Stimulants
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  • 1. Psycho-stimulants: Cocaine, Amphetamines ADD/ADHD Weight Loss Nasal Decongestants
  • 2. Map of Principal Coca-Growing Regions in South America
  • 3. History
  • 4.  
  • 5.
      • Coca leaves used indigenously in South America
      • Cocaine isolated from coca in 1859 by Niemann
      • Freud shared cocaine with his fiancee, composed a “Song of praise” to cocaine. Addicted in 1884, he named cocaine the “third scourge of humanity.” Title Page of Freud’s Tribute to the Virtues of Cocaine
    • .
  • 6.
    • 1888: Asa Candler, a devout Christian, bought the rights to CocaCola, a temperance beverage It contained cocaine until 1903
  • 7.  
  • 8. Reasons Why You Should Use Cocarettes!!
    • 1 st —They are not injurious.
    • 3 rd —They are made of the finest Sun-cured Virginia Tobacco
    • 5 th —The Coca neutralizes the depressing effects of the Nicotine in the tobacco.
    • 6 th - Coca is the finest nerve tonic and exhilarator ever discovered
    • 8 th – Can be freely used by persons in delicate health without injury and with positively beneficial effects
  • 9. Cocaine
    • Financial, psychological, & physical control over the user
    • 2 nd most common emergency dept visit (#1 alcohol in combo with other drugs) (DAWN 2004)
    • Street Names: snow, coke, blow, toot, white lady, crack, ready rock, rock candy
  • 10. Cocaine preparations
    • Coca leaves (1% cocaine)
    sulfuric acid Coca paste (60-80% cocaine) hydrochloric acid Cocaine HCl (80%+ cocaine, but less potent) Boil with water and either baking soda or ammonia Cocaine free base (No HCl) Crack cocaine Boil with ether
  • 11. Enzyme metabolism of cocaine
    • Butyrylcholinesterase (BChE)
        • Found in plasma and in red blood cells
        • Metabolizes cocaine, aspirin, amitriptyline; activates heroin
        • Red blood cell activity more effective metabolizing cocaine
          • Women have more red blood cell BChE
          • Women are less susceptible to cocaine effects
          • Women even more immune in luteal phase: Mucous secretion decreases absorption of snorted cocaine
      • BChE also protects against cocaine toxicity and nerve agent toxicity
  • 12. Administration
    • Powder most often inhaled (snorted)
        • Causes vasoconstriction limits amount absorbed
    • Injected (IV)
    • Swallowed (oral or by chewing coca leaves)
    • Smoked
      • Freebase
        • More intense effect direct systemic circulation
        • Dangerous to make & use, solvents flammable and may explode
      • Crack Cocaine
        • Freebase without volatile chemicals
        • Affordable, available is smaller amounts
  • 13.  
  • 14.  
  • 15. Pharmacokinetics
    • Absorption
      • Intranasal: 20-30%, plasma peaks in 30-60 min.
      • Smoke: 6-32%, plasma peaks at 5 min.
      • Intravenous: 100%, immediate, 60 sec to brain
    • Distribution
      • Easy access to brain
      • Concentration in brain exceeds plasma level
      • Crosses placental barrier freely: Crack babies
  • 16. Pharmacokinetics
    • Rapidly metabolized by liver
    • Elimination t 1/2 oral, nasal, IV (50, 80, 60 minutes)
    • User may need drug every ½ hr or less to maintain high
    • Metabolite benzoylecgonine 48 hrs-2 weeks
    • Metabolite cocaethylene results when cocaine and alcohol are in the body at the same time. Cocaethylene acts like cocaine, and is more toxic.
  • 17. Dose-dependent effects
    • Dosage/Method
    Outbursts Stereotypic Paranoia Insomnia Agitation Increase BP Lower appetite Improve mood Alertness Low Medium High
  • 18. Pharmacodynamics
    • Local anaesthetic and vasoconstrictor
    • Blocks reuptake of monoamine NTs
    • Blocking reuptake of DA produces stimulation and behavioral reinforcement.
    • Ventral tegmental area (VTA) DA neurons project to medial prefrontal cortex, nucleus accumbens, amygdala, and hippocampus.
    • Cocaine blocks DA transporter proteins.
  • 19. Stimulants Side Effects
  • 20.  
  • 21. Long-term Pharmacodynamics
    • Presynaptic DA transporter levels in nucleus accumbens and VTA rise with abstinence, then fall for several months.
    • These phenomena produce a prolonged abstinence syndrome in the reward systems.
    • Result? Feeling miserable and craving.
    • Tolerance develops through decreased numbers of postsynaptic receptors.
  • 22. Signs & Symptoms of Acute Intoxication
    • Increased, temp. stimulation, BP, HR
    • Euphoria, giddiness, boastfulness for 30 minutes, then 60-90 minutes of mild euphoria and anxiety
    • Anorexia
    • Agitation, insomnia
    • Hallucinations
    • Seizures, death
    • Restlessness, anxiety persists for hours; depression rebound
    • Nasal Passage Damage
    • Lung damage
    • Intense, short term high followed by dysphoria
    • Death from overdose
  • 23. Hazards of Use
    • Intense psychological & physical dependence
    • Life threatening cardiac dysrhythmias, hypertension, hemorrhagic cerebrovascular accident
  • 24.  
  • 25. PET images
  • 26.  
  • 27.  
  • 28.  
  • 29. High Dose Effects & Safety Risks
    • Lethal level
    • Chronic Users
      • Toxic paranoid psychosis
      • Skin Eruptions
        • Cocaine bugs
    • Circulatory Collapse
      • Strokes and myocardial infarction
    • Psychiatric disorder
      • Psychosis, suicide, delirium
  • 30. Reinforcement Potential of Cocaine
    • Low doses are reinforcing
    • Cocaine craving follows
    • Self-administration of cocaine persists in the face of punishment
    • Withdrawal increases craving
    • May heighten sexual interest, but does not improve potential or performance
  • 31. Fetal Effects
    • Vasoconstriction of uterus and placenta
      • Stillbirth and Preterm labor
    • Congenital Malformations
      • Aberrant brain and heart development
      • Cerebral infarction & hemorrhage
      • Sudden Infant Death
    • Neonatal Complications
      • Acute fetal withdrawal
      • Neurobehavioral delays
        • Educational difficulties, easily frustrated
        • Difficulty dealing with stimulation
        • Attachment disorder, AD/HD
  • 32. Treatment Models
    • Needs analysis
      • Begin abstinence
      • Diagnose co-morbid disorders
      • Relate cocaine use to disorders
      • Maintain abstinence while treating disorders
      • Prevent relapse
  • 33. Additional Treatment Models
    • Abstinence pattern analysis
      • Crash: 9 hours to 4 days, “out of it”
      • Withdrawal: 1 to 10 weeks, craving and relapse
      • Extinction: Indefinite, cued craving
    • Pharmacotherapy
      • Antagonize cocaine: Not yet
      • A cocaine version of Antabuse: Not yet
      • Treat comorbid problems: Antidepressants
      • Reduce cocaine craving: Dopamine agonists
  • 34. Amphetamines
    • Therapeutic Classification
      • Similar to natural catecholamines
        • Epinephrine, norepinephrine, dopamine
        • Sympathomimetic agents
    • Three Types
      • Amphetamine
        • Speed, amp, jelly, rippers, uppers, Bennies
      • Dextroamphetamine
        • Dexies
      • Methamphetamine
        • Moth, crystal, meth, black beauties
  • 35. Pharmacokinetics
    • Administration
      • Swallowed in pill or capsule
      • Injected into veins- orgasmic feeling “rush”
    • Alkalizing Urine to
        • pH of 5 T 1/2 = 5-6 hours
        • pH of 7 T 1/2 = 20 hours
  • 36. Pharmacodynamics
    • Peripheral NS effects: Sympathomimetic
      • Constrict blood vessels: Elevate blood pressure, heart rate
      • Irritability, nervousness, mood swings
    • CNS effects: Psychostimulant
      • Increases in motor activity
      • Insomnia, Loss of appetite
      • Hallucinations, paranoia, seizures, coma
  • 37. Neurotransmitter Effects
    • Increase release & block reuptake of natural catecholamines
      • Fight or Flight Effect
      • Dopamine and norepinephrine activation
      • Dopamine on basal ganglia: High dose stereotype and aggression
      • Counterintuitive calming effects in AD/HD
  • 38. Signs and Symptoms of Intoxication
    • Elevated HP, HR, dysrhythmias,
    • Dilated pupils reactive to light
    • Hyperactive tendon reflexes
    • Shallow respiration
    • Circulatory collapse
    • Clear or confused sensorium
      • Hallucinations, paranoid feelings
  • 39. Club Drug
    • MDMA (Ecstasy) 3,4-Methylenedioxymethamphetamine
      • Combined w/other substances of abuse
        • Heroin = chocolate chip cookie
        • CI no legit use, high abuse potential
      • Liver metabolized
      • Ingested
        • Onset 30-60 minutes up to 4 hours
        • ‘Crash’ 4-12 hrs after dose
        • Post depression can last up to 5 days
  • 40. Symptoms of Use Hazards
    • Muscle tension
    • Teeth clenching
    • Blurred vision
    • Faintness, chills & sweating
    • Confusion
    • Depression
    • Sleep disorders
    • Anxiety, paranoia
    • Long term memory impairment
    • Parkinson’s Dz
    • Eventual paralysis
  • 41. Attention Deficit Disorder & Attention Deficit Hyperactivity Disorder
  • 42. Sample Diagnostic Criteria
    • Inattention
      • Underperforming
      • Fails to notice details
      • Does not seem to listen/easily distracted
      • Lacks follow through
      • Lacks organization
      • Avoids sustained mental effort/focus
      • Loses things/forgetful
    • Hyperactivity-Impulsivity
      • Fidgets, leaves seat often
      • Runs, climbs excessively
      • Difficulty in quiet time
      • Talks excessively
      • “ on the go”, “driven by a motor”
  • 43. Stimulant treatment of AD/HD
    • 1.29 million children currently taking stimulants to treat AD/HD
      • About half of cases persist into adulthood
      • AD/HD increases antisocial personality disorder risk 10X, and perhaps in connection, quintuples incidence of drug abuse
      • Stimulants slow growth of children, but this also rebounds with abstinence: the drug holiday
    • See http://www.fmsnutrition.com/adhd_self_testing_or_test.htm for an AD/HD self-test.
    • How do stimulants treat AD/HD?
  • 44. Selected Stimulant Medications Long Acting Concerta, Metadate CD, Ritalin LA, Adderall XR, Dexedrine Spansules, Daytrana Patch Atomoxetine(Strattera) Intermediate Acting Metadate ER, Ritalin SR Short Acting Ritalin, Adderall, Dexedrine, Dextrostat
  • 45.  
  • 46. Anorectic Agents Oily spotting, flatus, discharge, fecal urgency, GI Orlistat (Xenical) Alli (OTC) Decrease absorption of fat Lipase Inhibitor FDA does not recommend. HTN, DM, glaucoma Ephedra, guarana, chromium picolinate Increase basal metabolic rate Herbals Nervous, HA, HR, BP, palpitations, irritable Fastin, Meridia Ionamin, Beta receptors in hypothalamus Stimulants Side Effects Agent MOA Drug Class
  • 47. Ephedra banned but………….
    • Bitter orange
    • Kola nut
    • Green tea extract
    • Creatine
    • Willow bark
    • Protein drinks
    • Caffeine products
    • Coffee caffeine 60-180mg/cup
    • Coffee decaf 3-5 mg
    • Tea 20-90 mg/cup
    • Colas 15-30 mg
    • Milk Chocolate 3-6 mg/ounce
    • Dark Chocolate 5-35mg/ounce
  • 48. Moderation Common Sense
  • 49.
    • Deconsal II (phenylephrine 20mg & guaifenesin 375mg)
  • 50. Ephedrine, pseudoephedrine, and phenylephrine for nasal decongestion