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Pharm Exam 3 > 34/35: Anticonvulsant Drugs > Flashcards

34/35: Anticonvulsant Drugs Flashcards

1
Q

define seizure

A

sudden, transient episode of brain dysfunction and altered behavior due to abnormally excessive, synchronous, and rhythmic firing of certain populations of hyper-excitable neurons in the brain

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2
Q

activation of motor neurons leading to involuntary contractions of skeletal muscle =

A

convulsions

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3
Q

chronic neurological disorder characterized by recurrent seizures =

A

epilepsy

primary/idiopathic - unknown origin

secondary - identifiable cause

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4
Q

describe a simple partial seizure

A
  • minimal spread of abnormal neuronal discharge
  • no loss of consciousness
  • limited motor or sensory manifestations
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5
Q

describe a complex partial seizure

A
  • starts in a small brain area but quickly spreads to other areas
  • altered consciousness with potential automatisms
  • strong emotional feelings, gradual recovery of consciousness within minutes
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6
Q

what are automatisms?

A

lip smacking, fumbling, swallowing, etc…

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7
Q

involve the entire brain with global EEG change and bilateral manifestations

A

generalized epileptic seizures

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8
Q

describe absence/ petit mal seizures

A
  • sudden onset and abrupt cessation
  • brief loss of consciousness
  • typically in children less than 15 yo
  • inducible by hyperventilation, stress or flash light
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9
Q

describe tonic-clonic/ grand mal seizures

A
  • tonic spasms and major convulsions of entire body bilaterally
  • loss of consciousness and profound CNS depression after seizure
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10
Q

what are the four phases of a tonic-clonic seizure?

A
  1. aura
  2. tonic (tense)
  3. clonic (convulsions)
  4. stuporous state and sleep
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11
Q

observe: child with sudden loss of postural tone resulting in falls or dropping of head and torso if in sitting position, may be wearing a helmet

A

atonic generalized seizure

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12
Q

recurrent myoclonic jerks of the body with sudden flexion or extension of the body and limbs

A

infantile spasms

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13
Q

what is status epilepticus?

A

continuous or very rapid recurrin seizures, usually of tonic-clonic type
- medical emergency requiring immediate therapy

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14
Q

mechanism generating epileptic seizures: 3 stages

A
  1. initiation (focal epileptogenesis)
  2. synchronization of surrounding
  3. propagation (recruitment of normal neurons)
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15
Q

goal of antiepileptic medications

A

restore normal patterns of electrical activity

inhibit seizures, partially effective as prophylaxis but not a cure

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16
Q

alternative treatment options for epilepsy (not meds)

A
  • surgery (resection, particularly in temporal lobe)

- vagus nerve stimulation (for drug-resistant patients with partial seizures)

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17
Q

what medications would you use for partial seizures (complex or simple) with or without secondarily generalized seizures?

A

carbamazepine
phenytoin
valproate

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18
Q

what medications would you use for tonic-clonic seizures, tonic seizures, or atonic seizures?

A

carbamazepine
phenytoin
valporate

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19
Q

what medications would you use for absence seizures?

A

ethosuximide

valproate

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20
Q

what medications would you use for myoclonic seizures?

A

clonazepam

valproate

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21
Q

what medications would you use for status epilepticus?

A

diazepam
larazepam
phenytoin
fosphenytoin

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22
Q

3 major MOA for anticonvulsant medications

A
  1. decrease excitatory effects of glutamate and repetitive firing of neurons
  2. increase inhibitory effects of GABA
  3. alter neuronal activation by altering movement of ions across neuronal membrane
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23
Q

anti-seizure medications can bind to Na channels in the _______ and prevent conversion ______

A

inactive; resting state

  • this prolongs Na channel inactivation and make neuronal membrane less excitable
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24
Q

what reduces the pacemaker current that underlies the thalamic rhythm in spikes and waves seen in absence/ petit mal seizures?

A

reducing the calcium influx

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25
Q

general side effects of anticonvulsants

A
  • sedation
  • diplopia
  • nystagmus
  • ataxia
  • GI upset
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26
Q

other side effects to watch for in anticonvulsants…

A
  • abrupt withdrawal can cause seizures
  • decreased efficacy of oral contraceptives
  • teratogenic
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27
Q

what drug is considered safest for pregnancy?

A

phenobarbital

28
Q

what is the elimination of phenytoin look like?

A

dose-dependent (zero order) elimination that is different for different patients

system can become saturated and transition ot a non-linear relationship

metabolized in liver, excreted in urine

29
Q

MOA phenytoin

A
  1. blocks and prolongs the inactivated state of voltage-gated Na channels
  2. enhances the release of GABA
  3. prevents seizure propagation
30
Q

clinical uses for phenytoin

A
  • grand mal
  • partial seizures
  • status epilepticus
31
Q

gingival hyperplasia is a negative side effect of what drug?

A

phenytoin

32
Q

what is fetal hyantoin syndrome?

A

teratogenic
cleft lip and palate

side effec tof phenytoin

33
Q

MOA carbamazepine

A

*inhibition of voltage gated Na channels

also blocks high frequency firing of neurons and decreases synaptic release of glutamate

34
Q

how is oxacarbazepine different than carbamazepine?

A

shorter half-life, but active metabolite has longer duration and fewer drug interactions

35
Q

drug of choice for trigeminal neuralgia

A

carbamazepine

36
Q

clinical uses for carbamazepine

A
  • grand mal
  • partial seizures
  • trigeminal neuralgia
37
Q

SIADH = ?

A

syndrome of inappropriate ADH secretion

side effect of carbamazepine that causes increased fluid retention and hyponatremia

38
Q

what drug interactions do you need to watch for with carbaamazepine?

A

phenytoin
valproate
phenobarbital

39
Q

MOA phenobarbital

A

enhances phasic GABAa receptor responses by increasing duration of Cl- channel opening

40
Q

drug of choice for seizures in infants

A

phenobarbital

41
Q

clinical use for phenobarbital

A

status epilepticus (and others)

42
Q

metabolized by the liver to phenobarbital

A

primidone

43
Q

drug of choice petit mal/ absence seizures

A

ethosuximide and valproic acid

44
Q

MOA ethosuximide

A

blocks presynaptic t-type Ca2+ channels to stop high-freqeuncy firing of neurons

45
Q

least sedating anticonvulsant

A

valproic acid

also chemically unrelated to other anticonvulsants

46
Q

MOA valproic acid

A
  • inhibition of presynaptic t-type Ca2+ channels to block neuronal firing
  • inhibition of GABA transaminase
47
Q

special adverse effects for valproic acid

A

hepatotoxic syndrome and spina bifida if preggers (teratogenic)

do not use less than 5 yo

48
Q

preferred initial agent for status epilepticus

A

diazepam

49
Q

how is lorazepam different than diazepam?

A

longer duration of action

50
Q

MOA diazepam

A
  • potentiates GABAa responses by increasing frequency of channel opening
51
Q

use limitations for diazepam

A

sedative effects and tolerance

52
Q

MOA gabapentin and pregabalin

A

GABA analogs that block presynaptic voltage-gated Ca2+ channels to decrease excitatory transmission

53
Q

clinical uses gabapentin

A
  • grand mal
  • partial seizures
  • neuropathic pain
54
Q

MOA lamotrigine

A

blocks presynaptic voltage-gated Na and Ca channels

55
Q

clinical uses for lamotrigine

A
  • partial and generalized seizures

- petit and grand mal

56
Q

adverse effect of lamotrigine

A

**stevens-johnson syndrome (rash)

especially if used with valproate

57
Q

MOA felbamate

A

blcok Na channels and glutamate receptors

58
Q

adverse effects felbamate

A

aplastic anemia, hepatic failure

59
Q

specifically designed as an inhibitor of GABA uptake

A

tiagabine

60
Q

MOA acetazolamide

A

carbonic anhydrase inhibitor

effect thought to be related to mild CNS acidosis

61
Q

spasticity v. spasm

both are the result of hyperexcitabiliyt of the neurons or muscle cells

A

primarily an exaggerated muscle stretch reflex syndrome that occurs following injury to the CNS

v.

an increase in muscle tension seen after certain musculoskeletal injuries and inflammation (injury is local and not in the CNS)

62
Q

goal of pharmacotherapy for muscle spasms and spasticity

A

normalize muscle excitability without causing a profound decrease in muscle function

63
Q

centrally acting muscle relaxants (2)

A

diazepam

baclofen

64
Q

how does diazepam act as a muscle relaxant?

A

works by increasing the central inhibitory actions of GABA on alpha motor neurons in the spinal cord

65
Q

treat spasms with _____; treat spasticity with _______

A

diazepam; baclofen

66
Q

MOA baclofen

A

GABAb receptor agonist

as effective as diazepam, but causes less sedation

Pharm Exam 3 (11 decks)

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