Anticonvulsants Flashcards

1
Q

4 ways to treat seizures

A
  1. Blockade of excitatory input
  2. Strengthening of inhibitory input (GABA)
  3. Block Na channels
  4. Block thalamic Ca channels
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

Block hyper-excitability by:

A

Elevate threshold for stimuli

Limit propagations discharged

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

Blockage of Na channel activation does what

A

Reduces the ability of Na channels to recover from inactivation to inhibit constant firing and increases threshold potential

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

Blocking of Ca channel does waht

A

ABSENCE SEIZURES

Reduces firing of thalamic neurons which are involved in cortical discharge and NT release (**)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

Activation of GABA(A) leads to

A

Increase inflow of Cl and inhibit post-synaptic cells

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

GABA transmission can be enhanced by

A

block of GAT1 transporter and increase concentration in cleft

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

Antagonists of NMDA and AMPA glutamate receptors do what

A

Anticonvulsant activity bc glutamate is an excitatory NT

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

PD Properties of Classical AEDs

A

Narrow therapeutics
CNS depression (valproic is the least sedatative)
Hypersensitivity and hematotoxicity rxns
Teratogenicity and can cause unplanned pregnancy
Long half life
Multiple times a day dosing
Increased risk of osteoporosis bc interfere with Vit D metabolism

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

Induction of P450

A

Phenobarbital
Phenytoin
Carbamazepine

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

Inhibition of P450

A

Valproic acid

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

Phenytoin

A

Dilantin

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

Phenytoin MOA

A

Slows the rate of recovery of Na channels from inactivation

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

Phenytoin treats

A

Partial and tonic-clonic seizures

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

Water soluble form of phenytoin

A

Fosphenytoin

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

Phenytoin Elimination

A

Halflife increases with dose increase but concentration disproportinately increases with dose increases

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

Phenytoin down sides

A

Metabolized by CYP so many drug interactions

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
17
Q

Phenytoin AE

A

CNS depression
Gingival hyperplasia
Inhibits release of ADH and insulin so hyperglycemia and glycosuria

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
18
Q

Carbamazepine

A

Tegretol

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
19
Q

Carbamazepine MOA

A

Slows the rate of recovery of Na channels from inactivation

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
20
Q

Carbamazepine treates

A

Partial and tonic clonic

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
21
Q

Down sides to carbamazepine

A

Induces its own metbaolism
Decreased halflife after chronic therapy
Active metabolites
Induces 2C, 3A, UGT

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
22
Q

Carbamazepine AE

A

Acute toxication (stuper, coma)
Long term: drowsiness, vertigo, ataxia
SJS and necrolysis

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
23
Q

Ethosuximide

A

Zarontin

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
24
Q

Ethosuximide MOA

A

Blocks T type Ca channels in thalamus

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
25
Q

Ethosuximide treats

A

absence seizures

26
Q

Ethosuximide Metabolism

A

Liver

Few drug drug interactions

27
Q

Ethosuximide AE

A

GI and CNS

28
Q

Valproic acid

A

Depakene

29
Q

Valproic acid MOA

A

Na blocker
Ca blocker
Enhances GABA

30
Q

Valproic acid treats

A

Partial
Generalized epilepsies
Absence and myoclonic seizures

31
Q

Valproic inhibits and metabolized where?

A

2C9 and UGT

Liver

32
Q

Valproic acid SE

A

GI
Weight gain
Hair loss in children
Minimal sedation

33
Q

Oxcarbazepine

A

Trileptal

34
Q

Oxcarbazepine MOA

A

Blocks Na channel

Similar to carbamazpine

35
Q

Oxcarbazepine PK

A

Pro-drug

Induces 3A4/5 and inhibits 2C19

36
Q

Oxcarbazepine Treats

A

Partial in >4 yo and can be mono or adjunct

37
Q

Oxcarbazepine AE

A

Dizziness
Headache
D/V/N
Ataxia

38
Q

Gabapentin

A

Neurontin

39
Q

Gabapentin MOA

A

Promotes release of GABA

40
Q

Gabapentin treats

A

Partial seizures 2nd line as adjunct

- Neuropathic pain, migraines and spasticity

41
Q

Upsides to gabapentin

A

No known interactions with other AEDS

Well toelrated

42
Q

Lamotrigine

A

Lamictal

43
Q

Lamotrigine MOA

A

Delays recovery of Na channels from inactivation

44
Q

Lamotrigine Treats

A

Partial seizures
Absences and GTCs
Drop attacks

45
Q

AE and upside

A

U: no enzyme induction
Dizziness, ataxia, N/V with other AEDs
Anti-folate activity (risk of doubled oral clefts)

46
Q

Topiramate

A

Topamax

47
Q

Topiramate MOA

A

Antagonizes AMPHA/kainate glutamate receptors
Block Na
Activates hyperpolarizing K channels

48
Q

Topiramate treats

A

Partial or primary generalized seizures as mono >10 yo or adjunct >2

49
Q

Topiramate SE

A

((TERATOGENIC (only new one to be)
Cognitive impairment (too fast titration)
Kidney stones**

50
Q

Levetiracetam

A

Keppra

51
Q

Levetiracetam MOA

A

Unknown

52
Q

Levetiracetam treats

A

Myoclonic, partial onset and GTCs

53
Q

Levetiracetam SE

A

Well tolerated with some CNS

Possible anti-epileptogenic properties

54
Q

Zonisamide

A

Zonegran

55
Q

Zonisamide MOA

A

Blocks Na and Ca channels

56
Q

Zonisamide treats

A

Adjunctive for partial seizures

57
Q

Zonisamide side effects

A

SULFA!!!
CNS
Kidney stones
Long-half life

58
Q

New Vs Old

A
Similar effectiveness
Less sedative
Well tolerated
Improved PK (few p450 and interactions)
Little to no teratogenicity (except topirimate)
59
Q

Outcomes with treatment

A

60% seizure free with AEDs
20% seizure reduction with AEDs
20% 2 drugs failed (pharmacoresistent and more common in kids)

60
Q

Ketogenic diet

A

high fat
low protein
low carbs
- Very hard!!