modafinil indications/contra

Stem definitionDrug idCAS RN
1826 68693-11-8

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • modafinil
  • (+/-)-Modafinil
  • modaphonil
  • modiodal
metabolite of adrafinyl; armodafinil is the (R)-isomer
  • Molecular weight: 273.35
  • Formula: C15H15NO2S
  • CLOGP: 0.94
  • LIPINSKI: 0
  • HAC: 3
  • HDO: 1
  • TPSA: 60.16
  • ALOGS: -2.64
  • ROTB: 5

Drug dosage:

DoseUnitRoute
0.30 g O

Approvals:

DateAgencyCompanyOrphan
Dec. 24, 1998 FDA CEPHALON

FDA Adverse Event Reporting System

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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 166.69 26.98 67 1457 32137 3352198
Drug interaction 161.46 26.98 73 1451 46739 3337596
Completed suicide 158.46 26.98 64 1460 31050 3353285
Mania 155.21 26.98 39 1485 4039 3380296
Anxiety 133.93 26.98 61 1463 39568 3344767
Headache 122.66 26.98 76 1448 91904 3292431
Cataplexy 119.21 26.98 20 1504 265 3384070
Fatigue 114.38 26.98 77 1447 107163 3277172
Insomnia 114.12 26.98 53 1471 35845 3348490
Drug ineffective 111.19 26.98 78 1446 116012 3268323
Depression 108.94 26.98 53 1471 39717 3344618
Psychotic disorder 105.04 26.98 34 1490 8700 3375635
Irritability 104.42 26.98 36 1488 11180 3373155
Nausea 98.99 26.98 76 1448 129569 3254766
Paranoia 98.98 26.98 27 1497 3832 3380503
Seizure 96.28 26.98 49 1475 40351 3343984
Suicide attempt 95.84 26.98 37 1487 15810 3368525
Toxicity to various agents 86.48 26.98 48 1476 47006 3337329
Agitation 84.69 26.98 36 1488 19670 3364665
Aggression 81.18 26.98 30 1494 11355 3372980
Suicidal ideation 78.24 26.98 33 1491 17672 3366663
Off label use 77.74 26.98 47 1477 53930 3330405
Hypersensitivity vasculitis 74.93 26.98 19 1505 2028 3382307
Rash 73.13 26.98 50 1474 70771 3313564
Drug hypersensitivity 72.69 26.98 39 1485 35641 3348694
Condition aggravated 71.95 26.98 40 1484 39193 3345142
Stevens-Johnson syndrome 71.85 26.98 24 1500 6748 3377587
Drug prescribing error 69.87 26.98 21 1503 4199 3380136
Nervousness 65.80 26.98 22 1502 6202 3378133
Hypertension 64.51 26.98 37 1487 38429 3345906

Pharmacologic Action:

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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)

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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 DOID:2848
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 DOID:988
Myocardial ischemia contraindication 414795007 DOID:3393

Acid dissociation constants calculated using MoKa v3.0.0

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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:

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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:

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IDSource
4021149 VUID
N0000148602 NUI
C0066677 UMLSCUI
7555 IUPHAR_LIGAND_ID
D01832 KEGG_DRUG
DB00745 DRUGBANK_ID
4236 PUBCHEM_CID
4021149 VANDF
N0000148602 NDFRT
N0000005978 NDFRT
005305 NDDF
d04378 MMSL
7873 MMSL
30125 RXNORM
116082007 SNOMEDCT_US
387004007 SNOMEDCT_US
52652 MMSL
CHEMBL1373 ChEMBL_ID
CHEBI:31859 CHEBI
R3UK8X3U3D UNII
6055 INN_ID
C048833 MESH_SUPPLEMENTAL_RECORD_UI

Pharmaceutical products:

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ProductCategoryIngredientsNDCFormQuantityRoute MarketingLabel
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
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
PROVIGIL HUMAN PRESCRIPTION DRUG LABEL 1 35356-372 TABLET 200 mg ORAL NDA 14 sections
Modafinil HUMAN PRESCRIPTION DRUG LABEL 1 42043-160 TABLET 100 mg ORAL ANDA 18 sections
Modafinil HUMAN PRESCRIPTION DRUG LABEL 1 42043-161 TABLET 200 mg ORAL ANDA 18 sections
Modafinil HUMAN PRESCRIPTION DRUG LABEL 1 42291-599 TABLET 100 mg ORAL ANDA 15 sections
Modafinil HUMAN PRESCRIPTION DRUG LABEL 1 42291-600 TABLET 200 mg ORAL ANDA 15 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 50268-570 TABLET 100 mg ORAL ANDA 18 sections
Modafinil HUMAN PRESCRIPTION DRUG LABEL 1 50268-571 TABLET 200 mg ORAL ANDA 18 sections
Provigil HUMAN PRESCRIPTION DRUG LABEL 1 50436-0201 TABLET 200 mg ORAL NDA 18 sections
Modafinil HUMAN PRESCRIPTION DRUG LABEL 1 50742-152 TABLET 100 mg ORAL ANDA 18 sections
Modafinil HUMAN PRESCRIPTION DRUG LABEL 1 50742-153 TABLET 200 mg ORAL ANDA 18 sections