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

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
Somnolence 162.41 27.19 58 937 23427 2333663
Drug interaction 135.96 27.19 54 941 29109 2327981
Cataplexy 129.20 27.19 20 975 180 2356910
Drug ineffective 111.04 27.19 70 925 101554 2255536
Headache 107.41 27.19 63 932 80116 2276974
Anxiety 104.87 27.19 45 950 29314 2327776
Suicide attempt 101.43 27.19 34 961 11248 2345842
Toxicity to various agents 90.63 27.19 42 953 32712 2324378
Insomnia 90.28 27.19 39 956 25748 2331342
Psychotic disorder 88.58 27.19 25 970 4654 2352436
Palpitations 85.30 27.19 33 962 16423 2340667
Depression 83.82 27.19 38 957 28094 2328996
Nausea 83.39 27.19 61 934 112128 2244962
Fatigue 81.35 27.19 54 941 84819 2272271
Hypersensitivity vasculitis 80.71 27.19 18 977 1284 2355806
Drug hypersensitivity 76.56 27.19 42 953 46601 2310489
Suicidal ideation 74.82 27.19 27 968 11060 2346030
Completed suicide 74.15 27.19 32 963 21002 2336088
Stevens-Johnson syndrome 72.70 27.19 21 974 4238 2352852
Seizure 72.66 27.19 33 962 24433 2332657
Polycystic ovaries 69.99 27.19 12 983 212 2356878
Irritability 68.26 27.19 22 973 6405 2350685
Hallucination, auditory 66.45 27.19 17 978 2175 2354915
Hypertension 66.09 27.19 32 963 27329 2329761
Maternal exposure during pregnancy 63.67 27.19 26 969 14837 2342253
Blood pressure increased 60.32 27.19 26 969 16960 2340130
Confusional state 57.33 27.19 28 967 24316 2332774
Mania 55.16 27.19 15 980 2425 2354665
Delusion 52.83 27.19 14 981 2051 2355039
Product prescribing error 52.29 27.19 15 980 2945 2354145
Narcolepsy 50.82 27.19 9 986 193 2356897
Pregnancy on oral contraceptive 50.39 27.19 10 985 403 2356687
Tremor 49.32 27.19 24 971 20637 2336453
Tachycardia 48.20 27.19 22 973 16387 2340703
Nervousness 47.95 27.19 16 979 5173 2351917
Weight decreased 47.63 27.19 26 969 28345 2328745
Dizziness 45.73 27.19 33 962 58632 2298458
Abnormal behaviour 45.27 27.19 15 980 4745 2352345
Agitation 42.77 27.19 18 977 11033 2346057
Overdose 41.21 27.19 21 974 19886 2337204
Product substitution issue 40.43 27.19 14 981 5055 2352035
Paranoia 38.65 27.19 11 984 2096 2354994
Sleep apnoea syndrome 38.55 27.19 11 984 2115 2354975
Therapeutic product effect decreased 36.56 27.19 16 979 10773 2346317
Feeling abnormal 35.14 27.19 20 975 23561 2333529
Hypersensitivity 35.13 27.19 20 975 23573 2333517
Incorrect dose administered 34.88 27.19 15 980 9680 2347410
Rash 34.28 27.19 28 967 59530 2297560
Premature labour 34.19 27.19 10 985 2096 2354994
Delirium 32.49 27.19 12 983 5211 2351879
Blood potassium decreased 32.30 27.19 12 983 5293 2351797
Euphoric mood 32.13 27.19 8 987 913 2356177
Urticaria 31.96 27.19 19 976 24242 2332848
Condition aggravated 31.94 27.19 21 974 31958 2325132
Tardive dyskinesia 31.72 27.19 9 986 1695 2355395
Exposure during pregnancy 31.28 27.19 19 976 25200 2331890
Rash erythematous 30.91 27.19 12 983 5964 2351126
Heart rate increased 29.80 27.19 14 981 11091 2345999
Galactorrhoea 29.40 27.19 8 987 1291 2355799
Drug withdrawal syndrome 29.37 27.19 12 983 6809 2350281
Amnesia 28.66 27.19 12 983 7241 2349849
Loss of consciousness 28.16 27.19 16 979 18751 2338339

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
Irritability 81.95 33.44 25 645 5507 1740604
Anxiety 80.46 33.44 32 638 15495 1730616
Completed suicide 78.93 33.44 32 638 16280 1729831
Condition aggravated 74.13 33.44 33 637 21117 1724994
Intentional product misuse 70.95 33.44 24 646 7334 1738777
Mania 70.03 33.44 18 652 2115 1743996
Agitation 68.66 33.44 26 644 11000 1735111
Aggression 68.65 33.44 24 646 8091 1738020
Psychotic disorder 62.86 33.44 20 650 5036 1741075
Tic 59.77 33.44 13 657 741 1745370
Psychotic symptom 55.49 33.44 10 660 213 1745898
Somnolence 54.97 33.44 25 645 16714 1729397
Cataplexy 54.41 33.44 9 661 113 1745998
Obsessive-compulsive disorder 53.09 33.44 12 658 816 1745295
Fatigue 51.82 33.44 35 635 50746 1695365
Paranoia 50.63 33.44 14 656 2167 1743944
Toxicity to various agents 47.20 33.44 27 643 29114 1716997
Nausea 46.81 33.44 33 637 51163 1694948
Hallucination, auditory 46.43 33.44 13 657 2104 1744007
Hallucination 46.24 33.44 18 652 8152 1737959
Drug interaction 45.52 33.44 26 644 27932 1718179
Hyperhidrosis 45.24 33.44 20 650 12468 1733643
Headache 43.07 33.44 27 643 34349 1711762
Delusion 41.28 33.44 12 658 2219 1743892
Seizure 38.66 33.44 21 649 20420 1725691
Insomnia 37.24 33.44 19 651 16257 1729854
Confusional state 35.14 33.44 20 650 21258 1724853
Asphyxia 34.82 33.44 9 661 1074 1745037
Cardiac arrest 34.71 33.44 18 652 15912 1730199
Hypertension 34.05 33.44 19 651 19429 1726682
Pulmonary hypoplasia 33.59 33.44 6 664 121 1745990

Pharmacologic Action:

SourceCodeDescription
ATC N06BA07 NERVOUS SYSTEM
PSYCHOANALEPTICS
PSYCHOSTIMULANTS, AGENTS USED FOR ADHD AND NOOTROPICS
Centrally acting sympathomimetics
FDA PE N0000175729 Central Nervous System Stimulation
FDA PE N0000175651 Increased Sympathetic Activity
FDA EPC N0000175769 Sympathomimetic-like Agent
CHEBI has role CHEBI:35337 central nervous system stimulant
CHEBI has role CHEBI:77567 eugeroic
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

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Narcolepsy indication 60380001 DOID:8986
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
D000077408 MESH_DESCRIPTOR_UI
4021149 VUID
N0000148602 NUI
C0066677 UMLSCUI
D01832 KEGG_DRUG
116082007 SNOMEDCT_US
4021149 VANDF
005305 NDDF
d04378 MMSL
7873 MMSL
30125 RXNORM
387004007 SNOMEDCT_US
52652 MMSL
CHEBI:31859 CHEBI
CHEMBL1373 ChEMBL_ID
DB00745 DRUGBANK_ID
R3UK8X3U3D UNII
6055 INN_ID
4236 PUBCHEM_CID
7555 IUPHAR_LIGAND_ID

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Modafinil HUMAN PRESCRIPTION DRUG LABEL 1 0143-9968 TABLET 100 mg ORAL ANDA 18 sections
Modafinil HUMAN PRESCRIPTION DRUG LABEL 1 0143-9969 TABLET 200 mg ORAL ANDA 18 sections
Modafinil HUMAN PRESCRIPTION DRUG LABEL 1 0378-5573 TABLET 100 mg ORAL ANDA 18 sections
Modafinil HUMAN PRESCRIPTION DRUG LABEL 1 0378-5575 TABLET 200 mg ORAL ANDA 18 sections
Modafinil HUMAN PRESCRIPTION DRUG LABEL 1 0591-3499 TABLET 100 mg ORAL ANDA 19 sections
Modafinil HUMAN PRESCRIPTION DRUG LABEL 1 0591-3500 TABLET 200 mg ORAL ANDA 19 sections
Modafinil HUMAN PRESCRIPTION DRUG LABEL 1 0904-6423 TABLET 100 mg ORAL ANDA 19 sections
Modafinil HUMAN PRESCRIPTION DRUG LABEL 1 0904-6424 TABLET 200 mg ORAL ANDA 19 sections
Modafinil HUMAN PRESCRIPTION DRUG LABEL 1 0904-6791 TABLET 100 mg ORAL ANDA 18 sections
Modafinil HUMAN PRESCRIPTION DRUG LABEL 1 0904-6792 TABLET 200 mg ORAL ANDA 18 sections
PROVIGIL HUMAN PRESCRIPTION DRUG LABEL 1 21695-234 TABLET 100 mg ORAL NDA 20 sections
PROVIGIL HUMAN PRESCRIPTION DRUG LABEL 1 21695-235 TABLET 200 mg ORAL NDA 20 sections
Modafinil HUMAN PRESCRIPTION DRUG LABEL 1 23155-604 TABLET 100 mg ORAL ANDA 17 sections
Modafinil HUMAN PRESCRIPTION DRUG LABEL 1 23155-605 TABLET 200 mg ORAL ANDA 17 sections
Modafinil HUMAN PRESCRIPTION DRUG LABEL 1 42043-160 TABLET 100 mg ORAL ANDA 17 sections
Modafinil HUMAN PRESCRIPTION DRUG LABEL 1 42043-161 TABLET 200 mg ORAL ANDA 17 sections
Modafinil HUMAN PRESCRIPTION DRUG LABEL 1 42291-599 TABLET 100 mg ORAL ANDA 19 sections
Modafinil HUMAN PRESCRIPTION DRUG LABEL 1 42291-600 TABLET 200 mg ORAL ANDA 19 sections
MODAFINIL HUMAN PRESCRIPTION DRUG LABEL 1 42549-678 TABLET 200 mg ORAL NDA authorized generic 15 sections
Modafinil HUMAN PRESCRIPTION DRUG LABEL 1 43353-831 TABLET 200 mg ORAL ANDA 14 sections
modafinil HUMAN PRESCRIPTION DRUG LABEL 1 43353-925 TABLET 200 mg ORAL NDA authorized generic 15 sections
Modafinil HUMAN PRESCRIPTION DRUG LABEL 1 43353-956 TABLET 200 mg ORAL NDA authorized generic 18 sections
Modafinil HUMAN PRESCRIPTION DRUG LABEL 1 46708-385 TABLET 100 mg ORAL ANDA 18 sections
Modafinil HUMAN PRESCRIPTION DRUG LABEL 1 46708-386 TABLET 200 mg ORAL ANDA 18 sections
Modafinil HUMAN PRESCRIPTION DRUG LABEL 1 49884-534 TABLET 100 mg ORAL NDA AUTHORIZED GENERIC 18 sections
Modafinil HUMAN PRESCRIPTION DRUG LABEL 1 49884-535 TABLET 200 mg ORAL NDA AUTHORIZED GENERIC 18 sections
Modafinil HUMAN PRESCRIPTION DRUG LABEL 1 50090-2472 TABLET 100 mg ORAL ANDA 18 sections
Modafinil HUMAN PRESCRIPTION DRUG LABEL 1 50090-2473 TABLET 200 mg ORAL ANDA 18 sections
Modafinil HUMAN PRESCRIPTION DRUG LABEL 1 50090-3865 TABLET 100 mg ORAL ANDA 19 sections
Modafinil HUMAN PRESCRIPTION DRUG LABEL 1 50090-4144 TABLET 200 mg ORAL ANDA 18 sections