Details of the Drug

General Information of Drug (ID: DM7SJD6)

Drug Name

Methylphenidate

Synonyms

Calocain; Centedein; Centedrin; Centredin; Concerta; Daytrana; Meridil; Metadate; Methylfenidan; Methylin; Methylofenidan; Methylphen; Methylphenidan; Methylphenidatum; Metilfenidato; Phenidylate; Plimasine; Riphenidate; Ritalin; Ritaline; Tsentedrin; Metadate CD; Metadate ER; Methyl phenidate; Methyl phenidyl acetate; Methyl phenidylacetate; Methylin ER; Metilfenidato [Italian]; Ritalin LA; Ritalin SR; Ritcher works; C 4311; Attenta (TN); Biphentin (TN); Concerta (TN); D-methylphenidate HCl; Daytrana (TN); Equasym (TN); Metadate ER (TN); Methylin (TN); Methylphenidate [INN:BAN]; Methylphenidatum [INN-Latin]; Metilfenidato [INN-Spanish]; Motiron (TN); PMS-Methylphenidate; Ritalin (TN); Ritalin LA (TN); Ritalin-SR; Rubifen (TN); Methylphenidate (USAN/INN); Alpha-Phenyl-2-piperidineacetic acid methyl ester; Methyl phenyl(piperidin-2-yl)acetate; Methyl alpha-phenyl-alpha-2-piperidinylacetate; Alpha-Phenyl-alpha-(2-piperidyl)acetic acid methyl ester; Methyl 2-phenyl-2-piperidin-2-ylacetate; Methyl alpha-phenyl-alpha-(2-piperidyl)acetate; Methyl (2-phenyl-2-(2-piperidyl)acetate); METHYLPHENIDATE (SEE ALSO: METHYLPHENIDATE HYDROCHLORIDE, CAS 298-59-9, NTPNO 10266-R); 2-Piperidineacetic acid, .alpha.-phenyl-, methyl ester; 2-Piperidineacetic acid, alpha-phenyl-, methyl ester

Indication

Disease Entry	ICD 11	Status	REF
Attention deficit hyperactivity disorder	6A05.Z	Approved	[1], [2]
Traumatic brain injury	NA07.Z	Phase 4	[1], [3]

Therapeutic Class

Central Nervous System Stimulants

Drug Type

Small molecular drug

Structure

3D MOL

2D MOL

#Ro5 Violations (Lipinski): 0

Molecular Weight (mw)

233.31

Topological Polar Surface Area (xlogp)

0.2

Rotatable Bond Count (rotbonds)

Hydrogen Bond Donor Count (hbonddonor)

Hydrogen Bond Acceptor Count (hbondacc)

ADMET Property

Absorption AUC: The area under the plot of plasma concentration (AUC) of drug is 50.4-121.5 mcgh/L [4]
Absorption Cmax: The maximum plasma concentration (Cmax) of drug is 6.0-15.0 mcg/L [4]
Absorption Tmax: The time to maximum plasma concentration (Tmax) is 8.1-9.4 h [4]
BDDCS Class: Biopharmaceutics Drug Disposition Classification System (BDDCS) Class 1: high solubility and high permeability [5]
Clearance: The sytemic clearance of drug is 10.2-10.5 L/h/kg [6]
Half-life: The concentration or amount of drug in body reduced by one-half in 2.4 hours (in children), and 2.1 hours (in adults) [4]
Metabolism: The drug is metabolized via the hepatic [4]
MRTD: The Maximum Recommended Therapeutic Dose (MRTD) of drug that ensured maximising efficacy and moderate side effect is 4.28609 micromolar/kg/day [7]
Unbound Fraction: The unbound fraction of drug in plasma is 0.85% [8]
Vd: The volume of distribution (Vd) of drug is 20 L/kg [6]

Chemical Identifiers

Formula: C14H19NO2
IUPAC Name: methyl 2-phenyl-2-piperidin-2-ylacetate
Canonical SMILES: COC(=O)C(C1CCCCN1)C2=CC=CC=C2
InChI: InChI=1S/C14H19NO2/c1-17-14(16)13(11-7-3-2-4-8-11)12-9-5-6-10-15-12/h2-4,7-8,12-13,15H,5-6,9-10H2,1H3
InChIKey: DUGOZIWVEXMGBE-UHFFFAOYSA-N

Cross-matching ID

PubChem CID: 4158
ChEBI ID: CHEBI:84276
CAS Number: 113-45-1
DrugBank ID: DB00422
TTD ID: D02PPN
VARIDT ID: DR00389
INTEDE ID: DR1054
ACDINA ID: D00419

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Dopamine transporter (DAT)	TTVBI8W	SC6A3_HUMAN	Blocker	[9]

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Drug Transporter (DTP)

DTP Name	DTP ID	UniProt ID	MOA	REF
Sodium- and chloride-dependent glycine transporter 2 (SLC6A5)	DTE8R17	SC6A5_HUMAN	Substrate	[10]

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Drug-Metabolizing Enzyme (DME)

DME Name	DME ID	UniProt ID	MOA	REF
Carboxylesterase 1 (CES1)_{Main DME}	DEB30C5	EST1_HUMAN	Substrate	[11]

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Molecular Interaction Atlas (MIA)

MIA Detail

Jump to Detail Molecular Interaction Atlas of This Drug

Molecular Expression Atlas of This Drug

The Studied Disease

Attention deficit hyperactivity disorder

ICD Disease Classification

6A05.Z

Molecule Name	Molecule Type	Gene Name	p-value	Fold-Change	Z-score
Dopamine transporter (DAT)	DTT	SLC6A3	1.08E-03	-3.08	-1.99
Sodium- and chloride-dependent glycine transporter 2 (SLC6A5)	DTP	GLYT2	5.44E-01	-6.94E-02	-3.09E-01
Carboxylesterase 1 (CES1)	DME	CES1	7.50E-01	1.51E-02	4.41E-02

Molecular Expression Atlas (MEA)

MEA Detail

Jump to Detail Molecular Expression Atlas of This Drug

Drug-Drug Interaction (DDI) Information of This Drug

Coadministration of a Drug Treating the Same Disease as Methylphenidate

DDI Drug Name	DDI Drug ID	Severity	Mechanism	Disease	REF
Desipramine	DMT2FDC	Moderate	Decreased metabolism of Methylphenidate caused by Desipramine.	Attention deficit hyperactivity disorder [6A05]	[33]
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Coadministration of a Drug Treating the Disease Different from Methylphenidate (Comorbidity)

DDI Drug Name	DDI Drug ID	Severity	Mechanism	Comorbidity	REF
Methylene blue	DMJAPE7	Major	Additive hypertensive effects by the combination of Methylphenidate and Methylene blue.	Acquired methaemoglobinaemia [3A93]	[34]
Linezolid	DMGFPU2	Major	Increased risk of hyperpyrexia by the combination of Methylphenidate and Linezolid.	Bacterial infection [1A00-1C4Z]	[34]
Phenylbutazone	DMAYL0T	Moderate	Decreased metabolism of Methylphenidate caused by Phenylbutazone.	Chronic pain [MG30]	[35]
Ethanol	DMDRQZU	Moderate	Additive CNS depression effects by the combination of Methylphenidate and Ethanol.	Cystitis [GC00]	[36]
Sertraline	DM0FB1J	Moderate	Decreased metabolism of Methylphenidate caused by Sertraline.	Depression [6A70-6A7Z]	[37]
Trimipramine	DM1SC8M	Moderate	Decreased metabolism of Methylphenidate caused by Trimipramine.	Depression [6A70-6A7Z]	[33]
Imipramine	DM2NUH3	Moderate	Decreased metabolism of Methylphenidate caused by Imipramine.	Depression [6A70-6A7Z]	[33]
Fluoxetine	DM3PD2C	Moderate	Decreased metabolism of Methylphenidate caused by Fluoxetine.	Depression [6A70-6A7Z]	[37]
Nortriptyline	DM4KDYJ	Moderate	Decreased metabolism of Methylphenidate caused by Nortriptyline.	Depression [6A70-6A7Z]	[33]
Paroxetine	DM5PVQE	Moderate	Decreased metabolism of Methylphenidate caused by Paroxetine.	Depression [6A70-6A7Z]	[37]
Selegiline	DM6034S	Major	Increased risk of hyperpyrexia by the combination of Methylphenidate and Selegiline.	Depression [6A70-6A7Z]	[34]
Vortioxetine	DM6F1PU	Moderate	Decreased metabolism of Methylphenidate caused by Vortioxetine.	Depression [6A70-6A7Z]	[37]
Isocarboxazid	DMAF1NB	Major	Increased risk of hyperpyrexia by the combination of Methylphenidate and Isocarboxazid.	Depression [6A70-6A7Z]	[34]
Escitalopram	DMFK9HG	Moderate	Decreased metabolism of Methylphenidate caused by Escitalopram.	Depression [6A70-6A7Z]	[37]
Tranylcypromine	DMGB5RE	Major	Additive hypertensive effects by the combination of Methylphenidate and Tranylcypromine.	Depression [6A70-6A7Z]	[34]
Phenelzine	DMHIDUE	Major	Increased risk of hyperpyrexia by the combination of Methylphenidate and Phenelzine.	Depression [6A70-6A7Z]	[34]
Clomipramine	DMINRKW	Moderate	Decreased metabolism of Methylphenidate caused by Clomipramine.	Depression [6A70-6A7Z]	[33]
Amoxapine	DMKITQE	Moderate	Decreased metabolism of Methylphenidate caused by Amoxapine.	Depression [6A70-6A7Z]	[33]
Doxepin	DMPI98T	Moderate	Decreased metabolism of Methylphenidate caused by Doxepin.	Depression [6A70-6A7Z]	[33]
Esketamine	DMVU687	Major	Additive hypertensive effects by the combination of Methylphenidate and Esketamine.	Depression [6A70-6A7Z]	[38]
Primidone	DM0WX6I	Minor	Decreased metabolism of Methylphenidate caused by Primidone mediated inhibition of CYP450 enzyme.	Epilepsy/seizure [8A61-8A6Z]	[39]
Fosphenytoin	DMOX3LB	Minor	Decreased metabolism of Methylphenidate caused by Fosphenytoin mediated inhibition of CYP450 enzyme.	Epilepsy/seizure [8A61-8A6Z]	[39]
Phenobarbital	DMXZOCG	Minor	Decreased metabolism of Methylphenidate caused by Phenobarbital mediated inhibition of CYP450 enzyme.	Epilepsy/seizure [8A61-8A6Z]	[39]
Procarbazine	DMIK367	Major	Increased risk of hyperpyrexia by the combination of Methylphenidate and Procarbazine.	Hodgkin lymphoma [2B30]	[34]
Propiomazine	DMKY8V1	Moderate	Antagonize the effect of Methylphenidate when combined with Propiomazine.	Insomnia [7A00-7A0Z]	[40]
Polyethylene glycol	DM4I1JP	Moderate	Increased risk of lowers seizure threshold by the combination of Methylphenidate and Polyethylene glycol.	Irritable bowel syndrome [DD91]	[41]
Ozanimod	DMT6AM2	Major	Additive hypertensive effects by the combination of Methylphenidate and Ozanimod.	Multiple sclerosis [8A40]	[34]
Prochlorperazine	DM53SRA	Moderate	Antagonize the effect of Methylphenidate when combined with Prochlorperazine.	Nausea/vomiting [MD90]	[40]
Promethazine	DM6I5GR	Moderate	Antagonize the effect of Methylphenidate when combined with Promethazine.	Nausea/vomiting [MD90]	[40]
Bupropion	DM5PCS7	Major	Increased risk of lowers seizure threshold by the combination of Methylphenidate and Bupropion.	Nicotine use disorder [6C4A]	[42]
Safinamide	DM0YWJC	Major	Additive hypertensive effects by the combination of Methylphenidate and Safinamide.	Parkinsonism [8A00]	[34]
Rasagiline	DM3WKQ4	Moderate	Additive hypertensive effects by the combination of Methylphenidate and Rasagiline.	Parkinsonism [8A00]	[34]
Lindane	DMB8CNL	Moderate	Increased risk of lowers seizure threshold by the combination of Methylphenidate and Lindane.	Pediculosis [1G00]	[43]
Levomepromazine	DMIKFEL	Moderate	Antagonize the effect of Methylphenidate when combined with Levomepromazine.	Psychotic disorder [6A20-6A25]	[40]
Fluphenazine	DMIT8LX	Moderate	Antagonize the effect of Methylphenidate when combined with Fluphenazine.	Psychotic disorder [6A20-6A25]	[40]
Mesoridazine	DM2ZGAN	Moderate	Antagonize the effect of Methylphenidate when combined with Mesoridazine.	Schizophrenia [6A20]	[40]
Thioridazine	DM35M8J	Moderate	Antagonize the effect of Methylphenidate when combined with Thioridazine.	Schizophrenia [6A20]	[40]
Haloperidol	DM96SE0	Moderate	Antagonize the effect of Methylphenidate when combined with Haloperidol.	Schizophrenia [6A20]	[40]
Perphenazine	DMA4MRX	Moderate	Antagonize the effect of Methylphenidate when combined with Perphenazine.	Schizophrenia [6A20]	[40]
Chlorpromazine	DMBGZI3	Moderate	Antagonize the effect of Methylphenidate when combined with Chlorpromazine.	Schizophrenia [6A20]	[40]
Trifluoperazine	DMKBYWI	Moderate	Antagonize the effect of Methylphenidate when combined with Trifluoperazine.	Schizophrenia [6A20]	[40]
Methdilazine	DMAUHQX	Moderate	Antagonize the effect of Methylphenidate when combined with Methdilazine.	Vasomotor/allergic rhinitis [CA08]	[40]
Trimeprazine	DMEMV9D	Moderate	Antagonize the effect of Methylphenidate when combined with Trimeprazine.	Vasomotor/allergic rhinitis [CA08]	[44]
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⏷ Show the Full List of 43 DDI Information of This Drug

Drug Inactive Ingredient(s) (DIG) and Formulation(s) of This Drug

DIG

DIG Name	DIG ID	PubChem CID	Functional Classification
Allura red AC dye	E00338	33258	Colorant
Aspartame	E00402	134601	Flavoring agent
Butylated hydroxytoluene	E00336	31404	Antioxidant
Cetyl alcohol	E00061	2682	Coating agent; Emollient; Emulsifying agent; Stiffening agent
D&C red no. 28	E00491	6097185	Colorant
FD&C blue no. 1	E00263	19700	Colorant
FD&C blue no. 2	E00446	2723854	Colorant
Kyselina citronova	E00014	311	Acidulant; Antioxidant; Buffering agent; Complexing agent; Flavoring agent
Mannitol	E00103	6251	Diluent; Flavoring agent; Lyophilization aid; Plasticizing agent; Tonicity agent
Oleic acid	E00421	445639	Emulsifying agent; Penetration agent; Solubilizing agent
Phosphoric acid	E00039	1004	Acidulant; Buffering agent
Quinoline yellow WS	E00309	24671	Colorant
Sodium stearyl fumarate	E00545	23665634	lubricant
Stearic acid	E00079	5281	Emulsifying agent; Solubilizing agent; Viscosity-controlling agent; lubricant
Succinic acid	E00044	1110	Buffering agent
Sucralose	E00370	71485	Flavoring agent
Sunset yellow FCF	E00255	17730	Colorant
Acetone	E00004	180	Solvent
Acetyltributyl citrate	E00127	6505	Plasticizing agent
Beta-D-lactose	E00099	6134	Diluent; Dry powder inhaler carrier; Lyophilization aid
Beta-maltose	E00104	6255	Binding agent; Diluent; Disintegrant; Flavoring agent
Carboxymethylcellulose sodium	E00621	Not Available	Adsorbent; Binding agent; Disintegrant; Emulsifying agent; Suspending agent; Viscosity-controlling agent
Cetostearyl alcohol	E00353	62238	Emollient; Emulsifying agent; Viscosity-controlling agent
Citric acid monohydrate	E00271	22230	Acidulant; Antioxidant; Buffering agent; Complexing agent; Flavoring agent
Eisenoxyd	E00585	56841934	Colorant
Ferric hydroxide oxide yellow	E00539	23320441	Colorant
Ferrosoferric oxide	E00231	14789	Colorant
Fructose	E00447	2723872	Flavoring agent
Lactose monohydrate	E00393	104938	Binding agent; Diluent; Dry powder inhaler carrier; Lyophilization aid
Magnesium stearate	E00208	11177	lubricant
Medium-chain triglyceride	E00640	Not Available	Emollient; Lubricant; Surfactant
Polyethylene glycol 3350	E00652	Not Available	Coating agent; Diluent; Ointment base; Plasticizing agent; Solvent; Suppository base; lubricant
Potassium hydroxide	E00233	14797	Alkalizing agent
Povidone	E00667	Not Available	Binding agent; Coating agent; Disintegrant; Film/membrane-forming agent; Solubilizing agent; Suspending agent
Propylene glycol	E00040	1030	Antimicrobial preservative; Humectant; Plasticizing agent; Solvent
Saccharose	E00091	5988	Binding agent; Coating agent; Cryoprotectant; Diluent; Flavoring agent; Suspending agent; Viscosity-controlling agent
Silicon dioxide	E00670	Not Available	Anticaking agent; Opacifying agent; Viscosity-controlling agent
Sodium chloride	E00077	5234	Diluent; Tonicity agent
Soybean lecithin	E00637	Not Available	Other agent
Talc	E00520	16211421	Anticaking agent; Diluent; Glidant; lubricant
Titanium dioxide	E00322	26042	Coating agent; Colorant; Opacifying agent
Triacetin	E00080	5541	Humectant; Plasticizing agent; Solvent
Triethyl citrate	E00128	6506	Plasticizing agent; Solvent
Water	E00035	962	Solvent
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⏷ Show the Full List of 44 Pharmaceutical Excipients of This Drug

Pharmaceutical Formulation

Formulation Name	Drug Dosage	Dosage Form	Route
Methylphenidate 18 mg tablet	18 mg	24 HR Extended Release Oral Tablet	Oral
Methylphenidate 27 mg tablet	27 mg	24 HR Extended Release Oral Tablet	Oral
Methylphenidate 36 mg tablet	36 mg	24 HR Extended Release Oral Tablet	Oral
Methylphenidate 54 mg tablet	54 mg	24 HR Extended Release Oral Tablet	Oral
Methylphenidate 17.3 mg tablet	17.3 mg	Disintegrating Oral Tablet	Oral
Methylphenidate 25.9 mg tablet	25.9 mg	Disintegrating Oral Tablet	Oral
Methylphenidate 8.6 mg tablet	8.6 mg	Disintegrating Oral Tablet	Oral
Methylphenidate 10 mg tablet	10 mg	Oral Tablet	Oral
Methylphenidate 20 mg tablet	20 mg	Oral Tablet	Oral
Methylphenidate 5 mg tablet	5 mg	Oral Tablet	Oral
Methylphenidate 10 mg tablet	10 mg	Chewable Tablet	Oral
Methylphenidate 2.5 mg tablet	2.5 mg	Chewable Tablet	Oral
Methylphenidate 5 mg tablet	5 mg	Chewable Tablet	Oral
Methylphenidate 30 mg capsule	30 mg	24 HR Extended Release Oral Capsule	Oral
Methylphenidate 40 mg capsule	40 mg	24 HR Extended Release Oral Capsule	Oral
Methylphenidate 20 mg tablet	20 mg	8 HR Extended Release Oral Tablet	Oral
Methylphenidate 10 mg tablet	10 mg	8 HR Extended Release Oral Tablet	Oral
Methylphenidate 20 mg capsule	20 mg	24 HR Extended Release Oral Capsule	Oral

Jump to Detail Pharmaceutical Formulation Page of This Drug

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