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pharmacology year 3.1 > anti-epileptic drugs > Flashcards

anti-epileptic drugs Flashcards

1
Q

what is meant by seizure?

A

abnormal, excessive excitation and synchronization of a population of cortical neurons

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2
Q

what is meant by epilepsy?

A

recurrent seizures unprovoked by any immediately identifiable cause

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3
Q

what can triggers seizure?

A
  • photic stimuli
  • sleep deprivation
  • infection, fever
  • trauma
  • drug that decrease seizure threshold
  • drug withdrawal
  • alcohol withdrawal
  • metabolic/ endocrine
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4
Q

the classification of seizure

A
  1. generalized seizure
  2. focal/ partial seizure
  3. unknown
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5
Q

what is generalize seizure?

A

originating at some point within and rapidly engaging bilaterally distributed networks

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6
Q

definition of focal/ partial seizure

A

originating in networks limited to one hemisphere

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7
Q

complications of partial seizure

A
  • impaired consciousness
  • ictal automatisms (automatic seizure)
  • abnormal behavior
  • confusion
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8
Q

characteristics of generalized seizure

A
  • immediated synchronous spike and wave discharge
  • involve both hemispheres
  • involve reticular activating system
  • immediate loss of consciousness
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9
Q

types of generalized seizure

A
  • tonic
  • clonic
  • tonic-clonic
  • myoclonic
  • atonic
  • absence
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10
Q

function of sodium channel blockers

A
  • block the excitation of cells that are firing repetitively

- the higher the frequency of firing, the greater the block

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11
Q

characteristics of phenytoin (PHT)

A
  • oral slow
  • 90% protein bound
  • enzyme inducer
  • zero order kinetic
  • steep dose-concentration relationship
  • most problematic drug interactions
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12
Q

function of phenytoin (PHT)

A
  • given IV
  • given once daily
  • can measure drug level
  • DO NOT use in absence seizure
  • used in PARTIAL + GENERALIZED seizures
  • used in status epilepticus
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13
Q

side effects of phenytoin (PHT)

A
  • cardiac and respi depress
  • malabsorption
  • osteoporosis
  • hepatitis
  • hirsutism
  • gum hyperplasia
  • mentation
  • teratogenic
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14
Q

what is fosphenytoin?

A
  • prodrug for phenytoin
  • given IV
  • infused 3 times faster then PHT
  • used in status epilepticus
  • cardiodepressant
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15
Q

characteristics of carbamazepine

A
  • given PO
  • Na+ channel blocker
  • half life 15-30 hours
  • 80% protein bound
  • NO IV
  • enzyme inducer
  • can measure drug levels
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16
Q

function of carbamazepine

A
  • treat depression
  • treat neuropathic pain
  • treat partial and secondary generalized seizures
  • no ABSENCE and MYOCLONIC
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17
Q

side effects of carbamazepine

A
  • hepatitis
  • hypersensitivity
  • hyponatremia
  • haematologic
  • skin reaction
  • dysrhythmias
  • dizzy, ataxia
  • steven johnson syndrome
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18
Q

characteristics of oxcarbazepine

A
  • Na+ channel blocker
  • less induction
  • oral half life 8 hours
  • 40% protein binding
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19
Q

functions of oxcarbazepine

A
  • used in partial seizure

- used in secondary generalized seizure

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20
Q

side effects of oxcarbazepine

A
  • somnolence
  • increase weight
  • dizzy, ataxia
  • headache
  • hyponatremia
  • alopecia (loss of hair)
  • rash
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21
Q

characteristics of lamotrigine

A
  • Na+ channel and Ca+ channel blocker
  • may make myoclonic WORSE
  • oral ONLY
  • good in elderly
  • not an inducer
  • 55% protein binding
  • hepatic metabolism
  • dose varies
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22
Q

functions of lamotrigine (LTG)

A
  • treat most seizure types
  • used in depression
  • neuropathic pain
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23
Q

side effects of lamotrigine (LTG)

A
  • AED hypersensitivity syndrome
  • rash, FUO, influenza
  • drowsy, headache, irritable
  • diplopia, ataxia, dizzy, tremor
  • haematologic
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24
Q

what is GABA?

A
  • major inhibitory neurotransmitter
  • cause Cl influx
  • hyperpolarisation
25
Q

type of GABA A receptor

A
  • benzodiazepine
  • barbiturates
  • clobazam
  • clonazepam
26
Q

list of GABA drugs that used in first line in treating epilepsy

A
  • gabapentin
  • pregabalin
  • valproate
27
Q

examples of drugs benzodiazepines

A
  • diazepam
  • clonazepam
  • lorazepam
  • midazolam (converted into neurosteroids)
28
Q

uses of benzodiazepines

A
  • sedation
  • muscle relaxant
  • anticonvulsants
  • alcohol withdrawal
  • given PO the best and IV if status epilepticus
29
Q

characteristics of benzodiazepines

A
  • 7 aromatic ring
  • lipid soluble
  • high therapeutic index
30
Q

side effects of benzodiazepines

A
  • decrease in motor skills
  • ataxia, fracture
  • vertigo
  • excitement
  • amnesia (partial/total loss of memory)
  • drowsiness
31
Q

main use of phenobarbitone and example of drug

A
  • in status epilepticus through IV

- eg: primidone

32
Q

side effects of phenobarbitone

A
  • inducer
  • sedation
  • ataxia
  • respiratory depression
  • rash
  • malabsorption
  • anemia
33
Q

characteristics of valproate

A
  • Na+ channel blocker
  • Ca+ channel blocker
  • usually given PO
  • half life 15 hours
  • bad for preggy mother
34
Q

functions of valproate

A
  • inhibits most seizures
  • increase GABA
  • used in depression
  • used in migraine
35
Q

side effects of valproate

A
  • hepatitis
  • pancreatitis
  • alopecia
  • weight gain
  • sedation
  • ataxia
  • tremor
  • increase ammonia
36
Q

function of gabapentin

A
  • decrease calcium influx
  • treat partial seizure
  • neuropathic pain
  • no interaction
37
Q

side effects of gabapentin

A
  • behaviour
  • cerebellar
  • rhinitis
  • pancreatitis
  • rash
  • joints
  • alopecia
38
Q

function of pregabalin

A
  • decrease calcium influx
  • partial seizures
  • neuropathic pain
  • anxiolytic
39
Q

side effects of pregabalin

A
  • ataxia
  • sleepiness
  • weight gain
  • sexual dysfunction
  • vision problem
40
Q

examples of calcium channel and what type of seizure?

A
  • ethosuximide (ETX)
  • zonisamide (ZNS)
  • treat ABSENCE epilepsy
41
Q

side effects of ethosuximide (ETX)

A
  • ANV (anticipatory nausea and vomiting)
  • dizziness
  • sleep
  • haematologic
  • behavioural
42
Q

characteristics of zonisamide (ZNS)

A
  • non-inducer
  • no interactions
  • once daily
  • 50% protein binding
  • ## half life 60 hours
43
Q

functions of zonisamide (ZNS)

A
  • acts at Na+ and at T-type Ca channel
  • inhibits carbonic anhydrase
  • as add-on therapy for partial, myoclonic and absence seizures
44
Q

side effects of zonisemide (ZNS)

A
  • PSYCHOSIS
  • TERATOGEN
  • coma, somnolence
  • stones
  • oligohidrosis (absence of sweating)
  • speech, cerebellar
45
Q

5 binding sites for glutamate

A
  1. NMDA
  2. AMPA
  3. KAINATE
  4. glycine
  5. glu A subunits
46
Q

postsynaptic blocker for glutamate

A 
AMPA blocker
- phenobarbitone
- topiramate
- lamotrigine
NMDA
- felbamate
47
Q

functions of topiramate (TPM)

A
  • inhibits Na and Ca ion channels
  • enhance K+ current
  • used for migraine
  • used for partial and generalized seizures
  • treat lennox gastaut
  • treat obesity
  • treat psychiatric disorder
48
Q

side effects of topiramate (TPM)

A
  • cognitive- verbal fluency
  • dizzy, ataxia
  • paresthesia
  • agitation
  • acidosis
  • hyperthermia
  • nephrolithiasis (kidney stones)
  • weight loss
49
Q

functions of levetiracetam (most ideal AED drug)

A
  • first line in partial and second in generalized seizure
  • alter Ca+ entry
  • regulates vesicular exocytosis
  • no metabolites
  • half life 6-8 hours
50
Q

side effects of levetiracetam

A
  • SUICIDE
  • somnolence
  • dizzy, ataxia, tremor
  • psychosis
  • cough
  • rash
  • ANV
  • haematological
51
Q

functions of lacosamide

A
  • enhances slow inactivation of voltage gated Na+ channels
  • inhibiting neuropathic factors
  • as add on therapy for treating partial seizures
52
Q

side effects of lacosamide

A
  • cerebellar
  • prolongs PR interval
  • headache, drowsiness
  • tremor
  • suicide
53
Q

functions of ezogabine (EZB)

A
  • add on treatment for partial seizures
  • promotes opening of voltage K+ channels
  • inhibits high frequency AP firing
54
Q

side effects of ezogabine (EZB)

A
  • urinary retention
  • suicide
  • ataxia, dizzy
  • somnolence
  • QT prolong
  • blue nails and retina pigment
55
Q

functions of perampanel

A
  • adjunctive therapy for partial seizure

- highly selective and non-competitive AMPA antagonist

56
Q

side effects of perampanel

A
  • psychiatric
  • behavioural
  • dizziness
  • somnolence
57
Q

definition of status epilepticus

A

more than 10 mins of continuous seizure OR 2 or more recurrent seizure without recovery cause by thymine deficiency

58
Q

medication for status epilepticus

A
  • diazepam (rectal)
  • midazolam
  • lorazepam (IV)
  • phenytoin
  • propofol (IV) (local anas)

pharmacology year 3.1 (8 decks)

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