methylphenidate (Ritalin, Concerta, Daytrana, Metadate CD, Centedrine)
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Introduction
Tradename: Ritalin. (methylphenidate hydrochloride) DEA-controlled substance: class 2.
Indications
- attention deficit hyperactivity disorder[17]
- narcolepsy
- depression[14]
- apathy[20]
- may improve cognition after traumatic brain injury in children[21]
Contraindications
Caution:
- hypertension
- seizures & EEG abnormalities
- high potential for abuse
Dosage
- 5-10 mg PO BID/TID, generally 30-45 minutes before meals
- average dose is 20-30 mg/day
- sustained release (SR) administered BID
- maximum dose: 60 mg/day
- Concerta: QAM dosing; 18-36 mg PO QD
- 18 mg QD is comparable to 5 mg Ritalin TID
- dosage should be taken in the morning
- generics for Concerta may not be bioequivalent[16]
- Metadate CD: QD dosing
- Ritalin LA: start 20 mg QD; max 60 mg QD[9]
- Daytrana patch: QD, patch worn 9 hours/day[11]
Tabs: 5, 10, 20 mg.
Ritalin LA: 20, 30 & 40 mg capsules.
Concerta: 18 & 36 mg.*
- dextro isomer (may have fewer adverse effects)
Daytrana patch[12]
* 2 generic versions of Concerta continue to be available in June 2015 months after the FDA deemed them not therapeutically equivalent[16]
* when switching methylphenidate products, discontinue existing treatment & titrate the new product using a titration schedule[22]
Pharmacokinetics
elimination via liver
elimination via kidney
Adverse effects
- common (> 10%)
- less common (1-10%)
- uncommon (< 1%)
- increased risk of cardiac arrhythmias (RR=1.6)[18]
- highest risk 1-3 days after initiation & in children with congenital heart disease
- increased risk for myocardial infarction within the 1st 2 months of treatment
- increased risk of hypertension 4-7 days after initiation[18]
- other[2][5][10]
- dry throat
- hallucinations
- suicidal ideation
- risk of suicide attempts is not due to methylphenidate but precedes it[19]
- no increased risk for suicide attempt after 90 days ofbmethylphenidate[19]
- psychotic or violent behavior
- chest pain
- Concerta tablets do NOT dissolve completely; ghost tablets may be seen in feces
- Daytrana patch
- skin irritation or hypersensitivity
- chemical leukoderma[17]
- not physically harmful, but is permanent
- may affect subsequent tolerance of oral methyphenidate
- priapism[15]
- drug adverse effects of ADHD medications
- drug adverse effects of analeptics
- drug adverse effects of psychotropic agents
- drug adverse effects of sympathomimetic(s)
Drug interactions
- methylphenidate decreases antihypertensive effect of guanethidine
- methylphenidate increases plasma levels of:
- MAO inhibitors may increase effects of methylphenidate
Laboratory
Mechanism of action
- piperidine derivative, structurally related to amphetamine
- mild CNS stimulant with actions similar to amphetamine
- inihibits dopamine reuptake
- inhibits norepinephrine reuptake Abuse:
More general terms
More specific terms
Additional terms
References
- ↑ The Pharmacological Basis of Therapeutics, 9th ed. Gilman et al, eds. Permagon Press/McGraw Hill, 1996
- ↑ 2.0 2.1 Drug Information & Medication Formulary, Veterans Affairs, Central California Health Care System, 1st ed., Ravnan et al eds, 1998
- ↑ Kaiser Permanente Northern California Regional Drug Formulary, 1998
- ↑ Prescriber's Letter 7(8):48 2000
- ↑ 5.0 5.1 Prescriber's Letter 7(9):51 2000
- ↑ Clinical Guide to Laboratory Tests, 3rd ed. Teitz ed., W.B. Saunders, 1995
- ↑ 7.0 7.1 Prescriber's Letter 8(2):11 2001
- ↑ Journal Watch 21(14):117, 2001 Pelham et al, Pediatrics 107:e105, 2001
- ↑ 9.0 9.1 Prescriber's Letter 9(8):47 2002
- ↑ 10.0 10.1 Prescriber's Letter 12(8): 2005 Safety Concerns of ADHD Drugs Detail-Document#: http://prescribersletter.com/(5bhgn1a4ni4cyp2tvybwfh55)/pl/ArticleDD.aspx?li=1&st=1&cs=&s=PRL&pt=3&fpt=25&dd=210810&pb=PRL (subscription needed) http://www.prescribersletter.com
- ↑ 11.0 11.1 11.2 Prescriber's Letter 13(2): 2006 Drug Treatment for Attention Deficit Hyperactivity Disorder Detail-Document#: http://prescribersletter.com/(5bhgn1a4ni4cyp2tvybwfh55)/pl/ArticleDD.aspx?li=1&st=1&cs=&s=PRL&pt=3&fpt=25&dd=220214&pb=PRL (subscription needed) http://www.prescribersletter.com
- ↑ 12.0 12.1 Prescriber's Letter 13(6): 2006 New Drug: Daytrana (Methylphenidate Transdermal System) Detail-Document#: http://prescribersletter.com/(5bhgn1a4ni4cyp2tvybwfh55)/pl/ArticleDD.aspx?li=1&st=1&cs=&s=PRL&pt=3&fpt=25&dd=220606&pb=PRL (subscription needed) http://www.prescribersletter.com
- ↑ Prescriber's Letter 14(9): 2007 Defective Daytrana Patches Detail-Document#: http://prescribersletter.com/(5bhgn1a4ni4cyp2tvybwfh55)/pl/ArticleDD.aspx?li=1&st=1&cs=&s=PRL&pt=3&fpt=25&dd=230903&pb=PRL (subscription needed) http://www.prescribersletter.com
- ↑ 14.0 14.1 Deprecated Reference
- ↑ 15.0 15.1 FDA MedWatch - Dec 17, 2012 Methylphenidate ADHD Medications: Drug Safety Communication - Risk of Long-lasting Erections http://www.fda.gov/Safety/MedWatch/SafetyInformation/SafetyAlertsforHumanMedicalProducts/ucm378876.ht16)
FDA Drug Safety and Availability. Nov 13, 2014 Methylphenidate Hydrochloride Extended Release Tablets (generic Concerta) made by Mallinckrodt and Kudco. [11-13-2014] FDA concerns about therapeutic equivalence with two generic versions of Concerta tablets (methylphenidate hydrochloride extended-release) http://www.fda.gov/Drugs/DrugSafety/ucm422568.htm
Orciari Herman A, Sadoughi S, Saitz R Generic ADHD Drugs Remain on the Market, Despite Lack of Therapeutic Equivalence. Physician's First Watch, June 18, 2015 David G. Fairchild, MD, MPH, Editor-in-Chief Massachusetts Medical Society http://www.jwatch.org - ↑ 16.0 16.1 16.2 FDA Safety Alert. 06/24/2015 Daytrana Patch (methylphenidate transdermal system): Drug Safety Communication - Permanent Skin Color Changes. http://www.fda.gov/Safety/MedWatch/SafetyInformation/SafetyAlertsforHumanMedicalProducts/ucm452595.htm
FDA Drug Safety Communication: 06/24/2015 FDA reporting permanent skin color changes associated with use of Daytrana patch (methylphenidate transdermal system) for treating ADHD. http://www.fda.gov/Drugs/DrugSafety/ucm452244.htm - ↑ 17.0 17.1 17.2 Storebo OJ et al Methylphenidate for attention-deficit/hyperactivity disorder in children and adolescents: Cochrane systematic review with meta-analyses and trial sequential analyses of randomised clinical trials. BMJ 2015;351:h5203 <PubMed> PMID: https://www.ncbi.nlm.nih.gov/pubmed/26608309 <Internet> http://www.bmj.com/content/351/bmj.h5203
Fazel M Methylphenidate for ADHD. BMJ 2015;351:h5875 <PubMed> PMID: https://www.ncbi.nlm.nih.gov/pubmed/26608974 <Internet> http://www.bmj.com/content/351/bmj.h5875 - ↑ 18.0 18.1 18.2 Shin JY et al Cardiovascular safety of methylphenidate among children and young people with attention-deficit/hyperactivity disorder (ADHD): nationwide self controlled case series study. BMJ 2016;353:i2550 <PubMed> PMID: https://www.ncbi.nlm.nih.gov/pubmed/27245699 Free PMC Article <Internet> http://www.bmj.com/content/353/bmj.i2550
Jackson JW The cardiovascular safety of methylphenidate. BMJ 2016;353:i2874 <PubMed> PMID: https://www.ncbi.nlm.nih.gov/pubmed/27245078 <Internet> http://www.bmj.com/content/353/bmj.i2874 - ↑ 19.0 19.1 19.2 Man KKC, Coghill D, Chan EW et al Association of Risk of Suicide Attempts With Methylphenidate Treatment. JAMA Psychiatry. Published online July 26, 2017. <PubMed> PMID: https://www.ncbi.nlm.nih.gov/pubmed/28746699 <Internet> http://jamanetwork.com/journals/jamapsychiatry/article-abstract/2645499
- ↑ 20.0 20.1 Padala PR, Padala KP, Lensing SY et al. Methylphenidate for apathy in community-dwelling older veterans with mild Alzheimer's disease: A double-blind, randomized, placebo-controlled trial. Am J Psychiatry 2017 Sep 15 PMID: https://www.ncbi.nlm.nih.gov/pubmed/28945120
- ↑ 21.0 21.1 LeBlond E, Smith-Paine J, Riemersma JJ et al. Influence of methylphenidate on long-term neuropsychological and everyday executive functioning after traumatic brain injury in children with secondary attention problems. J Int Neuropsychol Soc 2019 Aug; 25:740-749. PMID: https://www.ncbi.nlm.nih.gov/pubmed/31178001
- ↑ 22.0 22.1 22.2 Windle ML Rapid Rx Quiz: Stimulants Medscape.Oct 23, 2022 https://reference.medscape.com/viewarticle/981392