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48 Cards in this Set

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Lamotrigine


Mechanism of Action

Inactivates Na+ channel




Inhibits presynaptic voltage-gated Ca2+ channels = no excitatory NT release

Lamotrigine


Indications

Focal (partial) seizures




Generalized tonic-clonic seizures




Absence seizures

Lamotrigine


Side Effects

Rash - common in children

Lamotrigine


Drug Interactions

Decrease half-life: phenytoin, primidone, carbamazepine




Increase half-life: valproate

Levetiracetam


Mechanism of action

Inhibits Ca2+-dependent excitatory NT release by interfering with vesicle fusion


Protein ligand of synaptic vesicle protein 2A (SV2A)

Levetiracetam


Indications

Focal (partial) seizures




Generalized tonic-clonic seizures





Myoclonic seizures

Levetiracetam


Side Effects

Dizziness, somnolence, weakness, serious derm issues


Possible behavior changes (especially in pts with a psych condition)

Levetiracetam


Drug Interactions



No clinically significant drug-drug interactions

Carbamazepine


Oxacarbazepine


Mechanism of Action

Inactivates Na channel




Potentiates GABA response

Carbamazepine


Oxacarbazepine


Topiramate


Indications

Focal (partial) seizures




Generalized tonic-clonic seizures

Carbamazepine


Metabolism

Highly bound to proteins




Has an active metabolite

Carbamazepine


Side Effects

CNS side effects: diplopia, nystagmus, dizziness, ataxia


Aplastic anemia, blood dyscrasias


Rash (common) - derm issues in Chinese and South Asians

Carbamazepine


Drug Interactions

Drugs (cimetidine, propoxyphene, diltiazem, erythromycin, isoniazid, verapamil) inhibit hepatic metabolism = increased toxicity

Oxacarbazepine


Metabolism/Toxicities/Drug Interactions

Improved toxicity profile compared to carbamazepine (less induction of hepatic enzymes)

Ethosuximide


Mechanism of Action

Inhibits T-type Ca2+ channel activity in thalamic neurons

Ethosuximide


Indications

Absence seizures




Myoclonic seizures

Ethosuximide


Metabolism

Not protein bound




Metabolized by microsomal enzymes

Ethosuximide


Side Effects

Gastric distress: pain, nausea, vomiting




Considered safe

Valproic Acid


Mechanism of Action

Inactivates Na+ channel




Reduces T-type Ca2+ channel activity




Increases GABA by inhibiting GABA-T

Valproic Acid


Indications

Complex focal (partial) seizures




Generalized tonic-clonic seizures




Absence seizures




Myoclonic seizures

Valproic Acid


Metabolism

Well absorbed




Not clear what the active drug is

Valproic Acid


Side Effects

Gastric distress: nausea, vomiting, other




Little sedation




Hepatotoxicity can be severe

Benzodiazepines


Mechanism of action

Increase affinity of GABA for GABA-A receptor

Benzodiazepines


Indications

Status epilepticus

Clonazepam


Indications

Absence seizures




Generalized tonic-clonic seizures




Myoclonic seizures

Benzodiazepines


Metabolism

Well-absorbed




Widely distributed




Metabolised in liver by microsomal enzymes

Benzodiazepines


Side Effects

Sedative




Tolerance leads to withdrawal (limits usefulness in treating epilepsy)

Phenytoin


Mechanism of action

Inactivates Na+ channel



Phenytoin


Indications

Focal (partial) seizures




Generalized tonic-clonic seizures




Status epilepticus

Phenytoin


Side Effects

Arrhythmias with rapid infusion (for status epilepticus)


Gingival hyperplasia


Hirsutism


Rash (5-10%)


CNS depression, headache

Phenytoid


Toxicities

Acute oral overdose --> loss of balance

Gabapentin


Mechanism of action

Block voltage-gated Ca channel subunit --> decrease glutamate release




Inhibits GABA-T (at phsyiological concentrations?)

Gabapentin


Indications

Focal (partial) seizures w/ or w/o secondary generalizations - adjuvant therapy




Generalized tonic-clonic seizures

Gabapentin


Metabolized

Not protein bound




Not metabolized

Gabapentin


Drug Interactions

Interacts with cimetidine and AI/Mg antacids

Gabapentin


Alternative use

Used in chronic pain management

Vigabatrin


Mechanism of action

Inhibits GABA-T

Vigabatrin


Indications

Refractory (to several other AEDs) complex focal (partial) seizures - adjuvant therapy




Infantile spasms

Vigabatrin


Drug Interactions

Reduces plasma concentrations of primidone

Vigabatrin


Side effects

Potentially irreversible concentric visual field defect


Drowsiness, dizziness, weight gain

Topiramate


Mechanism of Action

Inactivates Na+ channels




Inhibits kainite and/or AMPA glutamate receptors




Enhances action of GABA

Topiramate


Side Effects

Somnolence, fatigue, weight loss, nervousness, cognitive impairment

Topiramate


Alternative use

Used in migraine prophylaxis

Zonisamide


Mechanism of action

Inactivates Na+ channels - primary site of action




Inhibits T-type Ca2+ channels

Zonisamide


Indications

Focal (partial) seizures - adjuvant therapy




Absence seizures




Myoclonic seizures




Infantile spasms

Zonisamide


Side Effects

Drowsiness, cognitive impairment, potentially serious skin rashes

Zonisamide


Drug Interactions

Does not interact with antiseizure drugs

Epilepsy and pregnancy

1. Epilepsy = 2-fold higher risk of birth defects


2. Antiepileptics implicated in birth defects


3. Lowest effective dose of monotherapy used


4. Drug withdrawal dangerous for fetus


5. Prophylactic folic acid


6. Some drugs cause vit K deficiency = risk of hemorrhage at birth