Pharm II (AED)

  1. What are different kinds of partial seizures?
    1. Simple partial seizures (consciousness not impaired)

    2.Complex partial seizures (with impairment of consciousness: may sometimes begin with simple symptomatology)

    3.Partial seizures evolving to secondarily generalized seizures (this may be generalized tonic-clonic, tonic, or clonic)
  2. What seizures can Valproic acid treat?
    -All Partial and Generalized types

    • -All Partials
    • -All partials
  3. What drugs are good for the treatment of Partial seizures?
    • NEWER
    • Gabapentin
    • Lamotrigine
    • Levetiracetam
    • Tiagabine
    • Zonisamide
    • Lacosamide
    • Pregabalin

    • Carbamazepine
    • Phenytoin
    • Valproic acid
  4. What is Lennox Gastaut syndrome?
    What is the best treatment?
    (LGS) is a difficult-to-treat form of childhood-onset epilepsy that most often appears between the second and sixth year of life, and is characterized by frequent seizures and different seizure types; itis often accompanied by mental retardation and psychological and behavioral problems.

    • -lamotrigine
    • -felbamate
    • -topiramate
    • -rufinamide
  5. What are Seizures induced by?

    What are seizures inhibited by?
    • Seizures induced by
    • –GABAA antagonists
    • –Glutamate receptor agonists
    • NMDA
    • AMPA (amino methyl propionic acid)
    • kainic acid

    • Seizures are inhibited by
    • -GABA agonists
    • -Glutamate receptor antagonists
  6. Name two Barbiturates and what they are used for.

    What are some of their adverse effects?
    When is it contraindicated?
    What is their Mech of action?
    • 1.Phenobarbital
    • 2.Primidone

    • Used to treat
    • –Partial seizures
    • –Generalized tonic-clonic seizures

    Folate deficiency, Irritability, Agitation, Confusion, Sedation

    May indice fatal attacks of porphyria in patients with acute intermittent porphyria

    -inhibition via GABA-A receptor
  7. Name the Hydantoins

    When are they used?
    Which have good solubility?
    What are some side effects?
    • Phenytoin
    • Fosphenytoin

    Used to treat all types of partial seizures and tonic-clonic seizures, but NOT absence seizures

    • -phenytoin – poor aqueous solubility
    • -fosphenytoin –good solubility
    • _________________
    • -Folate deficiency
    • -Vitamin D deficiency
    • -Teratogenic effects
    • -Drug interactions
  8. Name the Iminostilbenes

    What are they used for?
    What us the mechanism of action?
    • Carbamazepine
    • Oxcarbazepine

    • -Used to treat most types of seizures, except myoclonic and absence
    • -Also used for Trigeminal Neuralgia and Bipolar disorder

    -Na+ channels, by prolonging recovery from inactivation
  9. How is Carbamazepine metabolized?

    • Induces its own metabolism by Cyp3A4, thus requires adjustment after about 2-3 weeks
    • _________________________
    • -Less potent
    • -Can result in elevated levels of other Anti epileptic drugs like:phenytoin, valproic acid, lamotrigine
  10. Name the Succinimides

    What are they used for?
    • Ethosuximide
    • Phensuximide

    Treat Absence Seizures
  11. What is Ethosuximide Mech of action?

    What are some Adverse effects?
    -Inhibition of low threshold Ca2+ currents (T currents) in thalamic neurons which play a role in 3-Hz spike-wave rhythms typical of absence seizures.

  12. Valproic acid
    What is it used for?
    What is its Mech of action?
    What are some Adverse effects?
    used to treat all seizure types (also migrains, and bipolar disorders)

    Prolongs recovery (from inactivation) of voltage-activated Na+ channels [similar to carbamazepine]

    • -Reduces low-threshold Ca2+ currents
    • (T currents) in nodose ganglion [Similar to ethosuximide effects in thalamic neurons]

    • -Transient hair loss
    • -Weight gain
    • -Elevated hepatic enzymes
  13. What is Gabapentin used for?
    What is its Mech of action?
    Used in partial seizures with or without secondary generalizations

    -Not a GABA agonist (despite structure)

    • -Increase the release of GABA-->Inhibition of
    • L-type Ca2+ channels
  14. What is Lamotrigine used for?

    What is its mech of action?
    • –All seizure types
    • –Lennox-Gastaut syndrome
    • –Bipolar Disorder

    • –Use dependent Na+ channel inhibitor
    • –Reduces glutamate release
  15. What happens if you combine Valproate and Lamotrigine?

    What happens if you add Phenobarbital and carbamazepine to LTG?
    -Increase Lamotrigine concentrations by 2X

    -Decreases its concentrations by 40%
  16. What is Felbamate useful for?

    Why is it not 1st line?
    Useful for the treatment of:

    • –Partial seizures, with and without generalization
    • –Lennox-Gastaut syndrome

    -Not first line therapy due to significant increased risk of aplastic anemia and hepatic failure
  17. Levetiracetam

    What is it used for?
    • -partial seizures, with and without generalization
    • -myoclonic seizures in Juvenile Myoclonic Epileps
    • -Tonic-Clonic seizures in Idiopathic Generalized Epilepsy
  18. What is Tiagabine used for?

    What is its Mech of action?
    -Partial seizures, with and without generalization

    -Inhibits GABA transporter (GAT-1), thus increasing duration of action of GABA.
  19. What is Topiramate used for?

    What is its Mech of action?
    • -Adjunctive therapy for refractory partial or generalized seizures
    • -Lennox-Gastaut syndrome

    • –Blockade of use dependent Na+ channels
    • –Inhibition of L-type Ca2+ channels
    • –Enhancement of GABA activity
    • –Glutamate antagonism
  20. What is Zonisamide?

    What is its Mech of action?
    Adjunctive therapy for partial seizures

    • Inhibits low threshold Ca2+ currents (T currents)
    • –Probably also via Na+ channels, by prolonging recovery from inactivation (like carbamazepine and phenytoin)
  21. What is Vigabatrin used for?

    What is its Mech of action?

    What is an important side effect?
    • -Approved as monotherapy for infantile spasms
    • -adjunctive therapy for refractory epilepsy
    • -Used for partial seizures with or without secondary generalization
    • __________________________
    • -Irreversible inhibitor of GABA transaminase (GABA-T), thus increasing GABA levels

    Severe Peripheral Visual Field defects
  22. What is Lacosamide used for?
    -Adjunctive treatment in partial onset seizures

    • MOA:
    • –Enhances slow inactivation of voltage-gated Na+ channels
    • -Stabilization of hyperexcitable neuronal membranes
    • -Inhibition of repetitive neuronal firing
  23. What is Pregabalin used for?

    What is its MOA?
    -Partial seizures (also: Neuropathic pain due to Diabetes, Fibromyalgia, Post herpetic meuralgia)

    -Binds voltage gated Ca++ channels
  24. What is Rufinamide?
    • –Lennox-Gastaut syndrome
    • –Na+ channel modulation
Card Set
Pharm II (AED)
Pharm II (AED)