Anti-Epileptic Drugs (Aeds)

Front 1

What is a seizure?

Back 1

An abnormal neuronal firing which manifests clincally in changes in motor control, sensory, behavorial and or autonomic function

Front 2

Epilepsy is..

Back 2

recurrent spontaneous seizures from aberrant brain electrical activity

Represents the imbalance of exictatory and inhibitory currents in the brain

Front 3

Seizures are classified by:

Back 3

Partial onset seizures (Originate in the celebral cortex)
-Simple partial
-Complex partial
-Secondary Generalized Tonic-clonic (can spread into 2 hemispheres)

Generalized
-Absence
-Myoclonic
-Primary Genrealized Tonic Clonic seizures

Front 4

Pharmologic targets of AEDs include these 4:

Back 4

1)Voltage gated sodium channel
2) T-type & N type Ca channel
3) GABA system
4)Glutamate receptors

Front 5

You want to decrease glutamate, so you would:

Back 5

-block voltage gated Na+ channels- prevents a.p
- block activity of fusion with vessicles and pre sypnatic vessicles and membrane-inhibiit glumate from going to post sypnase
-block AMPA receptors and NMDA receptors

Front 6

To enhance GABA,you would:

Back 6

- block transporters

Front 7

Na+ channel antagonists use this idea of use dependence. What is this?

Back 7

They only block Na+ channels involved in seizure activities because of high frequency rather than other Na+ voltage gated channels

Front 8

What is the mechanism of action for Na+ blockers?

Back 8

Drugs bind to inactivated state and delays Na+ to go back to resting state

Front 9

What are 3 conformations that proteins exist in for voltage gated sodium channels?

Back 9

1)resting- channels closed, no NA+ passing
2)activated- sense a little change in voltage, activates it- allows passage of Na+(conformational change in protein)
3-inactivated- channels close- prevents passage of Na+

Front 10

Phenytoin(Dilantin) is a:
a) Na + channel antagonist
b) Ca+ channel antagonist
c) glutamate inhibitor
d) GABA like drug

Back 10

a) Na + channel antagonist

Front 11

Phenytoin is effective in:
a) Partial seizures
b) Tonic clonic seizures
c) Absence seizures
d) both a &b
e) All of the above

Back 11

d) both a &b-partial and tonic clonic seizures, NOT ABSENT!

Front 12

Phenytoin has non linear saturable kinetics..this means that you should be very careful in..

Back 12

increasing the dose- Phenytoin gets metabolized- enyzmes gets saturated, excess can not be cleared by CYP 450, any small increase in Phenytoin will lead to disportionally high PPB

Front 13

Some side effects of Phenytoin are that it caues:
a) Gingivial hyperplasia
b) hiristuium
c) Lymphadenopathy
d) Rash
e) All of the above

Back 13

e) All of the above

Front 14

The Steven Johnoson's Syndrome (TEN) is a cutaneous hypersentivity reaction which is cell mediated by these kind of cells.

Back 14

T-cells

Front 15

Phenytoin (Dilantan) is not soluble so you would...

Back 15

In preparing IVs, use propylene glycol, add NaOh- PH-12- causes irritation

Front 16

The gene that is involved in the SJS syndrome is HLAB *1502 whihc is the allele for leukocyte antigens. Which type of race is it prevalent in?

Back 16

Asian- You would want to screen for this allele before giving either Phenytoin or carbamezapine

Front 17

Fosphenytoin is the ___ of phenytoin and can be used IV or IM, It may be contraindicated with oral contraceptives.

Back 17

Prodrug.

Front 18

Carbamezapine is a ___channel antagonist. It is effective in treatment of partial and tonic clonic seizures,trigemental neuralagia, and bipolar disorders.

Back 18

Na+

Front 19

Carbemazapine also has ___ kinetics and has autoinduction and is metabolized by CYP3a4 to active metabolite.

Back 19

linear.

Front 20

Side effects of carbemazapine include:

Back 20

aplastic anemia, agranulocytics, stiumlates ADH release(be cautious in elderly, HTN, and Heart failure)

Front 21

Oxycarbapezine (Trileptal) has ___ CYP induction compared to carbamepzine, doesn't have side effcts of aplastic anemia or SJS syndrome.

Back 21

decreased

Front 22

Lamotrigine (Lamictal) is not only a Na+channel antagonist but also inhibits..

Back 22

neuronal glutamate release

Front 23

Lamotrogine is used for:
a) adjunctive treatment of partial seizures
b)adjunctive treatment of generalized
c)Bipolar Disorder
d) Lennox Gastaut seizures (pediatric)
e) All of the above

Back 23

e) All of the above

Front 24

Lamotrogine has hypersensitivity reactions, the same as SJS syndrome. True or false?

Back 24

FALSE. rash is dependant on dose given

Front 25

Low voltage (T-type) Calcium channels are linked to these type of seizures

Back 25

absence (petit mal)

Front 26

High voltage(N) Ca channels produce a high extent of voltage changes across a membrane, therefore leading to

Back 26

more passing of Ca+ ions

Front 27

Absence seizures are present in this part of the brian and it can lead to blank stares, and loss of consciousness.

Back 27

thalamus

Front 28

Ethosuximide(Zarontin) is a ___ antagonist

Back 28

T-type channel Ca+, only good for absence seizures!

Front 29

Zonisamide(Zonegran) is a T-type Ca+ channel antagonist, it also blocks Na+ channels. It is used adjunctive partial seizures as well as ___seizures. An unusual side effect is...

Back 29

partial seizures, metabolic acidosis

Front 30

What is the MOA of Gabapentin (Neurontin)?

Back 30

binds specific alpha 2, gamma subunit voltage gated calcium channel which reduces Ca influx mediated neurotransmitter release( glu, NE,DA,substance P)

Front 31

Gabapentin is an adjunctive treatment in partial seizures but is also an

Back 31

analegisc, antinoceptive for neuropathic pain, fibromyalgia, postherapic neuralgia

Front 32

How does the GABA system work?

Back 32

GABA comes from glutamate! In the glia cells, GABA is reuptaken by transporters GAT2 and GAT 3- gets metabolized by transamines which breaks down GABA. You want to block the transporter (which blocks the reuptake and block transaminase(enzyme inhibitor), and inhibit metabolism of GABA, which in turn enriches GABA content in neurons.

Front 33

GABA allosteric modulators are..

Back 33

benzodiazapenes

Front 34

GABA allosteric modulators/ agonists is

Back 34

Phenobarbital

Front 35

Tigabine(Gabatril) mechanism of action is that it

Back 35

inhibits GAT 1 transporter- which increases GABA and GABAa receptor activation

Front 36

The older AEDs are more effective and are:

Back 36

Phenobarbital, Valproic Acid, Phenytoin, and Carbamazepine

Front 37

Vigabatrin(Sabril) is an irreversible inhibitor of GABA-transaminase. What does this mean?

Back 37

binds to the enzyme's active site by covalently binding to it. The body needs to make new enzymes that is not covalently bound.

Front 38

One prevalent side effect with Vagabatrin is_____, however it is good for _________spasms.

Back 38

loss of vision, infantile

Front 39

Valproic acid is affected by CYP 450 because it is a fatty acid and is metabolized by mitochondrial B-oxidation.
True or false?

Back 39

FALSE- has nothing to do with CYP450

Front 40

One long term effect of Valproic acid is that it causes____.

Back 40

weight gain

Front 41

Valproic acid is the most _____ because it is a Na channel antagonist, T-type Ca channel antagonist, and it also enhances GABA transmission(upregulates gabba transaminase)

Back 41

broad spectrum

Front 42

Levetiracetam (Keppra) inhibits high volatge gated Ca channels, inhibits excitatory neurotransmitter release, and also does what..?

Back 42

reversal of of zinc induced inhibition of GABA

Front 43

Levtiracetam is well tolerated. True or False.

Back 43

True.

Front 44

Topiramate is an AMPA receptor antagonist and its unique side effect is..

Back 44

it promotes weight loss

Front 45

Which one of these is NOT purely an Na+ antagonist?
a)phenytoin
b)carbamezapin
c)zonisamide
d)Lamotrigine
e)a&c

Back 45

c)zonisamide

Front 46

Which one of these is purely a Ca+ channel antagonist?
a) Gabapentin
b) Ethosuximide
c)Zonisamide
d)Tigabine
e)a&c

Back 46

b) Ethosuximide

Front 47

Gabapentin and Pregrablin are___.

Back 47

N-type Ca+channel antagonists

Front 48

These two drugs affect both the GABA system and glutmate receptors.

Back 48

Phenobarbital & Felbamate

Front 49

Rufinamide(Banzel) and Lacosamide(Vimpat) is one of the newer voltage gated Na channel antagonists and is good for these type of patients

Back 49

pediatric

Front 50

Primidone (Mysoline) is one of the older drugs and can get metabolized into____. It also has a higher incidence of sedation and sexual dysfuntion compared to this drug, but still acts like this drug.

Back 50

Phenobarbital

Front 51

Valproate is an inducer and an inhibitor. True or false

Back 51

False! Just an inhibitor!

Front 52

Phenytoin, Phenobarbital, Primidone, Carbamezpine are all CYP 450 inhibitors. True or false

Back 52

False. Inducers!

Front 53

Felbamate, Oxcarbaezpine, and Topiramate are inducers and inhibitors. True or false.

Back 53

True! (Cyp3a4 inducers, and Cyp 2c19 inhibitors)