Pharmacology #2 (anticonvulsants and parkinsons)

  1. What are the 4 prototype drugs for tx of EPILEPSY?
    • carbamazepine
    • ethosuximide
    • valproic acid
    • lorazepam
  2. What are the 4 prototype drugs for tx of PARKINSONISM?
    • L-DOPA
    • Sinemet and Sinement-CR
    • bromocryptine
    • selegiline
  3. Sinemet is for tx of ________ and is combo of the drugs _________ and _________
    • Parkinsons
    • L-DOPA and carbidopa
  4. Epilepsy is a CHRONIC Neuro disorder, characterized by periodic, unpredictable _____________
  5. Seizures are cause by:
    disordered firing of lrg # of CNS neurons
  6. Pharm Tx of Epilepsy is:
  7. Is toxicity common in anticonvulsants?
  8. anticonvulsants have ______ TI.
  9. anticonvulsants are cleared mainly by
    hepatic metabolism
  10. The main type of hepatic metabolism of anticonvulsants is by _______________
  11. The main actions of anticonvulsants is to reduce what?
    excessive cortical excitability
  12. The 3 mechanisms of actions of anticonvulsants include:
    • 1) Blocking Na channels, enhancing spike inactivity
    • 2) Block Ca channels
    • 3) potentiate GABA
  13. Carbamazepine pharmacokinetics:
    • slow absorption and slow clearance.
    • induces liver P450, and during chronic use can reduce half life to 8-12 hrs.
  14. What drug is used as first line tx of partial complex seizures?
  15. Toxic sx of Carbamazepine:
    Diplopia and ataxia, GI upset, bleeding disorders
  16. What 2 drugs are in the anticonvulsants class that blocks Na channels?
    • Carbamazepine
    • phenytoin
  17. What anticolvulsant drug is in the that blocks Ca channels?
  18. What drug is the first choice for generalized absent seizures?
  19. Ethosuximide mechanism
    blocks t-type Ca channels in thalmic and cortical neurons
  20. Ethosuximide pharmacokinetics:
    NO plasma protein binding, so CSF and blood levels equal.  Long half life (40). linear relation btw dose and plasma levels.
  21. Ethosuximide toxicity
    Gastic pain and nausea can occur.  Avoided by: start level low and raise slowly
  22. What drugs are included in the GABA potentiation group of anticonvulsants?
    • Valproic Acid
    • benzo's
  23. What drug works well for absence seizures?
    Valproic Acid
  24. Why would Valproic Acid be preferred over ethosuximide?
    If absence seizures include generalized clonic-tonic seizures.
  25. Pharmacodynamics of Valproic Acid:
    90% bound to plasma protein.  rapid absorption, half life 9-8.
  26. Valproic Acid Toxicity:
    • gastric pain and nausea.  avoided by starting with low levels.
    • Hepatoxic in infants
  27. Benzodiazepines are absorbed _______ and have a _____ T1/2.
    rapidly, LONG
  28. can tolerance develop with benzos?
  29. Tx of status epilepticus
    • 1- asses airway, vitals, blood glucose assay
    • 2- lorazepam 0.1mg/kg (10-15min)
    • 3- fosphenytoin
    • 4- phenobarbitol
    • 5- midaz or propofol to induce gen anesthesia
  30. Topiramate is a recently introduced anticonvulsant acting with which 2 mechanisms?
    • Na channel blocker
    • GABA potentiating
  31. In what ways can anticonvulsants be teratogenic?
    • reduce folic acid
    • form active metabolites
  32. What causes Parkinsons disease?
    degeneration of dopaminergic neurons in the substantia negra
  33. What are the 3 strategies to tx of parkinsons?
    • 1- replace lost dopamine
    • 2- activate dopamine receptors in striatum
    • 3- neuroprotect w/ free radical scavenger, block dopamine metabolism
  34. L-dopa used in which strategy?
  35. does L-dopa cross the blood-brain barrier?
  36. in the brain, L-dopa in converted to ___________
  37. What does carbidopa do?
    allows more L-dopa to reach the brain
  38. bromocryptine is used for which parkinsons strategy?
  39. bromocryptine causes _____ dyskinesias than L-dopa
  40. bromocryptine has high CNS side-effects because...
    all D2 dopamine recpetors are activated
  41. What drug is used in parkinsons strategy 3?
  42. Selegiline is a _____ __________ ___ blocker
    monoamine oxidase B
  43. Selegiline improves motor function when used, but....
    worsens motor function when discontinued
  44. Selegiline somtimes used to delay motor complications of what drug?
  45. Huntington's is a autosomal ______ dz.
  46. What genetic defect is caused by Huntington's?
    expansion of a CAG repeat, encoding a polyglutamine stretch in the target protein.
  47. What is the frequency of Huntington's?
    5 on 100,000
  48. Huntington's causes what to occur in the body?
    Degeneration of GABAergic and colinergic neurons of striatum.
  49. Huntington's Tx?
    None proven.  Only tx of depression, anxiety and psychosis that are often seen in these pt's.
Card Set
Pharmacology #2 (anticonvulsants and parkinsons)
Drugs and info for pharm exam 2- anticonvuslants and parkinsons