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PT2T1 > AED - Epilepsy Meds Yoyoyo > Flashcards

AED - Epilepsy Meds Yoyoyo Flashcards

1
Q

What is the goal of Anti-epileptic drugs?

A

GOAL: max quality of life by minimizing seizures and adverse drug effects but may not be lifelong treatment

Decrease the frequency and/or severity of seizures

Treats the symptom of seizure but no the underlying epileptic condition

[currently, no anti-epileptogenic drugs available]

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2
Q

Factors to consider when selecting AED regimen?

Describe the difference between Narrow Spectrum and Broad Spectrum AEDs?

A

Seizure type!!!

Monotherapy vs polytherapy

Side Effects!!!

Patient Adherence

Narrow Spectrum - 1 Mechanism of Action for PArtial Seizures

Broad Spectrum - for all and have more than 1 mechanism of action

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3
Q

Name the Broad Spectrum drugs we learned about….Whats the way to remember them eh?

A

Valproate

Lamotrigine

Topiramate

Levetiracetam

Zonisamide

[Valery Likes To Lick Zeus}

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4
Q

Name the Narrow Spectrum Agents by old and new generation

A

Old - Carbamazepine, Phenytoin, Phenobarbital

CPP

New - Gabapentin, Oxcarbazepine, PRegabalin, Lacosamide

GLOP

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5
Q

What seizures are the Narrow Spectrum drugs (GLOP and CPP) used for?

A

Partial Onset that can be simple, complex, or tonic-clonic but with focal/partial onset

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6
Q

What is the Treatment for Absence seizures and briefly describe it’s mechanism of action?

A

Ethosuximide

Targets T type Caclcium channels

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7
Q

What is the like most severe way to KO generalized onset seizures?

A

Benzodiazepines or barbituates

Like hitting with a sledge hammer

very sedating

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8
Q

Describe the role of “weighted inhibition” or Inhibitory surround in the brain and what types of neurons are in competition for balance in the pathology of seizures.

A

Normally, Inhibitory (GABA/Glycine interneurons) outweigh excitatory NT/inputs - hence the term “Weighted Inhibition” and they perform surround inhibition to prevent synchronization of adjacent neurons so you dont get excitatory spread with signaling (excitatory signaling with Glutamate and Aspartate)

Seizure generation occurs when you lose GABA input and excitation is weighted more than inhibitory

  • get bursts of EPSPs and Na and Ca currents and burst firing in Paroxysmal Depolarization (generation of seizure)
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9
Q

Describe the cellular mechanisms for Partial and Secondary Generalized seizures and highlight the areas where we use drugs to intervene

A

Main Mechanism: Depolarizing Shift!!!

see burst of high electrical activity by a column of neurons that’s lost inhibitory inputs

Recurrent EPSP –> Ca spikes –> repetive spike

Rapid Neuronal Discharge at Seziure Foci OPENS NA CHANNEL!!

Therefore drug-targets are to either BLOCK NA CHANNELS or INCREASE GABA INHIBITIOIN

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10
Q

What are the Na Channel blockers used as narrow spectrum and how do they work?

A

Na Channel Blockers: Phenytoin, Carbamazepine, Oxcarbemazepine, ESL (Stedesa), Lacosamide

Prevent prolonged activation but dont block the initial opening of the channel so neurons retain their ability to generate APs at lower frequencies but not get rapid generation like with seizures

“Use-Dependent BLockade” = Work only AFTER channel has been opened under normal circumstances and prolons inactivation state and increased refractory period

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11
Q

How does Phenytoin work? What is it used for?

A

Phenytoin is a Na Channel blocker that is a first-line agent in treatment of partial seizures and should be considered/compared with Carbemazepine and Lamotrigine for risk/benefit

First line agent partial seizures

AND

GIVEN IV IN STATUS EPILEPTICUS

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12
Q

What are the “TO KNOW” Facts about Phenytoin?

Name some specific adverse events.

A

Phenytoin is 95% bound to plasma albumin, inactivated by metabolism in liver, is a P450 inducer (can induce its own metabolism)

SATURATION KINETICS (linear at low doses zero order at higher doses) so small increase in dose can cause large, unpredictable increase in plasma concentration

Adverse Effects:

  • Cerebellar effects= Ataxia, Nystagmus, Incoordination
  • Cerebral effects = Confusion
  • Ugly Effects = Hirsuitism and Facial coarsening and systemic skin rash

The worst - 15-50% get GINGIVAL HYPERPLASIA!

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13
Q

What kind of drug is Carbemazepine? How does it work? When is it used?

A

Carbemazepine is actually a tricyclic antidepressant that here is a Na-Channel blocker used as a first line agent in Partial Seizures (especially good when effects of Phenytoin are too great)

*Occasionally used in Tonic-Clonic *

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14
Q

What are the TO KNOW facts about Carbemazepine metabolism and side effects?

A

Carbemazepine is inactivated by metabolism in liver and its active metabolite, 10-11 Epoxy Metabolite, may contribute to neurotoxicity

It induces its own metabolism and increases rate of metab during first 3-6 weeks so neets to be titrated correctly, large doses may be necessary

_Side Effects: _

Sedation, Drowsiness

HA

Dizziness

Blurred Vision

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15
Q

What is Oxcarbazepine? How does it work? What is it used for?

A

Oxcarbazepine is a newer drug closely related to Carbamazapine but with a lower side effect profile and less induction of P450 enzymes in liver metabolism

Used in kids >4 yo

Used as _first-line monotherapy or in add-on therapy for partial seizures _

Slows Na channel recover - NA channel blocker

Also may augment K+ and Ca+ channels to help hyperpolarize cells

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16
Q

What are the TO KNOW facts about Oxcarbazepine and its side effects?

A

some induction of P450 but much less

LOW side effect profile including simply sedation!

**Watch out for low sodium of on concomitant Diuretics *

ORAL CONTRACEPTIVE INTERACTION

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17
Q

What is Elsicarbazepine Acetate (ELS/Stedesa)? How does it work? what is it used for?

A

similar to Carbamazepine/oxcarb by blocking fast-acting GV Na channel but has greater affinity for inactive state (vs resting state) so _more selective for rapidly firing neurons!!!! _

ELS is a pro-drug and so metabolized into active compound at active site so relatively little side effects

Used mostly now as add=on therapy for Partial Seizures

No auto-induction of metabolism

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18
Q

What are the TO KNOW facts for ESL/Stedesa and Adverse effects?

A

Decreases ORAL CONTRACEPTIVE AVAILABILITY

Favorable drug-drug interaction profile, low protein binding and minimal effect on hepatic cytochrome P450 enzyme

Well-tolerated and most common effects are **Dizziness, Somnolence, HA, N/V **

Once Daily Dosing

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19
Q

What is LAcosamide? How does it work/what is it used for?

Side effect?

A

**Add-on therapy for poorly controlled partial seizures **

Mechanism is unclear but appears to change shape of Na-Channel to slow rate of synaptic transmission

Well-tolerated - dizziness main side effect

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20
Q

What are the Benzodiazepines? What are they used for? How do they work?

A

_Benzodiazepines - Diazepam and Lorazepam _

Enhance effectiveness of GABA-mediated inhibtion and icnrease frequency of Cl channel opening when GABA bound to receptor

LAST LINE of choice bc prominent adverse effects and can develop **tolerance **

Now used only to ablate seizures acutely and _IV infusion for treatment of Status Epilepticus _

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21
Q

What are the TO KNOW facts and side effects about Benzodiazepines?

A

NOT first line choice - last line because prominent side effects of Sedation, Dizziness, Ataxia, Drowsiness

TOLERANCE - can lose effectiveness in as short as 6 months

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22
Q

What are the Barbituates used in Seizures? How do they work and how are they used?

What are the side effects?

A

Barbituates = Phenobarbital

GABA-mimetic and GABA-potentiating - can open Cl channel and interact with GABA-A at binding site separate from benzo site

Used in Partial Seizures and Tonic clonic as an alternative drug and used less clinically bc of heavy side effects:

- HEAVILY sedating

- Cognitive Defects

Tolerance and Withdrawal

23
Q

What are Gabapentin and PRegabalin? How do they work? How are they used?

A

Gabapentin (Neurontin) and Pregabalin (Lyrica) are GABA-like compounds that do NOT act at that receptor –> Instead, they acts on Alpha2-Delta1 subunit on VG Ca2+ channels on Excitatory neurons to reduce Ca current and decrease neuron firing and excitatory transmission

Used as add-on therapy for PArtial Seizures and Tonic Clonic seizures

24
Q

What are the TO KNOW about Gabapentin/Pregabalin?

A

Both are excreted unchanges into the urine and so do not interfere with the metabolism of other drugs!

Approved for children - BERRY FLAVORED LIQUID!

Well-tolerated with limited side effects including *Somnolence, Dizziness, Ataxia *

*Some behavior and learning difficulties reported in kids but less sedating than classic AEDs *

25
Q

What’s happening in the phases of Tonic Clonic seizures?

A

Tonic Phase - seizure with long train of neuronal firing from acute sudden loss of GABA input

Clonic Phase - Gaba back in alternating fashion and oscilation of currents

Post-Ictal GABA re-maintains inhibitory control

26
Q

What drugs are used as Broad Spectrum AEDs? just List them!

A

Valery Likes To Lick Zeus

Valproate

Lamotrigine

Topiramate

Levetiracetam

Zonisamide

27
Q

What is Valproate? Mechanism of Action and uses?

A

Valproate (Valproic Acid aka Depakene) has 3 mechanisms:

1) Inhibits Low-Threshold T-Type Ca Channels

2) Slows Rate of Na channel Recovery

3) Increases Availability of GABA at synapse

Has many uses:

First line Therapy for Generalized Seizures but also used in Partial and Absent Seizures

28
Q

What are the notable drug interactions for Valproate? aka What other AEDs would you NOT use Valproate with?

A

Valproate and Carbamazepine induce eachothers metabolism so dont used togheter

Valproate inhibits Phenobarbitol metabolism - so dont use together

Valproate displaces Phenytoin from binding proteins –> increases its concentration in plasma and increases toxicity

Dont use with old CPP PArtial Seizure Narrow Spectrum meds!

29
Q

What are the adverse effects of Valproate?

A

**Problematic Sedation **

Tremor, Hair Loss, WEight gain

Elevated liver enzymes

GI disturbances

TERATOGENICITY - Autism, Sensory deprivation, Spina bifida

30
Q

What is Lamotrigine? How does it work? What is it used for?

A

Lamotrigine (Lamictal) is a broad spectrum drug used as an add-on or monotherapy in **partial and Secondarily Generalized Tonic-Clonic seizures (not primary) **

MOA:

1) Slows rate of recovery of VG Na channels
2) Inhibits Glutamate Release
3) Potential inhibition of Ca channels

31
Q

What are the side effects of Lamotrigine? How is it metabolized?

A

Lamotrigine is well tolerated and less sedating than other AEDs but can cause severe dermatitis in 1-2% pediatric patients (esp if given too quickly so start slow)

Metabolized by Glucuronidation in the liver

32
Q

What is Zonisamide? How does it work and how is it used?

A

Zonisamide is a broad spectrum anti-convulsant efficacious as adjunctive therapy for all seizure types (including absence) but only FDA approved for Partial onset

_MOA: _

1) Blockade of Na channels
2) Reduction in VG T-type Ca Channels (like Ethosuximide)
3) REduction of glutamate induced synaptic transmission

33
Q

What is interesting about Zonisamide dosing and what are the side effects of zonisamide?

A

Very Long Half Life (1-3 days) so 1x/day dosing

Has Sulphonamide Groups - NOT USED IN PPL WITH ALLERGY TO SULFA DRUGS

Side Effects: Causes **Kidney stones and Anhydrosis **

34
Q

What are the newer agents that act to inhibit Glutamate Transmission?

A

Act on AMPA/NMDA receptors

  • Topiramate - highly pleiotropic
  • Felbmate

Reduce Glutamate Synaptic Transmission

  • **Levetiracetam **
35
Q

What is Topiramate? Mechanism of Action? Uses?

A

Topiramate is a broad spectrum agent used to treat Partial, Generalized Tonic-Clonic, Some Myoclonic seizures - NOT for Absence

MOA:

1) Glutamate receptor antagonism - AMPA rec (maybe Kainate)
2) GABA potentiation
3) Na and Ca Channel Blockade
4) Carbonic Anhydrase Inhibitor

36
Q

What are advantages of Topiramate? What else is it good for?

A

topiramate has minimal interactions with other drugs (excpet Oral Contraceptives)

Approved as a Monotherapy AND approved for kids 2yo and up

Can cause weight loss (although bad for kdis)

USED AND APPROVED FOR MIGRAINE PREVENTION

37
Q

What are the Side Effects and Bad things about Topiramate?

A

_Side effects: _

Kidney Stones

Cognitive/Language difficulties

Tingling Pins/Needles

decrease OC therapy

38
Q

What is Felbamate? How does it work and what is it used for?

A

Extremely potent antiepileptic with inhibition of NMDA and AMPA subtypes of Glutamate receptors

***restricted for use ONLY in patients with Refractory Epilepsy **

39
Q

What’s So bad about Felbamate that it’s only used for refractory epilepsy?

A

While it lacks sedative effects…..it does cause:

**Adverse Behavioral Effects **

Fatal Aplastic Anemia and LIver Failure!!!!!

40
Q

What is Levetiracetam? How does it work? What is it used for?

A

Levetiracetam (Keppra) is a broad spectrum AED with Novel mechanism of action where it **enhances Synaptic Vesicles (SV2A) release of GABA **

MAY PREVENT EPILPTOGENESIS (all others only treat symptoms)

Used for Partial and Generalized Seizures

41
Q

What are the Advantages of Levetiracetam that make it so ideal?

What are the side effects?

A

Levetiracetam (Keppra) is *EFFECTIVE AT INITIAL DOSE so no need to titrate (great for pts with frequent seizures)

Dose-Escalation can be fairly rapid

NO KNOWN INTERACTIONS WITH AEDs

Side Effects: well-tolerated

s**ome Mood irritability/psychosis seen **

42
Q

What are the different types of Generalized seizures and what do you see with them?

A

Absence - Petit Mal with staring, blinking, lip-smacking/hand movements

Tonic-Clonic - Gran Mal

Myoclonic - brief Jerks

Atonic - Drop attack

43
Q

What are the T-Type Ca channels involved in absence seizures? What’s happening where in the brain during an Absent Seizure?

A

T-Type channel is primary target in Absent Seizure Treatment bc:

Normally, Thalamus relay setup activated during sleep and T-Type burst firing occurs to maintain sleep state and slow sleep waves

BUT when it is active in awake state then awake but EEG looks like characteristic of sleep state

T-Type Channels fire while awake and causes you to be absent!

44
Q

What are the drugs that act on T-Type Calcium Channels?

A

Drugs reduce activation of T-Type channels in thalamus = Anti-Absence

Ethosuximide

Valproate

Zonisamide

45
Q

What is Ethosuximide? How does it work? when is it used?

A

First-line therapy for Absent Seizures - very effective for that!

acts specifically on T-Type Channels in thalamus

46
Q

How does Ethosuximide travel in body? Side Effects?

A

zero to low plasma protein binding

LEss sedating than other drugs and low incidence of adverse effects!

47
Q

What are the enzyme inducing AEDs for hepatic enzyme induction?

A

Carbamazepine

Phenytoin

Phenobarbital

Oxcarbazepine

Topiramate

48
Q

Drugs used for Epilepsy AND for Neuropathic Pain? easy way to rememebr

A

Gabapentin/Pregabalin

Carbamazepine/Oxcarbazepine

Lamotrogine

Levetiracetam

Valproate

[Valery Got Pain Like Lenny Cravitz Ought-to}

49
Q

AEDs used for Bipolar Disorder?

A

Lamotrogine

Carbamazepine

Valproate

50
Q

AED Drugs used for Migraine?

A

Valproate

Topiramate

Gabapentin

51
Q

2 DRUGS GIVEN FOR STATUS EPILEPTICUS:

A

IV Phenytoin

IV Benzodiazepines

52
Q

Drugs with ORal Contraceptive Interactions?

A

Oxcarbazepine

ELS (acetazolamide)

Topiramate

T.O.E.

53
Q

What is the ONLY AED with eleptogenic potential? What is it’s unique mechanism of action?

A

Leveitracetam

Helps with veiscle docking of SV2A on GABA neurons to increase releaes of GABA

54
Q

What are the drugs that act on T-Type Ca Channels?

A

Ethosuximide

Valproic Acid

Zonisamide

PT2T1 (38 decks)

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