Fitzy Pharm Seizures And Epilepsy Flashcards

1
Q

What drugs will treat absence seizures?

A

Ethosuxamide and valproic acid

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2
Q

Myoclonic clinic seizures

A

Benzodiazepines, clonazepam

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3
Q

Tonic clinic seizures

A

Narrow spectrum drugs: phenytoin and phenobarbital

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4
Q

Simple and complex seizures

A

Gabapentin, pregabalin, oxcarbamazepine, lacosamide, tiagabin, visabatrin, exogamous

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5
Q

Tonic clonic partial onset seizures

A

Narrow spectrum drugs: carbamazepine, phenytoin, phenobarbital
*cbz is only with partial onset seizures

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6
Q

What are the broad spectrum AED’s?

A

The treat generalized or partial onset seizures: Very low table lacks zest

  • valproic acid
  • lamotrigine
  • topic image
  • levetiracetam,
  • zonisamide.
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7
Q

Which AED’s will prolong the fast inactivation state of Na channels?

A

Lamotrigine and oxcarbamazepine

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8
Q

Which AED enhances slow inactivation?

A

Lacosamide

*important because of different mechanism

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9
Q

Which AED is slightly lipophilic?

A

Lamotrigine

* it just kinda sneaks to that internal binding site so it’s not as use-dependent as the other ones

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10
Q

Why do Na channel blockers act preferentially at the sites of epilepsy

A

They have the highest frequency of being open so the drug can bind to it!

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11
Q

Which drug is more effective in blocking high frequency firing? Phenytoin or carbamazepine?

A

Carbamazepine

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12
Q

What makes lamotrigine different from phenytoin or carbamazepine?

A

It also acts on other things like n and p type voltage gated calcium channels in the cortical neurons and neocortical potassium currents

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13
Q

What does lacosamide stabilize?

A

The slow inactivated state… The one where everything is totally shut
-works best when the stimulus was prolonged for tens of seconds

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14
Q

What kind of channels mediate absence seizures?

A

T-type calcium channels

*the 3 Hz spike is the dead giveaway

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15
Q

So, what drugs can be used to treat absence seizures?

A

-antagonists of t-type calcium channels
-narrow spectrum : ETHOSUXAMIDE
It sux because it’s only used for absence seizures and only limits excitation ….. And it’s non-sedating which sux as well

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16
Q

Valproate

A
  • 1st line for generalized onset seizures

- has intolerable adverse effects—- weight gain, hair loss, lethargy

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17
Q

Lamotrigine

A

Gets the Na v channels like cbz and phenytoin

-BUT it also acts at n and p type calcium channels in cortical neurons and neocortical potassium currents

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18
Q

Zonisamide

A
  • sulfanilamide derivative

- blocks Nav channels and t-type calcium channels

19
Q

What drugs will enhance the post-synaptic GABAergic neuronal transmission?

A
  • phenobarbital and related barbiturates
  • primidone…. Active metabolite is phenobarbital
  • benzodiazepines (diazepam and lorazepam and friends)
20
Q

What are phenobarbital’s complications?

A

Can cause significant sedation

  • lethal respiratory depression
  • has abuse and addiction potential
  • these suck, so benzodiazepines were made*
21
Q

How do benzodiazepines work?

A

Bind to distinct site… Aldosterone potentiation… GABA binds… There ya go….channel opens with greater FREQUENCY

22
Q

How does phenobarbital work?

A

Binds to distinct site on GABA receptor,

-increases the duration of the Cl- channel opening

23
Q

Why is the lethality of phenobarbital so much higher than benzodiazepine?

A

High douses of barbiturates are GABA independent

24
Q

What drugs are used to manage status epilepticus?

A

Diazepam or lorazepam with Fosphenytoin if needed

25
What is clonazepam very effective at treating?
The emergency treatment of status epilepticus
26
What actions does topirimate have?
Glutamate receptor antagonist, no depolarization there | GABA receptor agonist... Let's in Cl- and then hyperpolarization happens
27
MOA of Gabapentine
Binds to voltage dependent Calcium channels | -NO significant drug interactions
28
MOA of leviteracetam
Binds to synaptic vehicle ptn SV2A- blunts glutamate release | -well tolerated.... NO CYP INTERACTION WHICH IS NICE
29
Pregabalin MOA
Multiple.... 100% renal clearance so make sure their fucking kidneys work
30
Ezogabine MOA
Opens voltage gated potassium channels and causes urinary retention
31
What are the 4 pharmacokinetic properties?
ADME - absorption - distribution - metabolism - elimination
32
Which drug has zero order kinetics?
Phenytoin - so doubling dose does not necessarily double serum level - dose adjustment is very difficult
33
What are some complications with phenytoin?
Induce of hepatic cyp450n enzymes - gingival hyperplasia - hirsuitism - hypocalcemia - osteoporosis
34
What are some complications with carbamazepine?
Inducer of hepatic cyp450 enzymes - aplastic anemia - leukopenia, neutropenia, thrombocytopenia - hypocalcemia, osteoporosis
35
Why is the induction of CYP450 such a big deal?
When carbamazepine induces it, - creates the inactive form of vitamin D - osteopenia/osteoporosis - less vit D, less Ca2+ absorption in intestin - trigger compensatory PTH -mediated responses that demineralization bone
36
how do AED's mess with oral contraceptives?
Starting cbz can increase the clearance of oral contraceptives metabolized by CYP isoenzymes.... - 4 fold rise in OCP failure rate - risk for unplanned pregnancy
37
How do AED's mess with oral anticoagulants?
Increase the clearance of warfarin metabolized by,.... You guessed it.. CYP isoenzymes -too rapid coagulation.... High risk for AV thrombosis
38
What analogue of cbz has fewer side effects because of lack of formation of an active metabolite?
Oxcarbazepine
39
Which two AED's have 100% renal clearance?
Gabapentine Pregabalin -renal insufficiency requires dose adjustment
40
What are the adverse effects of OXCBZ
Hyponatremia and rash... More common in elderly
41
Adverse effects of tiagabine
Stupor
42
Adverse effects of topirimate
Nephrolithiasis, open angle glaucoma, hypohidrosis, in children
43
Adverse effects of zonisamide
Rash, renal calculus, hypohidrosis (mainly children)