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

Stem definitionDrug idCAS RN
dopamine receptor agonists, ergoline derivatives 2407 99755-59-6

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • rotigotine
  • neupro
  • leganto
  • (S)-(-)-Rotigotine
Rotigotine is a non-ergoline dopamine agonist. The precise mechanism of action of rotigotine as a treatment for Parkinson's disease is unknown, although it is thought to be related to its ability to stimulate dopamine receptors within the caudate-putamen in the brain. The precise mechanism of action of rotigotine as a treatment for Restless Legs Syndrome is unknown but is thought to be related to its ability to stimulate dopamine receptors.
  • Molecular weight: 315.48
  • Formula: C19H25NOS
  • CLOGP: 4.54
  • LIPINSKI: 0
  • HAC: 2
  • HDO: 1
  • TPSA: 23.47
  • ALOGS: -4.54
  • ROTB: 6
  • Status: OFP
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
6 mg TD

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 1 Benet LZ, Broccatelli F, Oprea TI
S (Water solubility) 5.60 mg/mL Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine) 0 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 0.36 µM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
Vd (Volume of distribution) 5.70 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 37 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) 4 hours Lombardo F, Berellini G, Obach RS

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
azlogd74 LogD at pH 7.4 3.921 Moderate 0.75
caco2-efflux Caco-2 efflux ratio (BA/AB) 0.785 Moderate 0.75
caco2-intrinsic-papp Caco-2 intrinsic apparent permeability 27.164 10^-6 cm/s Moderate 0.75
dh-clint Dog hepatocyte intrinsic clearance 70.632 uL/min/10^6 cells Moderate 0.75
dppb Dog plasma protein binding (% unbound) 2.040 % Moderate 0.75
fcs-ppb Fetal calf serum protein binding (% unbound) 4.110 % Moderate 0.75
herg hERG pIC50 5.717 pIC50 Moderate 0.75
hh-clint Human hepatocyte intrinsic clearance 53.211 uL/min/10^6 cells Moderate 0.75
hlm-clint Human liver microsomal intrinsic clearance 179.887 uL/min/mg protein Moderate 0.75
hppb Human plasma protein binding (% unbound) 1.590 % Moderate 0.75
kinase-safety-class ACVR2A,ACVR2B,AKT2,AKT3,AURKA,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK4,CDK5,CDK9,CHEK1,DDR1,DYRK1B,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,ITK,JAK2,JAK3,MAP2K6,MAP3K21,MAP3K7,MAPK10,MAPK12,MAPK7,MAPK9,MAPKAPK2,MET,MTOR,NTRK2,PDK1,PDK2,PDK4,PDPK1,PIK3CA,PIK3CB,PIM2,PRKCD,PRKDC,SIK2,SIK3,STK33,SYK,TEK,TGFBR1,TTK,ZAP70 52
kinase-selectivity-class AXL,BRAF,CDK4,CDK9,EIF2AK3,EPHB4,GRK2,MAP2K6,MAPK12,MTOR,PDK4,PRKCD,SIK2,STK33,TEK 15
mdck-mdr1-efflux MDCK-MDR1 efflux ratio 0.485 Moderate 0.75
mh-clint Mouse hepatocyte intrinsic clearance 198.153 Moderate 0.75
mppb Mouse plasma protein binding (% unbound) 3.870 Moderate 0.75
nih-mdck-mdr1-efflux NIH MDCK-MDR1 efflux ratio 1.219 Moderate 0.75
pfas-class PFAS structural alert (1 = True, 0 = False) 0
pppb Pig plasma protein binding (% unbound) 10.600 % Moderate 0.75
rh-clint Rat hepatocyte intrinsic clearance 264.241 uL/min/10^6 cells Moderate 0.75
rh-fuinc Rat hepatocyte fraction unbound in incubation 21.250 % Moderate 0.75
rppb Rat plasma protein binding (% unbound) 2.390 % Moderate 0.75
solubility-dd Solubility at pH 7.4 in DMSO 44.668 uM Moderate 0.75

Approvals:

DateAgencyCompanyOrphan
May 9, 2007 FDA UCB INC

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
Product adhesion issue 837.23 22.10 170 7943 4972 90615362
Dyskinesia 334.61 22.10 125 7988 36409 90583925
On and off phenomenon 263.78 22.10 58 8055 2485 90617849
Stoma site discharge 176.86 22.10 40 8073 1949 90618385
Application site pruritus 156.09 22.10 42 8071 4205 90616129
Stoma site pain 139.65 22.10 31 8082 1386 90618948
Stoma site erythema 137.97 22.10 31 8082 1465 90618869
Hallucination 134.75 22.10 80 8033 65879 90554455
Application site erythema 129.78 22.10 38 8075 5170 90615164
Freezing phenomenon 126.82 22.10 30 8083 1782 90618552
Fall 124.37 22.10 182 7931 481628 90138706
Device adhesion issue 108.05 22.10 35 8078 6656 90613678
Tremor 99.13 22.10 93 8020 153080 90467254
Dropped head syndrome 94.81 22.10 17 8096 248 90620086
Hallucination, visual 89.68 22.10 43 8070 23049 90597285
Muscle rigidity 88.80 22.10 37 8076 14272 90606062
Dysphagia 76.13 22.10 70 8043 112208 90508126
Application site reaction 75.45 22.10 17 8096 813 90619521
Dopamine dysregulation syndrome 73.61 22.10 13 8100 173 90620161
Stoma site extravasation 72.99 22.10 14 8099 300 90620034
Choking 70.93 22.10 30 8083 12003 90608331
Stoma site hypergranulation 69.16 22.10 14 8099 399 90619935
Stoma site infection 68.10 22.10 16 8097 922 90619412
Nocturia 65.26 22.10 27 8086 10228 90610106
Bradykinesia 61.21 22.10 23 8090 6765 90613569
Orthostatic intolerance 57.41 22.10 15 8098 1339 90618995
Therapeutic response shortened 55.33 22.10 31 8082 22848 90597486
Stoma site inflammation 55.13 22.10 13 8100 761 90619573
Loss of consciousness 54.61 22.10 65 8048 140173 90480161
Application site vesicles 51.05 22.10 14 8099 1503 90618831
Wrong technique in product usage process 49.22 22.10 45 8068 71526 90548808
Delusion 48.40 22.10 24 8089 13816 90606518
Sudden onset of sleep 47.88 22.10 11 8102 574 90619760
Decreased interest 47.39 22.10 17 8096 4390 90615944
Micturition urgency 46.91 22.10 22 8091 11211 90609123
Somnolence 45.25 22.10 73 8040 209011 90411323
Akinesia 44.71 22.10 13 8100 1723 90618611
Anosmia 43.34 22.10 20 8093 9828 90610506
Application site rash 43.24 22.10 14 8099 2655 90617679
Oromandibular dystonia 42.28 22.10 10 8103 593 90619741
Impulse-control disorder 42.22 22.10 11 8102 971 90619363
Dystonia 41.24 22.10 23 8090 16796 90603538
Deep brain stimulation 40.86 22.10 7 8106 77 90620257
Nightmare 40.82 22.10 25 8088 21700 90598634
Sleep talking 40.66 22.10 11 8102 1122 90619212
Compulsive shopping 39.86 22.10 10 8103 759 90619575
Drug dose titration not performed 39.82 22.10 10 8103 762 90619572
Gait disturbance 39.68 22.10 78 8035 260418 90359916
Pneumonia aspiration 38.90 22.10 31 8082 40909 90579425
Application site irritation 38.88 22.10 12 8101 1949 90618385
Product prescribing error 37.92 22.10 27 8086 30118 90590216
Depressed mood 37.33 22.10 33 8080 50189 90570145
Dermatitis contact 37.23 22.10 20 8093 13575 90606759
Device dislocation 36.87 22.10 27 8086 31455 90588879
Drooling 35.95 22.10 14 8099 4532 90615802
Middle insomnia 35.95 22.10 21 8092 16730 90603604
Device occlusion 35.16 22.10 17 8096 9265 90611069
Posture abnormal 35.06 22.10 12 8101 2699 90617635
Hyperkinesia 34.93 22.10 11 8102 1908 90618426
Device issue 33.84 22.10 25 8088 29512 90590822
Parkinsonism hyperpyrexia syndrome 33.47 22.10 7 8106 235 90620099
Antidiuretic hormone abnormality 32.03 22.10 5 8108 29 90620305
Gastrointestinal motility disorder 31.99 22.10 14 8099 6077 90614257
Speech disorder 31.99 22.10 29 8084 45556 90574778
Joint swelling 31.47 22.10 4 8109 503296 90117038
Balance disorder 31.36 22.10 41 8072 97039 90523295
Skin irritation 29.05 22.10 17 8096 13586 90606748
Ageusia 28.93 22.10 18 8095 16058 90604276
Application site discolouration 28.54 22.10 8 8105 930 90619404
Sexual dysfunction 28.38 22.10 12 8101 4792 90615542
Psychotic disorder 28.29 22.10 23 8090 31207 90589127
Anxiety 27.49 22.10 75 8038 309697 90310637
Disturbance in attention 27.38 22.10 27 8086 47082 90573252
Panic attack 27.28 22.10 21 8092 26344 90593990
Weight abnormal 26.86 22.10 9 8104 1898 90618436
Hallucination, auditory 26.53 22.10 17 8096 15958 90604376
Stoma site haemorrhage 25.74 22.10 8 8105 1330 90619004
Saliva altered 24.68 22.10 6 8107 400 90619934
Therapeutic product effect variable 24.63 22.10 8 8105 1531 90618803
Diarrhoea 24.40 22.10 29 8084 939161 89681173
Reduced facial expression 24.29 22.10 9 8104 2544 90617790
Application site dermatitis 24.20 22.10 5 8108 158 90620176
Altered state of consciousness 23.99 22.10 21 8092 31511 90588823
Constipation 23.01 22.10 66 8047 280329 90340005
Arthropathy 22.67 22.10 3 8110 366239 90254095
Panic disorder 22.55 22.10 9 8104 3106 90617228
Binge eating 22.30 22.10 6 8107 599 90619735

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
Product adhesion issue 544.72 22.20 115 9063 1624 42610533
On and off phenomenon 405.80 22.20 103 9075 3364 42608793
Hallucination 307.65 22.20 177 9001 57330 42554827
Dyskinesia 304.26 22.20 135 9043 25255 42586902
Freezing phenomenon 200.79 22.20 52 9126 1837 42610320
Impulse-control disorder 180.31 22.20 46 9132 1529 42610628
Stoma site discharge 168.44 22.20 43 9135 1433 42610724
Hallucination, visual 137.56 22.20 74 9104 20946 42591211
Bradykinesia 127.84 22.20 47 9131 5389 42606768
Stoma site erythema 123.02 22.20 31 9147 979 42611178
Muscle rigidity 121.82 22.20 57 9121 12002 42600155
Delusion 108.09 22.20 56 9122 14678 42597479
Application site reaction 104.73 22.20 23 9155 393 42611764
Device dislocation 101.30 22.20 44 9134 7787 42604370
Mobility decreased 99.96 22.20 73 9105 35233 42576924
Application site erythema 94.45 22.20 31 9147 2535 42609622
Hypersexuality 85.21 22.20 26 9152 1676 42610481
Application site pruritus 82.83 22.20 25 9153 1553 42610604
Dysphagia 79.86 22.20 88 9090 72631 42539526
Fall 78.01 22.20 162 9016 234358 42377799
Tremor 76.32 22.20 99 9079 96830 42515327
Stoma site pain 75.21 22.20 20 9158 783 42611374
Nocturia 74.64 22.20 41 9137 12071 42600086
Choking 73.74 22.20 33 9145 6265 42605892
Device issue 73.13 22.20 42 9136 13467 42598690
Akinesia 71.80 22.20 25 9153 2447 42609710
Stoma site inflammation 68.07 22.20 17 9161 517 42611640
Poor quality sleep 66.70 22.20 35 9143 9405 42602752
Memory impairment 64.36 22.20 66 9112 50156 42562001
Middle insomnia 63.91 22.20 32 9146 7801 42604356
Stoma site hypergranulation 63.42 22.20 14 9164 245 42611912
Dystonia 61.94 22.20 37 9141 12753 42599404
Stoma site reaction 60.43 22.20 14 9164 307 42611850
Hyperkinesia 60.10 22.20 21 9157 2077 42610080
Device occlusion 58.76 22.20 31 9147 8419 42603738
Balance disorder 58.14 22.20 61 9117 47584 42564573
Abnormal dreams 56.54 22.20 30 9148 8241 42603916
Sleep talking 55.57 22.20 15 9163 622 42611535
Gait disturbance 54.75 22.20 85 9093 97915 42514242
Device kink 53.99 22.20 14 9164 496 42611661
Anosmia 53.91 22.20 25 9153 5151 42607006
Cognitive disorder 51.36 22.20 49 9129 34123 42578034
Pneumonia aspiration 50.49 22.20 58 9120 50020 42562137
Speech disorder 50.04 22.20 45 9133 29076 42583081
Initial insomnia 50.01 22.20 22 9156 4008 42608149
Stoma site infection 49.59 22.20 15 9163 938 42611219
Application site rash 48.75 22.20 15 9163 994 42611163
Reduced facial expression 46.44 22.20 16 9162 1517 42610640
Gastrointestinal motility disorder 46.40 22.20 19 9159 2902 42609255
Posture abnormal 45.58 22.20 18 9160 2503 42609654
Application site vesicles 45.44 22.20 13 9165 669 42611488
Micturition urgency 43.97 22.20 29 9149 11869 42600288
Depressed mood 41.88 22.20 37 9141 23347 42588810
Libido increased 40.82 22.20 13 9165 965 42611192
Sexual dysfunction 39.18 22.20 22 9156 6753 42605404
Libido decreased 39.17 22.20 20 9158 5078 42607079
Dementia 37.63 22.20 30 9148 16450 42595707
Dropped head syndrome 36.92 22.20 9 9169 247 42611910
Gambling disorder 36.80 22.20 14 9164 1762 42610395
Restlessness 36.65 22.20 38 9140 29211 42582946
Anxiety 35.92 22.20 79 9099 118481 42493676
Toxicity to various agents 35.40 22.20 4 9174 229132 42383025
Stoma site haemorrhage 35.15 22.20 12 9166 1107 42611050
Device connection issue 34.67 22.20 10 9168 530 42611627
Psychomotor hyperactivity 34.05 22.20 24 9154 10934 42601223
Agitation 33.42 22.20 54 9124 64260 42547897
Drooling 33.42 22.20 17 9161 4282 42607875
Enteral nutrition 33.12 22.20 8 9170 211 42611946
Device breakage 33.02 22.20 16 9162 3633 42608524
Musculoskeletal stiffness 32.08 22.20 50 9128 57715 42554442
Stoma site induration 32.07 22.20 6 9172 43 42612114
Compulsive shopping 31.67 22.20 9 9169 452 42611705
Therapeutic response shortened 31.64 22.20 25 9153 13529 42598628
Application site irritation 31.56 22.20 10 9168 730 42611427
Stereotypy 30.29 22.20 10 9168 832 42611325
Unevaluable event 30.06 22.20 37 9141 34251 42577906
Gambling 28.28 22.20 7 9171 205 42611952
Fibroma 28.05 22.20 8 9170 407 42611750
Diarrhoea 27.99 22.20 35 9143 460814 42151343
Decreased interest 27.78 22.20 13 9165 2732 42609425
Device expulsion 27.74 22.20 6 9172 95 42612062
Tricuspid valve sclerosis 27.50 22.20 5 9173 30 42612127
Device adhesion issue 27.17 22.20 14 9164 3620 42608537
Stoma site odour 26.24 22.20 5 9173 40 42612117
Insomnia 25.35 22.20 69 9109 118184 42493973
Application site dermatitis 25.33 22.20 5 9173 49 42612108
Dermatitis allergic 25.02 22.20 18 9160 8465 42603692
Confusional state 24.90 22.20 86 9092 167511 42444646
Stoma site irritation 24.53 22.20 6 9172 167 42611990
Nightmare 23.57 22.20 28 9150 24984 42587173
Neuroleptic malignant syndrome 23.55 22.20 26 9152 21446 42590711
Parkinsonian crisis 23.34 22.20 4 9174 16 42612141
Neutropenia 23.32 22.20 7 9171 199424 42412733
Somnolence 23.26 22.20 75 9103 141030 42471127
Mucosal haemorrhage 22.95 22.20 10 9168 1780 42610377
Wrong technique in product usage process 22.41 22.20 36 9142 42599 42569558

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
On and off phenomenon 528.97 19.83 120 13440 4304 110571435
Dyskinesia 519.91 19.83 206 13354 51240 110524499
Product adhesion issue 449.86 19.83 98 13462 2908 110572831
Hallucination 352.61 19.83 194 13366 101238 110474501
Stoma site discharge 281.70 19.83 66 13494 2729 110573010
Freezing phenomenon 259.74 19.83 61 13499 2548 110573191
Hallucination, visual 189.68 19.83 94 13466 39511 110536228
Stoma site erythema 187.33 19.83 45 13515 2072 110573667
Impulse-control disorder 180.62 19.83 44 13516 2150 110573589
Stoma site pain 164.82 19.83 40 13520 1923 110573816
Muscle rigidity 161.24 19.83 72 13488 23959 110551780
Application site pruritus 148.26 19.83 43 13517 4117 110571622
Application site erythema 148.09 19.83 46 13514 5564 110570175
Bradykinesia 147.73 19.83 54 13506 10734 110565005
Fall 145.85 19.83 263 13297 603219 109972520
Choking 140.27 19.83 57 13503 15053 110560686
Dysphagia 138.50 19.83 129 13431 153471 110422268
Delusion 133.71 19.83 63 13497 23692 110552047
Nocturia 130.51 19.83 56 13504 16934 110558805
Tremor 129.36 19.83 141 13419 202091 110373648
Stoma site hypergranulation 120.64 19.83 25 13535 579 110575160
Dropped head syndrome 117.17 19.83 24 13536 524 110575215
Anosmia 105.41 19.83 44 13516 12428 110563311
Micturition urgency 104.93 19.83 50 13510 19270 110556469
Device dislocation 102.75 19.83 58 13502 31646 110544093
Stoma site infection 98.31 19.83 26 13534 1769 110573970
Dopamine dysregulation syndrome 96.90 19.83 21 13539 606 110575133
Akinesia 96.50 19.83 30 13530 3637 110572102
Sleep talking 92.10 19.83 23 13537 1245 110574494
Middle insomnia 90.30 19.83 46 13514 20456 110555283
Therapeutic response shortened 90.18 19.83 52 13508 29531 110546208
Decreased interest 87.91 19.83 30 13530 4878 110570861
Pneumonia aspiration 86.53 19.83 75 13485 81158 110494581
Stoma site inflammation 86.43 19.83 21 13539 1014 110574725
Sexual dysfunction 81.99 19.83 33 13527 8497 110567242
Gastrointestinal motility disorder 79.92 19.83 31 13529 7245 110568494
Device occlusion 78.52 19.83 38 13522 15147 110560592
Stoma site extravasation 77.23 19.83 16 13544 370 110575369
Application site reaction 74.91 19.83 18 13542 829 110574910
Device issue 72.85 19.83 48 13512 34487 110541252
Speech disorder 72.02 19.83 60 13500 61509 110514230
Dystonia 69.82 19.83 42 13518 25763 110549976
Compulsive shopping 69.37 19.83 17 13543 851 110574888
Hypersexuality 68.89 19.83 20 13540 1920 110573819
Sudden onset of sleep 67.56 19.83 16 13544 692 110575047
Depressed mood 66.49 19.83 57 13503 60752 110514987
Drooling 66.48 19.83 27 13533 7112 110568627
Reduced facial expression 64.15 19.83 22 13538 3629 110572110
Balance disorder 63.76 19.83 75 13485 116485 110459254
Gait disturbance 62.81 19.83 118 13442 278090 110297649
Ageusia 61.12 19.83 35 13525 19610 110556129
Somnolence 60.85 19.83 121 13439 297328 110278411
Libido decreased 60.65 19.83 24 13536 5911 110569828
Posture abnormal 59.95 19.83 22 13538 4416 110571323
Initial insomnia 59.83 19.83 28 13532 10361 110565378
Loss of consciousness 59.68 19.83 95 13465 196211 110379528
Application site vesicles 59.44 19.83 17 13543 1547 110574192
Hyperkinesia 55.22 19.83 19 13541 3165 110572574
Poor quality sleep 54.35 19.83 37 13523 28040 110547699
Parkinsonism hyperpyrexia syndrome 53.97 19.83 13 13547 605 110575134
Disturbance in attention 53.75 19.83 51 13509 61944 110513795
Nightmare 52.06 19.83 41 13519 38822 110536917
Application site rash 51.92 19.83 17 13543 2433 110573306
Drug dose titration not performed 51.59 19.83 14 13546 1051 110574688
Device kink 50.72 19.83 16 13544 2033 110573706
Orthostatic intolerance 50.03 19.83 16 13544 2125 110573614
Dementia 48.09 19.83 36 13524 31637 110544102
Constipation 46.88 19.83 122 13438 357664 110218075
Abnormal dreams 45.83 19.83 25 13535 12755 110562984
Neuroleptic malignant syndrome 45.76 19.83 36 13524 34023 110541716
Anxiety 44.52 19.83 117 13443 344961 110230778
Agitation 43.33 19.83 61 13499 112990 110462749
Joint swelling 42.71 19.83 3 13557 442842 110132897
Stoma site reaction 41.75 19.83 10 13550 454 110575285
Dermatitis contact 41.12 19.83 24 13536 13929 110561810
Toxicity to various agents 39.32 19.83 6 13554 480549 110095190
Restlessness 39.02 19.83 41 13519 56218 110519521
Panic disorder 38.91 19.83 15 13545 3446 110572293
Panic attack 37.61 19.83 30 13530 28910 110546829
Diarrhoea 36.61 19.83 52 13508 1139453 109436286
Stoma site haemorrhage 36.56 19.83 13 13547 2385 110573354
Mobility decreased 36.39 19.83 86 13474 237336 110338403
Persecutory delusion 36.36 19.83 17 13543 6274 110569465
Stoma site odour 35.61 19.83 7 13553 123 110575616
Infusion related reaction 35.57 19.83 3 13557 381159 110194580
Gambling disorder 33.87 19.83 12 13548 2179 110573560
Insomnia 33.72 19.83 109 13451 360481 110215258
Application site dermatitis 33.30 19.83 7 13553 174 110575565
Wrong technique in product usage process 33.27 19.83 47 13513 87301 110488438
Cognitive disorder 33.20 19.83 47 13513 87464 110488275
Memory impairment 33.11 19.83 74 13486 196870 110378869
Oromandibular dystonia 32.19 19.83 10 13550 1209 110574530
Device connection issue 31.75 19.83 10 13550 1264 110574475
Application site irritation 31.43 19.83 11 13549 1926 110573813
Tricuspid valve sclerosis 30.31 19.83 5 13555 30 110575709
Weight abnormal 29.96 19.83 11 13549 2210 110573529
Bezoar 29.93 19.83 13 13547 4041 110571698
Sensory disturbance 29.14 19.83 21 13539 17408 110558331
Sexually inappropriate behaviour 28.70 19.83 8 13552 663 110575076
Libido increased 28.53 19.83 11 13549 2528 110573211
Stoma site pruritus 28.36 19.83 4 13556 6 110575733
Febrile neutropenia 28.21 19.83 3 13557 316764 110258975
Stress 27.97 19.83 48 13512 105300 110470439
Arthralgia 26.59 19.83 34 13526 779598 109796141
Psychotic disorder 26.55 19.83 32 13528 50905 110524834
Camptocormia 26.40 19.83 7 13553 481 110575258
Psychomotor hyperactivity 26.31 19.83 21 13539 20256 110555483
Device breakage 26.30 19.83 18 13542 13751 110561988
Sleep attacks 26.16 19.83 6 13554 225 110575514
Antidiuretic hormone abnormality 26.00 19.83 5 13555 78 110575661
Disorientation 25.40 19.83 37 13523 70634 110505105
Drug titration error 25.38 19.83 9 13551 1638 110574101
Application site discolouration 25.17 19.83 8 13552 1041 110574698
Hypokinesia 24.95 19.83 21 13539 21805 110553934
Arthropathy 24.90 19.83 3 13557 287519 110288220
Product prescribing error 24.74 19.83 31 13529 51300 110524439
Binge eating 24.63 19.83 7 13553 623 110575116
Rapid eye movement sleep behaviour disorder 24.53 19.83 7 13553 632 110575107
Confusional state 24.50 19.83 118 13442 468562 110107177
Movement disorder 24.30 19.83 26 13534 36378 110539361
Device use issue 24.29 19.83 11 13549 3773 110571966
Delirium 24.12 19.83 52 13508 134973 110440766
Enteral nutrition 23.62 19.83 6 13554 348 110575391
Altered state of consciousness 23.42 19.83 32 13528 57594 110518145
Hallucination, auditory 23.41 19.83 22 13538 26375 110549364
Mucosal haemorrhage 23.33 19.83 10 13550 3010 110572729
Stoma site irritation 23.28 19.83 6 13554 369 110575370
Stomatitis 22.96 19.83 3 13557 270239 110305500
Fracture 22.64 19.83 21 13539 24767 110550972
Polycythaemia 22.56 19.83 10 13550 3265 110572474
Device adhesion issue 22.24 19.83 14 13546 9296 110566443
Withdrawal syndrome 21.99 19.83 23 13537 31357 110544382
Device alarm issue 21.92 19.83 9 13551 2437 110573302
Cough 21.75 19.83 15 13545 461626 110114113
Stoma site induration 21.48 19.83 4 13556 52 110575687
Intentional medical device removal by patient 21.47 19.83 6 13554 502 110575237
Device colour issue 21.34 19.83 4 13556 54 110575685
Stereotypy 21.32 19.83 7 13553 1010 110574729
Unevaluable event 21.27 19.83 31 13529 59196 110516543
Abnormal behaviour 21.13 19.83 25 13535 39014 110536725
Drug hypersensitivity 21.07 19.83 15 13545 454075 110121664
Motor dysfunction 21.00 19.83 20 13540 24386 110551353
Parkinsonian gait 20.96 19.83 7 13553 1065 110574674
Drug intolerance 20.81 19.83 12 13548 406500 110169239
Asthma 20.74 19.83 3 13557 250288 110325451
Product administered at inappropriate site 20.59 19.83 11 13549 5382 110570357
Headache 20.51 19.83 49 13511 882328 109693411

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC N04BC09 NERVOUS SYSTEM
ANTI-PARKINSON DRUGS
DOPAMINERGIC AGENTS
Dopamine agonists
FDA MoA N0000000117 Dopamine Agonists
MeSH PA D015259 Dopamine Agents
MeSH PA D018377 Neurotransmitter Agents
MeSH PA D018491 Dopamine Agonists
FDA EPC N0000175768 Nonergot Dopamine Agonist
CHEBI has role CHEBI:48407 antiparkinson drug

Related Drugs by ATC class:

N04BC Dopamine agonists 8 drugs
apomorphinebromocriptinecabergolinedihydroergocryptinepergolidepiribedilpramipexoleropinirole

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

DiseaseRelationSNOMED_IDDOID
Restless legs indication 32914008 DOID:0050425
Parkinson's disease indication 49049000 DOID:14330
Dyskinesia contraindication 9748009
Orthostatic hypotension contraindication 28651003
Hypertensive disorder contraindication 38341003 DOID:10763
Body fluid retention contraindication 43498006
Chronic heart failure contraindication 48447003
Acute nephropathy contraindication 58574008
Magnetic resonance imaging contraindication 113091000
Syncope contraindication 271594007
Drowsy contraindication 271782001
Peripheral edema contraindication 271809000
Breastfeeding (mother) contraindication 413712001




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 10.6 acidic
pKa2 8.87 Basic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
1MG/24HR NEUPRO UCB INC N021829 April 2, 2012 RX FILM, EXTENDED RELEASE TRANSDERMAL 8246979 Sept. 1, 2027 TREATMENT OF RESTLESS LEGS SYNDROME BY APPLICATION OF CLAIMED TRANSDERMAL DELIVERY SYSTEM
1MG/24HR NEUPRO UCB INC N021829 April 2, 2012 RX FILM, EXTENDED RELEASE TRANSDERMAL 8246979 Sept. 1, 2027 TREATMENT OF SIGNS AND SYMPTOMS OF PARKINSONS DISEASE BY APPLICATION OF CLAIMED TRANSDERMAL SYSTEM
2MG/24HR NEUPRO UCB INC N021829 May 9, 2007 RX FILM, EXTENDED RELEASE TRANSDERMAL 8246979 Sept. 1, 2027 TREATMENT OF RESTLESS LEGS SYNDROME BY APPLICATION OF CLAIMED TRANSDERMAL DELIVERY SYSTEM
2MG/24HR NEUPRO UCB INC N021829 May 9, 2007 RX FILM, EXTENDED RELEASE TRANSDERMAL 8246979 Sept. 1, 2027 TREATMENT OF SIGNS AND SYMPTOMS OF PARKINSONS DISEASE BY APPLICATION OF CLAIMED TRANSDERMAL SYSTEM
3MG/24HR NEUPRO UCB INC N021829 April 2, 2012 RX FILM, EXTENDED RELEASE TRANSDERMAL 8246979 Sept. 1, 2027 TREATMENT OF RESTLESS LEGS SYNDROME BY APPLICATION OF CLAIMED TRANSDERMAL DELIVERY SYSTEM
3MG/24HR NEUPRO UCB INC N021829 April 2, 2012 RX FILM, EXTENDED RELEASE TRANSDERMAL 8246979 Sept. 1, 2027 TREATMENT OF SIGNS AND SYMPTOMS OF PARKINSONS DISEASE BY APPLICATION OF CLAIMED TRANSDERMAL SYSTEM
4MG/24HR NEUPRO UCB INC N021829 May 9, 2007 RX FILM, EXTENDED RELEASE TRANSDERMAL 8246979 Sept. 1, 2027 TREATMENT OF RESTLESS LEGS SYNDROME BY APPLICATION OF CLAIMED TRANSDERMAL DELIVERY SYSTEM
4MG/24HR NEUPRO UCB INC N021829 May 9, 2007 RX FILM, EXTENDED RELEASE TRANSDERMAL 8246979 Sept. 1, 2027 TREATMENT OF SIGNS AND SYMPTOMS OF PARKINSONS DISEASE BY APPLICATION OF CLAIMED TRANSDERMAL SYSTEM
6MG/24HR NEUPRO UCB INC N021829 May 9, 2007 RX FILM, EXTENDED RELEASE TRANSDERMAL 8246979 Sept. 1, 2027 TREATMENT OF RESTLESS LEGS SYNDROME BY APPLICATION OF CLAIMED TRANSDERMAL DELIVERY SYSTEM
6MG/24HR NEUPRO UCB INC N021829 May 9, 2007 RX FILM, EXTENDED RELEASE TRANSDERMAL 8246979 Sept. 1, 2027 TREATMENT OF SIGNS AND SYMPTOMS OF PARKINSONS DISEASE BY APPLICATION OF CLAIMED TRANSDERMAL SYSTEM
8MG/24HR NEUPRO UCB INC N021829 April 2, 2012 RX FILM, EXTENDED RELEASE TRANSDERMAL 8246979 Sept. 1, 2027 TREATMENT OF RESTLESS LEGS SYNDROME BY APPLICATION OF CLAIMED TRANSDERMAL DELIVERY SYSTEM
8MG/24HR NEUPRO UCB INC N021829 April 2, 2012 RX FILM, EXTENDED RELEASE TRANSDERMAL 8246979 Sept. 1, 2027 TREATMENT OF SIGNS AND SYMPTOMS OF PARKINSONS DISEASE BY APPLICATION OF CLAIMED TRANSDERMAL SYSTEM

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
D(2) dopamine receptor GPCR AGONIST Ki 10.22 IUPHAR IUPHAR
D(3) dopamine receptor GPCR AGONIST Ki 8.40 IUPHAR
D(1A) dopamine receptor GPCR AGONIST Ki 5.60 IUPHAR
D(4) dopamine receptor GPCR AGONIST Ki 7.26 CHEMBL
D(1B) dopamine receptor GPCR AGONIST Ki 6 IUPHAR
D(1A) dopamine receptor GPCR Ki 6.30 CHEMBL
D(2) dopamine receptor GPCR Ki 7.82 CHEMBL

External reference:

IDSource
4025266 VUID
N0000171794 NUI
D05768 KEGG_DRUG
4025266 VANDF
C1700683 UMLSCUI
CHEBI:135351 CHEBI
R5F PDB_CHEM_ID
CHEMBL1303 ChEMBL_ID
DB05271 DRUGBANK_ID
C047508 MESH_SUPPLEMENTAL_RECORD_UI
59227 PUBCHEM_CID
941 IUPHAR_LIGAND_ID
7897 INN_ID
87T4T8BO2E UNII
616739 RXNORM
21751 MMSL
83818 MMSL
d05848 MMSL
011270 NDDF
421915002 SNOMEDCT_US
421924006 SNOMEDCT_US
87T4T8BO2E INXIGHT DRUGS

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Neupro HUMAN PRESCRIPTION DRUG LABEL 1 50474-801 PATCH, EXTENDED RELEASE 1 mg TRANSDERMAL NDA 32 sections
Neupro HUMAN PRESCRIPTION DRUG LABEL 1 50474-802 PATCH, EXTENDED RELEASE 2 mg TRANSDERMAL NDA 32 sections
Neupro HUMAN PRESCRIPTION DRUG LABEL 1 50474-803 PATCH, EXTENDED RELEASE 3 mg TRANSDERMAL NDA 32 sections
Neupro HUMAN PRESCRIPTION DRUG LABEL 1 50474-804 PATCH, EXTENDED RELEASE 4 mg TRANSDERMAL NDA 32 sections
Neupro HUMAN PRESCRIPTION DRUG LABEL 1 50474-805 PATCH, EXTENDED RELEASE 6 mg TRANSDERMAL NDA 32 sections
Neupro HUMAN PRESCRIPTION DRUG LABEL 1 50474-806 PATCH, EXTENDED RELEASE 8 mg TRANSDERMAL NDA 32 sections