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

Stem definitionDrug idCAS RN
local anaesthetics 723 50-36-2

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • cocaine
  • cocain
  • benzoylmethylecgonine
  • cocaine hydrochloride
  • cocaine HCl
An alkaloid ester extracted from the leaves of plants including coca. It is a local anesthetic and vasoconstrictor and is clinically used for that purpose, particularly in the eye, ear, nose, and throat. It also has powerful central nervous system effects similar to the amphetamines and is a drug of abuse. Cocaine, like amphetamines, acts by multiple mechanisms on brain catecholaminergic neurons; the mechanism of its reinforcing effects is thought to involve inhibition of dopamine uptake.
  • Molecular weight: 303.36
  • Formula: C17H21NO4
  • CLOGP: 2.57
  • LIPINSKI: 0
  • HAC: 5
  • HDO: 0
  • TPSA: 55.84
  • ALOGS: -1.78
  • ROTB: 5
  • 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
S (Water solubility) 1.60 mg/mL Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine) 1 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 4.95 µM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability) 57 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution) 2 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 32 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.12 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 0.76 hours Lombardo F, Berellini G, Obach RS

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
kinase-selectivity-class AXL,EIF2AK3,GRK2 3
kinase-safety-class ACVR2A,ACVR2B,AKT2,AURKA,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK4,CDK5,CDK9,CHEK1,DDR1,DYRK1B,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,ITK,JAK2,JAK3,MAP3K21,MAP3K7,MAPK10,MAPK7,MAPKAPK2,MET,NTRK2,PDK2,PDK4,PDPK1,PIK3CB,PIM2,PRKDC,SIK2,SIK3,STK33,SYK,TEK,TGFBR1,TTK,ZAP70 44
pfas-class PFAS structural alert (1 = True, 0 = False) 0

Approvals:

DateAgencyCompanyOrphan
Jan. 1, 1860 YEAR INTRODUCED

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
Drug abuse 5145.81 72.43 1305 9667 81042 90536433
Toxicity to various agents 2072.95 72.43 893 10079 286953 90330522
Substance use disorder 1902.41 72.43 309 10663 1711 90615764
Drug use disorder 1276.96 72.43 276 10696 8067 90609408
Completed suicide 1016.14 72.43 444 10528 144614 90472861
Cardio-respiratory arrest 834.77 72.43 306 10666 62834 90554641
Respiratory arrest 710.47 72.43 231 10741 33080 90584395
Cardiac arrest 580.26 72.43 273 10699 104662 90512813
Drug dependence 473.16 72.43 165 10807 29162 90588313
Substance abuse 460.02 72.43 111 10861 5295 90612180
Miosis 449.05 72.43 122 10850 9362 90608113
Death 428.50 72.43 388 10584 456163 90161312
Poisoning 421.68 72.43 129 10843 15088 90602387
Coma 398.01 72.43 188 10784 72444 90545031
Intentional product misuse 377.86 72.43 194 10778 89410 90528065
Poisoning deliberate 325.54 72.43 108 10864 16378 90601097
Mydriasis 271.23 72.43 92 10880 14920 90602555
Chemical submission 211.12 72.43 39 10933 491 90616984
Agitation 209.13 72.43 119 10853 66979 90550496
Bradypnoea 197.61 72.43 55 10917 4603 90612872
Suicide attempt 193.67 72.43 118 10854 75281 90542194
Altered state of consciousness 186.00 72.43 86 10886 31446 90586029
Overdose 179.07 72.43 150 10822 157559 90459916
Asphyxia 170.54 72.43 54 10918 7049 90610426
Suicidal ideation 136.42 72.43 94 10878 73761 90543714
Withdrawal syndrome 134.57 72.43 62 10910 22462 90595013
Victim of crime 134.00 72.43 29 10943 843 90616632
Substance abuser 128.24 72.43 22 10950 175 90617300
Somnolence 121.94 72.43 138 10834 208946 90408529
Substance use 119.52 72.43 28 10944 1171 90616304
Opiates positive 110.87 72.43 21 10951 305 90617170
Drug ineffective 108.24 72.43 19 10953 1384279 89233196
Incorrect route of product administration 106.80 72.43 70 10902 50556 90566919
Victim of sexual abuse 106.16 72.43 23 10949 672 90616803
Depressed level of consciousness 103.31 72.43 79 10893 72705 90544770
Pain 100.32 72.43 5 10967 996336 89621139
Tachycardia 95.15 72.43 106 10866 157567 90459908
Fatigue 89.74 72.43 16 10956 1154007 89463468
Unresponsive to stimuli 88.51 72.43 56 10916 38065 90579410
Diarrhoea 87.71 72.43 7 10965 939183 89678292
Prescription drug used without a prescription 83.35 72.43 26 10946 3229 90614246
Accidental overdose 79.63 72.43 47 10925 28226 90589249
Victim of chemical submission 77.58 72.43 18 10954 721 90616754
Intentional overdose 76.21 72.43 74 10898 93760 90523715
Respiratory depression 75.08 72.43 37 10935 15538 90601937

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
Drug abuse 10936.55 47.49 3512 21975 101259 42494589
Substance use disorder 3286.60 47.49 737 24750 4608 42591240
Toxicity to various agents 2986.33 47.49 1784 23703 227352 42368496
Drug use disorder 2564.94 47.49 687 24800 9646 42586202
Coma 1438.14 47.49 680 24807 52874 42542974
Miosis 1324.69 47.49 438 25049 13008 42582840
Drug dependence 1114.02 47.49 474 25013 28620 42567228
Intentional product misuse 973.72 47.49 549 24938 61351 42534497
Poisoning 862.71 47.49 326 25161 14373 42581475
Substance abuse 804.60 47.49 272 25215 8633 42587215
Cardio-respiratory arrest 680.95 47.49 428 25059 58208 42537640
Respiratory arrest 594.25 47.49 305 25182 28119 42567729
Asphyxia 585.36 47.49 211 25276 8115 42587733
Mydriasis 497.99 47.49 190 25297 8580 42587268
Altered state of consciousness 476.63 47.49 266 25221 28993 42566855
Completed suicide 426.81 47.49 396 25091 96069 42499779
Bradypnoea 419.61 47.49 140 25347 4253 42591595
Agitation 402.28 47.49 322 25165 63992 42531856
Overdose 388.20 47.49 391 25096 104873 42490975
Cardiac arrest 354.39 47.49 379 25108 108941 42486907
Poisoning deliberate 325.00 47.49 146 25341 9988 42585860
Somnolence 294.79 47.49 391 25096 140714 42455134
Drug ineffective 292.02 47.49 23 25464 630174 41965674
Substance use 276.76 47.49 82 25405 1669 42594179
Aggression 252.49 47.49 210 25277 43953 42551895
Diarrhoea 215.37 47.49 16 25471 460833 42135015
Fatigue 206.78 47.49 14 25473 435627 42160221
Off label use 196.63 47.49 69 25418 638266 41957582
Tachycardia 195.40 47.49 270 25217 100817 42495031
Drug detoxification 186.50 47.49 44 25443 349 42595499
Death 180.37 47.49 653 24834 470532 42125316
Respiratory depression 179.97 47.49 122 25365 18746 42577102
Depressed level of consciousness 177.88 47.49 179 25308 47791 42548057
Pyrexia 172.27 47.49 18 25469 394024 42201824
Pneumonia 161.67 47.49 29 25458 422120 42173728
Prescription drug used without a prescription 161.57 47.49 61 25426 2669 42593179
Withdrawal syndrome 161.44 47.49 104 25383 14671 42581177
Rash 147.24 47.49 4 25483 276950 42318898
Anaemia 129.90 47.49 10 25477 280268 42315580
Alcohol abuse 128.70 47.49 58 25429 3991 42591857
Incorrect route of product administration 127.35 47.49 110 25377 24195 42571653
Pulmonary oedema 127.19 47.49 158 25329 53114 42542734
Adulterated product 121.60 47.49 36 25451 730 42595118
Accidental death 120.22 47.49 51 25436 3032 42592816
Nausea 118.20 47.49 45 25442 396754 42199094
Rhabdomyolysis 115.51 47.49 184 25303 77835 42518013
Behaviour disorder 114.34 47.49 64 25423 6990 42588858
Substance abuser 110.52 47.49 27 25460 252 42595596
Suicidal ideation 110.42 47.49 140 25347 48021 42547827
Arthralgia 108.88 47.49 3 25484 205235 42390613
Asthenia 101.62 47.49 22 25465 280771 42315077
High risk sexual behaviour 101.13 47.49 21 25466 84 42595764
Postmortem blood drug level abnormal 97.21 47.49 26 25461 358 42595490
Dizziness 95.49 47.49 17 25470 249237 42346611
Dyspnoea 92.07 47.49 78 25409 442543 42153305
Condition aggravated 80.17 47.49 28 25459 260726 42335122
Sepsis 79.88 47.49 12 25475 199322 42396526
Thrombocytopenia 79.68 47.49 10 25477 190269 42405579
Pruritus 78.85 47.49 10 25477 188761 42407087
Pain 77.52 47.49 25 25462 244823 42351025
Opiates positive 75.16 47.49 23 25464 524 42595324
Drug withdrawal maintenance therapy 74.07 47.49 18 25469 164 42595684
Toxicologic test abnormal 72.87 47.49 22 25465 478 42595370
Decreased appetite 72.15 47.49 14 25473 193123 42402725
Substance-induced psychotic disorder 72.05 47.49 35 25452 2854 42592994
Weight decreased 71.78 47.49 18 25469 207930 42387918
Atrial fibrillation 70.62 47.49 3 25484 139590 42456258
Pneumonia aspiration 68.48 47.49 114 25373 49964 42545884
Suicide attempt 67.17 47.49 108 25379 45992 42549856
Toxic leukoencephalopathy 64.77 47.49 22 25465 705 42595143
Visceral congestion 62.91 47.49 23 25464 918 42594930
Oedema peripheral 62.54 47.49 5 25482 136071 42459777
Amphetamines positive 62.00 47.49 16 25471 190 42595658
Suicidal behaviour 58.37 47.49 25 25462 1521 42594327
Drug withdrawal syndrome 58.05 47.49 68 25419 21481 42574367
Cluster headache 58.01 47.49 19 25468 543 42595305
Constipation 56.08 47.49 14 25473 162277 42433571
Drug screen positive 55.03 47.49 33 25454 4098 42591750
Intentional overdose 54.76 47.49 105 25382 51351 42544497
Drug abuser 54.41 47.49 31 25456 3500 42592348
Disorientation 54.03 47.49 86 25401 36303 42559545
COVID-19 54.01 47.49 4 25483 115944 42479904
Behavioural addiction 53.35 47.49 12 25475 75 42595773
Dependence 52.82 47.49 23 25464 1457 42594391
Unresponsive to stimuli 51.92 47.49 78 25409 31325 42564523
Infection 51.82 47.49 4 25483 112064 42483784
Back pain 51.42 47.49 11 25476 141765 42454083
White blood cell count decreased 50.88 47.49 4 25483 110392 42485456
Renal impairment 50.78 47.49 4 25483 110224 42485624
Hypothermia 50.59 47.49 49 25438 12466 42583382
Pain in extremity 50.11 47.49 14 25473 150590 42445258
General physical health deterioration 48.61 47.49 15 25472 151231 42444617
Syncope 47.55 47.49 3 25484 99403 42496445

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
Drug abuse 16361.12 50.73 4683 30664 172728 110381224
Substance use disorder 5335.10 50.73 1042 34305 6248 110547704
Toxicity to various agents 4932.18 50.73 2578 32769 477977 110075975
Drug use disorder 3962.18 50.73 959 34388 17115 110536837
Miosis 1894.43 50.73 558 34789 21425 110532527
Coma 1861.64 50.73 855 34492 117014 110436938
Drug dependence 1614.14 50.73 605 34742 49415 110504537
Cardio-respiratory arrest 1469.37 50.73 723 34624 115113 110438839
Intentional product misuse 1418.31 50.73 738 34609 132166 110421786
Poisoning 1354.45 50.73 462 34885 28643 110525309
Respiratory arrest 1263.38 50.73 529 34818 57770 110496182
Completed suicide 1238.30 50.73 836 34511 241545 110312407
Substance abuse 1168.59 50.73 338 35009 12125 110541827
Cardiac arrest 912.52 50.73 640 34707 196113 110357839
Mydriasis 783.65 50.73 287 35060 21870 110532082
Asphyxia 765.38 50.73 252 35095 13963 110539989
Altered state of consciousness 709.45 50.73 353 34994 57273 110496679
Death 708.23 50.73 985 34362 697884 109856068
Agitation 683.23 50.73 434 34913 112617 110441335
Bradypnoea 646.77 50.73 197 35150 8452 110545500
Poisoning deliberate 613.88 50.73 252 35095 26079 110527873
Overdose 518.15 50.73 495 34852 233299 110320653
Somnolence 459.52 50.73 519 34828 296930 110257022
Substance use 412.81 50.73 106 35241 2400 110551552
Aggression 371.54 50.73 233 35114 58977 110494975
Drug ineffective 346.45 50.73 41 35306 1520499 109033453
Tachycardia 308.71 50.73 371 34976 226274 110327678
Fatigue 302.53 50.73 23 35324 1215935 109338017
Depressed level of consciousness 301.46 50.73 265 35082 112013 110441939
Withdrawal syndrome 290.72 50.73 159 35188 31221 110522731
Respiratory depression 290.55 50.73 160 35187 31841 110522111
Diarrhoea 287.86 50.73 20 35327 1139485 109414467
Drug detoxification 274.70 50.73 58 35289 530 110553422
Suicidal ideation 268.89 50.73 230 35117 93707 110460245
Suicide attempt 244.01 50.73 227 35120 103167 110450785
Prescription drug used without a prescription 242.72 50.73 84 35263 5412 110548540
Rash 238.54 50.73 5 35342 820959 109732993
Substance abuser 234.05 50.73 49 35298 428 110553524
Off label use 220.11 50.73 103 35244 1500082 109053870
Incorrect route of product administration 214.86 50.73 172 35175 63889 110490063
Pain 206.71 50.73 30 35317 954925 109599027
Rhabdomyolysis 206.01 50.73 222 35125 120179 110433773
Nausea 201.89 50.73 72 35275 1235618 109318334
Arthralgia 195.67 50.73 14 35333 779618 109774334
Pyrexia 192.57 50.73 29 35318 898236 109655716
Chemical submission 180.56 50.73 41 35306 539 110553413
Alcohol abuse 178.42 50.73 65 35282 4864 110549088
Opiates positive 175.79 50.73 44 35303 895 110553057
Pulmonary oedema 171.11 50.73 185 35162 100474 110453478
Accidental death 159.07 50.73 60 35287 4949 110549003
Victim of crime 158.89 50.73 44 35303 1339 110552613
Dyspnoea 154.43 50.73 81 35266 1106791 109447161
Pneumonia aspiration 153.54 50.73 158 35189 81075 110472877
Pneumonia 150.08 50.73 47 35300 876667 109677285
Adulterated product 143.13 50.73 39 35308 1116 110552836
Behaviour disorder 142.41 50.73 67 35280 9580 110544372
Pruritus 138.72 50.73 13 35334 581547 109972405
Amphetamines positive 136.47 50.73 29 35318 274 110553678
Postmortem blood drug level abnormal 134.97 50.73 33 35314 607 110553345
Anaemia 133.82 50.73 11 35336 547075 110006877
Condition aggravated 133.81 50.73 35 35312 734801 109819151
Dizziness 131.49 50.73 31 35316 698162 109855790
Drug withdrawal syndrome 125.06 50.73 101 35246 37953 110515999
Toxicologic test abnormal 124.87 50.73 36 35311 1271 110552681
Intentional overdose 121.63 50.73 179 35168 132322 110421630
Unresponsive to stimuli 120.40 50.73 124 35223 63666 110490286
Weight increased 119.97 50.73 3 35344 419641 110134311
Asthenia 119.50 50.73 36 35311 688963 109864989
Cough 116.51 50.73 8 35339 461633 110092319
Toxic leukoencephalopathy 113.07 50.73 35 35312 1582 110552370
High risk sexual behaviour 112.90 50.73 21 35326 91 110553861
Abdominal discomfort 111.89 50.73 3 35344 393855 110160097
Hypersensitivity 111.45 50.73 4 35343 403994 110149958
Drug intolerance 105.70 50.73 6 35341 406506 110147446
Drug screen positive 102.32 50.73 47 35300 6363 110547589
Pain in extremity 99.13 50.73 18 35329 487100 110066852
Peripheral swelling 99.10 50.73 8 35339 404026 110149926
Decreased appetite 95.93 50.73 18 35329 475828 110078124
Headache 94.44 50.73 86 35261 882291 109671661
Visceral congestion 93.58 50.73 29 35318 1316 110552636
Hypothermia 93.25 50.73 73 35274 26229 110527723
Infection 92.18 50.73 6 35341 362194 110191758
Drug withdrawal maintenance therapy 87.16 50.73 18 35329 146 110553806
Postmortem blood drug level 85.62 50.73 20 35327 300 110553652
Drug interaction 82.28 50.73 347 35000 499836 110054116
Accidental overdose 80.66 50.73 91 35256 51743 110502209
Oedema peripheral 79.22 50.73 7 35340 328653 110225299
Suspected suicide 78.54 50.73 53 35294 15146 110538806
Substance-induced psychotic disorder 78.00 50.73 37 35310 5387 110548565
Hypoaesthesia 77.65 50.73 6 35341 314217 110239735
Electrocardiogram QT prolonged 77.51 50.73 131 35216 108829 110445123
Alcohol poisoning 76.11 50.73 43 35304 8977 110544975
Dehydration 73.02 50.73 4 35343 279507 110274445
Sinusitis 72.38 50.73 6 35341 296682 110257270
Drug abuser 72.02 50.73 35 35312 5374 110548578
Urticaria 71.20 50.73 9 35338 318848 110235104
Hyperthermia 68.91 50.73 56 35291 21216 110532736
Thrombocytopenia 68.60 50.73 14 35333 348871 110205081
Haemoglobin decreased 66.75 50.73 3 35344 248724 110305228
Multiple injuries 65.64 50.73 29 35318 3585 110550367
Musculoskeletal stiffness 64.70 50.73 7 35340 279815 110274137
Sepsis 64.64 50.73 13 35334 327333 110226619
Sinus tachycardia 63.98 50.73 75 35272 44418 110509534
Constipation 63.21 50.73 18 35329 357768 110196184
Dependence 63.15 50.73 26 35321 2703 110551249
Blood ethanol 62.46 50.73 13 35334 110 110553842
Hallucination, visual 62.42 50.73 70 35277 39535 110514417
Respiratory acidosis 61.56 50.73 44 35303 13782 110540170
Weight decreased 61.09 50.73 37 35310 468020 110085932
Atrial fibrillation 60.88 50.73 3 35344 229639 110324313
General physical health deterioration 60.76 50.73 30 35317 425265 110128687
Muscular weakness 60.67 50.73 5 35342 248463 110305489
Synovitis 60.55 50.73 8 35339 274084 110279868
Brain death 60.00 50.73 33 35314 6540 110547412
Wheezing 60 50.73 6 35341 255224 110298728
Back pain 59.65 50.73 22 35325 370974 110182978
Brain oedema 57.84 50.73 60 35287 31038 110522914
White blood cell count decreased 57.75 50.73 4 35343 229386 110324566
Victim of chemical submission 57.17 50.73 18 35329 861 110553091
COVID-19 56.99 50.73 6 35341 245054 110308898
Drug diversion 56.73 50.73 20 35327 1360 110552592
Asthma 56.02 50.73 7 35340 250284 110303668
Blood pressure increased 55.99 50.73 8 35339 258365 110295587
Cluster headache 55.43 50.73 19 35328 1188 110552764
Pericarditis 54.65 50.73 4 35343 219110 110334842
Disorientation 54.32 50.73 88 35259 70583 110483369
Wound 53.85 50.73 6 35341 234431 110319521
Suicidal behaviour 53.82 50.73 25 35322 3472 110550480
Discomfort 53.32 50.73 4 35343 214703 110339249
Hepatic enzyme increased 51.63 50.73 19 35328 320873 110233079
Hyponatraemia 51.46 50.73 5 35342 217648 110336304
Abdominal pain 51.28 50.73 53 35294 512936 110041016
Loss of consciousness 50.79 50.73 158 35189 196148 110357804

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC N01BC01 NERVOUS SYSTEM
ANESTHETICS
ANESTHETICS, LOCAL
Esters of benzoic acid
ATC R02AD03 RESPIRATORY SYSTEM
THROAT PREPARATIONS
THROAT PREPARATIONS
Anesthetics, local
ATC S01HA01 SENSORY ORGANS
OPHTHALMOLOGICALS
LOCAL ANESTHETICS
Local anesthetics
ATC S02DA02 SENSORY ORGANS
OTOLOGICALS
OTHER OTOLOGICALS
Analgesics and anesthetics
MeSH PA D000777 Anesthetics
MeSH PA D000779 Anesthetics, Local
MeSH PA D002317 Cardiovascular Agents
MeSH PA D002492 Central Nervous System Depressants
MeSH PA D014179 Neurotransmitter Uptake Inhibitors
MeSH PA D014662 Vasoconstrictor Agents
MeSH PA D015259 Dopamine Agents
MeSH PA D018377 Neurotransmitter Agents
MeSH PA D018689 Sensory System Agents
MeSH PA D018765 Dopamine Uptake Inhibitors
MeSH PA D049990 Membrane Transport Modulators
CHEBI has role CHEBI:35337 central nervous system stimulant
CHEBI has role CHEBI:35524 sympathomimetic agent
CHEBI has role CHEBI:35640 adrenergic uptake inhibitor
CHEBI has role CHEBI:35703 xenobiotic
CHEBI has role CHEBI:36333 local anaesthetic
CHEBI has role CHEBI:38633 sodium channel blocker
CHEBI has role CHEBI:50514 vasoconstrictor agent
CHEBI has role CHEBI:50949 serotonin uptake inhibitor
CHEBI has role CHEBI:51039 dopamine uptake inhibitor
CHEBI has role CHEBI:75771 mouse metabolite
CHEBI has role CHEBI:76924 plant metabolite
CHEBI has role CHEBI:78298 environmental contaminant

Related Drugs by ATC class:

R02AD Anesthetics, local 4 drugs
ambroxolbenzocainedycloninelidocaine
S01HA Local anesthetics 7 drugs
chloroprocainecinchocainelidocaineoxybuprocaineprocaineproparacainetetracaine
S02DA Analgesics and anesthetics 3 drugs
cinchocainelidocainephenazone

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

DiseaseRelationSNOMED_IDDOID
Local anesthesia indication 386761002
Conduction disorder of the heart contraindication 44808001
Epilepsy contraindication 84757009 DOID:1826
Thyrotoxicosis contraindication 90739004 DOID:7997
Disorder of mucous membrane contraindication 95351003
Acute disease of cardiovascular system contraindication 128487001
Breastfeeding (mother) contraindication 413712001
Hypertensive urgency contraindication 443482000




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 8.27 Basic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
4% NUMBRINO OMNIVIUM PHARMS N209575 Jan. 10, 2020 RX SOLUTION NASAL 10016407 Feb. 7, 2037 METHOD OF ADMINISTERING A LOCAL ANESTHETIC PRIOR TO PERFORMING A DIAGNOSTIC OR SURGICAL PROCEDURE ON A SUBJECT WITH HEPATIC OR RENAL IMPAIRMENT
4% NUMBRINO OMNIVIUM PHARMS N209575 Jan. 10, 2020 RX SOLUTION NASAL 10016407 Feb. 7, 2037 METHOD OF ADMINISTERING A LOCAL ANESTHETIC TO THE MUCOUS MEMBRANES IN PATIENTS WITH HEPATIC IMPAIRMENT
4% NUMBRINO OMNIVIUM PHARMS N209575 Jan. 10, 2020 RX SOLUTION NASAL 10016407 Feb. 7, 2037 METHOD OF ADMINISTERING A LOCAL ANESTHETIC TO THE MUCOUS MEMBRANES IN PATIENTS WITH RENAL IMPAIRMENT
4% NUMBRINO OMNIVIUM PHARMS N209575 Jan. 10, 2020 RX SOLUTION NASAL 10149843 Feb. 7, 2037 METHOD FOR THE INDUCTION OF LOCAL ANESTHESIA PRIOR TO PERFORMING A PROCEDURE ON, THROUGH, OR ADJACENT TO THE MUCOUS MEMBRANES
4% NUMBRINO OMNIVIUM PHARMS N209575 Jan. 10, 2020 RX SOLUTION NASAL 10149843 Feb. 7, 2037 METHOD OF ADMINISTERING A LOCAL ANESTHETIC TO THE MUCOUS MEMBRANES
4% NUMBRINO OMNIVIUM PHARMS N209575 Jan. 10, 2020 RX SOLUTION NASAL 10413505 Feb. 7, 2037 METHOD FOR THE INDUCTION OF LOCAL ANESTHESIA OF THE MUCOUS MEMBRANES
4% NUMBRINO OMNIVIUM PHARMS N209575 Jan. 10, 2020 RX SOLUTION NASAL 10420760 Feb. 7, 2037 METHOD FOR THE INDUCTION OF LOCAL ANESTHESIA PRIOR TO PERFORMING A PROCEDURE ON, THROUGH, OR ADJACENT TO THE MUCOUS MEMBRANES
4% NUMBRINO OMNIVIUM PHARMS N209575 Jan. 10, 2020 RX SOLUTION NASAL 10857095 Feb. 7, 2037 METHOD FOR THE INDUCTION OF LOCAL ANESTHESIA OF THE MUCOUS MEMBRANES
4% NUMBRINO OMNIVIUM PHARMS N209575 Jan. 10, 2020 RX SOLUTION NASAL 10894012 Feb. 7, 2037 METHOD FOR THE INDUCTION OF LOCAL ANESTHESIA OF THE MUCOUS MEMBRANES
4% NUMBRINO OMNIVIUM PHARMS N209575 Jan. 10, 2020 RX SOLUTION NASAL 10933060 Feb. 7, 2037 METHOD FOR THE INDUCTION OF LOCAL ANESTHESIA OF THE MUCOUS MEMBRANES
4% NUMBRINO OMNIVIUM PHARMS N209575 Jan. 10, 2020 RX SOLUTION NASAL 10933060 Feb. 7, 2037 METHOD FOR THE INDUCTION OF LOCAL ANESTHESIA PRIOR TO PERFORMING A PROCEDURE ON, THROUGH, OR ADJACENT TO THE MUCOUS MEMBRANES
4% NUMBRINO OMNIVIUM PHARMS N209575 Jan. 10, 2020 RX SOLUTION NASAL 10973811 Feb. 7, 2037 A METHOD FOR TREATING A SUBJECT WITH UVEAL MELANOMA WITH UNRESECTABLE HEPATIC METASTASES
4% NUMBRINO OMNIVIUM PHARMS N209575 Jan. 10, 2020 RX SOLUTION NASAL 9867815 Feb. 7, 2037 METHOD OF ADMINISTERING A LOCAL ANESTHETIC PRIOR TO PERFORMING A DIAGNOSTIC OR SURGICAL PROCEDURE ON A SUBJECT WITH HEPATIC OR RENAL IMPAIRMENT
4% NUMBRINO OMNIVIUM PHARMS N209575 Jan. 10, 2020 RX SOLUTION NASAL 9867815 Feb. 7, 2037 METHOD OF ADMINISTERING A LOCAL ANESTHETIC TO THE MUCOUS MEMBRANES IN GERIATRIC PATIENTS
4% NUMBRINO OMNIVIUM PHARMS N209575 Jan. 10, 2020 RX SOLUTION NASAL 9867815 Feb. 7, 2037 METHOD OF ADMINISTERING A LOCAL ANESTHETIC TO THE MUCOUS MEMBRANES IN PATIENTS WITH HEPATIC IMPAIRMENT
4% NUMBRINO OMNIVIUM PHARMS N209575 Jan. 10, 2020 RX SOLUTION NASAL 9867815 Feb. 7, 2037 METHOD OF ADMINISTERING A LOCAL ANESTHETIC TO THE MUCOUS MEMBRANES IN PATIENTS WITH RENAL IMPAIRMENT
4% GOPRELTO LXO IRELAND N209963 Dec. 14, 2017 RX SOLUTION NASAL 10016407 Feb. 7, 2037 METHOD OF ADMINISTERING A LOCAL ANESTHETIC PRIOR TO PERFORMING A DIAGNOSTIC OR SURGICAL PROCEDURE ON A SUBJECT WITH HEPATIC OR RENAL IMPAIRMENT
4% GOPRELTO LXO IRELAND N209963 Dec. 14, 2017 RX SOLUTION NASAL 10149843 Feb. 7, 2037 METHOD FOR THE INDUCTION OF LOCAL ANESTHESIA PRIOR TO PERFORMING A PROCEDURE ON, THROUGH, OR ADJACENT TO THE MUCOUS MEMBRANES
4% GOPRELTO LXO IRELAND N209963 Dec. 14, 2017 RX SOLUTION NASAL 10149843 Feb. 7, 2037 METHOD OF ADMINISTERING A LOCAL ANESTHETIC TO THE MUCOUS MEMBRANES
4% GOPRELTO LXO IRELAND N209963 Dec. 14, 2017 RX SOLUTION NASAL 10413505 Feb. 7, 2037 METHOD OF ADMINISTERING A LOCAL ANESTHETIC TO THE MUCOUS MEMBRANES
4% GOPRELTO LXO IRELAND N209963 Dec. 14, 2017 RX SOLUTION NASAL 10420760 Feb. 7, 2037 METHOD FOR THE INDUCTION OF LOCAL ANESTHESIA PRIOR TO PERFORMING A PROCEDURE ON, THROUGH, OR ADJACENT TO THE MUCOUS MEMBRANES
4% GOPRELTO LXO IRELAND N209963 Dec. 14, 2017 RX SOLUTION NASAL 10857095 Feb. 7, 2037 METHOD FOR THE INDUCTION OF LOCAL ANESTHESIA OF THE MUCOUS MEMBRANES
4% GOPRELTO LXO IRELAND N209963 Dec. 14, 2017 RX SOLUTION NASAL 10894012 Feb. 7, 2037 METHOD FOR THE INDUCTION OF LOCAL ANESTHESIA OF THE MUCOUS MEMBRANES
4% GOPRELTO LXO IRELAND N209963 Dec. 14, 2017 RX SOLUTION NASAL 10933060 Feb. 7, 2037 METHOD FOR THE INDUCTION OF LOCAL ANESTHESIA OF THE MUCOUS MEMBRANES
4% GOPRELTO LXO IRELAND N209963 Dec. 14, 2017 RX SOLUTION NASAL 10973811 Feb. 7, 2037 METHOD OF ADMINISTERING A LOCAL ANESTHETIC TO THE MUCOUS MEMBRANES IN PATIENTS WITH RENAL IMPAIRMENT
4% GOPRELTO LXO IRELAND N209963 Dec. 14, 2017 RX SOLUTION NASAL 10987347 Feb. 7, 2037 METHOD OF ADMINISTERING A LOCAL ANESTHETIC TO THE MUCOUS MEMBRANES IN PATIENTS WITH HEPATIC IMPAIRMENT
4% GOPRELTO LXO IRELAND N209963 Dec. 14, 2017 RX SOLUTION NASAL 9867815 Feb. 7, 2037 METHOD OF ADMINISTERING A LOCAL ANESTHETIC TO THE MUCOUS MEMBRANES IN GERIATRIC PATIENTS
4% GOPRELTO LXO IRELAND N209963 Dec. 14, 2017 RX SOLUTION NASAL 9867815 Feb. 7, 2037 METHOD OF ADMINISTERING A LOCAL ANESTHETIC TO THE MUCOUS MEMBRANES IN PATIENTS WITH HEPATIC IMPAIRMENT
4% GOPRELTO LXO IRELAND N209963 Dec. 14, 2017 RX SOLUTION NASAL 9867815 Feb. 7, 2037 METHOD OF ADMINISTERING A LOCAL ANESTHETIC TO THE MUCOUS MEMBRANES IN PATIENTS WITH RENAL IMPAIRMENT

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
Sodium-dependent dopamine transporter Transporter INHIBITOR Ki 7.50 CHEMBL IUPHAR
Sodium channel protein type 5 subunit alpha Ion channel WOMBAT-PK
Sigma non-opioid intracellular receptor 1 Membrane receptor Ki 5.05 CHEMBL
Potassium voltage-gated channel subfamily H member 2 Ion channel IC50 5.14 WOMBAT-PK
Sodium-dependent serotonin transporter Transporter Ki 6.92 WOMBAT-PK
Sodium-dependent noradrenaline transporter Transporter Ki 5.57 WOMBAT-PK
Alpha-1A adrenergic receptor GPCR Ki 5.68 WOMBAT-PK
Histamine H1 receptor GPCR Ki 5.67 WOMBAT-PK
5-hydroxytryptamine receptor 1B GPCR Ki 5.47 WOMBAT-PK
5-hydroxytryptamine receptor 3A Ion channel Ki 5.71 WOMBAT-PK
Sodium- and chloride-dependent GABA transporter 1 Transporter IC50 5.50 WOMBAT-PK
Sodium channel protein type 11 subunit alpha Ion channel WOMBAT-PK
Kappa-type opioid receptor GPCR IC50 5.10 WOMBAT-PK
Cocaine- and amphetamine-regulated transcript protein Transcription factor WOMBAT-PK
Serotonin 3 receptor (5HT3) Ion channel ANTAGONIST Ki 4.80 IUPHAR
Sodium channel alpha subunits; brain (Types I, II, III) Ion channel IC50 4.31 CHEMBL
Dopamine transporter Transporter IC50 7.19 CHEMBL
Muscarinic acetylcholine receptor M1 GPCR Ki 4.21 CHEMBL
Sodium-dependent serotonin transporter Transporter Ki 7.35 CHEMBL
Sodium-dependent dopamine transporter Transporter Ki 7.49 CHEMBL
Transporter Transporter Ki 6.97 CHEMBL
Sodium-dependent dopamine transporter Transporter IC50 6.70 CHEMBL
Transporter Transporter Ki 5.50 CHEMBL
Dopamine transporter Transporter IC50 7.02 CHEMBL

External reference:

IDSource
4019690 VUID
N0000147782 NUI
D00110 KEGG_DRUG
53-21-4 SECONDARY_CAS_RN
2653 RXNORM
C0009170 UMLSCUI
CHEBI:27958 CHEBI
CCA PDB_CHEM_ID
CHEMBL370805 ChEMBL_ID
DB00907 DRUGBANK_ID
CHEMBL529437 ChEMBL_ID
D003042 MESH_DESCRIPTOR_UI
446220 PUBCHEM_CID
2286 IUPHAR_LIGAND_ID
I5Y540LHVR UNII
437 MMSL
4488 MMSL
d03878 MMSL
001369 NDDF
001370 NDDF
14816004 SNOMEDCT_US
387085005 SNOMEDCT_US
74273006 SNOMEDCT_US
4017521 VANDF
4019690 VANDF

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Goprelto HUMAN PRESCRIPTION DRUG LABEL 1 70839-359 SOLUTION 40 mg NASAL NDA 19 sections
COCAINE HYDROCHLORIDE HUMAN PRESCRIPTION DRUG LABEL 1 70839-362 SOLUTION 40 mg NASAL NDA authorized generic 19 sections
NUMBRINO HUMAN PRESCRIPTION DRUG LABEL 1 81665-300 SOLUTION 40 mg TOPICAL NDA 30 sections
cocaine hydrochloride nasal HUMAN PRESCRIPTION DRUG LABEL 1 81665-301 SOLUTION 40 mg TOPICAL NDA authorized generic 30 sections