Introduction to Stimulants

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Introduction to Stimulants

• Cesar A. Soutullo, M.D.
• UC-3 Psychopharm Lectures

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1. Stimulants

• Use throughout the day on wk-ends
• Not only during school
• Improve social interact, leisure particip.
• Improve oppositional, aggressive behaviors
• Methylphenidate short acting
• Dextroamphetamine long acting
• Ritalin-SR, Dex-Spans longer

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1. Stimulants

• Use throughout the day on wk-ends
• Not only during school
• Improve social interact, leisure particip.
• Improve oppositional, aggressive behaviors
• Methylphenidate short acting
• Dextroamphetamine long acting
• Ritalin-SR, Dex-Spans longer

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Stimulants Pharmacokinetics

• Ritalin Liver met, kidney excret
• Peak Serum Level 1.9 hr 0.3 - 4.4 hr
• SR 4.7 hr 1.3-8.2 range
• Half-life 2-2.5 hrs.
• Dexedrine Liver met, kidney excret
• Peak 2 hrs (Spansule 8-10 hr)
• Half-life 6-8 hr kids / 10-12 adults

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Stimulants Side Effects

• Appetite suppression HS snack
• Effect on height rarely clinically signif
• Sleep difficulty dose before 4 pm
• ? Systolic BP (mild)
• Exacerbate Tics Tourettes
• Psychosis discontinue
• Rebound effects
• excitability, irritability 4-5 hrs after dose
• give pm dose or use spansules

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1.a. Methylphenidate Ritalin

• Peak 1-2 hrs, half-life 2.5
• Total daily dose 1 mg/kg/day (0.6-2)
• In gt6 y.o. start 5 mg qd or bid (AM 12)
• raise 5-10 mg/wk, (can add 4 pm dose)
• Tablets 5, 10, 20 mg
• SR 20 mg
• Maxgt dose 60 mg/day

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1.b. Dextroamphetamine Dexedrine

• Half-life 6-8 hrs
• Optimal dose 0.3-1.5 mg/kg/day
• age 3-5 2.5 mg/d, ? 2.5 once-twice wk
• gt 6 yo 5 mg/d, ? 5 mg once-twice wk
• Tablets 5 mg, scored
• Spansules 5, 10, 15 mg
• Max dose 40 mg/day
• Better for pt. with Seizures

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1.c. Adderall dextr saccharate, sulph amphet
sulph, aspart

• Half-life 7-8 hrs
• Dose like Dexedrine
• Tablets 5, 10, 20, 30 mg

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1.d Mg Pemoline Cylert

• Least abuse potential
• Rx once a day 37.5 mg/d
• Max dose 112.5 mg/day
• Reduced use, Side effects
• choreoathetoid movements
• insomnia
• chronic hepatitis
• fulminant liver failure (rare)

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2. Antidepressants in ADHD

• TCAs Helpful but caution
• IMI. Cardiac SE, ? hyperactivity
  1 mg/kg/day over
• PR , 210 msec, QT lt 450 msec HRlt130 bpm
• Desipramine sudden death reports?
• Bupropion Sz
• SSRI Not helpful
• Venlafaxine Improves behavioral Sx?

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2.b. Bupropion Wellbutrin

• ? Hyperactivity-Impulsivity
• Improve cognitive performance?
• Effects DA reuptake block
• Start 37.5 to 50 mg bid, gradual increase
• Seizure risk
• Do not use gt 150 mg/dose or 450 mg/day
• Separate doses gt 4 hours

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3.a. Clonidine Catapress

• Presinaptic Alpha-agonist, ?NE release
• ? frustration tolerance, ? hyperarousal
• ? hyperactivity
• ClonidineRitalin 3 cases sudden death
• EKG, Hx of Syncope, FHx sudden death
• Helpful in ADHD Tics
• Start Dose 0.05 mg hs (tablets 0.1 mg)
• slow up to 0.15-0.3 mg/day
• Slow D/C, rebound hyypertension
• Skin patch toxic if eaten or damaged