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Pharmacology > Anti-epileptics > Flashcards

Anti-epileptics Flashcards

(41 cards)

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1
Q

Epilepsy

A

Chronic disorder of recurrent seizures

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2
Q

Seizures

A

Finite episodes of brain dysfunction resulting from abnormal discharge of cerebral neurons

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3
Q

Classification of Seizures

A
  1. Partial seizures
    - Simple partial seizures
    - Complex partial seizures
    - Partial w/ secondary generalized tonic-clonic seizures
  2. Generalized seizures
    - Tonic-clonic seizures
    - Absence seizures
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4
Q

Simple partial seizures

A
  • NO loss of consciousness

- Abnormal activity of 1 limb or muscle group

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5
Q

Complex partial

A
  • Loss of consciousness

- Motor dysfunction- chewing, movements, diarrhea & urination

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6
Q

Partial w. Secondary Generalized Tonic-Clonic Seizure

A

Partial seizure –> Tonic-clonic seizure

- Loss of consciousness

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7
Q

Generalized

A
  • IMMEDIATE loss of consciousness

- Convulsive or non-convulsive

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8
Q

Generalized Tonic-clonic

A
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9
Q

Absent seizures (Petit mal)

A
  • Brief & abrupt self-limiting loss of consciousness
  • Stares & has rapid eye-blinking
  • Usually children
  • 3Hz spike & wave pattern emerges abruptly & ceases after a few seconds on EEG
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10
Q

Other Generalized seizures

A
  • Atonic
  • Tonic
  • Clonic
  • Myoclonic
  • Febrile
  • Status epilepticus
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11
Q

Mechanism of seizures

A

Dec inhibitory synaptic activity (GABA) OR Inc excitatory activity (Glutamate)

  • GABAa antagonist & Glutamate agonist triggers seizures
  • Glutamate receptor antagonists & drugs that enhance GABAergic transmission inhibits seizure
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12
Q

MOA of Antiepileptic drugs

A
  1. Block Voltage-gated Ion Channels
    - Na+ channels
    - T-type Ca2+ channels
  2. Modulate Synaptic Transmission
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13
Q

Drugs that block Na+ channels

A
  • Phenytoin
  • Carbamazepine
  • Lamotrigine
  • Zonisamide
  • Oxcarbazepine

(May contribute to the effects of Phenobarbital, Valproate & Topiramate)

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14
Q

Drugs that block T-type Ca2+ channels

A
  • Ethosuximide
  • Valproate

Used for absent seizures (oscillatory neuronal activity between thalamus & cortex)

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15
Q

Drugs that enhance GABAergic transmission post-synaptically

A
  • Benzos
  • Barbiturates
  • Topiramate

Direct action on GABA receptors

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16
Q

Drugs that enhance GABAergic transmission pre-synaptically

A
  1. Tiagabine - Inhibits GABA reuptake

2. Vigabatrin - Inhibits GABA aminotransferase

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17
Q

Drugs that Reduce Glutamatergic Neurotransmission Post-synaptically

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A
  • Phenobarbital
  • Topiramate

Blocks Glutamate receptors

18
Q

Drugs that Reduce Glutamatergic Neurotransmission Pre-synaptically

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A
  • Gabapentin
  • Pregabalin
    Dec Glutamate release by blocking presynaptic voltage-gated Ca2+ channels
  • Levetiracetam
    Binds to Synaptic Vesicle Glycoprotein 2A (SV2A) –> Release of Glutamate & GABA
19
Q

Tonic-clonic seizure management

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A
  • Carbamazepine
  • Oxcarbazepine
  • Valproate
  • Lamotrigine
  • Phenytoin
  • Topiramate
20
Q

Absent seizure management

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A

Ethosuximide & Valproate (DOC)

  • If tonic-clonic is present use Valproate as DOC
  • Atypical absent seizure - Valproate

Lamotrigine also effective

21
Q

Myoclonic seizure management

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A

Valproate (DOC)
Topiramate
Levetiracetam - Adjunctive therapy

22
Q

Atonic seizure management

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A

Refractory to all drugs

- Valproate & Lamotrigine may be effective

23
Q

Febrile Convulsions management

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A

Seizure <15 minutes = Supportive treatment

Seizure > 15 minutes = Diazepam (IV or Rectal)

24
Q

Status Epilepticus

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A
  1. Single seizure lasting >5 minutes
    OR
  2. 2 or more seizures w/o recovery of consciousness
  • Convulsive or non-convulsive
  • Usually generalized tonic-clonic seizures
25
Status Epilepticus Management
Initial therapy 5-20 mins - Midazolam (IM) OR Lorazepam OR Diazepam (IV) Second therapy 20-40 mins - (IV) Fosphenytoin OR Valproic acid OR Levetiracetam - 2nd line = IV Phenobarbital Third therapy 40+ mins - Repeat 2nd therapy OR - IV Thiopental, Midazolam, Phenobarbital OR Propofol
26
Drug-induced seizure management in non-epileptics pts
- Diazepam - Lorazepam - Phenobarbital
27
Drugs that induce Cytochrome P450
- Carbamazepine - Phenobarbital - Phenytoin - Oxcarbazepine (weak)
28
Adverse effects of valproate
- Hepatotoxicity NB: It inhibits Cytochrome P450, metabolism of other drugs and itself
29
Adverse effects of Phenytoin
- Diplopia & ataxia - Gingival hyperplasia - Coarsening of facial features in children - Hirsutism - Rash (SJS) NOT given to children due to AE NB: Zero order kinetics of elimination
30
Adverse effects of Carbamazepine
- Aplastic anemia - Agranulocytosis - Rash (SJS)
31
Stevens- Johnson Syndrome & Toxic Epidermal Necrolysis (SJS/TEN)
- Phenytoin, Lamotrigine & Carbamazepine Discontinues at the 1st sign of rash when using Lamotrigine & Carbamazepine because of Black box warnings
32
Adverse effects of Phenobarbital
- Sedation & drowsiness - Tolerance & Dependence - Cognitive impairment - Hyperactivity - Rash (SJS) P450 inducer
33
Adverse effects of Primidone
Similar to its metabolite (phenobarbital) - Sedation & drowsiness - Tolerance & Dependence - Cognitive impairment - Hyperactivity - Rash (SJS) P450 inducer
34
Adverse effects of Vigabatrin
Visual field loss
35
Adverse effects of Felbamate
- Aplastic anemia - Hepatotoxicity USED for refractory epilepsy
36
Discontinuation of Anti-epileptic therapy
- 3-5 years seizure free Discontinuation should be slow and withdrawn gradually to avoid withdrawal seizures. If the pt. is on combination therapy, withdraw drugs one at a time
37
Overdose
Rarely lethal - Barbiturates may cause Resp. depression - Treatment is supportive Do NOT use Stimulants
38
Which drugs is Teratogenic
Valproate most risk of congenital malformation in infants NB: Folic acid dec. incidence of Neural tube defects but does not prevent it
39
Newborn Hemorrhagic Disease
Enzyme-inducing drugs that inc. Vit. K degradation in fetus --> Bleeding in fetus Vit. K supplement is recommended for mother in the final month of pregnancy
40
Other uses Of Anti-epileptic drugs
1. Carbamazepine = Neuropathic pain & bipolar 2. Gabapentin = Neuropathic pain 3. Lamotrigine = Bipolar Disorder 4. Pregabalin = Neuropathic pain 5. Topiramate = Migraine 6. Valproate = Bipolar disorder & Migraine 7. Primidone = DOC for essential tremor along with Propranolol
41
Non-pharmacologic approaches to Epilepsy
1. Surgery- resection of local area of brain 2. Ketogenic diet - 4:1:1 fat: protein: carbohydrate 3. Vagus nerve stimulation - stimulation of left vagus with implanted pace-maker-like device

Pharmacology (16 decks)

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