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
Q

Unknown - Seizure types

A

Juvenile myoclonic,

generalized adjunct

26
Q

Hydantoins - Drugs

A

First-line treatment for tonic-clonic and partial complex seizures

27
Q

Hydantoins - Seizure type

A

Stabilizes neuronal membranes and decreases seizure activity by increasing influx of sodium ions across
cell membranes in the motor cortex

28
Q

Hydantoins - Adr

A

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
Q

Hydantoins - Monitoring

A

Liver, renal baseline and periodic, TSH, OTC meds: ibuprofen, Antacids

30
Q

Hydantoins - interacions

A

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
Q

Carbamazepines - Seizure Type

A

Partial seizures, secondarily generalized seizures, and tonic-clonic seizures

32
Q

Carbamazepines - Moa

A

Depresses neuron transmission in the nucleus ventralis anterior of the thalamus
Has ability to induce its own metabolism

33
Q

Carbamazepines - ADR

A

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
Q

Carbamazepines Monitoring

A

Genetic testing of Asians; Baseline laboratory values: complete blood count, chemical panel, hepatic
panel, TSH level

35
Q

Carbamazepines - Interactions

A

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
Q

Succinimides - Seizure Type

A

Absence seizures in children and adults

37
Q

Succinimides - MOA

A

Suppresses seizures by delaying calcium influx into neurons

Decreases nerve impulses and transmission in the motor cortex

38
Q

Succinimides - ADR

A

GI most common; CNS: somnolence, fatigue, ataxia

Agranulcytosis, aplastic anemia, granulocytopenia

39
Q

Succinimides - Monitoring

A

CBC with differential. Liver, renal, MH

40
Q

Succinimides - Interactinos

A

Many: amphetamine, other AEDs, MAOIs, stimulants, TCAs

41
Q

Lamotrigine - Seizure Type

A

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
Q

Lamotrigine - MOA

A

Selectively binds sodium channels, stabilizing presynaptic neuronal membranes and inhibiting
glutamate release

43
Q

Lamotrigine - ADR

A

GI – mostly n/v, constipation; CV – chest pain, peripheral edema; CNS – somnolence, fatigue, dizziness,
anxiety insomnia, headache, amblyopia, nystagmus; dermatological – rashes

44
Q

Lamotrigine - Monitoring

A

Renal, liver

45
Q

Lamotrigine - Interactions

A

Levels decreased by barbiturates, estrogens, phenytoin, mefloquine
Levels increased by alcohol, carbamazepine, CNS depressants, valproic acid

46
Q

Rufinamide - Seizure Type

A

Adjunctive treatment for Lennox-Gastaut syndrome (LGS)

47
Q

Rufinamide - MOA

A

Modulates the activity of sodium channels

48
Q

Rufinamide - ADR

A

ADRs: dizziness, fatigue, headache, increased suicide risk, DRESS (drug rash with eosinophilia and
systemic symptoms)
Contraindicated in familial short QT syndrome

49
Q

Rufinamide - Monitoring

A

Drug levels might be helpful, concentrations differ markedly in patients on comparable doses

50
Q

Rufinamide - Interactions

A

Interactions: carbamazepine, phenobarbital, valproate
cytochrome P450 enzyme inducers, such as phenobarbital, primidone, phenytoin, and carbamazepine,
increase the clearance of rufinamide