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Neuro II Drugs > Seizure & Epilepsy Drugs > Flashcards

Seizure & Epilepsy Drugs Flashcards

1
Q

Generalized onset - Absence

A

Ethosoximide

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2
Q

Generalized onset - Myoclonic/atonic/clonic

A
  1. Benzodiazepines

2. Clonazepam

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3
Q

Generalized onset - Tonic-clonic

Narrow spectrum

A
  1. Phenytoin
  2. Phenobarbital
  3. Carbamezepine (partial onset)
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4
Q

Partial onset - simple/complex

Narrow spectrum

A
  1. Carbamazepine
  2. Gabapentin
  3. Pregabalin
  4. Oxcarbazepine
  5. Locosamide (new)
  6. Tiagabine
  7. Vigabatrin
  8. Ezogabaine
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5
Q

Broad spectrum

A
  1. Valproate
  2. Lamotrigine
  3. Topirimate
  4. Levetiracetam
  5. Zonisamide
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6
Q

Block Na channels

A 
Generalized onset: Tonic-clonic
1. Phenytoin
Partial Onset: Simple/complex
1. Carbamezepine
2. Oxcarbazepine
3. Locosamide
Broad spectrum 
1. Lamotrigine
2. Zonisamide 
3. Valproic acid
4. Topirimate
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7
Q

Block T-type Ca channels

A

Ethosoximide
Also: valproate and zonasimade
- these channel mediate 3Hz spike and wave activity in thalamus

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8
Q

Phenytoin

A
  • state dependent
  • slow recovery from inactivation
  • MOST effective at depolarized membrane potential + high frequency AP firing
  • minimum effect on cognition (low frequency firing)
    Adverse effects - 0 order, doubling dose does not double serum level, hepatic CYP450 enz, gingival hyperplasia, hirsutism, hypocalcemia, osteoporosis
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9
Q

Carbamazepine

A
  • state dependent
  • slow recovery from inactivation
  • binds Na with less efficiency but at MUCH FASTER RATE –> high efficiency in blocking high frequency firing (more than phenytoin)
    Adverse effects - hepatic CYP450 enz, induces own metab, loss of efficacy by day 14, aplastic anemia, leukopenia, neutropenia thrombocytopenia, hypocalcemia, osteoporosis, allergic rxn (Stevens-Johnson syndrome)
    If given with oral contraceptives - inc clearance by CYP (pregnancy!)
    If given with warfarin - inc clearance by CYP (inc risk of thrombosis)
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10
Q

Lamotrigine

A
  • voltage and use dependent
  • similar to phenytoin and carbamazepine
  • IN ADDITION acts on N and P-type VG Ca channels (careful: not T)
  • can cause S-J syndrome –> rash 12 weeks after, allergic rxn, life threatening (Risk factor - valproate)
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11
Q

Locosamide

A
  • enhances slow-inactivated state (vs others will prolong fast inactivated state)
  • lowers amplitude and frequency of firing spikes during prolonged stimulation
  • longer time scale than other drugs
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12
Q

Ethosoximide

A
  • ONLY for absence seizure
  • ONLY limits excitation (Ca channel)
  • NON-SEDATING drug
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13
Q

Zonisamide

A

Sulfonamide derivative

Adverse effect - rash, renal calculi, hypohidrosis

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14
Q

Which drug blocks VG Na channels and T-type VG Ca?

A

Zonisamide (also Valproic acid)

Note: Lamotrigine blocks VG Ca too but P and N type Ca channels not T-type!!!!!!!!!!!!! Nerd

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15
Q

Valproate

A
  • 1st line drug for generalized-onset seizure
  • intolerable side effects
  • NTD during pregnancy; atrial septal defect, cleft palate, polydactyl
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16
Q

Which drugs block GABA reuptake/metabolism?

A
  1. Tiagabine - reuptake (assoc with stupor)

2. Vigabatrin - metabolism

17
Q

Which drugs potentiate GABAa Rc Cl currents?

A
  1. Phenobarbital
  2. Primidone
  3. Benzodiazepines
18
Q

Phenobarbital

A
  • binds to distinct site
  • nonspecific CNS depressant, sedation, LETHAL resp depression
  • abuse/addiction potential
  • GABA INDEPENDENT
  • active metabolite of Primidone
19
Q

Benzodiazepines

A
  • bind to allosteric site
  • potential GABA binding –> Cl opened with greater frequency
  • GABA DEPENDENT
  • treatment of status epilepticus
20
Q

Stopping seizure treatment

A

Initial IV - Lorazepam/diazepam (5 mins, inc GABA)

If seizure not stopped - Fosphenytoin IV (Na channel block)

21
Q

Valproic acid acts on:

A

VG Na
T-type Ca
Inc GABA

22
Q

Topirimate acts on:

A 
VG Na
LG Na (AMPA/glut Rc)
Inc GABA
Potentiates GABAa Rc
Adverse effect - nephrolithiasis, open angle glaucoma, hypohidrosis
23
Q

Gabapentin

A
  • binds VG Ca

- no drug interactions

24
Q

Levetiracetam

A
  • binds synaptic vesicle protein (SV2A)
  • stop glutamate release
  • no CYP interactions
25
Q

Pregabalin

A
  • 100% renal clearance

- multiple mechanisms

26
Q

Ezogabaine

A
  • binds VG K channels

- urinary retention

27
Q

Which drugs induce CYP450 dependent Vit D catabolism?

A 
Phenytoin
Carbamazepine
Phenobarbital
Valproic acid
(Dec absorption of Ca triggers PTH response - demineralized bone)
28
Q

Renal clearance (100%)

A
  1. Gabapentin (VG Ca)

2. Pregabalin

29
Q

Minimizing drug interactions - renal clearance >50% of total

A

Topiramate/Oxcarbazepine

Levetiracetam/Zonisamide

30
Q

Oxcarbazepine

A
  • analog of carbamazepine; fewer side effects
  • lack of formation of active metabolite
  • metab in liver but min effects by CYP450
    Adverse effects: associated with hyponatremia (along with Carbamezepine), rash
31
Q

Drugs inhibiting conjugation of drugs by UGT enzymes

A
  1. Valproate

2. Lamotrigine

32
Q

Class D teratogens

A
  1. Valproic acid
  2. Carbamezepine
  3. Phenytoin
33
Q

Topirimate

A
  1. GABAa Rc agonist

2. Glutamate (AMPA) Rc antagonist

34
Q

Which drugs cause osteoporosis/osteopenia?

A
  1. Phenytoin
  2. Carbamazepine
  3. Phenobarbital
  4. Valproic acid

Neuro II Drugs (7 decks)

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