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Drugs And The Brain > anticonvulsants > Flashcards

anticonvulsants Flashcards

1
Q

focal seizures treatment

A

first line: carbamazepine, lamotrigine

second line: oxcarbazepine, valproate, levetiracetam

adjunct: combinations + gabapentin, topiramate

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2
Q

tonic clonic seizures treatment

A

first line: valproate (not WCBA), lamotrigine

second line: carbamazepine, oxcarbazepine

adjunct: combinations + levetiracetam, topiramate, clobazam

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3
Q

absence seizure treatment

A

first line: valproate (not WBCA), ethosuximide

second line: lamotrigine

adjunct: combinations + specialist advice

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4
Q

WCBA

A

women who are of child bearing age

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5
Q

mechanisms of anticonvulsants

A

calcium channel inhibition
GABAergic potentiation
-receptor potentiation
-uptake inhibition
-metabolism inhibition
sodium channel inhibition

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6
Q

phenytoin

A

stabilises voltage-gated sodium channels in inactivated state

effective against tonic clonic and partial seizures

can worsen absence and myoclonic seizures

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7
Q

phenytoin side effects

A

teratogenic
increased lupus risk
cerebellar atrophy
acne, hirsuitism
gingival overgrowth

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8
Q

gingival overgrowth

A

gums start to grow

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9
Q

carbamazepine mechanism

A

blocks voltage-gated sodium channels

may have secondary actions on GABA A receptors

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10
Q

uses of carbamazepine

A

focal seizures
useful for tonic-clonic seizures
mood stabiliser
to treat neuropathic pain

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11
Q

drugs related to carbamazepine

A

oxcarbazepine and eslicarbazepine

similar mechanisms, better side effect profile, fewer interactions

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12
Q

carbamazepine pharmacokinetics

A

auto-induces CYP3A4

-CYP3A4 metabolises carbamazepine so as people take more of the drug they produce more of this enzyme
-can take a while for the drug to reach a plateau

-means other drugs will be metabolised much more quickly, so must be careful with drug interactions

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13
Q

what inhibits enzyme CYP3A4

A

a component of grapefruit juice

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14
Q

side effects of carbamazepine

A

teratogenic
risk of lupus
worsens JME, absence seizures
cognitive problems
mood changes
psychosis in some people

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15
Q

mechanism of lamotrigine

A

sodium channel blocker

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16
Q

uses of lamotrigine

A

first line tonic clonic
second line absence
(can make myoclonic seizures worse at higher doses)
mood stabiliser- bipolar
can be asses to antipsychotic drugs for the treatment of schizophrenia

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17
Q

side effects of lamotrigine

A

not as bad as carbamazepine and phenytoin

sedation
sleep disturbances
rash
binds to eye pigment
steven-Johnsons syndrome (rare)

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18
Q

mechanism of benzodiazepines

A

potentiate actions of GABA A receptors by binding to allosteric sites on the receptor

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19
Q

clobazam

A

adjunct meditation
also used to treat anxiety
benzodiazepine

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20
Q

clonazepam

A

treat refractory epilepsy
benzodiazepine
also acts on calcium channels
only prescribed by specialists/ only on types of epilepsy not treatable by other drugs

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21
Q

diazepam

A

only really used for status epilepticus

acute serious situations, long term use = dependence

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22
Q

benzodiazepine side effects

A

sedation
tolerance and dependence build up very quickly
some cases: seizures on withdrawal

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23
Q

barbiturates as anticonvulsants

A

allosteric potentiators of GABA A receptors

side effects far worse, can directly activate the receptor making them dangerous in overdose

only prescribed by a specialist in difficulty situations

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24
Q

tiagabine mechanism

A

GAT1 inhibitor - increases the synaptic concentration of GABA as it cannot be taken up into the presynaptic nerve terminal

increasing inhibitory signals

25
what is tiagabine used for?
adjunct medication for focal seizures panic attacks? neuropathic pain?
26
tiagabine side effects
sedation dizziness paraesthesia provokes seizures in non epileptic patients
27
tiagabine overdose
very sedating causes seizures, amnesia and confusion
28
Vigabatrin mechanism
irreversible GABA transaminase inhibitor (short half life doesn't matter as it will covalently modify enzyme) increases presynaptic GABA concentration by stopping metabolism of GABA to SSA
29
uses of vigabatrin
adjunct medication addictions? panic attacks?
30
vigabatrin side effects
visual disturbances depression psychosis sedation teratogenic actions?
31
three forms of sodium valproate
sodium valproate, valproic acid and valproate semisodium (mixture of the two)
32
mechanism of sodium valproate
unclear most likely GABA transaminase inhibitor (increasing GABA synthesis) enhance post synaptic GABA function? inhibit sodium channels? inhibit calcium channels?
33
uses of sodium valporate
treat epilepsy treat bipolar disorder treat migraines sometimes add on treatment for schizophrenia
34
side effects of valproate
Liver toxicity (can be sudden onset) Teratogenic Cognitive changes/brain structure changes with long term use (debatable/?reversible when drug is withdrawn ).
35
what teratogenic side effects are associated with valproate?
Increased risk of: anencephaly, spina bifida (20 fold increased risk), autistic spectrum disorders, cleft palate, limb defects + many others...
36
presentation of foetal valproate syndrome
high forehead flat nasal bridge broad base of nose shallow philtrum long upper lip
37
gabapentinoids
gabapentin and pregablin
38
believed action of gabapentin and pregabalin
act on alpha 2 - delta subunit of calcium channel when this site is bound by natural ligands (leucine and isoleucine?) calcium channel complex transported to the cell surface if a gabapentinoids bind this site, the calcium channel is retained within the cell and broken down decreases the number of calcium channels at the cell surface
39
pregabalin secondary effect
increases glutamate decarboxylase (GAD) levels therefore increases synthesis of GABA
40
uses of gabapentinoids
Gabapentin and pregabalin: adjunct medication for focal seizures, neuropathic pain pregabalin: monotherapy and licenced for anxiety treatment
41
gabapentinoid side effects
Sedation/dizziness Suicidal thoughts Abuse potential (when you put these two together very worrying) Seizures upon withdrawal -precipitate return of epilepsy or even seizures you didn’t have before -particular problem for this drug
42
ethosuximide mechanism
blocks T type calcium channels
43
use of Ethosuximide
first choice drug for absence seizures, rarely used for other types of epilepsy (can exacerbate them)
44
what may ethosuximide be preferred to valproate?
lacks the liver toxicity there is an increased risk of birth defects, however this is less than with valproate
45
how does valproate produce teratogenic side effects?
at least partly by acting as a folic acid antagonist
46
side effects of ethosuximide
increased risk of birth defects sedation nausea mood changes
47
use of levetiracetam
can be used to treat focal, myoclonic and tonic-clonic seizures
48
mechanism of levetiracetam
inhibits presynaptic calcium channels? binds to SV2A? reduces neurotransmitter release
49
side effects of levetiracetam
Psychiatric common: depression, agitation, aggression rarer: suicide ideation, psychosis Steven Johnson syndrome- rarer
50
Steven Johnsons syndrome
some sort of immune reaction against the medication or a virus the patient has More serious form: toxic epidermal necrolysis
51
potential mechanism of topiramate
potentiation of GABAA receptors block of AMPA and kainate receptors block of sodium channels block of calcium channels inhibition of carbonic anhydrase
52
when is topiramate used?
an adjunct treatment for focal seizures and tonic-clonic seizures sometimes used in the treatment of migraines, bipolar disorder and alcoholism.
53
topiramate side effects
sedating can cause cognitive problems and have psychiatric side effects known to be teratogenic
54
what percentage of people are antiepileptic drugs successful for?
70%
55
what is suggested when antiepileptic drugs do not work
ketogenic diet -classic diet: 90% calories from fat therefore need professional dietician about 50% of children on it see a decrease in the number of seizures, some become seizure free
56
epilepsy surgery
localise the area of tissue generating the seizure and remove it or destroy it benefits often outweigh issues that may arise from surgery
57
corpus callosotomy
used for intractable epilepsy sever white matter tract, preventing seizures spreading from one hemisphere to the other
58
side effects corpus callosotomy
cognitive impairments difficulty with language alien hand syndrome
59

Drugs And The Brain (9 decks)

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