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

Stem definition	Drug id	CAS RN
	836	40431-64-9

Description:

Molecule	Description
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

Molecule

Description

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:

Dose	Unit	Route
15	mg	O

ADMET properties:

Property	Value	Reference
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:

Date	Agency	Company	Orphan
Nov. 13, 2001	FDA	NOVARTIS

FDA Adverse Event Reporting System (Female)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Product substitution issue	47.38	29.52	16	1110	14041	50589957
Abnormal behaviour	42.14	29.52	16	1110	19642	50584356

FDA Adverse Event Reporting System (Male)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Product substitution issue	198.50	42.37	57	2073	9115	29563282
Abnormal behaviour	172.10	42.37	64	2066	23063	29549334
Drug ineffective	110.54	42.37	132	1998	363038	29209359
Anger	80.31	42.37	30	2100	10860	29561537
Aggression	70.10	42.37	39	2091	35502	29536895
Irritability	59.81	42.37	30	2100	22122	29550275
Brugada syndrome	59.25	42.37	13	2117	688	29571709
Psychomotor hyperactivity	58.25	42.37	22	2108	8191	29564206
Disturbance in attention	57.80	42.37	29	2101	21395	29551002
Tic	56.16	42.37	15	2115	1820	29570577
Agitation	52.20	42.37	37	2093	51267	29521130
Attention deficit hyperactivity disorder	48.84	42.37	14	2116	2203	29570194
Product quality issue	44.28	42.37	22	2108	15873	29556524

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Product substitution issue	211.46	30.93	59	2169	17802	64478702
Abnormal behaviour	99.53	30.93	39	2189	33583	64462921
Anger	83.08	30.93	28	2200	15713	64480791
Tic	72.17	30.93	17	2211	2602	64493902
Brugada syndrome	63.20	30.93	13	2215	1065	64495439
Irritability	63.18	30.93	29	2199	36717	64459787
Aggression	62.73	30.93	31	2197	46201	64450303
Agitation	48.81	30.93	33	2195	88334	64408170
Disturbance in attention	42.59	30.93	23	2205	41051	64455453
Psychomotor hyperactivity	40.03	30.93	16	2212	14435	64482069
Crying	31.84	30.93	15	2213	20075	64476429
Anxiety	31.81	30.93	37	2191	202612	64293892

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	N06BA11	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|

Disease	Relation	SNOMED_ID	DOID
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 level	Dissociation constant	Type (acidic/basic)
pKa1	8.68	Basic

Orange Book patent data (new drug applications)

Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent 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 strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Exclusivity date	Description
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:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Sodium-dependent noradrenaline transporter	Transporter	P23975	SC6A2_HUMAN	INHIBITOR			WOMBAT-PK	CHEMBL
Sodium-dependent dopamine transporter	Transporter	Q01959	SC6A3_HUMAN	INHIBITOR	Ki	7.80	CHEMBL	CHEMBL
Sodium-dependent dopamine transporter	Transporter		SC6A3_RAT		Ki	7.13	CHEMBL
Transporter	Transporter		Q9WTR4_RAT		Ki	6.57	CHEMBL
Dopamine receptor	GPCR		DRD1_RAT DRD3_RAT DRD5_RAT DRD4_RAT DRD2_RAT		IC50	7.08	CHEMBL

External reference:

ID	Source
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
8289	INN_ID
7554	IUPHAR_LIGAND_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:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
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	0078-0382	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	0078-0431	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	0078-0433	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	0078-0493	CAPSULE, EXTENDED RELEASE	15 mg	ORAL	NDA	33 sections
FocalinXR	HUMAN PRESCRIPTION DRUG LABEL	1	0078-0608	CAPSULE, EXTENDED RELEASE	25 mg	ORAL	NDA	33 sections
FocalinXR	HUMAN PRESCRIPTION DRUG LABEL	1	0078-0609	CAPSULE, EXTENDED RELEASE	35 mg	ORAL	NDA	33 sections
Dexmethylphenidate Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0093-5045	CAPSULE, EXTENDED RELEASE	25 mg	ORAL	ANDA	28 sections
Dexmethylphenidate Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0093-5046	CAPSULE, EXTENDED RELEASE	35 mg	ORAL	ANDA	28 sections
Dexmethylphenidate Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0093-5550	CAPSULE, EXTENDED RELEASE	5 mg	ORAL	ANDA	28 sections
Dexmethylphenidate Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0093-5551	CAPSULE, EXTENDED RELEASE	10 mg	ORAL	ANDA	28 sections
Dexmethylphenidate Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0093-5552	CAPSULE, EXTENDED RELEASE	15 mg	ORAL	ANDA	28 sections
Dexmethylphenidate Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0093-5553	CAPSULE, EXTENDED RELEASE	20 mg	ORAL	ANDA	28 sections
Dexmethylphenidate Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0093-5554	CAPSULE, EXTENDED RELEASE	30 mg	ORAL	ANDA	28 sections
Dexmethylphenidate Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0093-5562	CAPSULE, EXTENDED RELEASE	40 mg	ORAL	ANDA	28 sections
Dexmethylphenidate hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0115-1682	CAPSULE, EXTENDED RELEASE	5 mg	ORAL	ANDA	21 sections
Dexmethylphenidate hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0115-1683	CAPSULE, EXTENDED RELEASE	10 mg	ORAL	ANDA	21 sections
Dexmethylphenidate hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0115-1684	CAPSULE, EXTENDED RELEASE	15 mg	ORAL	ANDA	21 sections
Dexmethylphenidate hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0115-1685	CAPSULE, EXTENDED RELEASE	20 mg	ORAL	ANDA	21 sections
Dexmethylphenidate hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0115-1686	CAPSULE, EXTENDED RELEASE	30 mg	ORAL	ANDA	21 sections
Dexmethylphenidate hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0115-1709	CAPSULE, EXTENDED RELEASE	25 mg	ORAL	ANDA	20 sections
Dexmethylphenidate hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0115-1710	CAPSULE, EXTENDED RELEASE	35 mg	ORAL	ANDA	20 sections
Dexmethylphenidate hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0115-9918	CAPSULE, EXTENDED RELEASE	5 mg	ORAL	ANDA	20 sections