (1 = True, 0 = False) 0

Approvals:

DateAgencyCompanyOrphan
Nov. 20, 2008 FDA JANSSEN 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
Toxicity to various agents 168.05 15.35 228 15595 287618 90325006
Drug interaction 149.36 15.35 211 15612 276242 90336382
Serotonin syndrome 138.84 15.35 85 15738 37802 90574822
Sopor 132.49 15.35 71 15752 24573 90588051
Paroxysmal extreme pain disorder 89.46 15.35 16 15807 110 90612514
Miosis 89.09 15.35 40 15783 9444 90603180
Chronic respiratory disease 87.12 15.35 18 15805 283 90612341
Degenerative bone disease 82.06 15.35 17 15806 271 90612353
Confusional arousal 80.86 15.35 17 15806 292 90612332
Drug abuse 80.58 15.35 85 15738 82262 90530362
Completed suicide 78.58 15.35 111 15712 144947 90467677
Post cholecystectomy syndrome 77.52 15.35 20 15803 861 90611763
Post procedural hypothyroidism 77.23 15.35 17 15806 366 90612258
HIV infection 73.02 15.35 17 15806 474 90612150
Electric shock 72.76 15.35 22 15801 1700 90610924
Agitation 72.40 15.35 73 15750 67025 90545599
Somnolence 69.36 15.35 128 15695 208956 90403668
Blood immunoglobulin A increased 65.61 15.35 19 15804 1264 90611360
Respiratory depression 64.97 15.35 38 15785 15537 90597087
Vitamin B12 increased 63.11 15.35 20 15803 1806 90610818
Granulocyte count increased 62.25 15.35 19 15804 1515 90611109
Delirium 61.21 15.35 83 15740 104276 90508348
Glomerular filtration rate increased 60.74 15.35 20 15803 2040 90610584
Polymyalgia rheumatica 59.87 15.35 25 15798 4952 90607672
Mouth injury 58.18 15.35 17 15806 1167 90611457
Rheumatoid factor increased 57.65 15.35 20 15803 2391 90610233
Abdominal discomfort 52.31 15.35 10 15813 477318 90135306
Post-traumatic stress disorder 52.29 15.35 25 15798 6803 90605821
Suicide attempt 52.05 15.35 65 15758 75334 90537290
Intervertebral discitis 52.02 15.35 22 15801 4498 90608126
Dactylitis 51.84 15.35 21 15802 3852 90608772
Aspartate aminotransferase 51.64 15.35 14 15809 731 90611893
Systemic lupus erythematosus 51.16 15.35 3 15820 361893 90250731
Intentional overdose 51.07 15.35 72 15751 93762 90518862
Hyperhidrosis 51.01 15.35 88 15735 136217 90476407
Tremor 48.55 15.35 92 15731 153081 90459543
Vitamin D deficiency 48.52 15.35 33 15790 17523 90595101
Overdose 46.65 15.35 92 15731 157617 90455007
Restlessness 46.30 15.35 43 15780 35677 90576947
Throat clearing 45.19 15.35 19 15804 3828 90608796
Hallucination 44.15 15.35 56 15767 65903 90546721
Tongue discomfort 44.04 15.35 17 15806 2748 90609876
Hyperthermia malignant 43.96 15.35 14 15809 1284 90611340
Blood uric acid increased 43.66 15.35 23 15800 7681 90604943
Abnormal dreams 43.13 15.35 26 15797 11231 90601393
Multiple sclerosis 42.99 15.35 37 15786 27803 90584821
Joint noise 42.44 15.35 20 15803 5270 90607354
Reflexes abnormal 42.05 15.35 12 15811 757 90611867
Disorientation 40.42 15.35 44 15779 44070 90568554
Hypertensive crisis 38.92 15.35 29 15794 17755 90594869
Wound 38.65 15.35 4 15819 302976 90309648
Vitamin B12 deficiency 38.63 15.35 21 15802 7465 90605159
Unresponsive to stimuli 38.43 15.35 40 15783 38081 90574543
Monocyte count increased 37.43 15.35 22 15801 9075 90603549
Arthropathy 37.39 15.35 9 15814 366233 90246391
Spinal disorder 37.23 15.35 24 15799 11655 90600969
Joint swelling 36.96 15.35 21 15802 503279 90109345
Mydriasis 36.30 15.35 26 15797 14986 90597638
Breast cancer metastatic 36.11 15.35 26 15797 15106 90597518
Loss of consciousness 35.80 15.35 77 15746 140161 90472463
White blood cells urine positive 35.69 15.35 19 15804 6479 90606145
Sepsis neonatal 35.48 15.35 10 15813 603 90612021
Syncope 35.20 15.35 74 15749 132589 90480035
Amnestic disorder 34.45 15.35 9 15814 407 90612217
Cholecystitis acute 34.18 15.35 21 15802 9383 90603241
Depressed level of consciousness 34.03 15.35 52 15771 72732 90539892
Embolism venous 33.14 15.35 15 15808 3605 90609019
Progressive multifocal leukoencephalopathy 33.08 15.35 25 15798 15630 90596994
Peptic ulcer 32.90 15.35 17 15806 5458 90607166
Confusional state 32.87 15.35 144 15679 386061 90226563
Hepatic enzyme increased 32.87 15.35 11 15812 360725 90251899
Maternal exposure during pregnancy 32.78 15.35 11 15812 360052 90252572
Seizure 32.50 15.35 78 15745 152551 90460073
Suicidal ideation 32.07 15.35 51 15772 73804 90538820
Blood pressure systolic decreased 31.91 15.35 20 15803 9250 90603374
Demyelination 31.70 15.35 19 15804 8121 90604503
Accidental exposure to product by child 31.65 15.35 11 15812 1322 90611302
Chemical burn of oral cavity 30.94 15.35 6 15817 67 90612557
Blister 30.93 15.35 4 15819 254994 90357630
Short-bowel syndrome 30.10 15.35 9 15814 669 90611955
Off label use 29.28 15.35 97 15726 1102155 89510469
Application site injury 29.15 15.35 5 15818 26 90612598
Aspartate aminotransferase abnormal 27.54 15.35 12 15811 2637 90609987
Cognitive disorder 27.52 15.35 46 15777 69361 90543263
Temperature intolerance 27.18 15.35 20 15803 12010 90600614
Bundle branch block left 27.12 15.35 17 15806 7868 90604756
Withdrawal syndrome 27.06 15.35 26 15797 22498 90590126
Eyelid skin dryness 27.01 15.35 8 15815 576 90612048
Osteopenia 26.60 15.35 26 15797 22976 90589648
Constipation 26.52 15.35 108 15715 280287 90332337
Allodynia 26.45 15.35 9 15814 1015 90611609
Drug screen negative 26.41 15.35 7 15816 335 90612289
Swelling 26.04 15.35 21 15802 419037 90193587
Renal cell carcinoma stage I 25.94 15.35 5 15818 54 90612570
Irritable bowel syndrome 25.78 15.35 3 15820 207445 90405179
Drug withdrawal syndrome neonatal 25.73 15.35 11 15812 2308 90610316
Malignant neoplasm progression 25.36 15.35 57 15766 106813 90505811
Middle insomnia 25.33 15.35 22 15801 16729 90595895
Gingivitis 24.44 15.35 17 15806 9352 90603272
Blood glucose decreased 24.36 15.35 25 15798 23404 90589220
Clubbing 23.78 15.35 7 15816 493 90612131
Depressed mood 23.64 15.35 36 15787 50186 90562438
Drug screen positive 23.54 15.35 12 15811 3745 90608879
Blood cholesterol increased 23.53 15.35 4 15819 208008 90404616
Application site ulcer 23.51 15.35 5 15818 91 90612533
Hypoglycaemia 23.41 15.35 43 15780 69805 90542819
Dyslipidaemia 23.28 15.35 17 15806 10090 90602534
Opiates negative 22.96 15.35 3 15820 0 90612624
Glycosylated haemoglobin increased 22.65 15.35 20 15803 15542 90597082
Gaze palsy 22.31 15.35 9 15814 1632 90610992
Nasal polyps 22.16 15.35 17 15806 10863 90601761
Nausea 21.78 15.35 292 15531 1110024 89502600
Infection 21.44 15.35 19 15804 362075 90250549
Disturbance in attention 21.09 15.35 33 15790 47076 90565548
Logorrhoea 20.93 15.35 10 15813 2717 90609907
Product prescribing error 20.81 15.35 26 15797 30119 90582505
Neutrophil count increased 20.72 15.35 21 15802 19369 90593255
Blood urea increased 20.63 15.35 26 15797 30387 90582237
Urinary retention 20.58 15.35 29 15794 37715 90574909
Bradyphrenia 20.30 15.35 14 15809 7598 90605026
Cardio-respiratory arrest 20.07 15.35 38 15785 63102 90549522
Labelled drug-drug interaction medication error 19.76 15.35 18 15805 14564 90598060
Therapeutic product effect decreased 19.75 15.35 12 15811 277559 90335065
Pharyngeal enanthema 19.73 15.35 4 15819 57 90612567
Synovectomy 19.34 15.35 5 15818 217 90612407
Thoracic vertebral fracture 19.32 15.35 12 15811 5462 90607162
Concomitant disease aggravated 19.20 15.35 16 15807 11502 90601122
Hyperresponsive to stimuli 19.18 15.35 4 15819 66 90612558
Psoriatic arthropathy 19.05 15.35 8 15815 228327 90384297
Coordination abnormal 19.04 15.35 21 15802 21335 90591289
Tinnitus 19.03 15.35 30 15793 43072 90569552
Myoclonic epilepsy 18.99 15.35 8 15815 1619 90611005
Pneumonia aspiration 18.78 15.35 29 15794 40911 90571713
Lymphoedema 18.68 15.35 17 15806 13736 90598888
Tachycardia 18.42 15.35 65 15758 157608 90455016
Presyncope 18.18 15.35 25 15798 31780 90580844
Alopecia 18.12 15.35 37 15786 495034 90117590
Liver injury 17.77 15.35 4 15819 170563 90442061
Bacteriuria 17.74 15.35 7 15816 1199 90611425
Small intestinal resection 17.67 15.35 6 15817 672 90611952
Blood test abnormal 17.64 15.35 20 15803 20932 90591692
Lower respiratory tract infection 17.61 15.35 11 15812 250648 90361976
Ulcer 17.53 15.35 25 15798 32857 90579767
Hypersensitivity 17.49 15.35 33 15790 454644 90157980
Nervous system disorder 17.15 15.35 20 15803 21573 90591051
Infusion related reaction 17.15 15.35 29 15794 416751 90195873
Pneumonia 16.98 15.35 56 15767 638003 89974621
Dyskinesia 16.93 15.35 26 15797 36508 90576116
Aortic valve stenosis 16.78 15.35 10 15813 4230 90608394
Treatment failure 16.75 15.35 17 15806 303911 90308713
Total bile acids increased 16.62 15.35 4 15819 129 90612495
Sedation 16.58 15.35 30 15793 48141 90564483
Contraindicated product administered 16.44 15.35 19 15804 320120 90292504
Lumbar vertebral fracture 15.96 15.35 12 15811 7446 90605178
Rhinitis allergic 15.82 15.35 17 15806 16768 90595856
Drug screen false positive 15.74 15.35 6 15817 937 90611687
Discomfort 15.52 15.35 15 15808 274320 90338304
Rash 15.47 15.35 79 15744 796021 89816603
Product use issue 15.45 15.35 21 15802 329898 90282726
Anal hypoaesthesia 15.43 15.35 3 15820 34 90612590

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
Serotonin syndrome 148.34 19.21 81 8339 25764 42587151
Delirium 137.43 19.21 100 8320 52419 42560496
Toxicity to various agents 131.99 19.21 192 8228 228944 42383971
Drug abuse 128.44 19.21 129 8291 104642 42508273
Quality of life decreased 117.31 19.21 43 8377 5333 42607582
Hyperaesthesia 116.66 19.21 44 8376 5908 42607007
Constipation 111.24 19.21 148 8272 162143 42450772
Allodynia 75.35 19.21 21 8399 1073 42611842
Drug dependence 72.86 19.21 54 8366 29040 42583875
Polyneuropathy in malignant disease 70.05 19.21 16 8404 360 42612555
Overdose 61.47 19.21 89 8331 105175 42507740
Confusional state 59.21 19.21 113 8307 167484 42445431
Sopor 58.56 19.21 35 8385 13167 42599748
Suicide attempt 53.14 19.21 55 8365 46045 42566870
Intentional overdose 51.57 19.21 57 8363 51399 42561516
Congenital megacolon 42.35 19.21 8 8412 67 42612848
Hallucination 40.09 19.21 53 8367 57454 42555461
Respiratory syncytial virus bronchitis 39.51 19.21 8 8412 99 42612816
Drug interaction 39.46 19.21 129 8291 266870 42346045
Somnolence 38.96 19.21 86 8334 141019 42471896
Withdrawal syndrome 38.27 19.21 28 8392 14747 42598168
Sleep deficit 37.98 19.21 12 8408 947 42611968
Testicular seminoma (pure) 34.18 19.21 8 8412 201 42612714
Loss of consciousness 32.20 19.21 62 8358 92292 42520623
Dysaesthesia 29.74 19.21 13 8407 2544 42610371
Xanthelasma 28.63 19.21 6 8414 89 42612826
Respiratory depression 28.26 19.21 26 8394 18842 42594073
Urinary retention 28.02 19.21 38 8382 42176 42570739
Malignant neoplasm progression 27.59 19.21 64 8356 108336 42504579
Application site hypersensitivity 27.48 19.21 6 8414 109 42612806
Metastases to bone 27.38 19.21 23 8397 14786 42598129
Post herpetic neuralgia 27.30 19.21 10 8410 1236 42611679
Drug screen positive 26.62 19.21 14 8406 4117 42608798
Drug withdrawal syndrome 25.33 19.21 26 8394 21523 42591392
Application site pain 24.38 19.21 11 8409 2318 42610597
Dermatitis allergic 24.08 19.21 17 8403 8466 42604449
Metastases to lung 23.75 19.21 19 8401 11405 42601510
Application site erythema 23.36 19.21 11 8409 2555 42610360
Adverse event 23.34 19.21 26 8394 23614 42589301
Poor feeding infant 23.16 19.21 8 8412 834 42612081
Tremor 22.26 19.21 55 8365 96874 42516041
Accidental exposure to product by child 21.64 19.21 9 8411 1558 42611357
Disorientation 21.53 19.21 31 8389 36358 42576557
Nausea 21 19.21 142 8278 396657 42216258
Reaction to excipient 21.00 19.21 7 8413 655 42612260
Pharyngeal inflammation 20.89 19.21 7 8413 665 42612250
Myofascial pain syndrome 20.57 19.21 6 8414 361 42612554
Depression 20.30 19.21 58 8362 111305 42501610
Sedation 19.57 19.21 27 8393 30448 42582467

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Toxicity to various agents 267.31 15.03 384 20183 480171 110088561
Drug abuse 205.02 15.03 206 20361 177205 110391527
Serotonin syndrome 187.68 15.03 124 20443 59029 110509703
Sopor 173.19 15.03 99 20468 36447 110532285
Drug interaction 147.72 15.03 302 20265 499881 110068851
Delirium 129.46 15.03 142 20425 134883 110433849
Hyperaesthesia 103.87 15.03 52 20515 14675 110554057
Allodynia 100.89 15.03 30 20537 2053 110566679
Suicide attempt 90.95 15.03 104 20463 103290 110465442
Constipation 90.42 15.03 203 20364 357583 110211149
Respiratory depression 89.33 15.03 62 20505 31939 110536793
Somnolence 86.89 15.03 179 20388 297270 110271462
Intentional overdose 85.46 15.03 114 20453 132387 110436345
Miosis 84.39 15.03 52 20515 21931 110546801
Quality of life decreased 82.55 15.03 44 20523 14125 110554607
Overdose 79.51 15.03 150 20417 233644 110335088
Confusional state 73.15 15.03 222 20345 468458 110100274
Accidental exposure to product by child 72.83 15.03 26 20541 3172 110565560
Post cholecystectomy syndrome 72.12 15.03 19 20548 833 110567899
Polyneuropathy in malignant disease 66.43 15.03 16 20551 485 110568247
Completed suicide 66.25 15.03 142 20425 242239 110326493
Disorientation 65.39 15.03 73 20494 70598 110498134
Loss of consciousness 63.09 15.03 123 20444 196183 110372549
Drug dependence 63.08 15.03 61 20506 49959 110518773
Tremor 61.73 15.03 124 20443 202108 110366624
Electric shock 57.79 15.03 19 20548 1809 110566923
Glomerular filtration rate increased 56.64 15.03 19 20548 1926 110566806
Blood immunoglobulin A increased 56.51 15.03 18 20549 1550 110567182
Agitation 56.27 15.03 86 20481 112965 110455767
Vitamin B12 increased 55.61 15.03 19 20548 2036 110566696
Granulocyte count increased 52.36 15.03 18 20549 1965 110566767
Rheumatoid factor increased 51.93 15.03 19 20548 2486 110566246
Post-traumatic stress disorder 48.61 15.03 24 20543 6572 110562160
Restlessness 48.46 15.03 56 20511 56203 110512529
Malignant neoplasm progression 47.35 15.03 102 20465 174465 110394267
Aspartate aminotransferase 47.12 15.03 14 20553 955 110567777
Hyperhidrosis 46.92 15.03 106 20461 187192 110381540
Dactylitis 45.96 15.03 20 20547 4113 110564619
Sepsis neonatal 45.80 15.03 9 20558 101 110568631
Vitamin D deficiency 44.99 15.03 33 20534 18519 110550213
Intervertebral discitis 41.54 15.03 22 20545 6968 110561764
Hallucination 39.41 15.03 69 20498 101363 110467369
Joint noise 38.75 15.03 19 20548 5124 110563608
Throat clearing 38.73 15.03 18 20549 4315 110564417
Depressed level of consciousness 38.07 15.03 72 20495 112206 110456526
Reflexes abnormal 37.65 15.03 12 20555 1035 110567697
Drug screen positive 37.60 15.03 20 20547 6390 110562342
Multiple sclerosis 37.51 15.03 34 20533 25664 110543068
Nausea 37.48 15.03 372 20195 1235318 109333414
Joint swelling 37.09 15.03 18 20549 442827 110125905
Off label use 36.95 15.03 149 20418 1500036 109068696
Testicular seminoma (pure) 36.21 15.03 8 20559 164 110568568
Withdrawal syndrome 35.36 15.03 36 20531 31344 110537388
Application site pain 34.65 15.03 18 20549 5481 110563251
Application site erythema 34.31 15.03 18 20549 5592 110563140
Temperature intolerance 34.25 15.03 25 20542 13925 110554807
Spinal disorder 33.37 15.03 23 20544 11705 110557027
Hypertensive crisis 33.15 15.03 31 20536 24341 110544391
Unresponsive to stimuli 32.40 15.03 49 20518 63741 110504991
White blood cells urine positive 31.97 15.03 19 20548 7505 110561227
Sleep deficit 31.34 15.03 12 20555 1780 110566952
Maternal exposure during pregnancy 31.20 15.03 5 20562 254878 110313854
Drug withdrawal syndrome neonatal 30.67 15.03 8 20559 337 110568395
Vitamin B12 deficiency 29.27 15.03 20 20547 10035 110558697
Sedation 29.16 15.03 49 20518 69634 110499098
Application site injury 29.00 15.03 5 20562 25 110568707
Pneumonia aspiration 28.66 15.03 53 20514 81180 110487552
Amnestic disorder 28.65 15.03 9 20558 741 110567991
Hepatic enzyme increased 28.49 15.03 12 20555 320880 110247852
Short-bowel syndrome 28.34 15.03 9 20558 767 110567965
Hyperthermia malignant 28.17 15.03 14 20553 3886 110564846
Mydriasis 27.89 15.03 27 20540 22130 110546602
Alopecia 27.37 15.03 17 20550 364736 110203996
Abdominal discomfort 27.36 15.03 20 20547 393838 110174894
Disturbance in attention 26.48 15.03 44 20523 61951 110506781
Monocyte count increased 26.41 15.03 21 20546 13272 110555460
Syncope 26.13 15.03 90 20477 202446 110366286
Demyelination 25.68 15.03 18 20549 9411 110559321
Xanthelasma 25.54 15.03 6 20561 163 110568569
Eyelid skin dryness 24.98 15.03 8 20559 701 110568031
Drug withdrawal syndrome 24.90 15.03 33 20534 38021 110530711
Pharyngeal inflammation 24.78 15.03 10 20557 1704 110567028
Chemical burn of oral cavity 24.63 15.03 5 20562 67 110568665
Infection 24.37 15.03 19 20548 362181 110206551
Aspartate aminotransferase abnormal 24.21 15.03 12 20555 3313 110565419
Blood cholesterol increased 24.07 15.03 3 20564 184782 110383950
Seizure 24.06 15.03 93 20474 221092 110347640
Hallucination, visual 23.87 15.03 33 20534 39572 110529160
Hypersensitivity 23.81 15.03 24 20543 403974 110164758
Arthropathy 23.58 15.03 12 20555 287510 110281222
Renal cell carcinoma stage I 23.57 15.03 5 20562 84 110568648
False positive investigation result 23.06 15.03 9 20558 1405 110567327
Blood pressure systolic decreased 22.04 15.03 19 20548 13422 110555310
Wheezing 21.93 15.03 10 20557 255220 110313512
Application site ulcer 21.84 15.03 5 20562 121 110568611
Psoriatic arthropathy 21.67 15.03 5 20562 196756 110371976
Urinary retention 21.56 15.03 43 20524 69640 110499092
Cholecystitis acute 21.32 15.03 20 20547 15762 110552970
Exposure during pregnancy 21.14 15.03 3 20564 167421 110401311
Benign prostatic hyperplasia 20.69 15.03 21 20546 18213 110550519
Dysphagia 20.46 15.03 69 20498 153531 110415201
Psychomotor skills impaired 20.46 15.03 14 20553 7044 110561688
Micturition disorder 20.32 15.03 12 20555 4686 110564046
Cognitive disorder 20.22 15.03 48 20519 87463 110481269
Progressive multifocal leukoencephalopathy 20.08 15.03 24 20543 24932 110543800
Clubbing 20.07 15.03 7 20560 798 110567934
Product prescribing error 20.03 15.03 35 20532 51296 110517436
Anal hypoaesthesia 19.81 15.03 4 20563 52 110568680
Blood uric acid increased 19.50 15.03 22 20545 21507 110547225
Swelling 19.40 15.03 22 20545 351019 110217713
Depressed mood 19.38 15.03 38 20529 60771 110507961
Hyperresponsive to stimuli 19.28 15.03 4 20563 60 110568672
Substance abuse 19.20 15.03 17 20550 12446 110556286
Ulcer 18.95 15.03 31 20536 43085 110525647
Thoracic vertebral fracture 18.81 15.03 13 20554 6642 110562090
Pharyngeal enanthema 18.70 15.03 4 20563 70 110568662
Metastases to bone 18.70 15.03 26 20541 31346 110537386
Lower respiratory tract infection 18.69 15.03 11 20556 243095 110325637
Dysaesthesia 18.48 15.03 13 20554 6834 110561898
Irritable bowel syndrome 18.43 15.03 4 20563 164211 110404521
Blood glucose decreased 18.42 15.03 25 20542 29463 110539269
Synovectomy 18.11 15.03 5 20562 262 110568470
Bradyphrenia 18.07 15.03 16 20551 11712 110557020
Impaired healing 18.03 15.03 7 20560 196710 110372022
Psychomotor hyperactivity 17.15 15.03 20 20547 20257 110548475
Embolism venous 17.06 15.03 11 20556 5012 110563720
Accident 16.99 15.03 15 20552 10937 110557795
Cachexia 16.65 15.03 16 20551 12989 110555743
Vertigo 16.26 15.03 44 20523 86826 110481906
Bacteriuria 16.12 15.03 7 20560 1431 110567301
Dermatitis allergic 16.04 15.03 20 20547 21704 110547028
Weight increased 15.84 15.03 34 20533 419610 110149122
Post herpetic neuralgia 15.78 15.03 9 20558 3292 110565440
Clonus 15.69 15.03 13 20554 8703 110560029
Asthenia 15.55 15.03 196 20371 688803 109879929
Gaze palsy 15.52 15.03 9 20558 3398 110565334
Intestinal obstruction 15.46 15.03 32 20535 53195 110515537
Spinal fracture 15.38 15.03 20 20547 22613 110546119
Blister 15.19 15.03 12 20555 227364 110341368
Coordination abnormal 15.17 15.03 21 20546 25207 110543525
Metastases to lung 15.09 15.03 20 20547 23043 110545689
Suicidal ideation 15.07 15.03 45 20522 93892 110474840

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC N02AX06 NERVOUS SYSTEM
ANALGESICS
OPIOIDS
Other opioids
FDA MoA N0000000174 Opioid Agonists
MeSH PA D000700 Analgesics
MeSH PA D000701 Analgesics, Opioid
MeSH PA D002492 Central Nervous System Depressants
MeSH PA D009294 Narcotics
MeSH PA D014179 Neurotransmitter Uptake Inhibitors
MeSH PA D018377 Neurotransmitter Agents
MeSH PA D018663 Adrenergic Agents
MeSH PA D018689 Sensory System Agents
MeSH PA D018759 Adrenergic Uptake Inhibitors
MeSH PA D049990 Membrane Transport Modulators
FDA EPC N0000175690 Opioid Agonist
CHEBI has role CHEBI:35480 analgesic
CHEBI has role CHEBI:35610 antineoplastic agent
CHEBI has role CHEBI:67079 anti-inflammatory agent

Related Drugs by ATC class:

N02AX Other opioids 6 drugs
dezocinemeptazinolnaloxoneoliceridinetilidinetramadol

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

DiseaseRelationSNOMED_IDDOID
Pain indication 22253000
Chronic obstructive lung disease contraindication 13645005 DOID:3083
Asthenia contraindication 13791008
Alcohol intoxication contraindication 25702006
Hypercapnia contraindication 29596007
Myxedema contraindication 43153006 DOID:11634
Paralytic ileus contraindication 55525008 DOID:8442
Substance abuse contraindication 66214007
Benign intracranial hypertension contraindication 68267002 DOID:11459
Sleep apnea contraindication 73430006 DOID:0050847
Pancreatitis contraindication 75694006 DOID:4989
Decreased respiratory function contraindication 80954004
Injury of head contraindication 82271004
Cor pulmonale contraindication 83291003 DOID:8515
Disorder of biliary tract contraindication 105997008 DOID:9741
Seizure disorder contraindication 128613002
Disease of liver contraindication 235856003 DOID:409
Morbid obesity contraindication 238136002 DOID:11981
Exacerbation of asthma contraindication 281239006
Lesion of brain contraindication 301766008
Coma contraindication 371632003
Hypoxia contraindication 389086002
Central nervous system depression contraindication 418072004
Acute exacerbation of asthma contraindication 708038006
Kyphoscoliosis with Respiratory Compromise contraindication




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 9.76 acidic
pKa2 9.12 Basic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
EQ 100MG BASE NUCYNTA ER COLLEGIUM PHARM INC N200533 Aug. 25, 2011 RX TABLET, EXTENDED RELEASE ORAL 11344512 April 21, 2028 A METHOD OF TITRATING AN OPIOID TO MANAGE NEUROPATHIC PAIN ASSOCIATED WITH DIABETIC PERIPHERAL NEUROPATHY SEVERE ENOUGH TO REQUIRE DAILY, AROUND-THE-CLOCK, LONG-TERM OPIOID TREATMENT AND FOR WHICH ALTERNATIVE TREATMENT OPTIONS ARE INADEQUATE
EQ 100MG BASE NUCYNTA ER COLLEGIUM PHARM INC N200533 Aug. 25, 2011 RX TABLET, EXTENDED RELEASE ORAL 11344512 April 21, 2028 A METHOD OF TITRATING AN OPIOID TO MANAGE PAIN SEVERE ENOUGH TO REQUIRE DAILY, AROUND-THE-CLOCK, LONG-TERM OPIOID TREATMENT AND FOR WHICH ALTERNATIVE TREATMENTS ARE INADEQUATE
EQ 150MG BASE NUCYNTA ER COLLEGIUM PHARM INC N200533 Aug. 25, 2011 RX TABLET, EXTENDED RELEASE ORAL 11344512 April 21, 2028 A METHOD OF TITRATING AN OPIOID TO MANAGE NEUROPATHIC PAIN ASSOCIATED WITH DIABETIC PERIPHERAL NEUROPATHY SEVERE ENOUGH TO REQUIRE DAILY, AROUND-THE-CLOCK, LONG-TERM OPIOID TREATMENT AND FOR WHICH ALTERNATIVE TREATMENT OPTIONS ARE INADEQUATE
EQ 150MG BASE NUCYNTA ER COLLEGIUM PHARM INC N200533 Aug. 25, 2011 RX TABLET, EXTENDED RELEASE ORAL 11344512 April 21, 2028 A METHOD OF TITRATING AN OPIOID TO MANAGE PAIN SEVERE ENOUGH TO REQUIRE DAILY, AROUND-THE-CLOCK, LONG-TERM OPIOID TREATMENT AND FOR WHICH ALTERNATIVE TREATMENTS ARE INADEQUATE
EQ 200MG BASE NUCYNTA ER COLLEGIUM PHARM INC N200533 Aug. 25, 2011 RX TABLET, EXTENDED RELEASE ORAL 11344512 April 21, 2028 A METHOD OF TITRATING AN OPIOID TO MANAGE NEUROPATHIC PAIN ASSOCIATED WITH DIABETIC PERIPHERAL NEUROPATHY SEVERE ENOUGH TO REQUIRE DAILY, AROUND-THE-CLOCK, LONG-TERM OPIOID TREATMENT AND FOR WHICH ALTERNATIVE TREATMENT OPTIONS ARE INADEQUATE
EQ 200MG BASE NUCYNTA ER COLLEGIUM PHARM INC N200533 Aug. 25, 2011 RX TABLET, EXTENDED RELEASE ORAL 11344512 April 21, 2028 A METHOD OF TITRATING AN OPIOID TO MANAGE PAIN SEVERE ENOUGH TO REQUIRE DAILY, AROUND-THE-CLOCK, LONG-TERM OPIOID TREATMENT AND FOR WHICH ALTERNATIVE TREATMENTS ARE INADEQUATE
EQ 250MG BASE NUCYNTA ER COLLEGIUM PHARM INC N200533 Aug. 25, 2011 RX TABLET, EXTENDED RELEASE ORAL 11344512 April 21, 2028 A METHOD OF TITRATING AN OPIOID TO MANAGE NEUROPATHIC PAIN ASSOCIATED WITH DIABETIC PERIPHERAL NEUROPATHY SEVERE ENOUGH TO REQUIRE DAILY, AROUND-THE-CLOCK, LONG-TERM OPIOID TREATMENT AND FOR WHICH ALTERNATIVE TREATMENT OPTIONS ARE INADEQUATE
EQ 250MG BASE NUCYNTA ER COLLEGIUM PHARM INC N200533 Aug. 25, 2011 RX TABLET, EXTENDED RELEASE ORAL 11344512 April 21, 2028 A METHOD OF TITRATING AN OPIOID TO MANAGE PAIN SEVERE ENOUGH TO REQUIRE DAILY, AROUND-THE-CLOCK, LONG-TERM OPIOID TREATMENT AND FOR WHICH ALTERNATIVE TREATMENTS ARE INADEQUATE
EQ 50MG BASE NUCYNTA ER COLLEGIUM PHARM INC N200533 Aug. 25, 2011 RX TABLET, EXTENDED RELEASE ORAL 11344512 April 21, 2028 A METHOD OF TITRATING AN OPIOID TO MANAGE NEUROPATHIC PAIN ASSOCIATED WITH DIABETIC PERIPHERAL NEUROPATHY SEVERE ENOUGH TO REQUIRE DAILY, AROUND-THE-CLOCK, LONG-TERM OPIOID TREATMENT AND FOR WHICH ALTERNATIVE TREATMENT OPTIONS ARE INADEQUATE
EQ 50MG BASE NUCYNTA ER COLLEGIUM PHARM INC N200533 Aug. 25, 2011 RX TABLET, EXTENDED RELEASE ORAL 11344512 April 21, 2028 A METHOD OF TITRATING AN OPIOID TO MANAGE PAIN SEVERE ENOUGH TO REQUIRE DAILY, AROUND-THE-CLOCK, LONG-TERM OPIOID TREATMENT AND FOR WHICH ALTERNATIVE TREATMENTS ARE INADEQUATE
EQ 100MG BASE NUCYNTA ER COLLEGIUM PHARM INC N200533 Aug. 25, 2011 RX TABLET, EXTENDED RELEASE ORAL 8536130 Sept. 22, 2028 MANAGEMENT OF NEUROPATHIC PAIN ASSOCIATED WITH DIABETIC PERIPHERAL NEUROPATHY
EQ 150MG BASE NUCYNTA ER COLLEGIUM PHARM INC N200533 Aug. 25, 2011 RX TABLET, EXTENDED RELEASE ORAL 8536130 Sept. 22, 2028 MANAGEMENT OF NEUROPATHIC PAIN ASSOCIATED WITH DIABETIC PERIPHERAL NEUROPATHY
EQ 200MG BASE NUCYNTA ER COLLEGIUM PHARM INC N200533 Aug. 25, 2011 RX TABLET, EXTENDED RELEASE ORAL 8536130 Sept. 22, 2028 MANAGEMENT OF NEUROPATHIC PAIN ASSOCIATED WITH DIABETIC PERIPHERAL NEUROPATHY
EQ 250MG BASE NUCYNTA ER COLLEGIUM PHARM INC N200533 Aug. 25, 2011 RX TABLET, EXTENDED RELEASE ORAL 8536130 Sept. 22, 2028 MANAGEMENT OF NEUROPATHIC PAIN ASSOCIATED WITH DIABETIC PERIPHERAL NEUROPATHY
EQ 50MG BASE NUCYNTA ER COLLEGIUM PHARM INC N200533 Aug. 25, 2011 RX TABLET, EXTENDED RELEASE ORAL 8536130 Sept. 22, 2028 MANAGEMENT OF NEUROPATHIC PAIN ASSOCIATED WITH DIABETIC PERIPHERAL NEUROPATHY

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
EQ 100MG BASE NUCYNTA COLLEGIUM PHARM INC N022304 Nov. 20, 2008 RX TABLET ORAL July 3, 2026 NEW PATIENT POPULATION
EQ 50MG BASE NUCYNTA COLLEGIUM PHARM INC N022304 Nov. 20, 2008 RX TABLET ORAL July 3, 2026 NEW PATIENT POPULATION
EQ 75MG BASE NUCYNTA COLLEGIUM PHARM INC N022304 Nov. 20, 2008 RX TABLET ORAL July 3, 2026 NEW PATIENT POPULATION
EQ 20MG BASE/ML **Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons** NUCYNTA COLLEGIUM PHARM INC N203794 Oct. 15, 2012 DISCN SOLUTION ORAL July 3, 2026 NEW PATIENT POPULATION
EQ 100MG BASE NUCYNTA COLLEGIUM PHARM INC N022304 Nov. 20, 2008 RX TABLET ORAL Jan. 3, 2027 PEDIATRIC EXCLUSIVITY
EQ 50MG BASE NUCYNTA COLLEGIUM PHARM INC N022304 Nov. 20, 2008 RX TABLET ORAL Jan. 3, 2027 PEDIATRIC EXCLUSIVITY
EQ 75MG BASE NUCYNTA COLLEGIUM PHARM INC N022304 Nov. 20, 2008 RX TABLET ORAL Jan. 3, 2027 PEDIATRIC EXCLUSIVITY
EQ 20MG BASE/ML **Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons** NUCYNTA COLLEGIUM PHARM INC N203794 Oct. 15, 2012 DISCN SOLUTION ORAL Jan. 3, 2027 PEDIATRIC EXCLUSIVITY

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
Mu-type opioid receptor GPCR AGONIST Ki 7.02 WOMBAT-PK CHEMBL
Sodium-dependent noradrenaline transporter Transporter INHIBITOR Ki 6.32 WOMBAT-PK CHEMBL
Solute carrier family 22 member 1 Transporter IC50 4.66 CHEMBL

External reference:

IDSource
4029061 VUID
N0000179820 NUI
D06007 KEGG_DRUG
175591-23-8 SECONDARY_CAS_RN
4029061 VANDF
4029062 VANDF
C2001271 UMLSCUI
CHEBI:135935 CHEBI
CHEMBL1201776 ChEMBL_ID
CHEMBL1201777 ChEMBL_ID
D000077432 MESH_DESCRIPTOR_UI
DB06204 DRUGBANK_ID
7477 IUPHAR_LIGAND_ID
8216 INN_ID
H8A007M585 UNII
9838022 PUBCHEM_CID
787390 RXNORM
165888 MMSL
26545 MMSL
303726 MMSL
35753 MMSL
d07453 MMSL
013168 NDDF
013169 NDDF
441757005 SNOMEDCT_US
442004000 SNOMEDCT_US
442699004 SNOMEDCT_US
H8A007M585 INXIGHT DRUGS

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
TAPENTADOL HUMAN PRESCRIPTION DRUG LABEL 1 0054-0936 TABLET, FILM COATED, EXTENDED RELEASE 50 mg ORAL NDA authorized generic 39 sections
TAPENTADOL HUMAN PRESCRIPTION DRUG LABEL 1 0054-0937 TABLET, FILM COATED, EXTENDED RELEASE 100 mg ORAL NDA authorized generic 39 sections
TAPENTADOL HUMAN PRESCRIPTION DRUG LABEL 1 0054-0938 TABLET, FILM COATED, EXTENDED RELEASE 150 mg ORAL NDA authorized generic 39 sections
TAPENTADOL HUMAN PRESCRIPTION DRUG LABEL 1 0054-0939 TABLET, FILM COATED, EXTENDED RELEASE 200 mg ORAL NDA authorized generic 39 sections
TAPENTADOL HUMAN PRESCRIPTION DRUG LABEL 1 0054-0940 TABLET, FILM COATED, EXTENDED RELEASE 250 mg ORAL NDA authorized generic 39 sections
TAPENTADOL HUMAN PRESCRIPTION DRUG LABEL 1 0054-0942 TABLET, FILM COATED 50 mg ORAL NDA authorized generic 39 sections
TAPENTADOL HUMAN PRESCRIPTION DRUG LABEL 1 0054-0943 TABLET, FILM COATED 75 mg ORAL NDA authorized generic 39 sections
TAPENTADOL HUMAN PRESCRIPTION DRUG LABEL 1 0054-0945 TABLET, FILM COATED 100 mg ORAL NDA authorized generic 39 sections
NUCYNTA HUMAN PRESCRIPTION DRUG LABEL 1 16590-289 TABLET, FILM COATED 100 mg ORAL NDA 35 sections
NUCYNTA HUMAN PRESCRIPTION DRUG LABEL 1 16590-863 TABLET, FILM COATED 50 mg ORAL NDA 35 sections
NUCYNTA HUMAN PRESCRIPTION DRUG LABEL 1 16590-889 TABLET, FILM COATED 75 mg ORAL NDA 32 sections
NUCYNTA HUMAN PRESCRIPTION DRUG LABEL 1 21695-069 TABLET, FILM COATED 50 mg ORAL NDA 34 sections
Nucynta HUMAN PRESCRIPTION DRUG LABEL 1 24510-050 TABLET, FILM COATED 50 mg ORAL NDA 39 sections
NucyntaER HUMAN PRESCRIPTION DRUG LABEL 1 24510-058 TABLET, FILM COATED, EXTENDED RELEASE 50 mg ORAL NDA 39 sections
Nucynta HUMAN PRESCRIPTION DRUG LABEL 1 24510-075 TABLET, FILM COATED 75 mg ORAL NDA 39 sections
Nucynta HUMAN PRESCRIPTION DRUG LABEL 1 24510-100 TABLET, FILM COATED 100 mg ORAL NDA 39 sections
NucyntaER HUMAN PRESCRIPTION DRUG LABEL 1 24510-116 TABLET, FILM COATED, EXTENDED RELEASE 100 mg ORAL NDA 39 sections
NucyntaER HUMAN PRESCRIPTION DRUG LABEL 1 24510-174 TABLET, FILM COATED, EXTENDED RELEASE 150 mg ORAL NDA 39 sections
NucyntaER HUMAN PRESCRIPTION DRUG LABEL 1 24510-232 TABLET, FILM COATED, EXTENDED RELEASE 200 mg ORAL NDA 39 sections
NucyntaER HUMAN PRESCRIPTION DRUG LABEL 1 24510-291 TABLET, FILM COATED, EXTENDED RELEASE 250 mg ORAL NDA 39 sections
Tapentadol Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 42806-626 TABLET, FILM COATED 50 mg ORAL ANDA 34 sections
Tapentadol Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 42806-627 TABLET, FILM COATED 75 mg ORAL ANDA 34 sections
Tapentadol Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 42806-628 TABLET, FILM COATED 100 mg ORAL ANDA 34 sections
Nucynta HUMAN PRESCRIPTION DRUG LABEL 1 54868-5979 TABLET, FILM COATED 50 mg ORAL NDA 33 sections
Nucynta HUMAN PRESCRIPTION DRUG LABEL 1 54868-6002 TABLET, FILM COATED 75 mg ORAL NDA 33 sections
Nucynta HUMAN PRESCRIPTION DRUG LABEL 1 54868-6039 TABLET, FILM COATED 100 mg ORAL NDA 33 sections
Nucynta HUMAN PRESCRIPTION DRUG LABEL 1 69865-210 TABLET, FILM COATED 50 mg ORAL NDA 37 sections
Nucynta HUMAN PRESCRIPTION DRUG LABEL 1 69865-220 TABLET, FILM COATED 75 mg ORAL NDA 37 sections
Nucynta HUMAN PRESCRIPTION DRUG LABEL 1 69865-230 TABLET, FILM COATED 100 mg ORAL NDA 37 sections
NucyntaER HUMAN PRESCRIPTION DRUG LABEL 1 69865-240 TABLET, FILM COATED, EXTENDED RELEASE 50 mg ORAL NDA 38 sections