15- Anticonvulsants Flashcards
1
Q
diazepam (Valium)
A
Benzodiazepine Anticonvulsant (emergent only)
- enhances GABA receptor activation to inc. inhibitory tone and prevent nerve impulse transmission
- Used for: emergency treatment of status epilepticus (IV)
- tolerance develops in 1-6 months
2
Q
lorazepam (Ativan)
A
Benzodiazepine Anticonvulsant (emergent only)
- enhances GABA receptor activation to inc. inhibitory tone and prevent nerve impulse transmission
- Used for: emergency treatment of status epilepticus (IV)
- tolerance develops in 1-6 months
3
Q
carbamazepine (Tegretol)
A
- inhibits VGNa+ channels
- Used for: simple, partial complex & tonic-clonic seizures
- Highly lipid soluble (into CNS quickly)
- Metabolized by CYPs and can induce CYPs
- Metabolism inhibited by several drugs
- S/FX: hepatotoxicity, teratogenic
4
Q
ethosuximide (Zarontin)
A
Anticonvulsant
- inhibits VGCa++ channels in thalamus preventing rhythmic depolarization of neurons
- drug of choice for absence seizures
- not bound to plasma proteins
- 75% metabolized by CYPs
5
Q
gabapentin (Neurontin)
A
Anticonvulsant
- inhibits Ca++ channels
- enhances inhibitory GABA neurotransmission
- Used for: simple, complex partial seizures; generalized tonic-clonic seizures
- not metabolized and does not induce CYPs
- does not bind to plasma proteins
- negligible drug interactions
6
Q
lamotrigine (Lamictal)
A
Anticonvulsant
- inhibits Na+ channels, and Ca++ channels (possibly prevents glutamate release)
- Used for: simple, and complex partial seizures; generalized tonic-clonic seizures
- Half-life decreased by enzyme inducing drugs but inc. by valproic acid
7
Q
phenobarbital (Luminal)
A
Barbiturate Anticonvulsant
- enhances GABA receptor activation to inc. inhibitory tone thus inhibiting impulse transmission
- Used for: simple partial seizures, recurrent tonic-clonic seizures; febrile seizures
- freely penetrates brain
- 75% inactivated by hepatic microsomal system
- S/FX: teratogenic, megaloblastic anemia
8
Q
phenytoin (Dilantin)
A
Anticonvulsant
- inhibits VGNa+ channels
- drug of choice for initial therapy of adult epilepsy (oral)
- Used for: partial simple, complex; tonic clonic seizures
- can be used IV for emergency tx of status epilepticus
- NOT USED: in absence seizures (makes worse)
- High plasma protein binding (90%) and 95% metabolized by P450 system
- enhances CYP metabolism of other drugs and certain drugs inc./dec. phenytoin metabolism
- S/FX: gingival hyperplasia, megoblastic anemia, teratogenic
9
Q
valproic acid/Valproate (Depakene)
A
Anticonvulsant
- mainly inhibits Na+ channels and Ca++ channels
- enhances inhibitory GABA receptor activation
- drug of choice for myoclonic seizures
- high plasma protein binding (90%)
- metabolized by CYPs
- S/FX: nausea
- Divalproex reduces GI irritation
10
Q
pregabalin (Lyrica)
A
Anticonvulsant
- inhibits Ca++ channels thus preventing glutamate release
- Used for: simple and complex partial seizures
- S/FX: thrombocytopenia
11
Q
topiramate (Topamax)
A
Anticonvulsant
- inhibits Na+ channels
- inhibits GABA
- Used for: simple, and complex partial seizures, and generalized tonic-clonic seizures
12
Q
levetiracetam (Keppra)
A
Anticonvulsant
- modifies glutamate and GABA release by binding to synaptic protein SV2A
- Used for: simple and complex partial seizures, & generalized tonic-clonic seizures
13
Q
primidone (Mysoline)
A
Barbiturate Anticonvulsant
- prodrug that metabolizes to phenobarbital
- enhances GABA receptor activation to inc. inhibitory tone thus inhibiting impulse transmission
- Used for: simple partial seizures, recurrent tonic-clonic seizures; febrile seizures
- freely penetrates brain
- 75% inactivated by hepatic microsomal system
- S/FX: teratogenic, megaloblastic anemia
14
Q
clonazepam (Klonopin)
A
Benzodiazepine Anticonvulsant (more long term)
- enhances GABA receptor activation to inc. inhibitory tone and prevent nerve impulse transmission
- Used for: myoclonic and absence seizures
- tolerance develops in 1-6 months
