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Identification
- Summary
Methylphenidate is a stimulant used in the management of Attention Deficit Hyperactivity Disorder (ADHD).
- Brand Names
- Aptensio, Biphentin, Concerta, Cotempla, Daytrana, Foquest, Jornay, Metadate, Methylin, Quillichew, Quillivant, Relexxii, Ritalin
- Generic Name
- Methylphenidate
- DrugBank Accession Number
- DB00422
- Background
Methylphenidate is a central nervous system stimulant used most commonly in the treatment of Attention-Deficit/Hyperactivity Disorder (ADHD) and for narcolepsy. Also known as the marketed products Ritalin, Concerta, or Biphentin, methylphenidate is used with other treatment modalities (psychological, educational, cognitive behaviour therapy, etc) to improve the following group of developmentally inappropriate symptoms associated with ADHD: moderate-to-severe distractibility, short attention span, hyperactivity, emotional lability, and impulsivity. Long-acting formulations of psychostimulants such as methylphenidate, Dextroamphetamine, and Lisdexamfetamine are considered the most effective and widely used treatment for ADHD, and are considered first-line options for children, adolescents, and adults as recommended by CADDRA (Canadian ADHD Resource Alliance). 12 CADDRA recommends the use of methylphenidate due to long term studies, of over twenty years in duration, which show methylphenidate is safe and effective.
While its exact mechanism is unclear, methylphenidate (MPH) has been shown to act as a norepinephrine and dopamine reuptake inhibitor (NDRI), thereby increasing the presence of these neurotransmitters in the extraneuronal space and prolonging their action.6 There is a dose-related effect of psychostimulants on receptor stimulation, where higher doses are shown to increase norepinephrine (NE) and dopamine (DA) efflux throughout the brain which can result in impaired cognition and locomotor-activating effects. In contrast, low doses are found to selectively activate NE and DA neurotransmission within the prefrontal cortex which is an area of the brain thought to play a prominent role in ADHD pathophysiology, thereby improving clinical efficacy and preventing side effects.8 The lower doses used to treat ADHD are not associated with the locomotor-activating effects associated with higher doses and instead reduce movement, impulsivity, and increase cognitive function including sustained attention and working memory.6,7 Methylphenidate's beneficial effects in sustaining attention have also been shown to be mediated by alpha-1 adrenergic receptor activity.9 Clinical findings have shown that children with ADHD have an abnormality in the dopamine transporter gene (DAT1), the D4 receptor gene (DRD-4), and/or the D2 receptor gene that may be at least partly overcome by the dopaminergic effects of methylphenidate, suggesting a possible mode of action.16
When provided as Biphentin®, methylphenidate is released through a multi-layer release delivery system (MLRTM) where 40% of the dose is provided as an immediate release and 60% is provided through a gradual release. Biphentin was designed to be an alternative to separate doses of immediate-release (IR) methylphenidate by providing a biphasic concentration-time profile when given as a single dose. The MLRTM release system allows for a sustained effect for 10-12 hours, allowing for once-daily dosing that covers the major times that ADHD impairment might occur (such as school, homework periods, during the work day, etc).
When provided as Concerta®, methylphenidate is released through the patented Osmotic Controlled-Release Oral Delivery (OROS) system where 22% of the dose is provided as an immediate release and 78% is provided through a gradual release.1 OROS is comprised of an osmotically active trilayer core surrounded by a semipermeable membrane with an immediate-release drug overcoat. Within an aqueous environment, such as the stomach, the drug overcoat, which consists of 22% of the dose, dissolves within one hour, providing an initial immediate-release formulation of methylphenidate. Water then permeates through the membrane into the tablet core where the osmotically active polymer excipients expand, allowing methylphenidate to release slowly through the orifice over a period of 6-7 hours. Concerta also provides a sustained 10-12 hour effect, allowing for once-daily dosing.
Methylphenidate contains a blackbox warning stating that CNS stimulants, including methylphenidate-containing products and amphetamines, have a high potential for abuse and dependence. This abuse potential is likely related to the effects associated with higher doses of methylphenidate, which induce surface expression of the dopamine transporter (DAT).10 In particular, increased dopamine in key brain areas is associated with the reinforcing and addictive properties of psychostimulants such as methylphenidate, and even amplifies the potency and reinforcing effects of other drugs of abuse such as amphetamines, making ADHD sufferers more susceptible to their addictive effects.11 Concerns about abuse potential have spurred research into medications with fewer effects on DAT and the use of non-stimulant ADHD medications including Atomoxetine and Guanfacine.
- Type
- Small Molecule
- Groups
- Approved, Investigational
- Structure
Structure for Methylphenidate (DB00422)
- Weight
- Average: 233.3062
Monoisotopic: 233.141578857 - Chemical Formula
- C14H19NO2
- Synonyms
- Methyl phenidylacetate
- methyl phenyl(piperidin-2-yl)acetate
- methyl α-phenyl-α-(2-piperidyl)acetate
- methyl α-phenyl-α-2-piperidinylacetate
- Methylphenidan
- Methylphenidate
- Methylphenidatum
- Metilfenidato
- MPH
- α-phenyl-2-piperidineacetic acid methyl ester
Pharmacology
- Indication
Methylphenidate is indicated for the treatment of Attention Deficit Hyperactivity Disorder (ADHD) in patients 6 years of age and older and for the treatment of narcolepsy.
Reduce drug development failure ratesBuild, train, & validate machine-learning modelswith evidence-based and structured datasets.Build, train, & validate predictive machine-learning models with structured datasets.- Associated Conditions
Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Treatment of Attention deficit hyperactivity disorder (adhd) •••••••••••• •••••••• •••••••• •••••••• •••••••• •••••• ••••••••• ••••••••••• •••••••• •••••••• ••••••• ••••••• ••••••••• •••••••• •••••••• ••••••• •••••••• •••••••• ••••••• •••••• ••••••••••••••• ••••••• ••••••• Treatment of Narcolepsy •••••••••••• ••••••••• •••••• - Contraindications & Blackbox Warnings
Prevent Adverse Drug Events TodayTap into our Clinical API for life-saving information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events with our Clinical API- Pharmacodynamics
Methylphenidate is a racemic mixture comprised of the d- and l-isomers. The d-isomer is more pharmacologically active than the l-isomer. Radioligand binding studies demonstrate that binding of methylphenidate in the brain is localized to dopamine-rich areas, in particular in the prefrontal cortex which has been demonstrated to play a prominent role in ADHD pathophysiology.8 In a number of animal models, methylphenidate enhances locomotor activity and induces stereotypic behaviours.
- Mechanism of action
While its exact mechanism is unclear, methylphenidate (MPH) has been shown to act as a norepinephrine and dopamine reuptake inhibitor (NDRI), thereby increasing the presence of these neurotransmitters in the extraneuronal space and prolonging their action.6 There is a dose-related effect of psychostimulants on receptor stimulation, where higher doses are shown to increase norepinephrine (NE) and dopamine (DA) efflux throughout the brain which can result in impaired cognition and locomotor-activating effects. In contrast, low doses are found to selectively activate NE and DE neurotransmission within the prefrontal cortex which is an area of the brain thought to play a prominent role in ADHD pathophysiology, thereby improving clinical efficacy and preventing side effects.8 The lower doses used to treat ADHD are not associated with the locomotor-activating effects associated with higher doses and instead reduce movement, impulsivity, and increase cognitive function including sustained attention and working memory.6,7 Methylphenidate's beneficial effects in sustaining attention have also been shown to be mediated by alpha-1 adrenergic receptor activity.9
Clinical findings have shown that children with ADHD have an abnormality in the dopamine transporter gene (DAT1), the D4 receptor gene (DRD-4), and/or the D2 receptor gene that may be at least partly overcome by the dopaminergic effects of methylphenidate, suggesting a possible mode of action.16
Target Actions Organism ASodium-dependent dopamine transporter inhibitorHumans U5-hydroxytryptamine receptor 1A Not Available Humans USodium-dependent noradrenaline transporter inhibitorHumans - Absorption
Concerta®: Methylphenidate is readily absorbed. Following oral administration of Concerta, plasma methylhphenidate concentrations reach an initial maximum at about 1 hour followed by gradual ascending concentrations over the next 5-9 hours. Mean times to reach peak plasma concentrations across all doses of Concerta occurred between 6-10 hours. Once daily dosing minimizes the fluctuations between peak and trough concentrations associated with multiple doses of immediate-release methylphenidate treatments.16 Depending on the doses provided, Cmax was found to range from 6.0-15.0ng/mL, Tmax ranged from 8.1-9.4h, and AUC ranged from 50.4-121.5 ng·h/mL in children.16
When provided as Concerta®, methylphenidate is released through the patented Osmotic Controlled-Release Oral Delivery (OROS) system where 22% of the dose is provided as an immediate release and 78% is provided through a gradual release.1 OROS is comprised of an osmotically active trilayer core surrounded by a semipermeable membrane with an immediate-release drug overcoat. Within an aqueous environment, such as the stomach, the drug overcoat, which consists of 22% of the dose, dissolves within one hour, providing an initial immediate-release formulation of methylphenidate. Water then permeates through the membrane into the tablet core where the osmotically active polymer excipients expand, allowing methylphenidate to release slowly through the orifice over a period of 6-7 hours. Concerta also provides a sustained 10-12 hour effect, allowing for once-daily dosing.
Biphentin®: Methylphenidate is rapidly and extensively absorbed following oral administration, with peak blood levels obtained in 1-3 hours.17
When provided as Biphentin®, methylphenidate is released through a multi-layer release delivery system (MLRTM) where 40% of the dose is provided as an immediate release and 60% is provided through a gradual release. Biphentin was designed to be an alternative to separate doses of immediate-release (IR) methylphenidate by providing a biphasic concentration-time profile when given as a single dose. The MLRTM release system allows for a sustained effect for 10-12 hours, allowing for once-daily dosing that covers the major times that ADHD impairment might occur (such as school, homework periods, during the workday, etc).
Methylphenidate (immediate release): Methylphenidate hydrochloride is rapidly and extensively absorbed from the tablets following oral administration; however, owing to extensive first-pass metabolism, bioavailability is low (approx. 30%) and large individual differences exist (11-52%). In one study, the administration of methylphenidate hydrochloride with food accelerated absorption but had no effect on the amount absorbed. Peak plasma concentrations of 10.8 and 7.8 ng/mL were observed, on average, 2 hours after administration of 0.30 mg/kg in children and adults, respectively. Peak plasma concentrations showed marked variability between subjects. Both the area under the concentration-time curve (AUC), and the peak plasma concentrations (Cmax) showed dose-proportionality.18
- Volume of distribution
Concerta: Plasma methylphenidate concentrations in adults decline bi-exponentially following oral administration.16
Biphentin: The apparent distribution volume of methylphenidate in children is approximately 20 L/kg, with substantial variability (11 to 33 L/kg).17
Methylphenidate (immediate release): The apparent distribution volume of methylphenidate in children was approximately 20 L/kg, with substantial variability (11-33 L/kg). The volume of distribution after an intravenous dose (Vss) is 2.23 L/kg for the racemate in healthy adult volunteers.18
- Protein binding
Concerta: In humans, 15 ± 5% of methylphenidate in the blood is bound to plasma proteins. 16
Biphentin: In blood, methylphenidate and its metabolites are distributed between plasma (57%) and erythrocytes (43%). Methylphenidate and its metabolites exhibit low plasma protein binding (approximately 15%).17
Methylphenidate (immediate release): In blood, methylphenidate and its metabolites are distributed between plasma (57%) and erythrocytes (43%). Methylphenidate and its metabolites exhibit low plasma protein binding (approx. 15%).18
- Metabolism
Methylphenidate is hepatically metabolized. More specifically, it is rapidly and extensively metabolized by carboxylesterase CES1A1. Via this enzyme, methylphenidate undergoes de-esterification to ritalinic acid (a-phenyl-2-piperidine acetic acid, PPAA), which has little to no pharmacologic activity.
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- Route of elimination
After oral administration of an immediate release formulation of methylphenidate, 78%-97% of the dose is excreted in the urine and 1%-3% in the feces in the form of metabolites within 48-96 hours. Only small quantities (<1%) of unchanged methylphenidate appear in the urine. Most of the dose is excreted in the urine as ritalinic acid (60%-86%), the remainder being accounted for by minor metabolites.
- Half-life
Concerta: The half-life of methylphenidate in adults following oral administration of Concerta® was approximately 3.5 h.16
Biphentin: Methylphenidate is eliminated from plasma with a mean half-life of 2.4 hours in children and 2.1 hours in adults.17
Methylphenidate (immediate release): Methylphenidate is eliminated from the plasma with a mean half-life of 2.4 hours in children and 2.1 hours in adults.18
- Clearance
The apparent mean systemic clearance after an oral dose is 10.2 and 10.5 L/h/kg in children and adults, respectively for a 0.3 mg/kg dose, and 0.565 L/h/kg after an intravenous dose of the racemate in healthy adult volunteers.18
- Adverse Effects
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Symptoms of overdose include vomiting, agitation, tremors, hyperreflexia, muscle twitching, convulsions (may be followed by coma), euphoria, confusion, hallucinations, delirium, sweating, flushing, headache, hyperpyrexia, tachycardia, palpitations, cardiac arrhythmias, hypertension, mydriasis, and dryness of mucous membranes. LD50=190mg/kg (orally in mice)
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs
- Not Available
Interactions
- Drug Interactions
- This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Drug Interaction Integrate drug-drug
interactions in your softwareAcebutolol Methylphenidate may decrease the antihypertensive activities of Acebutolol. Aceclofenac The risk or severity of hypertension can be increased when Methylphenidate is combined with Aceclofenac. Acemetacin The risk or severity of hypertension can be increased when Methylphenidate is combined with Acemetacin. Acenocoumarol The metabolism of Acenocoumarol can be decreased when combined with Methylphenidate. Acetazolamide The therapeutic efficacy of Acetazolamide can be decreased when used in combination with Methylphenidate. - Food Interactions
- Avoid alcohol. Co-administration with alcohol may cause a "dose-dumping" effect with some extended-release formulations of methylphenidate. It may also potentiate the CNS effects of methylphenidate.
- Take with or without food. Patients may take methylphenidate with food to alleviate GI upset.
Products
Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.- Product Ingredients
Ingredient UNII CAS InChI Key Methylphenidate hydrochloride 4B3SC438HI 23655-65-4 JUMYIBMBTDDLNG-UHFFFAOYSA-N - Product Images
- International/Other Brands
- Equasym XL / Medikinet XL / Quillivant / Riphenidate / Rubifen SR
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Adhansia XR Capsule, extended release 70 mg/1 Oral Adlon Therapeutics L.P. 2019-07-01 2023-11-30 US 
Adhansia XR Capsule, extended release 35 mg/1 Oral Adlon Therapeutics L.P. 2019-07-01 2023-09-30 US Adhansia XR Capsule, extended release 55 mg/1 Oral Adlon Therapeutics L.P. 2019-07-01 2023-11-30 US Adhansia XR Capsule, extended release 25 mg/1 Oral Adlon Therapeutics L.P. 2019-07-01 2023-11-30 US Adhansia XR Capsule, extended release 85 mg/1 Oral Adlon Therapeutics L.P. 2019-07-01 2023-11-30 US - Generic Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Metadate ER Tablet, extended release 20 mg/1 Oral Upstate Pharma, LLC 2014-11-01 Not applicable US Metadate ER Tablet, extended release 20 mg/1 Oral Lannett Company, Inc. 2014-11-01 Not applicable US Metadate ER Tablet, extended release 20 mg/1 Oral Unither Pharmaceuticals 1988-06-01 Not applicable US Methylin Tablet 20 mg/1 Oral Golden State Medical Supply 2010-05-20 2015-06-30 US Methylin Tablet 10 mg/1 Oral Golden State Medical Supply 2010-05-20 2015-06-30 US
Categories
- ATC Codes
- N06BA04 — Methylphenidate
- Drug Categories
- Acids, Carbocyclic
- Agents that produce hypertension
- Agents that reduce seizure threshold
- Central Nervous System Agents
- Central Nervous System Stimulants
- Central Nervous System Stimulation
- Centrally Acting Sympathomimetics
- Dopamine Agents
- Dopamine Uptake Inhibitors
- Heterocyclic Compounds, Fused-Ring
- Membrane Transport Modulators
- Methylphenidate and isomer
- Nervous System
- Neurotransmitter Agents
- Neurotransmitter Uptake Inhibitors
- Phenylacetates
- Piperidines
- Psychoanaleptics
- Psychostimulants, Agents Used for ADHD and Nootropics
- Respiratory and CNS Stimulants
- Chemical TaxonomyProvided by Classyfire
- Description
- This compound belongs to the class of organic compounds known as aralkylamines. These are alkylamines in which the alkyl group is substituted at one carbon atom by an aromatic hydrocarbyl group.
- Kingdom
- Organic compounds
- Super Class
- Organic nitrogen compounds
- Class
- Organonitrogen compounds
- Sub Class
- Amines
- Direct Parent
- Aralkylamines
- Alternative Parents
- Piperidines / Benzene and substituted derivatives / Methyl esters / Amino acids and derivatives / Monocarboxylic acids and derivatives / Dialkylamines / Azacyclic compounds / Organopnictogen compounds / Organic oxides / Hydrocarbon derivatives show 1 more
- Substituents
- Amino acid or derivatives / Aralkylamine / Aromatic heteromonocyclic compound / Azacycle / Benzenoid / Carbonyl group / Carboxylic acid derivative / Carboxylic acid ester / Hydrocarbon derivative / Methyl ester show 10 more
- Molecular Framework
- Aromatic heteromonocyclic compounds
- External Descriptors
- piperidines, methyl ester, beta-amino acid ester (CHEBI:84276)
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- 207ZZ9QZ49
- CAS number
- 113-45-1
- InChI Key
- DUGOZIWVEXMGBE-UHFFFAOYSA-N
- 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
- IUPAC Name
- methyl 2-phenyl-2-(piperidin-2-yl)acetate
- SMILES
- COC(=O)C(C1CCCCN1)C1=CC=CC=C1
References
- Synthesis Reference
- US2512572
- General References
- Keating GM, McClellan K, Jarvis B: Methylphenidate (OROS formulation). CNS Drugs. 2001;15(6):495-500; discussion 501-3. [Article]
- Markowitz JS, DeVane CL, Pestreich LK, Patrick KS, Muniz R: A comprehensive in vitro screening of d-, l-, and dl-threo-methylphenidate: an exploratory study. J Child Adolesc Psychopharmacol. 2006 Dec;16(6):687-98. [Article]
- Fone KC, Nutt DJ: Stimulants: use and abuse in the treatment of attention deficit hyperactivity disorder. Curr Opin Pharmacol. 2005 Feb;5(1):87-93. [Article]
- Sharma RP, Javaid JI, Pandey GN, Easton M, Davis JM: Pharmacological effects of methylphenidate on plasma homovanillic acid and growth hormone. Psychiatry Res. 1990 Apr;32(1):9-17. [Article]
- Hodgkins P, Shaw M, Coghill D, Hechtman L: Amfetamine and methylphenidate medications for attention-deficit/hyperactivity disorder: complementary treatment options. Eur Child Adolesc Psychiatry. 2012 Sep;21(9):477-92. doi: 10.1007/s00787-012-0286-5. Epub 2012 Jul 5. [Article]
- Berridge CW, Devilbiss DM, Andrzejewski ME, Arnsten AF, Kelley AE, Schmeichel B, Hamilton C, Spencer RC: Methylphenidate preferentially increases catecholamine neurotransmission within the prefrontal cortex at low doses that enhance cognitive function. Biol Psychiatry. 2006 Nov 15;60(10):1111-20. doi: 10.1016/j.biopsych.2006.04.022. Epub 2006 Jun 23. [Article]
- Solanto MV: Neuropsychopharmacological mechanisms of stimulant drug action in attention-deficit hyperactivity disorder: a review and integration. Behav Brain Res. 1998 Jul;94(1):127-52. [Article]
- Brennan AR, Arnsten AF: Neuronal mechanisms underlying attention deficit hyperactivity disorder: the influence of arousal on prefrontal cortical function. Ann N Y Acad Sci. 2008;1129:236-45. doi: 10.1196/annals.1417.007. [Article]
- Berridge CW, Shumsky JS, Andrzejewski ME, McGaughy JA, Spencer RC, Devilbiss DM, Waterhouse BD: Differential sensitivity to psychostimulants across prefrontal cognitive tasks: differential involvement of noradrenergic alpha(1) - and alpha(2)-receptors. Biol Psychiatry. 2012 Mar 1;71(5):467-73. doi: 10.1016/j.biopsych.2011.07.022. Epub 2011 Sep 3. [Article]
- Calipari ES, Ferris MJ, Salahpour A, Caron MG, Jones SR: Methylphenidate amplifies the potency and reinforcing effects of amphetamines by increasing dopamine transporter expression. Nat Commun. 2013;4:2720. doi: 10.1038/ncomms3720. [Article]
- Marshall CA, Brodnik ZD, Mortensen OV, Reith MEA, Shumsky JS, Waterhouse BD, Espana RA, Kortagere S: Selective activation of Dopamine D3 receptors and norepinephrine transporter blockade enhances sustained attention. Neuropharmacology. 2019 Apr;148:178-188. doi: 10.1016/j.neuropharm.2019.01.003. Epub 2019 Jan 8. [Article]
- CADDRA - Canadian ADHD Practice Guidelines [Link]
- Concerta FDA label [Link]
- FDA Approved Drug Products: Daytrana® transdermal system [Link]
- FDA Approved Drug Products: Aptensio XR (methylphenidate hydrochloride) extended-release capsules for oral use [Link]
- Health Canada Label - Concerta [File]
- Health Canada Label - Biphentin [File]
- Health Canada - Ritalin [File]
- External Links
- Human Metabolome Database
- HMDB0014566
- KEGG Drug
- D04999
- KEGG Compound
- C07196
- PubChem Compound
- 4158
- PubChem Substance
- 46505929
- ChemSpider
- 4015
- BindingDB
- 50062912
- 6901
- ChEBI
- 84276
- ChEMBL
- CHEMBL796
- Therapeutic Targets Database
- DAP000024
- PharmGKB
- PA10054
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- PDRhealth
- PDRhealth Drug Page
- Wikipedia
- Methylphenidate
Clinical Trials
- Clinical Trials
Clinical Trial & Rare Diseases Add-on Data Package
Explore 4,000+ rare diseases, orphan drugs & condition pairs, clinical trial why stopped data, & more. Preview package Phase Status Purpose Conditions Count Start Date Why Stopped 100+ additional columns Unlock 175K+ rows when you subscribe.View sample dataNot Available Completed Not Available ADHD - Inattentive Type / Attention Deficit Hyperactivity Disorder (ADHD) 1 somestatus stop reason just information to hide Not Available Completed Not Available Attention Deficit Hyperactivity Disorder (ADHD) 6 somestatus stop reason just information to hide Not Available Completed Not Available Eating Disorders 1 somestatus stop reason just information to hide Not Available Completed Not Available Healthy Volunteers (HV) 1 somestatus stop reason just information to hide Not Available Completed Not Available Psychosis 1 somestatus stop reason just information to hide
Pharmacoeconomics
- Manufacturers
- Shire development inc
- Ucb inc
- Novartis pharmaceuticals corp
- Mallinckrodt inc
- Tris pharma inc
- Ortho mcneil janssen pharmaceutical inc
- Able laboratories inc
- Actavis elizabeth llc
- Watson laboratories inc
- Ortho-McNeil-Janssen Pharmaceuticals, Inc.
- Packagers
- Alliant Pharmaceuticals Inc.
- Alza Corp.
- Apothecon
- Bryant Ranch Prepack
- Cardinal Health
- Caremark LLC
- Chattem Chemicals Inc.
- D.M. Graham Laboratories Inc.
- Dispensing Solutions
- Elan Pharmaceuticals Inc.
- Eurand Pharmaceuticals Inc.
- Janssen-Ortho Inc.
- Major Pharmaceuticals
- Mallinckrodt Inc.
- Mckesson Corp.
- McNeil Laboratories
- Novartis AG
- Noven Pharmaceuticals Inc.
- Nucare Pharmaceuticals Inc.
- Ortho Mcneil Janssen Pharmaceutical Inc.
- Patriot Pharmaceuticals
- PD-Rx Pharmaceuticals Inc.
- Physicians Total Care Inc.
- Purdue Pharma LP
- Qualitest
- Quality Care
- Sandoz
- Sciele Pharma Inc.
- Shire Inc.
- Stat Rx Usa
- Superior Pharmeceuticals
- UCB Pharma
- Upstate Pharma LLC
- Watson Pharmaceuticals
- Dosage Forms
Form Route Strength Tablet, extended release Oral 18.000 mg Capsule, extended release Oral 25 mg/1 Capsule, extended release Oral 35 mg/1 Capsule, extended release Oral 45 mg/1 Capsule, extended release Oral 55 mg/1 Capsule, extended release Oral 70 mg/1 Capsule, extended release Oral 85 mg/1 Capsule, extended release Oral 15 mg/1 Capsule, extended release Oral 10 mg Capsule, extended release Oral 15 mg Capsule, extended release Oral 20 mg Capsule, extended release Oral 30 mg Capsule, extended release Oral 40 mg Capsule, extended release Oral 50 mg Capsule, extended release Oral 60 mg Capsule, extended release Oral 80 mg Tablet Oral 54.000 mg Tablet, extended release Oral 18 mg Tablet, extended release Oral 18 mg/1 Tablet, extended release Oral 27 mg/1 Tablet, extended release Oral 27 mg Tablet, extended release Oral 36 mg Tablet, extended release Oral 36 mg/1 Tablet, extended release Oral 54 mg Tablet, extended release Oral 54 mg/1 Tablet Oral 18 mg Tablet Oral 36 mg Tablet Oral 54 mg Tablet, film coated Oral 18 mg Tablet, film coated Oral 27 mg Tablet, film coated Oral 36 mg Tablet, film coated Oral 54 mg Tablet Auricular (otic) 44.280 mg Tablet, orally disintegrating Oral 17.3 mg/1 Tablet, orally disintegrating Oral 25.9 mg/1 Tablet, orally disintegrating Oral 8.6 mg/1 Patch Transdermal 10 mg/9h Patch Transdermal 15 mg/9h Patch Transdermal 20 mg/9h Patch Transdermal 30 mg/9h Capsule Oral 10 MG Capsule Oral 30 MG Capsule Oral 40 MG Capsule Oral 50 MG Capsule Oral 60 MG Capsule Oral 100 mg/1 Capsule Oral 20 mg/1 Capsule Oral 40 mg/1 Capsule Oral 60 mg/1 Capsule Oral 80 mg/1 Tablet Oral Capsule Oral 5 MG Capsule, extended release Oral 5 MG Capsule Oral 34.6000 mg Capsule, delayed release pellets Oral 10 mg Capsule, delayed release pellets Oral 20 mg Capsule, delayed release pellets Oral 30 mg Capsule, delayed release pellets Oral 40 mg Capsule, delayed release pellets Oral 5 mg Capsule, delayed release Oral 10 mg Capsule Oral Capsule, delayed release Oral 20 mg Capsule, delayed release Oral 30 mg Capsule, delayed release Oral 40 mg Capsule, delayed release Oral 5 mg Capsule, delayed release Oral 50 mg Capsule, delayed release Oral 60 mg Tablet, extended release Oral 10 mg/1 Capsule, extended release Oral 10 mg/1 Capsule, extended release Oral 20 mg/1 Capsule, extended release Oral 30 mg/1 Capsule, extended release Oral 50 mg/1 Tablet Oral 2.5 mg/1 Tablet, chewable Oral 10 mg/1 Tablet, chewable Oral 2.5 mg/1 Tablet, chewable Oral 5 mg/1 Patch Transdermal 1.1 mg/1h Patch Transdermal 1.6 mg/1h Patch Transdermal 2.2 mg/1h Patch Transdermal 3.3 mg/1h Tablet Oral 20 mg/1 Tablet Oral 5 mg/1 Capsule, extended release Oral 40 mg/1 Capsule, extended release Oral 60 mg/1 Solution Oral 1 mg/1mL Solution Oral 10 mg/5mL Solution Oral 10 mg/10mL Solution Oral 2 mg/1mL Solution Oral 5 mg/5mL Tablet Oral 10 mg/1 Tablet Oral 18 mg/1 Tablet Oral 27 mg/1 Tablet Oral 36 mg/1 Tablet Oral 54 mg/1 Tablet, extended release Oral 20 mg/1 Tablet, extended release Oral 45 mg/1 Tablet, extended release Oral 63 mg/1 Tablet, extended release Oral 72 mg/1 Tablet, film coated, extended release Oral 18 mg/1 Tablet, film coated, extended release Oral 27 mg/1 Tablet, film coated, extended release Oral 36 mg/1 Tablet, film coated, extended release Oral 54 mg/1 Tablet, film coated, extended release Oral 20 mg/1 Patch Transdermal 27.5 mg/1mg Patch Transdermal 41.3 mg/1mg Patch Transdermal 55 mg/1mg Patch Transdermal 82.5 mg/1mg Tablet Oral 10.00 mg Tablet Oral 20.00 mg Tablet Oral 5.00 mg Tablet Oral 10 mg Tablet Oral 20 mg Tablet Oral 5 mg Tablet, chewable, extended release Oral 20 mg/1 Tablet, chewable, extended release Oral 30 mg/1 Tablet, chewable, extended release Oral 40 mg/1 Powder Oral 5 mg / mL Suspension, extended release Oral 300 mg/60mL Suspension, extended release Oral 600 mg/120mL Suspension, extended release Oral 750 mg/150mL Suspension, extended release Oral 900 mg/180mL Capsule, extended release Oral 5.000 mg Capsule Oral 20 mg Tablet, film coated Oral 20 mg Tablet, extended release Oral 20 mg Tablet Oral 10.000 mg Tablet Oral 18.000 mg - Prices
Unit description Cost Unit Daytrana 30 15 mg/9hr Patches Box 175.64USD box Daytrana 30 30 mg/9hr Patches Box 174.73USD box Daytrana 30 10 mg/9hr Patches Box 172.78USD box Daytrana 30 20 mg/9hr Patches Box 168.72USD box Methylphenidate hcl powder 44.62USD g Concerta er 54 mg tablet 25.45USD tablet Concerta er 36 mg tablet 23.38USD tablet Concerta er 27 mg tablet 22.65USD tablet Concerta er 18 mg tablet 22.11USD tablet Metadate cd 50 mg capsule 7.08USD capsule Metadate cd 60 mg capsule 7.02USD capsule Concerta 54 mg Controlled Release Tabs 6.18USD tab Metadate cd 40 mg capsule 5.77USD capsule Concerta 36 mg Controlled Release Tabs 5.72USD tab Focalin xr 30 mg capsule 5.42USD capsule Focalin XR 20 mg 24 Hour Capsule 5.31USD capsule Daytrana 10 mg/9 hr patch 5.16USD patch Daytrana 15 mg/9 hr patch 5.16USD patch Daytrana 20 mg/9 hour patch 5.16USD patch Daytrana 30 mg/9 hour patch 5.16USD patch Focalin xr 15 mg capsule 5.16USD capsule Focalin xr 20 mg capsule 5.16USD capsule Focalin XR 30 mg 24 Hour Capsule 5.15USD capsule Focalin xr 10 mg capsule 5.02USD capsule Concerta 18 mg Controlled Release Tabs 5.0USD tab Concerta 27 mg Controlled Release Tabs 5.0USD tab Focalin XR 10 mg 24 Hour Capsule 4.96USD capsule Focalin xr 5 mg capsule 4.95USD capsule Concerta 54 mg tablet sa 4.91USD tablet Focalin XR 15 mg 24 Hour Capsule 4.89USD capsule Focalin XR 5 mg 24 Hour Capsule 4.83USD capsule Ritalin la 40 mg capsule 4.55USD capsule Concerta 36 mg tablet sa 4.51USD tablet Ritalin la 30 mg capsule 4.43USD capsule Ritalin LA 10 mg 24 Hour Capsule 4.42USD capsule Ritalin LA 20 mg 24 Hour Capsule 4.42USD capsule Ritalin LA 30 mg 24 Hour Capsule 4.42USD capsule Ritalin LA 40 mg 24 Hour Capsule 4.42USD capsule Concerta 27 mg tablet sa 4.37USD tablet Ritalin la 10 mg capsule 4.33USD capsule Ritalin la 20 mg capsule 4.33USD capsule Concerta 18 mg tablet sa 4.27USD tablet Metadate cd 20 mg capsule 4.24USD capsule Metadate cd 30 mg capsule 4.24USD capsule Metadate cd 10 mg capsule 4.2USD capsule Methylphenidate er 10 mg tablet 3.24USD tablet Ritalin SR 20 mg Controlled Release Tabs 3.0USD tab Ritalin sr 20 mg tablet 2.67USD tablet Ritalin 20 mg tablet 1.87USD tablet Focalin 10 mg tablet 1.7USD tablet Ritalin 5 mg tablet 1.42USD tablet Metadate er 20 mg tablet 1.32USD tablet Methylin ER 20 mg Controlled Release Tabs 1.3USD tab Ritalin 10 mg tablet 1.29USD tablet Metadate er 10 mg tablet sa 1.28USD tablet Focalin 5 mg tablet 1.26USD tablet Methylphenidate HCl CR 20 mg Controlled Release Tabs 1.2USD tab Methylin er 20 mg tablet 1.12USD tablet Methylphenidate HCl 20 mg tablet 1.05USD tablet Methylin ER 10 mg 1.0USD tab Methylphenidate HCl 10 mg tablet 0.95USD tablet Methylphenidate HCl 5 mg tablet 0.94USD tablet Methylin er 10 mg tablet 0.84USD tablet Focalin 2.5 mg tablet 0.76USD tablet Methylin 20 mg tablet 0.69USD tablet Methylphenidate 20 mg tablet 0.69USD tablet Ritalin 20 mg Tablet 0.67USD tablet Ritalin Sr 20 mg Extended-Release Tablet 0.67USD tablet Methylin 10 mg tablet 0.48USD tablet Methylphenidate 10 mg tablet 0.48USD tablet Ritalin 10 mg Tablet 0.38USD tablet Apo-Methylphenidate 20 mg Tablet 0.37USD tablet Apo-Methylphenidate Sr 20 mg Extended-Release Tablet 0.37USD tablet Pms-Methylphenidate 20 mg Tablet 0.37USD tablet Sandoz Methylphenidate 20 mg Extended-Release Tablet 0.37USD tablet Methylin 5 mg tablet 0.33USD tablet Methylphenidate 5 mg tablet 0.33USD tablet Apo-Methylphenidate 10 mg Tablet 0.17USD tablet Pms-Methylphenidate 10 mg Tablet 0.17USD tablet Pms-Methylphenidate 5 mg Tablet 0.1USD tablet DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region US5958446 No 1999-09-28 2012-12-12 US CA2355644 No 2009-01-20 2019-12-17 Canada 
CA2264852 No 2005-11-01 2017-09-16 Canada US8999386 No 2015-04-07 2033-04-14 US US6919373 Yes 2005-07-19 2018-01-31 US US6930129 Yes 2005-08-16 2018-01-31 US US9000038 Yes 2015-04-07 2018-01-31 US US9144549 No 2015-09-29 2017-07-31 US US9029416 No 2015-05-12 2017-07-31 US US8163798 Yes 2012-04-24 2018-01-31 US US8629179 Yes 2014-01-14 2018-01-31 US US6344215 No 2002-02-05 2020-10-27 US US6228398 No 2001-05-08 2019-11-01 US US6635284 No 2003-10-21 2015-12-04 US US7431944 No 2008-10-07 2015-12-04 US US5837284 No 1998-11-17 2015-12-04 US US7691880 No 2010-04-06 2024-10-07 US US6210705 No 2001-04-03 2018-09-30 US US6348211 No 2002-02-19 2018-09-30 US US8632802 No 2014-01-21 2025-10-07 US US9034370 No 2015-05-19 2025-10-07 US US8062667 No 2011-11-22 2029-03-29 US US8465765 No 2013-06-18 2031-02-15 US US8778390 No 2014-07-15 2031-02-15 US US8563033 No 2013-10-22 2031-02-15 US US8956649 No 2015-02-17 2031-02-15 US US9040083 No 2015-05-26 2031-02-15 US US8287903 No 2012-10-16 2031-02-15 US US9295642 No 2016-03-29 2033-08-14 US US8202537 No 2012-06-19 2027-03-15 US US7438930 Yes 2008-10-21 2020-06-16 US US9066869 Yes 2015-06-30 2020-06-16 US US7247318 Yes 2007-07-24 2020-06-16 US US7083808 Yes 2006-08-01 2020-06-16 US US6419960 Yes 2002-07-16 2020-06-16 US US8580310 Yes 2013-11-12 2020-06-16 US US8840924 No 2014-09-23 2026-06-05 US US9668981 No 2017-06-06 2025-10-07 US US9545399 No 2017-01-17 2033-08-14 US US9089496 No 2015-07-28 2032-06-28 US US9072680 No 2015-07-07 2032-06-28 US US9844544 No 2017-12-19 2033-08-14 US US9801823 Yes 2017-10-31 2020-06-16 US US10039719 Yes 2018-08-07 2020-06-16 US US9498447 No 2016-11-22 2032-03-23 US US9283214 No 2016-03-15 2032-03-23 US US9023389 No 2015-05-05 2032-03-23 US US8927010 No 2015-01-06 2032-03-23 US US9028868 No 2015-05-12 2032-03-23 US US9034902 No 2015-05-19 2032-03-23 US US9603809 No 2017-03-28 2032-03-23 US US8916588 No 2014-12-23 2032-03-23 US US10182995 No 2019-01-22 2032-03-23 US US10111839 No 2018-10-30 2035-10-30 US US9974752 No 2018-05-22 2035-10-30 US US10292939 No 2019-05-21 2035-10-30 US US10292938 No 2019-05-21 2035-10-30 US US10292937 No 2019-05-21 2032-03-23 US US10449159 No 2019-10-22 2035-10-30 US US10463624 No 2019-11-05 2019-12-16 US US10512613 No 2019-12-24 2035-10-30 US US10500162 No 2019-12-10 2035-10-30 US US10507186 No 2019-12-17 2035-10-30 US US10512612 No 2019-12-24 2035-10-30 US US10568841 No 2020-02-25 2035-10-30 US US10617651 No 2020-04-14 2032-03-23 US US10688060 No 2020-06-23 2035-10-30 US US10722473 No 2020-07-28 2038-11-19 US US10857143 No 2020-12-08 2033-08-14 US US10881618 No 2021-01-05 2032-03-23 US US10905652 No 2021-02-02 2032-03-23 US US11103495 No 2021-08-31 2033-08-14 US US11103494 No 2021-08-31 2033-08-14 US US11166947 No 2021-11-09 2038-01-25 US US11241391 No 2012-03-23 2032-03-23 US US11241392 No 2012-03-23 2032-03-23 US US11633389 No 2013-08-14 2033-08-14 US US11911518 No 2012-03-23 2032-03-23 US
Properties
- State
- Solid
- Experimental Properties
Property Value Source water solubility 1255mg/L Not Available - Predicted Properties
Property Value Source Water Solubility 0.182 mg/mL ALOGPS logP 1.47 ALOGPS logP 2.25 Chemaxon logS -3.1 ALOGPS pKa (Strongest Basic) 9.09 Chemaxon Physiological Charge 1 Chemaxon Hydrogen Acceptor Count 2 Chemaxon Hydrogen Donor Count 1 Chemaxon Polar Surface Area 38.33 Å2 Chemaxon Rotatable Bond Count 4 Chemaxon Refractivity 66.73 m3·mol-1 Chemaxon Polarizability 25.91 Å3 Chemaxon Number of Rings 2 Chemaxon Bioavailability 1 Chemaxon Rule of Five Yes Chemaxon Ghose Filter Yes Chemaxon Veber's Rule Yes Chemaxon MDDR-like Rule No Chemaxon - Predicted ADMET Features
Property Value Probability Human Intestinal Absorption + 0.9941 Blood Brain Barrier + 0.9663 Caco-2 permeable + 0.6564 P-glycoprotein substrate Substrate 0.5466 P-glycoprotein inhibitor I Non-inhibitor 0.7964 P-glycoprotein inhibitor II Non-inhibitor 0.9601 Renal organic cation transporter Inhibitor 0.532 CYP450 2C9 substrate Non-substrate 0.7897 CYP450 2D6 substrate Non-substrate 0.9116 CYP450 3A4 substrate Non-substrate 0.5985 CYP450 1A2 substrate Non-inhibitor 0.592 CYP450 2C9 inhibitor Non-inhibitor 0.897 CYP450 2D6 inhibitor Non-inhibitor 0.5245 CYP450 2C19 inhibitor Non-inhibitor 0.9265 CYP450 3A4 inhibitor Non-inhibitor 0.8539 CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.9328 Ames test Non AMES toxic 0.9133 Carcinogenicity Non-carcinogens 0.9648 Biodegradation Not ready biodegradable 0.5759 Rat acute toxicity 2.7718 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.8466 hERG inhibition (predictor II) Non-inhibitor 0.7491
Spectra
- Mass Spec (NIST)
- Download (7.79 KB)
- Spectra
- Chromatographic Properties
Collision Cross Sections (CCS)
Adduct CCS Value (Å2) Source type Source [M-H]- 163.3366387 predictedDarkChem Lite v0.1.0 [M-H]- 152.06747 predictedDeepCCS 1.0 (2019) [M+H]+ 163.9146387 predictedDarkChem Lite v0.1.0 [M+H]+ 154.42548 predictedDeepCCS 1.0 (2019) [M+Na]+ 163.6404387 predictedDarkChem Lite v0.1.0 [M+Na]+ 160.51863 predictedDeepCCS 1.0 (2019)
Targets
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Inhibitor
- General Function
- Mediates sodium- and chloride-dependent transport of dopamine (PubMed:10375632, PubMed:11093780, PubMed:1406597, PubMed:15505207, PubMed:19478460, PubMed:8302271). Also mediates sodium- and chloride-dependent transport of norepinephrine (also known as noradrenaline) (By similarity). Regulator of light-dependent retinal hyaloid vessel regression, downstream of OPN5 signaling (By similarity)
- Specific Function
- amine binding
- Gene Name
- SLC6A3
- Uniprot ID
- Q01959
- Uniprot Name
- Sodium-dependent dopamine transporter
- Molecular Weight
- 68494.255 Da
References
- Volkow ND, Fowler JS, Gatley SJ, Dewey SL, Wang GJ, Logan J, Ding YS, Franceschi D, Gifford A, Morgan A, Pappas N, King P: Comparable changes in synaptic dopamine induced by methylphenidate and by cocaine in the baboon brain. Synapse. 1999 Jan;31(1):59-66. [Article]
- Wayment HK, Deutsch H, Schweri MM, Schenk JO: Effects of methylphenidate analogues on phenethylamine substrates for the striatal dopamine transporter: potential as amphetamine antagonists? J Neurochem. 1999 Mar;72(3):1266-74. [Article]
- Dresel SH, Kung MP, Huang X, Plossl K, Hou C, Shiue CY, Karp J, Kung HF: In vivo imaging of serotonin transporters with [99mTc]TRODAT-1 in nonhuman primates. Eur J Nucl Med. 1999 Apr;26(4):342-7. [Article]
- Volkow ND, Wang GJ, Fowler JS, Fischman M, Foltin R, Abumrad NN, Gatley SJ, Logan J, Wong C, Gifford A, Ding YS, Hitzemann R, Pappas N: Methylphenidate and cocaine have a similar in vivo potency to block dopamine transporters in the human brain. Life Sci. 1999;65(1):PL7-12. [Article]
- Izenwasser S, Coy AE, Ladenheim B, Loeloff RJ, Cadet JL, French D: Chronic methylphenidate alters locomotor activity and dopamine transporters differently from cocaine. Eur J Pharmacol. 1999 Jun 4;373(2-3):187-93. [Article]
- Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
- Tatsumi M, Groshan K, Blakely RD, Richelson E: Pharmacological profile of antidepressants and related compounds at human monoamine transporters. Eur J Pharmacol. 1997 Dec 11;340(2-3):249-58. [Article]
- Viggiano D, Vallone D, Sadile A: Dysfunctions in dopamine systems and ADHD: evidence from animals and modeling. Neural Plast. 2004;11(1-2):97-114. [Article]
- Tilley MR, Gu HH: The effects of methylphenidate on knockin mice with a methylphenidate-resistant dopamine transporter. J Pharmacol Exp Ther. 2008 Nov;327(2):554-60. doi: 10.1124/jpet.108.141713. Epub 2008 Aug 12. [Article]
- Markowitz JS, DeVane CL, Pestreich LK, Patrick KS, Muniz R: A comprehensive in vitro screening of d-, l-, and dl-threo-methylphenidate: an exploratory study. J Child Adolesc Psychopharmacol. 2006 Dec;16(6):687-98. [Article]
- Berridge CW, Devilbiss DM, Andrzejewski ME, Arnsten AF, Kelley AE, Schmeichel B, Hamilton C, Spencer RC: Methylphenidate preferentially increases catecholamine neurotransmission within the prefrontal cortex at low doses that enhance cognitive function. Biol Psychiatry. 2006 Nov 15;60(10):1111-20. doi: 10.1016/j.biopsych.2006.04.022. Epub 2006 Jun 23. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- General Function
- G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various drugs and psychoactive substances. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors, such as adenylate cyclase. Beta-arrestin family members inhibit signaling via G proteins and mediate activation of alternative signaling pathways. Signaling inhibits adenylate cyclase activity and activates a phosphatidylinositol-calcium second messenger system that regulates the release of Ca(2+) ions from intracellular stores. Plays a role in the regulation of 5-hydroxytryptamine release and in the regulation of dopamine and 5-hydroxytryptamine metabolism. Plays a role in the regulation of dopamine and 5-hydroxytryptamine levels in the brain, and thereby affects neural activity, mood and behavior. Plays a role in the response to anxiogenic stimuli
- Specific Function
- G protein-coupled serotonin receptor activity
- Gene Name
- HTR1A
- Uniprot ID
- P08908
- Uniprot Name
- 5-hydroxytryptamine receptor 1A
- Molecular Weight
- 46106.335 Da
References
- Markowitz JS, DeVane CL, Ramamoorthy S, Zhu HJ: The psychostimulant d-threo-(R,R)-methylphenidate binds as an agonist to the 5HT(1A) receptor. Pharmazie. 2009 Feb;64(2):123-5. [Article]
- Markowitz JS, DeVane CL, Pestreich LK, Patrick KS, Muniz R: A comprehensive in vitro screening of d-, l-, and dl-threo-methylphenidate: an exploratory study. J Child Adolesc Psychopharmacol. 2006 Dec;16(6):687-98. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Mediates sodium- and chloride-dependent transport of norepinephrine (also known as noradrenaline) (PubMed:2008212, PubMed:8125921). Can also mediate sodium- and chloride-dependent transport of dopamine (PubMed:11093780, PubMed:8125921)
- Specific Function
- actin binding
- Gene Name
- SLC6A2
- Uniprot ID
- P23975
- Uniprot Name
- Sodium-dependent noradrenaline transporter
- Molecular Weight
- 69331.42 Da
References
- Yang L, Wang YF, Li J, Faraone SV: Association of norepinephrine transporter gene with methylphenidate response. J Am Acad Child Adolesc Psychiatry. 2004 Sep;43(9):1154-8. [Article]
- Williard RL, Middaugh LD, Zhu HJ, Patrick KS: Methylphenidate and its ethanol transesterification metabolite ethylphenidate: brain disposition, monoamine transporters and motor activity. Behav Pharmacol. 2007 Feb;18(1):39-51. [Article]
- Chuhan YS, Taukulis HK: Impairment of single-trial memory formation by oral methylphenidate in the rat. Neurobiol Learn Mem. 2006 Mar;85(2):125-31. Epub 2005 Oct 24. [Article]
- Gray JD, Punsoni M, Tabori NE, Melton JT, Fanslow V, Ward MJ, Zupan B, Menzer D, Rice J, Drake CT, Romeo RD, Brake WG, Torres-Reveron A, Milner TA: Methylphenidate administration to juvenile rats alters brain areas involved in cognition, motivated behaviors, appetite, and stress. J Neurosci. 2007 Jul 4;27(27):7196-207. [Article]
- Sandoval V, Riddle EL, Ugarte YV, Hanson GR, Fleckenstein AE: Methamphetamine-induced rapid and reversible changes in dopamine transporter function: an in vitro model. J Neurosci. 2001 Feb 15;21(4):1413-9. [Article]
- Tatsumi M, Groshan K, Blakely RD, Richelson E: Pharmacological profile of antidepressants and related compounds at human monoamine transporters. Eur J Pharmacol. 1997 Dec 11;340(2-3):249-58. [Article]
- Tilley MR, Gu HH: The effects of methylphenidate on knockin mice with a methylphenidate-resistant dopamine transporter. J Pharmacol Exp Ther. 2008 Nov;327(2):554-60. doi: 10.1124/jpet.108.141713. Epub 2008 Aug 12. [Article]
- Markowitz JS, DeVane CL, Pestreich LK, Patrick KS, Muniz R: A comprehensive in vitro screening of d-, l-, and dl-threo-methylphenidate: an exploratory study. J Child Adolesc Psychopharmacol. 2006 Dec;16(6):687-98. [Article]
- Berridge CW, Devilbiss DM, Andrzejewski ME, Arnsten AF, Kelley AE, Schmeichel B, Hamilton C, Spencer RC: Methylphenidate preferentially increases catecholamine neurotransmission within the prefrontal cortex at low doses that enhance cognitive function. Biol Psychiatry. 2006 Nov 15;60(10):1111-20. doi: 10.1016/j.biopsych.2006.04.022. Epub 2006 Jun 23. [Article]
Enzymes
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Not Available
- Specific Function
- hydrolase activity
- Gene Name
- CES1A1a
- Uniprot ID
- Q6LAP9
- Uniprot Name
- Carboxylesterase
- Molecular Weight
- 1908.25 Da
References
- Sun Z, Murry DJ, Sanghani SP, Davis WI, Kedishvili NY, Zou Q, Hurley TD, Bosron WF: Methylphenidate is stereoselectively hydrolyzed by human carboxylesterase CES1A1. J Pharmacol Exp Ther. 2004 Aug;310(2):469-76. doi: 10.1124/jpet.104.067116. Epub 2004 Apr 13. [Article]
Drug created at June 13, 2005 13:24 / Updated at October 08, 2024 09:29