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Pharmacology > EXAM #3: ANTICONVULSANTS II > Flashcards

EXAM #3: ANTICONVULSANTS II Flashcards

1
Q

What two drugs are Hydantoins?

A

Phenytoin

Fos-phenytoin

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2
Q

What is the difference between Phenytoin and Fos-phenytoin?

A

Fos-phenytoin is a prodrug that is more soluble, making it available for IV and IM preparations

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3
Q

What is the effect of Phenytoin on metabolism?

A

Induction of cytochome p450

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4
Q

What type of elimination does Phenytoin undergo?

A

Zero-order i.e. system can become SATURATED

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5
Q

What is the mechanism of action of Phenytoin?

A

1) Blocks Na+ channels by binding the voltage gated Na+ channel in the inactivated state
2) Enhances GABA release
3) Decreases glutamate release
4) Prevents seizure propagation

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6
Q

What are the clinical indications for Phenytoin?

A

1) Grand mal seizure
2) Patrial seizure
3) Status epilepticus

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7
Q

What is the unique adverse effect that is strongly associated with Phenytoin?

A

Gingival Hyperplasia

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8
Q

What is Fetal Hydantoin Syndrome?

A

Teratrogenic syndrome including cleft lip and palate cause by Phenytoin ingestion during pregnancy

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9
Q

What class of drug is Carbamazepine?

A

Tricyclic

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10
Q

What is the mechanism of action of Carbamazepine?

A

Inhibition of voltage-gated Na+ channels

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11
Q

What is the effect of Carbamazepine on metabolism?

A

Potent induction of CYP p450

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12
Q

What is Oxacarbazepine?

A

New drug with similar structure to Carbamazepine that has FEWER side effects

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13
Q

What are the clinical indications for Carbamazepine?

A

1) General tonic-clonic seizures
2) Partial seizures
3) Trigeminal neuralgia
4) Bipolar disorder (manic phase)

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14
Q

What is the drug of choice for trigeminal neuralgia?

A

Carbamazepine

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15
Q

What is the unique side effect of Carbamazepine?

A

SIADH i.e “Syndrome of Inappropriate ADH Secretion” leading to fluid retention and hyponatremia

Also, like Phenytoin, a potent Teratogen

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16
Q

What is the mechanism of action of Phenobarbital?

A

Increases the duration of opening of GABA receptors on the post-synpatic cell

17
Q

What is Phenobarbital commonly clinically used for?

A

1) Neonatal seizures
2) Seizures in pregnancy
3) Status epileptics

18
Q

What is Primidone?

A

Prodrug of Phenobarbital

19
Q

What type of seizure is Ethosuximide used to treat?

A

Petite mal

20
Q

What is the mechanism of action of Ethosuximide?

A

Blocks pre-synpatic T-type Ca++ channels

21
Q

What is the second drug used to treat Petite Mal seizures?

A

Valproic acid

22
Q

What is the mechanism of action of Valproic acid ?

A

1) T-type Ca++ channel blocker

2) Inhibition of GABA transaminase (increase GABA in synapse)

23
Q

What are the unique side effects of Valproic acid ?

A

1) Hepatotoxic syndrome

2) Teratogenic risk

24
Q

What is the preferred initial agent for status epilepticus?

A

Diazepam

Note that this is relatively short acting and requires an additional drug to maintain cessation of seizure activity*

25
Q

What is the difference between Lorazepam and Diazepam?

A

Lorazepam is longer acting in status epilepticus

26
Q

What is the mechanism of action for Diazepam?

A

Increases the frequency of GABA-A channel opening

27
Q

What is the mechanism of action of Gabapentin?

A

Synthetic GABA analog that BLOCKS pre-synapatic Ca++ channels

(Counter-intuitive)

28
Q

What are the clinical indications for Gabapentin?

A

1) Grand mal seizure

2) Neuropathic pain

29
Q

What is Pregablin?

A

Lyrcia, a newer GABA analog

30
Q

What is the mechanism of action of Lamotrigine?

A

Blocks pre-synaptic Na+ and Ca++ channels

31
Q

What is the unique adverse effect associated with Lamotrigine?

A

Stevens Johnson Syndrome

32
Q

What is the mechanism of action of Felbamate?

A

Blocks Na+ and glutamate receptors

33
Q

What adverse effects as associated with Felbamate?

A
  • Aplastic anemia

- Liver failure

34
Q

What is the mechanism of action of Tiagabine?

A

Inhibits GABA uptake

35
Q

What are the two major drugs we discussed as muscle-relaxants?

A

1) Diazepam

2) Baclofen

36
Q

What is the mechanism of action of diazepam as a muscle relaxant?

A

Increases frequency of central GABA-A receptor opening to increase central inhibitor effect

37
Q

What is the difference GABA-A and GABA-B receptors?

A 
A= Cl- ion channel 
B= GPRC that increases K+ conductance
38
Q

What is the mechanism of action of Baclofen?

A

GABA-B receptor agnoist that increases K+ conductance

39
Q

Clinically, what is the difference between Diazepam and Baclofen?

A

Baclofen causes less sedation

Pharmacology (64 decks)

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