Overview
| Generic Names: | Methyl phenidyl acetate; Methylphenidate HCl; Methylphenidate hydrochloride; Methylphenidatum [INN-Latin]; Methylphenidylacetate hydrochloride; Metilfenidat hydrochloride; Metilfenidato [INN-Spanish]; Metilfenidato [Italian]; Phenidylate; d-methylphenidate HCl; methylphenidate |
|---|---|
| Trade Names: | 4311/B Ciba; Calocain; Centedein; Centedrin; Centedrine; Centredin; Concerta; Daytrana; Focalin; Focalin XR; Meridil; Metadate; Metadate CD; Metadate ER; Methylin; Methylin ER; Methylofenidan; Methylphen; Methylphenidan; Methypatch; PMS-Methylphenidate; Plimasine; Riphenidate; Ritalin; Ritalin LA; Ritalin SR; Ritalin hydrochloride; Ritalin-SR; Ritaline; Ritcher Works |
| PharmGKB Accession Id: | PA450464 |
Description
A central nervous system stimulant used most commonly in the treatment of attention-deficit disorders in children and for narcolepsy. Its mechanisms appear to be similar to those of dextroamphetamine. PubChem (source: Drug Bank)
Indication
For use as an integral part of a total treatment program which typically includes other remedial measures (psychological, educational, social) for a stabilizing effect in children with a behavioral syndrome characterized by the following group of developmentally inappropriate symptoms: moderate-to-severe distractibility, short attention span, hyperactivity, emotional lability, and impulsivity. (source: Drug Bank)
ATC Therapeutic Category
- N06BA:Centrally acting sympathomimetics
Pharmacology, Interactions, and Contraindications
Mechanism Of Action
Methylphenidate blocks dopamine uptake in central adrenergic neurons by blocking dopamine transport or carrier proteins. Methylphenidate acts at the brain stem arousal system and the cerebral cortex and causes increased sympathomimetic activity in the central nervous system. Alteration of serotonergic pathways via changes in dopamine transport may result. (source: Drug Bank)
Pharmacology
Methylphenidate is a central nervous system stimulant used most commonly in the treatment of attention-deficit disorders in children and for narcolepsy. Its mechanisms appear to be similar to those of dextroamphetamine. (source: Drug Bank)
Food Interactions
Avoid alcohol.
Avoid excessive quantities of coffee or tea (Caffeine).
Take on empty stomach: 1 hour before or 2 hours after meals.
(source:
Drug Bank)
Absorption, Distribution, Metabolism, Elimination & Toxicity
Biotransformation
Hepatic, methylphenidate is metabolized primarily by de-esterification to ritalinic acid (α-phenyl-2-piperidine acetic acid, PPAA), which has little to no pharmacologic activity. (source: Drug Bank)
Protein Binding
Low (approximately 15%) (source: Drug Bank)
Absorption
Readily absorbed in a biphasic manner. It reaches peak absorption at approximately two hours for the first phase and five hours for the second phase. Bioavailability is low (approximately 30%) (source: Drug Bank)
Toxicity
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. LD<sub>50</sub>=190mg/kg (orally in mice) (source: Drug Bank)
Isomeric SMILES Code:
COC(=O)C(c1ccccc1)C2CCCCN2 (source: Drug Bank)
The following genes are in curated knowledge about this drug.
| Gene | Relationship | Evidence | |
|---|---|---|---|
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ADRA2A |
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Publications |
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CES1 |
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Publications |
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COMT |
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Publications |
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DRD4 |
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Publications |
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SLC6A3 |
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Publications |
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SNAP25 |
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Publications |
A list of non-curated publications that mention this drug along with other genes is available.
Drug Targets
| Gene | Description | |
|---|---|---|
| SLC6A3 |
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(source: Drug Bank) |
| SLC6A2 |
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(source: Drug Bank) |
| SLC6A4 |
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(source: Drug Bank) |
The following drugs are in curated knowledge about this drug.
| Drug | Relationship | Evidence | |
|---|---|---|---|
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warfarin |
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Publications |
A list of non-curated publications that mention this drug along with other drugs is available.
Drug Interactions
| Drug | Description | |
|---|---|---|
| carbamazepine |
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Carbamazepine could reduce the effect of methylphendiate (source: Drug Bank) |
| cyclosporine |
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Methylphenidate increases the effect and toxicity of cyclosporine (source: Drug Bank) |
| guanethidine |
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The agent decreases the effect of guanethidine (source: Drug Bank) |
| isocarboxazid |
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Possible hypertensive crisis with this combination (source: Drug Bank) |
| phenelzine |
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Possible hypertensive crisis with this combination (source: Drug Bank) |
| tranylcypromine |
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Possible hypertensive crisis with this combination (source: Drug Bank) |
Curated Information
The following diseases are in curated knowledge about this drug.
| Disease | Relationship | Evidence | |
|---|---|---|---|
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Attention Deficit Disorder with Hyperactivity |
|
Publications |
Non-Curated Information
A list of non-curated publications that mention this drug along with other diseases is available.
Additional Datasets
These datasets are minimally curated and are sorted alphabetically by title.
LinkOuts
Common Searches
Search PubMed
Search Medline Plus
Search PubChem
Search CTD
Non-Curated Publications
A list of non-curated publications that mention this drug is available.
