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

Stem definitionDrug idCAS RN
anorexics 195 300-62-9

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • amphetamine aspartate monohydrate
  • benzadrine
  • amphetamine
  • adderall
  • 1-Benzylethylamine
  • phenedrine
  • (+/-)-1-Phenyl-2-aminopropane
  • amfetamine
  • amphetamine sulfate
  • amphetamine aspartate
  • amphetamine adipate
  • amphetamine resin complex
A powerful central nervous system stimulant and sympathomimetic. Amphetamine has multiple mechanisms of action including blocking uptake of adrenergics and dopamine, stimulation of release of monamines, and inhibiting monoamine oxidase. Amphetamine is also a drug of abuse and a psychotomimetic. The l- and the d,l-forms are included here. The l-form has less central nervous system activity but stronger cardiovascular effects. The d-form is DEXTROAMPHETAMINE.
  • Molecular weight: 135.21
  • Formula: C9H13N
  • CLOGP: 1.74
  • LIPINSKI: 0
  • HAC: 1
  • HDO: 1
  • TPSA: 26.02
  • ALOGS: -1.89
  • ROTB: 2

  • Status: OFP

  • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
15 mg O
15 mg P

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 0 Benet LZ, Broccatelli F, Oprea TI
S (Water solubility) 30 mg/mL Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine) 40 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 7.40 ยตM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
Vd (Volume of distribution) 6.10 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 9.70 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.80 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 7.30 hours Lombardo F, Berellini G, Obach RS

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
kinase-safety-class ACVR2A,ACVR2B,AKT1,AKT2,AKT3,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK5,CDK9,DDR1,DYRK1B,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,ITK,JAK2,JAK3,MAP2K6,MAP3K21,MAP3K7,MAPK12,MAPK7,MET,NTRK2,PDK2,PDK4,PIM2,PRKCD,PRKDC,SIK2,SIK3,STK33,SYK,TEK,TGFBR1 40
kinase-selectivity-class AKT2,AKT3,AXL,FLT3,GRK2,PDK4,PRKCD,SIK2 8
pfas-class PFAS structural alert (1 = True, 0 = False) 0

Approvals:

DateAgencyCompanyOrphan
Sept. 9, 1955 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
Toxicity to various agents 1562.72 20.42 690 8280 287156 90332321
Completed suicide 1171.01 20.42 463 8507 144595 90474882
Drug abuse 1142.79 20.42 392 8578 81955 90537522
Cardio-respiratory arrest 426.08 20.42 178 8792 62962 90556515
Respiratory arrest 329.90 20.42 124 8846 33187 90586290
Cardiac arrest 311.41 20.42 168 8802 104767 90514710
Overdose 168.33 20.42 133 8837 157576 90461901
Poisoning 162.79 20.42 60 8910 15157 90604320
Coronary artery dissection 109.04 20.42 24 8946 930 90618547
Substance abuse 79.45 20.42 27 8943 5379 90614098
Renal infarct 76.77 20.42 20 8950 1595 90617882
Exposure via ingestion 75.60 20.42 22 8948 2645 90616832
Intentional overdose 74.87 20.42 67 8903 93767 90525710
Death 74.57 20.42 149 8821 456402 90163075
Agitation 70.17 20.42 56 8914 67042 90552435
Suspected suicide 64.44 20.42 27 8943 9541 90609936
Miosis 51.54 20.42 23 8947 9461 90610016
Unresponsive to stimuli 46.79 20.42 35 8935 38086 90581391
Intestinal infarction 44.91 20.42 12 8958 1055 90618422
Intentional product misuse 42.01 20.42 48 8922 89556 90529921
Drug screen positive 40.84 20.42 15 8955 3742 90615735
Tachycardia 40.65 20.42 63 8907 157610 90461867
Serotonin syndrome 40.40 20.42 32 8938 37855 90581622
Accidental overdose 39.32 20.42 28 8942 28245 90591232
Brain oedema 35.81 20.42 22 8948 17363 90602114
Somnolence 34.92 20.42 69 8901 209015 90410462
Drug dependence 33.94 20.42 26 8944 29301 90590176
Mydriasis 33.50 20.42 20 8950 14992 90604485
Metabolic acidosis 33.43 20.42 34 8936 55642 90563835
Product substitution issue 32.60 20.42 21 8949 17987 90601490
Drug intolerance 30.77 20.42 4 8966 447587 90171890
Suicide attempt 29.75 20.42 37 8933 75362 90544115
Brachial artery entrapment syndrome 29.60 20.42 5 8965 45 90619432
Infusion related reaction 28.00 20.42 4 8966 416776 90202701
Anterograde amnesia 26.35 20.42 7 8963 602 90618875
Product administration interrupted 26.22 20.42 16 8954 12476 90607001
Depressed level of consciousness 26.00 20.42 34 8936 72750 90546727
Diarrhoea 25.98 20.42 33 8937 939157 89680320
Substance use disorder 25.47 20.42 9 8961 2011 90617466
Systemic lupus erythematosus 25.44 20.42 3 8967 361893 90257584
Physical abuse 25.10 20.42 4 8966 24 90619453
Hepatic necrosis 23.87 20.42 12 8958 6426 90613051
Respiratory depression 22.99 20.42 16 8954 15559 90603918
Locked-in syndrome 22.93 20.42 6 8964 486 90618991
Substance abuser 22.76 20.42 5 8965 192 90619285
Amphetamines positive 22.30 20.42 5 8965 211 90619266
Joint swelling 22.28 20.42 11 8959 503289 90116188
Poisoning deliberate 22.17 20.42 16 8954 16470 90603007
Electrocardiogram QT prolonged 21.58 20.42 31 8939 72425 90547052
Arthropathy 21.40 20.42 5 8965 366237 90253240
Cardiogenic shock 20.54 20.42 18 8952 24450 90595027

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
Toxicity to various agents 3014.92 28.01 1338 9325 227798 42382874
Drug abuse 2356.57 28.01 903 9760 103868 42506804
Completed suicide 582.94 28.01 338 10325 96127 42514545
Substance abuse 373.29 28.01 123 10540 8782 42601890
Respiratory arrest 365.26 28.01 166 10497 28258 42582414
Overdose 277.25 28.01 221 10442 105043 42505629
Cardio-respiratory arrest 272.22 28.01 174 10489 58462 42552210
Cardiac arrest 230.70 28.01 202 10461 109118 42501554
Intentional product misuse 204.66 28.01 149 10514 61751 42548921
Brain oedema 186.58 28.01 88 10575 16239 42594433
Poisoning 176.54 28.01 82 10581 14617 42596055
Aggression 168.32 28.01 116 10547 44047 42566625
Pulmonary oedema 155.38 28.01 119 10544 53153 42557519
Respiratory depression 145.75 28.01 78 10585 18790 42591882
Myelopathy 141.69 28.01 45 10618 2846 42607826
Drug dependence 138.92 28.01 88 10575 29006 42581666
Decreased eye contact 117.06 28.01 27 10636 496 42610176
Oppositional defiant disorder 114.66 28.01 27 10636 545 42610127
Bruxism 99.06 28.01 32 10631 2137 42608535
Substance use disorder 83.94 28.01 36 10627 5309 42605363
Drug use disorder 83.38 28.01 44 10619 10289 42600383
Homicidal ideation 79.77 28.01 29 10634 2765 42607907
Rhabdomyolysis 75.13 28.01 95 10568 77924 42532748
Serotonin syndrome 71.48 28.01 56 10607 25789 42584883
Crying 65.51 28.01 32 10631 6362 42604310
Compartment syndrome 64.63 28.01 26 10637 3263 42607409
Abnormal behaviour 59.86 28.01 51 10612 26400 42584272
Internal injury 58.02 28.01 9 10654 12 42610660
Choreoathetosis 57.40 28.01 18 10645 1091 42609581
Diarrhoea 57.27 28.01 22 10641 460827 42149845
Trismus 53.93 28.01 22 10641 2862 42607810
Exposure via ingestion 53.13 28.01 20 10643 2102 42608570
Substance use 53.08 28.01 19 10644 1732 42608940
Dyskinesia 51.50 28.01 46 10617 25344 42585328
Accidental poisoning 50.65 28.01 17 10646 1279 42609393
Miosis 50.39 28.01 35 10628 13411 42597261
Drug interaction 49.65 28.01 163 10500 266836 42343836
Unresponsive to stimuli 48.63 28.01 49 10614 31354 42579318
Pulmonary congestion 47.67 28.01 36 10627 15694 42594978
Quadriparesis 47.64 28.01 19 10644 2331 42608341
Dyspnoea 47.40 28.01 26 10637 442595 42168077
Pyrexia 46.97 28.01 20 10643 394022 42216650
Accidental overdose 45.33 28.01 45 10618 28285 42582387
Withdrawal syndrome 45.19 28.01 34 10629 14741 42595931
Coordination abnormal 45.13 28.01 27 10636 8023 42602649
Anaemia 44.94 28.01 8 10655 280270 42330402
Psychomotor hyperactivity 44.56 28.01 30 10633 10928 42599744
Intentional overdose 43.79 28.01 59 10604 51397 42559275
Spinal shock 43.70 28.01 8 10655 42 42610630
Hyperkinesia 42.66 28.01 17 10646 2081 42608591
Pneumonia 42.08 28.01 27 10636 422122 42188550
Suicidal ideation 39.13 28.01 54 10609 48107 42562565
Bladder dilatation 38.97 28.01 15 10648 1675 42608997
Vertebral artery dissection 38.69 28.01 7 10656 34 42610638
Irritability 38.35 28.01 41 10622 28087 42582585
Prescription drug used without a prescription 38.34 28.01 17 10646 2713 42607959
Affect lability 37.75 28.01 19 10644 4025 42606647
Poor quality sleep 36.37 28.01 25 10638 9415 42601257
Off label use 35.80 28.01 66 10597 638269 41972403
Mood altered 35.77 28.01 26 10637 10692 42599980
Mydriasis 35.63 28.01 24 10639 8746 42601926
Streptococcal infection 35.50 28.01 21 10642 6111 42604561
Stress cardiomyopathy 34.85 28.01 16 10647 2769 42607903
Counterfeit product administered 34.34 28.01 9 10654 285 42610387
Thrombocytopenia 33.79 28.01 4 10659 190275 42420397
Drug screen positive 31.65 28.01 17 10646 4114 42606558
Rash 31.47 28.01 15 10648 276939 42333733
Impaired driving ability 30.90 28.01 15 10648 2940 42607732
Sepsis 29.21 28.01 7 10656 199327 42411345
Cluster headache 28.58 28.01 9 10654 553 42610119

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 4471.06 21.97 1925 15594 478630 110093150
Drug abuse 3546.20 21.97 1245 16274 176166 110395614
Completed suicide 1672.23 21.97 796 16723 241585 110330195
Respiratory arrest 731.49 21.97 293 17226 58006 110513774
Cardio-respiratory arrest 715.31 21.97 354 17165 115482 110456298
Cardiac arrest 569.93 21.97 366 17153 196387 110375393
Overdose 437.90 21.97 333 17186 233461 110338319
Substance abuse 395.92 21.97 125 17394 12338 110559442
Poisoning 342.99 21.97 140 17379 28965 110542815
Intentional product misuse 236.70 21.97 184 17335 132720 110439060
Brain oedema 206.24 21.97 100 17419 30998 110540782
Aggression 203.31 21.97 123 17396 59087 110512693
Respiratory depression 182.86 21.97 93 17426 31908 110539872
Drug dependence 164.24 21.97 101 17418 49919 110521861
Pulmonary oedema 150.75 21.97 126 17393 100533 110471247
Death 132.70 21.97 321 17198 698548 109873232
Oppositional defiant disorder 129.60 21.97 27 17492 491 110571289
Exposure via ingestion 126.45 21.97 42 17477 4858 110566922
Accidental overdose 122.04 21.97 85 17434 51749 110520031
Coronary artery dissection 120.89 21.97 30 17489 1218 110570562
Serotonin syndrome 118.65 21.97 88 17431 59065 110512715
Substance use disorder 117.38 21.97 44 17475 7246 110564534
Decreased eye contact 114.30 21.97 27 17492 888 110570892
Intentional overdose 105.27 21.97 117 17402 132384 110439396
Drug use disorder 104.61 21.97 53 17466 18021 110553759
Miosis 103.11 21.97 56 17463 21927 110549853
Unresponsive to stimuli 99.93 21.97 82 17437 63708 110508072
Bruxism 90.94 21.97 33 17486 4961 110566819
Homicidal ideation 81.41 21.97 28 17491 3599 110568181
Agitation 79.93 21.97 94 17425 112957 110458823
Abnormal behaviour 78.09 21.97 58 17461 38981 110532799
Diarrhoea 76.37 21.97 43 17476 1139462 109432318
Suspected suicide 74.86 21.97 40 17479 15159 110556621
Drug screen positive 69.25 21.97 29 17490 6381 110565399
Pulmonary congestion 66.44 21.97 48 17471 30918 110540862
Mydriasis 65.80 21.97 42 17477 22115 110549665
Off label use 57.06 21.97 94 17425 1500091 109071689
Dyskinesia 56.32 21.97 54 17465 51392 110520388
Renal infarct 52.87 21.97 20 17499 3375 110568405
Drug interaction 51.42 21.97 185 17334 499998 110071782
Dyspnoea 51.38 21.97 60 17459 1106812 109464968
Rhabdomyolysis 51.03 21.97 78 17441 120323 110451457
Pyrexia 50.58 21.97 41 17478 898224 109673556
Suicidal ideation 50.28 21.97 68 17451 93869 110477911
Choreoathetosis 49.65 21.97 16 17503 1682 110570098
Drug intolerance 49.39 21.97 4 17515 406508 110165272
Amphetamines positive 48.83 21.97 11 17508 292 110571488
Irritability 48.25 21.97 48 17471 47761 110524019
Accidental poisoning 47.40 21.97 17 17502 2470 110569310
Anaemia 47.30 21.97 14 17505 547072 110024708
Substance use 47.28 21.97 17 17502 2489 110569291
Psychomotor hyperactivity 47.11 21.97 33 17486 20244 110551536
Internal injury 46.50 21.97 11 17508 364 110571416
Physical abuse 46.45 21.97 8 17511 48 110571732
Trismus 46.09 21.97 22 17497 6574 110565206
Pneumonia 44.57 21.97 44 17475 876670 109695110
Withdrawal syndrome 44.29 21.97 38 17481 31342 110540438
Hyperkinesia 43.31 21.97 17 17502 3167 110568613
Joint swelling 40.78 21.97 10 17509 442835 110128945
Infusion related reaction 40.61 21.97 6 17513 381156 110190624
Tachycardia 40.53 21.97 102 17417 226543 110345237
Prescription drug used without a prescription 40.46 21.97 19 17500 5477 110566303
Compartment syndrome 39.14 21.97 19 17500 5891 110565889
Arthralgia 38.61 21.97 40 17479 779592 109792188
Cardiogenic shock 37.74 21.97 46 17473 57292 110514488
Malaise 37.35 21.97 31 17488 671788 109899992
Hepatic enzyme increased 36.73 21.97 4 17515 320888 110250892
Crying 36.10 21.97 31 17488 25597 110546183
Intestinal infarction 35.87 21.97 12 17507 1418 110570362
Streptococcal infection 35.74 21.97 22 17497 10868 110560912
Suicide attempt 35.64 21.97 61 17458 103333 110468447
Rash 35.42 21.97 47 17472 820917 109750863
Stress cardiomyopathy 35.04 21.97 25 17494 15781 110555999
Pruritus 34.65 21.97 25 17494 581535 109990245
Arthropathy 34.44 21.97 3 17516 287519 110284261
Cyanosis 34.04 21.97 32 17487 29709 110542071
Counterfeit product administered 33.69 21.97 8 17511 269 110571511
Coordination abnormal 32.49 21.97 29 17490 25199 110546581
Mood altered 32.46 21.97 27 17492 21348 110550432
Impaired driving ability 32.03 21.97 17 17502 6353 110565427
Thrombocytopenia 31.87 21.97 8 17511 348877 110222903
Vomiting 31.83 21.97 60 17459 910615 109661165
Pain 31.59 21.97 65 17454 954890 109616890
Asthenia 31.20 21.97 38 17481 688961 109882819
Coma 31.13 21.97 62 17457 117807 110453973
Nasopharyngitis 30.75 21.97 12 17507 394349 110177431
Condition aggravated 30.74 21.97 43 17476 734793 109836987
Somnolence 30.49 21.97 110 17409 297339 110274441
Swelling 30.28 21.97 9 17510 351032 110220748
Alcohol abuse 30.12 21.97 15 17504 4914 110566866
Vertebral artery dissection 30.00 21.97 7 17512 218 110571562
General physical health deterioration 29.92 21.97 15 17504 425280 110146500
Nausea 29.53 21.97 99 17420 1235591 109336189
Drug hypersensitivity 29.08 21.97 18 17501 454072 110117708
Product substitution issue 28.69 21.97 26 17493 23035 110548745
Accident 28.22 21.97 19 17500 10933 110560847
Metabolic acidosis 28.20 21.97 54 17465 99690 110472090
Asphyxia 28.15 21.97 21 17498 14194 110557586
Treatment failure 28.10 21.97 5 17514 277229 110294551
Abdominal discomfort 27.54 21.97 14 17505 393844 110177936
Affect lability 27.18 21.97 23 17496 18614 110553166
Stomatitis 27.12 21.97 5 17514 270237 110301543
Contraindicated product administered 26.22 21.97 4 17515 248263 110323517
Depressed level of consciousness 26.06 21.97 56 17463 112222 110459558
Brachial artery entrapment syndrome 26.02 21.97 5 17514 59 110571721
Substance-induced psychotic disorder 25.94 21.97 14 17505 5410 110566370
Neuromuscular blockade 25.86 21.97 8 17511 736 110571044
Cluster headache 25.86 21.97 9 17510 1198 110570582
Paranoia 25.46 21.97 24 17495 22350 110549430
Drug ineffective 25.20 21.97 140 17379 1520400 109051380
Therapeutic product effect incomplete 25.08 21.97 3 17516 223802 110347978
Loss of consciousness 24.89 21.97 78 17441 196228 110375552
Drug diversion 24.68 21.97 9 17510 1371 110570409
Screaming 24.47 21.97 13 17506 4868 110566912
Pericarditis 24.39 21.97 3 17516 219111 110352669
Wound 24.26 21.97 4 17515 234433 110337347
C-reactive protein increased 24.22 21.97 3 17516 217916 110353864
Accidental death 24.15 21.97 13 17506 4996 110566784
Poisoning deliberate 23.95 21.97 25 17494 26306 110545474
Cough 23.60 21.97 23 17496 461618 110110162
Rheumatoid arthritis 23.54 21.97 9 17510 299604 110272176
Speech disorder 23.46 21.97 38 17481 61531 110510249
Postmortem blood drug level abnormal 22.75 21.97 7 17512 633 110571147
Hyperthermia 22.66 21.97 22 17497 21250 110550530
Peripheral swelling 21.99 21.97 19 17500 404015 110167765
Hypersensitivity 21.98 21.97 19 17500 403979 110167801

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC N06BA01 NERVOUS SYSTEM
PSYCHOANALEPTICS
PSYCHOSTIMULANTS, AGENTS USED FOR ADHD AND NOOTROPICS
Centrally acting sympathomimetics
CHEBI has role CHEBI:35523 bronchodilator agent
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:37962 adrenergic agent
CHEBI has role CHEBI:48560 dopaminergic agent
CHEBI has role CHEBI:50910 neurotoxin
CHEBI has role CHEBI:51039 dopamine uptake inhibitor
CHEBI has role CHEBI:78298 environmental contaminant
MeSH PA D000697 Central Nervous System Stimulants
MeSH PA D002491 Central Nervous System Agents
MeSH PA D013566 Sympathomimetics
MeSH PA D014179 Neurotransmitter Uptake Inhibitors
MeSH PA D015259 Dopamine Agents
MeSH PA D018377 Neurotransmitter Agents
MeSH PA D018663 Adrenergic Agents
MeSH PA D018759 Adrenergic Uptake Inhibitors
MeSH PA D018765 Dopamine Uptake Inhibitors
MeSH PA D049990 Membrane Transport Modulators
FDA PE N0000175729 Central Nervous System Stimulation
FDA EPC N0000175739 Central Nervous System Stimulant
CHEBI has role CHEBI:74518 anti-obesity agent

Related Drugs by ATC class:

N06BA Centrally acting sympathomimetics 14 drugs

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

DiseaseRelationSNOMED_IDDOID
Narcolepsy indication 60380001 DOID:8986
Attention deficit hyperactivity disorder indication 406506008
Obesity indication 414916001 DOID:9970
Ocular hypertension contraindication 4210003 DOID:9282
Gilles de la Tourette's syndrome contraindication 5158005 DOID:11119
Suicidal thoughts contraindication 6471006
Dependent drug abuse contraindication 6525002
Alcoholism contraindication 7200002
Hyperammonemia contraindication 9360008
Chronic obstructive lung disease contraindication 13645005 DOID:3083
Bipolar disorder contraindication 13746004 DOID:3312
Hepatic encephalopathy contraindication 13920009 DOID:13413
Myocardial infarction contraindication 22298006 DOID:5844
Glaucoma contraindication 23986001 DOID:1686
Feeling agitated contraindication 24199005
Hyperthyroidism contraindication 34486009 DOID:7998
Depressive disorder contraindication 35489007
Hypertensive disorder contraindication 38341003 DOID:10763
Hyperactive behavior contraindication 44548000
Conduction disorder of the heart contraindication 44808001
Chronic heart failure contraindication 48447003
Disorder of cardiovascular system contraindication 49601007 DOID:1287
Anorexia nervosa contraindication 56882008 DOID:8689
Hepatic failure contraindication 59927004
Aggressive behavior contraindication 61372001
Substance abuse contraindication 66214007
Psychotic disorder contraindication 69322001
Arteriosclerotic vascular disease contraindication 72092001
Hepatic coma contraindication 72836002 DOID:12550
Diabetes mellitus contraindication 73211009 DOID:9351
Sleep apnea contraindication 73430006 DOID:0050847
Open-angle glaucoma contraindication 84494001 DOID:1067
Cardiomyopathy contraindication 85898001 DOID:0050700
Weight loss contraindication 89362005
Kidney disease contraindication 90708001 DOID:557
Structural disorder of heart contraindication 128599005
Seizure disorder contraindication 128613002
Motor tic disorder contraindication 230337001
Cerebrovascular accident contraindication 230690007
Mania contraindication 231494001
Disease of liver contraindication 235856003 DOID:409
Sleep automatism contraindication 247962006
Anemia contraindication 271737000 DOID:2355
Pregnancy, function contraindication 289908002
Thrombocytopenic disorder contraindication 302215000 DOID:1588
Neutropenic disorder contraindication 303011007 DOID:1227
Angle-closure glaucoma contraindication 392291006 DOID:13550
Cardiovascular event risk contraindication 395112001
Visual impairment contraindication 397540003
Respiratory insufficiency contraindication 409623005
Breastfeeding (mother) contraindication 413712001
Disorder of coronary artery contraindication 414024009
Myocardial ischemia contraindication 414795007 DOID:3393
Myocardial infarction in recovery phase contraindication 418044006
Porphyria contraindication 418470004
Hypertensive urgency contraindication 443482000
Acute exacerbation of asthma contraindication 708038006




๐Ÿถ Veterinary Drug Use

None

๐Ÿถ Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 9.89 Basic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
12.5MG;12.5MG;12.5MG;12.5MG MYDAYIS TAKEDA PHARMS USA N022063 June 20, 2017 RX CAPSULE, EXTENDED RELEASE ORAL 9173857 May 12, 2026 TREATMENT OF ATTENTION DEFICIT HYPERACTIVITY DISORDER
3.125MG;3.125MG;3.125MG;3.125MG MYDAYIS TAKEDA PHARMS USA N022063 June 20, 2017 RX CAPSULE, EXTENDED RELEASE ORAL 9173857 May 12, 2026 TREATMENT OF ATTENTION DEFICIT HYPERACTIVITY DISORDER
6.25MG;6.25MG;6.25MG;6.25MG MYDAYIS TAKEDA PHARMS USA N022063 June 20, 2017 RX CAPSULE, EXTENDED RELEASE ORAL 9173857 May 12, 2026 TREATMENT OF ATTENTION DEFICIT HYPERACTIVITY DISORDER
9.375MG;9.375MG;9.375MG;9.375MG MYDAYIS TAKEDA PHARMS USA N022063 June 20, 2017 RX CAPSULE, EXTENDED RELEASE ORAL 9173857 May 12, 2026 TREATMENT OF ATTENTION DEFICIT HYPERACTIVITY DISORDER
2MG/ML;EQ 0.5MG BASE/ML DYANAVEL XR TRIS PHARMA INC N208147 Oct. 19, 2015 RX SUSPENSION, EXTENDED RELEASE ORAL 11590228 Sept. 7, 2036 METHOD OF TREATING ATTENTION DEFICIT HYPERACTIVITY DISORDER
10MG EVEKEO ODT AZURITY N209905 Jan. 30, 2019 DISCN TABLET, ORALLY DISINTEGRATING ORAL 11896562 March 10, 2037 TREATMENT OF ATTENTION DEFICIT HYPERACTIVITY DISORDER (ADHD) IN PEDIATRIC PATIENTS
15MG EVEKEO ODT AZURITY N209905 Jan. 30, 2019 DISCN TABLET, ORALLY DISINTEGRATING ORAL 11896562 March 10, 2037 TREATMENT OF ATTENTION DEFICIT HYPERACTIVITY DISORDER (ADHD) IN PEDIATRIC PATIENTS
20MG EVEKEO ODT AZURITY N209905 Jan. 30, 2019 DISCN TABLET, ORALLY DISINTEGRATING ORAL 11896562 March 10, 2037 TREATMENT OF ATTENTION DEFICIT HYPERACTIVITY DISORDER (ADHD) IN PEDIATRIC PATIENTS
5MG EVEKEO ODT AZURITY N209905 Jan. 30, 2019 DISCN TABLET, ORALLY DISINTEGRATING ORAL 11896562 March 10, 2037 TREATMENT OF ATTENTION DEFICIT HYPERACTIVITY DISORDER (ADHD) IN PEDIATRIC PATIENTS
12MG;EQ 3MG BASE DYANAVEL XR 15 TRIS PHARMA INC N210526 Nov. 4, 2021 RX TABLET, EXTENDED RELEASE ORAL 11590081 Sept. 24, 2038 METHOD OF TREATING ATTENTION DEFICIT HYPERACTIVITY DISORDER
16MG;EQ 4MG BASE DYANAVEL XR 20 TRIS PHARMA INC N210526 Nov. 4, 2021 RX TABLET, EXTENDED RELEASE ORAL 11590081 Sept. 24, 2038 METHOD OF TREATING ATTENTION DEFICIT HYPERACTIVITY DISORDER
4MG;EQ 1MG BASE DYANAVEL XR 5 TRIS PHARMA INC N210526 Nov. 4, 2021 RX TABLET, EXTENDED RELEASE ORAL 11590081 Sept. 24, 2038 METHOD OF TREATING ATTENTION DEFICIT HYPERACTIVITY DISORDER
8MG;EQ 2MG BASE DYANAVEL XR 10 TRIS PHARMA INC N210526 Nov. 4, 2021 RX TABLET, EXTENDED RELEASE ORAL 11590081 Sept. 24, 2038 METHOD OF TREATING ATTENTION DEFICIT HYPERACTIVITY DISORDER
12MG;EQ 3MG BASE DYANAVEL XR 15 TRIS PHARMA INC N210526 Nov. 4, 2021 RX TABLET, EXTENDED RELEASE ORAL 12458592 Feb. 11, 2040 METHOD OF TREATING ATTENTION DEFICIT HYPERACTIVITY DISORDER
16MG;EQ 4MG BASE DYANAVEL XR 20 TRIS PHARMA INC N210526 Nov. 4, 2021 RX TABLET, EXTENDED RELEASE ORAL 12458592 Feb. 11, 2040 METHOD OF TREATING ATTENTION DEFICIT HYPERACTIVITY DISORDER
4MG;EQ 1MG BASE DYANAVEL XR 5 TRIS PHARMA INC N210526 Nov. 4, 2021 RX TABLET, EXTENDED RELEASE ORAL 12458592 Feb. 11, 2040 METHOD OF TREATING ATTENTION DEFICIT HYPERACTIVITY DISORDER
8MG;EQ 2MG BASE DYANAVEL XR 10 TRIS PHARMA INC N210526 Nov. 4, 2021 RX TABLET, EXTENDED RELEASE ORAL 12458592 Feb. 11, 2040 METHOD OF TREATING ATTENTION DEFICIT HYPERACTIVITY DISORDER

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Sodium-dependent dopamine transporter Transporter RELEASING AGENT Ki 6.94 PDSP CHEMBL
Sodium-dependent noradrenaline transporter Transporter RELEASING AGENT CHEMBL CHEMBL
Alpha-1A adrenergic receptor GPCR WOMBAT-PK
Cocaine- and amphetamine-regulated transcript protein Transcription factor WOMBAT-PK
Alpha-2A adrenergic receptor GPCR WOMBAT-PK
Trace amine-associated receptor 1 GPCR AGONIST EC50 6.22 SCIENTIFIC LITERATURE
Sodium-dependent serotonin transporter Transporter Ki 5.75 PDSP
Sodium-dependent dopamine transporter Transporter IC50 6.02 CHEMBL
Amine oxidase [flavin-containing] A Enzyme Ki 4.91 CHEMBL
Sodium-dependent noradrenaline transporter Transporter IC50 6 CHEMBL
5-hydroxytryptamine receptor 2B GPCR Kd 5.27 CHEMBL
Sodium-dependent serotonin transporter Transporter IC50 4.35 CHEMBL
Transporter Transporter IC50 6.70 CHEMBL
Serotonin (5-HT) receptor GPCR Kd 5.27 CHEMBL
Serotonin 1 (5-HT1) receptor GPCR Ki 5.12 CHEMBL
Serotonin 2 (5-HT2) receptor GPCR Ki 4.37 CHEMBL

External reference:

IDSource
4019611 VUID
N0000147705 NUI
D02074 KEGG_DRUG
60-13-9 SECONDARY_CAS_RN
221057 RXNORM
C0002658 UMLSCUI
CHEBI:2679 CHEBI
CHEMBL405 ChEMBL_ID
CHEMBL501 ChEMBL_ID
CHEMBL1200377 ChEMBL_ID
CHEMBL1200387 ChEMBL_ID
DB00182 DRUGBANK_ID
C090411 MESH_SUPPLEMENTAL_RECORD_UI
64770-51-0 SECONDARY_CAS_RN
3007 PUBCHEM_CID
290726 MMSL
31375 MMSL
4188 MMSL
4189 MMSL
6025 MMSL
d00803 MMSL
D000661 MESH_DESCRIPTOR_UI
377 INN_ID
4804 IUPHAR_LIGAND_ID
4018832 VANDF
4018833 VANDF
4018834 VANDF
4019611 VANDF
4022215 VANDF
CK833KGX7E UNII
001790 NDDF
001791 NDDF
001792 NDDF
006719 NDDF
116344009 SNOMEDCT_US
22672005 SNOMEDCT_US
232451000087107 SNOMEDCT_US
703842006 SNOMEDCT_US
87148003 SNOMEDCT_US
CK833KGX7E INXIGHT DRUGS

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Dextroamphetamine Saccharate, Amphetamine Aspartate, Dextroamphetamine Sulfate and Amphetamine Sulfate HUMAN PRESCRIPTION DRUG LABEL 4 0115-1328 CAPSULE, EXTENDED RELEASE 1.25 mg ORAL NDA AUTHORIZED GENERIC 36 sections
Dextroamphetamine Saccharate, Amphetamine Aspartate, Dextroamphetamine Sulfate and Amphetamine Sulfate HUMAN PRESCRIPTION DRUG LABEL 4 0115-1329 CAPSULE, EXTENDED RELEASE 2.50 mg ORAL NDA AUTHORIZED GENERIC 36 sections
Dextroamphetamine Saccharate, Amphetamine Aspartate, Dextroamphetamine Sulfate and Amphetamine Sulfate HUMAN PRESCRIPTION DRUG LABEL 4 0115-1330 CAPSULE, EXTENDED RELEASE 3.75 mg ORAL NDA AUTHORIZED GENERIC 36 sections
Dextroamphetamine Saccharate, Amphetamine Aspartate, Dextroamphetamine Sulfate and Amphetamine Sulfate HUMAN PRESCRIPTION DRUG LABEL 4 0115-1331 CAPSULE, EXTENDED RELEASE 5 mg ORAL NDA AUTHORIZED GENERIC 36 sections
Dextroamphetamine Saccharate, Amphetamine Aspartate, Dextroamphetamine Sulfate and Amphetamine Sulfate HUMAN PRESCRIPTION DRUG LABEL 4 0115-1332 CAPSULE, EXTENDED RELEASE 6.25 mg ORAL NDA AUTHORIZED GENERIC 36 sections
Dextroamphetamine Saccharate, Amphetamine Aspartate, Dextroamphetamine Sulfate and Amphetamine Sulfate HUMAN PRESCRIPTION DRUG LABEL 4 0115-1333 CAPSULE, EXTENDED RELEASE 7.50 mg ORAL NDA AUTHORIZED GENERIC 36 sections
Dextroamphetamine Saccharate, Amphetamine Aspartate Monohydrate, Dextroamphetamine Sulfate and Amphetamine Sulfate HUMAN PRESCRIPTION DRUG LABEL 4 0115-1486 CAPSULE 1.25 mg ORAL ANDA 29 sections
Dextroamphetamine Saccharate, Amphetamine Aspartate Monohydrate, Dextroamphetamine Sulfate and Amphetamine Sulfate HUMAN PRESCRIPTION DRUG LABEL 4 0115-1486 CAPSULE 1.25 mg ORAL ANDA 29 sections
Dextroamphetamine Saccharate, Amphetamine Aspartate Monohydrate, Dextroamphetamine Sulfate and Amphetamine Sulfate HUMAN PRESCRIPTION DRUG LABEL 4 0115-1487 CAPSULE 2.50 mg ORAL ANDA 29 sections
Dextroamphetamine Saccharate, Amphetamine Aspartate Monohydrate, Dextroamphetamine Sulfate and Amphetamine Sulfate HUMAN PRESCRIPTION DRUG LABEL 4 0115-1487 CAPSULE 2.50 mg ORAL ANDA 29 sections
Dextroamphetamine Saccharate, Amphetamine Aspartate Monohydrate, Dextroamphetamine Sulfate and Amphetamine Sulfate HUMAN PRESCRIPTION DRUG LABEL 4 0115-1488 CAPSULE 3.75 mg ORAL ANDA 29 sections
Dextroamphetamine Saccharate, Amphetamine Aspartate Monohydrate, Dextroamphetamine Sulfate and Amphetamine Sulfate HUMAN PRESCRIPTION DRUG LABEL 4 0115-1488 CAPSULE 3.75 mg ORAL ANDA 29 sections
Dextroamphetamine Saccharate, Amphetamine Aspartate Monohydrate, Dextroamphetamine Sulfate and Amphetamine Sulfate HUMAN PRESCRIPTION DRUG LABEL 4 0115-1489 CAPSULE 5 mg ORAL ANDA 29 sections
Dextroamphetamine Saccharate, Amphetamine Aspartate Monohydrate, Dextroamphetamine Sulfate and Amphetamine Sulfate HUMAN PRESCRIPTION DRUG LABEL 4 0115-1489 CAPSULE 5 mg ORAL ANDA 29 sections
Dextroamphetamine Saccharate, Amphetamine Aspartate Monohydrate, Dextroamphetamine Sulfate and Amphetamine Sulfate HUMAN PRESCRIPTION DRUG LABEL 4 0115-1490 CAPSULE 6.25 mg ORAL ANDA 29 sections
Dextroamphetamine Saccharate, Amphetamine Aspartate Monohydrate, Dextroamphetamine Sulfate and Amphetamine Sulfate HUMAN PRESCRIPTION DRUG LABEL 4 0115-1490 CAPSULE 6.25 mg ORAL ANDA 29 sections
Dextroamphetamine Saccharate, Amphetamine Aspartate Monohydrate, Dextroamphetamine Sulfate and Amphetamine Sulfate HUMAN PRESCRIPTION DRUG LABEL 4 0115-1491 CAPSULE 7.50 mg ORAL ANDA 29 sections
Dextroamphetamine Saccharate, Amphetamine Aspartate Monohydrate, Dextroamphetamine Sulfate and Amphetamine Sulfate HUMAN PRESCRIPTION DRUG LABEL 4 0115-1491 CAPSULE 7.50 mg ORAL ANDA 29 sections
Dextroamphetamine Saccharate, Amphetamine Aspartate Monohydrate, Dextroamphetamine Sulfate and Amphetamine Sulfate HUMAN PRESCRIPTION DRUG LABEL 4 0185-0831 TABLET 1.25 mg ORAL ANDA 22 sections
Dextroamphetamine Saccharate, Amphetamine Aspartate Monohydrate, Dextroamphetamine Sulfate and Amphetamine Sulfate HUMAN PRESCRIPTION DRUG LABEL 4 0185-0842 TABLET 2.50 mg ORAL ANDA 22 sections
Dextroamphetamine Saccharate, Amphetamine Aspartate Monohydrate, Dextroamphetamine Sulfate and Amphetamine Sulfate HUMAN PRESCRIPTION DRUG LABEL 4 0185-0853 TABLET 5 mg ORAL ANDA 22 sections
Dextroamphetamine Saccharate, Amphetamine Aspartate Monohydrate, Dextroamphetamine Sulfate and Amphetamine Sulfate HUMAN PRESCRIPTION DRUG LABEL 4 0185-0864 TABLET 7.50 mg ORAL ANDA 22 sections
Dextroamphetamine Saccharate, Amphetamine Aspartate Monohydrate, Dextroamphetamine Sulfate and Amphetamine Sulfate HUMAN PRESCRIPTION DRUG LABEL 4 0185-2098 TABLET 1.25 mg ORAL ANDA 22 sections
Dextroamphetamine Saccharate, Amphetamine Aspartate Monohydrate, Dextroamphetamine Sulfate and Amphetamine Sulfate HUMAN PRESCRIPTION DRUG LABEL 4 0185-2099 TABLET 7.50 mg ORAL ANDA 22 sections
Dextroamphetamine saccharate, amphetamine aspartate monohydrate, dextroamphetamine sulfate, amphetamine sulfate HUMAN PRESCRIPTION DRUG LABEL 4 0228-3059 CAPSULE, EXTENDED RELEASE 2.50 mg ORAL ANDA 26 sections
Dextroamphetamine saccharate, amphetamine aspartate monohydrate, dextroamphetamine sulfate, amphetamine sulfate HUMAN PRESCRIPTION DRUG LABEL 4 0228-3059 CAPSULE, EXTENDED RELEASE 2.50 mg ORAL ANDA 26 sections
Dextroamphetamine saccharate, amphetamine aspartate monohydrate, dextroamphetamine sulfate, amphetamine sulfate HUMAN PRESCRIPTION DRUG LABEL 4 0228-3060 CAPSULE, EXTENDED RELEASE 5 mg ORAL ANDA 26 sections
Dextroamphetamine saccharate, amphetamine aspartate monohydrate, dextroamphetamine sulfate, amphetamine sulfate HUMAN PRESCRIPTION DRUG LABEL 4 0228-3060 CAPSULE, EXTENDED RELEASE 5 mg ORAL ANDA 26 sections
Dextroamphetamine saccharate, amphetamine aspartate monohydrate, dextroamphetamine sulfate, amphetamine sulfate HUMAN PRESCRIPTION DRUG LABEL 4 0228-3061 CAPSULE, EXTENDED RELEASE 7.50 mg ORAL ANDA 26 sections
Dextroamphetamine saccharate, amphetamine aspartate monohydrate, dextroamphetamine sulfate, amphetamine sulfate HUMAN PRESCRIPTION DRUG LABEL 4 0228-3061 CAPSULE, EXTENDED RELEASE 7.50 mg ORAL ANDA 26 sections