Description

Simple

A medication used to treat ADHD with other therapies.

Clinical

A norepinephrine-dopamine reuptake inhibitor used in the treatment of ADHD in conjunction with other therapies.

Overview

Dexmethylphenidate is the dextrorotary form of methylphenidate introduced in 2002[2]. It is a norepinephrine-dopamine reuptake inhibitor (NDRI) and thus a psychostimulant[5]. It is used for treatment of Attention Deficit Hyperactivity Disorder (ADHD)[Label,2]. The d-isomer is thought to have greater effect with fewer side effects than the l-isomer or the racemic mixture[2].

Pharmacology

Indication

Dexmethylphenidate is used as a treatment for ADHD, ideally in conjunction with psychological, educational, behavioral or other forms of treatment[ Read more

Pharmacodynamic

Dexmethylphenidate is the d-enantiomer of methylphenidate[Label]. This enantiomer is more pharmacologically active than the racemic mixture and may block norepinephrine and dopamine reuptake in synapses[Label].

Mechanism of action

Methylphenidate inhibits dopamine and norepinephrine reuptake transporters in synapses, especially in the thalamus and striatum[ Read more

Absorption

Taking dexmethylphenidate with or without food does not affect patients in a clinically relevant way[ Read more

Protein binding

12-15% of dexmethylphenidate is protein bound[Label]. However, other studies have observed 15.2±5.2% protein binding in children and 16.2±1.1% in adults[ Read more

Volume of distribution

2.65L/kg when administered intravenously[4].

Clearance

0.40L/hr/kg following an intravenous dose and a renal clearance of 0.005L/hr/kg[ Read more

Half life

The mean terminal half life is approximately 2.2 hours[Label]. However other studies have shown 3.8-3.9 hours[ Read more

Route of elimination

Dexmethylphenidate is mainly eliminated renally[4]. After... Read more

Toxicity

There is no difference in effect across genders[ Read more

Adverse Effects

Contraindications

  • Route:
    • Oral
  • Dose Form:
    • Tablet
    • Tablet, extended release
  • Hypersensitivity:
    • true
  • Sex Group: all
  • Regions: US
  • Route:
    • Oral
  • Dose Form:
    • Tablet
    • Tablet, extended release
  • Regions: US
  • With Categories Coadmin:
      • Name: Monoamine Oxidase Inhibitors
      • Drugbank Id: DBCAT001004
      • Mesh Id: D008996
  • Route:
    • Oral
  • Dose Form:
    • Tablet
    • Tablet, extended release
  • Regions: US
  • Patient Conditions:
      • Name: Diagnosed tourette's syndrome
      • Drugbank Id: DBCOND0108452
  • Route:
    • Oral
  • Dose Form:
    • Tablet
    • Tablet, extended release
  • Regions: US
  • Patient Conditions:
      • Name: Family history of Tourette’s syndrome
      • Drugbank Id: DBCOND0108451
  • Route:
    • Oral
  • Dose Form:
    • Tablet
    • Tablet, extended release
  • Regions: US
  • Patient Conditions:
      • Name: Motor tics
      • Drugbank Id: DBCOND0107725
  • Route:
    • Oral
  • Dose Form:
    • Tablet
    • Tablet, extended release
  • Regions: US
  • Patient Conditions:
      • Name: Glaucoma
      • Drugbank Id: DBCOND0010013
  • Route:
    • Oral
  • Dose Form:
    • Tablet
    • Tablet, extended release
  • Regions: US
  • Patient Conditions:
      • Name: Agitation
      • Drugbank Id: DBCOND0017779
  • Route:
    • Oral
  • Dose Form:
    • Tablet
    • Tablet, extended release
  • Regions: US
  • Patient Conditions:
      • Name: Tension
      • Drugbank Id: DBCOND0018825
  • Route:
    • Oral
  • Dose Form:
    • Tablet
    • Tablet, extended release
  • Regions: US
  • Patient Conditions:
      • Name: Anxiety
      • Drugbank Id: DBCOND0018828

Food Interactions

  • Avoid alcohol. Alcohol inhibits the metabolism of dexmethylphenidate.
  • Take with or without food.

Interactions

Type in a drug name to check for interaction with Dexmethylphenidate
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  • Paracetamol(acetaminophen)
  • Paxil(paroxetine)
  • Pamelor(nortriptyline)
  • Panadol(acetaminophen)
  • Patanol(olopatadine ophthalmic)
  • Pataday(olopatadine ophthalmic)
  • Parnate(tranylcypromine)
  • Pazeo(olopatadine ophthalmic)
(R)-warfarin
The metabolism of (R)-warfarin can be decreased when combined with Dexmethylphenidate.
(S)-Warfarin
The metabolism of (S)-Warfarin can be decreased when combined with Dexmethylphenidate.
1-benzylimidazole
The risk or severity of hypertension can be increased when 1-benzylimidazole is combined with Dexmethylphenidate.
2,5-Dimethoxy-4-ethylamphetamine
The risk or severity of serotonin syndrome can be increased when 2,5-Dimethoxy-4-ethylamphetamine is combined with Dexmethylphenidate.
2,5-Dimethoxy-4-ethylthioamphetamine
The risk or severity of adverse effects can be increased when Dexmethylphenidate is combined with 2,5-Dimethoxy-4-ethylthioamphetamine.
3,5-Dinitrocatechol
The risk or severity of adverse effects can be increased when Dexmethylphenidate is combined with 3,5-Dinitrocatechol.
4-Bromo-2,5-dimethoxyamphetamine
The risk or severity of adverse effects can be increased when 4-Bromo-2,5-dimethoxyamphetamine is combined with Dexmethylphenidate.
4-hydroxycoumarin
The serum concentration of the active metabolites of 4-hydroxycoumarin can be increased when 4-hydroxycoumarin is used in combination with Dexmethylphenidate.
4-Methoxyamphetamine
The risk or severity of adverse effects can be increased when 4-Methoxyamphetamine is combined with Dexmethylphenidate.
4-methylumbelliferyl beta-D-glucoside
The serum concentration of the active metabolites of 4-methylumbelliferyl beta-D-glucoside can be increased when 4-methylumbelliferyl beta-D-glucoside is used in combination with Dexmethylphenidate.
5-methoxy-N,N-dimethyltryptamine
The risk or severity of adverse effects can be increased when Dexmethylphenidate is combined with 5-methoxy-N,N-dimethyltryptamine.
7-Nitroindazole
The risk or severity of adverse effects can be increased when 7-Nitroindazole is combined with Dexmethylphenidate.
7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline
7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline may increase the hypertensive activities of Dexmethylphenidate.
Abediterol
The risk or severity of hypertension can be increased when Dexmethylphenidate is combined with Abediterol.
Acebutolol
Dexmethylphenidate may decrease the antihypertensive activities of Acebutolol.
Aceclofenac
The risk or severity of hypertension can be increased when Dexmethylphenidate is combined with Aceclofenac.
Acemetacin
The risk or severity of hypertension can be increased when Dexmethylphenidate is combined with Acemetacin.
Acenocoumarol
The serum concentration of the active metabolites of Acenocoumarol can be increased when Acenocoumarol is used in combination with Dexmethylphenidate.
Acepromazine
The risk or severity of adverse effects can be increased when Acepromazine is combined with Dexmethylphenidate.
Aceprometazine
The risk or severity of adverse effects can be increased when Aceprometazine is combined with Dexmethylphenidate.
7 References
  1. 1 . 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.PubMed: 15082749
  2. 2 . Liu F, Minami H, Silva RR: Dexmethylphenidate hydrochloride in the treatment of attention deficit hyperactivity disorder. Neuropsychiatr Dis Treat. 2006 Dec;2(4):467-73.PubMed: 19412495
  3. 3 . Modi NB, Wang B, Noveck RJ, Gupta SK: Dose-proportional and stereospecific pharmacokinetics of methylphenidate delivered using an osmotic, controlled-release oral delivery system. J Clin Pharmacol. 2000 Oct;40(10):1141-9.PubMed: 11028253
  4. 4 . Kimko HC, Cross JT, Abernethy DR: Pharmacokinetics and clinical effectiveness of methylphenidate. Clin Pharmacokinet. 1999 Dec;37(6):457-70. doi: 10.2165/00003088-199937060-00002.PubMed: 10628897
  5. 5 . Tremblay S, Pieper F, Sachs A, Joober R, Martinez-Trujillo J: The Effects of Methylphenidate (Ritalin) on the Neurophysiology of the Monkey Caudal Prefrontal Cortex. eNeuro. 2019 Mar 4;6(1). pii: eN-NWR-0371-18. doi: 10.1523/ENEURO.0371-18.2018. eCollection 2019 Jan-Feb.PubMed: 30847388
  6. 6 . Focalin (Dexmethylphenidate) FDA Label File
  7. 7 . Dexmethylphenidate XR FDA Label File