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Pharm Exam 2 > Antiepileptics > Flashcards

Antiepileptics Flashcards

1
Q

Describe the mechanism of action of lamotrigine.

A

It increases Na+ channel inactivation and inhibits the release of excitatory amino acids by acting on presynaptic voltage-gated Ca++ channels

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2
Q

Describe the adverse effects associated with lamotrigine.

A

Rash (usually in children)

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3
Q

Name the drug interactions that can occur with lamotrigine.

A

Phenytoin, primidone, and carbamazepine reduce its half-life and valproate prolongs it.

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4
Q

What are the clinical indications for lamotrigine?

A

Focal seizures, GTCs, and status epilepticus (similar to phenytoin)

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5
Q

Describe the mechanism of action of levetiracetam.

A

Believed to inhibit Ca++ dependent excitatory amino acid transmitter release by interfering with vesicle fusion

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6
Q

Describe the side effects associated with levetiracetam (Keppra).

A

Dizziness, somnolence, weakness, dermatologic conditions, behavioral changes (esp w/ psychiatric conditions), low incidence of adverse cognitive effects

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7
Q

Describe the drug interactions that can occur with levetiracetam (Keppra).

A

None

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8
Q

What are the clinical indications for levetiracetam (Keppra)?

A

Focal seizures and GTCs

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9
Q

Describe the mechanism of action of carbamazepine.

A

It is a TCA and blocks tetanic firing by inactivating Na+ channels reducing neurotransmitter release; potentiates GABA responses.

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10
Q

Describe the side effects associated with carbamazepine.

A

CNS (ataxia, diplopia, nystagmus, dizziness), rash, aplastic

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11
Q

What drug interactions can occur with carbamazepine?

A

Drugs that inhibit hepatic metabolism lead to toxicity (e.g. erythromycin, isoniazid, verapamil, etc)

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12
Q

What are the clinical indications for carbamazepine?

A

Focal partial seizures, GTCs, and trigeminal disorders

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13
Q

Describe the pharmacokinetic properties of carbamazepine.

A

70% is protein bound and it has active metabolites

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14
Q

Describe the clinical indications for oxycarbazepine.

A

Focal partial seizures and GTCs

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15
Q

Describe the mechanism of action of ethosuximide.

A

It inhibits T-type Ca++ channel activity in thalamic neurons

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16
Q

Describe the adverse effects associated with ethosuximide.

A

Toxicity causes GI distress, generally safe.

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17
Q

What are the clinical indications for ethosuximide?

A

Absence seizures and myoclonic seizures

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18
Q

Describe the mechanism of action of valproic acid.

A

Blocks tetanic firing by increasing Na+ channel inactivation and reducing transmitter release

19
Q

Describe the adverse effects associated with valproic acid.

A

Nausea, vomiting, GI distress, hepatotoxicity can be severe

20
Q

Describe the pharmacokinetic properties of valproic acid.

A

It is well absored and 90% protein-bound.

21
Q

Name the alternative agents that can be used in the treatment of seizures.

A

Phenytoin (Dilantin), gabapentin (Neurontin), vigabatrin, topiramate, zonisamide

22
Q

Describe the mechanism of action of phenytoin (Dilantin).

A

It blocks the tetanic firing by inactivating Na+ channels and reducing neurotransmitter release

23
Q

Describe the adverse effects associated with phenytoin (Dilantin).

A

Arrhythmias (esp w/ rapid infusion), CNS depression, loss of balance in acute overdose, gingival hyperplasia and hirsutism

24
Q

Name the drugs of choice for treating seizures.

A

Lamotrigine, levetiracetam (Keppra), carbamazepine, oxycarbazepine, ethosuximide, valproic acid, and diazepam (Valium)

25
Q

Describe the mechanism of action of gabapentin (Neurontin).

A

It binds to voltage-gated Ca++ channel subunits to decrease glutamate release and inhibits GABA transaminase

26
Q

Describe the clinical uses for gabapentin (Neurontin).

A

It is an adjuvant therapy for focal seizures and is also used in chronic pain management

27
Q

Describe the mechanism of action of vigabatrin

A

It inhibits GABA transaminase (GABA-T) to prevent degradation of GABA

28
Q

Describe the adverse effects associated with vigabatrin

A

It can cause potentially irreversible concentric visual field deficits, drowsiness, dizziness, weight gain

29
Q

Describe the clinical uses of vigabatrin

A

It is an adjuvant therapy for complex partial seizures refractory to AEDs

30
Q

Describe the mechanism of action of topiramate

A

It is similar to phenytoin and carbamazepine; increases Na+ channel inactivation, inhibitis kainate and/or AMPA receptors (these are types of glutamate receptors), enhances actions of GABA

31
Q

Describe the adverse effects associated with topiramate

A

Somnolence, fatigue, weight loss, nervousness, cognitive impairment

32
Q

Describe the clinical use of topiramate

A

Focal seizures and primary GTCs; also approved for migraines

33
Q

Describe the mechanism of action of zonisamide

A

Primarily acts on Na+ channels but also T-type voltage-gated Ca++ channels

34
Q

Describe the adverse effects associated with zonisamide

A

Drowsiness, cognitive impairment, serious skin rashes

35
Q

Describe the drug interactions associated with zonisamide

A

There are none

36
Q

Describe the clinical use of zonisamide

A

Adjuvant therapy for focal seizures; broad spectrum absence, myoclonic, infantile spasms)

37
Q

Which drugs can be used for focal seizures and GTCs?

A

Lamotrigine, topiramate,
carbamazepine, oxycarbazepine, phenytoin (both)
Levetiracetam (focal only)

38
Q

Which drugs can be used in status epilepticus?

A

Phenytoin, lorazepam, diazepam, phenobarbital

39
Q

Describe the pathophysiology of seizures

A

Initiated by high frequency bursts of action potentials and hypersynchronization. Increase in extracellular K+ depolarizes neighboring neurons and the accumulation of Ca++ in presynaptic terminals enhances neurotransmitter release. Depolarization induced activation of glutamate (NMDA) receptors results in Ca++ influx

40
Q

Compare the toxicity profiles of carbamazepine and oxycarbazepine

A

They are closely related by oxycarbazepine may have improved toxicity profile (less induction of hepatic enzymes)

41
Q

What drugs inactivate Na+ channels?

A

Phenytoin, carbamazepine, lamotrigine, topiramate, primidone, and valproate

42
Q

Name the drugs that reduce flow of current through T-type Ca++ channels.

A

Valproate and ethosuximide

43
Q

Absence seizures are associated with what channel?

A

T-type Ca++ channels

44
Q

Which drugs can be used for myoclonic seizures?

A

Valproic acid and clonazepam

Pharm Exam 2 (6 decks)

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