11 A) - ANTIEPILEPTIC DRUGS

Question 1

TOPIRAMATE.

Answer 1

RECENT BLOCK OF NA+ HANNELS

Na+ channel blockade
AMPA/kainate blockade
Potentiates GABA
Few adverse Rx
Few interactions
Teratogen risk
Wide spectrum

Question 2

FELBAMATE

Answer 2

RECENT BLOCK OF NA+ HANNELS
Na+ channel blockade
NMDA blockade
(not clear)
Hepatic failure
Aplastic anemia
Wide spectrum
Refractory cases in
children
Syndrome of Lennox- Gastaut

Question 3

LAMOTRIGINE

Answer 3

RECENT BLOCK OF NA+ HANNELS
Na+ channel blockade
Θ glutamate release
Better tolerated than
classical drugs
Skin rashes
Wide spectrum
Better studie

Question 4

ETHOSUXIMIDE

Answer 4

CLASSICAL BLOCK OF CA+2 CHANNELS

Blockade of voltage- gated Ca2+ T- channels
Nauseas, anorexia
May produce tonic-clonic
crisis
“Restricted to absence
seizures”

Question 5

GABAPENTIN

Answer 5

RECENT BLOCK OF CA+2 CHANNELS
Multiple
Developed as a GABA
agonist
Ligand of presynaptic
Ca2+ α2 δ channels
Without serious toxic effects,
dizziness, sedation…
Few drug interactions (renal
excretion)
Administration 2-3/day
- General resistant partial
crisis
Not very effective in
monotherapy
- Neuropathic pain

Question 6

PREGABALIN; Lyrica

Answer 6

CLASSICAL BLOCK OF CA+2 CHANNELS

Ligand of presynaptic
Ca2+ α2 δ channels
Without serious toxic effects,
asthenia, dizziness
Few drug interactions (renal
excretion)
Administration 2-3/day
- General resistant partial
crisis
Not very effective in
monotherapy
- Neuropathic pain

Question 7

CLASSICAL ANTIEPILEPTIC DRUGS (1st generation):

Answer 7

PHENYTOIN, PHENOBARBITAL, ETHOSUXIMIDE, CARBAMAZEPINE,

VALPROIC ACID, DIAZEPAM, CLONAZEPAM

Question 8

RECENT ANTIEPILEPTIC DRUGS:

Answer 8

VIGABATRIN, LAMOTRIGINE, GABAPENTIN, PREGABALIN, TIAGABINE,

TOPIRAMATE, FELBAMATE, LEVETIRACETAM

Question 9

PHENOBARBITAL

Answer 9

POTENTIATE NEURONAL INHIBITION; CLASSICAL

Potentiate
GABAA
receptor
activation

High sedation
Osteomalacia
Hypersensitivity
Hepatic inductor

2nd choice
in all types
Crisis in newborns

Question 10

DIAZEPAM- CLONAZEPAM

Answer 10

POTENTIATE NEURONAL INHIBITION; CLASSICAL

Potentiate GABAA
receptor
activation
Sedation
Withdrawal syndrome …
Tolerance
Epileptic mal i.v.
(Status epilepticus)
Febrile seizures
Not for chronic use

Question 11

VIGABATRIN

Answer 11

POTENTIATE NEURONAL INHIBITION; RECENT
Inhibit GABA- transaminase
(GABA-T)
(Irreversible)
Less than previous drugs:
Reduced visual field
Depression, somnolence
Psychomotor disturbance
All types

Question 12

TIAGABINE

Answer 12

POTENTIATE NEURONAL INHIBITION; RECENT

(-) GABA reuptake Somnolence
Confusion
Visual disturbance
Not completely evaluated