Stem definition | Drug id | CAS RN |
---|---|---|
local anaesthetics | 723 | 50-36-2 |
None
Property | Value | Reference |
---|---|---|
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 ยตM/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 |
Date | Agency | Company | Orphan |
---|---|---|---|
Jan. 1, 1860 | YEAR INTRODUCED |
MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
---|---|---|---|---|---|---|
Drug abuse | 3772.94 | 80.52 | 947 | 5245 | 71571 | 63411259 |
Toxicity to various agents | 1709.94 | 80.52 | 697 | 5495 | 246553 | 63236277 |
Completed suicide | 854.13 | 80.52 | 368 | 5824 | 145305 | 63337525 |
Cardio-respiratory arrest | 692 | 80.52 | 248 | 5944 | 59711 | 63423119 |
Respiratory arrest | 621.90 | 80.52 | 197 | 5995 | 32448 | 63450382 |
Cardiac arrest | 508.20 | 80.52 | 224 | 5968 | 92321 | 63390509 |
Death | 354.86 | 80.52 | 291 | 5901 | 374090 | 63108740 |
Intentional product misuse | 275.22 | 80.52 | 129 | 6063 | 60788 | 63422042 |
Substance abuse | 256.38 | 80.52 | 65 | 6127 | 4742 | 63478088 |
Poisoning deliberate | 222.58 | 80.52 | 70 | 6122 | 11148 | 63471682 |
Drug dependence | 221.59 | 80.52 | 85 | 6107 | 24398 | 63458432 |
Miosis | 189.00 | 80.52 | 56 | 6136 | 7297 | 63475533 |
Poisoning | 154.77 | 80.52 | 56 | 6136 | 13644 | 63469186 |
Overdose | 146.24 | 80.52 | 107 | 6085 | 114971 | 63367859 |
Coma | 100.60 | 80.52 | 68 | 6124 | 64296 | 63418534 |
Bradypnoea | 95.41 | 80.52 | 28 | 6164 | 3522 | 63479308 |
Opiates positive | 93.12 | 80.52 | 18 | 6174 | 368 | 63482462 |
Suicide attempt | 89.60 | 80.52 | 62 | 6130 | 60856 | 63421974 |
Accidental overdose | 88.78 | 80.52 | 44 | 6148 | 23265 | 63459565 |
Asphyxia | 87.89 | 80.52 | 30 | 6162 | 6151 | 63476679 |
Incorrect route of product administration | 84.81 | 80.52 | 45 | 6147 | 27407 | 63455423 |
Mydriasis | 81.93 | 80.52 | 34 | 6158 | 11922 | 63470908 |
MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
---|---|---|---|---|---|---|
Drug abuse | 8289.54 | 50.96 | 2572 | 12211 | 96524 | 34845624 |
Toxicity to various agents | 2439.91 | 50.96 | 1319 | 13464 | 199043 | 34743105 |
Intentional product misuse | 767.38 | 50.96 | 377 | 14406 | 45234 | 34896914 |
Drug dependence | 726.31 | 50.96 | 300 | 14483 | 23917 | 34918231 |
Coma | 575.43 | 50.96 | 311 | 14472 | 45367 | 34896781 |
Cardio-respiratory arrest | 556.94 | 50.96 | 325 | 14458 | 54948 | 34887200 |
Poisoning | 475.93 | 50.96 | 183 | 14600 | 12043 | 34930105 |
Respiratory arrest | 468.41 | 50.96 | 231 | 14552 | 27812 | 34914336 |
Miosis | 441.19 | 50.96 | 162 | 14621 | 9373 | 34932775 |
Substance abuse | 433.48 | 50.96 | 151 | 14632 | 7490 | 34934658 |
Asphyxia | 391.26 | 50.96 | 136 | 14647 | 6699 | 34935449 |
Completed suicide | 361.30 | 50.96 | 312 | 14471 | 97856 | 34844292 |
Cardiac arrest | 287.41 | 50.96 | 272 | 14511 | 95887 | 34846261 |
Overdose | 248.31 | 50.96 | 245 | 14538 | 90814 | 34851334 |
Substance use disorder | 226.91 | 50.96 | 55 | 14728 | 724 | 34941424 |
Agitation | 217.93 | 50.96 | 186 | 14597 | 57213 | 34884935 |
Mydriasis | 194.20 | 50.96 | 83 | 14700 | 7154 | 34934994 |
Drug use disorder | 189.26 | 50.96 | 70 | 14713 | 4121 | 34938027 |
Poisoning deliberate | 174.97 | 50.96 | 79 | 14704 | 7765 | 34934383 |
Depressed level of consciousness | 150.70 | 50.96 | 133 | 14650 | 42708 | 34899440 |
Bradypnoea | 149.21 | 50.96 | 53 | 14730 | 2776 | 34939372 |
Drug ineffective | 148.93 | 50.96 | 12 | 14771 | 456739 | 34485409 |
Diarrhoea | 143.28 | 50.96 | 5 | 14778 | 389907 | 34552241 |
Pulmonary oedema | 135.08 | 50.96 | 131 | 14652 | 47398 | 34894750 |
Death | 131.74 | 50.96 | 417 | 14366 | 397632 | 34544516 |
Altered state of consciousness | 116.12 | 50.96 | 88 | 14695 | 22805 | 34919343 |
Incorrect route of product administration | 114.99 | 50.96 | 74 | 14709 | 14771 | 34927377 |
Alcohol abuse | 113.42 | 50.96 | 50 | 14733 | 4640 | 34937508 |
Fatigue | 112.08 | 50.96 | 13 | 14770 | 370640 | 34571508 |
Withdrawal syndrome | 111.35 | 50.96 | 68 | 14715 | 12387 | 34929761 |
Pneumonia | 108.94 | 50.96 | 13 | 14770 | 362614 | 34579534 |
Respiratory depression | 108.92 | 50.96 | 74 | 14709 | 16171 | 34925977 |
Postmortem blood drug level abnormal | 107.15 | 50.96 | 25 | 14758 | 276 | 34941872 |
Aggression | 95.23 | 50.96 | 99 | 14684 | 38865 | 34903283 |
Pyrexia | 92.78 | 50.96 | 15 | 14768 | 332998 | 34609150 |
Asthenia | 90.43 | 50.96 | 3 | 14780 | 245248 | 34696900 |
Drug detoxification | 88.25 | 50.96 | 21 | 14762 | 254 | 34941894 |
Nausea | 84.82 | 50.96 | 20 | 14763 | 339888 | 34602260 |
Rhabdomyolysis | 81.69 | 50.96 | 121 | 14662 | 68042 | 34874106 |
Prescription drug used without a prescription | 79.29 | 50.96 | 31 | 14752 | 2123 | 34940025 |
Toxicologic test abnormal | 78.10 | 50.96 | 22 | 14761 | 534 | 34941614 |
Rash | 77.84 | 50.96 | 4 | 14779 | 222748 | 34719400 |
Opiates positive | 77.15 | 50.96 | 22 | 14761 | 559 | 34941589 |
Dyspnoea | 68.82 | 50.96 | 37 | 14746 | 376745 | 34565403 |
Dizziness | 67.60 | 50.96 | 7 | 14776 | 218514 | 34723634 |
Suicidal behaviour | 67.55 | 50.96 | 25 | 14758 | 1472 | 34940676 |
Anaemia | 66.05 | 50.96 | 10 | 14773 | 233325 | 34708823 |
Cluster headache | 64.36 | 50.96 | 19 | 14764 | 547 | 34941601 |
Somnolence | 62.33 | 50.96 | 142 | 14641 | 110974 | 34831174 |
Amphetamines positive | 61.28 | 50.96 | 15 | 14768 | 206 | 34941942 |
Off label use | 60.91 | 50.96 | 53 | 14730 | 419471 | 34522677 |
Mixed anxiety and depressive disorder | 60.40 | 50.96 | 13 | 14770 | 96 | 34942052 |
Tachycardia | 57.47 | 50.96 | 117 | 14666 | 84655 | 34857493 |
Drug abuser | 55.44 | 50.96 | 29 | 14754 | 3925 | 34938223 |
Intentional overdose | 54.41 | 50.96 | 79 | 14704 | 43595 | 34898553 |
Weight decreased | 53.60 | 50.96 | 6 | 14777 | 176295 | 34765853 |
Intentional product use issue | 53.53 | 50.96 | 93 | 14690 | 59723 | 34882425 |
MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
---|---|---|---|---|---|---|
Drug abuse | 12023.23 | 55.11 | 3411 | 16620 | 159280 | 79565077 |
Toxicity to various agents | 3843.69 | 55.11 | 1923 | 18108 | 419617 | 79304740 |
Cardio-respiratory arrest | 1176.25 | 55.11 | 563 | 19468 | 107947 | 79616410 |
Intentional product misuse | 1052.95 | 55.11 | 501 | 19530 | 94664 | 79629693 |
Respiratory arrest | 1020.42 | 55.11 | 422 | 19609 | 57128 | 79667229 |
Completed suicide | 1008.34 | 55.11 | 674 | 19357 | 245093 | 79479264 |
Drug dependence | 913.40 | 55.11 | 354 | 19677 | 40415 | 79683942 |
Cardiac arrest | 733.27 | 55.11 | 484 | 19547 | 171612 | 79552745 |
Poisoning | 650.47 | 55.11 | 243 | 19788 | 25029 | 79699328 |
Miosis | 644.55 | 55.11 | 214 | 19817 | 15575 | 79708782 |
Coma | 637.66 | 55.11 | 365 | 19666 | 100284 | 79624073 |
Substance abuse | 553.68 | 55.11 | 173 | 19858 | 10353 | 79714004 |
Death | 500.17 | 55.11 | 659 | 19372 | 565855 | 79158502 |
Asphyxia | 458.92 | 55.11 | 154 | 19877 | 11566 | 79712791 |
Poisoning deliberate | 366.87 | 55.11 | 148 | 19883 | 18680 | 79705677 |
Overdose | 345.03 | 55.11 | 319 | 19712 | 183887 | 79540470 |
Substance use disorder | 289.42 | 55.11 | 63 | 19968 | 875 | 79723482 |
Agitation | 284.03 | 55.11 | 220 | 19811 | 99495 | 79624862 |
Mydriasis | 280.61 | 55.11 | 120 | 19911 | 17523 | 79706834 |
Bradypnoea | 238.73 | 55.11 | 80 | 19951 | 5972 | 79718385 |
Drug use disorder | 236.36 | 55.11 | 87 | 19944 | 8564 | 79715793 |
Depressed level of consciousness | 213.58 | 55.11 | 184 | 19847 | 96468 | 79627889 |
Altered state of consciousness | 204.80 | 55.11 | 131 | 19900 | 43691 | 79680666 |
Drug ineffective | 198.35 | 55.11 | 21 | 20010 | 1080892 | 78643465 |
Diarrhoea | 191.15 | 55.11 | 7 | 20024 | 880482 | 78843875 |
Fatigue | 175.84 | 55.11 | 16 | 20015 | 929711 | 78794646 |
Incorrect route of product administration | 174.66 | 55.11 | 109 | 19922 | 34820 | 79689537 |
Respiratory depression | 163.33 | 55.11 | 96 | 19935 | 27534 | 79696823 |
Opiates positive | 162.95 | 55.11 | 40 | 19991 | 964 | 79723393 |
Pulmonary oedema | 147.98 | 55.11 | 144 | 19887 | 88110 | 79636247 |
Alcohol abuse | 146.73 | 55.11 | 54 | 19977 | 5309 | 79719048 |
Withdrawal syndrome | 144.94 | 55.11 | 88 | 19943 | 26766 | 79697591 |
Postmortem blood drug level abnormal | 136.89 | 55.11 | 32 | 19999 | 622 | 79723735 |
Nausea | 133.37 | 55.11 | 38 | 19993 | 957158 | 78767199 |
Suicide attempt | 131.01 | 55.11 | 131 | 19900 | 82801 | 79641556 |
Aggression | 126.88 | 55.11 | 104 | 19927 | 50854 | 79673503 |
Drug detoxification | 123.95 | 55.11 | 27 | 20004 | 376 | 79723981 |
Rash | 123.93 | 55.11 | 5 | 20026 | 578353 | 79146004 |
Dyspnoea | 123.12 | 55.11 | 32 | 19999 | 856993 | 78867364 |
Pain | 123 | 55.11 | 16 | 20015 | 703786 | 79020571 |
Toxicologic test abnormal | 122.78 | 55.11 | 34 | 19997 | 1326 | 79723031 |
Amphetamines positive | 122.63 | 55.11 | 26 | 20005 | 316 | 79724041 |
Rhabdomyolysis | 119.07 | 55.11 | 138 | 19893 | 102993 | 79621364 |
Intentional overdose | 117.69 | 55.11 | 139 | 19892 | 105821 | 79618536 |
Asthenia | 104.52 | 55.11 | 6 | 20025 | 511683 | 79212674 |
Prescription drug used without a prescription | 103.94 | 55.11 | 39 | 19992 | 4046 | 79720311 |
Accidental overdose | 103.21 | 55.11 | 83 | 19948 | 39498 | 79684859 |
Pneumonia | 99.93 | 55.11 | 22 | 20009 | 660224 | 79064133 |
Pyrexia | 98.02 | 55.11 | 25 | 20006 | 678684 | 79045673 |
Somnolence | 94.05 | 55.11 | 194 | 19837 | 238787 | 79485570 |
Dizziness | 89.44 | 55.11 | 13 | 20018 | 526428 | 79197929 |
Cough | 79.06 | 55.11 | 3 | 20028 | 366786 | 79357571 |
Anaemia | 75.53 | 55.11 | 11 | 20020 | 445004 | 79279353 |
Suicidal ideation | 74.74 | 55.11 | 94 | 19937 | 76246 | 79648111 |
Postmortem blood drug level | 72.69 | 55.11 | 17 | 20014 | 331 | 79724026 |
Tachycardia | 70.69 | 55.11 | 145 | 19886 | 177623 | 79546734 |
Condition aggravated | 69.37 | 55.11 | 20 | 20011 | 501104 | 79223253 |
Off label use | 69.01 | 55.11 | 76 | 19955 | 907139 | 78817218 |
Drug abuser | 67.24 | 55.11 | 32 | 19999 | 5981 | 79718376 |
Pruritus | 66.39 | 55.11 | 10 | 20021 | 394638 | 79329719 |
Headache | 65.33 | 55.11 | 42 | 19989 | 653730 | 79070627 |
Cluster headache | 63.53 | 55.11 | 19 | 20012 | 977 | 79723380 |
Hypothermia | 62.06 | 55.11 | 49 | 19982 | 22697 | 79701660 |
Unresponsive to stimuli | 61.58 | 55.11 | 73 | 19958 | 55715 | 79668642 |
Suicidal behaviour | 61.40 | 55.11 | 25 | 20006 | 3222 | 79721135 |
Accidental death | 61.06 | 55.11 | 27 | 20004 | 4264 | 79720093 |
Weight decreased | 57.49 | 55.11 | 10 | 20021 | 355188 | 79369169 |
Decreased appetite | 56.85 | 55.11 | 9 | 20022 | 342409 | 79381948 |
MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
---|---|---|---|---|---|---|
Sudden infant death syndrome | 17.98 | 15.80 | 3 | 3 | 53 | 89733 |
Source | Code | Description |
---|---|---|
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 | D002491 | Central Nervous System Agents |
MeSH PA | D002492 | Central Nervous System Depressants |
MeSH PA | D015259 | Dopamine Agents |
MeSH PA | D018765 | Dopamine Uptake Inhibitors |
MeSH PA | D049990 | Membrane Transport Modulators |
MeSH PA | D018377 | Neurotransmitter Agents |
MeSH PA | D014179 | Neurotransmitter Uptake Inhibitors |
MeSH PA | D018373 | Peripheral Nervous System Agents |
MeSH PA | D018689 | Sensory System Agents |
MeSH PA | D014662 | Vasoconstrictor Agents |
CHEBI has role | CHEBI:35337 | analeptic |
CHEBI has role | CHEBI:35524 | sympathomimetic |
CHEBI has role | CHEBI:35640 | adrenergic uptake inhibitors |
CHEBI has role | CHEBI:35703 | Xenobiotic |
CHEBI has role | CHEBI:36333 | local anesthetics |
CHEBI has role | CHEBI:38633 | sodium channel blockers |
CHEBI has role | CHEBI:50949 | SSRI |
CHEBI has role | CHEBI:51039 | dopamine reuptake inhibitor |
CHEBI has role | CHEBI:75771 | Mus musculus metabolites |
CHEBI has role | CHEBI:76924 | plant metabolites |
CHEBI has role | CHEBI:78298 | environmental contaminants |
CHEBI has role | CHEBI:77746 | Homo sapiens metabolite |
Disease | Relation | SNOMED_ID | DOID |
---|---|---|---|
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 |
None
None
Dissociation level | Dissociation constant | Type (acidic/basic) |
---|---|---|
pKa1 | 8.27 | Basic |
Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Patent number | Patent expiration date | Patent use |
---|---|---|---|---|---|---|---|---|---|---|
4% | GOPRELTO | GENUS LIFESCIENCES | 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 | GENUS LIFESCIENCES | 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 | GENUS LIFESCIENCES | N209963 | Dec. 14, 2017 | RX | SOLUTION | NASAL | 10149843 | Feb. 7, 2037 | METHOD OF ADMINISTERING A LOCAL ANESTHETIC TO THE MUCOUS MEMBRANES |
4% | GOPRELTO | GENUS LIFESCIENCES | N209963 | Dec. 14, 2017 | RX | SOLUTION | NASAL | 10413505 | Feb. 7, 2037 | METHOD OF ADMINISTERING A LOCAL ANESTHETIC TO THE MUCOUS MEMBRANES |
4% | GOPRELTO | GENUS LIFESCIENCES | 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 | GENUS LIFESCIENCES | N209963 | Dec. 14, 2017 | RX | SOLUTION | NASAL | 10857095 | Feb. 7, 2037 | METHOD FOR THE INDUCTION OF LOCAL ANESTHESIA OF THE MUCOUS MEMBRANES |
4% | GOPRELTO | GENUS LIFESCIENCES | N209963 | Dec. 14, 2017 | RX | SOLUTION | NASAL | 10894012 | Feb. 7, 2037 | METHOD FOR THE INDUCTION OF LOCAL ANESTHESIA OF THE MUCOUS MEMBRANES |
4% | GOPRELTO | GENUS LIFESCIENCES | N209963 | Dec. 14, 2017 | RX | SOLUTION | NASAL | 10933060 | Feb. 7, 2037 | METHOD FOR THE INDUCTION OF LOCAL ANESTHESIA OF THE MUCOUS MEMBRANES |
4% | GOPRELTO | GENUS LIFESCIENCES | 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 | GENUS LIFESCIENCES | 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 | GENUS LIFESCIENCES | 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 | GENUS LIFESCIENCES | 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 | GENUS LIFESCIENCES | 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 |
Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Exclusivity date | Description |
---|---|---|---|---|---|---|---|---|---|
4% | NUMBRINO | CODY LABS INC | N209575 | Jan. 10, 2020 | RX | SOLUTION | NASAL | Jan. 10, 2023 | NEW PRODUCT |
Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
---|---|---|---|---|---|---|---|---|---|
Sodium-dependent dopamine transporter | Transporter | INHIBITOR | Ki | 7.50 | CHEMBL | IUPHAR | |||
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 | |||||
Sodium channel protein type 5 subunit alpha | Ion channel | WOMBAT-PK | |||||||
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 | 7.19 | CHEMBL | |||||
Dopamine transporter | Transporter | IC50 | 7.02 | CHEMBL |
ID | Source |
---|---|
4019690 | VUID |
N0000147782 | NUI |
D00110 | KEGG_DRUG |
53-21-4 | SECONDARY_CAS_RN |
2653 | RXNORM |
4017521 | VANDF |
4019690 | VANDF |
C0009170 | UMLSCUI |
CHEBI:27958 | CHEBI |
CCA | PDB_CHEM_ID |
CHEMBL370805 | ChEMBL_ID |
CHEMBL120901 | 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 |
Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
---|---|---|---|---|---|---|---|---|
NUMBRINO | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0527-1961 | SOLUTION | 40 mg | NASAL | NDA | 30 sections |
NUMBRINO | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0527-1961 | SOLUTION | 40 mg | NASAL | NDA | 30 sections |
cocaine hydrochloride nasal | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0527-1971 | SOLUTION | 40 mg | TOPICAL | NDA authorized generic | 30 sections |
cocaine hydrochloride nasal | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0527-1971 | SOLUTION | 40 mg | TOPICAL | NDA authorized generic | 30 sections |
cocaine hydrochloride nasal | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0527-1971 | SOLUTION | 40 mg | TOPICAL | NDA authorized generic | 30 sections |
GOPRELTO | HUMAN PRESCRIPTION DRUG LABEL | 1 | 64950-359 | SOLUTION | 40 mg | NASAL | NDA | 35 sections |
GOPRELTO | HUMAN PRESCRIPTION DRUG LABEL | 1 | 64950-359 | SOLUTION | 40 mg | NASAL | NDA | 35 sections |
cocaine hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 64950-362 | SOLUTION | 40 mg | NASAL | NDA AUTHORIZED GENERIC | 35 sections |
cocaine hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 64950-362 | SOLUTION | 40 mg | NASAL | NDA AUTHORIZED GENERIC | 35 sections |