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Pharmacology > Anticonvulsants > Flashcards

Anticonvulsants Flashcards

1
Q

Epilepsy?

A

a chronic brain disorder characterised by recurrent unprovoked seizures

Abnormal electrical discharges: loss of consciousness, abnormal
movements, odd behaviour, distorted perceptions

  • Origin of abnormal firing determines symptoms
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2
Q

Generalised seizures?

A

aberrant electrical discharge diffusely
involves the entire cortex of both hemispheres from the onset,
consciousness in usually lost
result most often from metabolic disorders and sometimes
from genetic disorders.
include infantile spasms, absence seizures, tonic-clonic
seizures, atonic seizures, myoclonic seizures.

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3
Q

Focal (Partial) seizures?

A

excess neuronal discharge occurs in
one cerebral cortex
most often results from structural abnormalities.
may be simple (no impairment of consciousness) or complex
(↓ but not complete loss of consciousness).
may be followed by a generalised seizure.
Seizures may be preceded by an aura - may consists of
sensory, autonomic or psychic sensations; most seizures end
spontaneously in 1 to 2 min

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4
Q

Status epilepticus?

A

involves at least one of the following:
‣tonic-clonic seizure activity lasting > 5 to 10 min
‣≥ 2 seizures between which patients do not fully regain
consciousness.

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5
Q

Epilepsy treatment goals?

A

Treatment Goals
Keep patients free of seizures without dose-dependent
toxicity phenomena

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6
Q

Monotherapy?

A

f possible, it is better to treat a patient
with only one anticonvulsant
* If fits are not controlled with the max dose of a drug,
replace it with another; withdraw old drug in gradually
decreasing doses while introducing the new drug.

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7
Q

What causes epilepticus?

A

The abrupt withdrawal of these drugs may cause status
epilepticus.

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8
Q

Anti-Epileptic drugs and cure of epilepsy ?

A

Do not cure epilepsy; they control the seizures and usually
have to be taken for life.
‣The choice of drug is made on the acceptability of side
effects and how the number of doses influences lifestyle

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9
Q

Phenytoin MOA?

A

blocks voltage-gated sodium channels

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10
Q

Phenytoin I?

A

focal and generalised tonic-clonic seizures (all forms of
epilepsy except absence seizures), status epilepticus.

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11
Q

Phenytoin A/E?

A

PHENYTOIN

P-450 drug Interactions
Hirsutism
Enlarged Gums(Ginigival Hyperplasia)
Nystagmus
Yellow discolouration of skin
Tetratogenic
Osteomalacia
Interfere with folTE/B12 Absorption
Neuropathies:vertigo and ataxia

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12
Q

Carbamazepine MOA?

A

blocks sodium channels → inhibit the generation of
repetitive action potentials in epileptic focus and prevents their
spread

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13
Q

Carbamazepine CI?

A

Abscence Seizure, Mixed and Myoclonic Seizure

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14
Q

Carbamazepine I?

A

First line monotherapy for generalised tonic-clonic and partial
seizures (focal); Other: trigeminal neuralgia, bipolar disorder

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15
Q

Carbamazepine DI?

A
  1. induces hepatic enzymes; increases the toxicity of MAOIs (tranylcypromine) by an unknown mechanism;
    discontinue MAOI use 14 d before starting carbamazepine
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16
Q

Carbamazepine A/E?

A

ataxia, dizziness, sedation; N, V; rashes including SJS,
jaundice, dry mouth, aplastic anaemia, leukopenia,
hyponatraemia (esp. in elderly)

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17
Q

Lamotrigine MOA?

A

Blocks sodium channels and HV-dependent calcium
channels

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18
Q

Lamotrigine S/E?

A

Ataxia, dizziness, blurred vision, rash.

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19
Q

Lamotrigine Dosage?

A

slow up-titration of dose essential to minimise risk of
serious and life-threatening skin reactions (Stevens-Johnson
syndrome)

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20
Q

Topiramate MOA?

A
  • Blocks voltage-dependent sodium channels
  • Reduce high-voltage calcium currents
  • Targets glutamate (NMDA) sites
21
Q

Topiramate I?

A

partial and primary generalised seizures (other: migraine
headache, obesity)

22
Q

Topiramate A/E?

A

drowsiness, fatigue, weight loss, nervousness, renal stones,
glaucoma, hyperthermia, paraesthesia

23
Q

Gabapentini MOA?

A

an analogue of GABA (no effects on GABA receptors)

24
Q

Gabapentini I?

A

focal seizures (other: post-herpetic neuralgia)

25
Q

Gabapentini Dose?

A

dose adjustment in renal disease is required
(well tolerated by the elderly population with partial seizures, with
fewer drug interactions)

26
Q

Gabapentini A/E?

A

fatigue, dizziness, drowsiness, ataxia

27
Q

Vigabatrin MOA?

A

irreversibly inhibits ꝩ-aminobutyric acid transaminase
(GABA-T) enzyme (enzyme responsible for metabolism of
GABA)

28
Q

Vigabatrin I?

A

FOR INFANTS

infantile spasms (west syndrome)

29
Q

Vigabatrin A/E?

A

dizziness, drowsiness, weight gain, mental confusion,
psychosis

30
Q

Pregabalin
MOA?

A

binds to auxiliary subunit of voltage-gated calcium
channels

31
Q

Pregabalin I?

A

dosage adjustments needed in renal disease

32
Q

Pregabalin A/E?

A

weight gain, impaired memory, peripheral oedema

33
Q

Levetiracetam
MOA?

A

High affinity for a synaptic vesicle protein (SV2A)

34
Q

Levetiracetam I?

A

focal, myoclonic, generalised tonic-clonic seizures (other:
perioperative neurosurgery)

35
Q

Levetiracetam A/E?

A

mood alterations, ataxia, somnolence, dizziness, agitation

36
Q

Ethosuximide
MOA?

A

Inhibits T-type calcium channels → reduced propagation
of abnormal electrical activity in the brain
I: first line monotherapy for typical absence seizures

37
Q

Valproic acid
MOA

A

Blockade of sodium channel
*Blockade of GABA transaminase
*Blockade of T-type calcium channels

38
Q

Ethosuximide A/E?

A

nausea, vomiting, headache, sedation, ataxia, dizziness,
euphoria, git disturbances (gastric pain), skin rashes (e.g. SJS),
bone marrow suppression.

39
Q

Valproic I?

A

focal, and primary generalised seizures; all forms of epilepsy,
first choice for patient on ART

40
Q

Valproic Dose?

A

valproic acid 500 mg po bd, max 2500 mg daily

41
Q

Valproic A/E?

A

N, anorexia/↑appetite, ataxia, sedation, hepatotoxicity,
alopecia and thrombocytopenia, teratogenicity

42
Q

Benzodiazepines that treat Anticonvulsants?

A

Clonazepam, clobazam, diazepam

43
Q

Benzodiazepines MOA?

A

bind to GABA inhibitory receptors to reduce firing rate

44
Q

Benzodiazepines I?

A

reserved for emergencies or seizure attacks

45
Q

Adjunctive therapy for particular types of seizures?

A

Clonazepam andclobazam

46
Q

Diazepam Admin in children?

A

Available for rectal admin. (children)

47
Q

Diazepam Fxn?

A

To avoid or interrupt prolonged generalised tonic-clonic
seizures

48
Q

Choice of Antiepileptic drug treatment:
should be based on?

A

*Classification of the seizures
*Patient-specific variables (age, co-morbidities, lifestyle,
etc.)
*Drug characteristics (drug interactions, cost, etc.)

Pharmacology (44 decks)

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