Pharm Mod 3 CNS

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  1. Amino acid building block of Serotonin.
    tryptophan
  2. Amino acid building block of NE.
    Tyrosine
  3. With depression, there is decreased ______ and/or _______ neurotransmission
    • serotonin
    • norepinephrine
  4. Purpose of serotonin or NE binding to autoreceptor.
    provides negative feedback to neuron to stop synthesis or release of NT
  5. SSRIs inhibit __________ back into the cell
    transport of 5HTP
  6. When serotonin or NE is reuptaken into cell, what two things could happen?
    • repackaged and released
    • broken down by MAO
  7. After some time of treatment with antidepressants, _______ are downregulated.
    • autoreceptors (which provide neg feedback)
    • = significant increase in NT in the synapse
  8. Type of serotonin receptor responsible for improved mood.
    5HT1a
  9. Agonism of 5HT2 receptor (a SE of Serotoin) results in?
    increased anxiety, jitteriness, sexual dysfunction, sleep disturbances- (initially)
  10. Agonism of 5HT3 receptor (a SE of Serotoin) results in?
    nausea, diarrhea
  11. SE of NE.
    increased HR, BP, anxiety
  12. Off-target receptor effects of 5HT.
    • H1 = sedation & wt gain
    • M1 anticholinergic receptors
    • alpha 1 noradrenergic antagonism = vasodilation, hypotension, orthostasis
  13. How do MAOIs work?
    Inhibit monoamine oxidase, which is responsible for degradation of Dopa, NE, Epi, and serotonin
  14. TCAs inhibit what?
    reuptake of NE and Serotonin (nonselective)
  15. SSRIs inhibit what?
    reuptake of Serotonin (selective)
  16. Nonselective, irreversible MAOIs.
    • phenelzine (Nardil)
    • isocarboxazid (Marplan)
  17. Nonselective, reversible MAOI.
    tranylcypromine (Parnate)
  18. Selective, reversible MAO-A inhibitors (RIMA).
    • meclobemide
    • befloxatone
    • brofaromine
  19. _______ and _______ are irreversible against MAO-B, antagonizes both (transdermal patch)
    • Selegiline
    • Rasagiline
  20. Inhibition of MAO inhibits degradation of monoamines which increases available _______________
    5HT and NE
  21. AE of MAOIs
    • Tyramine toxicity via inhibition of GI and hepatic MAO, which is responsible for tyramine metabolism;
    • tyramine displaces catecholamines = HTN crisis
  22. PK of MAOI
    • Well-absorbed
    • Lipophilic
  23. MAOI DI
    • TCAs
    • SSRIs
    • pseudoephedrine
    • dextromethorphan
  24. MAOIs are Hepatically metabolized to _______ metabolites which are subsequently hepatically _______ and _______ excreted
    • active
    • inactivated
    • renally
  25. MAO-A inhibits degradation of __________.
    serotonin, NE, & Epi
  26. MAO-B inhibits degradation of _________; at higher doses they can __________.
    • Dopamine
    • inhibit MAO-A
  27. Foods high in tyramine (avoid with MAOIs)
    • processed meats
    • some cheeses
    • red wine
  28. How is tyramine toxicity avoided with MAOIs?
    transdermal patch (avoid GI tract & first-pass)
  29. It could be dangerous to give MAOIs to what type of pt?
    hepatic dysfunction
  30. Doxepin (Sinequan)and Clomipramine (Anafranil) are what class of drugs?
    tertiary amines (TCAs)
  31. Imipramine (Tofranil) is a ______ and is metabolized to ________.
    • tertiary amine (TCA)
    • desipramine
  32. What is the effect when Imipramine and Amitriptyline are metabolized (TCAs)?
    More effect on NE
  33. Which TCAs have less AE and why?
    • secondary amines:  
    • Less or no effect on H1, M1, α1 adrenergic receptors
  34. ______ amines have more effect on NE than 5HTP.
    secondary
  35. _________ amines (TCAs) have more effect on 5HTP than NE.
    tertiary
  36. Amitriptyline (Elavil) is a _________ and is  metabolized to _________.
    • tertiary amine (TCA)
    • nortriptyline
  37. Doxepin (Sinequan)and Clomipramine (Anafranil) have more effect on ________ than _________.
    • 5HTP
    • NE
  38. Nortriptyline (Pamelor) and Desipramine (Norpramine) have more effect on ____ than on _______.
    • NE
    • 5HTP
  39. TCAs are very specific for ______ and ______ and do not have an effect on ________.
    • NE & 5HTP
    • Dopamine
  40. TCA's are used to treat _______ in low doses.
    pain (specifically neuropathic)
  41. AE of TCAs (normally at higher doses).
    • first-degree AV block
    • bundle branch block
  42. TCAs antagonize ________ receptors which causes n/v, anorexia, dry mouth, blurred vision, confusion, constipation, tachycardia, urinary retention.
    muscarinic cholinergic
  43. TCAs antagonize ________ receptors which causes sedation, wt gain, confusion.
    histamine
  44. TCAs antagonize __________ which causes orthostatic hypotension, reflex tachy, drowsiness, dizziness.
    adrenergic receptors
  45. TCAs are substrates of CYP450, especially _______.
    2D6
  46. AEs of SSRIs.
    • **sexual dysfunction (5HT2)
    • serotonin syndrome-hyperthermia
    • muscle rigidity
    • myoclonus
    • rapid fluctuations in mental status and vital signs
  47. Fluoxetine and paroxetine (SSRIs) are substrates and inhibitors of _______.
    CYP2D6
  48. Sertraline (Zoloft) is metab by?
    CYP3A4
  49. Two SSRIs with least DI potential.
    • Citalopram (Celexa)
    • Escitalopram (Lexapro)
  50. What are the two SNRI's?
    • Venlafaxine (Effexor)
    • Duloxetine (Cymbalta)
  51. Venlafaxine (Effexor) is metabolized to active metabolite __________ by ________.
    • desvenlafaxine (Pristiq)
    • 2D6
  52. AE of Effexor (SNRI).
    increased BP
  53. AE of Cymbalta (SNRI).
    • increased transaminases
    • slight chance of increased BP
  54. SNRI effective for depression and neuropathic pain.
    Cymbalta
  55. Cymbalta is Metabolized by _________m
    CYP2D6 and 1A2
  56. Bupropion (Wellbutrin) inhibits ______ and _____ reuptake.
    • dopamine
    • NE
  57. CI to Bupropion.
    seizure disorder, eating disorder
  58. Bupropion (Atypical Antidepressant) is hepatically metabolized by _______.
    CYP2B6
  59. Why does Bupropion have the least sexual SE?
    because it does not affect serotonin
  60. SE of Bupropion.
    Can cause insomnia
  61. Mirtazapine (Remeron) antagonizes ______ and  _______ receptors more at higher doses and ________ receptors more at lower doses.
    • 5HT2/3
    • α2 adrenergic
    • histamine
  62. AE of Mirtazapine (Remeron) due to agonism of histamine.
    • increased appetite
    • sedation
  63. How can you decrease the SE of the atypical antidepressant,  Mirtazapine (Remeron)?
    increase the dose
  64. Mirtazapine (Remeron) is a substrate of _______.
    CYP3A4
  65. Nefazodone (Serzone) inhibits ______ transporter and antagonizes ______, causing less sexual dysfunction and has antianxiety properties.
    • 5HT
    • 5HT2
  66. Nefazodone (Serzone) antagonizes ________ and ________ receptors, causing sedation, & orthostasis.
    • histamine
    • α1 adrenergic
  67. AE of Nefazodone (Serzone).
    • hepatotoxicity
    • fulminant liver failure (2nd or 3rd line drug)
  68. Nefazodone (Serzone) is a substrate and inhibitor of ________.
    CYP3A4
  69. Trazadone is used as an antidepressant only at _________ doses and as a sleep agent at _______ doses.
    • very high
    • low
  70. Which atypical antidepressant has the AE of priapism? What kind of dose causes this?
    • Trazadone
    • higher doses
  71. Trazadone is metabolized by ________.
    CYP3A4
  72. Atypical antidepressant used for anxiety only.
    Buspirone (Buspar)
  73. Buspirone (Buspar) agonizes _______ receptor.
    5HT1A
  74. Two drugs used to tx narcolepsy.
    • modafinil (Prodigal)
    • armodafinil (Nuvigil)
  75. TI of LIthium.
    0.7 - 1.2
  76. What can increase lithium levels? Why?
    • diuretics
    • probenecid
    • renal insufficiency 
    • (it is secreted and reabsorbed in renal tubules)
  77. What is LIthium used to control?
    mania & depression
  78. Two drugs other than Lithium used to tx Bipolar.
    • Carbamazepine
    • Valproic Acid
  79. AE of Lithium (generally w/ higher doses).
    • nausea, thirst, polyuria,
    • hypothyroidism, tremor,
    • weakness, mental confusion,
    • teratogenesis (do not give to pg women)
  80. Half-life of Lithium.
    12-27 hours
  81. Diuretics can confuse Lithium for _____ and result in ________.
    • Na+
    • Lithium toxicity
  82. How will Probenecid effect Lithium?
    • prevent secretion of Lithium into renal tubules &
    • increase serum levels of Lithium
  83. Triptans act as _______ agonists in vasculature, causing __________ of intracranial blood vessels.
    • 5HT 1B/1D
    • Potent vasoconstriction
  84. What class of drugs is specific for migraine therapy?
    Triptans
  85. Which triptan has the fastest onset of action? The longest?
    • fastest = rizatriptan (Maxalt)
    • longest = naratriptan (Amerge)
  86. __________ can significantly inhibit metabolism of rizatriptan (Maxalt).
    propanolol
  87. Two triptans that can be administered as a nasal spray (important when pt has n/v).
    • Sumatriptan (Imitrex)
    • Zolmitriptan (Zomig)
  88. CI of Triptans.
    • ischemic heart disease
    • uncontrolled HTN
    • ischemic stroke,
    • pregnancy
  89. Most triptans are metabolized by _____, except for which ones? Why is this important?
    • MAO
    • eletriptan, frovatriptan, naratriptan
    • DIs with MAOIs
  90. Eletriptan is metabolized by ______ – do not administer within 72 hours of potent _______ inhibitors.
    • CYP3A4
    • CYP3A4
  91. There is a risk of ____________ when triptans are used in combination with SSRIs and SNRIs.
    serotonin syndrome
  92. _________ are 5HT1B/1D agonists.
    Ergots and Triptans
  93. Avoid Ergotamines in patients with _____________.
    • CAD, PVD, HTN,
    • hepatic or renal disease
  94. Ergotamine may be useful in patients with _________.
    prolonged duration of migraine attacks (>48 hrs)
  95. CI of DHE 45.
    • HTN 
    • ischemic heart disease 
    • *in combination with MAOIs 
    • elderly
  96. Benzamides butyrophenones, & phenothiazines are anti-emetics that antagonize __________.
    dopamine
  97. Class of antiemetic drugs with least SE. Why?
    • 5HT3 antagonists
    • only work on serotonin
  98. 5HT3 antagonists used as antiemetics.
    • Zofran
    • Anzemet
    • Kytril

Card Set Information

Author:
MeganM
ID:
316051
Filename:
Pharm Mod 3 CNS
Updated:
2016-02-21 22:21:03
Tags:
GU Pharm
Folders:
GU,Pharm
Description:
Exam 2
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