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Introduction to Stimulants

Introduction to Stimulants. Cesar A. Soutullo, M.D. UC-3 Psychopharm Lectures. 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

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Introduction to Stimulants

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  1. Introduction to Stimulants Cesar A. Soutullo, M.D. UC-3 Psychopharm Lectures

  2. 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

  3. 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

  4. 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

  5. Stimulants: Side Effects • Appetite suppression: HS snack • Effect on height rarely clinically signif • Sleep difficulty: dose before 4 pm •  Systolic BP (mild) • Exacerbate Tics & Tourette’s • Psychosis: discontinue • Rebound effects: • excitability, irritability 4-5 hrs after dose • give pm dose or use spansules

  6. 1.a. Methylphenidate [Ritalin] • Peak 1-2 hrs, half-life 2.5 • Total daily dose 1 mg/kg/day (0.6-2) • In >6 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 • Max> dose: 60 mg/day

  7. 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 • > 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

  8. 1.c. Adderall [dextr saccharate, sulph & amphet sulph, aspart] • Half-life 7-8 hrs • Dose like Dexedrine • Tablets 5, 10, 20, 30 mg

  9. 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)

  10. 2. Antidepressants in ADHD • TCAs: Helpful but caution • IMI. Cardiac SE,  hyperactivity 1 mg/kg/day & over • PR , 210 msec, QT < 450 msec HR<130 bpm • Desipramine: sudden death reports? • Bupropion: Sz • SSRI: Not helpful • Venlafaxine: Improves behavioral Sx?

  11. 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 > 150 mg/dose or 450 mg/day • Separate doses > 4 hours

  12. 3.a. Clonidine [Catapress] • Presinaptic Alpha-agonist, NE release •  frustration tolerance,  hyperarousal •  hyperactivity • Clonidine+Ritalin: 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

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