CNS stimulant

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CNS stimulant
2013-07-10 13:43:31

CNS stimulant
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  1. Direct acting adrenergic agonist
    Epi bind to a1 (vasoconstriction), b1 (inc HR), b2 (bronchodilation)
  2. Indirect acting adrenergic agonist
    block reuptake, block degradation, inc release (transporter)
  3. Mix-acting adrenergic agonist
    • Combination of direct and indirect
    • bind to post-receptor.
  4. a2 adrenergic receptor
    • high [] of NE at the junction --> bind to a2 --> dec release of NE 
    • adrenergic agonist acts as antagonist
  5. CNS Stimulants: use
    ◦Attention Deficit Hyperactivity Disorder


    ◦Weight Loss (suppress appetite)
  6. Narcolepsy
    quickly falls asleep (enter REM stage I real quick)
  7. Attention Deficit Hyperactivity Disorder (ADHD)
    —Epidemiology - usually > 3 years old

    —Incidence - occurs in 6% of all school-aged children

    —Genetic predisposition
  8. ADHD Diagnosis
    —Diagnosis: Based on 1994 American Psychiatric Association's DSM-IV

    • ◦Signs & Symptoms At Least Moderate In
    • Degree, In At Least 2 Settings

    • ◦Signs & Symptoms Present Before 7
    • Years Old, For At Least 6 Months

    • ◦Signs & Symptoms Should Be Considered
    • Inappropriate & Unmanageable
  9. ADHD diagnosis: symptoms
    • inattention
    • hyperactivity
    • impulsivity
  10. ADHD DSM-IV Classifications
    —Predominantly Inattentive

    —Predominantly Hyperactive/Impulsive

  11. ADHD - American Academy of Pediatrics (AAP) Recommendations
    —Use DSM-IV Criteria

    —Symptoms Must Be Present In More Than 1 Environment

    —Extensive Exam

    —Treat As a Chronic Condition
  12. ADHD Differential Diagnoses
    —Tourette’s syndrome

    —Conduct disorder

    —Learning disorders

  13. ADHD Comorbidities
    • —Learning Disabilities
    • ◦15-20% Of ADHD Patients
    • ◦50% Of LD Patients Have ADHD

    —Anxiety Or Mood Disorders = 10-20%

    —Oppositional Disorder/Antisocial Behavior In ~50% (ODD need to put to sleep during dental procedure)

    —Tic Disorders/Tourette’s Disorder In 60%

  14. need to put to sleep during dental procedure
    • ODD
    • Oppositional Disorder/Antisocial Behavior
  15. ADHD - Pharmacotherapy
    • —Methylphenidate
    • ◦Blocks Mainly Dopamine Reuptake

    • —Dextroamphetamine/Amphetamine
    • ◦Blocks Dopamine/Norepinephrine Reuptake
    • ◦Releases Dopamine/Norepi
    • ◦Mild MAO Inhibition

  16. ADHD medication in normal vs ADHD pt
    • normal: excitation
    • ADHD pt: calm down
  17. ADHD Stimulant Medications
    • —Motor Tics
    • ◦Decrease Or Stop Dose
    • ◦Add Clonidine (Atypical Antipsychotics??)

    —Drug Holidays (doesn't have to take daily)

    • —Efficacy
    • ◦Core Symptoms
    • ◦Helpful In Mental Retardation, Learning
    • Disabilities
  18. ADHD Stimulant Dosage Forms:
    Most common drug

    ◦Extended-release amphetamine and dextroamphetamine salts

    ◦Must be > 6 years old 

    Controlled substance -- need prescription: for abused drug
  19. ADHD – Norepi. Reuptake Inhibitor
    —Atomoxetine (Strattera®)
    • antidepressant 
    • work only on NE 
    • ◦Reported Helpful in Both ADD and ADHD

    ◦CYP2D6 Metabolized

  20. ADHD - Clonidine or Guanfacine
    • —α-2
    • Agonists

    —Alone Or With Stimulants

    —Slower Onset Than Stimulants

    —Not Effective For Inattention

    • —Uses:
    • ◦Most Commonly To Treat Drug-induced
    • Insomnia***
    • ◦Impulsivity, Hyperactivity & Conduct
    • Disorder
    • ◦Helpful In Tic Disorders
  21. ◦Modafinil (Provigil) - for narcolepsy
    ◦Increases Dopamine & Norepi Release

    ◦Increases Hypothalamic Histamine Levels (not scheduled drug)

    ◦Abuse Potential?

    ◦Amphetamines Also Used
  22. Phentermine (Adipex-P) - for weight loss
    • ◦Stimulates CNS Dopamine and Norepi
    • Release
    • → Appetite Suppression

    • ◦Activates Hypothalamus to Stimulate
    • Adrenal Norepi Release
  23. Ephedrine
    —Mixed-acting Adrenergic Stimulant: cause release of NE and act on a and b receptor 

    —“Gentle Epinephrine”: moderate in BP and HR (compared to epi) --> used in anesthesia and 

    —Used in Anesthesia Practice

    • —Was Used In Past For Weight Loss & Asthma
    • ◦No Longer Marketed Orally
    • ◦Pseudoephedrine Now Used (less abused, not affecting CNS and PNS) 

    —Drug Interactions

    —Was Present in Past in Ma Huang and Other Herbal Products
  24. Meth-ephedamine
    rush release of dopamine acting on the pleasure center

    high abuse potentials
  25. Sympathomimetic Stimulants : adverse rxn



    • ◦Cardiovascular stimulation
    • –Hypertension
    • –Sudden death

    • ◦Abuse
    • liability
  26. Xanthine Derivatives: caffeine, theophylline salt
    Pharm effect
    ◦CNS stimulation

    • ◦Cardiovascular effects similar to
    • epinephrine
  27. Xanthine Derivatives: caffeine, theophylline salt
    Mechenism of action
    ◦Adenosine receptor antagonism

    ◦Blockade of phosphodiesterases (e.g., PDE IV)

    ◦Histone deacetylase activation

    ◦Acetylated Histones Activate Some DNA
  28. Theophylline salts
    bronchodilation for asthma  

    narrow margin of therapeutic
  29. PDE IV inhibitor
    inc HR and BP (mild)
  30. Xanthine Derivatives: —Therapeutics
    ◦Bronchial asthma (theophylline)

    ◦Chronic obstructive pulmonary disease (theophylline)

    ◦Premature apnea (caffeine)

    ◦Increased wakefulness (caffeine)

    ◦In analgesics (caffeine)
  31. Xanthine Derivatives: adverse effect

    ◦Cardiovascular stimulation

    ◦CNS stimulation/insomnia/seizures