Stimulant Medications for Patient Requiring Stimulation
Methylphenidate (MPH), dextroamphetamine (DEX), or amphetamine (AMP) are the recommended first-line stimulant medications, with methylphenidate typically preferred as the initial choice due to its slightly more favorable side effect profile regarding appetite and sleep. 1
Primary Stimulant Options
The American Academy of Child and Adolescent Psychiatry guidelines establish three primary stimulant medications for clinical use:
- Methylphenidate (MPH) - Starting dose of 5 mg, typically given twice daily (morning and noon), with titration in 5 mg increments 1
- Dextroamphetamine (DEX) - Starting dose of 2.5 mg, may require only once-daily dosing initially 1
- Mixed amphetamine salts (AMP) - Starting dose of 2.5 mg, similar dosing pattern to DEX 1
Methylphenidate is generally selected first because amphetamine and dextroamphetamine produce greater problematic effects on appetite and sleep, consistent with their longer excretion half-lives. 1
Clinical Indications for Stimulant Use
Stimulants are indicated for the following conditions:
- ADHD (all subtypes) - Patients must demonstrate moderate to severe impairment in at least two different settings 1
- ADHD with comorbid conditions - Including oppositional defiant disorder, conduct disorder, anxiety disorders, and learning disorders 1
- Narcolepsy - Patients with excessive sleepiness, recurrent sleep attacks, and cataplexy 1
- Apathy due to general medical condition - Brain injury from cerebrovascular accident, trauma, HIV, or degenerative neurological illness; doses typically lower than ADHD treatment 1
- Adjuvant medical uses - Severe psychomotor retardation in medically ill patients secondary to illness, sedative pain medications, or chemotherapy; low doses enable increased alertness and energy 1
- Treatment-refractory depression - Methylphenidate used to augment tricyclic antidepressants; doses lower than ADHD treatment 1
Absolute Contraindications
Do not prescribe stimulants under these circumstances:
- Concomitant MAO inhibitor use - Results in severe hypertension and cerebrovascular accident risk; MAO inhibitors must be discontinued at least 2 weeks before starting stimulants 1, 2
- Active psychotic disorder - Stimulants are psychotomimetic in schizophrenia, psychosis NOS, or manic episodes with psychosis 1, 2
- Glaucoma - Sympathomimetic effects may increase intraocular pressure 1, 2
- Symptomatic cardiovascular disease, hyperthyroidism, or hypertension - Stimulants cause clinically important increases in heart rate and blood pressure 1, 2
- Previous sensitivity to stimulant medications 1
- Pemoline specifically - Contraindicated with preexisting liver disease or abnormal liver function tests due to documented hepatotoxicity and risk of total liver failure 1, 2
Relative Contraindications Requiring Caution
- History of stimulant abuse or dependence - Not an absolute contraindication but requires controlled setting or close supervision; patients with other substance use histories (alcohol, opiates, benzodiazepines) may still receive stimulants with careful monitoring 1, 2
- Unstable mood disorders - Stimulants can produce dysphoria in vulnerable patients 1, 2
- Seizure disorders - Stabilize on anticonvulsants before initiating stimulant treatment 1, 2
Conditions No Longer Considered Contraindications
Recent controlled trials have refuted several traditional contraindications:
- Motor tics and Tourette's syndrome - Controlled studies show methylphenidate does not worsen motor tics 1, 2
- Anxiety disorders - Children with comorbid anxiety improve on methylphenidate 1, 2
- Age under 6 years - Eight published reports demonstrate methylphenidate efficacy in this age range, though package inserts still warn against use 1, 2
Dosing Algorithm
Initial titration schedule:
- Week 1 (Baseline) - Obtain blood pressure, pulse, height, weight, and ADHD rating scales 1
- Week 2 - MPH 5 mg or DEX/AMP 2.5 mg twice daily (after breakfast and lunch); assess via office visit 1
- Week 3 - MPH 10 mg or DEX/AMP 5 mg twice daily; assess via office visit or phone 1
- Week 4 - MPH 15 mg or DEX/AMP 7.5 mg twice daily (omit in children <20 kg); assess via office visit or phone 1
- Week 5 - MPH 20 mg or DEX/AMP 10 mg twice daily; assess via office visit 1
Maximum doses:
- Children and adolescents - MPH up to 60 mg/day or 1.0 mg/kg; DEX/AMP up to 40 mg/day or 0.9 mg/kg 1
- Adults - Similar maximum doses, though higher total daily doses may be needed to cover longer waking hours 1
Response Optimization
Approximately 70% of patients respond to either DEX or MPH alone; nearly 90% respond if both stimulants are tried sequentially. 1 If the first stimulant fails or produces prohibitive side effects, switch to the alternative stimulant rather than abandoning stimulant therapy. 1
Critical Monitoring Requirements
- Baseline assessment - Physical examination including blood pressure, pulse, height, and weight before initiating treatment 1
- Children - Annual vital sign checks during routine physical examination 1
- Adults - Quarterly blood pressure and pulse monitoring 1
- Growth monitoring - Essential in pediatric patients; interrupt treatment if not growing or gaining weight as expected 2
Common Pitfalls to Avoid
Do not use pemoline as a first-line agent - Despite efficacy, it carries risk of hepatic failure with 13 documented cases of total liver failure (11 resulting in death or transplantation), representing a rate 4-17 times higher than expected in the normal population. 1
Avoid premature dose escalation - Use minimum effective doses to initiate therapy and titrate based on validated rating scales from multiple sources (teachers, parents, significant others), not solely on subjective patient report. 1
Do not overlook cardiovascular screening - All patients require baseline cardiovascular assessment, as stimulants cause clinically significant increases in heart rate and blood pressure. 2