Anti-Convulsants Flashcards by Stephanie Davison

Epilepsy treatment aimed at

elevating seizure threshold (stabilize membrane) or

2. limiting propagation (reduce synaptic transmission or nerve conduction)

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MOA of gabapentin and pregabalin

VSCC at A2-Delta ligand binding site

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MOA of valproic acid, divaloproex

?VSSC at unknown binding site

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MOA of lamotrigine and carbamazepine

L: VSCC (decrease Glu release) and VSSC (suppress repetitive APs)

C: VSSC at channel site in Alpha subunit

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tx of Grand mal (Generalized Tonic-Clonic) seizures

Valproate
Levetriacetam
Lamotrigine

*also tx of Atonic myclonic sz

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tx of Generalized Absence seizures (Petit mal)

Ethosuximide

2. Valproate

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A 9-year-old boy is sent for neurologic evaluation because of episodes of apparent inattention. Over the past year, the child has experienced episodes during he develops a blank look on his face and his eyes blink for 15 sec. He immediately resumes his previous activity. Which one of the following best describes this patient’s seizures? 
A.  Simple partial 
B.  Complex partial 
C.  Tonic-clonic 
D.  Absence
E.  Myoclonic

D.  Absence

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A 42-year-old man undergoes a neurologic examination because of episodes of apparent confusion. Over the past year, the man has experienced episodes during which he develops a blank look on his face and fails to respond to questions. Moreover, it appears to take several minutes before the man recovers from the episodes. Which of the following best describes this type of seizure? 
A.  Focal-simple partial 
B.  Focal-complex partial 
C.  Tonic-clonic 
D.  Absence 
E.  Myoclonic

B.  Focal-complex partial

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Tx of Partial seizures

Carbamazepine (Tegretol)*
Levetiracetam
Lamotrigine

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A young male patient suffers from a seizure disorder characterized by tonic rigidity of the extremities followed in 15-30 sec of tremor progressing to massive jerking of the body. This clonic phase lasts for 102 min, leaving the patient in a stuporous state. Of the following drugs, which is most suitable for long-term management of this patient? 
A.  Lamotrigine 
B.  Ethosuximide 
C.  Diazepam 
D.  Carbamazepine 
E.  Gabapentin

A.  Lamotrigine

D.  Carbamazepine

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A 52-year-old man has had several focal complex partial seizures over the last year. Which of the following therapies would be the most appropriate initial therapy for this patient? 
A.  Lamotrigine plus carbamazepine 
B.  Levetiracetam 
C.  Clonazepam 
D.  Ethosuximide 
E.  Phenytoin 
F.   Watchful waiting

B.  Levetiracetam

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Which of the following anticonvulsive agents does NOT result in additive CNS depression (increased somnolence) when given with opioid analgesics?
A.  Phenytoin (Dilantin ®)
B.  Carbamazepine (Tegretol®)
C.  Phenobarbital (Luminal®)
D.  Diazepam (Valium®)
E.  Levetiracetam (Keppra®)
F.   All of the above will produce additive CNS depression

F.   All of the above will produce additive CNS depression

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Potential mechanisms of action of anticonvulsant drugs include all of the following EXCEPT:
A.  Enhancement of GABA activity
B.  Enhancement of glutamate activity
C.  Decrease spread of abnormal neuronal foci through normal tissue
D.  Blockade of sodium channel to suppress repetitive action potential
E.  Blockade of T-type Ca++ channels in thalamocortical pathways

B.  Enhancement of glutamate activity

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What drugs?

MOA: inhibit sodium channel fxn to suppress repetitive AP firing

Phenytoin
Carbamazepine
Lamotrigine
topiramate

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What drugs?

MOA: enhance the inhibitory effect of GABA via increased opening of Cl channels

Benzos and phenobarbital

*Valproate partly works by increased GABA action

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Which anticonvulsant drug is INCORRECTLY matched
with its mechanism of action?
A.  Valproic acid–> enhancement of GABA activity B.  Levetiracetam –> block of Ca++-mediated release of glutamate activity
C.  Carbamazepine –> enhancement of GABA activity
D.  Phenytoin –> block of VSSC –> suppress repetitive action potential
E.  Ethosuximide –> block of T-type Ca++ channels in thalamocortical pathways
F.   Diazepam –> block of VSSC –> suppress repetitive action potential

C.  Carbamazepine –> enhancement of GABA activity

***Inhibits Na channels and repetivtive AP firing

F.   Diazepam –> block of VSSC –> suppress repetitive action potential

MOA of what anti-seizure drug?

Decrease in low-threshold Ca++ (T-type) current
-Oscillatory currents in thalamic neurons are abnormal in absence seizures - blocked by ____

ethosuximide

MOA of what anti-seizure drug?

Inhibition of high-voltage activated Ca++-channels
-VSCC (aka N-type) involved in regulation of glutamate NT release- ___

lamotrigine

MOA of what anti-seizure drug?

Inhibits function of synaptic vesicle protein SV2A  
-Impairs Ca++-mediated neurotransmitter release - __

levetiracetam

Adverse reactions of Carbamazepine (Tegretol)

Diplopa-ataxia-sedation (DD)
GI upset
Aplastic anemia-agranulocytosis
Hepatotxicity
DDI: strong inducer of CYP450

The mechanism of antiseizure activity of carbamazepine is:
A.  Block of calcium ion channels
B.  Facilitation of GABA actions on chloride ion channels
C.  Glutamate receptor antagonism
D.  Inhibition of GABA transaminase
E.  Block of sodium ion channels

E.  Block of sodium ion channels

Which statement about phenytoin is accurate?
A.  Displaces sulfonamides from plasma proteins
B.  Drug of choice in myoclonic seizures
C.  Can be used for tonic-clonic seizures
D.  Half-life is increased if used with phenobarbital
E.  Isoniazid decreases steady-state blood levels
F.   Toxic effects may occur with only incremental increases in dose

C.  Can be used for tonic-clonic seizures

F.   Toxic effects may occur with only incremental increases in dose

Adverse reactions of Phenytoin (Dilantin)

Nystagmus-diplopia- ataxia- sedation (DD)
Rash
Gingival Hyperplasia
Hirsutisim
LT: Osteomalacia,
periperal neuropathy
DDI: Strong inducer of CYP450

With chronic use in seizure states, the adverse effects of this drug include coarsening of facial features, hirsutism, and gingival hyperplasia. 
A.  Carbamazepine 
B.  Clonazepam 
C.  Ethosuximide 
D.  Phenobarbital 
E.  Phenytoin

E.  Phenytoin

Adverse Effects of Lamotrigine (Lamictal)

* similar to phenytoin (lower incidence) 1. diplopia 2. ataxia 3. dizzy 4. skin rashes 5. sedation

Adverse effects of Levetiracetam (Keppra)

1. Sleepy 2. Asthenia 3. dizzy 4. low incidence of cognitive effects 5. miminal DDI--> NO CYP450 metabolism

``` A patient with focal complex seizures has been treated for 6 months with carbamazepine but, recently has been experiencing breakthrough seizures on a more frequent basis. You are considering adding a second drug to the antiseizure regimen. Which of the following drugs is least likely to have a pharmacokinetic interaction with carbamazepine? A.  Topiramate B.  Lamotrigine C.  Levetiracetam D.  Valproic acid E.  Phenytoin ```

C.  Levetiracetam *No CYP450 metabolism

A 25-year-old woman with myoclonic seizures is well controlled on valproic acid. She indicates that she is interested in becoming pregnant in the next year. With respect to her antiepilepsy medication, which of the following should be considered? A.  Leave her on her current therapy B.  Consider switching to levetiracetam C.  Consider adding a second antiseizure medication D.  Decrease her valproate dose

B.  Consider switching to levetiracetam (keppra)

A young female patient suffers from absence seizures. Which of the following statements about her proposed drug management is NOT accurate? A.  Ethosuximide and valproic acid are preferred drugs B.  GI side effects are common with ethosuximide C.  Patient should be examined every 2-3 months for deep tendon reflex activity D.  The use of valproic acid in pregnancy may cause congenital malformations E.  Weight gain is common in patients on valproic acid

C.  Patient should be examined every 2-3 months for deep tendon reflex activity

Adverse drug reactions for Ethosuximide (Zaronitin)

* generally few 1. Gastric distress-N/V, pain (MC) (DD) 2. Transient lethargy-fatigue 3. dizzy 4. HA 5. DDI: CYP inhibitors or inducers

Adverse reactions for Valproate (Depakote)

1. GI upset (N/V, pain) (DD) 2. Wt. gain 3. BLACK BOX: - Hepatic failure --> death if <2y/o (monitor LFTs) - Pancreatitis (monitor sx) - Neural tube defects/teratogenic effects (weight benefit-risk)

``` A 9-year-old child is having learning difficulties at school. He has brief lapses of awareness with eyelid fluttering that occur every 5-10 min. EEG studies reveal a brief 3- Hz spike and wave discharges appearing synchronously in all fields, Which drug would be effective in the this child without the disadvantages of excessive sedation or tolerance development? A.  Clonazepam B.  Diazepam C.  Ethosuximide D.  Phenobarbital E.  Valproic acid ```

C.  Ethosuximide** E.  Valproic acid dx: absense sizures

``` Which drug used in management of seizure disorders is most likely to elevate the plasma concentrations of other drugs administered concomitantly? A.  Carbamazepine B.  Phenobarbital C.  Phenytoin D.  Valproic acid E.  Levetiracetam ```

D.  Valproic acid

``` A child is experiencing absence seizures that interrupt his ability to pay attention during school and activities. Which of the following therapies would be most appropriate for this patient? A.  Carbamazepine B.  Ethosuximide C.  Diazepam D.  Phenytoin E.  Valproic acid F.   Watchful waiting ```

B.  Ethosuximide** | E.  Valproic acid

Drug of choice for status epilepticus

Diazepam (Valium)

``` Patients should be carefully monitored for gingival hyperplasia if they are taking: A.  Clozapine (Clozaril®) B.  Alprazolam (Xanax®) C.  Carbamazepine (Tegretol®) D.  Phenytoin (Dilantin ®) E.  Valproic acid (Depakote®) F.   Zolpidem (Ambien®) G.  Phenelzine (Nardil®) ```

D.  Phenytoin (Dilantin ®)

``` Of the currently available anticonvulsant agents listed below, which is the preferred agent for the initial treatment of status epilepticus or local anesthetic-induced seizures? A.  Carbamazepine (Tegretol®) B.  Diazepam (Valium ®) C.  Ethosuximide (Zarontin®) D.  Phenobarbital (Luminal®) E.  Phenytoin (Dilantin®) F.   Valproic acid (Depakote®) G.  Midazolam (Versed ®) ```

B.  Diazepam (Valium ®)** | G.  Midazolam (Versed ®)

Risk to offspring from antiepileptic drugs generally __ risk from maternal seizures during pregnancy

less than

What anticonvulsants have the highest risk of fetal abnormalities and what have lower rates

Highest: Valproate, phenobarbital Lower: Carbamazepine, phenytoin, lamotrigine *monotherapy preferred and lower dose