dexmethylphenidate 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
836 40431-64-9

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • focalin
  • dexmethylphenidate
  • Methyl D-phenidate
  • d-threo-Methylphenidate
  • dexmethylphenidate hydrochloride
  • dexmethylphenidate HCl
A methylphenidate derivative, DOPAMINE UPTAKE INHIBITOR and CENTRAL NERVOUS SYSTEM STIMULANT that is used in the treatment of ATTENTION DEFICIT HYPERACTIVITY DISORDER.
  • Molecular weight: 233.31
  • Formula: C14H19NO2
  • CLOGP: 2.56
  • LIPINSKI: 0
  • HAC: 3
  • HDO: 1
  • TPSA: 38.33
  • ALOGS: -3.11
  • ROTB: 4
  • Status: OFP
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
15 mg O

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 1 Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine) 0.50 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 1.06 µM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
Vd (Volume of distribution) 2.65 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 6.67 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.87 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 8 hours Lombardo F, Berellini G, Obach RS

Approvals:

DateAgencyCompanyOrphan
Nov. 13, 2001 FDA NOVARTIS

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
Claustrophobia 94.80 34.48 18 2127 1000 63485877
Product tampering 89.59 34.48 15 2130 403 63486474
Adulterated product 89.40 34.48 14 2131 244 63486633
Pulse abnormal 79.67 34.48 18 2127 2346 63484531
Somatic symptom disorder 77.56 34.48 18 2127 2642 63484235
Mood swings 68.32 34.48 25 2120 18223 63468654
Neurological symptom 63.69 34.48 18 2127 5765 63481112
Hyperreflexia 63.23 34.48 18 2127 5916 63480961
Brain injury 60.18 34.48 18 2127 7025 63479852
Disturbance in attention 59.62 34.48 28 2117 38161 63448716
Paranoia 59.00 34.48 20 2125 11659 63475218
Suicidal ideation 57.34 34.48 32 2113 62389 63424488
Amenorrhoea 54.12 34.48 18 2127 9896 63476981
Withdrawal syndrome 48.52 34.48 20 2125 19977 63466900
Hypertensive crisis 46.51 34.48 18 2127 15268 63471609
Product substitution issue 45.72 34.48 18 2127 15978 63470899
Feeling abnormal 40.21 34.48 36 2109 148356 63338521
Intentional product misuse 37.12 34.48 24 2121 60893 63425984

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
Product substitution issue 223.77 34.95 63 2294 10032 34944542
Abnormal behaviour 175.02 34.95 65 2292 24904 34929670
Drug ineffective 110.11 34.95 143 2214 456608 34497966
Anger 83.32 34.95 31 2326 11853 34942721
Aggression 80.17 34.95 43 2314 38921 34915653
Tic 64.94 34.95 17 2340 2041 34952533
Disturbance in attention 60.05 34.95 31 2326 25914 34928660
Irritability 58.58 34.95 30 2327 24660 34929914
Brugada syndrome 58.38 34.95 13 2344 788 34953786
Attention deficit hyperactivity disorder 56.70 34.95 16 2341 2543 34952031
Psychomotor hyperactivity 56.27 34.95 22 2335 9600 34944974
Agitation 55.23 34.95 39 2318 57360 34897214
Product quality issue 44.20 34.95 22 2335 17013 34937561
Crying 43.66 34.95 16 2341 5846 34948728
Suicidal ideation 40.11 34.95 28 2329 40360 34914214
Anxiety 38.39 34.95 40 2317 99388 34855186
Emotional disorder 36.72 34.95 14 2343 5702 34948872

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
Product substitution issue 231.82 33.47 68 3263 20188 79720869
Abnormal behaviour 92.52 33.47 40 3291 36381 79704676
Claustrophobia 86.99 33.47 18 3313 1252 79739805
Product tampering 86.04 33.47 15 3316 413 79740644
Disturbance in attention 85.75 33.47 42 3289 50759 79690298
Adulterated product 84.59 33.47 14 3317 280 79740777
Anger 79.14 33.47 29 3302 17133 79723924
Somatic symptom disorder 74.58 33.47 18 3313 2519 79738538
Tic 71.67 33.47 18 3313 2968 79738089
Pulse abnormal 69.43 33.47 18 3313 3366 79737691
Mood swings 67.94 33.47 27 3304 19853 79721204
Suicidal ideation 62.04 33.47 39 3292 76301 79664756
Aggression 59.73 33.47 33 3298 50925 79690132
Brugada syndrome 58.93 33.47 13 3318 1225 79739832
Neurological symptom 56.42 33.47 19 3312 8764 79732293
Amenorrhoea 54.83 33.47 18 3313 7674 79733383
Irritability 54.78 33.47 29 3302 41115 79699942
Withdrawal syndrome 53.81 33.47 25 3306 26829 79714228
Hyperreflexia 53.31 33.47 18 3313 8367 79732690
Paranoia 51.47 33.47 22 3309 19410 79721647
Brain injury 47.73 33.47 18 3313 11499 79729558
Agitation 39.59 33.47 33 3298 99682 79641375
Hypertensive crisis 37.50 33.47 18 3313 20752 79720305
Educational problem 35.05 33.47 7 3324 407 79740650
Psychomotor hyperactivity 34.72 33.47 16 3315 16833 79724224

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC N06BA11 NERVOUS SYSTEM
PSYCHOANALEPTICS
PSYCHOSTIMULANTS, AGENTS USED FOR ADHD AND NOOTROPICS
Centrally acting sympathomimetics
ATC N06BA15 NERVOUS SYSTEM
PSYCHOANALEPTICS
PSYCHOSTIMULANTS, AGENTS USED FOR ADHD AND NOOTROPICS
Centrally acting sympathomimetics
FDA PE N0000175729 Central Nervous System Stimulation
FDA EPC N0000175739 Central Nervous System Stimulant
CHEBI has role CHEBI:37962 adrenergic agents
MeSH PA D002491 Central Nervous System Agents
MeSH PA D000697 Central Nervous System Stimulants
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

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

DiseaseRelationSNOMED_IDDOID
Attention deficit hyperactivity disorder indication 406506008
Gilles de la Tourette's syndrome contraindication 5158005 DOID:11119
Dependent drug abuse contraindication 6525002
Alcoholism contraindication 7200002
Sinus tachycardia contraindication 11092001
Bipolar disorder contraindication 13746004 DOID:3312
Myocardial infarction contraindication 22298006 DOID:5844
Glaucoma contraindication 23986001 DOID:1686
Feeling agitated contraindication 24199005
Hypertensive disorder contraindication 38341003 DOID:10763
Chronic heart failure contraindication 48447003
Tension contraindication 53489000
Aggressive behavior contraindication 61372001
Psychotic disorder contraindication 69322001
Severe anxiety (panic) contraindication 80583007
Leukopenia contraindication 84828003 DOID:615
Cardiomyopathy contraindication 85898001 DOID:0050700
Structural disorder of heart contraindication 128599005
Seizure disorder contraindication 128613002
Motor tic disorder contraindication 230337001
Cerebrovascular accident contraindication 230690007
Mania contraindication 231494001
Anemia contraindication 271737000 DOID:2355
Thrombocytopenic disorder contraindication 302215000 DOID:1588
Visual impairment contraindication 397540003
Disorder of coronary artery contraindication 414024009
Life-Threatening Cardiac Arrhythmias contraindication




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 8.68 Basic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
EQ 10.4MG BASE;EQ 52.3MG BASE AZSTARYS COMMAVE THERAP N212994 May 7, 2021 RX CAPSULE ORAL 10858341 Dec. 9, 2037 TREATMENT OF ATTENTION-DEFICIT HYPERACTIVITY DISORDER (ADHD) WITH SERDEXMETHYLPHENIDATE AND DEXMETHYLPHENIDATE
EQ 10.4MG BASE;EQ 52.3MG BASE AZSTARYS COMMAVE THERAP N212994 May 7, 2021 RX CAPSULE ORAL 10954213 Dec. 9, 2037 TREATMENT OF ATTENTION-DEFICIT HYPERACTIVITY DISORDER (ADHD) WITH SERDEXMETHYLPHENIDATE AND DEXMETHYLPHENIDATE
EQ 5.2MG BASE;EQ 26.1MG BASE AZSTARYS COMMAVE THERAP N212994 May 7, 2021 RX CAPSULE ORAL 10858341 Dec. 9, 2037 TREATMENT OF ATTENTION-DEFICIT HYPERACTIVITY DISORDER (ADHD) WITH SERDEXMETHYLPHENIDATE AND DEXMETHYLPHENIDATE
EQ 5.2MG BASE;EQ 26.1MG BASE AZSTARYS COMMAVE THERAP N212994 May 7, 2021 RX CAPSULE ORAL 10954213 Dec. 9, 2037 TREATMENT OF ATTENTION-DEFICIT HYPERACTIVITY DISORDER (ADHD) WITH SERDEXMETHYLPHENIDATE AND DEXMETHYLPHENIDATE
EQ 7.8MG BASE;EQ 39.2MG BASE AZSTARYS COMMAVE THERAP N212994 May 7, 2021 RX CAPSULE ORAL 10858341 Dec. 9, 2037 TREATMENT OF ATTENTION-DEFICIT HYPERACTIVITY DISORDER (ADHD) WITH SERDEXMETHYLPHENIDATE AND DEXMETHYLPHENIDATE
EQ 7.8MG BASE;EQ 39.2MG BASE AZSTARYS COMMAVE THERAP N212994 May 7, 2021 RX CAPSULE ORAL 10954213 Dec. 9, 2037 TREATMENT OF ATTENTION-DEFICIT HYPERACTIVITY DISORDER (ADHD) WITH SERDEXMETHYLPHENIDATE AND DEXMETHYLPHENIDATE

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
EQ 10.4MG BASE;EQ 52.3MG BASE AZSTARYS COMMAVE THERAP N212994 May 7, 2021 RX CAPSULE ORAL May 7, 2026 NEW CHEMICAL ENTITY
EQ 5.2MG BASE;EQ 26.1MG BASE AZSTARYS COMMAVE THERAP N212994 May 7, 2021 RX CAPSULE ORAL May 7, 2026 NEW CHEMICAL ENTITY
EQ 7.8MG BASE;EQ 39.2MG BASE AZSTARYS COMMAVE THERAP N212994 May 7, 2021 RX CAPSULE ORAL May 7, 2026 NEW CHEMICAL ENTITY

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
Sodium-dependent noradrenaline transporter Transporter INHIBITOR WOMBAT-PK CHEMBL
Sodium-dependent dopamine transporter Transporter INHIBITOR Ki 7.80 CHEMBL CHEMBL
Sodium-dependent dopamine transporter Transporter Ki 7.13 CHEMBL
Transporter Transporter Ki 6.57 CHEMBL
Dopamine receptor GPCR IC50 7.08 CHEMBL

External reference:

IDSource
D03721 KEGG_DRUG
19262-68-1 SECONDARY_CAS_RN
352372 RXNORM
4021285 VANDF
4028927 VANDF
C1169997 UMLSCUI
CHEBI:51860 CHEBI
CHEMBL827 ChEMBL_ID
DB06701 DRUGBANK_ID
CHEMBL904 ChEMBL_ID
D064699 MESH_DESCRIPTOR_UI
154101 PUBCHEM_CID
7554 IUPHAR_LIGAND_ID
8289 INN_ID
M32RH9MFGP UNII
110936 MMSL
16208 MMSL
39360 MMSL
42461 MMSL
d04777 MMSL
009511 NDDF
009512 NDDF
385555005 SNOMEDCT_US
767702004 SNOMEDCT_US
767715008 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Focalin HUMAN PRESCRIPTION DRUG LABEL 1 0078-0380 TABLET 2.50 mg ORAL NDA 33 sections
Focalin HUMAN PRESCRIPTION DRUG LABEL 1 0078-0380 TABLET 2.50 mg ORAL NDA 33 sections
Focalin HUMAN PRESCRIPTION DRUG LABEL 1 0078-0380 TABLET 2.50 mg ORAL NDA 33 sections
Focalin HUMAN PRESCRIPTION DRUG LABEL 1 0078-0380 TABLET 2.50 mg ORAL NDA 33 sections
Focalin HUMAN PRESCRIPTION DRUG LABEL 1 0078-0381 TABLET 5 mg ORAL NDA 33 sections
Focalin HUMAN PRESCRIPTION DRUG LABEL 1 0078-0381 TABLET 5 mg ORAL NDA 33 sections
Focalin HUMAN PRESCRIPTION DRUG LABEL 1 0078-0381 TABLET 5 mg ORAL NDA 33 sections
Focalin HUMAN PRESCRIPTION DRUG LABEL 1 0078-0381 TABLET 5 mg ORAL NDA 33 sections
Focalin HUMAN PRESCRIPTION DRUG LABEL 1 0078-0382 TABLET 10 mg ORAL NDA 33 sections
Focalin HUMAN PRESCRIPTION DRUG LABEL 1 0078-0382 TABLET 10 mg ORAL NDA 33 sections
Focalin HUMAN PRESCRIPTION DRUG LABEL 1 0078-0382 TABLET 10 mg ORAL NDA 33 sections
Focalin HUMAN PRESCRIPTION DRUG LABEL 1 0078-0382 TABLET 10 mg ORAL NDA 33 sections
FocalinXR HUMAN PRESCRIPTION DRUG LABEL 1 0078-0430 CAPSULE, EXTENDED RELEASE 5 mg ORAL NDA 33 sections
FocalinXR HUMAN PRESCRIPTION DRUG LABEL 1 0078-0430 CAPSULE, EXTENDED RELEASE 5 mg ORAL NDA 33 sections
FocalinXR HUMAN PRESCRIPTION DRUG LABEL 1 0078-0430 CAPSULE, EXTENDED RELEASE 5 mg ORAL NDA 33 sections
FocalinXR HUMAN PRESCRIPTION DRUG LABEL 1 0078-0431 CAPSULE, EXTENDED RELEASE 10 mg ORAL NDA 33 sections
FocalinXR HUMAN PRESCRIPTION DRUG LABEL 1 0078-0431 CAPSULE, EXTENDED RELEASE 10 mg ORAL NDA 33 sections
FocalinXR HUMAN PRESCRIPTION DRUG LABEL 1 0078-0431 CAPSULE, EXTENDED RELEASE 10 mg ORAL NDA 33 sections
FocalinXR HUMAN PRESCRIPTION DRUG LABEL 1 0078-0432 CAPSULE, EXTENDED RELEASE 20 mg ORAL NDA 33 sections
FocalinXR HUMAN PRESCRIPTION DRUG LABEL 1 0078-0432 CAPSULE, EXTENDED RELEASE 20 mg ORAL NDA 33 sections
FocalinXR HUMAN PRESCRIPTION DRUG LABEL 1 0078-0432 CAPSULE, EXTENDED RELEASE 20 mg ORAL NDA 33 sections
FocalinXR HUMAN PRESCRIPTION DRUG LABEL 1 0078-0433 CAPSULE, EXTENDED RELEASE 30 mg ORAL NDA 33 sections
FocalinXR HUMAN PRESCRIPTION DRUG LABEL 1 0078-0433 CAPSULE, EXTENDED RELEASE 30 mg ORAL NDA 33 sections
FocalinXR HUMAN PRESCRIPTION DRUG LABEL 1 0078-0433 CAPSULE, EXTENDED RELEASE 30 mg ORAL NDA 33 sections
FocalinXR HUMAN PRESCRIPTION DRUG LABEL 1 0078-0434 CAPSULE, EXTENDED RELEASE 40 mg ORAL NDA 33 sections
FocalinXR HUMAN PRESCRIPTION DRUG LABEL 1 0078-0434 CAPSULE, EXTENDED RELEASE 40 mg ORAL NDA 33 sections
FocalinXR HUMAN PRESCRIPTION DRUG LABEL 1 0078-0434 CAPSULE, EXTENDED RELEASE 40 mg ORAL NDA 33 sections
FocalinXR HUMAN PRESCRIPTION DRUG LABEL 1 0078-0493 CAPSULE, EXTENDED RELEASE 15 mg ORAL NDA 33 sections
FocalinXR HUMAN PRESCRIPTION DRUG LABEL 1 0078-0493 CAPSULE, EXTENDED RELEASE 15 mg ORAL NDA 33 sections
FocalinXR HUMAN PRESCRIPTION DRUG LABEL 1 0078-0493 CAPSULE, EXTENDED RELEASE 15 mg ORAL NDA 33 sections