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FS V, Module I > 5. Anticonvulsants > Flashcards

5. Anticonvulsants Flashcards

1
Q

I. Classification (Simplified) of Seizures
A. Generalized Seizures
____
____ (absence) or loss (tonic-clonic) of consciousness

1. \_\_\_\_
Carbamazepine (TEGRETOL) Phenobarbital*
Phenytoin (DILANTIN)
Primidone (MYSOLINE)
Topiramate (TOPAMAX)
Valproic Acid (DEPAKENE; DEPAKOTE)
  1. ____
    Acetazolamide (DIAMOX)
    Clonazepam (KLONOPIN) Ethosuximide (ZARONTIN) Trimethadione (TRIDIONE)
    Valproic Acid (DEPAKENE; DEPAKOTE)
A

bilateral
reduced

tonic-clonic (grand mal)
absence (petit mal)

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2
Q

B. Partial Seizures (Focal)
____.
Occurs in one ____ or group of muscles.

  1. Simple Partial
    No loss of ____. Drugs: same as for ____.
    Felbamate Gabapentin Lamotrigine Levetiracetam Oxcarbazepine Tiagabine Topiramate Vigabatrin Zonisamide
    (FELBATOL) (NEURONTIN) (LAMICTAL) (KEPPRA) (TRILEPTAL) (GABITRIL) (TOPAMAX) (SABRIL) (ZONEGRAN)
  2. Complex Partial
    Starts as simple: spreads to ____ area. Associated with ____.
    Drugs: same as for ____.
A

unilateral
one

consciousness
tonic-clonic

wider
confusion
tonic-clonic

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3
Q

II. Seizure Production

A. Etiology
Primary: most ____
Secondary: various causes incl. head ____ & brain tumors

B. Seizure Focus
Always ____
Abnormal ____ even in seizure-free periods; diagnostic value

C. Triggering Factors
Changes in plasma ____, pH and pCO2
Emotional stress
____ changes (e.g., strobe lights, flickering TV screen)

D. Protective Effect of Anticonvulsants
Prevent spread of abnormal ____ stimuli
Stabilize neurons surrounding the seizure focus

A

cases
trauma

present
EEG

electrolytes
visual
electrical

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4
Q

Facilitate GABA Activity

  1. Increase ____ of Opening of GABA-A-Activated Cl- Channel
    ____ (e.g., phenobarbital) / ____

2.Increase ____ of Opening of GABA-A-Activated Cl- Channel ____ (e.g., clonazepam)

  1. Increase Synaptic ____ of GABA
    ____
A

duration
barbiturate
primidone

frequency
benzodiazepines

concentration
valproic acid

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5
Q 
IV. Enzyme Inducers
\_\_\_\_ 
Felbamate 
Phenobarbital 
Phenytoin 
Primidone 
Topiramate

V. Therapeutic Levels
Best correlation with efficacy: ____ plasma levels
Currently used: ____ (free + bound)

Take a look at the table!

A

carbamazepine
free [unbound]
total

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6
Q

FREE fraction > normal in:

  • ____ disease (esp. renal failure)
  • ____ disease
  • critically ill ____ pts
  • or any other condition associated with ____
A

renal
liver
trauma
hypoalbuminemia

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7
Q

Warnings for Antiepileptic Medications

Increase in ____ on some of these drugs too

A

suicide

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8
Q

PK (Pharmacokinetic) Data
These are inducers. These other drugs are mainly renaly excreted which means that the doctor needs to know if they’re on kidney disease. If low GFR and if the drug is not highly biotransformed then the ____ is responsible for metabolism. If highly biotransformed then the ____ is responsible for metabolism. Impacts on prescriber to check all medical issues.

High protein binding. 80%+ bound to protein is at risk of interaction because that means that 20% is free. ____ are important to know- bound about 98% to plasma protein meaning only 2% is producing therapeutic affect. If knocked off by another drug and then at 4% because other drug is interacting at protein, then you’re effectively ____ the effect of the drug.

A

kidney
liver
oral anticoagulants
doubling

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9
Q

BARBITURATES

____
Metharbital(GEMONIL) [N-methylbarbital -> barbital] Mephobarbital (MEBARAL) [N-methyl phenobarbital -> phenobarbital]

ADRs
Sedation
Confusion
Dizziness

Ataxia (muscle incoordination) Blurred vision

Anxiety
Insomnia

Agitation
Hyperkinesia (increased activity)

Rash

____ deficiency

  • -Osteomalacia
  • -Rickets

____ Deficiency
–Anemia

\_\_\_\_ Deficiency (in neonate born to mother taking these drugs) 
--Increased bleeding
A

phenobarbital
vitamin D
folic acid
vitamin K

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10
Q 
Barbiturate-Related 
\_\_\_\_ (MYSOLINE)
Parent compound (primidone) is active; also two active metabolites: 
- \_\_\_\_
- \_\_\_\_

Uses
Similar to barbiturates
ADRs
Similar to barbiturates

A

primidone
phenylethylmalonamide
phenobarbital

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11
Q 
HYDANTOINS
\_\_\_\_ (DILANTIN) 
Mephenytoin (MESANTOIN) \_\_\_\_ (PEGANONE)
Less \_\_\_\_ effects than barbiturates 
Also used as anti-arrhythmic agent

ADRs
____ vision
Weakness / Dizziness / ____ / Drowsiness

A 
phenytoin
ethotoin
sedative
blurred
confusion
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12
Q

HYDANTOINS

Nystagmus: > ____ ug/mL plasma*
Ataxia: > ____ ug/mL plasma*
Lethargy: > ____ ug/mL plasma*
* at these levels, biotransformation becomes ____ order: - a small increase in dose will produce a much ____
elevation of plasma level (very disproportionate)

A 
20
30
40
zero
larger
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13
Q

HYDANTOINS

ADRs
Hallucinations / Hyperactivity Peripheral neuropathy

____ (drug withdrawal does not cause reversal)

Hirsutism

N & V / Epigastric pain / Anorexia

Decreased insulin secretion = hyperglycemia & glycosuria

____: hypocalcemia due to induced Vitamin D deficiency

Hypersensitivity reaction: ____ Syndrome
- severe–can be ____–form of erythema multiforme - if this rash occurs, must D/C immediately

____ Reactions Leukopenia
Thrombocytopenia
Anemia
Hypoprothrombinemia due to induced Vitamin K deficiency

Liver damage

A 
gingival hyperplasia
osteomalacia
stevens-johnson
fatal
hematological
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14
Q

HYDANTOINS

Enzyme Induction
Chronic administration usually produces enzyme induction:
- plasma levels ____
- pt experiences increased frequency of ____
- small increase in dose may re-establish ____ level

Monitoring
Plasma levels of ____ phenytoin provide best parameter for management of pts.
Levels in ____ correlate more reliably to concentations of free phenytoin in plasma than to total phenytoin in plasma.
Use of only the total phenytoin level may cause intoxication.

A

decrease
seizures
therapeutic

free
brain

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15
Q

HYDANTOINS

Pediatric monitoring
Can use saliva levels:
- very ____ protein
- no ____

Excellent correlation with free phenytoin levels
Saliva phenytoin
 ----------------  
Plasma phenytoin 
= (1.39/1.00)
  • higher levels in ____ due possibly to active transport of phenytoin from blood —> saliva

Advantages for pediatric monitoring include:

  • can be performed at ____
  • daily measurement
  • no ____
    • improvement in compliance
    • enhanced ____ relationship
A

low
albumin

saliva
home
trauma

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16
Q

SUCCINIMIDES
Ethosuximide (ZARONTIN)
Phensuximide (MILONTIN)

ADRs
\_\_\_\_ depression similar to barbiturates
Parkinson-like reactions
\_\_\_\_ (increased sensitivity to light)
Anemia
A

CNS

photophobia

17
Q

BENZODIAZEPINES
____ (KLONOPIN)
Clorazepate (TRAXENE)
____ (VALIUM)

Development of ____ limits use

ADRs
CNS depression similar to–but less intense than–barbiturates Wider margin of ____
Generally less ____ depression than barbiturates

A 
clonazepam
diazepam
tolerance
safety
respiratory
18
Q

Carbamazepine (TEGRETOL)

Regarded by many neurologists as DOC in ____

Also used in:

  • pain (tic doulourex)
  • ____ disorders (e.g., schizophrenia, bipolar)
ADRs
CNS depression: similar to barbiturates Ataxia
\_\_\_\_ vision
Agranulocytosis
Rash
\_\_\_\_ (possibly due to water retention)
A

partial seizures
psychiatric

double
hypertension

19
Q

Felbamate (FELBATOL)

Effective in ____: monotherapy + polytherapy (phenytoin or carbamazepine)
- induces enzymes
- lowers ____ & phenytoin levels
Also efficacious in pts with ____ syndrome
- occurs in childhood
- multiple seizure types + mental retardation
- refractory to standard ____ drugs

ADRs
____ / blurred vision
N & V / anorexia
____

A

partial seizures
carbamazepine
lennox-gastaut syndrome
anticonvulsant

double
insomnia

20
Q

Keppra® (levetiracetam)
Ethyl-2-oxo-1-pyrrolidine acetamide.
____ unrelated to existing antiepileptic drugs (AEDs).

Mechanism of Action
     Precise mechanism(s) by which levetiracetam exerts its
     antiepileptic effect is \_\_\_\_.

In vitro and in vivo recordings of epileptiform activity from hippocampus show it inhibits burst firing without affecting normal neuronal excitability – may selectively prevent both:
● hypersynchronization of ____ burst firing
● propagation of ____ activity.

A

chemically
unknown
epileptiform
seizure

21
Q

Keppra (levetiracetam)

 Did not demonstrate binding affinity for variety of known
     receptors:
          ● \_\_\_\_
          ● \_\_\_\_
          ● \_\_\_\_

No effect on neuronal voltage-gated ____ or T-type calcium
currents

 Shown to block negative modulators of \_\_\_\_- and glycine-gated
 currents.

 Partially inhibits \_\_\_\_-type calcium currents in neuronal cells. -> reduced \_\_\_\_ release

 Effective  as adjunctive therapy in adult patients with refractory partial onset seizures with or without secondary generalization.
A 
GABA
glycine
NMDA (N-methyl-D-aspartate)
sodium
GABA
N
NT
22
Q

Keppra (levetiracetam)

This chart shows whats taking effect. Reduction in dosage when there is a decrease in kidney function. Not as much biotransformation. If the organ isn’t functioning well theres an issue. Low biotransformation means its processed in ____. (said this a few times) High biotransformation takes place in the ____.

A

kidney

liver

23
Q 
Valproic Acid (DEPAKENE)
DEPAKOTE: enteric-coated product
Mechanisms:
1. Blockade of \_\_\_\_+ channel
2. Inhibition of \_\_\_\_ (catabolic GABA enzyme)

ADRs
Sedation / Ataxia
Tremor
N & V / Anorexia

____:

  • can be fatal!
  • > 60 deaths have already occurred
  • generally occurs within ____ months of initiation of therapy
  • may be ____ if therapy terminated in time

Plasma Protein Binding
Valproic acid is highly ____ bound.

Free levels increase:

  • as dose ____ (disproportionate)
  • when competing drugs are added to therapy (e.g., ____)
A

Na
GABA transaminase

hepatotoxicity
six
reversible

protein

increase
ASA

24
Q

WITHDRAWAL of ANTICONVULSANT THERAPY
Can be considered for some pts

if seizure-free for at least ____ years. Must be withdrawn ____ (i.e., over a ____-month period).

% of ____ remaining seizure-free (70-90%) > % of adults(60-65%)

Best chance of success includes pt with:

  • no mental ____
  • ____
A

2
slowly
6

children
retardation
monotherapy

25
Q 
EPIDOLEX
Contains \_\_\_\_ (CBD).    Oral solution: 100 mg/mL

Approved for two potentially fatal forms of severe childhood epilepsy:

  • ____ syndrome
  • ____ syndrome in pts 2 years of age and older.

DOSAGE AND ADMINISTRATION
Due to risk of hepatocellular injury, obtain serum ____ (ALT
and AST) and total bilirubin levels in all patients prior to starting treatment with Epidiolex

Obtain serum transaminases(ALT and AST) and total bilirubin levels in all patients prior to starting treatment.

Recommended starting dosage: ____mg/kg BID (5mg/kg/day).
After one week, dosage can be increased to maintenance dosage of 5
mg/kg BID

A

cannabidiol
lennox-gastaut
dravet

transaminases

2.5

26
Q

EPIDOLEX

CLINICAL PHARMACOLOGY
Precise mechanisms by which EPIDIOLEX exerts its anticonvulsant effect
in humans are unknown.
Cannabidiol does not appear to exert its anticonvulsant effects through interaction with receptors.
Elimination T1/2 – approx. ____ hours.

BIOTRANSFORMATION
Highly biotransformed by ____ and CYP3A4 enzymes

Moderate or strong inhibitors & inducers of ____ or CYP2C19 may require dosage adjustments.

ADRs
Most common (10% or more): ____; decreased appetite; diarrhea;
transaminase elevations; fatigue, malaise, and asthenia; rash;
insomnia, sleep disorder, poor quality sleep; and infections..

A 
cannabinoid
60
CYP2C19
CYP3A4
somnolence
27
Q

TERATOGENICITY
Anticonvulsant-____ epilepsy > non-____ epilepsy > normal

Teratogens include:

  • ____ (possible “Fetal Benzodiazepine Syndrome”)
  • ____ (“Fetal Hydantoin Syndrome”)
  • ____ (“Fetal Valproate Syndrome”)

____ > benzodiazepines

____ (2 or more anticonvulsant drugs) > monotherapy
- benzodazepines may ____ valproate teratogenicity

A

treated
treated

benzodiazepines
phenytoin
valproic acid

valproic acid
polytherapy
enhance

28
Q

Valproic Acid Cases
1. At 12 weeks gestation:
- serum alpha-fetoprotein [AFP] level = ____ mmol/L [N = < 20]
AFP is plasma protein produced by fetal tisues (e.g., liver, GI)

also by neoplastic tissue in adults (can be employed to monitor efficacy of chemotherapy)

during pregnancy, some AFP normally crosses placental barrier

____ levels are elevated in amniotic fluid and maternal blood when fetus has neural tube defect

some states in USA mandate that a pregnant woman is to be notified of possible neural tube defect

A

90

AFP

29
Q

Valproic Acid Cases

At 33 weeks gestation:

  • myelomeningocele & ____ verified by ultrasound
  • parents rejected option of abortion

At 38 weeks gestation:

  • ____ delivery
  • open lumbosacral myelomeningocele
  • sensorimotor deficits from L-3 down
  • hydrocephalus required ventriculo-peritoneal shunt (day 7)
  • dysmorphic features (chromosomal investigation was ____)

At two years of age:

  • severe psychomotor retardation with autistic traits
  • no speech ____
A

hydrocephalus
C-section
normal
development

30
Q

STATUS EPILEPTICUS
According to the Epilepsy Foundation of America, status epilepticus is more than ____ minutes of:
1. “continuous ____ activity”
or
2. “two or more ____ seizures without full recovery of consciousness between seizures.”

Causes
Include--but NOT limited to--the following:
- medication change
- fever/infection (children > adult)
- \_\_\_\_ infection (children > adults)
- \_\_\_\_ (includes alcohol) related (adults > children) 
- head trauma
- brain tumors (adults > children)
A 
30
seizure
sequential
CNS
drug
31
Q

STATUS EPILEPTICUS

Treatment
1. ____

  1. Muscle paralysis
    - only ____ use of short-acting neuromuscular blocker
    - NOT effective in terminating seizure activity in brain:
    - abnormally increased CNS activity continues
    - can result in ____ brain damage if not stopped
  2. ____
    - usually ____ occurs first
    - induces secretion of insulin
    - secondary ____ (usually > 2 hrs after attack begins) - need determination of blood glucose level
    - if hypoglycemia is present–or glucose level can not be
    determined–glucose should be administered
  3. Blood Pressure
    - usually ____ occurs first (first 30-45 min) - hypotension may occur later
    - may lead to reduced cerebral perfusion
    - potentiation of excitotoxic brain damage
    - support BP (if necessary with vasopressors)
A

oxygenation
acute
permanent

glucose
hyperglycemia
hypoglycemia

hypertension

32
Q

STATUS EPILEPTICUS (continued)

  1. Anticonvulsants
    ____
    DOC if pt is currently convulsing (acute management)

Diazepam*
High ____ solubility (oral!) —-> rapid entrance into brain

Rapid ____: brain & plasma levels fall
quickly

____ can recur within 10-20 minutes

May cause respiratory depression & hypotension

Can be given by ____ solution (not suppository) when seizures begin at home.

A 
benzodiazepines
lipid
redistribution
seizures
rectal
33
Q

STATUS EPILEPTICUS (continued)
5. Anticonvulsants Benzodiazepines
DOC if pt is currently convulsing (acute management)

Lorazepam*
Less \_\_\_\_ soluble
Longer \_\_\_\_ of action
Clinical study indicated that efficacy = \_\_\_\_ 
Same ADRs

Midazolam
High frequency of respiratory ____
Rapid & complete absorption after IM administration

A

lipid
duration
diazepam
depression

34
Q

STATUS EPILEPTICUS (continued)
5. Anticonvulsants Benzodiazepines
DOC if pt is currently convulsing (acute management)

Phenytoin*
DOC if pt has stopped ____
Can be added to benzodiazepines
Longer ____ of action than benzodiazepines ADRs include:
- ____
- cardiac disturbances
- less respiratory depression & sedation than benzodiazepines and phenobarbital

Phenobarbital
Older drug used for many years
Efficacy = combination of \_\_\_\_ 
ADRs include:
- significant \_\_\_\_
- " respiratory depression 
- " hypotension
  • ____ routes of administration for certain benzodiazepines and phenytoin are unreliable; therefore, NOT recommended.
A 
convulsing
onset
hypotension
diazepam + phenytoin
sedation
IM
35
Q

A relatively good prognosis of SE is found when the underlying cause is associated with low ____ drug levels or ____ abuse

A

antiepileptic

alcohol

FS V, Module I (7 decks)

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