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Synonyms: Concerta® | Jornay PM® (a.k.a. HLD200) | Ritalin®
methylphenidate is an approved drug (FDA (1955))
Compound class: Synthetic organic
Comment: Methylphenidate is a racemic mixture of optical isomers (enantiomers). We show the chemical structure without specified stereochemistry to represent the mixture. The most active (R,R) enantiomer is the approved drug dexmethylphenidate. Methylphenidate is administered as the hydrochloride salt (PubChem CID 9280).
Ligand Activity Visualisation Charts
These are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts.✖
View more information in the IUPHAR Pharmacology Education Project: methylphenidate
|No information available.|
|Summary of Clinical Use|
|Used alongside educational and psychosocial intervention to treat attention deficit hyperactivity disorder (ADHD) and to treat narcolepsy.
An extended release, chewable formulation of methylphenidate hydrochloride (QuilliChew ER) was approved by the US FDA in December 2015. Cotempla XR-ODT, an extended-release orally disintegrating methylphenidate-containing tablet was FDA approved for ADHD in June 2017.
|Mechanism Of Action and Pharmacodynamic Effects|
|This drug blocks the reuptake of norepinephrine and dopamine into presynaptic neurons, resulting in increased levels of monoamines active in the extraneuronal space. Neurotransmitter reuptake is performed by the transporter proteins SLC6A3 (dopamine) and SLC6A2 (norepinephrine). As these neurotransmitters are involved in maintaining alertness and sustaining thought and motivation this action may underlie the clinical benefits in ADHD. However the full molecular mechanism of action remains to be fully resolved. See the DrugBank link for further details.|
For extended ADME data see the following:
Electronic Medicines Compendium (eMC)