Anticonvulsants Flashcards

1
Q

Seizure

A

The clinical manifestation of an abnormal hypersynchronized discharge in a population of
cortical excitatory neurons

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2
Q

Epilepsy

A

A tendency toward recurrent seizures unprovoked by acute systemic or neurologic insults

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3
Q

Focal classifications

A

simple partial
complex partial
secondarily generalized

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4
Q

Generalized classifications

A
absense
myoclonic
clonic
tonic
tonic clonic
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5
Q

An antiepileptic drug (AED) is a drug which

A

decreases the frequency and/or severity of

seizures in people with epilepsy

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6
Q

Antiepileptic Drug (AED) - treates

A

Treats the symptom of seizures, not the underlying epileptic condition

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7
Q

Antiepileptic Drug (AED) - does not

A
Does not prevent the development of epilepsy in individuals who have acquired a risk
for seizures (e.g., after head trauma, stroke, tumor)
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8
Q

Antiepileptic Drug (AED) goal of therapy

A

Goal of therapy is to maximize quality of life by eliminating seizures (or diminish seizure
frequency) while minimizing adverse drug effects
• AEDs have wanted and unwanted effects on target organ

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9
Q

Excitation (too much)

A
  • Ionic: inward Na+ and Ca++ currents

* Neurotransmitter: glutamate, aspartate

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10
Q

nhibition (too little)

A

Ionic: inward CI-
, outward K+ currents
• Neurotransmitter: GABA

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11
Q

Ion Channel
Modulators
(reduce neuron
excitability - Traget molecule

A

Partial, secondary
(2ndary)generalized or
generalized tonicclonic

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12
Q

Ion Channel
Modulators
(reduce neuron
excitability - Drugs

A
Ethosuximide, gabapentin, pregabalin
Retigabin
Carbamazepine, eslicarbazepine, lamotrigine,
oxycarbazepine, phenytoin, zonisamide,
lacosamide, fosphenytoin, Rufinamide
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13
Q

Ion Channel
Modulators
(reduce neuron
excitability - Seizure type

A

Calcium ion channel
Potassium ion channel
Sodium ion channel

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14
Q
Enhancers of
GABAergic
transmission
(enhancer
inhibitory
transmission) - Target molecule
A
Emergency treatment
Partial, 2nd line add on
Refractory complex
adjunctive
Partial, 2ndary T-C
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15
Q
Enhancers of
GABAergic
transmission
(enhancer
inhibitory
transmission) - Drugs
A
Clobazam, Clonazepam, Diazepam,midazolam
phenobarbital, primidone
Tiagabine
Vigabatrin
Gabapentin, Pregabalin,
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16
Q
Enhancers of
GABAergic
transmission
(enhancer
inhibitory
transmission) - Seizure Type
A

GABAA receptor agonists
GABA Reuptake inhibitor
GABA Transaminase inhibitor
Potential GABA

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17
Q

Glutamate
modulators
(direct and
indirect) - Target Molecule

A

AMPA receptor

NMDA receptor

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18
Q
Glutamate
modulators
(direct and
indirect)
- Drugs
A

Perampanel

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19
Q
Glutamate
modulators
(direct and
indirect)
 - Seizure Type
A

Partial onset, 2ndary

generalized

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20
Q

Multiple modes
of action
- Target Molecule

A

Na ion, GABAA receptors, NMDA
Na ion, AMPA/kainite,GABAA
Na ion, GABA turnover, NMDA

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21
Q

Multiple modes
of action
- Drugs

A

Felbamate
Topiramate
Valproate

22
Q

Multiple modes
of action
- Seizure Type

A

Multiple*
Multiple
Wide range of seizures

23
Q

Unknown- Targt molecule

A

Human synaptic vessel protein

(SV2A)?

24
Q

Unknown Drugs

A

Levetiracetam

25
Unknown - Seizure types
Juvenile myoclonic, | generalized adjunct
26
Hydantoins - Drugs
First-line treatment for tonic-clonic and partial complex seizures
27
Hydantoins - Seizure type
Stabilizes neuronal membranes and decreases seizure activity by increasing influx of sodium ions across cell membranes in the motor cortex
28
Hydantoins - Adr
Nystagmus, dizziness, pruritus, paresthesia, headache, somnolence, ataxia, confusion Cardiovascular effects: hypotension, tachycardia Gastrointestinal (GI) effects: n/v, anorexia, constipation, dry mouth, gingival hyperplasia Genitourinary effects: urinary retention, urine discoloration
29
Hydantoins - Monitoring
Liver, renal baseline and periodic, TSH, OTC meds: ibuprofen, Antacids
30
Hydantoins - interacions
CYP2C9 enzyme system Levels will increase with cimetidine, diazepam, acute alcohol intake, valproic acid, allopurinol Decreases effects with barbiturates, antacids, calcium, chronic alcohol use Causes the decreased effect of: carbamazepine, estrogens, acetaminophen, corticosteroids, levadopa, sulfonylureas, cardiac glycosides
31
Carbamazepines - Seizure Type
Partial seizures, secondarily generalized seizures, and tonic-clonic seizures
32
Carbamazepines - Moa
Depresses neuron transmission in the nucleus ventralis anterior of the thalamus Has ability to induce its own metabolism
33
Carbamazepines - ADR
Black Box warning for causing blood dyscrasias Depression of bone marrow Liver damage, impairs thyroid function Drowsiness, dizziness, blurred vision, n/v, dry mouth, diplopia, headache (HA)
34
Carbamazepines Monitoring
Genetic testing of Asians; Baseline laboratory values: complete blood count, chemical panel, hepatic panel, TSH level
35
Carbamazepines - Interactions
nduces metabolism of many CYP450 substrates Drug levels increase with concurrent use of propoxyphene (Darvocet), cimetidine, erythromycin, clarithromycin, verapamil, hydantoins, grapefruit/juice Decreases plasma levels of several drugs: beta blockers, warfarin, doxycycline, succinimides, haloperidol
36
Succinimides - Seizure Type
Absence seizures in children and adults
37
Succinimides - MOA
Suppresses seizures by delaying calcium influx into neurons | Decreases nerve impulses and transmission in the motor cortex
38
Succinimides - ADR
GI most common; CNS: somnolence, fatigue, ataxia | Agranulcytosis, aplastic anemia, granulocytopenia
39
Succinimides - Monitoring
CBC with differential. Liver, renal, MH
40
Succinimides - Interactinos
Many: amphetamine, other AEDs, MAOIs, stimulants, TCAs
41
Lamotrigine - Seizure Type
Adjunctive treatment of primary generalized tonic-clonic seizures and partial seizures in adults and children older than 2 years of age Concurrent use with valproic acid, phenytoin
42
Lamotrigine - MOA
Selectively binds sodium channels, stabilizing presynaptic neuronal membranes and inhibiting glutamate release
43
Lamotrigine - ADR
GI – mostly n/v, constipation; CV – chest pain, peripheral edema; CNS – somnolence, fatigue, dizziness, anxiety insomnia, headache, amblyopia, nystagmus; dermatological – rashes
44
Lamotrigine - Monitoring
Renal, liver
45
Lamotrigine - Interactions
Levels decreased by barbiturates, estrogens, phenytoin, mefloquine Levels increased by alcohol, carbamazepine, CNS depressants, valproic acid
46
Rufinamide - Seizure Type
Adjunctive treatment for Lennox-Gastaut syndrome (LGS)
47
Rufinamide - MOA
Modulates the activity of sodium channels
48
Rufinamide - ADR
ADRs: dizziness, fatigue, headache, increased suicide risk, DRESS (drug rash with eosinophilia and systemic symptoms) Contraindicated in familial short QT syndrome
49
Rufinamide - Monitoring
Drug levels might be helpful, concentrations differ markedly in patients on comparable doses
50
Rufinamide - Interactions
Interactions: carbamazepine, phenobarbital, valproate cytochrome P450 enzyme inducers, such as phenobarbital, primidone, phenytoin, and carbamazepine, increase the clearance of rufinamide