Teaching Point | Dexmethylphenidate [Focalin] Date: 12/05/2017

Dexmethylphenidate Drug Information

Brand Name: Focalin
Drug Class: Central Nervous System (CNS) Stimulant
Structure: Methylphenidate analog (dextro-rotatory enantiomer)

Methylphenidate [Ritalin] Dexmethylphenidate [Focalin]

Mechanism:
o Same as methylphenidate Catecholamines in the synaptic cleft, especially
norepinephrine (NE) and dopamine (DA) by blocking their reuptake
Note that amphetamines are similar, but they also have the additional mechanism
of increasing/stimulating neurotransmitter release.
Clinical Uses & Effects:
o ADHD
Used in combination with psychological, educational, behavioral or other forms
of treatment
Works by improving concentration, helping avoiding distractions and controlling
behavior
FDA approved in ages 6 years and adults
o Enhancing Performance (Off-Label)
E.g. Study-Aid or Test-Taking Aid
Works by improving cognition, including working memory, episodic memory,
and inhibitory control.
Side-Effects:
o Focalin (and Ritalin) are generally very well-tolerated
o Central nervous system:
Anxiety, depression
Dizziness
Emotional lability
Headache
Insomnia
Irritability, jitteriness
o Dermatologic: Pruritus
o Gastrointestinal:
Teaching Point | Dexmethylphenidate [Focalin] Date: 12/05/2017

Abdominal pain
Anorexia
Decreased appetite
Dyspepsia
Nausea/Vomiting
Xerostomia
o Respiratory:
Nasal congestion
Pharyngolaryngeal pain
Contraindications (i.e. Do not use in patients with the following):
o Marked anxiety, tension, and agitation
o Hypersensitivity to methylphenidate or any component of the formulation;
o Glaucoma
o Motor tics, family history or diagnosis of Tourette syndrome
o Concurrent use with or within 14 days following discontinuation with monoamine
oxidase inhibitor (MAOi) therapy.
Pharmacokinetics:
o Onset of action: Rapid, within 1 to 2 hours of an effective dose
o Duration of action:
Immediate release: 3 to 5 hours
Extended release: 9 to 12 hours
o Absorption:
Immediate release: Rapid
Extended release: Bimodal (with 2 peak concentrations ~4 hours apart)
o Metabolism: Via de-esterification to inactive metabolite, d--phenyl-piperidine acetate
(d-ritalinic acid)
o Bioavailability: 22% to 25%
o Half-life elimination - Immediate release:
2 to 3 hours (Children)
2 to 4.5 hours (Adults)
o Time to Peak - Fasting:
Immediate release: 1 to 1.5 hours; after a high-fat meal: 2.9 hours
Extended release: First peak: 1.5 hours (range: 1 to 4 hours); Second peak: 6.5
hours (range: 4.5 to 7 hours)
o Excretion: Urine (90%, primarily as inactive metabolite)

References:
o https://www.uptodate.com/contents/pharmacology-of-drugs-used-to-treat-attention-
deficit-hyperactivity-disorder-in-children-and-adolescents
o https://www.uptodate.com/contents/dexmethylphenidate-pediatric-drug-information
o https://www.uptodate.com/contents/treatment-of-attention-deficit-hyperactivity-
disorder-in-children-beyond-the-basics
o https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/021278s016lbl.pdf