EXAM #3: ANTICONVULSANTS II Flashcards Preview

Pharmacology > EXAM #3: ANTICONVULSANTS II > Flashcards

Flashcards in EXAM #3: ANTICONVULSANTS II Deck (39):
1

What two drugs are Hydantoins?

Phenytoin
Fos-phenytoin

2

What is the difference between Phenytoin and Fos-phenytoin?

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

3

What is the effect of Phenytoin on metabolism?

Induction of cytochome p450

4

What type of elimination does Phenytoin undergo?

Zero-order i.e. system can become SATURATED

5

What is the mechanism of action of Phenytoin?

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

6

What are the clinical indications for Phenytoin?

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

7

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

Gingival Hyperplasia

8

What is Fetal Hydantoin Syndrome?

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

9

What class of drug is Carbamazepine?

Tricyclic

10

What is the mechanism of action of Carbamazepine?

Inhibition of voltage-gated Na+ channels

11

What is the effect of Carbamazepine on metabolism?

Potent induction of CYP p450

12

What is Oxacarbazepine?

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

13

What are the clinical indications for Carbamazepine?

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

14

What is the drug of choice for trigeminal neuralgia?

Carbamazepine

15

What is the unique side effect of Carbamazepine?

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

****Also, like Phenytoin, a potent Teratogen****

16

What is the mechanism of action of Phenobarbital?

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

17

What is Phenobarbital commonly clinically used for?

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

18

What is Primidone?

Prodrug of Phenobarbital

19

What type of seizure is Ethosuximide used to treat?

Petite mal

20

What is the mechanism of action of Ethosuximide?

Blocks pre-synpatic T-type Ca++ channels

21

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

Valproic acid

22

What is the mechanism of action of Valproic acid ?

1) T-type Ca++ channel blocker
2) Inhibition of GABA transaminase (increase GABA in synapse)

23

What are the unique side effects of Valproic acid ?

1) Hepatotoxic syndrome
2) Teratogenic risk

24

What is the preferred initial agent for status epilepticus?

Diazepam

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

25

What is the difference between Lorazepam and Diazepam?

Lorazepam is longer acting in status epilepticus

26

What is the mechanism of action for Diazepam?

Increases the frequency of GABA-A channel opening

27

What is the mechanism of action of Gabapentin?

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

(Counter-intuitive)

28

What are the clinical indications for Gabapentin?

1) Grand mal seizure
2) Neuropathic pain

29

What is Pregablin?

Lyrcia, a newer GABA analog

30

What is the mechanism of action of Lamotrigine?

Blocks pre-synaptic Na+ and Ca++ channels

31

What is the unique adverse effect associated with Lamotrigine?

Stevens Johnson Syndrome

32

What is the mechanism of action of Felbamate?

Blocks Na+ and glutamate receptors

33

What adverse effects as associated with Felbamate?

- Aplastic anemia
- Liver failure

34

What is the mechanism of action of Tiagabine?

Inhibits GABA uptake

35

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

1) Diazepam
2) Baclofen

36

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

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

37

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

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

38

What is the mechanism of action of Baclofen?

GABA-B receptor agnoist that increases K+ conductance

39

Clinically, what is the difference between Diazepam and Baclofen?

Baclofen causes less sedation

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