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Pharmacology > Antiepileptic Drugs > Flashcards

Antiepileptic Drugs Flashcards

1
Q

Epilepsy Pathophysiology

A

Causes:
50% idiopathic & 50% caused by a) genetic disorder – runs in the family
b) head trauma
c) brain conditions- brain tumours & stroke are leading cause of adult epilepsy d) infectious diseases- AIDS, meningitis & viral encephalitis
e) prenatal injury
Age – children & older adults more likely Family history
Stroke & vascular disease Dementia→risk in adults
Complications:
Falling & drowning -Car accidents ➤Pregnancy complications Emotional health issues

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2
Q

Absence seizure pathophysiology

A

● Most often they affect children.
● They can be caused by hyperventilation.
● “Safer” in terms of neurological complications.
● Treatment with inhibition of calcium channels T.
● Considered as petit mal seizures.
● Ethosuxymide and valproate.

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3
Q

Newly Diagnosed Focal

Monotherapy: 1st line agents

A 
Carbamazepine
Gabapentin
Lamotrigine
Levetiracetam
Valproic
Oxcarbazepine
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4
Q

Newly Diagnosed Focal

Polytherapy: 1st line + 2nd line

A

Topirmate, Phenobarbital, Phenytoin

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5
Q

Newly Diagnosed Focal

Polytherapy: 1st line + 3rd line

A

Vigabatrin, tiagabine, lacosamide, Pregablin, Zonisamide

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6
Q

Newly Diagnosed Generalised tonic-clonic

1st line agents

A

Valproic Acid, Lamotrigin, Levetiracetam

Carbamazepine or oxcarbazepine may ↑ number of myoclonic events

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7
Q

Newly Diagnosed Generalised tonic-clonic

1st line + 2nd line

A

Topiramate, Zonisamide, Clobazam

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8
Q

As a medical professional what is the course of action of a patient with juvenile epilepsy and a myoclonic attack ?

A

AVOID Carbamazepine, Oxcarbazepine, Pregablin, Gabadentin, Phenytoin, Vigabatrin, Tiagabine if patients has JUVENILE EPILEPSY + MYOCLONIC ATTACK (use barbiturates instead)

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9
Q

De novo Diagnosed
Generalised Myoclonic

Monotherapy: 1st line agents

A

Valproic Acids

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10
Q

De novo Diagnosed Generalised Myoclonic

1st Line + 2nd line

A

Lamotrigin, Levetiracetam

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11
Q

De novo Diagnosed Generalised Myoclonic

1st line + 2rd line

A

Clonazepam, Zonisamide, Piracetiam

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12
Q

De novo Diagnosed Generalised Atonic and Tonic

1st line agents

A

Valproic Acids

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13
Q

De novo Diagnosed Generalised Atonic and Tonic

1st Line + 2nd line

A

Lamotrigine

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14
Q

De novo Diagnosed Generalised Atonic and Tonic

1st line + 2rd line

A

Topiramate

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15
Q

WHAT IS USED IN DRUG RESISTANT EPILEPSY?

A

EPIDIOLEX (cannabidiol)

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16
Q

WHAT IS USED IN STATUS EPILEPTICUS

A

Benzodiazepines

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17
Q

Broad spectrum vs narrow spectrum

A

● Both focal and generalised seizures- broad spectrum

● Partial or absence seizures - narrow spectrum

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18
Q

Idiosyncrasy

A

In modern medicine, the term idiosyncrasy refers to the state of increased reactiveness of the body to a specific chemical compound. This quantitatively different reaction to the drug, associated with individual sensitivity, is due to abnormalities of the drug metabolism in the body.

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19
Q

Pregnancy and epilepsy

A

● Monotherapy with lowest effective dose.
● Valproate therapies are not recommended. (The safest seem to be levetiracetam and
lamotrigine.)

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20
Q

Benzodiazepines Antidote

A

flumazenil

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21
Q

Benzodiazepines EXAMPLES

A

Diazepam (long lasting)
Lorazepam (short lasting)
Clonazepam

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22
Q

Diazepam (long lasting)

A

● available for rectal administration to avoid or interrupt prolonged generalized tonic–clonic seizures or clusters when oral administration is not possible

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23
Q

clonazepam

A

● may be prescribed as adjunctive therapy for particular types of seizures

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24
Q

Benzodiazepines

MOA:

A

● Benzodiazepines bind to GABA inhibitory receptors to reduce the firing rate.
● Enhance GABA receptor responses

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25
Q

Benzodiazepines

USES

A

● Status epilepticus (Diazepam, Lorazepam)
● Absence and myoclonic seizures (clonazepam)
● Infantile spasms (clonazepam)

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26
Q

Benzodiazepines

SIDE EFFECT

A

● Sedation

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27
Q

What type of drug is carbamazepine?

A

A Tricyclic

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28
Q

Carbamazepine

MOA

A

● blocks sodium channels, thereby possibly inhibiting the generation of repetitive action potentials in the epileptic focus and preventing spread.
● Decreases glutamate release

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29
Q

Carbamazepine

USES

A 
● treatment of focal seizures
● generalized tonic–clonic seizures
● trigeminal neuralgia
● bipolar disorder
● Partial seizures
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30
Q

Carbamazepine

Side Effects

A 
● Hyponatremia
● Ataxia
● Diplopia
● Headache
● Nausea
● Weight gain
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31
Q

Carbamazepine

Contraindication:

A

● absence seizures (because it may cause an increase in seizures)

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32
Q

What type of drug is phenytoin?

A

A Cyclic ureides

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33
Q

Phenytoin

MOA

A

● Blocks voltage gated Na channels
● blocks voltage-gated sodium channels by selectively binding to the channel in the
inactive state and slowing its rate of recovery

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34
Q

Phenytoin

USES

A

Generalised tonic-clonic and partial seizures

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35
Q

Phenytoin

SIDE EFFECTS

A 
● Ataxia
● Diplopia
● Gingival hyperplasia
● Hirsutism
● Neuropathy
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36
Q

What type of drug is Phenobarbital

A

Cyclic ureides

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37
Q

Phenobarbital

MOA

A

Enhances GABA receptor responses

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38
Q

Phenobarbital

Therapeutic uses

A

Generalised tonic-clonic and partial seizures

39
Q

Phenobarbital

SIDE EFFECTS

A

● Ataxia

● Sedation

40
Q

What type of drug is Ethosuximide:

A

cyclic ureide.

41
Q

Ethosuximide MOA

A

● Decreases calcium ion current (t-type)
● reduces propagation of abnormal electrical activity in the brain, most likely by inhibiting
T-type calcium channels

42
Q

Ethosuximide USES

A

● Absence seizures

43
Q

Ethosuximide: SIDE EFFECTS

A

● GI distress
● Dizziness
● Headache

44
Q

What is Gabapentin:

A

● analog of GABA

45
Q

Gabapentin: MOA

A

● Blocks calcium ion channels
● gabapentin binds to the α2δ(alpha 2 delta) subunit of voltage-gated calcium channels
● Blocks gaba-t

46
Q

Gabapentin: USES

A

● Generalised tonic-clonic and partial seizures
● adjunct therapy for focal seizures
● treatment of postherpetic neuralgia
● good choice for the older patient (there are few drug interactions)

47
Q

Gabapentin: SIDE EFFECTS

A

● Ataxia
● Dizziness
● Somnolence
● Weight gain

48
Q

Gabapentin: CONTRAINDICATIONS

A

● Renal patients

49
Q

What type of drug is Pregabalin

A

GABA DERVIVATIVE

50
Q

Pregabalin

MOA

A

● Blocks calcium ion channels
● gabapentin binds to the α2δ(alpha 2 delta) subunit of voltage-gated calcium channels
● inhibiting excitatory neurotransmitter release

51
Q

Pregabalin

USES

A

● Partial seizures
● diabetic peripheral neuropathy
● postherpetic neuralgia
● fibromyalgia

52
Q

Pregabalin: SIDE EFECTS

A

● Ataxia
● Dizziness
● Somnolence
● Weight gain

53
Q

Pregabalin: CONTRAINDICATION

A

● Renal dysfunction

54
Q

Pregabalin: CONTRAINDICATION

A

● Renal dysfunction

55
Q

Vigabatrin

MOA

A

● irreversible inhibitor of GABA-Transaminase

56
Q

Vigabatrin

USE

A

● Partial seizures

57
Q

Vigabatrin: SIDE EFFECTS

A

● Drowsiness
● Dizziness
● Psychosis
● Ocular effects

58
Q

Lacosamide

MOA:

A

● Blocks Na channels
● resulting in stabilization of hyperexcitable neuronal membranes and inhibition of
repetitive neuronal firing

59
Q

Lacosamide

Therapeutic uses:

A

● Focal seizures

● Generalised seizures

60
Q

Lacosamide

Adverse effects:

A

● Dizziness ● Headache ● Diplopia

● Fatigue

61
Q

Lamotrigine

MOA

A

● Blocks sodium and calcium channels

● Decreases neuronal glutamate release

62
Q

Lamotrigine

Therapeutic uses:

A 
● Generalised tonic-clonic seizures
● Partial seizures
● Myoclonic seizures
● Absence seizures
● Lennox-Gastaut syndrome
● bipolar disorder
● Preganacy
63
Q

Lamotrigine

Adverse effects:

A

● Dizziness ● Headache ● Diplopia

● Rash

64
Q

Levetiracetam

MOA:

A

● Binds to synaptic protein SV2A
● Modifies gaba and glutamate release
● Blocks calcium channels

65
Q

Levetiracetam

Therapeutic uses:

A 
● Generalised tonic-clonic seizures
● Partial seizures
● Focal-onset seizures,
● Myoclonic seizures
● Pregnancy
66
Q

Levetiracetam

Adverse effects:

A 
● Dizziness
● Nervousness
● Depression
● Seizures
● mood alterations
● Psychomotor anxiety
67
Q

Perampanel

MOA:

A

● Blocks glutamate AMPA receptors

68
Q

Perampanel

A

● Focal seizures

● Generalised tonic-clonic seizures

69
Q

Perampanel

Adverse effects:

A 
● Dizziness
● Headache
● Somnolence
● Behavioral changes
● serious psychiatric
● behavioral reactions
● Aggression
● Hostility
● Irritability
● Anger
● homicidal ideation.
70
Q

Rufinamide

MOA:

A

● Blocks Na channels

71
Q

Rufinamide

Therapeutic uses:

A

● Lennox-gastaut syndrome

● Focal seizures

72
Q

Rufinamide

Adverse effects:

A

● Somnolence
● Diarrhea
● Fever
● shortened QT intervals

73
Q

Rufinamide

CONTRAINDICATIONS

A

Familial shortened QT interval

74
Q

Tiagabine

MOA:

A

● Blocks GABA reuptake
● blocks GABA uptake into presynaptic neurons permitting more GABA to be available for
receptor binding and thereby enhancing inhibitory activity

75
Q

Tiagabine

Therapeutic uses

A

● Partial seizures

● focal seizures

76
Q

Tiagabine

Adverse effects:

A

● Dizziness
● Nervousness
● Depression
● Seizures

77
Q

Tiagabine

CONTRAINDICATIONS

A

● should not be used for indications other than epilepsy

78
Q

Topiramate

MOA:

A

● Increase GABA effect
● blocks voltage-dependent sodium channels
● reduces high-voltage calcium currents (L type)
● carbonic anhydrase inhibitor

79
Q

Topiramate

Therapeutic uses:

A 
● Generalised tonic-clonic seizures
● Absence seizures
● Partial seizures
● Migraine
● focal and primary generalized epilepsy
80
Q

Topiramate

Adverse effects:

A 
● Sleepiness
● Cognitive slowing
● Confusion
● Paresthesias
● weight loss
● Renal stones
● Glaucoma
● oligohidrosis (decreased sweating)
● Hyperthermia
● Articulation disorder
● Anorexia nervosa
81
Q

Valproate

MOA:

A

● Blocks high frequency firing

● Blocks Na channels

82
Q

Valproate

Therapeutic uses:

A

● Generalised tonic-clonic seizures
● Partial seizures
● Myoclonic seizures

83
Q

Valproate

Adverse effects:

A

● Nausea
● Alopecia
● Weight gain
● Teratogenic

84
Q

Valproate CONTRAINDICATION

A

● Pregnancy

85
Q

Zonisamide

MOA:

A

● Blocks sodium channels and T-type calcium currents

86
Q

Zonisamide

USES

A

● Generalised tonic-clonic seizures
● Partial seizures
● Myoclonic seizures
● focal epilepsy

87
Q

Zonisamide

Adverse effects:

A 
● Sleepiness
● Cognitive slowing
● Poor concentration
● Paresthesias
● kidney stones
● Oligohidrosis
88
Q

Zonisamide

CONTRAINDICATION

A

sulfonamide or carbonic anhydrase inhibitor hypersensitivity

89
Q

Retigabine

A

● It affects the opening of potassium channels.
● Recommended as an additional drug.
● Low antiepileptic potential.

90
Q

Retigabine

MOA

A

● Activates potassium channels

91
Q

Retigabine

Therapeutic uses:

A

● Focal seizures

92
Q

Retigabine

Adverse effects:

A

● Dizziness
● Somnolence
● Retinal changes

93
Q

Felbamate

A

● It probably reacts with NMDA.
● Used to treat Lennox-Gastaut type of childhood epilepsy.
● Transaminases monitoring.

Pharmacology (22 decks)

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