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SUM '20 - Pharm II > Week 1 Antiepileptic 1 of 4 > Flashcards

Week 1 Antiepileptic 1 of 4 Flashcards

1
Q

collective term used to designate a group of chronic CNS disorders characterized by the onset of sudden disturbances of sensory, motor, autonomic, or psychic origin:

A

epilepsy

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2
Q

Epilepsy is generally transient with what exception?

A

status epilepticus

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3
Q

what % of people will report at least one seizure in their lifetime?

A

10%

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4
Q

What % of worldwide population meets the dx criteria for epilepsy?

A

1-2%

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5
Q

Classification of epileptic seizures Table 13-1:

1.) Partial Seizures (beginning locally):

A
  • Simple partial seizures (consciousness not impaired)
  • Complex partial seizures (consciousness impaired)
  • Partial seizures evolving into secondary generalized seizures
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6
Q

Classification of epileptic seizures Table 13-1:

2.) Generalized Seizures (non-convulsive & convulsive):

A
  • Absence seizures (petit mal)
  • Myoclonic seizures
  • Clonic Seizures
  • Tonic seizures
  • Tonic-clonic seizures

**and there are “unclassified seizures”

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7
Q

30% of pts with seizures have

A

an identifiable neurologic or systemic d/o

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8
Q

**Epilepsy Tx goal:

A

control seizures w/minimal medication related adverse effects

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9
Q

70% of pts w/epilepsy will be seizure free using

A

a single epileptic drug

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10
Q

30% of pts w/epilepsy may require

A
  • transitioning to another drug
  • combining w/primary drug
  • vagal nerve stimulator
  • neurosurgical resection
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11
Q

With drug failure, epileptic pts may use:

A
  • vagal nerve stimulator

- Neurosurgical resection

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12
Q

antiepileptic medications becoming more preferred by patients are

A

sustained released

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13
Q

GI absorption is

A

slow (over hours) and may be incomplete

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14
Q

Protein binding varies greatly.

Name least and greatest?

A
  • Gabapentin 0%

- Phenytoin >= 90%

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15
Q

What may necessitate dose adjustments?

A

hepatic and renal disease

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16
Q

Name antiepileptic medications that rely on RENAL excretion:

A
  • Gabapentin*
  • Levetiracetam*
  • Pregabalin*
  • Vigabatrin
  • Zonisamide

*remaining drugs should be dosed according to pts liver dysfunction

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17
Q

Drugs with clearance/elimination half time ranges from HOURS:

A
  • Carbamazepine
  • Gabapentin
  • Primidone
  • Valproate
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18
Q

Drugs with clearance/elimination half time ranges from DAYS:

A
  • Lamotrigine
  • Phenytoin
  • Phenobarbital
  • Zonisamide
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19
Q

antiepileptic drugs all have the ability to do what to drug metabolism?

A

induce or inhibit

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20
Q

All antiepileptic drugs may be associated with interactions (resulting interactions of plasma drug concentrations) EXCEPT:

A
  • Gabapentin
  • Levetiracetam
  • Vigabatrin

“GLV” “gotta love Vigabatrin” (so not to mix up with valproate if he tried to trick!)

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21
Q

Highly bound protein drugs:

A
  • Carbamazepine
  • Phenytoin
  • Valproate

VCP - “very competitive Proteins”

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22
Q

What is significant about antiepileptic and protein binding drug interactions?

A

medications that compete for pr binding sites of highly bound antiepileptic drugs can displace them.
- increasing plasma levels of pharmacologically active antiepileptic drugs

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23
Q

Name some commonly used highly pr bound medications used:

A
  • Salicylates
  • Thyroxine
  • Phenylbutazone
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24
Q

why is Phenylbutazone (NSAID) no longer used in the US?

A
  • highly pr bound

- bone marrow suppression and dangerously low WBC

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25
Q

The principle binding site for antiepileptic drugs is?

A

Albumin

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26
Q

Hypoalbuminemia my be seen in what kinds of patients?

A
  • renal or hepatic disease
  • malnutrition
  • book says pregnancy as well*
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27
Q

Hypoalbuminemia in a pt taking antiepileptics may result in:

A
  • increased plasma concentrations of unbound antiepileptic drug
  • resulting in TOXICITY despite therapeutic plasma concentrations
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28
Q

hypoalbuminemia in pregnancy is due to

A

progressive increase in central volume
(Increased plasma volumes

  • this is more dilutional
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29
Q

dosing for antiepileptic medications should be

A

gradual dose titration

-except in an emergency

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30
Q

Dosing for antiepileptics is guided by

A

clinical response over time

31
Q

Noncompliance is high in

A

elderly and adolescents

32
Q

failure to achieve sufficient high plasma concentrations is

A

medication ineffectiveness

33
Q

Dosing at 1/2 the drug’s elimination half time ensures what?

$$ Exam Q$$

A

that a single dose missed will not result in sub-therapeutic plasma concentrations (pt won’t have a seizure)

34
Q

to ensure that a single missed dose of an antiepileptic medication will not result in a sub-therapeutic level (or induce a seizure), what is done?

A

dosing at 1/2 the drug’s elimination half-time

$$

35
Q

Review Table 13-2: MOA, Targeted Seizure, Dosage

Carbamazepine
Gabapentin
Phenobarbital
Phenytoin
Topiramate
Valproate
A
  • Carbamazepine - Na-ch blockade; partial seizures; 10-40mg/kg/day 2-3x day
  • Gabapentin - Unknown MOA (?increases GABA release?); partial/generalized seizures; 10-60 mg/kg/day
  • Phenobarbital: Cl-ch; P&G seizures; 2-5mg/kg/day every day in two doses
  • Phenytoin: Na-ch blockade; Ca-ch; NMDA receptors; P&G; 3-7mg/kg/day in 3 doses
  • Topiramate: Na-ch blockade, enhanced GABA activity, Ca-ch blockade; P&G; 500-3000mg/day in 2-4 divided doses
  • Valproate: Na-ch blockade; Ca-ch; P&G; 500-3000mg/day in 2-4 divided doses
36
Q

which antiepileptic drug requires routine (lab) monitoring?

37
Q

Titration to _____ is recommended for guiding the ______ of antiepileptic drugs.

A
  • clinical efficacy

- dosages

38
Q

If a pt is not responding as expected what is done?

A

-plasma drug levels may help determine compliance and pharmacokinetic interactions

39
Q

for most patients, epileptic seizure activity has a

A

localized or focal origin

40
Q

The cause for high frequency and synchronous firing in a seizure focus:

A 
- is usually unknown 
Possible Explanations:
local biochemical changes
Ischemia
loss of cellular inhibitory systems
Infection
Head trauma
41
Q

Neurons in a chronic seizure focus exhibit

A

denervation hypersensitivity with regard to excitatory stimuli

42
Q

Normal Inhibitory mechanisms presumably restrain

A

the spread of seizure activity to neighboring normal cells

43
Q

Factors that may facilitate the spread of a seizure focus into areas of the normal brain:

A

-Blood glucose concentrations
-PaO2
-PaCO2
-pH
Endocrine fxn
-Stress
-Fatigue
-Electrolyte balance

44
Q

If the spread of a seizure focus is extensive enough what can occur?

A
  • the entire brain is activated

- tonic-clonic seizure with unconsciousness

45
Q

If the spread of seizure focus is localized the seizure produces

A

s/s characteristic to the area of anatomic focus

46
Q

Once a seizure is initiated it’s likely to be maintained by:

A

reentry of EXCITATORY impulses in a closed feedback pathway (that may not even include the original seizure focus)

47
Q

The brain is divided into:

A

two halves:

  • right hemisphere
  • left cerebral hemisphere
48
Q

the left side of the brain controls the

A

right side of the body

49
Q

the right side of the brain controls the

A

left side of the body

50
Q

$$ What part of the brain controls muscle movements, thinking, and JUDGMENT?

A

Frontal lobe

51
Q

$$ What part of the brain controls sense of Touch, response to Pain and Temperature, and understanding of language?

A

Parietal lobe

52
Q

$$ What part of the brain controls vision?

A

Occipital lobe

53
Q

$$ What part of the brain controls hearing and memory?

A

Temporal lobe

54
Q

$$ What part of the brain controls balance?

A

Cerebellum

55
Q

$$ What part of the brain controls breathing and regulates Heartbeat?

A

Brain Stem

56
Q

The frontal lobe controls:

A

muscle movements, thinking, and JUDGMENT

57
Q

Parietal lobe controls:

A

sense of touch, response to pain/temp and understanding of language

58
Q

the occipital lobe controls:

59
Q

the temporal lobe controls:

A

hearing and memory

60
Q

the cerebellum controls:

61
Q

the brain stem controls:

A

breathing and heartbeat regulation

-“life sustaining”

62
Q

MOA of antiepileptic drugs is not completely understood.

  • It may control seizures by:
  • This may be achieved by:
A

control by:

  • decreasing neuronal excitability or
  • enhancing inhibition of neurotransmission

Achieved by:

  • altering intrinsic membrane ion currents (na, k, Ca) conductance or
  • by affecting activity of inhibitory NT’s
63
Q

What ion currents are primarily affected by antiepileptic drugs?

A

voltage-gated sodium and

calcium channels

64
Q

Drugs that delay reactivation of Na-channels during high frequency neuronal firing produce;

A

an inhibitory effect on creation of AP’s until neuronal d/c is blocked

65
Q

Name some antiepileptic drugs that act on the Na-Channels:

A 
1-Carbamazepine
2-Lamotrigine
3-Phenytoin
4-Primidone
5-Valproate
66
Q

Name some antiepileptic drugs that act on BOTH Na and Ca channels:

A

1- Carbamazepine
2-Lamotrigine
3- Phenytoin
4-valproate

67
Q

Name some antiepileptic drugs that act selectively on ca channels

A
  1. Ethosuximide

2. phenobarbital

68
Q

Drugs that alter synaptic function act primarily by

A

enhancing GABA mediated neuronal inhibition

69
Q

$$ Phenobarbital (and other barbiturates) increase the:

A

Duration of GABA ion channel openings

70
Q

$$ Benzodiazepines increase

A

frequency of GABA mediated ion channel openings

71
Q

$$ What is the difference b/w Phenobarbital and benzodiazepines and their MOA on the GABA ion channels?

A

Phenobarbital - increases DURATION of channel opening

Benzo’s - increase the FREQUENCY of channel openings

72
Q

Tiagabine effectively enhances GABA-mediated neuronal inhibition after synaptic release of the NT by doing what?

A

Delaying the REUPTAKE of GABA from synaptic clefts

73
Q

what drug delays the reuptake of GABA from the synaptic clefts to effectively enhance GABA inhibition?

SUM '20 - Pharm II (30 decks)

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