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Pharm Test 4 > Anti-Epileptic Drugs > Flashcards

Anti-Epileptic Drugs Flashcards

1
Q

MOA of Phenytoin

A

Antagonist to voltage gated Na+ channel and is also secondary Ca2+ channel blocker. This delays the onset of neuron firing.

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2
Q

MOA for Oxcarbazepine

A

Antagonist to voltage gated Na+ channel

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3
Q

What Na+ voltage gated channel antagonist is preferred for children?

A

Oxcarbazepine

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4
Q

Phenytoin is used to treat what type of seizures?

A

All generalized partial and tonic-clonic seizures.

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5
Q

What is phenytoin a BIG NO for?

A

Treating juvenile myoclonic seizure because PHT aggravates JM seizures

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6
Q

Adverse effects for phenytoin

A

Gingival hyperplasia and Hirsutism

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7
Q

Phenytoin increases the conversion of of primidone to what compound?

A

phenobarbital

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8
Q

Concurrent administration of Phenytoin and carbamazepine does what?

A

Enhances metabolism of each other due to hepatic cytochrome P450 enzymes

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9
Q

Felbamate MOA:

A

Glutamatergic receptor antagonist

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10
Q

Felbamate is used only in…

A

1) Lennox-Gastaut Syndrome or

2) in patients highly refractory to other drugs.

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11
Q

Why is febamate rarely used?

A

Causes hepatic failure

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12
Q

What is the action of felbamate (FBM) on NMDA receptor?

A

1) FBM inhibits NMDA channel in a use-dependent manner.
2) FBM binds to NR2B and NR1 subunits in a voltage-independent manner.
3) FBM delays the recovery of desensitized NMDA channels. FBM is a weak positive modulator of GABA-AR Cl- current.

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13
Q

List 3 GABA regulating drugs:

A

Gabapentin, Tiagabine, Vigabatrin

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14
Q

MOA of Gabapentin

A

Releases GABA from glial cells. New drug, lipophilic, crosses BBB. Does NOT bind to GABA analog GAABA-AR.

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15
Q

MOA for Tiagabine

A

Inhibits reuptake of GABA by GABA transporter (GAT-1).

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16
Q

MOA for Vigabatrin:

A

inhibits the metabolism of GABA by GABA transaminase.

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17
Q

Therapeutic uses for Gabapentin:

A

used for neuropathic pain and migraine, but not effective for controlling seizures.

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18
Q

Therapeutic uses for Tiagabine

A

Controls tonic clonic seizures for children below 12 years old.

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19
Q

Therapeutic uses for Vigabatrin

A

First oral drug approved recently for treatment of INFANTILE SPASM and REFRACTORY COMPLEX partial seizures that are not controlled by usual treatments.

20
Q

Adverse effects of Vigabatrin

A

VGB causes liver failure, psychotic disorder, suicidal thoughts, and visual field defect.

21
Q

What are 3 drugs that can be used to treat myoclonic seizures?

A

Valproic acid, Zonisamide, Lamotrigine

22
Q

Describe Myoclonic seizures:

A

1) Common in juvenile, but rare in childhood.
2) Single multiple clonic jerks in the face, neck, upper arms.
3) Most myoclonic seizures originate from the brainstem in the CNS.

23
Q

What drugs aggravate juvenile myoclonic seizures?

A

Phenytoin and Carbamazepine

24
Q

Valproic acid is used for treatment of juvenile myoclonic seizures. What is the mechanism of action?

A

Blocker of NA+ channel and Ca2+ channel, also decreases GABA metabolism. It prolongs the recovery of voltage-activated Na+ channel from inactivation.

25
Q

Adverse effects of Valproic acid (VPA)

A

Hepatotoxic, during pregnancy can cause spina bifida (folic acid deficiency). If pregnant and need to control seizures, give VPA with folate.

26
Q

What is Zonisamide used to treat and what is the MOA?

A

Myoclonic seizures: an antagonist to NA+ and Ca2+ channels. It can cause renal stone formation.

27
Q

What type of seizure can lamotrigine treat and what is the MOA?

A

A Na+ channel blocker also effective against myoclonic seizure in children with mild side effects of dizziness, rash and headache.

28
Q

What type of seizure is this? Onset 4-12 years old and continues to adolescnece. Brief and abrupt unconsciousness (5-10sec). High voltage bilaterally synchronous spike-wave discharge is typically 2.5-3.5 Hz.

A

Absence seizure (Petit Mal)

29
Q

Drug of choice to treat Absence seizures

A

Ethosuximide (ESX)

30
Q

MOA of Ethosuximide

A

Blocks T-Type Ca+ channel. Known to inhibit GABA-T.

31
Q

Other drugs for treatment of Absent Seizures

A

Valporate and Lamotrigine (a Na+ channel blocker)

32
Q

Current Definition of Status Epilepticus

A

Seizure activity lasts for 10 min w/o recovery, or two or more seizures within 30 min.

33
Q

What was once used to treat Status Epilepticus seizures?

A

Phenobarbital- sedative and hypnotic schedule

34
Q

What has largely replaced phenobarbital for Status Epilepticus seizures?

A

Safer benzodiazepines: Lorazepam and Diazepam

35
Q

Diazepam vs Lorazepam: Which drug has a high lipid solubility?

A

Diazepam. Lorazepam has low lipid solubility.

36
Q

Diazepam vs Lorazepam: Which drug has a rapid action onset?

A

Diazepam. Lorazepam is delayed 2 min

37
Q

Diazepam vs Lorazepam: Which drug has a longer Anti-epileptic effect?

A

Lorazepam (6-12 hr). Diazepam last 15-30 min.

38
Q

Diazepam vs Lorazepam: Which drug has a longer half-life?

A

Diazepam (20-100 hr-can cause toxicity). Lorazepam (10-20 hrs).

39
Q

Diazepam vs Lorazepam: WHich drug has less respiratory depression?

A

Lorazepam. Diazepam has Resp. depression and hypotension.

40
Q

MOA for Lorazepam and Diazepam?

A

Binding of benzodiazepine to GABA receptor forms a positive allosteric effector. This stabilizes the receptor conformation to keep Cl- channel open. This increase Cl- ion influx to cause hyperpolarization, which prevents repetitive neuron firing.

41
Q

Preferred drugs for partial and generalized seizures?

A

Phenytoin, Oxcarbazepine (child), Gabapentin

42
Q

Preferred drug for myoclonic seizures?

A

Valproic Acid (Never Carbamazepine/Phenytoin)

43
Q

Preferred drug for Absence Seizures?

A

Ethosuximide (Children, adult)

44
Q

Preferred drug for Status Epilepticus?

A

Lorazepam and Diazepam

45
Q

Preferred drug for infantile spasms?

A

Vigabatrin

Pharm Test 4 (8 decks)

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