Pregnancy

• Risk Category C [some animal studies show adverse effects; no controlled studies in humans]

• Infants whose mothers took methylphenidate during pregnancy may experience withdrawal symptoms

• Use in women of childbearing potential requires weighing potential benefits to the mother against potential risks to the fetus

✽ For ADHD patients, methylphenidate should generally be discontinued before anticipated pregnancies

Breast Feeding

• Unknown if methylphenidate is secreted in human breast milk, but all psychotropics assumed to be secreted in breast milk

✽ Recommended either to discontinue drug or bottle feed

• If infant shows signs of irritability, drug may need to be discontinued

METHYLPHENIDATE (D): THE ART OF PSYCHOPHARMACOLOGY

Potential Advantages

• The active d enantiomer of methylphenidate may be slightly more than twice as efficacious as racemic d,l-methylphenidate

Potential Disadvantages

• Patients with current or past substance abuse, bipolar disorder, or psychosis

Primary Target Symptoms

• Concentration, attention span

• Motor hyperactivity

• Impulsiveness

• Physical and mental fatigue

• Daytime sleepiness

• Depression

Pearls

• May be useful for treatment of depressive symptoms in medically ill elderly patients

• May be useful for treatment of post-stroke depression

• A classical augmentation strategy for treatment-refractory depression

• Specifically, may be useful for treatment of cognitive dysfunction and fatigue as residual symptoms of major depressive disorder unresponsive to multiple prior treatments

• May also be useful for the treatment of cognitive impairment, depressive symptoms, and severe fatigue in patients with HIV infection and in cancer patients

• Can be used to potentiate opioid analgesia and reduce sedation, particularly in end-of- life management

• Atypical antipsychotics may be useful in treating stimulant or psychotic consequences of overdose

• Some patients respond to or tolerate methylphenidate better than amphetamine, and vice versa

• Taking with food may delay peak actions of immediate-release d-methylphenidate for 2–3 hours

• Half-life and duration of clinical action tend to be shorter in younger children

• Drug abuse may actually be lower in ADHD adolescents treated with stimulants than in ADHD adolescents who are not treated

• New extended-release formulation is truly a once daily dose

• Extended-release capsule can be sprinkled over applesauce for patients unable to swallow the capsule

• Some patients may benefit from an occasional addition of an immediate-release dose of d-methylphenidate to the daily base dose of extended-release d-methylphenidate

Suggested Reading

Dexmethylphenidate – Novartis/Celgene. Focalin, D-MPH, D-methylphenidate hydrochloride, D-methylphenidate, dexmethylphenidate, dexmethylphenidate hydrochloride. Drugs R D 2002;3(4):279–82.

Keating GM, Figgitt DP. Dexmethylphenidate. Drugs 2002;62(13):1899–904.

METHYLPHENIDATE (D,L)

METHYLPHENIDATE (D,L): THERAPEUTICS

Brands

• Concerta

• Metadate CD

• Ritalin

• Ritalin LA

• Daytrana

see index for additional brand names

Generic?

Yes

Class

• Stimulant

Commonly Prescribed for

(bold for FDA approved)

• Attention deficit hyperactivity disorder (ADHD) in children and adults (approved ages vary based on formulation)

• Narcolepsy (Metadate ER, Methylin ER, Ritalin, Ritalin SR)

• Treatment-resistant depression

How the Drug Works

✽ Increases norepinephrine and especially dopamine actions by blocking their reuptake

• Enhancement of dopamine and norepinephrine actions in certain brain regions (e.g., dorsolateral prefrontal cortex) may improve attention, concentration, executive function, and wakefulness

• Enhancement of dopamine actions in other brain regions (e.g., basal ganglia) may improve hyperactivity

• Enhancement of dopamine and norepinephrine in yet other brain regions (e.g., medial prefrontal cortex, hypothalamus) may improve depression, fatigue, and sleepiness