modafinil Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
1826 68693-11-8

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • modafinil
  • (+/-)-Modafinil
  • modaphonil
  • modiodal
A benzhydryl acetamide compound, central nervous system stimulant, and CYP3A4 inducing agent that is used in the treatment of NARCOLEPSY and SLEEP WAKE DISORDERS.
  • Molecular weight: 273.35
  • Formula: C15H15NO2S
  • CLOGP: 0.94
  • LIPINSKI: 0
  • HAC: 3
  • HDO: 1
  • TPSA: 60.16
  • ALOGS: -2.64
  • ROTB: 5

  • Status: OFP

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

Drug dosage:

DoseUnitRoute
0.30 g O

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 2 Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine) 8 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 20.90 ┬ÁM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability) 80 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H

Approvals:

DateAgencyCompanyOrphan
Dec. 24, 1998 FDA CEPHALON
Feb. 21, 2020 PMDA Alfresa Pharma Corporation

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
Multiple sclerosis relapse 366.10 11.07 250 25738 41875 46618199
Cataplexy 217.00 11.07 61 25927 1102 46658972
Multiple sclerosis 184.68 11.07 134 25854 24657 46635417
Depression 162.90 11.07 318 25670 169786 46490288
Pre-existing condition improved 139.95 11.07 70 25918 6542 46653532
Sleep apnoea syndrome 125.80 11.07 102 25886 22099 46637975
Suicidal ideation 105.49 11.07 143 25845 56239 46603835
Anxiety 81.26 11.07 254 25734 181703 46478371
Rheumatoid arthritis 77.90 11.07 19 25969 240196 46419878
Narcolepsy 70.76 11.07 26 25962 1133 46658941
Influenza like illness 65.41 11.07 116 25872 57454 46602620
Somnambulism 63.88 11.07 38 25950 4999 46655075
Balance disorder 56.04 11.07 116 25872 64405 46595669
Somnolence 51.90 11.07 198 25790 156323 46503751
Death 50.35 11.07 68 25920 335480 46324594
Snoring 49.02 11.07 28 25960 3414 46656660
Gait disturbance 42.70 11.07 177 25811 145086 46514988
Migraine 42.16 11.07 109 25879 69917 46590157
Enuresis 41.80 11.07 21 25967 1979 46658095
Acute kidney injury 40.44 11.07 43 25945 235812 46424262
Fall 40.37 11.07 317 25671 328780 46331294
Muscle spasticity 39.89 11.07 40 25948 11400 46648674
Polycystic ovaries 39.50 11.07 18 25970 1366 46658708
Joint swelling 38.96 11.07 22 25966 166051 46494023
Therapeutic response unexpected 37.71 11.07 45 25943 15571 46644503
Memory impairment 37.28 11.07 111 25877 77226 46582848
Psychotic disorder 37.25 11.07 54 25934 22567 46637507
Fatigue 35.49 11.07 504 25484 608193 46051881
Seizure 33.87 11.07 147 25841 122907 46537167
Hypoaesthesia 32.71 11.07 142 25846 118727 46541347
Off label use 31.09 11.07 108 25880 379733 46280341
Pregnancy on oral contraceptive 30.83 11.07 15 25973 1319 46658755
Neutropenia 30.77 11.07 21 25967 143183 46516891
Magnetic resonance imaging abnormal 30.48 11.07 19 25969 2717 46657357
Sleep paralysis 30.37 11.07 11 25977 460 46659614
Secondary progressive multiple sclerosis 29.05 11.07 14 25974 1206 46658868
Treatment failure 28.91 11.07 8 25980 93079 46566995
Stress 28.74 11.07 78 25910 51473 46608601
Thrombocytopenia 27.95 11.07 18 25970 126563 46533511
Parasomnia 27.91 11.07 10 25978 405 46659669
Febrile neutropenia 27.81 11.07 9 25979 94618 46565456
Histoplasmosis 27.48 11.07 15 25973 1675 46658399
Hypersensitivity vasculitis 27.35 11.07 21 25967 4200 46655874
Pancytopenia 27.00 11.07 7 25981 85051 46575023
Feeling abnormal 26.83 11.07 139 25849 124921 46535153
Disturbance in attention 26.52 11.07 56 25932 31504 46628570
Heart rate 26.39 11.07 6 25982 43 46660031
Hypersomnia 25.62 11.07 37 25951 15402 46644672
Urinary incontinence 25.58 11.07 52 25936 28478 46631596
Muscular weakness 25.47 11.07 110 25878 91734 46568340
Insomnia 25.44 11.07 168 25820 164756 46495318
Central nervous system lesion 25.37 11.07 29 25959 9586 46650488
Hypnagogic hallucination 24.76 11.07 7 25981 129 46659945
Tremor 24.43 11.07 128 25860 115511 46544563
Substance use 23.78 11.07 9 25979 426 46659648
Synovitis 23.73 11.07 3 25985 61072 46599002
Malignant neoplasm progression 23.36 11.07 4 25984 64922 46595152
Diarrhoea 23.13 11.07 200 25788 559402 46100672
Bipolar disorder 23.03 11.07 24 25964 7153 46652921
Hypnopompic hallucination 22.90 11.07 5 25983 29 46660045
Hallucination, auditory 22.75 11.07 29 25959 10727 46649347
Mania 22.56 11.07 29 25959 10817 46649257
Feeling drunk 22.30 11.07 18 25970 3869 46656205
Abnormal dreams 22.19 11.07 28 25960 10251 46649823
Enterococcal sepsis 22.09 11.07 12 25976 1328 46658746
Pneumonia 21.67 11.07 122 25866 376198 46283876
Irritability 21.63 11.07 49 25939 28897 46631177
Anaemia 21.38 11.07 72 25916 255707 46404367
Cardiac failure 21.14 11.07 9 25979 79939 46580135
Platelet count decreased 21.04 11.07 15 25973 100009 46560065
Restless legs syndrome 20.71 11.07 34 25954 15809 46644265
Panic attack 20.71 11.07 39 25949 20203 46639871
Optic neuritis 20.32 11.07 22 25966 6849 46653225
Renal impairment 20.27 11.07 8 25980 74364 46585710
Paranoia 19.98 11.07 27 25961 10570 46649504
General physical health deterioration 18.83 11.07 22 25966 115747 46544327
Injection site scar 18.72 11.07 9 25979 771 46659303
Progressive multifocal leukoencephalopathy 18.55 11.07 27 25961 11319 46648755
Illness 18.42 11.07 28 25960 12196 46647878
Dysstasia 18.02 11.07 34 25954 17634 46642440
Infusion related reaction 17.83 11.07 18 25970 101190 46558884
Cognitive disorder 17.81 11.07 53 25935 36830 46623244
Blood pressure increased 17.72 11.07 126 25862 126540 46533534
Lymphocyte count decreased 17.67 11.07 42 25946 25547 46634527
White blood cells urine positive 17.45 11.07 16 25972 4084 46655990
Paraesthesia 17.12 11.07 118 25870 117319 46542755
Blood pressure measurement 17.06 11.07 6 25982 230 46659844
Postural orthostatic tachycardia syndrome 17.04 11.07 8 25980 650 46659424
Vision blurred 16.67 11.07 88 25900 79620 46580454
International normalised ratio increased 16.62 11.07 3 25985 46880 46613194
Amnesia 16.61 11.07 56 25932 41575 46618499
Haemoglobin decreased 16.53 11.07 29 25959 128920 46531154
Depersonalisation/derealisation disorder 16.52 11.07 9 25979 1001 46659073
Surgery 16.49 11.07 44 25944 28741 46631333
Coordination abnormal 16.39 11.07 25 25963 10924 46649150
Muscle spasms 16.37 11.07 121 25867 122992 46537082
Disease progression 16.35 11.07 16 25972 91284 46568790
Hunger 16.25 11.07 15 25973 3860 46656214
Endometriosis 16.14 11.07 15 25973 3895 46656179
Abnormal sleep-related event 16.07 11.07 8 25980 739 46659335
Product use in unapproved indication 15.96 11.07 16 25972 90257 46569817
Abdominal pain 15.84 11.07 70 25918 229961 46430113
Plasma cell myeloma 15.44 11.07 3 25985 44475 46615599
Dyskinesia 15.35 11.07 43 25945 28882 46631192
Oedema mouth 15.08 11.07 12 25976 2529 46657545
Crying 14.93 11.07 35 25953 21106 46638968
Hypertension 14.91 11.07 171 25817 196185 46463889
Weight decreased 14.85 11.07 181 25807 210668 46449406
Sleep-related eating disorder 14.43 11.07 7 25981 612 46659462
Headache 14.11 11.07 357 25631 477995 46182079
Rash 13.98 11.07 129 25859 356383 46303691
Loss of consciousness 13.61 11.07 105 25883 108133 46551941
Peripheral swelling 13.53 11.07 44 25944 158027 46502047
Urine analysis abnormal 13.43 11.07 14 25974 4176 46655898
C-reactive protein increased 13.38 11.07 8 25980 58582 46601492
Lower respiratory tract infection 13.34 11.07 7 25981 55082 46604992
Movement disorder 13.12 11.07 29 25959 16820 46643254
Drug ineffective 13.09 11.07 283 25705 677555 45982519
Urine leukocyte esterase positive 13.00 11.07 11 25977 2524 46657550
Seasonal affective disorder 12.97 11.07 5 25983 249 46659825
Urinary tract infection 12.97 11.07 183 25805 220083 46439991
Completed suicide 12.93 11.07 40 25948 145880 46514194
Lymphopenia 12.68 11.07 27 25961 15266 46644808
CD4 lymphocytes decreased 12.66 11.07 9 25979 1601 46658473
Drug tolerance 12.62 11.07 12 25976 3206 46656868
T-lymphocyte count increased 12.57 11.07 4 25984 112 46659962
Incoherent 12.57 11.07 14 25974 4498 46655576
Major depression 12.54 11.07 17 25971 6673 46653401
Intervertebral disc protrusion 12.51 11.07 32 25956 20373 46639701
Hypotension 12.51 11.07 77 25911 232512 46427562
Injection site reaction 12.27 11.07 56 25932 47793 46612281
Laboratory test abnormal 12.16 11.07 34 25954 22813 46637261
Dyspnoea 12.15 11.07 208 25780 515340 46144734
Urinary sediment 12.05 11.07 3 25985 33 46660041
Post-traumatic stress disorder 12.04 11.07 13 25975 4035 46656039
Hangover 11.98 11.07 8 25980 1287 46658787
Toxicity to various agents 11.97 11.07 69 25919 211697 46448377
Hysterectomy 11.93 11.07 18 25970 7788 46652286
Hyponatraemia 11.92 11.07 24 25964 101308 46558766
Cardiac arrest 11.89 11.07 20 25968 90379 46569695
Asthma exercise induced 11.83 11.07 4 25984 136 46659938
Septic shock 11.76 11.07 9 25979 57884 46602190
Renal failure 11.65 11.07 29 25959 113565 46546509
Loss of control of legs 11.49 11.07 8 25980 1376 46658698
Product use issue 11.49 11.07 22 25966 94622 46565452
Delusion of grandeur 11.46 11.07 4 25984 150 46659924
Transient acantholytic dermatosis 11.45 11.07 3 25985 41 46660033
Uterine leiomyoma 11.43 11.07 18 25970 8081 46651993
Cervical spinal stenosis 11.19 11.07 9 25979 1926 46658148

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
Cataplexy 162.79 14.92 35 9892 338 29942213
Sleep apnoea syndrome 128.22 14.92 76 9851 16781 29925770
Multiple sclerosis relapse 98.69 14.92 55 9872 10807 29931744
Pre-existing condition improved 77.50 14.92 28 9899 1973 29940578
Depression 67.28 14.92 113 9814 90324 29852227
Anxiety 63.82 14.92 110 9817 89761 29852790
Multiple sclerosis 58.47 14.92 34 9893 7233 29935318
Suicidal ideation 53.73 14.92 63 9864 36051 29906500
Somnolence 53.07 14.92 106 9821 96657 29845894
Therapeutic response unexpected 49.67 14.92 33 9894 8870 29933681
Narcolepsy 49.32 14.92 14 9913 450 29942101
Sleep paralysis 48.52 14.92 11 9916 138 29942413
Tic 48.51 14.92 20 9907 2012 29940539
Obsessive-compulsive disorder 46.07 14.92 24 9903 4117 29938434
Cognitive disorder 43.25 14.92 46 9881 23644 29918907
Memory impairment 41.21 14.92 56 9871 37118 29905433
Foetal malnutrition 33.95 14.92 7 9920 54 29942497
Bipolar disorder 33.95 14.92 19 9908 3757 29938794
Delusion 32.65 14.92 29 9898 11960 29930591
Tourette's disorder 31.32 14.92 7 9920 82 29942469
Acute kidney injury 31.23 14.92 27 9900 273815 29668736
Psychotic disorder 31.10 14.92 37 9890 21478 29921073
Insomnia 29.99 14.92 83 9844 93253 29849298
Mania 28.69 14.92 24 9903 9130 29933421
Irritability 27.49 14.92 36 9891 23014 29919537
Migraine 27.11 14.92 27 9900 12847 29929704
Anaemia 26.90 14.92 18 9909 207974 29734577
Condition aggravated 26.58 14.92 103 9824 137763 29804788
Concussion 26.03 14.92 13 9914 2041 29940510
Wrong dose 25.90 14.92 8 9919 346 29942205
Somnambulism 25.75 14.92 15 9912 3199 29939352
Foetal hypokinesia 25.40 14.92 8 9919 369 29942182
Paranoia 24.53 14.92 23 9904 10165 29932386
Gait disturbance 24.51 14.92 67 9860 74710 29867841
Abnormal sleep-related event 22.97 14.92 8 9919 506 29942045
Headache 22.94 14.92 120 9807 182186 29760365
Psychotic symptom 22.74 14.92 10 9917 1179 29941372
Post concussion syndrome 22.66 14.92 5 9922 55 29942496
Road traffic accident 22.46 14.92 28 9899 17043 29925508
Fall 21.71 14.92 118 9809 181754 29760797
Renal failure 21.40 14.92 8 9919 128958 29813593
Fatigue 21.40 14.92 180 9747 320493 29622058
Neutropenia 21.28 14.92 8 9919 128532 29814019
Feeling abnormal 20.77 14.92 53 9874 56703 29885848
Post-traumatic stress disorder 19.82 14.92 10 9917 1605 29940946
Aggression 19.66 14.92 40 9887 36867 29905684
Hypnagogic hallucination 19.50 14.92 4 9923 30 29942521
Thrombocytopenia 18.88 14.92 11 9916 137033 29805518
Trismus 18.85 14.92 11 9916 2354 29940197
Urinary tract infection 18.43 14.92 60 9867 73599 29868952
Magical thinking 17.74 14.92 3 9924 6 29942545
Schizotypal personality disorder 17.74 14.92 3 9924 6 29942545
Secondary progressive multiple sclerosis 17.45 14.92 6 9921 365 29942186
Congenital torticollis 17.14 14.92 3 9924 8 29942543
Death 17.12 14.92 61 9866 357222 29585329
Disturbance in attention 16.87 14.92 28 9899 22101 29920450
Pulmonary hypoplasia 16.57 14.92 6 9921 425 29942126
Influenza like illness 16.39 14.92 30 9897 25575 29916976
Rib hypoplasia 16.21 14.92 3 9924 12 29942539
Hallucination, auditory 16.10 14.92 18 9909 9771 29932780
Antiphospholipid antibodies 15.67 14.92 3 9924 15 29942536
Abnormal dreams 15.23 14.92 16 9911 8099 29934452
Hypotension 15.23 14.92 27 9900 200538 29742013
Muscle spasticity 15.02 14.92 13 9914 5175 29937376

Pharmacologic Action:

SourceCodeDescription
ATC N06BA07 NERVOUS SYSTEM
PSYCHOANALEPTICS
PSYCHOSTIMULANTS, AGENTS USED FOR ADHD AND NOOTROPICS
Centrally acting sympathomimetics
FDA PE N0000175651 Increased Sympathetic Activity
FDA PE N0000175729 Central Nervous System Stimulation
FDA EPC N0000175769 Sympathomimetic-like Agent
MeSH PA D002491 Central Nervous System Agents
MeSH PA D000697 Central Nervous System Stimulants
MeSH PA D065701 Cytochrome P-450 CYP3A Inducers
MeSH PA D065606 Metabolic Side Effects of Drugs and Substances
MeSH PA D064690 Wakefulness-Promoting Agents
CHEBI has role CHEBI:35337 analeptic drug
CHEBI has role CHEBI:77567 wake-promoting drug

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Narcolepsy indication 60380001 DOID:8986
Hypersomnia indication 77692006
Sleepiness Due To Obstructive Sleep Apnea indication
Sleepiness Due To Shift Work Sleep Disorder indication
Suicidal thoughts contraindication 6471006
Alcoholism contraindication 7200002
Myocardial infarction contraindication 22298006 DOID:5844
Depressive disorder contraindication 35489007
Hypertensive disorder contraindication 38341003 DOID:10763
Left ventricular hypertrophy contraindication 55827005
Acute nephropathy contraindication 58574008
Hepatic failure contraindication 59927004
Aggressive behavior contraindication 61372001
Psychotic disorder contraindication 69322001
Mania contraindication 231494001
Acute coronary syndrome contraindication 394659003
Mitral valve prolapse contraindication 409712001
Myocardial ischemia contraindication 414795007 DOID:3393

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 12.23 acidic

Orange Book patent data (new drug applications)

None

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 5.84 DRUG MATRIX CHEMBL
Cytochrome P450 2C19 Enzyme WOMBAT-PK
Cytochrome P450 1A2 Enzyme Ki 4.40 WOMBAT-PK
Alpha-1B adrenergic receptor GPCR WOMBAT-PK
D(2) dopamine receptor GPCR EC50 6.62 WOMBAT-PK
Sodium-dependent dopamine transporter Transporter Ki 5.60 CHEMBL
Transporter Transporter IC50 4.19 CHEMBL

External reference:

IDSource
4021149 VUID
N0000148602 NUI
D01832 KEGG_DRUG
4021149 VANDF
C0066677 UMLSCUI
CHEBI:31859 CHEBI
CHEMBL1373 ChEMBL_ID
D000077408 MESH_DESCRIPTOR_UI
DB00745 DRUGBANK_ID
7555 IUPHAR_LIGAND_ID
6055 INN_ID
R3UK8X3U3D UNII
4236 PUBCHEM_CID
30125 RXNORM
52652 MMSL
7873 MMSL
d04378 MMSL
005305 NDDF
116082007 SNOMEDCT_US
387004007 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Modafinil HUMAN PRESCRIPTION DRUG LABEL 1 0591-3499 TABLET 100 mg ORAL ANDA 30 sections
Modafinil HUMAN PRESCRIPTION DRUG LABEL 1 0591-3500 TABLET 200 mg ORAL ANDA 30 sections
Modafinil HUMAN PRESCRIPTION DRUG LABEL 1 0904-6423 TABLET 100 mg ORAL ANDA 29 sections
Modafinil HUMAN PRESCRIPTION DRUG LABEL 1 0904-6424 TABLET 200 mg ORAL ANDA 29 sections
Modafinil HUMAN PRESCRIPTION DRUG LABEL 1 0904-6791 TABLET 100 mg ORAL ANDA 19 sections
Modafinil HUMAN PRESCRIPTION DRUG LABEL 1 0904-6792 TABLET 200 mg ORAL ANDA 19 sections
PROVIGIL HUMAN PRESCRIPTION DRUG LABEL 1 21695-234 TABLET 100 mg ORAL NDA 25 sections
PROVIGIL HUMAN PRESCRIPTION DRUG LABEL 1 21695-235 TABLET 200 mg ORAL NDA 25 sections
Modafinil Human Prescription Drug Label 1 23155-604 TABLET 100 mg ORAL ANDA 24 sections
Modafinil Human Prescription Drug Label 1 23155-605 TABLET 200 mg ORAL ANDA 24 sections
Modafinil HUMAN PRESCRIPTION DRUG LABEL 1 42043-160 TABLET 100 mg ORAL ANDA 29 sections
Modafinil HUMAN PRESCRIPTION DRUG LABEL 1 42043-161 TABLET 200 mg ORAL ANDA 29 sections
Modafinil HUMAN PRESCRIPTION DRUG LABEL 1 42291-599 TABLET 100 mg ORAL ANDA 30 sections
Modafinil HUMAN PRESCRIPTION DRUG LABEL 1 42291-600 TABLET 200 mg ORAL ANDA 30 sections
MODAFINIL HUMAN PRESCRIPTION DRUG LABEL 1 42549-678 TABLET 200 mg ORAL NDA authorized generic 25 sections
Modafinil HUMAN PRESCRIPTION DRUG LABEL 1 43353-831 TABLET 200 mg ORAL ANDA 28 sections
modafinil HUMAN PRESCRIPTION DRUG LABEL 1 43353-925 TABLET 200 mg ORAL NDA authorized generic 25 sections
Modafinil HUMAN PRESCRIPTION DRUG LABEL 1 43353-956 TABLET 200 mg ORAL NDA authorized generic 28 sections
Modafinil Human Prescription Drug Label 1 46708-385 TABLET 100 mg ORAL ANDA 29 sections
Modafinil Human Prescription Drug Label 1 46708-386 TABLET 200 mg ORAL ANDA 29 sections
Modafinil Human Prescription Drug Label 1 50090-2472 TABLET 100 mg ORAL ANDA 29 sections
Modafinil Human Prescription Drug Label 1 50090-2473 TABLET 200 mg ORAL ANDA 29 sections
Modafinil HUMAN PRESCRIPTION DRUG LABEL 1 50090-3865 TABLET 100 mg ORAL ANDA 29 sections
Modafinil HUMAN PRESCRIPTION DRUG LABEL 1 50090-4144 TABLET 200 mg ORAL ANDA 19 sections
Modafinil HUMAN PRESCRIPTION DRUG LABEL 1 50268-570 TABLET 100 mg ORAL ANDA 29 sections
Modafinil HUMAN PRESCRIPTION DRUG LABEL 1 50268-571 TABLET 200 mg ORAL ANDA 29 sections
PROVIGIL HUMAN PRESCRIPTION DRUG LABEL 1 54868-4492 TABLET 100 mg ORAL NDA 25 sections
PROVIGIL HUMAN PRESCRIPTION DRUG LABEL 1 54868-4897 TABLET 200 mg ORAL NDA 25 sections
Modafinil HUMAN PRESCRIPTION DRUG LABEL 1 55253-801 TABLET 100 mg ORAL NDA AUTHORIZED GENERIC 29 sections
Modafinil HUMAN PRESCRIPTION DRUG LABEL 1 55253-802 TABLET 200 mg ORAL NDA AUTHORIZED GENERIC 29 sections