Pharm Mod 3 CNS part 2

  1. Phenytoin (Dilantin), Fosphenytoin (Cerebyx) are _______ channel inhibitors. Which one is a prodrug and which one is active?
    • Na+
    • Fosphenytoin is a prodrug and is converted to
    • Phenytoin, the active drug
  2. Phenytoin (Dilantin) &  Fosphenytoin (Cerebyx), Na+ channel inhibitors, are hepatically metabolized by and inducers of ____________________.
    CYP3A4, 2C9, 2C19
  3. Phenytoin uses ________ kinetics, where ________ amount of drug eliminated per unit of time and the rate of drug elimination is  _______ drug concentration.
    • zero-order
    • constant
    • independent of
  4. What does a small increase in the dose of Phenytoin mean?
    a large increase in plasma concentration
  5. TI of Phenytoin including free and protein-bound.
    10-20  mcg/m
  6. TI of free Phenytoin.
    1-2 mcg/m
  7. Make sure to watch total levels and _______ and also  _______ with Phenytoin.
    • albumin
    • CrCl
  8. Boxed warning (IV only) of Phenytoin.
    severe hypotension and cardiac arrhythmias (infusion rate dependent); do not administer rapidly
  9. The anticonvulsant drug, ____________  can be administered faster.
    Fosphenytoin (prodrug)
  10. SE of Phenytoin.
    • SJS
    • Hirsutism, gingival hyperplasia, acne
    • Alteration of vitamin D metabolism (osteoporosis)
    • hematological abnormalities
  11. Carbamazapine is an autoinducer & potent inducer of  ________.
    • CYP3A4
    • 1A2 
    • 2C9/19
  12. Carbamazepine (Tegretol) exhibits _________ kinetics; Phenytoin exhibits ______ kinetics.
    • first-order
    • zero-order
  13. Boxed warnings for Carbamazepine (Tegretol).
    • Serious dermatological reactions (SJS/TEN)
    • Aplastic anemia
    •  agranulocytosis
  14. Carbamazepine (Tegretol) is associated with what AE?
    • Cholestatic jaundice
    • hyponatremia
  15. TI for Carbamazepine (Tegretol).
    6–12 mcg/mL
  16. _________ has a similar MOA as Phenytoin, but is less protein bound and has less DIs.
    Lamotrigine (Lamictal)
  17. Why is it important to slowly titrate Lamotrigine (Lamictal).
    Too fast can  = rash (SJS)
  18. NA+ channel inhibitor assoc with blood dyscrasias such as neutropenia & thrombocytopenia.
    Lamotrigine (Lamictal)
  19. First order kinetics mean a constant ________ of the drug is elminated per unit of time and that the rate of drug elimination is __________  drug concentration.
    • fraction
    • proportional to
  20. First order kinetics mean a constant ________ of the drug is elminated per unit of time and that the rate of drug elimination is __________  drug concentration.
    • fraction
    • proportional to
  21. Lacosamide (Vimpat) should be used with caution with what type of pt?
    with cardiac arrhythmias
  22. How is Gabapentin eliminated?
    100% RENALLY
  23. Common AE of Gabapentin.
    • CNS depression, dizziness
    • peripheral edema
  24. _________  and ________ are anticonvulsants but not very effective for seizures.
    • Gabapentin
    • Pregabalin (Lyrica)
  25. _________ is more potent than Gabapentin.
    Pregabalin (Lyrica)
  26. AE of Pregabalin (Lyrica)
    Angioedema, peripheral edema
  27. The only K+ channel inhibior available.
    Ezogabine (Potiga)
  28. Boxed warning for Ezogabine (Potiga).
    • retinal abnormalities
    • potential vision loss
  29. Which anticonvulsant can cause urinary retention, neuropsychiatric events, &  QT prolongation?
    Ezogabine (Potiga)
  30. Common AE of all anticonvulsants.
    CNS depression
  31. How is Ezogabine (Potiga) metabolized?
    glucorinidation & acetylation
  32. Boxed warning: permanent vision loss (anticonvulsant).
    Vigabatrin (Sabril)
  33. Stimulation of D1 receptors is ________; stimulation of D2 receptors is _________.
    • excitatory
    • inhibitory
  34. Dopamine stimulates the ________ pathway, enabling moment; and will inhibit the ________ pathway.
    • direct
    • D2
  35. Levadopa is converted to dopamine in the CNS, but also in the __________ which can cause _________.
    • GI tract
    • nausea
  36. Why is carbidopa administered with Levodopa?
    • Carbidopa inhibits conversion of Levadopa to dopamine in the periphery (otherwise, w/o carbidopa only 1-3% reaches CNS).
    • Carbidopa does not cross BBB, so now more levadopa can cross and be converted to dopamine
  37. Sinemet most effective for Parkinsons, but what is the downfall?
    • Pt's build a tolerance, so higher doses are needed
    • "on" and "off" moments
    • can lead to dyskinesias
  38. AE of Dopamine receptor agonists
    • sedation
    • vivid dreams, hallucinations
  39. Selegiline (Eldepryl) and rasagiline (Azilect) are __________ inhibitors.
  40. Tolcapone (Tasmar) and entacapone (Comtan)  are __________ inhibitors. Which one works peripherally only?
    • COMPT (an enzyme that breaks down dopamine)
    • entacapone
  41. Trihexyphenidyl (Artane) and  benztropine (Cogentin) can reduce _________ by antagonizing the _________ receptors.
    • tremor
    • muscarinic
  42. Most atypical antipsychotics are more effective at treating negative symptoms, but _________ is more effective than haloperidol at treating positive symptoms.
  43. Lower potency typical antipsychotics have more _______ effects than D2-related effects.
  44. ___________ of dopamine improves negative symptoms.
  45. _________ of dopamine improves positive symptoms.
  46. Side effects from blocking D2 (higher potency especially): will increase _______ symptoms and will cause ________.
    • negative
    • EPS
  47. 40% D2 saturation will cause ______.
  48. 60% D2 saturation will improve _______.
    positive symptoms
  49. 80% D2 saturation will cause _______.
  50. Acute EPS.
    • dystonia (muscle stiffness)
    • akathisia (restlessness)
  51. Chronic EPS.
    • pseudoparkinsonism
    • tardive dyskinesia
  52. What can be used to tx akathisia (restlessness)?
    BB (propanolol)
  53. What can be used to tx pseudoparkinsonism (rigidity, bradykinesia, tremor)?
    anticholinergics; amantadine (releases dopamine)
  54. What can be used to tx dystonia (muscle stiffness)?
    • anticholinergics restore balance
    • benzos relax muscles
  55. S/S of NMS.
    • fever (hyperthermia)
    • muscle rigidity (tx w/ dantrolene, bromocriptine)
    • increased CPK, myoglobin (renal failure - hydration)
    • delirium
  56. Clozapine and Olanazapine are metabolized by _______, so smoking increases metabolism.
  57. MANY CNS drugs are metabolized by _______.
Card Set
Pharm Mod 3 CNS part 2
Exam 2