Details
| Stereochemistry | ABSOLUTE |
| Molecular Formula | C14H19NO2 |
| Molecular Weight | 233.3062 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 2 / 2 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
[H][C@]1(CCCCN1)[C@@H](C(=O)OC)C2=CC=CC=C2
InChI
InChIKey=DUGOZIWVEXMGBE-STQMWFEESA-N
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/t12-,13-/m0/s1
Methylphenidate is a CNS stimulant approved for the treatment of narcolepsy and attention deficit hyperactivity disorder. The drug is believed to bind the dopamine transporter in the presynaptic cell membrane, thereby blocking the reuptake of dopamine and causing an increase in extracellular dopamine levels.
Originator
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
Target ID: Q01959 Gene ID: 6531.0 Gene Symbol: SLC6A3 Target Organism: Homo sapiens (Human) |
Conditions
| Condition | Modality | Targets | Highest Phase | Product |
|---|---|---|---|---|
| Primary | RITALIN Approved UseRitalin is indicated for the treatment of Attention Deficit Disorders and Narcolepsy. Launch Date1955 |
|||
| Primary | RITALIN Approved UseRitalin is indicated for the treatment of Attention Deficit Disorders and Narcolepsy. Launch Date1955 |
Cmax
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
3.7 ng/mL |
18 mg single, oral dose: 18 mg route of administration: Oral experiment type: SINGLE co-administered: |
METHYLPHENIDATE HYDROCHLORIDE plasma | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
AUC
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
41.8 ng × h/mL |
18 mg single, oral dose: 18 mg route of administration: Oral experiment type: SINGLE co-administered: |
METHYLPHENIDATE HYDROCHLORIDE plasma | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
T1/2
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
3.5 h |
18 mg single, oral dose: 18 mg route of administration: Oral experiment type: SINGLE co-administered: |
METHYLPHENIDATE HYDROCHLORIDE plasma | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
Funbound
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
90% |
unknown, unknown |
METHYLPHENIDATE HYDROCHLORIDE plasma | Homo sapiens population: UNKNOWN age: UNKNOWN sex: UNKNOWN food status: UNKNOWN |
Doses
| Dose | Population | Adverse events |
|---|---|---|
700 mg multiple, oral Studied dose Dose: 700 mg Route: oral Route: multiple Dose: 700 mg Sources: |
unhealthy, 45 years n = 1 Health Status: unhealthy Condition: Attention Deficit Hyperactivity Disorders Age Group: 45 years Sex: M Population Size: 1 Sources: |
Other AEs: Abuse... |
210 mg 1 times / day single, oral Studied dose Dose: 210 mg, 1 times / day Route: oral Route: single Dose: 210 mg, 1 times / day Sources: |
unhealthy, 8 years n = 1 Health Status: unhealthy Condition: Attention Deficit Hyperactivity Disorders Age Group: 8 years Sex: F Population Size: 1 Sources: |
Other AEs: Hypertension, Tachycardia... Other AEs: Hypertension (grade 1) Sources: Tachycardia (grade 1) Confusion Irritability Agitation Hallucinations |
15 mg 2 times / day single, oral (mean) Recommended Dose: 15 mg, 2 times / day Route: oral Route: single Dose: 15 mg, 2 times / day Sources: Page: nda/2002/21-284_Ritalin%20LA_medr.pdf - p.15 |
healthy, mean age 30 years n = 61 Health Status: healthy Age Group: mean age 30 years Sex: M+F Population Size: 61 Sources: Page: nda/2002/21-284_Ritalin%20LA_medr.pdf - p.15 |
Disc. AE: Headache, Nausea... AEs leading to discontinuation/dose reduction: Headache (1.6%) Sources: Page: nda/2002/21-284_Ritalin%20LA_medr.pdf - p.15Nausea (1.6%) Hot flushes (1.6%) Panic attack (1.6%) Nausea (1.6%) Vomiting (1.6%) Dizziness (1.6%) |
12.5 mg 2 times / day multiple, oral (mean) Recommended Dose: 12.5 mg, 2 times / day Route: oral Route: multiple Dose: 12.5 mg, 2 times / day Sources: Page: nda/2002/21-284_Ritalin%20LA_medr.pdf - p.15 |
unhealthy, median age 9 years n = 65 Health Status: unhealthy Condition: Attention Deficit Hyperactivity Disorders Age Group: median age 9 years Sex: M+F Population Size: 65 Sources: Page: nda/2002/21-284_Ritalin%20LA_medr.pdf - p.15 |
Disc. AE: Fatigue, Lethargy... AEs leading to discontinuation/dose reduction: Fatigue (1.5%) Sources: Page: nda/2002/21-284_Ritalin%20LA_medr.pdf - p.15Lethargy (1.5%) Hypomania (1.5%) Anger (1.5%) Anxiety (1.5%) Migraine (1.5%) Depression (1.5%) |
AEs
| AE | Significance | Dose | Population |
|---|---|---|---|
| Abuse | 700 mg multiple, oral Studied dose Dose: 700 mg Route: oral Route: multiple Dose: 700 mg Sources: |
unhealthy, 45 years n = 1 Health Status: unhealthy Condition: Attention Deficit Hyperactivity Disorders Age Group: 45 years Sex: M Population Size: 1 Sources: |
|
| Agitation | 210 mg 1 times / day single, oral Studied dose Dose: 210 mg, 1 times / day Route: oral Route: single Dose: 210 mg, 1 times / day Sources: |
unhealthy, 8 years n = 1 Health Status: unhealthy Condition: Attention Deficit Hyperactivity Disorders Age Group: 8 years Sex: F Population Size: 1 Sources: |
|
| Confusion | 210 mg 1 times / day single, oral Studied dose Dose: 210 mg, 1 times / day Route: oral Route: single Dose: 210 mg, 1 times / day Sources: |
unhealthy, 8 years n = 1 Health Status: unhealthy Condition: Attention Deficit Hyperactivity Disorders Age Group: 8 years Sex: F Population Size: 1 Sources: |
|
| Hallucinations | 210 mg 1 times / day single, oral Studied dose Dose: 210 mg, 1 times / day Route: oral Route: single Dose: 210 mg, 1 times / day Sources: |
unhealthy, 8 years n = 1 Health Status: unhealthy Condition: Attention Deficit Hyperactivity Disorders Age Group: 8 years Sex: F Population Size: 1 Sources: |
|
| Irritability | 210 mg 1 times / day single, oral Studied dose Dose: 210 mg, 1 times / day Route: oral Route: single Dose: 210 mg, 1 times / day Sources: |
unhealthy, 8 years n = 1 Health Status: unhealthy Condition: Attention Deficit Hyperactivity Disorders Age Group: 8 years Sex: F Population Size: 1 Sources: |
|
| Hypertension | grade 1 | 210 mg 1 times / day single, oral Studied dose Dose: 210 mg, 1 times / day Route: oral Route: single Dose: 210 mg, 1 times / day Sources: |
unhealthy, 8 years n = 1 Health Status: unhealthy Condition: Attention Deficit Hyperactivity Disorders Age Group: 8 years Sex: F Population Size: 1 Sources: |
| Tachycardia | grade 1 | 210 mg 1 times / day single, oral Studied dose Dose: 210 mg, 1 times / day Route: oral Route: single Dose: 210 mg, 1 times / day Sources: |
unhealthy, 8 years n = 1 Health Status: unhealthy Condition: Attention Deficit Hyperactivity Disorders Age Group: 8 years Sex: F Population Size: 1 Sources: |
| Dizziness | 1.6% Disc. AE |
15 mg 2 times / day single, oral (mean) Recommended Dose: 15 mg, 2 times / day Route: oral Route: single Dose: 15 mg, 2 times / day Sources: Page: nda/2002/21-284_Ritalin%20LA_medr.pdf - p.15 |
healthy, mean age 30 years n = 61 Health Status: healthy Age Group: mean age 30 years Sex: M+F Population Size: 61 Sources: Page: nda/2002/21-284_Ritalin%20LA_medr.pdf - p.15 |
| Headache | 1.6% Disc. AE |
15 mg 2 times / day single, oral (mean) Recommended Dose: 15 mg, 2 times / day Route: oral Route: single Dose: 15 mg, 2 times / day Sources: Page: nda/2002/21-284_Ritalin%20LA_medr.pdf - p.15 |
healthy, mean age 30 years n = 61 Health Status: healthy Age Group: mean age 30 years Sex: M+F Population Size: 61 Sources: Page: nda/2002/21-284_Ritalin%20LA_medr.pdf - p.15 |
| Hot flushes | 1.6% Disc. AE |
15 mg 2 times / day single, oral (mean) Recommended Dose: 15 mg, 2 times / day Route: oral Route: single Dose: 15 mg, 2 times / day Sources: Page: nda/2002/21-284_Ritalin%20LA_medr.pdf - p.15 |
healthy, mean age 30 years n = 61 Health Status: healthy Age Group: mean age 30 years Sex: M+F Population Size: 61 Sources: Page: nda/2002/21-284_Ritalin%20LA_medr.pdf - p.15 |
| Nausea | 1.6% Disc. AE |
15 mg 2 times / day single, oral (mean) Recommended Dose: 15 mg, 2 times / day Route: oral Route: single Dose: 15 mg, 2 times / day Sources: Page: nda/2002/21-284_Ritalin%20LA_medr.pdf - p.15 |
healthy, mean age 30 years n = 61 Health Status: healthy Age Group: mean age 30 years Sex: M+F Population Size: 61 Sources: Page: nda/2002/21-284_Ritalin%20LA_medr.pdf - p.15 |
| Nausea | 1.6% Disc. AE |
15 mg 2 times / day single, oral (mean) Recommended Dose: 15 mg, 2 times / day Route: oral Route: single Dose: 15 mg, 2 times / day Sources: Page: nda/2002/21-284_Ritalin%20LA_medr.pdf - p.15 |
healthy, mean age 30 years n = 61 Health Status: healthy Age Group: mean age 30 years Sex: M+F Population Size: 61 Sources: Page: nda/2002/21-284_Ritalin%20LA_medr.pdf - p.15 |
| Panic attack | 1.6% Disc. AE |
15 mg 2 times / day single, oral (mean) Recommended Dose: 15 mg, 2 times / day Route: oral Route: single Dose: 15 mg, 2 times / day Sources: Page: nda/2002/21-284_Ritalin%20LA_medr.pdf - p.15 |
healthy, mean age 30 years n = 61 Health Status: healthy Age Group: mean age 30 years Sex: M+F Population Size: 61 Sources: Page: nda/2002/21-284_Ritalin%20LA_medr.pdf - p.15 |
| Vomiting | 1.6% Disc. AE |
15 mg 2 times / day single, oral (mean) Recommended Dose: 15 mg, 2 times / day Route: oral Route: single Dose: 15 mg, 2 times / day Sources: Page: nda/2002/21-284_Ritalin%20LA_medr.pdf - p.15 |
healthy, mean age 30 years n = 61 Health Status: healthy Age Group: mean age 30 years Sex: M+F Population Size: 61 Sources: Page: nda/2002/21-284_Ritalin%20LA_medr.pdf - p.15 |
| Anger | 1.5% Disc. AE |
12.5 mg 2 times / day multiple, oral (mean) Recommended Dose: 12.5 mg, 2 times / day Route: oral Route: multiple Dose: 12.5 mg, 2 times / day Sources: Page: nda/2002/21-284_Ritalin%20LA_medr.pdf - p.15 |
unhealthy, median age 9 years n = 65 Health Status: unhealthy Condition: Attention Deficit Hyperactivity Disorders Age Group: median age 9 years Sex: M+F Population Size: 65 Sources: Page: nda/2002/21-284_Ritalin%20LA_medr.pdf - p.15 |
| Anxiety | 1.5% Disc. AE |
12.5 mg 2 times / day multiple, oral (mean) Recommended Dose: 12.5 mg, 2 times / day Route: oral Route: multiple Dose: 12.5 mg, 2 times / day Sources: Page: nda/2002/21-284_Ritalin%20LA_medr.pdf - p.15 |
unhealthy, median age 9 years n = 65 Health Status: unhealthy Condition: Attention Deficit Hyperactivity Disorders Age Group: median age 9 years Sex: M+F Population Size: 65 Sources: Page: nda/2002/21-284_Ritalin%20LA_medr.pdf - p.15 |
| Depression | 1.5% Disc. AE |
12.5 mg 2 times / day multiple, oral (mean) Recommended Dose: 12.5 mg, 2 times / day Route: oral Route: multiple Dose: 12.5 mg, 2 times / day Sources: Page: nda/2002/21-284_Ritalin%20LA_medr.pdf - p.15 |
unhealthy, median age 9 years n = 65 Health Status: unhealthy Condition: Attention Deficit Hyperactivity Disorders Age Group: median age 9 years Sex: M+F Population Size: 65 Sources: Page: nda/2002/21-284_Ritalin%20LA_medr.pdf - p.15 |
| Fatigue | 1.5% Disc. AE |
12.5 mg 2 times / day multiple, oral (mean) Recommended Dose: 12.5 mg, 2 times / day Route: oral Route: multiple Dose: 12.5 mg, 2 times / day Sources: Page: nda/2002/21-284_Ritalin%20LA_medr.pdf - p.15 |
unhealthy, median age 9 years n = 65 Health Status: unhealthy Condition: Attention Deficit Hyperactivity Disorders Age Group: median age 9 years Sex: M+F Population Size: 65 Sources: Page: nda/2002/21-284_Ritalin%20LA_medr.pdf - p.15 |
| Hypomania | 1.5% Disc. AE |
12.5 mg 2 times / day multiple, oral (mean) Recommended Dose: 12.5 mg, 2 times / day Route: oral Route: multiple Dose: 12.5 mg, 2 times / day Sources: Page: nda/2002/21-284_Ritalin%20LA_medr.pdf - p.15 |
unhealthy, median age 9 years n = 65 Health Status: unhealthy Condition: Attention Deficit Hyperactivity Disorders Age Group: median age 9 years Sex: M+F Population Size: 65 Sources: Page: nda/2002/21-284_Ritalin%20LA_medr.pdf - p.15 |
| Lethargy | 1.5% Disc. AE |
12.5 mg 2 times / day multiple, oral (mean) Recommended Dose: 12.5 mg, 2 times / day Route: oral Route: multiple Dose: 12.5 mg, 2 times / day Sources: Page: nda/2002/21-284_Ritalin%20LA_medr.pdf - p.15 |
unhealthy, median age 9 years n = 65 Health Status: unhealthy Condition: Attention Deficit Hyperactivity Disorders Age Group: median age 9 years Sex: M+F Population Size: 65 Sources: Page: nda/2002/21-284_Ritalin%20LA_medr.pdf - p.15 |
| Migraine | 1.5% Disc. AE |
12.5 mg 2 times / day multiple, oral (mean) Recommended Dose: 12.5 mg, 2 times / day Route: oral Route: multiple Dose: 12.5 mg, 2 times / day Sources: Page: nda/2002/21-284_Ritalin%20LA_medr.pdf - p.15 |
unhealthy, median age 9 years n = 65 Health Status: unhealthy Condition: Attention Deficit Hyperactivity Disorders Age Group: median age 9 years Sex: M+F Population Size: 65 Sources: Page: nda/2002/21-284_Ritalin%20LA_medr.pdf - p.15 |
Overview
| CYP3A4 | CYP2C9 | CYP2D6 | hERG |
|---|---|---|---|
OverviewOther
| Other Inhibitor | Other Substrate | Other Inducer |
|---|---|---|
Drug as perpetrator
| Target | Modality | Activity | Metabolite | Clinical evidence |
|---|---|---|---|---|
| no | ||||
| no | ||||
| no | ||||
| no | ||||
| no | ||||
| no | ||||
| no |
Drug as victim
| Target | Modality | Activity | Metabolite | Clinical evidence |
|---|---|---|---|---|
| no |
Tox targets
| Target | Modality | Activity | Metabolite | Clinical evidence |
|---|---|---|---|---|
PubMed
| Title | Date | PubMed |
|---|---|---|
| Letter: Methylphenidate reaction. | 1975 Jun |
|
| Synthesis and pharmacology of site specific cocaine abuse treatment agents: a new synthetic methodology for methylphenidate analogs based on the Blaise reaction. | 2001 Apr |
|
| Toward individualized evidence-based medicine: five "N of 1" trials of methylphenidate in geriatric patients. | 2001 Apr |
|
| Pharmacotherapeutic management of autism. | 2001 Apr |
|
| Present and future pharmacotherapeutic options for adult attention deficit/hyperactivity disorder. | 2001 Apr |
|
| An adolescent who abruptly stops his medication for attention-deficit hyperactivity disorder. | 2001 Apr |
|
| The influence of a token economy and methylphenidate on attentive and disruptive behavior during sports with ADHD-diagnosed children. | 2001 Apr |
|
| Understanding Rx options for the youngest patients. | 2001 Aug |
|
| Concerns about Ritalin. | 2001 Aug |
|
| Rewarding properties of methylphenidate: sensitization by prior exposure to the drug and effects of dopamine D1- and D2-receptor antagonists. | 2001 Aug |
|
| [Methylphenidate therapy in 141 patients with hyperkinetic disorder or with pervasive developmental disorder and hyperkinesia]. | 2001 Jul |
|
| A comparison of the visual symptoms between ADD/ADHD and normal children. | 2001 Jul |
|
| Stimulant drugs for severe hyperactivity in childhood. | 2001 Jul |
|
| Rehabilitative management of post-stroke visuospatial inattention. | 2001 Jul 10 |
|
| Methylphenidate increases the motor effects of L-Dopa in Parkinson's disease: a pilot study. | 2001 Jul-Aug |
|
| Correlations between motor persistence and plasma levels in methylphenidate-treated boys with ADHD. | 2001 Jun |
|
| Advances in paediatric neuropsychopharmacology: an overview. | 2001 Jun |
|
| Adult ADHD. Controlled medication assessment. | 2001 Jun |
|
| Effect of repeated methylphenidate administration on presynaptic dopamine and behaviour in young adult rats. | 2001 Jun |
|
| Comparison in symptoms between aged and younger patients with narcolepsy. | 2001 Jun |
|
| The development of selective attention in children with attention deficit hyperactivity disorder. | 2001 Jun |
|
| Attention deficit hyperactivity disorder and substance use disorders: Is there a causal link? | 2001 Jun |
|
| Effects of TENS and methylphenidate in tuberculous meningo-encephalitis. | 2001 Jun |
|
| Explosive outbursts associated with methylphenidate. | 2001 Jun |
|
| Managing stimulant medication for attention-deficit/hyperactivity disorder. | 2001 Jun |
|
| Once-a-day Concerta methylphenidate versus three-times-daily methylphenidate in laboratory and natural settings. | 2001 Jun |
|
| Reinforcing and subject-rated effects of methylphenidate and d-amphetamine in non-drug-abusing humans. | 2001 Jun |
|
| Practice parameters for the treatment of narcolepsy: an update for 2000. | 2001 Jun 15 |
|
| Commentary on Greene and Ablon: What does the MTA study tell us about effective psychosocial treatment for ADHD? | 2001 Mar |
|
| Assessing the abuse potential of methylphenidate in nonhuman and human subjects: a review. | 2001 Mar |
|
| alpha(2C)-Adrenoceptors modulate the effect of methylphenidate on response rate and discrimination accuracy in an operant test. | 2001 Mar 15 |
|
| [Prescription of central nervous system stimulants]. | 2001 Mar 20 |
|
| [Neuropsychological follow-up of attention deficit/hyperactive disorder in adulthood before and after treatment with methylphenidate]. | 2001 May |
|
| Short-term cardiovascular effects of methylphenidate and adderall. | 2001 May |
|
| Psychostimulants in preschool children with attention-deficit/hyperactivity disorder: clinical evidence from a developmental disorders institution. | 2001 May |
|
| An auditable protocol for treating attention deficit/hyperactivity disorder. | 2001 May |
|
| Methylphenidate sensitization is modulated by valproate. | 2001 May 25 |
|
| [Is Ritalin prescribed insufficiently to hyperactive children in Nordland?]. | 2001 May 30 |
|
| Methylphenidate for fatigue in advanced cancer: a prospective open-label pilot study. | 2001 May-Jun |
|
| Gilles de la Tourette Syndrome. | 2001 May-Jun |
|
| Emergence of tics in children with attention deficit hyperactivity disorder treated with stimulant medications. | 2001 May-Jun |
|
| Methylphenidate improves HIV-1-associated cognitive slowing. | 2001 Spring |
|
| Methylphenidate in stimulants abuse: three case reports. | 2001 Spring |
|
| Retrospective comparison of Adderall and methylphenidate in the treatment of attention deficit hyperactivity disorder. | 2001 Spring |
|
| Early methylphenidate administration to young rats causes a persistent reduction in the density of striatal dopamine transporters. | 2001 Spring |
|
| Can methylphenidate facilitate sleep in children with attention deficit hyperactivity disorder? | 2001 Spring |
|
| Methylphenidate augmentation of citalopram in elderly depressed patients. | 2001 Summer |
|
| Myoclonus during prolonged treatment with sertraline in an adolescent patient. | 2001 Summer |
|
| Pharmacokinetic interactions between cyclosporine and bupropion or methylphenidate. | 2001 Summer |
|
| Efficacy of Adderall and methylphenidate in attention deficit hyperactivity disorder: a reanalysis using drug-placebo and drug-drug response curve methodology. | 2001 Summer |
Sample Use Guides
Administer in divided doses 2 or 3 times daily, preferably 30 to 45 minutes before meals. Average dosage is 20 to 30 mg daily. Some patients may require 40 to 60 mg daily. In children the starting dose is 5 mg twice daily (before breakfast and lunch) with gradual increments of 5 to 10 mg weekly.
Route of Administration:
Oral
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| Code System | Code | Type | Description | ||
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IS6UTS8ES9
Created by
admin on Sat Dec 16 19:07:33 GMT 2023 , Edited by admin on Sat Dec 16 19:07:33 GMT 2023
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40431-62-7
Created by
admin on Sat Dec 16 19:07:33 GMT 2023 , Edited by admin on Sat Dec 16 19:07:33 GMT 2023
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10657292
Created by
admin on Sat Dec 16 19:07:33 GMT 2023 , Edited by admin on Sat Dec 16 19:07:33 GMT 2023
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SUBSTANCE RECORD
