Med Chem: Anti-epileptics

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  1. Phenytoin (Dilantin) MOA
    • Blocks high-frequency firing of neurons through inhibitory actions on VG-Na+ channels
    • → Slows channel recovery from inactivated state
    • → Use-dependent effect
  2. Phenytoin (Dilantin) ADR
    • Must have a slow administration or else it will precipitate out & will go back to original state (unionized)
    • IV- risk of cardiac arrhythmia
    • SJS
    • Hirsutism
    • Gingival hyperplasia
    • Hepatotoxicity
    • Nystagmus
    • Ataxia
    • Dizziness
    • Confusion
    • Behavioral changes
    • Anemia
    • Bone marrow suppression
    • “Fetal hydantoin syndrome”- teratogenic
  3. Phenytoin (Dilantin) Indications
    Partial and tonic-clonic seizures
  4. Fosphenytoin (Cerebyx) MOA
    • Prodrug of phenytoin: increased aqueous solubility
    • → Plasma esterases
  5. Fosphenytoin (Cerebyx) ADR
    • Similar to phenytoin
    • → Cardiac effects if given too quickly
  6. Carbamazepine (Tegretol) Indications
    • Simple and complex partial seizures
    • Generalized tonic-clonic seizures
  7. Carbamazepine (Tegretol) metabolism
    Autoinduction: CYP2C, CYP3A4, UGT enzymes
  8. Carbamazepine (Tegretol) MOA
    • Similar to phenytoin
    • → Na+ channel blocker
  9. Oxycarbamzepine MOA
    • Prodrug of carbamazepine
    • Similar to carbamazepine (phenytoin-like)
  10. Ethosuximide (Zarontin) MOA
    • Succinimide
    • Reduce T-type Ca2+ currents in thalamic neurons
  11. Ethosuximide (Zarontin) Indications
    DOC for absence seizures
  12. Ethosuximide (Zarontin) ADR
    Few ADRs
  13. Phenobarbital Indications
    • Generalized tonic-clonic seizures
    • Partial seizures
  14. Phenobarbital MOA
    Binds to GABA receptor- activating it
  15. Phenobarbital ADR
    • Potent P-450 inducer
    • Increased metabolism of estrogen, steroids, warfarin, carbamazepine, diazepam
  16. Benzodiazepines MOA
    • Enhance effect of GABA on the GABA-A Cl- channel
    • → GABA agonist
  17. Diazepam Indiactions
    Staus Epilepticus
  18. Clorazepate (Tranxene) Indications
    Adjunct in partial seizures
  19. Clorazepate (Tranxene) MOA
    • Prodrug of diazepam
    • → Decarboxylated by acidity of stomach to dismethyldiazepam
    • Same as diazepam
    • Carboxylate group: a beta-keto acid
  20. Gabapentin (Neurontin) MOA
    MOA unclear
  21. Gabapentin (Neurontin) Indications
    • Partial seizures
    • Migraines
    • Chronic pain
    • Bipolar disorder
  22. Vigabatrin (Sabril) MOA
    • Vinyl GABA Transaminase Inhibitor
    • → Irreversible (suicide) inhibitor of GABA aminotransferase
  23. Vigabatrin (Sabril) Indications
    Complex partial seizures
  24. Vigabatrin (Sabril) ADR
    Retinal damage
  25. Pregabalin (Lyrica) MOA
    • Binds Ca2+ channels
    • Inhibits Ca2+ dependent release of glutamate
  26. Tiagabine (Gabitril) MOA
    GABA reuptake transporter (GAT-1) antagonist
  27. Tiagabine (Gabitril) Indications
    • Partial seizures
    • → w/ or w/out secondarily generalization in adults
  28. Lamotrigine (Lamictal) Indications
    • Partial seizures
    • Secondary generalized seizures
  29. Lamotrigine (Lamictal) MOA
    • Delays recovery from inactivation of recombnant Na+ channels
    • → Reduces presynaptic release of excitatory glutamate
  30. S(-) Levetiracetam (Keppra) Indications
    • Partial seizures
    • Secondary generalized seizures
  31. S(-) Levetiracetam (Keppra) MOA
    • Unknown
    • Probably the synaptic vesicle protein SV2A (inhibits glutamate release)
  32. Valproic Acid (Depakene) MOA
    • Unknown
    • Multiple sites of action
    • → acts on Na+ channels like phenytoin
    • → increases GABA in the brain
    • → blocks NMDA receptors
  33. Valproic Acid (Depakene) Indications
    • Broad spectrum
    • → Absence seizures
    • → Myoclonic seizures
    • → Partial seizures
    • → Tonic-clonic seizures
  34. Zonisamide (Zonegran) MOA
    • Sulfonamide
    • Blocks Na+ channels
    • Blocks Ca2+ channels
    • Inhibition of carbonic anhydrase
  35. Topiramate (Topamax) MOA
    • Sulamate, note acetonide
    • Unclear, may be multi-factorial
    • → Blocks Na channels
    • → Augments GABA at GABA-A receptor
    • → Antagonist at glutamate receptors
    • → Inhibits carbonic anhydrase
  36. Topiramate (Topamax) Indications
    • Partial seizures
    • Primary generalized tonic-clonic
    • Lennox-Gastaut Syndrome >2 yrs
  37. Acetazolamide (Diamox) MOA
    • Tiadiazole & sulfonamide
    • Inhibits carbonic anhydrase in the brain
    • → Retards abnormal firing of neurons
  38. Acetazolamide (Diamox) Indications
    Absence seizures
  39. Lacosamide (Vimpat) MOA
    • Enhances slow inactivation of voltage-gated sodium channels
    • → Stabilization of hyperexcitable neuronal membranes
    • → Inhibition of repetitive firing
  40. Lacosamide (Vimpat) Indications
    Adjunctive therapy for partial-onset seizures >17 yrs

Card Set Information

Author:
ebmalonzo
ID:
315943
Filename:
Med Chem: Anti-epileptics
Updated:
2016-02-15 15:43:01
Tags:
MedChem Anti epileptics
Folders:
IT 2
Description:
IT 2 (MT 3): Med Chem (Anti-epileptics)
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