Dexmethylphenidate: Difference between revisions

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== Pharmacology==
== Pharmacology==
{{main|Methylphenidate#Pharmacology}}
{{main|Methylphenidate#Pharmacology}}
Dexmethylphenidate has a 4–6 hour duration of effect. A long-acting formulation, Focalin XR, which spans 12 hours is also available and has been shown to be as effective as <small>DL (dextro-, levo-)</small>-TMP (threo-methylphenidate) XR (extended release) (Concerta, Ritalin LA), with flexible dosing and good tolerability.<ref>{{cite journal | vauthors = McGough JJ, Pataki CS, Suddath R | title = Dexmethylphenidate extended-release capsules for attention deficit hyperactivity disorder | journal = Expert Review of Neurotherapeutics | volume = 5 | issue = 4 | pages = 437–41 | date = July 2005 | pmid = 16026226 | doi = 10.1586/14737175.5.4.437 | s2cid = 6561452}}</ref><ref>{{cite journal | vauthors = Silva R, Tilker HA, Cecil JT, Kowalik S, Khetani V, Faleck H, Patin J | title = Open-label study of dexmethylphenidate hydrochloride in children and adolescents with attention deficit hyperactivity disorder | journal = Journal of Child and Adolescent Psychopharmacology | volume = 14 | issue = 4 | pages = 555–63 | year = 2004 | pmid = 15662147 | doi = 10.1089/cap.2004.14.555}}</ref> It has also been demonstrated to reduce ADHD symptoms in both children<ref>{{cite journal | vauthors = Arnold LE, Lindsay RL, Conners CK, Wigal SB, Levine AJ, Johnson DE, West SA, Sangal RB, Bohan TP, Zeldis JB | title = A double-blind, placebo-controlled withdrawal trial of dexmethylphenidate hydrochloride in children with attention deficit hyperactivity disorder | journal = Journal of Child and Adolescent Psychopharmacology | volume = 14 | issue = 4 | pages = 542–54 | date =Winter 2004 | pmid = 15662146 | doi = 10.1089/cap.2004.14.542}}</ref> and adults.<ref>{{cite journal | vauthors = Spencer TJ, Adler LA, McGough JJ, Muniz R, Jiang H, Pestreich L | title = Efficacy and safety of dexmethylphenidate extended-release capsules in adults with attention-deficit/hyperactivity disorder | journal = Biological Psychiatry | volume = 61 | issue = 12 | pages = 1380–7 | date = June 2007 | pmid = 17137560 | doi = 10.1016/j.biopsych.2006.07.032 | s2cid = 45976373 | doi-access = free}}</ref> d-MPH  has a similar side-effect profile to MPH<ref name="Dexmethylphenidate" /> and can be administered without regard to food intake.<ref>{{cite journal | vauthors = Teo SK, Scheffler MR, Wu A, Stirling DI, Thomas SD, Stypinski D, Khetani VD | title = A single-dose, two-way crossover, bioequivalence study of dexmethylphenidate HCl with and without food in healthy subjects | journal = Journal of Clinical Pharmacology | volume = 44 | issue = 2 | pages = 173–8 | date = February 2004 | pmid = 14747426 | doi = 10.1177/0091270003261899 | s2cid = 20694072}}</ref>
Dexmethylphenidate has a 4–6 hour duration of effect. A long-acting formulation, Focalin XR, which spans 12 hours is also available and has been shown to be as effective as <small>DL (dextro-, levo-)</small>-TMP (threo-methylphenidate) XR (extended release) (Concerta, Ritalin LA), with flexible dosing and good tolerability.<ref>{{cite journal | vauthors = McGough JJ, Pataki CS, Suddath R | title = Dexmethylphenidate extended-release capsules for attention deficit hyperactivity disorder | journal = Expert Review of Neurotherapeutics | volume = 5 | issue = 4 | pages = 437–41 | date = July 2005 | pmid = 16026226 | doi = 10.1586/14737175.5.4.437 | s2cid = 6561452}}</ref><ref>{{cite journal | vauthors = Silva R, Tilker HA, Cecil JT, Kowalik S, Khetani V, Faleck H, Patin J | title = Open-label study of dexmethylphenidate hydrochloride in children and adolescents with attention deficit hyperactivity disorder | journal = Journal of Child and Adolescent Psychopharmacology | volume = 14 | issue = 4 | pages = 555–63 | year = 2004 | pmid = 15662147 | doi = 10.1089/cap.2004.14.555}}</ref> It has also been demonstrated to reduce ADHD symptoms in both children<ref>{{cite journal | vauthors = Arnold LE, Lindsay RL, Conners CK, Wigal SB, Levine AJ, Johnson DE, West SA, Sangal RB, Bohan TP, Zeldis JB | title = A double-blind, placebo-controlled withdrawal trial of dexmethylphenidate hydrochloride in children with attention deficit hyperactivity disorder | journal = Journal of Child and Adolescent Psychopharmacology | volume = 14 | issue = 4 | pages = 542–54 | date =Winter 2004 | pmid = 15662146 | doi = 10.1089/cap.2004.14.542| hdl = 1811/51584 | hdl-access = free }}</ref> and adults.<ref>{{cite journal | vauthors = Spencer TJ, Adler LA, McGough JJ, Muniz R, Jiang H, Pestreich L | title = Efficacy and safety of dexmethylphenidate extended-release capsules in adults with attention-deficit/hyperactivity disorder | journal = Biological Psychiatry | volume = 61 | issue = 12 | pages = 1380–7 | date = June 2007 | pmid = 17137560 | doi = 10.1016/j.biopsych.2006.07.032 | s2cid = 45976373 | doi-access = free}}</ref> d-MPH  has a similar side-effect profile to MPH<ref name="Dexmethylphenidate" /> and can be administered without regard to food intake.<ref>{{cite journal | vauthors = Teo SK, Scheffler MR, Wu A, Stirling DI, Thomas SD, Stypinski D, Khetani VD | title = A single-dose, two-way crossover, bioequivalence study of dexmethylphenidate HCl with and without food in healthy subjects | journal = Journal of Clinical Pharmacology | volume = 44 | issue = 2 | pages = 173–8 | date = February 2004 | pmid = 14747426 | doi = 10.1177/0091270003261899 | s2cid = 20694072}}</ref>


'''CTx-1301''' is an experimental medication that is an extended-release formulation of dexmethylphenidate that has a half life more than an hour longer than extended-release dexmethylphenidate (d-MPH-ER). It is under development for ADHD.<ref>{{cite journal | vauthors = Brady LS, Lisanby SH, Gordon JA | title = New directions in psychiatric drug development: promising therapeutics in the pipeline | journal = Expert Opinion on Drug Discovery | volume = 18 | issue = 8 | pages = 835–850 | date = 3 August 2023 | pmid = 37352473 | doi = 10.1080/17460441.2023.2224555 | s2cid = 259240509}}</ref><ref>{{cite journal | vauthors = Childress AC, Beltran N, Supnet C, Weiss MD | title = Reviewing the role of emerging therapies in the ADHD armamentarium | journal = Expert Opinion on Emerging Drugs | volume = 26 | issue = 1 | pages = 1–16 | date = March 2021 | pmid = 33143485 | doi = 10.1080/14728214.2020.1846718 | s2cid = 226251694}}</ref><ref>{{cite journal | vauthors = Ryst E, Childress A | title = An updated safety review of the current drugs for managing ADHD in children | journal = Expert Opinion on Drug Safety | volume = 22 | issue = 11 | pages = 1025–1040 | date = 2023 | pmid = 37843488 | doi = 10.1080/14740338.2023.2271392 | s2cid = 264144450}}</ref><ref>{{cite journal | vauthors = Harris E |title=Industry update: what is new in the field of therapeutic delivery? |journal=Therapeutic Delivery |date=1 February 2018 |volume=9 |issue=3 |pages=155–161 |doi=10.4155/tde-2017-0117|doi-access=free}}</ref><ref>{{cite journal | vauthors = Childress AC, Komolova M, Sallee FR | title = An update on the pharmacokinetic considerations in the treatment of ADHD with long-acting methylphenidate and amphetamine formulations | journal = Expert Opinion on Drug Metabolism & Toxicology | volume = 15 | issue = 11 | pages = 937–974 | date = November 2019 | pmid = 31581854 | doi = 10.1080/17425255.2019.1675636 | s2cid = 203660100 | doi-access = free}}</ref>
'''CTx-1301''' is an experimental medication that is an extended-release formulation of dexmethylphenidate that has a half life more than an hour longer than extended-release dexmethylphenidate (d-MPH-ER). It is under development for ADHD.<ref>{{cite journal | vauthors = Brady LS, Lisanby SH, Gordon JA | title = New directions in psychiatric drug development: promising therapeutics in the pipeline | journal = Expert Opinion on Drug Discovery | volume = 18 | issue = 8 | pages = 835–850 | date = 3 August 2023 | pmid = 37352473 | doi = 10.1080/17460441.2023.2224555 | s2cid = 259240509}}</ref><ref>{{cite journal | vauthors = Childress AC, Beltran N, Supnet C, Weiss MD | title = Reviewing the role of emerging therapies in the ADHD armamentarium | journal = Expert Opinion on Emerging Drugs | volume = 26 | issue = 1 | pages = 1–16 | date = March 2021 | pmid = 33143485 | doi = 10.1080/14728214.2020.1846718 | s2cid = 226251694}}</ref><ref>{{cite journal | vauthors = Ryst E, Childress A | title = An updated safety review of the current drugs for managing ADHD in children | journal = Expert Opinion on Drug Safety | volume = 22 | issue = 11 | pages = 1025–1040 | date = 2023 | pmid = 37843488 | doi = 10.1080/14740338.2023.2271392 | s2cid = 264144450}}</ref><ref>{{cite journal | vauthors = Harris E |title=Industry update: what is new in the field of therapeutic delivery? |journal=Therapeutic Delivery |date=1 February 2018 |volume=9 |issue=3 |pages=155–161 |doi=10.4155/tde-2017-0117|doi-access=free}}</ref><ref>{{cite journal | vauthors = Childress AC, Komolova M, Sallee FR | title = An update on the pharmacokinetic considerations in the treatment of ADHD with long-acting methylphenidate and amphetamine formulations | journal = Expert Opinion on Drug Metabolism & Toxicology | volume = 15 | issue = 11 | pages = 937–974 | date = November 2019 | pmid = 31581854 | doi = 10.1080/17425255.2019.1675636 | s2cid = 203660100 | doi-access = free}}</ref>

Latest revision as of 02:28, 9 June 2025

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Dexmethylphenidate, sold under the brand name Focalin among others, is a central nervous system (CNS) stimulant used in the treatment of attention deficit hyperactivity disorder (ADHD) in those over the age of five years.[1] It is taken by mouth.[1] The immediate-release formulation lasts up to five hours while the extended-release formulation lasts up to twelve hours.[2] It is the more active enantiomer of methylphenidate.[1]

Common side effects include abdominal pain, loss of appetite, and fever.[1] Serious side effects may include psychosis, sudden cardiac death, mania, anaphylaxis, seizures, and priapism.[1] Safety during pregnancy and breastfeeding is unclear.[3]

Dexmethylphenidate was approved for medical use in the United States in 2001.[4] It is available as a generic medication.[1] In 2022, it was the 109th most commonly prescribed medication in the United States, with more than 5Template:Nbspmillion prescriptions.[5][6] Template:TOC limit

Medical uses

Dexmethylphenidate is used as a treatment for attention deficit hyperactivity disorder (ADHD), usually along with psychological, educational, behavioral or other forms of treatment. It is proposed that stimulants help ameliorate the symptoms of ADHD by making it easier for the user to concentrate, avoid distraction, and control behavior. Placebo-controlled trials have shown that once-daily dexmethylphenidate XR was effective and generally well tolerated.[7]

Improvements in ADHD symptoms in children were significantly greater for dexmethylphenidate XR versus placebo.[7] It also showed greater efficacy than osmotic controlled-release oral delivery system (OROS) methylphenidate over the first half of the laboratory classroom day but assessments late in the day favoured OROS methylphenidate.[7]

Contraindications

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Adverse effects

Template:Transcluded section Products containing dexmethylphenidate have a side effect profile comparable to those containing methylphenidate.[8] Template:Trim

Interactions

Template:Transcluded section Template:Trim

Pharmacology

Script error: No such module "Labelled list hatnote". Dexmethylphenidate has a 4–6 hour duration of effect. A long-acting formulation, Focalin XR, which spans 12 hours is also available and has been shown to be as effective as DL (dextro-, levo-)-TMP (threo-methylphenidate) XR (extended release) (Concerta, Ritalin LA), with flexible dosing and good tolerability.[9][10] It has also been demonstrated to reduce ADHD symptoms in both children[11] and adults.[12] d-MPH has a similar side-effect profile to MPH[8] and can be administered without regard to food intake.[13]

CTx-1301 is an experimental medication that is an extended-release formulation of dexmethylphenidate that has a half life more than an hour longer than extended-release dexmethylphenidate (d-MPH-ER). It is under development for ADHD.[14][15][16][17][18]

Mechanism of action

Methylphenidate is a catecholamine reuptake inhibitor that indirectly increases catecholaminergic neurotransmission by inhibiting the dopamine transporter (DAT) and norepinephrine transporter (NET),[19] which are responsible for clearing catecholamines from the synapse, particularly in the striatum and meso-limbic system.[20] Moreover, it is thought to "increase the release of these monoamines into the extraneuronal space."[21]

Although four stereoisomers of methylphenidate (MPH) are possible, only the threo diastereoisomers are used in modern practice. There is a high eudysmic ratio between the SS and RR enantiomers of MPH. Dexmethylphenidate (d-threo-methylphenidate) is a preparation of the RR enantiomer of methylphenidate.[22][23] In theory, D-TMP (d-threo-methylphenidate) can be anticipated to be twice the strength of the racemic product.[19][24]

Compd[25] DAT (Ki) DA (IC50) NET (Ki) (IC50)
D-TMP 161 23 206 39
L-TMP 2250 1600 >10K 980
DL-TMP 121 20 788 51

Notes

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References

Template:Reflist

Template:ADHD pharmacotherapies Template:Drug use Script error: No such module "Navbox". Template:Monoamine reuptake inhibitors Template:Sigma receptor modulators Script error: No such module "Navbox". Template:Portal bar

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