Pharmacology Final

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Rx2013
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55157
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Pharmacology Final
Updated:
2010-12-11 23:32:51
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Drugs Abuse
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Drugs of Abuse
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  1. drug abuse
    drug used for non-medical purpose
  2. drug misuse
    drug is taken for a medical purpose incorrectly
  3. Psychological dependance
    • drug seeking behavior
    • always comes first
  4. Physiological dependance
    signs of withdrawl
  5. Drug withdrawl results in
    drug-class specific physiological changes
  6. Drug addiction
    when use becomes excessive and difficult for the person to stop using the drug
  7. Tolerance
    • decreased response to effects of the drug over time
    • marked increase in the amount of substance required to achieve the same effect
  8. metabolic tolerance
    • increased metabolism of the drug
    • ex. decreased half life of barbiturates
  9. Behavioral tolerance
    • a learned skill to reduce drug's influence
    • ex. alcohol
  10. Functional tolerance
    • compensatory changes in receptor
    • most common tolerance
    • receptor internalization
  11. Reverse tolerance
    • increased response with repitition of the same drug dose
    • ex. amphetamine
  12. Cross tolerance
    • tolerance to other drugs
    • ex. amphetamine vs. meth
    • caffeine vs. nicotine
    • psilocybin vs. mescaline
  13. Detoxification
    • treatment for drug dependance
    • substitute a longer acting drug
    • prevent withdrawl symptoms
  14. Goal of detoxification
    acheive a complete withdrawal of drug while not inducing any withdrawal syndromes
  15. Areas in the brain that produce dopamine
    • ventral tegamental area
    • substantia nigra
  16. most important area in the brain for drug abuse
    • VTA
    • mesolimbic pathway
  17. Therapeutic form of dopamine
    L-Dopa
  18. 4 major dopaminergic pathways
    • mesolimbic pathway
    • mesocortical pathway
    • nigrostraital pathway
    • tuberoinfundibular pathway
  19. Mesolimbic pathway
    • drug dependance
    • VTA-nucleus accumbens
  20. Mesocortical pathway
    • schizophrenia
    • VTA-frontal cortex
  21. Nigrostriatal pathway
    • motor control
    • parkinsons disease
    • substantia nigra-striatum
  22. Tuberoinfundibular Pathway
    • hormone secretion
    • hypothalamus-pituitary
  23. Which one of the following dopamine pathway is associated with PD?
    A. Mesocortical
    B. Nigrostriatal
    C. Tueroinfundibular
    D. Mesolimbic
    B. Nigrostriatal
    (this multiple choice question has been scrambled)
  24. Hijacked brain hypothesis
    • brain is hijacked during recreational use
    • not true because only occurs in 32% of tobacco users
  25. FosB/DFosB
    • postsynaptic molecule in dopamine signaling
    • Genetic basis of adiction
  26. Nonaddictive drugs act on this area of the brain
    cortical and thalamic
  27. LSD acts on this receptor
    5-HT2A in prefrontal cortex
  28. PCP and ketamine act on
    NMDA glutamate receptor
  29. Long term effects of chronic PCP use
    irreversible schizophrenia like psychosis
  30. Drugs taht bind and activate G-protein coupled receptors
    • Opioids
    • Cannabinoids
    • GHB
    • LSD, mescaline, psilcybin
  31. Opioids
    • MU-OR
    • Agonist
    • disinihibition of DA
    • 4
  32. Cannabinoids
    • CB1-R
    • Agonist
    • Disinhibition of DA
    • 2
  33. Y-Hydroxybutyric acid (GHB)
    • GABAb - R
    • Weak agonist
    • Disinhibition of DA
  34. LSD, Mescaline, Psilocybin
    • 5-HT2A-R
    • Partial agonist
    • 1
  35. Drugs that bind to ionotropic receptors and ion channels
    • nicotine
    • alcohol
    • benzodiazepines
    • phencyclidine, ketamine
  36. Nicotine
    • nACh - R
    • Agonist
    • Excitation of DA neurons
    • 4
  37. Alcohol
    • GABAa, 5-HT3, nACh, NMDA, Kir3
    • Excitation/disinhibition of DA neurons
    • 3
  38. Benzodiazepines
    • GABAa
    • Positive modulator
    • disinhibition of DA neurons
    • 3
  39. Phencyclidine, ketamine
    • NMDA
    • antagonist
    • 1
  40. Drugs that bind to biogenic amines
    • Cocaine
    • Amphetamine
    • Ecstacy
  41. Cocaine
    • DAT, SERT, NET
    • Inhibitor
    • blocks DA uptake
    • 5
  42. Amphetamine
    • DAT,NET,SERT,VMAT
    • reverses transport
    • Blocks DA uptake, synaptic depletion
    • 5
  43. Ecstasy
    • SERT > DAT
    • reverses transport
    • blocks DA uptake
  44. Schedule I
    • high abuse potential
    • no medical use
  45. Schedule II
    • High abuse potential
    • Medical use with severe restriction
    • Psychological and physical dependance
  46. Schedule III
    • Abuse potential less than I and II
    • mediacl use
    • moderate or low psyc and phys. dependance
  47. Schdule IV
    • abuse potential less than III
    • aceptable medical use
    • Psyc and phys. dependance less than III
  48. Schedule V
    • Minimal abuse potential
    • acceptable medical use
    • limited dependance risk
  49. Schedule I drugs
    • MDMA
    • Ecstasy
    • GHB
    • heroin
    • psilocybin/psilocyn
    • mescaline
    • LSD
  50. Schedule II Drugs
    • Cocaine
    • Codeine
  51. Schedule III drugs
    • anabolic steroids
    • buprenorphine
    • dronabinol
    • ketamine
  52. schedule IV drugs
    pams
  53. scheduel V drugs
    codeine preparations
  54. 4 major types of opioids
    • natural
    • semi-synthetic
    • synthetic
    • endogenous
  55. Natural opiods
    • morphine
    • codeine
    • thebaine
  56. Semi-synthetic opioids
    heroin
  57. synthetic opioids
    • fentanyl
    • methadone
    • meperidine
  58. Endogenous opioids
    • endorphin
    • enkephalins
    • dynorphin
  59. Drugs abused by healthcare professionals
    • fentanyl
    • heroin
    • meperidine
  60. Opioid receptors
    • MU
    • delta
    • kappa
  61. Drugs that bind the MU receptor
    • morphine
    • heroin
  62. drugs that bind the delta opioid receptor
    enkephalin
  63. drugs that bind the kappa opioid receptor
    dynorphin and other endogenous
  64. drugs that have poor oral bioavalibility
    • heroin
    • morphine
  65. drugs used to treat acute and chronic pain
    • fentanyl
    • oxymorphone
    • hydromorphone
    • morphine
  66. drugs used to treat cough
    • codeine
    • dihydrocodeine
    • ethylmorphine
  67. drugs used to treat diarrhea
    • loperamide
    • difenoxin
    • morphine
  68. Drugs used to treat severe diarrhea
    morphine
  69. drugs used to treat anxiety due to shortness of breath
    • oxymorphone
    • dihydrocodeine
  70. ways to use heroin
    • sniffing
    • orally
    • smoking
  71. Typical heroin dose produces effec within
    3-5 hours
  72. Early withdawal symptoms
    • lacrimation
    • rhinorrhea
    • yawning
    • sweating
  73. Later symptoms of withdrawal
    • hypothermia
    • hypotension
    • bradycardia
    • mydriasis
  74. Withdrawal syndrom can be precipitated by administereing an
    antagonist
  75. Treatment for addiction
    • Naloxone
    • Methadone
    • Clonidine
  76. Naloxone
    • acute toxicity by heroin
    • short half life
  77. methadone
    longer acting
  78. clonidine
    inhibit sympathetic overactivity like nausea, vomitting, cramps, hypertension
  79. Morphine and disease/pregnancy
    • enhances HIV replication
    • accelerates HIV/AIDS
    • reduces IFN-alpha expression
    • increases HCV replication
    • Increases bacterial infection (morph and codeine)
    • low birthweight & development delay (heroin, MSO4)
  80. Marijuana
    tip of femal plant used for smoking
  81. Hasish
    concentrated resin physically extracted by rubbing or with ice
  82. kief
    sticky resin of the plant before pressed into hasish
  83. Hash oil
    ethanol extract of cannabis
  84. tetrahydrocannabinol (THC)
    bind cannabinoid receptor
  85. three types of cannabinoids
    • Phytocannabinoids
    • endogenous cannabinoids
    • synthetic cannabinoids
  86. marinol (dronabinol)
    • analgesic
    • appetite stimulant
    • antiemetic
    • schedule III
  87. Nabilone (cesamet)
    schedule 2
  88. Sativex
    cannabinoid extract oral spray
  89. Treatment for marijuana addiction
    rimonabant CB1 antagonist
  90. LSD, Mescaline & Psilocybin
    • hallucinogens
    • psychotomimetics
    • GPCR 5-HT2A
  91. LSD is an antagonist for
    5-HT2
  92. LSD is an Agonist for
    5-HT1A & 5-HT1C
  93. 5-HT2 activity has good correlation with
    hallucinogenic potency
  94. Effects of LSD
    • distorted sensory perception
    • colors seem bright & vivid
    • objects appear distorted
    • Auditory perception is enhanced
    • time sense is distorted
  95. physical effects of LSD
    • increased HR and BP
    • n/v
    • stomach pain
  96. Mescaline
    • cactus buds
    • 1000-3000x less potent than LSD
    • 30x less potent than psilocin
  97. Receptor that mescaline acts on
    5-HT2A
  98. Psilocybin
    • found in fungi
    • a prodrug for psilocin
  99. psilocybin acts on the ____ receptor
    5-HT1A/2A/2C
  100. Psilocybin is metabolized by
    • MAO in the liver
    • MAOIs would inhance effects
  101. GHB
    • a neuroprotective drug for narcolepsy
    • acts through GABAb
    • date rape drug
    • alcohol enhances sedative effects
  102. Active metabolite of nicotine
    cotinine
  103. Nicotine acts on the ____ receptors
    nAChRs
  104. Alcohol
    • most widely used substance
    • third leading cause of death
  105. binge drinking
    • >4 femal
    • >5 male
  106. Heavy drinking
    • >1 F
    • >2 M
  107. Alcohol metabolism
    • 90% oxidized in the liver
    • remainder is excreted in the lungs and urine
  108. Two major pathways of alcohol metabolism
    • alcohol dehydrogenase pathway
    • Microsomal Ethanol Oxidizing System (CYP2E1)
  109. CNS effects of alcohol consumption
    • sedation and anxiolytic
    • slurred speech
    • ataxia
    • impaired judgement
  110. CV effects of alcohol
    depressed myocardial contractility
  111. Smooth muscle effects of alcohol
    • muscle relaxtion due to aldehyde
    • hypothermia
  112. Women are more susceptible to alcohol effects because
    less alcohol dehydrogenase
  113. Immune system effects of alcohol
    • decreas in:
    • alveolar macrophage
    • T cell & B cell
    • aquired immune response
    • Th1/Th2 switch
  114. Not so common Fetal Alcohol Syndrome abnormalities
    • congenital heart defects
    • neurological deficits
  115. Treatment for alcoholism
    • naltrexone
    • acamprosate
    • disulfiram
  116. Naltrexone
    • orally active MU opioid receptor antagonist
    • do not use in pt. on opioids
  117. Acamprosate
    • reduces relaps when used with psychotherapy
    • may cause GI discomfort and rash
  118. Disulfiram
    • aldehyde dehydrogenase inhibitor
    • acetaldehyde accumulates in the system
    • no effects on non-drinkers
    • causes flushing, throbbing, n/v, hypotension in alcoholics
  119. Three types of benzodiazepines
    • short term
    • medium and long acting
  120. BZDs for anticonvulsant use
    • lorazepam
    • diazepam
  121. BZD for anxiolytic
    • bromazepam
    • chlordiazepoxide
    • clorazepate
    • medazepam
    • nordazepam
  122. BZDs for mild insomnia
    • flurazepam
    • quazepam
    • estazolam
  123. BZDs for moderate insomnia
    • lormetazepam
    • midazolam
    • loprazolam
    • brotizolam
    • nitrazepam
  124. BZDs for severe insomnia
    • triazolam
    • nimetazepam
    • temazepam
    • flunitrazepam
    • flutoprazepam
  125. BZDs used to premedicate for procetures
    • Diazepam
    • Temazepam
  126. BZDs used for ETOH dependancy
    • Diazepam
    • Chlordiazepoxide
    • Lorazepam
    • Oxazepam
  127. Contraindications for BZDs
    • pregnancy
    • labor
    • lactation
    • mysthania gravis
    • chronic psychosis driving
  128. BZD interaction with ETOH
    synergistic effect
  129. BZD with antacid
    slows down absorption
  130. BZD with oral contraceptives
    increases half life
  131. BZDs + Isoniazid
    increased half life
  132. BZDs+Rifmpacin
    increase metabolism rate
  133. BZDs with L-Dopa
    worsening of parkinsonian symptoms
  134. Ketamine and PCP
    • both developed as anesthetics
    • only ketamine is used
  135. shows neuroprotective against ischemic brain injury
    ketamine
  136. Cocain
    • tropane alkaloid
    • CNS stimulant
    • appetite suppressant
    • inhibits SET, DAT and NET reuptake
  137. Physical effects of amphetamines
    • reduced appetite
    • increased/distorted sensations
    • hyperactivity
    • dilated pupils
    • flushing
    • ED, increased RR and BP
  138. Psychological effects
    • anxiety/nercousness
    • euphoria
    • creative thinking
    • increased energy/well being sense
    • goal oriented thoughts
  139. Ecstasy (MDMA) results in
    • Hyperthermia
    • dehydration
    • serotonin syndrome
    • seizure

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