CNS stimulant

The flashcards below were created by user ghrelin23187 on FreezingBlue Flashcards.

  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
Card Set:
CNS stimulant
2013-07-10 17:43:31

CNS stimulant
Show Answers: