Methylphenidate

See Also

Indications
Methylphenidate (Ritalin)

Attention Deficit Hyperactivity Disorder (ADHD)
Narcolepsy
Depression in medically ill elderly patients
Enhanced pain control in patients on Opiates

Contraindications

See Drug Interactions below
Congenital Heart Defect (ask related PMH, Family History and screen on ADHD exam)
1. Consider an EKG before prescribing
2. Vetter (2008) Circulation 117(18):2407-23. [PubMed]
Motor Tics or Tourette's Syndrome
Glaucoma
Seizure Disorder
Hypertension
Pregnancy

Mechanism

See ADHD Medication
As with other Amphetamine-like drugs, Methylphenidate triggers release of biogenic amines
1. Norepinephrine, Dopamine and Serotonin are released from storage Vesicles
Effects
1. CNS Stimulation
  1. Inhibits fast-rate behavior in hyperkinetic, hyperactive children
  2. Speeds slow-rate behavior (e.g. improves memory and learning)
2. Decreases appetite
3. Ergogenic Aid in athletes (illicit use)

Precautions

See ADHD Medication for overall approach and medication selection
Maximum Dosing
1. Adults and older adolescents (>50 kg) may in some cases need dosing in excess of listed maximum
2. Exercise caution and Informed Consent as these doses are not FDA approved
  1. Exceed the manufacturers recommendation
3. Absolute maximum doses
  1. Methylphenidate: 100 mg per day in divided doses
  2. Concerta 108 mg per day
4. (2013) Presc Lett 20(9): 50-1

Pharmacokinetics
Methylphenidate

Immediate Release: Ritalin-IR, Methylin IR
1. Onset of action: within 20 to 30 minutes of dose (up to 60 minutes)
2. Peaks at 1.9 hours on average
3. Duration: 3 to 6 hours
Immediate Release: Focalin (Dexmethylphenidate)
1. D-isomer of Ritalin (l-isomer is inactive)
2. Prescribed at half dose of Ritalin
3. Same Pharmacokinetics as immediate release Methylphenidate
4. Fewer Headaches but more Stomache pain than with Methylphenidate
Long-Acting: Ritalin-LA
1. Duration: 8 hours
2. Biphasic release
  1. Immediate release: 50%
  2. Modified release beads: 50%
3. Preferred over Ritalin SR
Long-Acting: Ritalin-SR, Metadate ER, Methylin ER
1. Onset of action: within 90 minutes of dose
2. Peaks at 3 hours on average
3. Duration: 5-8 hours (gradual decrease after 3 hours)
4. Less effective than Ritalin IR twice daily
5. Other sustained release forms are preferred
Very-Long-Acting: Concerta
1. Onset of action: within 60 to 120 minutes of dose
2. Duration: 12 hours
3. Comparable to Ritalin-IR three times daily
Very-Long-Acting: Metadate-CD
1. Flat concentration curve despite biphasic release
2. Duration: 8-10 hours
3. Biphasic peaks at 1.5 hours and again at 4.5 hours
  1. Immediate release beads: 30%
  2. Extended release beads: 70%
Very-Long Acting: Quillivant XR
1. Combination of Immediate release Methylphenidate (20%) and extended release Methylphenidate (80%)
2. Peaks at 5 hours
3. Duration: 12 hours
4. Niche is that it is suspension (compounded by pharmacy) at 5 mg/ml
  1. Other stimulant capsules can be sprinkled on apple sauce (Focalin XR, Metadate CD, Ritalin LA, Adderall XR)
5. References
  1. (2013) Presc Lett 20(2): 8-9

Dosing
Children (over age 6 years)

Maximum total daily dose: 60 mg/day
Immediate Release: Methylphenidate
1. Usual Range: 0.5 - 1 mg/kg/day
2. Start: 2.5 to 5 mg per dose, twice daily
3. Initial Schedule (lasts 4 hours - dose up to 4 times daily)
  1. Morning: 2.5 to 5 mg PO 30 minutes before breakfast
  2. Noon: 2.5 to 5 mg PO 30 minutes before lunch
  3. Afternoon: 1.25 to 2.5 mg PO at 3-4 pm
4. Titrate dose up weekly
  1. Increase dose by 0.1 mg/kg/dose (or 5-10 mg/day)
5. Maximum dose: 2 mg/kg/day or 60 mg/day (some sources suggest maximum up to 90)
Immediate Release: Focalin (Dexmethylphenidate)
1. Start: 2.5 mg orally twice daily
2. Usual Dose: 5-10 mg orally twice daily
3. Maximum Dose: 20 mg orally daily
Sustained Release
1. Concerta 18 to 54 mg orally daily
  1. Start: 18 mg qAM
  2. May increase weekly by 18 mg/day
  3. Conversions
    1. Ritalin 5 mg or 20 mg SR: Concerta 18 mg
    2. Ritalin 10 mg or 40 mg SR: Concerta 36 mg
    3. Ritalin 15 mg or 60 mg SR: Concerta 54 mg
  4. Maximum: 72 mg/day
2. Ritalin LA or Metadate CD
  1. Start: 20 mg orally daily
  2. May increase weekly by 10-20 mg/day
  3. Usual dose: 20-40 mg orally once daily
  4. Maximum: 60 mg/day
3. Ritalin-SR (Other long-acting agents are preferred)
  1. Dose: 0.6 to 2 mg/kg up to 20-40 mg orally daily
  2. Dose is directly converted from Regular Ritalin
  3. Conversion to Ritalin SR (Metadate ER, Methylin ER)
  4. Administer cumulative 8 hour regular dose
  5. Example: Conversion
    1. Child takes Ritalin 10 mg, 5 mg, and 5 mg
    2. Ritalin SR dosing will be 20 mg qAM
  6. Example: Schedule
    1. Morning: 20-40 mg orally
    2. Early afternoon: 20 mg orally
4. Daytrana (Methylphenidate patch)
  1. Start: 10 mg patch worn 9 hours daily
  2. Max: 30 mg patch worn 9 hours daily
  3. Skin irritation or rash may occur

Dosing
Adults with ADHD or Narcolepsy

Maximum total daily dose: 90 mg
Regular Release: 5 to 20 mg PO bid to tid at meals
Sustained Release: 20 mg PO up to q8 hours

Dosing
Elderly with comorbid Depression

Maximum total daily dose: 30 mg
Regular Release: 5 to 10 mg bid to tid

Management Difficulty Swallowing Medication - Long Acting Methylphenidate

Generic
1. Ritalin LA
2. Metadate CD Sprinkle caps
Trade Name - Expensive ($300/month)
1. Aptensio XR spinkle caps (lasts 12 hours)
2. QuilliChew ER chewable 20 and 40 mg tabs (lasts 8-13 hours)
3. Quillavant XR Suspension 5 mg/ml (lasts 12 hours)
4. Adhansia XR (lasts 13 hours)
5. Jornay PM (taken at night and peaks 14 hours later, the next morning)
6. Contempla XR 17.3 mg dissolving tablets (lasts 12 hours)
7. Daytrana Transdermal Patch 10 mg (lasts 10-12 hours)
References
1. (2016) Presc Lett 23(3):16

Drug Interactions

Avoid concurrent Decongestant use
Avoid within 14 days of MAO Inhibitor

Safety

Pregnancy Category C
Unknown safety in Lactation

Monitoring
Each Visit

Height
Weight
Blood Pressure
Pulse

Adverse Effects

See ADHD Medication

References